Antibiotics

Antibiotiki, 1982, 27(7), 535 - 9
{Acute toxic action of combinations of antibiotics with isoniazid}; Ziia AV et al.; Acute toxicity of isoniazid combinations with rifampicin or various streptomycin salts was studied on 1237 noninbred mice . The toxic effect of the combinations of the drugs in different weight ratios was estimated with the method of graphic analysis of Leve and Muischnek . The experiments showed that rifampicin and streptomycin had no effect on isoniazid ability to induce spasms . The combination of isoniazid with rifampicin had an additive action with an insignificant decrease in the toxic effect . 1 : 2 was the most optimal ratio of the drugs . When the mixture of isoniazid and streptomycin was used in the same syringe, the toxicity increased . However, injection of these drugs alone with an interval of 1-2 minutes had a more favourable additive effect when used in an optimal ratio of 1 : 1.6.

Antibiotiki, 1982, 27(7), 483 - 7
{Identification of the antibiotic formed by a Str . canulus 106/78 culture with antibiotic CC-1065}; Frolova VI et al.; An antibiotic with a melting point of at least 340 degrees C, {alpha}D + 100 degrees (c 1 per cent in dimethylformamide) was isolated from the mycelium of Str . canulus 106/78 . Calculated (%): C 60.63, H 4.69, N 13.6 . The UV spectrum of the antibiotic (in methanol solution) showed the terminal absorption, shoulder at 265 nm and maximum at 375 nm . In dimethylformamide solution the UV absorption maximum was observed at 370 nm with E1 1% cm 845 . The IR, FMR and 13C-NMR spectra of antibiotic 106 are analogous to the respective spectra of antibiotic CC-1065 which is indicative of their identity.

Acta Obstet Gynecol Scand, 1982, 61(3), 247 - 51
Antibiotic levels in plasma and peritoneal fluid after amoxycillin, ampicillin, and bacampicillin treatment for pelvic inflammatory disease; Onsrud M et al.; Fifteen patients with pelvic inflammatory disease had a thin polyethylene catheter inserted through the abdominal wall into the pouch of Douglas for sampling of peritoneal fluid . At hourly intervals peritoneal fluid and capillary blood were collected . Five patients each received a single oral dose of either 0.5 g of ampicillin or amoxycillin, or 0.8 g of bacampicillin (approximately equimolar doses) . This highest median peak plasma level was observed after bacampicillin . Bacampicillin also showed less variation in individual plasma concentration . The area below the plasma curve was similar for amoxycillin and bacampicillin, whereas that of ampicillin was significantly smaller (p less than 0.01) . The rate of penetration into peritoneal fluid was slower for amoxycillin than for bacampicillin, even though the area below the peritoneal fluid curve was similar for the two drugs . Therapeutic levels were maintained for 5--8 hours, longer after amoxycillin than after bacampicillin.

Methods Find Exp Clin Pharmacol, 1982, 4(5), 337 - 41
Effect of aminoglycoside antibiotics on the contractility of the uterus; Paradelis AG et al.; In the present study the inhibitory effect of five aminoglycoside antibiotics on the contractility of rat uterus was investigated . We found that all the antibiotics tested inhibited the contractility of the isolated rat uterus and only quantitative differences existed among them . The inhibitory potency of the aminoglycoside antibiotics appears to be as follows: sisomicin greater than gentamicin greater than tobramycin greater than dibekacin greater than amikacin . Calcium not only has the ability to restore the normal contractility of the uterus but also to exert protective action against the inhibitory effect of aminoglycoside antibiotics on the uterus contractility.

Rev Fr Mal Respir, 1982, 10(3), 195 - 203
{Pharmacokinetic basis for antibiotic therapy in broncho-pulmonary bacterial infections (author's transl)}; Grosset J et al.; Pharmacokinetics is the study of the absorption, distribution and elimination of a drug in the body . Applied to antibiotic therapy it gives information on the concentrations of antibiotic that reach the bacteria at a given time at their site of multiplication for a given dose and route of administration . The future of an antibiotic within a body is largely related to passive transfer . This can be compared to the dialysis of molecules across a semi-permeable membrane, the passage from one side to the other being a function of the concentration of molecules in the "upstream" side, the size of the molecules and their own particular transfer speed . The final result is affected by 1) the partition coefficient itself related to the degree of aqueous and lipid solubility of the molecules, 2) the degree of ionisation of the molecules, non-ionised molecules being the only ones to be transferred, 3) protein binding as only the unbound fraction is biologically active and capable of diffusing across the membranes, 4) by the interplay of the combined phenomena of resorption, distribution and elimination . Penicillins and macrolides are the antibiotics of choice in broncho-pulmonary infections . The tetracyclines and the sulfamethoxazole-trimethoprim combination come second . The combination of a beta-lactam, an aminoglycoside and/or metronidazole are reserved for the most severe infections . The lung is a particularly well vascularised organ, the pulmonary concentrations of the antibiotic may equal the serum levels . But the concentration in the bronchial secretions only reaches 55% of the serum levels for clindamycin, 25 to 30% for aminoglycosides, minocycline and bacampicillin, 20% for cephalosporins and doxycycline and less than 10% for ampicillin and erythromycin . Only oleandomycine, spiramycin and trimethoprim are present in concentrations equal to those in the serum.

Folia Microbiol (Praha), 1982, 27(3), 167 - 72
A new streptomycete and a new polyene antibiotic, acmycin; Chakrabarti S et al.; A new antifungal antibiotic named acmycin was isolated from a soil streptomycete . Detailed comparative taxonomic studies showed that the organism differed from three related species of streptomycetes . The organism was referred to as Streptomyces sp . AC2 . The isolated antibiotic appears to be of polyene nature.

Cancer Chemother Pharmacol, 1982, 8(2), 157 - 62
Antitumor activity of mitoxantrone against murine experimental tumors: comparative analysis against various antitumor antibiotics; Fujimoto S et al.; 1,4-Dihydroxy-5,8-bis(((2-{(2-hydroxyethyl) amino} ethyl)amino))-9,10-anthracenedione dihydrochloride (mitoxantrone) was tested for antitumor activity against experimental tumors in mice and the results were compared with those of seven antitumor antibiotics: adriamycin (ADM), daunomycin (DM), aclarubicin, mitomycin C (MNC), bleomycin, neocarzinostatin, and chromomycin A3 . The drugs were given IP or IV, in general on days 1, 5, and 9 following tumor inoculation . Mitoxantrone given IP at the optimal dose (1.6 mg/kg/day; as a free base) produced a statistically significant number of 60-day survivors (curative effect) in mice with IP implanted L1210 leukemia . The curative effect was not observed with any of the other antibiotics . In the case of IV implanted L1210 leukemia, there was an increase in lifespan (ILS) by more than 100% in the mice following IV treatment with mitoxantrone or DM . In IP implanted P388 leukemia, the curative effect was elicited by IP treatment with mitoxantrone or MMC . In IP implanted B16 melanoma, both the curative effect and a more than 100% ILS in mice that did die were produced by IP treatment with mitoxantrone or ADM . In SC implanted Lewis lung carcinoma, mitoxantrone and ADM administered IV also showed effective antitumor activities and produced a 60% and a 45% ILS, respectively . In conclusion, mitoxantrone and ADM had a wider spectrum of antitumor activity against mouse tumors, including two leukemias and two solid tumors, than did the other drugs; however, mitoxantrone elicited higher antitumor effects than ADM on mouse leukemias, especially on L1210 leukemias . Moreover, mitoxantrone possessed much higher therapeutic indices than ADM against IP implanted P388 (optimal dose/ILS40; greater than 128 versus 15.2) and L1210 (optimal dose/ILS25; 72.7 versus 4.8) leukemias . In addition, mitoxantrone showed moderate activity against DM-resistant L1210 leukemia.

ORL J Otorhinolaryngol Relat Spec, 1982, 44(3), 156 - 69
Ototoxicity of aminoglycoside antibiotics by rapid intravenous injection; Ohtani I et al.; The ototoxicity and nephrotoxicity of aminoglycoside antibiotics (dibekacin, gentamicin and kanamycin) administered to rabbits by rapid intravenous or intramuscular injections were histopathologically compared . Comparative evaluations between the two routes were further made concerning the levels of the antibiotics in serum and in perilymph . The results revealed that, although the peak serum level after a rapid intravenous injection was significantly higher than that observed after an intramuscular injection, no differences in the transfer into the perilymph, and in inner ear or renal damage were seen between the two different routes . In other words, the results of the present study did not support the conventional idea that the higher the peak blood levels of the aminoglycoside antibiotics, the greater the risk of damage to the inner ear or kidney.

Nephron, 1982, 30(3), 262 - 8
Prevention of scarring in experimental pyelonephritis in the rat by early antibiotic therapy; Slotki IN et al.; Experimental pyelonephritis was produced by either retrograde or direct infection of rat kidneys by Escherichia coli 078 . Combined antibiotic therapy with amoxycillin and gentamicin, commenced within 23 h of direct infection, prevented acute suppuration and subsequent scarring . The same antibiotics combination commenced 24 h after both retrograde and direct infection did not significantly reduce acute suppuration but did reduce scarring . Treatment begun later than 24 h after infection had no effect on the outcome of pyelonephritis induced by either route . Significantly lower peak levels of serum antibody to the O antigen of E . coli 078 were obtained in rats treated at 24 h after retrograde pyelonephritis than in those in which treatment was started later . Kidney scarring could not be prevented if antibiotic therapy was commenced after the appearance of mononuclear cells in the inflammatory lesion.

Digestion, 1982, 23(1), 9 - 15
Effect of antibiotics in the prevention of jejunoileal bypass-induced liver dysfunction; Vanderhoof JA et al.; Administration of antibiotics has been reported to prevent or minimize liver dysfunction in experimental animals having been subjected to jejunoileal bypass, suggesting that jejunoileal bypass-induced liver dysfunction results from production of toxic substances by bacteria in the defunctionalized bowel . However, improved absorption will also prevent bypass-induced liver injury . We studied the effects of tetracycline on the development of bypass-induced liver dysfunction and compared it to the mucosal adaptation of the intact bowel after bypass . After 6 weeks, rats subjected to bypass but not given antibiotics had decreased levels of serum triglycerides, hepatic cytochrome P-450, and hepatic pentobarbital hydroxylase . Evaluation of intestinal mucosal hyperplasia after bypass indicated that animals given antibiotics after bypass developed greater increases in mucosal DNA content, mucosal protein, and mucosal weight than bypassed animals not receiving antibiotics . We speculate that the beneficial effects of antibiotic administration on liver function after bypass may be a result of improved absorption.

Rev Fr Mal Respir, 1982, 10(1), 45 - 52
{An inquiry into the use of antibiotics in acute respiratory infections in primary health care centres in Algeria during 1980 (author's transl)}; Chaulet P et al.; In an acute respiratory infection the prescription of antibiotics is often still routine in Algeria . Antibiotic consumption has accounted for 20 to 28% of the drug bill in recent years . A prospective pilot study was carried out in 1980 in 26 health centres in different parts of the country . This has allowed an evaluation to be made of the importance of acute respiratory infections in the demand for primary health care and the frequency of antibiotic prescriptions . In 1980 acute respiratory infections accounted for 23% of consultations in primary medical care . In 69% of cases they were for upper respiratory tract above the glottis sometimes extending to the bronchi; in 28% the infections were isolated to the trachea and bronchi; in 3% the infections were bronchiolar, alveolar or pleural . Although the localisation of acute respiratory infections suggests a predominantly viral origin, antibiotics were prescribed in 76% of cases; these prescriptions depend more on the habit of the prescriber than the observed pathology . An agreed strategy is required to deal with acute respiratory infections at the primary care level and is a priority for health care . It should now go beyond the theoretical model to the level of realistic and rational therapeutic decisions.

Vopr Pitan, 1982 Jan-Feb, (1), 50 - 3
{Hygienic significance of the use of feed antibiotics in animal husbandry}; Priputina LS et al.; Introduction of kormogrisein-10 and fradizin-10 into feeds of farm animals did not lead to accumulation in the animals' meat of grisin and tilozin residues or to an adverse effect of such meat on the body of experimental rats . In the course of oral administration of the preparations to the animals the authors determined the period of detectability of antibiotic residues in muscles and organs and the minimal toxic doses of the preparations.

J Physiol, 1982 Jan, 322, 447 - 55
Inhibition, by trichothecene antibiotics, of brain protein synthesis and fever in rabbits; Cannon M et al.; 1 . To test further the hypothesis that brain protein synthesis is necessary for fever, three structurally similar trichothecene antibiotics were injected into the cerebral ventricles of rabbits . They were 3,15-diacetoxy-12-hydroxytrichothec-9-ene (DAHT), 3,15-didesacetyl-calonectrin (DDAC) and T-2 toxin . Their actions on hypothalamic incorporation of {14C}leucine and fever were compared . 2 . DDAC (60 micrograms) and T-2 toxin (10 micrograms) strongly inhibited leucine incorporation and fever . DAHT (60 micrograms) did not diminish fever and had a smaller effect upon leucine incorporation . 3 . The findings strengthen considerably earlier suggestions that brain protein synthesis is an essential step in pyrogenesis.

J Antibiot (Tokyo), 1982 Jan, 35(1), 62 - 6
Structure and conformation of fourteen antibiotics of the quinoxaline group determined by 1H NMR; Williamson MP et al.; Nuclear magnetic resonance has been employed to characterize fourteen new antibiotics belonging to the quinoxaline group, produced by feeding aromatic acids to Streptomyces echinatus . Twelve of the antibiotics are the expected substituted quinomycins and adopt conformations very similar to that of echinomycin . This is discussed in relation to their different DNA-binding characteristics . The other two antibiotics are triostins, supporting the proposal that triostins serve as biosynthetic precursors of the quinomycins.

Folia Microbiol (Praha), 1982, 27(1), 43 - 8
Inhibition of the incorporation of 14C-precursors in Mycobacterium smegmatis by antibiotics and chemotherapeutics; Majtan V et al.; Twenty antituberculostatics and twelve other compounds were divided into three groups according to their ability to influence the rate of incorporation of 14C-adenine and 14C-leucine in M . smegmatis . The first group includes compounds significantly inhibiting the incorporation of 14C-leucine, the second group comprises compounds inhibiting simultaneously the incorporation of both 14C-precursors, the third group contains compounds that do not bring about a 50% decrease of the rate of incorporation even at a concentration of 400 micrograms/mL.

Antibiotiki, 1982 Jan, 27(1), 3 - 6
{Azotobacter chroococcum, a producer of a new antifungal antibiotic}; Pridachina NN et al.; Strain 92 of Azotobacter chroococcum was obtained as result of natural selection . It produces an antibiotic active against phytopathogenic fungi . The antibiotic was isolated from the bacterial mass of the culture with ethanol extraction followed by column and thin-layer chromatography on silica gel . The pure antibiotic is a viscous oily substance of a yellowish colour, readily soluble in the majority of the organic solvents, not soluble in water, readily oxidized by air oxygen . The UV absorption spectrum of the antibiotic ethanol solution had bonds characteristic of the conjugated tetraene system . The presence of ketone and enol groups in the antibiotic molecule was shown with the colour reactions . It was confirmed by the data of the antibiotic IR spectrum investigation . According to the data of high resolution mass spectroscopy the empirical formula of the antibiotic is C20H30O4, the molecular weight is 334 . It is suggested that the antibiotic is an ester of aliphatic tetraenic acid differing from the known antibiotics produced by Azotobacter.

Neurosurgery, 1982 Jan, 10(1), 50 - 4
Intraventricular cerebrospinal fluid antibiotic concentrations in patients with intraventricular infections; James HE et al.; The antibiotic concentration of the fluid from either lateral ventricle was determined 104 times in 37 patients through direct ventricular puncture, external ventricular drainage (EVD), or cerebrospinal fluid shunt sampling . The patients were 1 month to 12 years old . When the patients were receiving maximal intravenous antibiotic therapy alone, the concentrations for the most part were below 5 microgram/ml, whereas patients receiving an antibiotic through direct ventricular puncture, EVD, or a shunt reservoir usually had concentrations over 5 microgram/ml . However, wide variations from patient to patient were found with all forms of treatment despite similar dosages . Clustering of the concentration tended to occur in each individual patient . The authors conclude that, to obtain a high concentration of an antibiotic in the ventricular fluid, one should administer it directly into the ventricle.

J Chromatogr, 1982 Jan 1, 234(1), 187 - 200
High-performance liquid chromatographic resolution and quantification of a dilactonic antibiotic mixture (antimycin A); Abidi SL; High-performance liquid chromatographic (HPLC) conditions are presented for the separation and quantitative determination of a homologous antibiotic complex (antimycin A) . Combined HPLC and chemical ionization mass spectrometry proved to be exceptionally useful for the structural identification of chromatographic components . Using electrochemical, fluorescence, and ultraviolet detectors, the minimum detectable amounts of the antibiotics were found to be in the ranges 0.10-1.12, 0.31-1.69, and 4.10-28.2 ng, respectively . Advantages of the preparation of Dns derivatives for use in fluorescence detection are discussed . Application of the HPLC technique to the analysis of the antibiotic mixture in organic tissues is demonstrated.

Pediatrics, 1982 Jan, 69(1), 1 - 3
Prophylactic antibiotics in pediatric surgery; Kesler RW et al.; The frequency and appropriateness of prophylactic antibiotic use in children less than 6 years of age who received surgery were examined . Antibiotics were prescribed for 62% of children who had surgery, and prophylaxis was the sole reason for antibiotic use in 73% of the patients . Prophylactic antibiotics were administered inappropriately with respect to timing or duration to 42% of the children receiving preoperative prophylaxis, 67% receiving intraoperative prophylaxis, and 55% receiving postoperative prophylaxis . Thus, prophylaxis alone is the major indication for antibiotic use in pediatric surgical patients, and prophylactic antibiotics are frequently administered inappropriately.

Cancer Res, 1982 Jan, 42(1), 280 - 4
Differential effect of imidazole antibiotics on untransformed and virus-transformed rat cell lines; Kuwano M et al.; The imidazole antimycotics clotrimazole and miconazole were tested on untransformed rat cell line 3Y1-B clone 1-6 (3Y1) and six transformed cell lines, which were independently isolated from 3Y1 or 3Y1-B clone 1 after infection with adenovirus 12 (AD-12) or with SV40, to determine their sensitivities to these drugs . The relative plating efficiency of three cell lines (T3, W4, and W5) transformed with AD-12 was reduced to 10(-1( of the initial value by clotrimazole (2 to 4 microgram/ml), whereas that of the parental cell line 3Y1 was reduced to 10(-1) of the initial value by clotrimazole (20 to 25 microgram/ml) . By contrast, the differential effect of miconazole on 3Y1 and AD-12-transformed cell lines was found to be a factor of 2 . The sensitivity of the SV40-transformed 3Y1 and the AD-12-transformed cell lines . The cellular sensitivity of untransformed 3Y1 cells to clotrimazole was significantly enhanced when exposed to various doses of the unsaturated fatty acid, linoleic acid . The untransformed and transformed cell lines showed sensitivities similar to the cytocidal activity of sterol-binding antimycotics, amphotericin B and filipin.

J Urol (Paris), 1982, 88(3), 159 - 62
{Prophylactic antibiotic therapy in endoscopic resection of the prostate . Randomized study of 47 cases (author's transl)}; Gattegno B et al.; The authors investigated the effect of giving a single injection of the antibiotic gentamycin one hour before endoscopic resection of the prostate, by random case selection in a group of 47 cases . The untreated and the treated cases were considered quite comparable . The presence of bacteriurea greater than 10(5) per ml during the first 15 postoperative days was significantly greater in the untreated group than in the preoperatively treated group . The results showed 44% for the untreated group and 14% for the treated group . After 15 days the results were identical for the two groups.

Crit Rev Microbiol, 1982, 9(2), 101 - 38
Sublethal concentrations of antibiotics, effects on bacteria and the immune system; Atkinson BA et al.; Biological specimens obtained from patients with infections that are treated with antibiotics at dosages that resulted in body fluid concentrations below those that are minimally inhibitory, exhibit abnormal forms of bacteria . Identical morphological changes can be induced in vitro when the parental normal forms of the bacteria . Identical morphological changes can be induced in vitro when the parental normal forms of the bacteria are exposed to subminimal concentrations of certain antibiotics . The phenomenon of induced abnormal morphology and ultrastructure has received consideration in terms of: (1) the relationship of the induced alterations of the specific bacterial species to the given antibiotic, (2) in vitro conditions required for antibiotic induced alterations, (3) the mechanisms of action; (4) immune responses to the abnormal forms, and (5) relationship between abnormal structure and the inhibition of bacterial replication . This review provides the reader with a description and the significance of current research in the above areas which together comprise the growing field of subinhibitory concentrations of antibiotics.

Surv Ophthalmol, 1982 Jan-Feb, 26(4), 204 - 6
Intravitreal administration of antibiotic in the treatment of bacterial endophthalmitis . III . Consensus; Baum J et al.; Five years ago, we established the Viewpoints section on the premise that written constructive expression of differences of opinion about ophthalmic problems would increase the level of understanding in the profession . Since we thought that neither eloquence of expression nor vigor of debate would resolve the questions, we avoided a response-rebuttal format and simply asked each author to express his or her point of view along with the evidence supporting it, without seeing the other's manuscript . Rather than rigidly cementing opinions, we hoped this approach would maintain maleable minds in the search for solutions to perplexing problems . In the inaugural Viewpoints section, Baum and Peyman discussed periocular versus intravitreal administration of antibiotics in the treatment of bacterial endophthalmitis (Antibiotic administration in the treatment of bacterial endophthalmitis . I . Baum JL: Periocular injections . II . Peyman GA: Intravitreal injections . Surv Ophthalmol 21:332-346, 1977) . Now, in a novel format, the authors reappraise the subject and come to a consensus that minimizes the therapeutic quandary engendered by the original articles . While acknowledging that intravitreal administration of antibiotic is the preferred route for the treatment of bacterial endophthalmitis, the authors emphasize the lack of controlled and randomized clinical trials in this area . Their practical recommendations will assist the ophthalmologist who tries to forestall the devastation of bacterial endophthalmitis.

Acta Odontol Scand, 1982, 40(5), 341 - 52
Antibiotic compounds and enamel demineralization . An in vitro study; Bjorvatn K; Discoloration, pigmentation and even caries-like lesions have been reported in teeth subsequent to per oral administration of antibiotics . The present in vitro study examines the possible medicament/tooth reaction by exposing plane, polished enamel surfaces to aqueous solutions or oily suspensions of various commonly used penicillin compounds, or to solutions of tetracycline sodium . The teeth were examined by visual inspection, microhardness tests, scanning electron microscopy and microradiography . pH and {Ca2+} of the test solutions were analyzed by potentiometry . Surface or subsurface lesions and a decline in microhardness were found in (most) enamel specimens exposed to aqueous solutions of the medicaments . Similar changes were found in test specimens immersed in deionized water, while saliva, oily suspensions of the medicaments and aqueous solutions made from ordinary Ca-penicillin had no adverse affect on the enamel . The most serious destruction was seen in enamel specimens submerged in watery solutions made from effervescent (citrate-containing) Ca-penicillin, or from tetracycline . A slight decline in pH was observed in the aqueous solutions during the experiment . The calcium ion concentration did not increase parallel to enamel destruction.

Methods Find Exp Clin Pharmacol, 1982, 4(5), 343 - 5
Interaction of aminoglycoside antibiotics with oxytocin and prostaglandin E2 on uterine contractility; Paradelis AG et al.; In the present study the interaction of aminoglycoside antibiotics with oxytocin and prostaglandin E2 on the contractility of the rat uterus was investigated . It was found that oxytocin and prostaglandin E2 were able to completely reverse the uterine relaxing effect of aminoglycoside antibiotics and when administered concomitantly they exert a protective action . These findings support the view that aminoglycoside antibiotics affect superficially bound extracellular calcium only, since oxytocin and prostaglandins primarily act on intracellular calcium.

Z Allg Mikrobiol, 1982, 22(3), 191 - 6
Spore differentiation in relation to certain antibiotics in the blue-green alga Nodularia spumigena Mertens; Pandey RK et al.; Induction of spore differentiation is achieved within three days in Nodularia spumigena by incubating the cultures at 35 degrees C in the light . Morphologically detectable sporulation and spore germination could not occur in the presence of chloramphenicol, streptomycin and penicillin . But chloramphenicol-supplemented cultures developed prominent cyanophycin granules . Synthesis of these granules seems to be a non-ribosomal phenomenon.

Am J Hosp Pharm, 1982 Jan, 39(1), 104 - 8
Effect of freezing and microwave thawing on the stability of six antibiotic admixtures in plastic bags; Holmes CJ et al.; The stability of six antibiotics in intravenous fluids in polyvinyl chloride containers after freezing and microwave-thawing is reported . Tobramycin sulfate 160 mg, amikacin sulfate 1 g, ticarcillin disodium 3 g, clindamycin phosphate 300 mg, nafcillin sodium 1 g, and ampicillin sodium was also diluted in plastic bags of 0.9% sodium chloride injection 50 ml . For each antibiotic except ampicillin sodium, three bags were prepared and assayed immediately for antibiotic content . Two of the bags were frozen at -20 degrees C for 30 days and then thawed, one by exposure to room-temperature air and the other by microwave radiation . Each was assayed immediately and after 8 and 24 hours storage at room temperature . The third bag was not frozen, but was stored at room temperature and assayed at 8 and 24 hours . Five bags of ampicillin sodium were prepared-three in 0.9% sodium chloride, which were frozen at -20, -30, and -70 degrees C, and two in 5% dextrose, which were frozen at -30 and -70 degrees C . All ampicillin solutions were stored 30 days, assayed, microwave-thawed, and assayed again . All antibiotics except ampicillin retained 90% or more potency when microwave-thawed after storage at -20 degrees C for 30 days, and after subsequent storage at room temperature for 24 hours . Ampicillin sodium was stable in 0.9% sodium chloride when stored at -30 or -70 degrees C, microwave-thawed, and stored up to eight hours at room temperature . Ampicillin sodium was stable in 5% dextrose when stored at -70 degrees C and microwaved-thawed, but its potency declined to 70.5% after eight hours storage at room temperature.

Mead Johnson Symp Perinat Dev Med, 1982, (21), 52 - 6
Antibiotic pharmacokinetics in newborns; Smith AL; Non-metabolized polar antibiotics have a volume of distribution roughly equivalent to the extracellular fluid compartment and are cleared by the kidney . The volume of the ECF, therefore, affects the magnitude of Cmax when a constant dose is administered . Variations in glomerular filtration rate, or in the case of beta-lactams renal plasma flow, vary the rate at which the drug is cleared from the body . The pharmacokinetics of metabolizable antibiotics is complex; not only does prodrug pharmacokinetics affect the observed serum concentration of the active agent, but hepatic blood flow and biliary flow rate affect the rate at which such antibiotics (i.e., chloramphenicol) are removed from the serum . In these, general dosage guidelines are almost impossible in newborns; monitoring the serum concentrations is mandatory.

Acta Microbiol Acad Sci Hung, 1982, 29(3), 161 - 71
Escherichia coli strains isolated from surface waters . Distribution by resistance to antibiotics and R-plasmid transfer; Lantos J et al.; Samples were taken from surface waters in Csongrad county in the months March through December, 1980 . Escherichia coli isolates selected at random were tested for resistance to 5 antibiotics and for R-plasmid carriership . Of the strains isolated from Tisza river at each of 8 sampling sites, 50-60% were sensitive to all the 5 antibiotics . The percentage of sensitivity was much lower if only the strains isolated during the summer months, when the water level was high, or those isolated from affluents and backwaters were taken into account . The frequency of resistance was the highest for tetracycline, followed in order by ampicillin, streptomycin, kanamycin and chloramphenicol . R-plasmid was carried by 43% of the resistant isolates tested, mainly by multiresistant ones.

Antibiotiki, 1982, 27(9), 643 - 5
{Developmental cycle and the cytomorphological characteristics of the oleandomycin producer Streptomyces antibioticus}; Zhuravleva NP et al.; The developmental cycle and cytomorphological features of the industrial strain OL-1 and its variant 0968 of the oleandomycin-producing organism were studied . Variant 0968 was obtained as a result of exposure of the spores of strain OL-1 to UV light . When grown under submerged conditions in flasks with the rich medium, the strains were characterized by a complete developmental cycle consisting of three generations of the hyphae . Every generation had a tendency for formation of submerged spores . The UV-induced variant differed from the industrial strain by higher levels of the antibiotic accumulation which correlated with higher rates of the spore germination . The strains were characterized by polymorphism of the mycelium and formation of submerged spores during their cultivation which is likely to prolong the antibiotic synthesis from 120 to 216 hours from the inoculation moment . The long-term selection of the oleandomycin-producing organism on the rich medium markedly changed the culture genotype and resulted in significant changes in the developmental cycle under submerged cultivation conditions . The data may be used for the microscopic control of the process of oleandomycin production.

Antibiotiki, 1982, 27(9), 693 - 7
{Use of luminescent analysis for studying the characteristics of the virus-inhibiting action of polyene antibiotics}; Shneider MA et al.; The inhibitory effect of flavopentin was shown on the models of infectious and oncogenic viruses . Flavopentin is a polyenic antibiotic belonging to pentaenes . The characteristic features of the polyene interaction with the plasma membrane of the host cell were defined with the use of the luminescence analysis, when the antibiotic was applied with the therapeutic or prophylactic purposes in experimental influenzal infection.

Antibiotiki, 1982, 27(7), 496 - 501
{Mechanism of polyene antibiotic inactivation . Changes in the physicochemical characteristics and the destruction of the polyene chromophore levorin during inactivation}; Bronov LV et al.; The results of studying free radicals of some polyenic antibiotics with the EPR method are presented . It is shown that the number of free radicals increased by 100 per cent with a 2-fold decrease in the biological activity . A qualitative change in the EPR spectrum due to the presence of a new radical type was also observed . The changes in the spectral characteristics of levorin allowed one to demonstrate that breaking of the links and formation of the polymer products during oxidative destruction of the polyenic chromophore resulted from attachment of the radicals through the antibiotic double bonds . The data correlate with the results of the quantum-chemical evaluation of the polyenic chromophore.

Int Arch Allergy Appl Immunol, 1982, 69(3), 279 - 81
Inhibition of mitogen-induced human lymphocyte responsiveness by polymixin antibiotics; Ferrante A et al.; Polymixin antibiotics, polymixin B and polymixin E (colistin) inhibited the mitogen-induced lymphoproliferative response of human lymphocytes . Inhibition of the lymphocyte response to PHA, PWM and Con A was evident at a low concentration of 1 U/ml of antibiotics . Lymphocytes in which the signals for proliferation had occurred were similarly prevented from proliferating . The effects were not due to cell death (toxicity) . Since polymixin concentrations at which inhibition of lymphocyte proliferation was observed are employed in tissue culture medium and are also attained in plasma of patients, the results suggest that the use of the antibiotics in lymphocyte cultures limits lymphocyte responsiveness and that patients receiving polymixin antibiotics may experience a state of immunosuppression.

Res Commun Chem Pathol Pharmacol, 1982 Jan, 35(1), 63 - 78
An investigation of the effects of aminoglycoside antibiotics on Na+-K+ ATPase as a possible mechanism of toxicity; Chahwala SB et al.; An investigation was made of the effect of aminoglycoside antibiotics on Na+-K+ ATPase to determine whether their toxicity might be attributable to an inhibition of this enzyme . Three preparations were used: human erythrocyte ghosts; microsomal fractions of the cortex and outer medulla of the guinea-pig kidney; rat isolated renal tubules . In all three preparations marked inhibition of Na+-K+ ATPase (50-100%) was seen only at very high concentrations of drug (10(-2)M) . Although aminoglycoside antibiotics are known to accumulate to high concentrations in vivo, particularly in the renal cortex, it is argued that these findings suggest that an effect on Na+-K+ ATPase is unlikely to be their primary mechanism of toxicity.

J Bacteriol, 1982 Jan, 149(1), 92 - 8
Differential effects of antibiotics inhibiting gyrase; Engle EC et al.; Both oxolinic acid and coumermycin A1, inhibitors of DNA gyrase, block DNA synthesis in Escherichia coli . At low concentrations of oxolinic acid, the rate of bacterial DNA synthesis first declines rapidly but then gradually increases . This gradual increase in synthesis rate depended on the presence of wild-type recA and lexA genes; mutations in either gene blocked the increase in synthesis rate . In such mutants, oxolinic acid caused a rapid decline, followed by a slow, further decrease in DNA synthesis rate . Coumermycin A1, however, produced a more gradual decline in synthesis rate which is unaffected by defects in the recA or lexA genes . An additional difference between the two drugs was observed in a dnaA mutant, in which initiation of replication is temperature sensitive . Low concentrations of oxolinic acid, but not coumermycin A1, reduced thermal inhibition of DNA synthesis rate.

Antibiotiki, 1982, 27(9), 658 - 61
{Method of determining the acid-base properties of antibiotics in water-alcohol solutions}; Komarov EV et al.; The pH scale of aqueous-alcoholic solutions titrated with aqueous solutions of hydrochloric acid and sodium hydrate was developed . These agents are most frequently used in investigation of the acid and basic transformations of antibiotics . The use of the scale was exemplified with the study of acid and basic properties of gramicidin S containing 2 amino groups in the side chain . Calculation of the constants of protonization of the amino groups of gramicidin S showed their significant differences depending on the solvent nature.

Cytogenet Cell Genet, 1982, 33(1-2), 35 - 41
Hyperthermic potentiation of chromosome aberrations by anticancer antibiotics; Vig BK et al.; In view of the success of hyperthermia as a modality in cancer treatment, we have studied its effect on chromosomes in combination with anticancer antibiotics . Three classes of chemicals, one with a non-delayed type of effect (adriamycin), one with a delayed type of effect (mitomycin C), and one with a truely radio-mimetic effect (bleomycin) were selected for study on human lymphocytes and Chinese hamster K-1 cells . Propane sultone was also included because its effect on plants is suppressed by hyperthermia . The data show increased because its effect on plants is suppressed by hyperthermia . The data show increased potential of these chemicals to induce chromosome aberrations when applied at temperatures higher than 37 degrees C, irrespective of the phase of cell cycle . The potentiation may be due to true synergism (bleomycin) of facilitation of entry of larger quantities of the drug (adriamycin) . No potentiating effect was observed on the induction of sister chromatid exchanges (SCEs).

Int Arch Allergy Appl Immunol, 1982, 68(1), 35 - 40
Antigenicity of beta-lactam antibiotic preparations: production of IgE antibodies to beta-lactam antibiotic and their cross-reaction within the antibiotic group; Iwata M et al.; BALB/C mice were immunized with conjugate of benzylpenicillin or ampicillin with Ascaris suum extract . The mice developed IgE antibodies to penicillin, which were found to react with commercially available penicillin preparations in the PCA system . Elimination of polymerized penicillin by Sephadex chromatography from tested preparations could not diminish their activities to elicit PCA . High pressure liquid chromatographic (HPLC) separation of PcG preparation yielded fractions unable to elicit PCA . On the other hand, all fractions from ABPC retained the activity even after the HPLC purification . A comparative estimation of cross-reactivity of IgE and IgE antipenicillin antibodies showed that IgE antibodies cross-reacted with a variety of beta-lactam antibiotics in a high degree.

Neoplasma, 1982, 29(1), 37 - 42
Inhibition of RNA dependent DNA polymerases by anthracycline antibiotics; Bogdany L et al.; In our experimental work we intended to study the effect of certain anthracycline antibiotics, like Adriamycin, Daunomycin, Carminomycin on the RNA dependent DNA polymerase, i.e . reverse transcriptase (RT) system . Over the direct effect on the RT our aim was to find out the rate of selectivity of above antibiotics on the RT . For doing this we compared the above effects to those found on natural nucleic acid polymerases . These experiments were confirmed using synthetic polynucleotid template poly(rA)n(dT)12-18 for the Rauscher RT enzyme and poly(dA)n . poly(dT)n for E . coli DNA polymerase I . In our work we have shown that Carminomycin, in contrast to Adriamycin and Daunomycin, possesses a highly specific inhibitory effect on the RT enzyme system.

J Antibiot (Tokyo), 1982 Jan, 35(1), 67 - 73
Comparative study of field desorption and secondary ion mass spectra for antibiotics; Kambara H et al.; Nonvolatile and thermolabile antibiotics are investigated both by field desorption and by secondary ion mass spectrometry (SIMS) . It has been successfully demonstrated that these two methods are complementary in obtaining informations about molecular weight and structure . Although FD is most widely used for the investigation of nonvolatile biologically active compounds, there are some compounds of which FD can not provide reliable information . SIMS is successfully applied to obtain structural information of these compounds . SIMS spectra frequently depend on the surface conditions of sample holder materials.

Int J Clin Pharmacol Ther Toxicol, 1982 Jan, 20(1), 12 - 8
Recent studies on antibiotics and small molecular immunomodulators with potential usefulness in treating lung cancer: Part I - Antitumor antibiotics and their derivatives; Umezawa H; Aclacinomycin, isolated from the culture of a Streptomyces, and 4'-O-tetrahydropyranyladriamycin, prepared by chemical derivation, exhibit significantly low cardiac toxicity and more effectiveness than does adriamycin . Pepleomycin, a new derivative of bleomycin, has 4-5 times lower pulmonary toxicity and more potent activity than the parent antibiotic . The future prospects of studies on antibiotics with potential usefulness in treatment of lung cancer are discussed.

Scand J Infect Dis Suppl, 1982, 33, 108 - 14
Differential effects of antibiotics on adhesins of antibiotic resistant strains of Escherichia coli; Eisenstein BI et al.; Sublethal concentrations of antibiotics that inhibit protein synthesis were found to diminish the ability of strains of Escherichia coli to bind to human leukocytes and to oral epithelial cells, guinea pig erythrocytes, and mannan-containing yeast cells . In general depressed adherence correlated with diminished production of type 1 fimbriae by the drug-treated bacteria and was affected by the antibiotics in the following order: aminoglycoside (gentamicin, streptomycin, neomycin) greater than spectinomycin greater than tetracycline greater than chloramphenicol . With one notable exception, mutation to resistance to antibiotic-induced growth inhibition resulted in resistance to the sublethal, anti-adherence effects of the same antibiotic . The exceptional strain, VL-2, was the only one out of many streptomycin-resistant strains that was not also resistant to the anti-adherence effects of subinhibitory concentrations of the drug . Compared to control cultures of VL-2, those grown in antibiotic demonstrated decreased amounts of mannose-sensitive hemagglutination (by greater than 99%) and adherence to human epithelial cells (58%) and leukocytes (93%) . When treated bacteria were examined by electron microscopy, they were found to be as heavily fimbriate as control bacteria, but their fimbriae were twice as long . Moreover, fimbriae isolated and purified from drug-treated bacteria had no lectin-like properties . Thus, although most antibiotics diminished the adhesive properties only the antibiotics-sensitive bacteria, streptomycin caused one streptomycin-resistant strain of bacteria to produce aberrant (non-adhesive) fimbrial protein.

Experientia, 1981 Dec 15, 37(12), 1318 - 20
Effect of enkephalins in the presence of the antibiotic bacitracin in the longitudinal muscle strip preparation from guinea-pig ileum; Aleixandre A et al.; The antibiotic bacitracin (5 x 10(-5) -4 x 10(-4) M) increase the inhibition of the contractile response caused by both enkephalin release and direct application of Met-enkephalin 5 x 10(-7) M in the longitudinal muscle strip preparation from guinea-pig ileum . This effect is attributed to an inhibition of enkephalin degrading peptidases by bacitracin.

Biochim Biophys Acta, 1981 Dec 14, 638(2), 234 - 41
Characterization of a respiratory mutant of Escherichia coli with reduced uptake of aminoglycoside antibiotics; Muir ME et al.; A strain of Escherichia coli (NSW77) which is partially resistant to streptomycin was isolated by selecting for growth on plates supplemented with 12.5 micrograms/ml streptomycin, a concentration which completely inhibits growth of wild-type strains . The low-level resistance of the mutant appears to result from a reduced ability to accumulate streptomycin intracellularly . In addition, the mutant strain is unable to use succinate for growth because of a defective respiratory chain . Thus, membranes of the mutant strain were found to have approximately half the NADH and D-lactate oxidase activity of the parent strain . Moreover, membranes of the mutant were found to contain demethyl-menaquinone and, in place of ubiquinone, a structural analogue, 2-octaprenyl-3-methyl-6-methoxy-1,4 benzoquinone . The mutation responsible for both the Suc-phenotype and partial resistance to streptomycin was found to be located near minute 15 on the bacterial chromosome . Both the biochemical and genetic evidence suggests the the mutation in strain NSW77 resides in the ubi F gene . Another previously characterized ubi F strain was also found to have a reduced capacity to take up an aminoglycoside antibiotic (gentamicin) . These results suggest that the respiratory defects in ubi F strains are responsible for the reduced capacity of such strains to accumulate aminoglycosides.

J Vet Pharmacol Ther, 1981 Dec, 4(4), 277 - 84
The pharmacokinetics of some aminoglycoside antibiotics in the horse; Baggot JD et al.; The disposition kinetics and bioavailability of streptomycin, kanamycin and neomycin were determined following their administration as parenteral preparations to horses . Single doses (10 mg/kg) of each aminoglycoside were given by the intravenous (i.v.) and intramuscular (i.m.) routes and, at a later time, seven intramuscular doses were injected at 12-h intervals . The pharmacokinetic behaviour of the three aminoglycosides was similar, in that a rapid distribution phase was followed by a relatively short half-life . The half-life (mean +/- SD, n = 6) of kanamycin (1.80 +/- 0.17 h) was significantly (P less than 0.01; t test, 10 d.f.) shorter than that of streptomycin (3.40 +/- 0.42 h), while neomycin half-life (2.10 +/- 0.97 h) was of an intermediate length . The apparent volume of distribution of neither kanamycin nor neomycin varied significantly (P greater than 0.05) from that of streptomycin and numerically (V1 d congruent to 230 ml/kg) was the same as the extracellular fluid volume . The body clearance of kanamycin (88.5 +/- 11.3 ml/kg.h) was significantly (P less than 0.01) larger than that of streptomycin (47.5 +/- 7.9 ml/kg.h), while a significant difference in this parameter did not exist (P greater than 0.05) between neomycin and streptomycin . Following intramuscular injection, each aminoglycoside was rapidly and completely absorbed from the injection site, although neomycin showed wide individual variation in the fraction absorbed . The administration of multiple doses did not change either the bioavailability or the apparent half-life from the values obtained after a single dose . The only pharmacokinetic difference between these aminoglycosides that is of clinical importance lies in the rate of their elimination . A dosage interval of 8 h would be appropriate for kanamycin compared with a 12-h interval for streptomycin . The dosage interval for neomycin based on half-life should be 8 h but, due to the relatively greater toxicity of this aminoglycoside, an interval of 12 h might be recommended . The height of the peak serum concentration is determined by the size of the dose.

Jpn J Exp Med, 1981 Dec, 51(6), 355 - 62
Binding of antibiotics to human liver glutathione S-transferases; Nishiya H et al.; Glutathione S-transferases (GSH S-transferases) are multifunctional enzymes and are known to play an important role as intracellular binding protein in human liver . Binding of several antibiotics, including cefotetan, benzylpenicillin, cefazolin, chloramphenicol and gentamicin, to cationic and anionic GSH S-transferases isolated from human liver, and to human serum albumin, has been investigated by using the centrifuge column technique, which is supposed to be an excellent one for its sensitivity and rapidity in ligand binding studies . The dissociation constants (Kd) of the antibiotics for human liver GSH S-transferases and for human serum albumin, and the number of binding sites for the antibiotics on a molecule of human liver GSH S-transferases and of human serum albumin have been evaluated by means of Scatchard plots . This study has shown that cefotetan is bound to cationic GSH S-transferases to the greatest extent, followed by benzylpenicillin, cefazolin and chloramphenicol, gentamicin being bound to the smallest extent . It has been confirmed that not only cationic GSH S-transferases but also anionic GSH S-transferases have the binding capacity to the antibiotics, and that the extent of binding of the antibiotics to anionic GSH S-transferases is similar to the one to cationic GSH S-transferases . Therefore, anionic GSH S-transferases are supposed to play nearly the same role as cationic GSH S-transferases in transport of the antibiotics in human liver . The fact that the extent of binding of the antibiotics to human liver GSH S-transferases is closely correlated with the extent of biliary excretion of the antibiotics suggests that human liver GSH S-transferases play an important role in the transport of certain antibiotics from plasma, through hepatocytes, into bile.

Resuscitation, 1981 Dec, 9(4), 267 - 73
The combined use of hyperbaric oxygen, antibiotics and surgery in the treatment of gas gangrene; Guidi ML et al.; The clinical course and treatment of 21 critically ill patients suffering from gas gangrene are reported . Analysis of the results has underlined the importance of intensive care and hyperbaric management to prevent the evolution of disease and to improve patients' clinical conditions for surgical procedures.

Antibiotiki, 1981 Dec, 26(12), 906 - 12
{Interaction of the antitumor antibiotic olivomycin with Mg2+ ions}; Pitina LR et al.; The study on the mechanisms of olivomycin and olivin interaction with the magnesium ions showed that formation of the olivomycin complexes with Mg2+ involved 2 stages . At the first (rapid) stage Mg2+ is attached to keto-oxygen of the aglycone polycyclic part . At the second (slow) stage the complex is relaxed into the stable state with a more compact configuration . the equilibrium constants (Ce) of the main processes of olivomycin and olivin interaction with Mg2+ were determined . In the first case Ce = 3 . 10(3) M+1 and in the second case Ce = 1.6 . 10(2) M-1 . It was shown that the geometric and optic characteristics of the complexes were consistently related: formation of the stable complex was accompanied by a 10-time decrease in the fluorescence quantum efficiency.

Am Surg, 1981 Dec, 47(12), 515 - 8
Diffusion of antibiotics from a polytetrafluoroethylene-benzalkonium surface; Prahlad A et al.; The ability to bond antibiotics non-covalently to polytetrafluoroethylene surfaces was evaluated in an animal model . Grafts soaked or bonded in (14)C-penicillin were placed in subcutaneous pockets in rats and harvested at various time intervals . The amount of antibiotic present on grafts and in local tissue were evaluated by liquid scintillation counting . Antibiotic bonding resulted in higher concentrations of antibiotic present on the graft at implantation . Diffusion of antibiotics from the graft into surrounding tissues was also slowed by the bonding process . However, all grafts retained minimal activity at the end of 24 hours . The possibility of managing vascular prostheses with antibiotic bonding and local antibiotic irrigation is raised.

Am J Med, 1981 Dec, 71(6), 941 - 4
Reduction in antibiotic costs by restricting use of an oral cephalosporin; Seligman SJ; Antibiotic cost control programs are important; however, they may be difficult to implement if they include intensive involvement of infectious diseases specialists . In a large municipal hospital, review of antibiotic cost data indicated that 31 percent of the total antibiotic expenditure was for an oral cephalosporin, cephalexin . The requirement that an antibiotic justification form be completed did not decrease use of the drug . However, the requirement that the prescribing physician telephone an infectious diseases specialist resulted in marked restriction of the oral cephalosporin and was accompanied by a 29 percent reduction (adjusted for inflation) in total antibiotic costs . Since comparatively few telephone requests were made and since the decision process to use an oral cephalosporin is comparatively simple, marked reduction in antibiotic costs was achieved with relatively little effort by the infectious disease expert.

J Hyg (Lond), 1981 Dec, 87(3), 511 - 23
Effect of cooking and cold storage on biologically active antibiotic residues in meat; O'Brien JJ et al.; An investigation was undertaken to see if cooking or cold storage would destroy or decrease the level of biologically active antibiotic in tissues from animals given therapeutic doses of antibiotic on three occasions prior to slaughter . The effects of cooking and cold storage on the biological activity of the residues of ampicillin, chloramphenicol, oxytetracycline, streptomycin and sulphadimidine were varied; in some instances the effects were minimal, in others nil.

Med Biol, 1981 Dec, 59(5-6), 360 - 7
Polyamines and antibiotic effects on translation; Goldemberg SH et al.; Protein synthesis was studied in polyamine-auxotrophic mutants of Escherichia coli . The decreased protein synthesizing rate observed both in vivo and in vitro in polyamine-starved bacteria is due to defective 30S ribosomal subparticles which are impaired in the initiation step of translation . Analysis of peptides synthesized in vivo suggests a more extensive misreading by putrescine-depleted bacteria . Cells grown without polyamine show a markedly decreased response to the inhibitory effect and the misreading inducing action of streptomycin in vivo and in vitro . The polyamine-starved bacteria are also less sensitive to other aminoglycoside antibiotics such as neomycin, kanamycin and kasugamycin.

J Hyg (Lond), 1981 Dec, 87(3), 477 - 83
Escherichia coli resistant to tetracyclines and to other antibiotics in the faeces of U.K . chickens and pigs in 1980; Smith HW et al.; A survey conducted in 1980, 9 years after the banning of the use of tetracyclines as feed additives in the U.K., indicated that table chickens and pigs were still a large reservoir of tetracycline-resistant Escherichia coli; the incidence of transferable tetracycline resistance was greater in chicken E . coli strains (68%) than in pig E . coli strains (20%) . Large amounts of sulphonamide-resistant and of furazolidone-resistant E . coli were found in the faeces of chickens; E . coli resistant to both sulphonamides and streptomycin were common in the faeces of chickens and pigs . E . coli with transferable or mobilizable trimethoprim resistance were present in the faeces of most pigs and in the faeces of 10% of chickens.

Klin Monatsbl Augenheilkd, 1981 Dec, 179(6), 512 - 3
{Treatment of bacterial endophthalmitis by vitrectomy and intraocularly administered antibiotics (author's transl)}; Faulborn J; Local and systemic applications of antibiotics in cases of vitreous bacterial infections have proved insufficient because of blood-vitreous barriers . Intravitreal antibiotic injections overcome these barriers and may control the infection . Recommendations are given for intravitreal therapy with Gentamicin, combined with a pars plana vitrectomy in advanced infections.

Biometrics, 1981 Dec, 37(4), 753 - 61
A statistical test for classification, with applications to the characterization of pathogens according to antibiotic susceptibility patterns; Grimson RC et al.; If n different analytical procedures are applied to a culture of a pathogen, then that pathogen is characterized by an ordered sequence or vector of length n . A group of such sequences (or 'susceptibility patterns' as they are called in this context) can be generated by applying this process to cultures taken from infected individuals in an epidemic . This paper introduced statistical tests that can be used to determine whether a pattern obtained from the culture of a single case differs from those patterns obtained from cultures of a group of infected individuals . The methods are applied to come nosocomial epidemics . These taxonomic techniques extend beyond the present application to other classification problems in the biological and medical sciences.

Arch Intern Med, 1981 Dec, 141(13), 1789 - 93
Antibiotic combination-associated nephrotoxicity in granulocytopenic patients with cancer; Wade JC et al.; Antibiotic combination-associated nephrotoxicity was reviewed in 491 granulocytopenic patients with cancer and fever . Nephrotoxicity was defined as a rise in the serum creatinine level of more than 0.4 mg/dL . The different aminoglycosides, when combined with ticarcillin disodium, were found to have an equivalent nephrotoxic potential and, for the purpose of analysis, were combined and termed "aminoglycoside plus ticarcillin" (Ags + ticarcillin) . Groups treated with gentamicin or amikacin plus cephalothin sodium were combined and termed "aminoglycoside plus cephalothin" (Ags + cephalothin) . The rate of nephrotoxicity was statistically less for the Ags + ticarcillin group, eight (3.1%) of 262 patients, than for the Ags + cephalothin group, 23 (18.3%) of 126 patients . Age greater than 50 years was a potentiating factor for the occurrence of nephrotoxicity in the Ags + cephalothin group . We have concluded that for granulocytopenic patients with cancer and fever, the antibiotic combination of the Ags + cephalothin should not be used as empiric antibiotic therapy.

Antibiotiki, 1981 Dec, 26(12), 915 - 9
{Effect of the antitumor antibiotic actinoxanthine on cells cultured in vitro}; Borodina VM et al.; Significant changes in the nucleus structure, complete suppression of the mitotic activity, markedly decreased synthesis of RNA (by 70--80 per cent according to incorporation of 3H-uridine) and decreased levels of DNA (by 40 per cent according to olivomycin binding) were observed in the fibroblasts cultivated in vitro due to exposure to actinoxanthine in an amount of 50 microgram/ml . The data indicate direct damaging effect of the drug on the cell chromatin . The above nuclear changes were also observed after a short-term exposure of the cells to the drug (up to 5 minutes) . Still, they became evident only after the subsequent incubation of the cells in a pure culture medium for at least 15 minutes . No such changes in the nucleus structure were detected when after the 5-minute exposure to actinoxanthine the cells were exposed to trypsin for 3 minutes . When the time of exposure to actinoxanthine was longer (15 minutes and higher), trypsin suppressed the manifestation of the above nuclear changes . The two-stage mechanism of the damaging effect of actinoxanthine on the chromatin of the cells cultivated in vitro is discussed . The damaging effect of actinoxanthine on the cells begins from binding of the drug with the cell membrane . After that a short incubation period follows and then the characteristic changes in the nucleus structure appear.

Biochemistry, 1981 Nov 24, 20(24), 7042 - 6
Glutamate as the common precursor for the aglycon of the naturally occurring C-nucleoside antibiotics; Suhadolnik RJ et al.; Pyrazofurin is one of four naturally occurring C-nucleoside antibiotics; it is elaborated by Streptomyces candidus . The biosynthesis of the pyrazole ring of pyrazofurin has been studied by using 13C- and 14C-labeled acetate . Carbon-13 incorporation into pyrazofurin was observed by proton-decoupled 13C Fourier transform NMR spectroscopy . The incorporation of 14C from {1-14C}acetate was 0.7% . The enrichment of carbons 3, 4, and 5 of pyrazofurin from {2-13C}acetate by S . candidus confirms earlier findings that acetate is converted to glutamate by the combined action of the Krebs cycle and malic enzyme {Elstner, E . F., Suhadolnik, R . J., & Allerhand, A . (1973) J . Biol . Chem . 248, 5385} . Malic enzyme will give rise to {1,2-13C}acetate from {2-13C}acetate . The {1,2-13C}acetate is then converted to glutamate labeled with 13C in carbons 2--5 . The 13C incorporation data indicate that carbons 1, 2, 3, and 4, but not 5, of glutamate serve as the four-carbon donor for the carboxamide carbon, C-5, C-4, and C-3, respectively, of the pyrazole ring of pyrazofurin.

Rev Infect Dis, 1981 Nov-Dec, 3 suppl, S216 - 23
Effects of antibiotic-diuretic interactions in the guinea pig model of ototoxicity; Brummett RE; The guinea pig model has been useful for estimating quantitatively the ototoxic effects of many different drugs . Our model utilizes measures of the Preyer pinna reflex, the alternating current cochlear potential and sensory hair-cell morphology to access drug effects . The principle pathophysiologic lesion of aminoglycoside-induced permanent ototoxicity appears to be sensory hair-cell loss in the organ of Corti . Aminoglycoside antibiotics were found to interact with loop-inhibiting diuretics, and the augmented ototoxic effects were attributed to hair-cell destruction . The interaction is specific for loop-inhibiting diuretics but not for the aminoglycosides since nonaminoglycoside antibiotics, such as viomycin and polymixin B, interacted similarly . Noninteractive antibiotics include amphotericin B and vancomycin . The absence of ototoxic effects with vancomycin is of interest in view of its broadening clinical utility.

Antibiotiki, 1981 Nov, 26(11), 809 - 13
{Action of acridine dyes on antibiotic, pigment and aerial mycelium formation in streptomycete producers of multicomponent antibiotics}; Lapchinskaia OA et al.; The ability of 5 streptomycetous species synthesizing multicomponent antibiotic to produce the antibiotic and water-soluble pigment and to form the aerial mycelium in the presence of acridine dyes was studied . It was found that the character of the produced complex changed, when acridine dyes were added to the medium under conditions not affecting the culture growth and the temperature was elevated . Colonies deficient with respect to formation of the aerial mycelium and with changed pigment and antibiotic production were detected in the monospore cultures of the streptomycetes treated with acridine dyes, when the spore survival was equal to 100 percent, the frequency of the colonies being about 40 per cent.

Antibiotiki, 1981 Nov, 26(11), 807 - 9
{Quantitative mycelial growth and antibiotic biosynthesis patterns in actinomycete producers of heliomycin}; Kozhevina LS et al.; The quantitative regularities of the mycelium growth and antibiotic biosynthesis were studied in submerged cultures of the heliomycin-producing organisms . The following regularities of the mycelium growth were observed: the growth of the growth tubes proceeds according to the exponential law (the first exponential phase of the culture growth), the growth of separate branching hyphae submits to the linear dependence, the total length of the branching mycelium increases exponentially (the second phase of the culture exponential growth) . During the first exponential phase the specific rate of the antibiotic biosynthesis is equal to the specific rate of the mycelium growth and the synthesis of heliomycin balanced with the mycelium growth . During the second exponential phase the specific rate of heliomycin biosynthesis exceeds the specific growth rate which is evident of the antibiotic overproduction . The changes in the ratio of the specific growth rate and antibiotic biosynthesis coincide with the changes in the intracellular localization of heliomycin . When the synthesis of heliomycin is balanced with the culture growth, the antibiotic is in the form showing yellow luminescence . With the beginning of the antibiotic overproduction heliomycin in the form of granules with bright orange luminescence is detected in the mycelium along with the yellow luminescence form . It is suggested that formation of the granules during the antibiotic overproduction is one of the mechanisms of the antibiotic excess removal.

Am J Otolaryngol, 1981 Nov, 2(4), 299 - 306
Alteration of aminoglycoside antibiotic ototoxicity by hyper- and hypohydration; Prazma J et al.; The ototoxicities of tobramycin sulfate and gentamicin sulfate were investigated in guinea pigs under conditions of normal, increased, and decreased hydration . Increased hydration was associated with no decline in the amplitude of the cochlear microphonics, a lesser decline in the eighth nerve action potentials and lesser damage to the organ of Corti . Decreased hydration was associated with an increase in the threshold of the cochlear microphonics and the eighth nerve action potentials, a decline in the amplitude of the cochlear microphonics, a greater decline in the eighth nerve action potentials, and greater damage to the organ of Corti . Tobramycin sulfate was substantially less toxic than gentamicin sulfate with normal, increased and decreased hydration . These findings suggest the preferential use of tobramycin sulfate for patients with normal renal function, and especially patients with renal impairment.

Pharmazie, 1981 Nov, 36(11), 763 - 7
{Isolation and structure of the main metabolite of macrolide antibiotic turimycin H (author's transl)}; Fricke H et al.; Turimycin H0 was isolated from the bile of rats as main metabolite after i.v . administration of turimycin H . It was also obtained by incubation of turimycin H with liver homogenates of dogs and rats . Degradation of turimycin H by liver homogenate of pigs was found to be relatively slow . Turimycin H0 was identified as 4"-deacylturimycin H by MS.

J Antibiot (Tokyo), 1981 Nov, 34(11), 1408 - 15
Virantmycin, a new antiviral antibiotic produced by a strain of Streptomyces; Nakagawa A et al.; Virantmycin, a novel chlorine-containing antiviral antibiotic, has been isolated from Streptomyces nitrosporeus No . AM-2722 . The active substance in culture broth is isolated as colorless needles by solvent extraction followed by high performance liquid chromatography on silicic acid . The molecular formula is C19H26NO3Cl (molecular weight 351) from the elemental analysis and mass spectrum . The antibiotic possesses antifungal activity and potent inhibitory activity against various RNA and DNA viruses.

Am Surg, 1981 Nov, 47(11), 511 - 4
Preservation of an infected arterial graft with combination systemic-topical antibiotic therapy; Hinton PJ et al.; A case is presented which illustrates the unusual ability to retain a bifurcation aortofemoral vascular graft with the graft-to-femoral-artery anastomosis involved in a groin abscess . The drainage of the abscess, debridement of devitalized tissue, and the combined application of topical and systemic antibiotic therapy was successful . Some authors report that should an anastomosis of a bifurcation vascular graft, in the vicinity of the groin, become involved in infection, the threat of anastomotic disruption and continued sepsis may lead to amputation, death, or both . It is not the purpose of this report to advocate conservative management of a vascular graft infection with suture line involvement based on anecdotal experience . However, the case reported here and the experience of other authors mentioned suggest that an attempt to treat an infected graft without its removal may be indicated in selected patients where extra anatomical revascularization would be hazardous.

Prikl Biokhim Mikrobiol, 1981 Nov-Dec, 17(6), 890 - 5
{Effect of triterpene glycosides and polyene antibiotics on cell membrane permeability for K+ ions and UV-absorbing substances}; Anisimov MM et al.; The effect of triterpene glycosides (cauloside C from Caulophyllum robustum, theasaponine from Thea sinensis, cucumarioside G from Cucumaria fraudatrix stichoposide A from Stichopus japonicus S., holothurines A and B from Holothuria mexicana, holothurine C from Bohadschia sp.) on the membrane permeability for K+ ions and UV-absorbing substances was compared with that of polyene antibiotics, viz., amphotericine B and nystatine . As a biological model fertilized eggs of sea urchin Strongylocentrotus nudus and yeast Saccharomyces carlsbergensis were used . In the sea urchin study most triterpene glycosides in low concentrations induced the outflux of K+ and in hgih concentrations that of both K+ and UV-absorbing agents . In the yeast study triterpene glycosides at identical doses induced the outflux of both K+ and UV-absorbing agents . The membranotropic effect of triterpene glycosides depended on the medium temperature and the biological system used.

Obstet Gynecol, 1981 Nov, 58(5 Suppl), 95S - 9S
Considerations of antibiotic therapy during pregnancy; Schwarz RH; The use of antibiotics in pregnancy requires that the clinician consider both toxicity to and pharmacokinetics for mother and fetus . Although most adverse reactions to antibiotics in the adult are not modified by pregnancy, those to tetracycline and erythromycin estolate are the exceptions . Tetracycline is contraindicated throughout pregnancy because of fetal effects, whereas sulfa preparations, trimethoprim, and chloramphenicol are contraindicated only at specific times during gestation . The pharmacokinetics of antibiotics in the mother are such that lower serum concentrations are achieved for a given dose, which may be important in serious or resistant infections . Fetal kinetics are such that transfer to amniotic fluid and distribution within the fetus may not provide adequate protection for the fetus in cases of chorioamnionitis.

J Antibiot (Tokyo), 1981 Nov, 34(11), 1389 - 401
Fredericamycin A, a new antitumor antibiotic . I . Production, isolation and physicochemical properties; Pandey RC et al.; A new antitumor antibiotic, fredericamycin A (FCRC-A48, NSC-305263), has been isolated from a strain of Streptomyces griseus (FCRC-48) . Based on its unique ultraviolet-visible spectrum, infrared spectrum, proton and carbon-13 nuclear magnetic resonance spectra and mass spectra, it is judged to be a novel acid-base indicator type of compound . Its production, isolation and physicochemical properties are discussed . The isolation, ultraviolet-visible spectrum and some biological properties of two minor components, fredericamycin B and fredericamycin C, are also described.

Antibiotiki, 1981 Nov, 26(11), 816 - 20
{Structure of the tricyclic triaminotricarboxylic acid (Y) from the antibiotic actinoidin}; Berdnikova TF; The products of triaminotricarboxylic acid (Y) transformation in alkaline and reduction (HI/P) hydrolysis and the PMR spectra of the Y-Phe dipeptide were studied and the nature of the 3 amino acid substitutes and their position in the aromatic nuclei were determined . With regard to the data on the structure of the aromatic skeleton published earlier the structure of the Y amino acid as 3-(2-chlor-4-seryl-phenoxy)-5-(4-seryl-phenoxy)-p-hydroxyphenylglycine was suggested . The presence of 2 alcoholic groups of the phenylserine fragments of the Y amino acid in the actinoidine aglycone was shown with additional acetylation (Ac2O/Py) of N-acetylmethoxyaglycone . It was found with O-acetylation of N-acetylmethoxyactinosaminyl aglycone that the actinosamine amino sugar in the actinoidine molecule was bound with one of the above groups.

Biochim Biophys Acta, 1981 Oct 27, 655(3), 335 - 41
Crystal and molecular structure of the antibiotic blasticidin S hydrochloride pentahydrate; Swaminathan V et al.; The three-dimensional structure of blasticidin S hydrochloride pentahydrate, a member of the cytosine amino nucleoside antibiotics, has been solved using diffractometer data and refined to an R value of 0.115 . The crystal data are a = 13.500(5), b = 20.387(7), c = 4.824 A, beta = 98.66(3) degrees, Z = 2, Dc = 1.389 g .cm-3, space group P21 . The nucleoside base conformation is anti(chi = 86 degrees) and the 2',3'-unsaturated pyranosyl sugar exhibits a half-chair (degree H5) conformation . The amide plane is twisted from the trans position by about 10 degrees . The guanidium group and the amino group of the amino acid chain are positively charged, while the carboxyl group of the sugar is ionized . The chloride ion is surrounded by water molecules only, in a trigonal prismatic arrangement . The molecule has an extended conformation and there is an intramolecular hydrogen bond between the ammonium group and the carboxyl group . A striking feature of blasticidin is that all the hydrophilic groups lie on one side of the molecule and the hydrophobic groups on the other . Amicetin also shows a similar feature and this might be linked to the commonality of their antibiotic functions . Hydrogen bonds link the hydrophilic sides of adjacent molecules forming double chains parallel to the b-axis . The hydrophobic sides of adjacent double chains are separated by a water layer.

Lancet, 1981 Oct 24, 2(8252), 883 - 7
Therapy of acute otitis media: myringotomy, antibiotics, or neither? A double-blind study in children; van Buchem FL et al.; In a double-blind study 171 children with acute otitis media (239 affected ears) were treated by four different methods: neither antibiotics nor myringotomy; myringotomy only; antibiotics only; or both antibiotics and myringotomy . All received symptomatic treatment . There were no significant differences in clinical course (pain, temperature, duration of discharge, otoscopic appearances, audiography, recurrence rate) between the four groups . In the groups treated without antibiotics, the ears discharge for slightly longer and the eardrums took a little longer to heal; these differences were not significant . No complications were seen . Symptomatic therapy with nosedrops and analgesics seems a reasonable initial approach to acute otitis media in children . Myringotomy and antibiotics can be reserved for cases in which the course of otitis is irregular, there are complications such as mastoiditis, or ear discharge continues beyond 14 days.

Br Med J (Clin Res Ed), 1981 Oct 3, 283(6296), 883 - 4
Antibiotic use in otitis media: patient simulations as an aid to audit; Chaput de Saintonge DM et al.; Diagnostic and prescribing practices in otitis media vary, and audit is difficult because doctors may not see comparable cases . Seven general practitioners took part in a pilot study to discover if simulated patients evoked the same diagnostic and treatment responses as reveal patients . Forty-eight patients entered the study over three weeks and provided data for two simulations; one included the doctor's description of the ear and the other a photograph instead . Each doctor was shown the two sets of simulations and asked to state his diagnosis and treatment . The diagnoses each doctor reached agreed significantly with those reached on the simulations of the same patients . The decisions to prescribe antibiotics also showed good agreement.

Laryngol Rhinol Otol (Stuttg), 1981 Oct, 60(10), 553 - 7
{Experimental investigations of the ototoxicity of aminoglycoside antibiotics and their clinical importance (author's transl)}; Federspil P; The problems of the clinical evaluation of the ototoxicity of an aminoglycoside antibiotic are mentioned . The criteria for a correct performance of experimental ototoxicity tests and the applied methods concerning the functional ahd histological investigations are reported on . The results obtained by the experimental evaluation of the ototoxicity of the clinically important newer aminoglycoside antibiotics (gentamicin, tobramycin, sisomicin, dibekacin, and netilmicin) on the market are described my means of representative graphs . Possible sources of error by using the applied or other tests are discussed . An exact correlation of results obtained by neat experiments and the clinical data is found and by that also the necessity of experimental investigations as to the ototoxicity of new ototoxic drugs before their clinical trials.

Avian Dis, 1981 Oct-Dec, 25(4), 857 - 65
Comparison of low dietary calcium and sodium sulfate for the potentiation of tetracycline antibiotics in broiler diets; Waldroup PW et al.; Three experiments were conducted to compare different methods of short-term potentiation of tetracycline antibiotics for broiler chicks . Reduction of dietary calcium and addition to sodium sulfate were compared in different combinations with various levels of chlortetracycline (CTC) and oxytetracycline (OTC) . Reducing dietary calcium from 0.8 to 0.4% significantly increased serum levels of CTC and OTC . Adding sodium sulfate (1.25%) also increased serum levels; the majority of the response occurred at the higher calcium level . There was no benefit from adding sodium sulfate to the low-calcium diet . Neither body weight gain nor feed utilization were adversely affected during the 5-day test period.

Biull Eksp Biol Med, 1981 Oct, 91(10), 458 - 60
{Activity of nonspecific hepatic oxidases and the biological effects of the antineoplastic antibiotic adriamycin}; Bogush TA et al.; It was shown in male CBA mice that toxic doses (15 and 20 mg/kg) of adriamycin (AD) inhibited the activity of nonspecific liver oxidases and noticeably increased the duration of the animals' sleep after injection of hexenal which is a substrate of this enzymatic system . The inhibitory effect of AD remained unchanged in the course of 9 days of the experiment . The nontoxic dose of AD (5 mg/kg) inhibited the activity of the enzymatic system on the 2nd--3rd days after the injection of the drug . Meanwhile the activity of the enzymatic system returned to the level seen in intact animals by days 5--6 . The toxic action of AD declined on activation of nonspecific liver oxidases with phenobarbital and rose as a result of administering the inhibitor SKF 525-A . The authors discuss whether it is possible to use the data obtained for clinical application of AD.

Toxicol Lett, 1981 Oct, 9(2), 107 - 12
Comparative evaluation of the neuromuscular blocking activity of three new aminoglycoside antibiotics in rats; Renna G et al.; The effects of three aminoglycoside antibiotics on the rat isolated phrenic nerve-diaphragm preparation and on the sciatic nerve-gastrocnemius muscle preparation were investigated . Tobramycin, amikacin and ribostamycin produced dose-dependent neuromuscular blockade of the diaphragm twitches . Comparison of results showed that the neuromuscular blocking potency was as follows: tobramycin greater than amikacin greater than ribostamycin . The neuromuscular blockade produced gy these antibiotics was reversed by calcium chloride, whereas it was not influenced by neostigmine methylsulfate . Furthermore, the neuromuscular blocking potency in vitro of these three aminoglycosides was paralleled by their activity in vivo on the sciatic nerve-gastrocnemius muscle preparation.

Am J Hosp Pharm, 1981 Oct, 38(10), 1480 - 3
Training patients to administer intravenous antibiotics at home; Swenson JP; A home intravenous antibiotic infusion program (HIAP) implemented in a 256-bed, nonteaching, primary-care hospital is described . Physicians initiate participation in the program by referring a patient to clinical pharmacists and intravenous team nurses . Patients are evaluated on the basis of the following five criteria: (1) the infectious process has responded clinically to treatment, the patient has been afebrile for at least five days, and the physician has noted that the patient could be discharged if continued i.v . antibiotic therapy were not necessary; (2) the patient has successfully completed the pharmacist's teaching sessions on aseptic technique, the heparin-lock system, and the mechanics of i.v . antibiotic piggyback administration; (3) the patient has a family member or close friend who can attend the patient instruction sessions; (4) the patient has reasonably good veins, i.e., they have not readily developed phlebitis or heparin-lock occlusions, and there are a number of viable sites or the antecubital veins are accessible for insertion of a catheter, if necessary; and (5) a preliminary cost comparison indicates that the patient's participation in the HIAP would result in a cost savings . The therapeutic results of the HIAP were considered successful by the physicians . The i.v . team nurses noted no increase in heparin-lock site problems . The pharmacists spent an average of four hours teaching the HIAP patients, at a rate of $25 per hour . This cost was billed as a part of pharmacy services . Most of the insurance companies were willing to pay the entire charge for the HIAP . For eight patients treated in the program, savings of 128 bed-days and $18,968 were shown . the HIAP was found to be successful in terms of medical treatment and cost containment in a medium-sized, primary-care hospital.

Surg Gynecol Obstet, 1981 Oct, 153(4), 573 - 6
The role of systemic antibiotics in operations upon the colon; Mehigan D et al.; A prospective randomized clinical trial was carried out to evaluate the role of parenteral antibiotics in elective operations upon the colon . All patients received a mechanical intestinal preparation, neomycin and erythromycin base orally and topical antibiotic administration intra-abdominally and to the wound at the time of operation . The patients were further randomized into three groups . One group received no parenteral antibiotics; the second group received parenteral cefamandole, and the third group received parenteral penicillin, gentamicin and clindamycin . One hundred and thirteen patients completed the study . The sepsis rate postoperatively was similar for all three groups . When oral and topical antibiotics are used in elective operations upon the colon, parenteral antibiotics provide no additional benefit.

Ann Surg, 1981 Oct, 194(4), 502 - 9
Effect of prophylactic antibiotics in acute nonperforated appendicitis: a prospective, randomized, double-blind clinical study; Busuttil RW et al.; A prospective, randomized, double-blind clinical study was performed to determined the efficacy of short-term (24 hr) perioperative antibiotics in preventing septic complications after emergency appendectomy for nonperforated appendicitis . The patients were stratified into three clinical arms: Group I (placebo, n = 45), Group II (cefamandole, n = 46) and Group III (cefamandole plus carbenicillin, n = 45) . The three groups of patients were similar in regard to age, sex, duration of operation and pathologic classification of the appendix . The overall incidence of infection in the study was 5.1% . The infection rates in Groups II (2.2%) and III (0%) were significantly lower than Group I (placebo) (13.3%), (p less than 0.05) . No difference was observed between cefamandole alone and cefamandole plus carbenicillin . Average postoperative hospital days per patient for each group was: Group I - 3.8 days; Group II - 2.9 days; Group III - 3.1 days . Cost analysis of hospitalization including cost of prophylactic antibiotics revealed a $247.99 per patient saving for Group II versus Group I and $95.53 for Group III versus Group I . Systemic prophylactic antibiotics can successfully reduce septic complications after appendectomy for nonperforated appendicitis, and a single drug (cefamandole) directed at the facultative pathogens is as effective as double drug therapy, which includes specific anaerobic coverage.

Br J Vener Dis, 1981 Oct, 57(5), 320 - 4
Gonorrhoea in men with homosexual contacts . Serogroups of isolated gonococcal strains related to antibiotic susceptibility, site of infection, and symptoms; Bygdeman S; In 37 homosexual men the incidences of urethral, rectal, and pharyngeal gonorrhoea were 45.9%, 56.8%, and 27% respectively . Local symptoms were present in all men with urethral gonorrhoea but in only 25% of those with pharyngeal or rectal gonorrhoea or both . Infection at two sites was found in 29.7% of the patients . Forty-nine gonococcal isolates from the 37 patients were serogrouped by coagglutination into one of the serogroups WI, WII, and WIII, and their susceptibility to benzylpenicillin, ampicillin, cefuroxime, doxycycline, and spectinomycin tested . Only one gonococcal isolate from each patient was counted when two isolates belonged to the same serogroup and had the same antibiotic susceptibility . Thus, 15.4%, 76.9%, and 7.7% of the gonococcal strains belonged to serogroups WI, WII, and WIII respectively . There was a significantly lower incidence of WI strains and a significantly higher incidence of WII strains among men with homosexual contacts than among other patients with gonorrhoea from the same geographical region . Gonococcal strains of serogroup WI were significantly more resistant to all antibiotics tested, except to spectinomycin, than randomly chosen WI strains . Among WII and WIII strains the incidence of diminished susceptibility to all antibiotics tested was about the same.

Wien Med Wochenschr, 1981 Sep 15, 131(17), 431 - 4
{Treatment of subacute pelvic inflammatory diseases with the antibiotic compound sulfametrol-trimethroprim (author's transl)}; Burmucic R et al.; 40 patients with subacute pelvic inflammations were treated with the antibiotic compound sulfametrol-trimethoprim . The patients received twice a day 2 tablets with some liquid in the morning and evening . The average duration of treatment was 16.1 days . In 37 patients (92.5%) the disease could be cured completely or a distinct improvement could be achieved . In 3 cases (7.5%) the results were unsatisfactory . Side-effects were seen merely in 2 cases (sickness with allergic exanthem and diarrhea respectively).

Postgrad Med J, 1981 Sep, 57(671), 599 - 601
Recurrent colitis following antibiotic-associated pseudomembranous colitis; Davies J et al.; A patient who developed severe pseudomembranous colitis following clindamycin therapy, and who went on to have recurrent attacks of non-specific colitis, histologically confirmed over the following 19 months, is described.

J Antibiot (Tokyo), 1981 Sep, 34(9), 1175 - 82
Resistance mechanisms of kanamycin-, neomycin-, and streptomycin-producing streptomycetes to aminoglycoside antibiotics; Hotta K et al.; Streptomyces kanamyceticus ISP5500, S . fradiae ISP5063 and S . griseus ISP5236, which produce kanamycin, neomycin or streptomycin respectively, were highly resistant to the antibiotics they produced . Polyphenylalanine synthesis in cell free systems was also resistant to the action of the antibiotics . Reciprocal exchange between ribosomes and S150 fractions from the three strains revealed that the S150 fraction of each strain had an enzyme activity that inactivated the appropriate antibiotic whereas the ribosomes were susceptible to the antibiotics . It was concluded that the resistance of the in vitro polyphenylalanine synthesizing systems of these antibiotics was due to the presence of inactivating enzymes . Furthermore, S . fradiae and S . kanamyceticus were highly resistant to aminocyclitol-containing aminoglycoside antibiotics other than those produced by the two strains . In these cases, the inactivating enzymes were found to have a major role in the resistance mechanism . However, the resistance of S . kanamyceticus ISP5500 to streptomycin seems to be due to resistance at the ribosomal level.

J Antibiot (Tokyo), 1981 Sep, 34(9), 1090 - 100
Studies on a new aminoglycoside antibiotic, dactimicin . II . Isolation, structure and chemical degradation; Ohba K et al.; A new aminoglycoside antibiotic, dactimicin produced by a Dactylosporangium matsuzakiense SF-2052 has been isolated by column chromatography on a cation-exchange resin and CM-sephadex . The structure of dactimicin was determined to be 4-amino-1,4-dideoxy-3-O-(2,6-diamino-2,3,4,6,7-pentadeoxy-beta-L-lyxo- heptopyranosyl)-1-{(N-formimidoylglycyl)-methylamino}-6-O-methyl-L-chiro-inosit ol . Alkaline hydrolysis of dactimicin afforded 1-N-(N-formylglycyl)fortimicin B, fortimicin B, fortimicin A and an acyl migration product, 2'-N-(N-formylglycyl)fortimicin B.

Arq Neuropsiquiatr, 1981 Sep, 39(3), 286 - 8
The use of prophylactic systemic antibiotics in compound depressed skull fractures in infancy and childhood; Plese JP et al.; The authors described their experience with the use of prophylactic antibiotics in children with compound depressed skull fractures . The analysis of the results of the treatment of patients with or without systemic antibiotics and with or without the replacement of the bone fragments showed no difference in the infection rate, any one was the method used.

Antibiotiki, 1981 Sep, 26(9), 692 - 4
{Changes in the state of plasma membrane proteins of tumor cells exposed to a polyene antibiotic and cyclophosphamide}; Oksman AIa et al.; The fractional composition of the proteins of the plasmatic membranes of the Ehrlich's tumor cells treated with various drugs was studied with the use of electrophoresis in polyacrylamide gel . It was shown that the character of the changes in the fractional composition of the plasmatic membrane proteins under the effect of levorin and cyclophosphamide was different . When the drugs were used in combination, summation of the changes induced by every drug alone was observed . Possible causes of the changes in the fractional composition of the membrane proteins are discussed.

Ann Plast Surg, 1981 Sep, 7(3), 207 - 12
Atypical mycobacterial cervical lymphadenitis--treatment with surgery and antibiotics; Lesesne CB et al.; Five patients, ages 2 to 5 years, were successfully treated for cervical lymphadenitis caused by the avium intercellulari complex of atypical bacteria . Preoperative treatment with standard antituberculosis therapy had been unsuccessful . Extensive surgery requiring a conservative radical neck dissection was sometimes required . Three patients had such extensive and progressive disease that immediate excision was impossible . These patients received a course of Amikacin with considerable improvement, permitting adequate excision and reconstruction . A fourth patient who received Amikacin did not respond, although sufficient excision was possible . This preliminary data indicates that a combined treatment of Amikacin and surgery in extensive cases may be useful in the treatment of cervical lymphadenitis due to atypical mycobacteria.

J Clin Gastroenterol, 1981 Sep, 3(3), 221 - 4
Antibiotic-associated colitis--an abating enigma; Tedesco FJ; In the past decade, C . difficile has been implicated as the putative organism in antibiotic-associated pseudomembranous colitis . The natural history, clinical features, and pathologic features have been better defined . Vancomycin is the current drug of choice in treating this illness, but other therapies as well as exciting epidemiologic areas need to be explored . The role of C . difficile toxin in chronic inflammatory bowel disease is another area which also must be evaluated.

Fundam Appl Toxicol, 1981 Sep-Oct, 1(5), 395 - 402
The ototoxicity of hydroxygentamicin, a new aminoglycoside antibiotic, in guinea pigs; Neidl MJ et al.; The comparative ototoxicity of hydroxygentamicin (Win 42,122-2), a new aminoglycosidic antibiotic, gentamicin and kanamycin was evaluated in guinea pigs by assessment of the Preyer (pinna) reflex response to pure tone frequencies ranging from 2.5 to 20.0 KHz, and by histologic examination of surface preparations of the organ of Corti . Daily subcutaneous administration of 80.0 mg/kg of gentamicin or 240.0 mg/kg of kanamycin to groups of six guinea pigs for 18 to 45 days resulted in loss of the Preyer reflex in all animals . The Preyer reflex was retained in 5 of 6 guinea pigs given 80.0 mg/kg/day of hydroxygentamicin for 77 days and in 6 of 6 guinea pigs given 160.0 mg/kg/day for the same period . Microscopic examination of cochleas from guinea pigs given gentamicin or kanamycin revealed extensive outer and inner hair cell loss in all animals . Cytocochleograms of 5 of 6 guinea pigs medicated with 160.0 mg/kg of hydroxygentamicin were comparable to those of the controls . In the sixth guinea pig there was a localized lesion involving all three rows of outer hair cells and some inner hair cells in the second turn . The results of this study indicated that hydroxygentamicin may be tolerated better than gentamicin in the guinea pig and therefore warrants further development as a new and less toxic aminoglycosidic antibiotic.

Antibiotiki, 1981 Sep, 26(9), 655 - 9
{Identification and the physicochemical characteristics of the extrachromosomal DNA from a Streptomyces antibioticus strain}; Orlova VA et al.; The data on centrifugation of DNA in the density gradient of caesium chloride-ethidium bromide, electron microscopy and electrophoresis of the DNA restricts from the satellite gradient band indicate that Str . antibioticus, the oleandomycin-producing organism possessed extrachromosomal cyclic DNA with the molecular weight of 21.3 . 10(6) +/- +/- 0.3 10(6) daltons . The extrachromosomal cyclic DNA had 7 identification sites for endonuclease BamHI, 5 sites for PstI, 12 sites for PvuII, more than 14 sites for SmaI and non for endonucleases Eco RI and HindIII.

Acta Otolaryngol, 1981 Sep-Oct, 92(3-4), 285 - 91
Variation in bacterial count in otorrhea from cases of chronic otitis media depending upon the method of antibiotic administration; Sugiyama M et al.; Patients with chronic otitis media (COM) were divided into two groups, one to be given Cephalexin (CEX) orally and the other to be given CEX ear drops locally . The counts of viable bacteria in otorrheal samples collected before and after CEX administration were determined . The incidence of decrease in the count of bacteria was higher in the group given ear drops than in the group given oral doses . The magnitude of decrease was greater in the former group . Various concentration of CEX representing the levels of the drug considered available at an otitis focus following oral administration were added to otorrheal preparations placed in biophotometer cells . After 24 hours of incubation, bacteria as undetected initially in the otorrhea were found in the biophotometer cells in 3 of 14 cases of COM.

Clin Orthop, 1981 Sep, (159), 194 - 200
Systemic antibiotics and gentamicin-containing bone cement in the prophylaxis of postoperative infections in total hip arthroplasty; Josefsson G et al.; In a prospective controlled multicenter study, the prophylactic effect of gentamicin-containing bone cement on postoperative infections in total hip arthroplasties was compared with that of systemically given antibiotics; 812 arthroplasties were randomly assigned to an antibiotic and 821 to a gentamicin-cement group . When the patients had been followed for a period of one to two years, 13 deep infections were diagnosed in the antibiotic group and three in the gentamicin-cement group . The difference was statistically significant.

Lancet, 1981 Aug 22, 2(8243), 407 - 9
Survey of antibiotic prescribing in a district general hospital . II . Lower respiratory tract infection; Moss FM et al.; A 28 day survey of all antibiotic prescriptions in a district general hospital included a brief interview with the prescriber of each prescription . One hundred and nineteen antibiotic courses were stated, by the prescriber, to be for the treatment of lower respiratory tract infection . By combining the prescriber's clinical evidence, laboratory data, and radiographic findings, an "index of infection" was produced for 94 patients . This index reflected features associated with bacterial infection of the lower respiratory tract and suggested that 49% of the antibiotic courses prescribed were justifiable, 11% were questionable, and 40% were unjustifiable . The choice of antibiotic was usually appropriate to the prescriber's diagnosis . Over 80% of the antibiotics used were of the penicillin group . Ampicillin, the single most frequently prescribed drug, accounted for 60% of the prescriptions . The frequency of diagnosis of chest infection increased with age . Almost 40% of patients over 81 years old who were admitted to hospital during the survey were prescribed antibiotics for chest infection . A higher proportion of older than of younger patients had low indices of infection.

Antibiotiki, 1981 Aug, 26(8), 592 - 4
{Effect of the antibiotic granulation method on the quality of semisynthetic penicillin capsules (e.g., the sodium salt of dicloxacillin)}; Grakovskaia LK et al.; A procedure for dry granulation of antibiotics consisting in dry compacting of a powder-like composition followed by its grinding to granules was developed . The advantages of dicloxacyllin capsules manufactured by dry granulation over the capsules manufactured by moist granulation are shown with respect to the content of the light absorbing admixtures during the capsule manufacture and storage . The conditions for estimation of the antibiotic dissolution from the capsule were developed with the use of a "Rotating Basket" apparatus . Comparative evaluation of disintegration and dissolution of the capsules prepared by dry or moist granulation showed practical equivalence of both types of the capsules with respect to these characteristics.

Antibiotiki, 1981 Aug, 26(8), 578 - 80
{Effect of the method of preserving actinomycetes in an isotonic sodium chloride solution on their cultural and morphological properties as well as on their antibiotic activity}; Orlova RS et al.; The effect of storage of the organisms producing celicomycin and antibiotic 1321 in sodium chloride isotonic solution on their survival, cultural and morphological properties and antibiotic was studied . It was found that this method of the actinomycete storage did not induce any significant changes in the above features and had no effect on the survival of the cultures . The study showed the usefulness of the method with respect to the actinomycetes producing the above antibiotics.

Zentralbl Bakteriol A, 1981 Aug, 249(3), 400 - 6
Studies on the effect of antibiotic substances on leptospires and their cultivation from material with a high bacterial count; Schonberg A; Leptospira species are difficult to isolate from sperm specimens because rapid growth of the contaminant flora will kill the pathogen . The resistance of 5 Leptospira strains to 5 different antibiotics was examined with a view to an inhibition of such contaminant growth . Neomycin (10, 20, 30 mg/l), vancomycin (5, 8, 10 mg/l), nalidixic acid (50, 75, 100 mg/l), streptomycin (5, 8, 10 mg/l) and chloramphenicol (5, 10, 20 mg/l) were added separately to Korthof's culture medium containing rabbit serum . The comparative growth rates of the leptospires were evaluated . Against the control medium, all 5 antibiotics were found to have an adverse influence on the multiplication phase . In conformity with literature data, vancomycin (10 mg/l) and nalidixic acid (50 mg/l) were found to have the lowest effect . In the cases of streptomycin and chloramphenicol, there was a high reduction of the leptospiral count and even a complete lack of multiplication . A combination of vancomycin (10 mg2l) and nalidixic acid (50 mg/l) was used for the recovery of leptospires from porcine sperm . To inhibit a growth of Ps . aeruginosa, 5000 U/l polymyxin B were added . The strongly inhibitory action of polymyxin B on leptospiral growth could be eliminated by subculturing in a medium free from inhibitory substances after 2 days.

Br J Clin Pharmacol, 1981 Aug, 12(2), 111 - 5
A pharmacokinetic and tolerance study of Ro13-9904, a new cephalosporin antibiotic; Pickup ME et al.; 1 Six healthy male volunteers received a total of 2500 mg of a new cephalosporin antibiotic Ro13-9904 by intramuscular injection in five divided doses at intervals of 12 h . 2 No significant systemic side-effects were observed and this was confirmed haematologically and biochemically . 3 The drug was distributed following intramuscular injection reaching a mean peak plasma concentration of 55 micrograms ml-1 (range 46-66) 1 to 2 h after the first injection . 4 Monoexponential elimination of drug was demonstrated . No significant difference was recorded in the plasma half-life after the initial dose (mean 6.7 h) and at steady state (mean 6.7 h) . The half-life is long compared with other cephalosporin antibiotics . 5 On the basis of the observed half-life, steady state should be reached within 48 h . A mean peak plasma concentration of 74 micrograms ml-1 (range 65-87) was recorded at steady state . Steady state plasma concentrations of Ro13-9904 with a dose of 500 mg every 13 h may be predicted from the pharmacokinetics of a single dose.

Biokhimiia, 1981 Aug, 46(8), 1499 - 509
{Changes in the structural state of boundary lipids in bacterial membrane under effect of the membranotropic antibiotic gramicidin S}; Dergunov AD et al.; Using data from measurements of excimerization at different wave-lengths of fluorescence excitation of the fluorescent probe pyrene in isolated M . lysodeikticus membranes and using the phenomenon of energy transfer in the protein tryptophanyl-pyrene system, a method for monitoring the probe population localized in the immediate proximity to protein structures, has been developed . This method allows to detect the existence within the physiological temperature range of a specific lipid population or a boundary lipid vicinal to the membrane proteins . The changes in this region under membrane treatment with the cyclodecapeptide antibiotic gramicidin S were studied . Incubation of membranes with the antibiotic increases the efficiency of quenching of membrane protein fluorescence by the quenchers localized in the membrane phase, i.e . 2-(14-carboxytetradecyl)-2-ethyl-4,4-dimethyl-3-oxasolidinyloxyl, cetylpyridinium chloride and pyrene, and changes the protein chromophore accessibility for J- . The lateral mobility of pyrene during gramicidin S adsorption on the lipid and protein-lipid membranes is decreased . The results obtained are interpreted in favour of partial disturbance in the interaction of the boundary lipid and membrane proteins under effects of gramicidin S.

Mycopathologia, 1981 Jul 10, 75(1), 45 - 9
{Preliminary investigation of the in vitro inhibitory effect of antibiotics on algae of the genus Prototheca}; Casal M et al.; We investigated the possible inhibitory action 'in vitro' by antibiotic containing discs against microscopic alga that are potential human pathogens of the genus Prototheca especially P . wickerhamii . The results indicated that inhibitors in vitro included amikacin, colistin, dibecacin, framicetin, gentamycin, kanamycin, lividomycin, neomycin, polymyxin, paromomycin, ribostamycin, sisomycin and tobramycin . We emphasize the interest in the effectiveness at these drugs in a case of human protothecosis.

Nucleic Acids Res, 1981 Jul 10, 9(13), 3175 - 86
Equilibrium binding of carcinogens and antitumor antibiotics to DNA: site selectivity, cooperativity, allosterism; Winkle SA et al.; The equilibrium binding of the carcinogens N-hydroxy-N-acetyl-2-amino-fluorene (HAAF) and 4-nitroquinoline-1-oxide (NQO) to phi X174RF DNA have been studied by phase partition techniques . Both molecules bind in a cooperative manner with only a few carcinogen molecules binding to each phi X174RF DNA molecule . The binding data for both HAAF and NQO fit a model in which two carcinogens cluster into a small number of sites--four sites for HAAF and twelve sites for NQO . Phase partition techniques were also used to study the binding of actinomycin D to both calf thymus DNA and poly (dG-dC) . poly (dG-dC) at much lower r values than had been previously reported . These data exhibit humped Scatchard plots which are indicative of cooperative binding; the overall shape of the Scatchard plots are consistent with a model for drug induced allosteric transitions in the DNA structure . The cooperativity in the actinomycin D binding to calf thymus DNA increases with decreasing sodium chloride concentration, suggesting a role for DNA flexibility in allosteric binding.

Ann Microbiol (Paris), 1981 Jul-Aug, 132B(1), 51 - 6
{Study of "in vitro" susceptibility of "Mycobacterium fortuitum" to aminoglycoside and beta-lactam antibiotics (author's transl)}; Casal M et al.; A study was made of the in vitro susceptibility of 39 strains of Mycobacterium fortuitum to 14 beta-lactamins and 11 aminoglycosides using disc diffusion techniques on Mueller-Hinton agar plates . Amikacin, lividomycin, neomycin and kanamycin inhibited clearly all the strains, while penicillins, cephalosporins and streptomycin proved inactive . In addition, other tested aminoglycosides inhibited poorly all the strains.

J Antibiot (Tokyo), 1981 Jul, 34(7), 856 - 61
Antitumor activity of an antibiotic identical with or closely related to xanthomycin A; Nishimura T et al.; An antibiotic, identical with or closely related to xanthomycin A, was isolated from a soil Streptomyces . The antibiotic displayed significant therapeutic activity by i.p . administration against i.p.-implanted mouse tumors: Ehrlich carcinoma, sarcoma 180 and P388 leukemia . Less therapeutic activity was observed by i.p . injection in mice bearing s.c . solid tumors of Ehrlich carcinoma and sarcoma 180 . No significant activity was found against L1210 leukemia, B16 melanoma and Lewis lung carcinoma . In vitro the antibiotic exhibited a potent cytotoxicity to human leukemia K562 and mouse lymphoblastoma L5178Y cells . DNA strand scission of PM2 phage was caused by the antibiotic in the presence of dithiothreitol.

J Antibiot (Tokyo), 1981 Jul, 34(7), 830 - 5
Importance of antibiotic production in antagonism of selected Streptomyces species to two soil-borne plant pathogens; Rothrock CS et al.; Antagonism of ten Streptomyces spp., five of which produce antibiotics, to the plant pathogens Rhizoctonia solani and Phytophthora megasperma var . sojae was studied . Antibiotic activity was detected in culture for the five antibiotic producers . S . griseus, S . hygroscopicus var . geldanus, and S . noursei produced wide zones of inhibition to R . solani and P . megasperma var . sojae . Similar activity was found for S . reticuli var . protomycicus to P . megasperma var . sojae . S . cellulosae reduced Rhizoctonia root rot on pea when sterile soil was infested simultaneously with the antagonist and R . solani . S . hygroscopicus gave almost complete disease control when the streptomycete was added 7 days prior to infesting the soil with R . solani . Several of the Streptomyces spp . reduced Phytophthora root rot on soybean when the streptomycetes were added to soil at the same time as P . megasperma var . sojae or 7 days prior to adding the pathogen . S . herbaricolor and S . coeruleofuscus gave the most consistent control . No relationship was found between reported antibiotic activity or antagonism on agar media and reduction in disease severity . Only S . hygroscopicus var . geldanus gave both control of Rhizoctonia root rot and large zones of inhibition on agar media when the streptomycetes were preincubated in soil for 7 days.

Isr J Med Sci, 1981 Jul, 17(7), 661 - 6
Antibiotic sensitivity patterns in field isolates of Mycoplasma gallisepticum as a guide to chemotherapy; Levisohn S; Control of Mycoplasma gallisepticum (Mg) infection in commercial poultry flocks has sometimes been achieved by the intensive use of antibiotics . In some cases, a single drug, tylosin tartrate, has been used repeatedly in prophylactic and therapeutic applications . It appears that this selective pressure can lead to the emergence of strains with reduced sensitivity to tylosin . This was observed in Mg strains isolated in 1978 from turkey breeding flocks repeatedly treated with tylosin, but not in isolates from acute disease outbreaks . Moreover, in a study of four recent outbreaks of mycoplasma respiratory disease in poultry, some of the Mg strains isolated in each of the outbreaks showed reduced sensitivity to tylosin and, at the same time, to spiramycin . This suggests that the buildup of these strains in the general pool of Mg is playing an increasingly significant role in clinical outbreaks . Periodic in vitro antibiotic sensitivity testing of field isolates of mycoplasma is indicated as a means of monitoring the impact of mass medication programs and as a guide to therapeutic treatment.

Antibiotiki, 1981 Jul, 26(7), 532 - 7
{Increase in the specific activity of killed influenza vaccines by using polyene antibiotics}; Shneider MA et al.; It was shown experimentally that polyenic antibiotics, i . e . amphotericin B and sodium levorin markedly increased the specific immunogenic properties and interferonogenic activity of inactivated influenza virus vaccine prepared with various methods from highly reproductive recombinants . The rate of pneumonia and death from influenza among the vaccinated mice treated with inactivated influenza virus vaccine and one of the polyenic antibiotics was lower than that among the animals treated with the vaccine alone (P less than 0.05) . Correlation between the increase in the immunological response, the decrease in the virus reproduction rate in the lungs and addition of the antibiotics into the vaccine was also observed . It is recommended that inactivated influenza virus vaccine be used in conjunction with polyenic antibiotics.

J Pharm Sci, 1981 Jul, 70(7), 772 - 7
Intestinal absorption mechanism of amphoteric beta-lactam antibiotics II: Michaelis-Menten kinetics of cyclacillin absorption and its pharmacokinetic analysis in rats; Tsuji A et al.; The absorption of cyclacillin at pH 7.0 by the rat small intestine was investigated using in situ perfusion . At the lowest dose of 95 microgram/ml, the antibiotic disappearance was rapid and followed first-order kinetics, with the disappearance being 85% at 100 min . At the intermediate concentrations of 770 and 1200 microgram/ml, the disappearance after 100 min was 69 and 54%, respectively, and semilogarithmic plots clearly showed convex curvatures . At the highest concentration of 30 mg/ml, cyclacillin disappeared slowly from the perfusate, in an apparent first-order fashion . The disappearance was 26% after 100 min of perfusion and was similar in extent at 5.2 mg/ml . This concentration-time profile was satisfactorily fitted to the simultaneous Michaelis-Menten and first-order kinetic equations . The area under the blood concentration versus time curve (AUC) after a single intraduodenal dose of cyclacillin was almost consistent with the AUC after the equivalent intravenous dose (10 mg/kg) . Additional evidence from a pharmacokinetic analysis of steady-state blood concentrations after constant infusion of cyclacillin through the portal vein and the small intestinal lumen indicated that cyclacillin absorption by the rat intestinal tissue at relatively low concentrations (less than 1 mg/ml) followed solely Michaelis-Menten kinetics . Cyclacillin may be transported by certain types of carrier-mediated mechanisms.

J Pharm Sci, 1981 Jul, 70(7), 768 - 72
Intestinal absorption mechanism of amphoteric beta-lactam antibiotics I: Comparative absorption and evidence for saturable transport of amino-beta-lactam antibiotics by in situ rat small intestine; Tsuji A et al.; The disappearance of various beta-lactam antibiotics from in situ rat small intestinal loops was studied at pH 7.4 . For monobasic penicillins, despite the wide variety of apparent partition coefficients in isobutyl alcohol-water, the disappearance from the jejunal loops was almost 30% (+/- 5% SD) . On the other hand, the disappearance of amphoteric derivatives of penicillins and cephalosporins having very low lipid solubility varied widely between 12 and 80% . The peak blood levels after intraduodenal administration to the rats correlated well with the extent of disappearance of amphoteric penicillins from the intestinal loops . Absorption studies utilizing in situ intestinal loops were performed at variable dose ranges to yield a clear dose-dependent disappearance . It is suggested that certain carrier-mediated transport systems underlie the absorption mechanism of amphoteric beta-lactam antibiotics.

Br J Haematol, 1981 Jul, 48(3), 369 - 75
Treatment of refractory adult acute lymphocytic leukaemia and acute undifferentiated leukaemia with an anthracycline antibiotic and cytosine arabinoside; Early AP et al.; Ten patients with acute lymphocytic leukaemia (ALL) and four patients with acute undifferentiated leukaemia (AUL) in relapse or refractory to conventional therapy were treated with remission induction therapy consisting of an anthracycline antibiotic and cytosine arabinoside . Twelve patients had previously demonstrated resistance to vincristine-prednisone and nine patients had prior anthracycline therapy . Nine patients achieved complete remission after one course of therapy with a median time to remission of 30 d . Of five nonresponders, three died of sepsis with marrow hypocellularity and no evidence of residual leukaemia . Only two patients had unequivocal evidence for resistance to an anthracycline-cytosine arabinoside regimen . Myelosuppression and infection were the most significant complications of therapy . The data presented indicate that marrow ablative chemotherapy with an anthracycline antibiotic and cytosine arabinoside is an effective regimen for remission induction in adults with ALL and AUL refractory to vincristine-prednisone . The use of these agents in remission consolidation therapy may offer the possibility of providing a reduction in residual resistant cells that are present after successful remission induction therapy with conventional agents.

Arthritis Rheum, 1981 Jul, 24(7), 905 - 11
Antibiotic therapy of septic bursitis . Its implication in the treatment of septic arthritis; Ho G Jr et al.; Infected olecranon, prepatellar, and infrapatellar bursae offer a unique opportunity to study the response of a closed-space infection to antibiotic therapy . Using percutaneous needle aspirations, serial bursal fluids were cultured . The length of time necessary to achieve culture sterility with antibiotic therapy (an average of 4 days in 25 patients) was correlated with the duration of symptoms prior to diagnosis (r = 0.68, P less than 0.001) . In patients treated within 2 weeks from onset of symptoms, bursal fluid sterility was achieved within 1 week of therapy, while longer duration of symptoms was associated with delayed response . When antibiotic therapy was continued for 5 additional days after documented culture sterility, all 19 patients in the prospective trial were cured (average followup period of 6.8 months) . In septic bursitis, the effects of delay in treatment are deleterious by prolonging culture-positivity despite adequate antibiotic therapy . By analogy, delay in treatment of septic arthritis may result in the persistence of an adverse environment which can lead to further articular damage . After accurate diagnosis of septic bursitis, a therapeutic approach consisting of prompt and appropriate antibiotic usage, frequent needle drainage, and treatment duration based on the culture results of serial aspirations is effective and may be applicable in the management of certain nongonococcal bacterial joint infections.

Am J Hosp Pharm, 1981 Jul, 38(7), 1034 - 5
Treatment of antibiotic-associated pseudomembranous colitis with metronidazole; Johnson TA et al.; A case of successful treatment of antibiotic-associated pseudomembranous colitis with oral metronidazole is reported . A 67-year-old man developed diarrhea shortly after a 10-day course of oral ampicillin . His diarrhea, consisting of 10 to 12 loose stools a day, had continued for approximately two weeks and was accompanied with abdominal cramping, fever, anorexia, and weight loss . Stool specimen was streaked with blood . Proctoscopic examination revealed a spotty mucous exudate . Rectal biopsy analysis was consistent with pseudomembranous colitis . Metronidazole was initiated at a dose of 500 mg orally three times daily and continued for 10 days . By the third day, the patient was having one bowel movement daily . Proctoscopic examination after 10 days of therapy showed marked improvement with no evidence of pseudomembranous exudate . One month later the patient remained symptom-free.

Antibiotiki, 1981 Jul, 26(7), 546 - 9
{Immunodepressive action of anthracycline antibiotics studied on 2 different transplantation immunity models}; Liashenko VA et al.; The effect of carminomycin and rubomycin in equitoxic doses on the reaction of rejection of the allogenic skin graft and the reaction of the transplant to the host in mice (RTAH) was studied . Carminomycin significantly hampered the rejection of the skin graft and under certain conditions prevented development of the RTAH which indicated suppression of the formation of the clone of the immune T-killers . Rubomycin almost did not hamper the rejection of the skin graft and had no effect on the RTAH which indicated the absence of the selective effect on the system of K-killers . Carminomycin eliminated the RTAH only when it was administered to the recipients of the allogenic lymphoid cells 24 hours after implantation of the cells to the mice treated with cyclophosphamide . When carminomycin was administered to the donors of lymphoid cells 24 hours before the beginning of the experiment, it did not suppress the ability of the cells from these donors to induce the RTAH . Therefore, its effect was directed to the precursors of T-killers activated in the host of the allogenic recipient.

Ann Surg, 1981 Jul, 194(1), 51 - 6
Effectiveness of steroid/antibiotic treatment in primates administered LD100 Escherichia coli; Hinshaw LB et al.; Early aggressive therapy with maintenance infusions of methylprednisolone sodium succinate and gentamicin sulfate significantly increases the probability for survival of baboons given LD100 Escherichia coli . The present study was designed to determine if baboons would recover when initiation of treatment was delayed until they had sustained E . coli-induced systemic hypotension for a period of approximately three hours . Sixteen adult baboons were each administered a two-hour infusion of LD100 E . coli . All eight untreated animals died within 42 hours . Five of the eight baboons treated after approximately three hours of hypotension with methylprednisolone sodium succinate and gentamicin sulfate survived . Treated animals had significantly higher blood glucose and insulin levels and lower blood urea nitrogen concentrations than baboons receiving E . coli alone . E . coli blood concentrations were lower in the treated than in the untreated baboon group by the sixth hour (less than 0.02) . Heart rates increased in all animals but were not as high in the treated baboons . Both groups experienced similar decreases in mean systemic arterial pressure, PCO2, base excess, leukocyte, lymphocyte, and platelet concentrations, and increases in creatinine and lactate concentrations . Data from the present study indicate that the probability of recovery from shock is significantly increased even when initiation of steroid/antibiotic therapy is postponed until baboons have experienced sustained systemic hypotension.

Clin Chem, 1981 Jul, 27(7), 1190 - 7
Fluorescence polarization immunoassay . I . Monitoring aminoglycoside antibiotics in serum and plasma; Jolley ME et al.; Fluorescence polarization immunoassays of the aminoglycoside antibiotics gentamicin, tobramycin, and amikacin in plasma and serum are described and shown to be clinically useful . The aminoglycoside tracers were prepared by reacting the parent compounds with 5-{(4,6-dichlorotriazin-2-yl)-amino} fluorescein . Antisera specific for the compounds were raised in rabbits by conventional procedures . Tracer, sample, and diluted antiserum are combined and, after a 15-min incubation at ambient temperature, the polarization of the fluorescence of the tracer is determined in a specially designed fluorometer . The assays are designed to give accurate trough (i.e., minimum during therapy) values and to be free of matrix effects . Severely icteric samples may interfere, but this can be overcome by blank subtraction . The performance of the assays with clinical specimens compared favorably with that of some commercially available assays.

Antibiotiki, 1981 Jul, 26(7), 483 - 8
{New antitumor antibiotics 5590 and 2928}; Gauze GF et al.; Antibiotics with an in vivo antiblastomic activity were isolated from the actinomycetous culture 5590 and 2928 . The antibiotics were prepared in the crystalline form . The conditions for the biosynthesis of the antibiotics, their physicochemical constants and UV and IR spectra were determined . The acid hydrolysates of the antibiotics were studied . The antibiotics contained the same chromophore and different sets of amino acids . Antibiotics 5590 and 2928 were classified as peptides containing the chromophore group.

Antibiotiki, 1981 Jul, 26(7), 522 - 6
{Role of sterols in the interaction of polyene antibiotics with lipid membranes}; Feigin AM et al.; The problem whether the membrane sterols are indirect acceptors of polyenic antibiotics or they play the role of substances providing conditions (at the expense of putting in order the membrane phospholipids) for formation of conductive complexes (ionic canals) from the antibiotic molecules is discussed . The comparative study on the ability of sterols of various structure (ergosterol, 7-dehydrocholesterol, cholesterol, 5 alpha-cholestan-3 beta-ol) to interact with the membrane phospholipids and to increase the sensitivity of such membranes to amphotericin B showed no correlation between the levels of these properties . The value of the changes in the cross elasticity module (E) of artificial bilayer lipid membranes from egg lecithin on introduction of the above sterols into their composition was used as the criterion for the interaction level . The absence of correlation between the above properties of the sterols indicated that the role of the sterols in interaction of polyenic antibiotics with the membranes could not be considered as the only effect of the sterols on putting in order the phospholipids, which confirmed the hypothesis on the acceptor function of the sterols with respect to polyenic antibiotics . The study of the effect of amphotericin B on the elastic properties of the cholesterol-containing bilayer membranes isolated from egg lecithin showed tha the values of the longitudinal and cross elasticity modules of the membranes did not change during introduction into the membranes of the ionic canals.

Am J Surg Pathol, 1981 Jul, 5(5), 507 - 16
Electron microscopy in the long-term follow-up of Whipple's disease . Effect of antibiotics; Denholm RB et al.; The electron-microscopic and light-microscopic findings on jejunal biopsies from a case of Whipple's disease are described . Seven biopsies were obtained over a 3-year period . Rapid clinical recovery was accompanied by the disappearance of interstitial and intracellular bacteria from the lamina propria . The pathognomonic PAS-positive material on light microscopy corresponding to the phagocytic vacuoles in the macrophages of the lamina propria decreased markedly in amount but persisted throughout the 3-year-period . The sequential changes in the jejunal mucosa and in particular those occurring in macrophages are described and their relation to pathogenesis is discussed.

Biochim Biophys Acta, 1981 Jun 22, 644(2), 369 - 72
Potential-dependent formation of single conducting ion channels in lipid bilayers induced by the polyene antibiotic levorin A; Kasumov KM et al.; The aromatic polyene antibiotic levorin A2 forms ion channels permeable to monovalent cations, in lipid membranes containing cholesterol or ergosterol . Channel conductivity is in the range 0.3-0.5 pS . The channel has two main states: conducting (open) and nonconducting (closed) . The potential-dependent formation of levorin A2 channels is observed in lipid membranes . The system responsible for the ion-channel selectively is localized on the hydrophilic side of the lactone ring of the polyene molecule.

Fortschr Med, 1981 Jun 11, 99(22), 864 - 8
{Effect of a fibrin-antibiotic compound in bone and soft tissue infections}; Ulatowski L et al.; It is reported on experimental experiences in the use of a biological adhesive system--highly concentrated native fibrinogen, thrombin and clotting factor XIII--in conjunction with local antibiotics . The results in animals are: Antibiotics in conjunction with the mentioned adhesive system give a high local concentration for a short time . The activity of the antibiotics decreases quickly within some activity of the antibiotics decreases quickly within some hours, there is no more antibiotic effect after 36 hours.

J Antibiot (Tokyo), 1981 Jun, 34(6), 719 - 26
Macrolide antibiotics M-4365 produced by Micromonospora . IV . Antimycoplasmal activity of antibiotic M-4365 G2 (de-epoxy rosamicin); Onta T et al.; In vitro activities of M-4365 G2, a new basic 16-membered macrolide antibiotic, against a total 19 strains including human, bovine, porcine, rodent, avian and saprophytic mycoplasmas were compared with those of three other macrolide antibiotics, josamycin, erythromycin and tylosin . M-4365 G2 exhibited stronger activities than the other macrolide antibiotics against 11 strains of mycoplasma tested . Especially, its higher activities against M . pneumoniae Mac and FU, U . urealyticum T-960, M . mycoides PG-1 and M . gallisepticum Kp-13, PG-31 and 9-49A were to be noticed (final minimum inhibitory concentrations: 0.0001 approximately 0.049 microgram/ml) . Higher antimycoplasmal activity of M-4365 G2 than that of tylosin was also proved in experimental treatment of chickens intranasally inoculated with M . gallisepticum Kp-13 by feeding a diet containing the drug . M . gallisepticum Kp-13 was not isolated from the infected chickens fed a diet containing 0.0063% or more of M-4365 G2.

J Antibiot (Tokyo), 1981 Jun, 34(6), 675 - 80
Studies on neplanocin A, new antitumor antibiotic . II . Structure determination; Hayashi M et al.; The structure and stereochemistry of neplanocin A was determined on the basis of its spectral and chemical evidences as {1R-(la,2a,3b)}-3-(6-amino-9-yl)-5-(hydroxy-methyl)-4-cyclopentene-1,2-diol . For the final proof of the structure, X-ray crystallographic analysis of neplanocin A was carried out.

Antibiotiki, 1981 Jun, 26(6), 441 - 4
{Determination of the biological activity of aminoglycoside antibiotics on a dry nutrient medium of Soviet manufacture}; Grigor'eva VM et al.; Possible use of the dry nutrient medium manufactured in the USSR for the assay of aminoglycoside antibiotic activity with the agar diffusion method was studied . The optimal conditions for the antibiotic activity assay on this medium were developed . The dry nutrient medium may be used for the activity assay of the aminoglycoside antibiotics, i . e . streptomycin sulfate, dihydrostreptomycin sulfate, neomycin sulfate, monomycin and gentamicin sulfate.

Antibiotiki, 1981 Jun, 26(6), 427 - 31
{Acid-base properties of the polyene antibiotic nystatin}; Travkin OV et al.; The acid-base properties and transformation of nystatin in water, methanol, 80 per cent ethanol, 70 per cent propanol and 70 per cent dimethylsulfoxide were studied . The data are indicative of a significant difference in the protolytic properties of the antibiotic in various solutions . Nonreversible conformative conversions of nystatin in water and methanol not connected with the loss of the antibiotic activity were observed . It is suggested that the molecule of nystatin in the above solutions could be in 3 main states, i . e . inert native and activated . The results of the study may be of use in development of the schemes for isolation of nystatin from the mycelium preparation of some of its water soluble forms.

Antibiotiki, 1981 Jun, 26(6), 414 - 9
{Polyene antibiotic solubilization by bile acid salts in aqueous solutions}; Etingova NI; The process of solubilization of polyenic antibiotics, such as amphotericin B, mycoheptin, levorin and nystatin in aqueous solutions of sodium salts of bile acids: desoxycholic, cholic and dehydrocholic was studied . It was shown that amphotericin B and mycoheptin had the highest capacity for solubilization . No solubilization of the antibiotics was observed in the solutions of sodium dehydrocholate . Thermodynamic estimation of the solubilization process with sodium desoxycholate is presented.

Br J Pharmacol, 1981 Jun, 73(2), 535 - 47
Antibiotic-associated colitis: an in vitro investigation of the effects of antibiotics on intestinal motility; Lees GM et al.; 1 Nine antibiotic compounds in common use were studied to determine their ability to affect intestinal motility in vitro, in the guinea-pig ileum and rabbit colon . 2 Ampicillin, doxycycline, mecillinam and metronidazole were without effect over a concentration range which included typical serum levels found when these drugs are used therapeutically . 3 Clindamycin, gentamicin, kanamycin, pivmecillinam and trimethoprim were all found to inhibit evoked and reflex responses of the guinea-pig ileum but only clindamycin and trimethoprim also affected evoked responses of the rabbit colon . 4 Kanamycin and gentamicin appeared to have a predominantly pre-junctional action, pivmecillinam and trimethoprim a predominantly post-junctional action . Clindamycin had a pre-junctional action at low concentrations and long exposure times, and a post-junctional action at high concentrations and short exposure times . 5 The concentration of each antibiotic required to inhibit the peristaltic reflex of the guinea-pig ileum was less than that required to inhibit its responses to electrical stimulation or exogenous acetylcholine or histamine but greater than the serum levels associated with their respective use in therapeutic doses . 6 A sequence of events whereby antibiotic-induced alterations in gastro-intestinal motility could lead to the development of pseudomembranous colitis is proposed.

J Antibiot (Tokyo), 1981 Jun, 34(6), 701 - 7
Gilvocarcins, new antitumor antibiotics . 3 . Antitumor activity; Morimoto M et al.; Gilvocarcin V, isolated rom a Streptomyces culture showed activity against experimental tumors such as sarcoma 180, Ehrlich carcinoma, Meth 1 fibrosarcoma, MH134 hepatoma and lymphocytic leukemia P388 . In particular, 40% of treated mice survived for 60 days, after intraperitoneal administration of gilvocarcin V to mice bearing Ehrlich ascites carcinoma . But it was marginally active against B16 melanoma and did not produce prolongation of lifespan of mice bearing Lewis lung carcinoma.

Vet Med (Praha), 1981 Jun, 26(6), 367 - 77
{The effect of the non-antibiotic growth stimulators, Carbadox and Cyadox, on reproduction in laboratory animals}; Sykora I et al.; The effect of growth stimulators Carbadox and Cyadox was studied in laboratory rats and mice as exerted on their fertility, gravidity, embryo ontogenesis, and genetic efficacy of these drugs was also tested . In all tests one dose approaching the dose used in practice and multiple doses were administered . No antifertility effects were observed in either sex of rats, slight reduction in fertility was found in treated male mice . No teratogenic effect was observed, but both stimulators acted highly embryotoxically . Irrespective of the dose, genetic hazard occurred, influencing the first stages of spermatogenesis (spermatogony), and increasing the incidence ob abnormalities of spermatozoon heads after Carbadox treatment . In all tests Cyadox was less harmful than Carbadox . The results show that it is somewhat hazardous to use both growth stimulators in the period of animal reproduction.

J Antibiot (Tokyo), 1981 Jun, 34(6), 758 - 62
Studies on protein binding of antibiotics . III . Effect of novobiocin on protein binding and pharmacokinetics of cefoperazone and cefazolin; Watanabe Y et al.; The drug-protein interactions between cefoperazone (CPZ) and novobiocin (NB), and between cefazolin (CEZ) and NB were investigated . Though there was a remarkable reduction of CPZ or CEZ binding to rabbit serum and human serum albumin with increases in drug concentrations above 3.0x10-4M (CPZ: 200 microgram/ml, CEZ: 140 microgram/ml), NB binding was not affected . In addition, when CPZ or CEZ was added to the NB solution, NB binding was not altered and remained above 90% . Therefore, it was evident that NB had a high capacity for binding to protein, compared with CPZ or CEZ . From the competitive study, the main binding site of NB to protein appeared to differ from that of CPZ or CEZ . The CPZ or CEZ serum levels in rabbits for the simultaneous adminstration of NB were significantly higher than those for the control experiments, however, the NB serum levels were not greatly affected by CPZ or CEZ.

J Antibiot (Tokyo), 1981 Jun, 34(6), 753 - 7
Studies on protein binding of antibiotics . II . Effect of apalcillin on protein binding and pharmacokinetics of cefoperazone and cefazolin; Watanabe Y et al.; The drug-protein interactions between cefoperazone (CPZ) and apalcillin (APPC), and between cefazolin (CEZ) and APPC were investigated in in vitro and in vivo experiments . Through the binding rates of CPZ or CEZ to rabbit serum and human serum albumin subsided remarkably with increased drug concentrations, APPC was not greatly affected, even at high concentrations . It appeared that APPC had a higher binding capacity to protein than CPZ or CEZ . From the results of competitive study, it became clear that APPC partially shared the binding sites on protein with CPZ or CEZ . The CPZ or CEZ serum levels in rabbits administered together with APPC were not different from those for the single administration, but APPC levels for the simultaneous administration were slightly lower.

J Antibiot (Tokyo), 1981 Jun, 34(6), 708 - 12
Interaction of cytotoxic antibiotic dactylarin with glycolytic thiol enzymes in Ehrlich ascites carcinoma cells; Sturdik E et al.; Cytotoxic effect of dactylarin on Ehrlich ascites carcinoma cells is caused by the inhibition of some SH-dependent glycolytic enzymes, especially of hexokinase (EC 2.7.1.1), glyceraldehyde-3-phosphate dehydrogenase (EC 1.2.1.12) and 6-phosphofructokinase (EC 2.7.1.11) . Dactylarin interacts with thiols, which explains its inhibitory effectiveness on the above glycolytic enzymes.

Proc Natl Acad Sci U S A, 1981 Jun, 78(6), 3333 - 7
Hydrogen bonding, overlap geometry, and sequence specificity in anthracycline antitumor antibiotic.DNA complexes in solution; Patel DJ et al.; We have deduced structural aspects of the intercalation complex of the anthracycline antitumor antibiotic daunomycin and its analogs with the synthetic DNA poly(dA-dT) by 1H and 31P NMR in high-salt solution . We demonstrate that the base pairs are intact at the antibiotic binding site and that the anthracycline phenolic hydroxyls form intramolecular hydrogen bonds with the quinone carbonyls and are shielded from solvent in the intercalation complex . The complexation shifts of the exchangeable phenolic and nonexchangeable aromatic protons demonstrate that rings B and C of the anthracycline chromophore overlap with adjacent base pairs, while anthracycline ring D passes right through the intercalation site in the complex . We observe two resolved 31P resonances attributable to the dA-dT and dT-dA phosphodiester linkages in the phosphorus spectra of the neighbor-exclusion daunomycin.poly(dA-dT) complex . This suggests that the anthracycline antitumor antibiotic exhibits a sequence specificity in its intercalation complex with alternating purine-pyrimidine synthetic DNAs in solution . These conclusions on hydrogen bonding and overlap geometry at the intercalation site and sequence specificity for the daunomycin.poly(dA-dT) complex in solution are in agreement with the structure of the daunomycin.dC-dG-dT-dA-dC-dG hexanucleotide duplex crystalline complex at atomic resolution published recently {Quigley, G . J., Wang, A . H.-J., Ughetto, G., van der Marel, G., van Boom, J . H . & Rich, A . (1980) Proc . Natl . Acad . Sci . USA 77, 7204-7208}.

Eur J Biochem, 1981 Jun, 117(1), 27 - 31
Effects of antibiotics, N-acetylaminoacyl-tRNA and other agents on the elongation-factor-Tu dependent and ribosome-dependent GTP hydrolysis promoted by 2'(3')-O-L-phenylalanyladenosine; Campuzano S et al.; GTP hydrolysis on elongation factor (EF) Tu . ribosome complexes has been assayed in the presence of 2'(3')-O-L-phenylalanyladenosine (AdoPhe), i.e . the 3'-terminal portion of Phe-tRNAPhe . Several requirements of the reaction have been characterized . Maximal activity is observed at 60-120 mM NH4Cl and 5-15 mM magnesium acetate . The reaction requires the free sulfhydryl group of EF-Tu normally implicated in aminoacyl-tRNA binding . Intact EF-Tu cannot be replaced by a large tryptic fragment of EF-Tu (Mr 39,000) that retains the ability to bind guanosine nucleotides . The aminoglycoside antibiotics, neomycin C and several kanamycins and gentamicins, stimulate the AdoPhe-promoted GTPase . Surprisingly, however, other closely related antibiotics, like neomycin B, paromomycin and ribostamycin, are ineffectual, thus indicating subtle differences in the actions of these antibiotics . AcPhe-tRNAPhe, bound to the ribosomal A-site, stimulates the AdoPhe-promoted GTPase, but this compound or AcTyr-tRNATyr, present in unbound form, strongly inhibits the reaction . These results suggest that N-blocked aminoacyl-tRNAs form ternary complexes with EF-Tu . GTP, which have not been previously detected because of their low stability.

Cancer, 1981 May 15, 47(10), 2422 - 9
Protected environment - prophylactic antibiotic program for malignant sarcomas: randomized trial during remission induction chemotherapy; Bodey GP et al.; Fifty-one valuable patients with malignant sarcomas were randomly allocated to receive three courses of remission induction chemotherapy with cyclophosphamide, vincristine, Adriamycin, and dimethyl triazeno imidazole carboxamide (CYVADIC) on the protected environment-prophylactic antibiotic for the control group (P = 0.22) . The response rates (complete plus partial) were 71% and 67%, respectively . The durations of response were similar for both groups of patients, but the PEPA patients survived substantially longer (median, 84 weeks vs . 58 weeks) . The frequency of infection was significantly lower among the PEPA patients, and the doses of CYVADIC could be escalated more often among these patients . Dosage escalation was associated with a higher complete remission rate and lower fatality rate.

Sem Hop, 1981 May 8-15, 57(17-18), 909 - 11
{Parietal complications of cholecystectomy : results of prophylactic antibiotic therapy with cefazoline (author's transl)}; Mourot N et al.; Patients undergoing cholecystectomy were randomly divided into two groups . The effects of a single injection of one gram of cefazoline given thirty minutes before operation to 30 patients were compared with those obtained in a second group of 29 untreated cases . The efficiency of the second generation cephalosporins in preventing postoperative complications of this type was confirmed . Prophylactic administration of this antibiotic therapy before uncomplicated biliary tract surgery can significantly reduce the incidence of postoperative parietal infections and therefore the duration of hospitalization.

Thorax, 1981 May, 36(5), 330 - 7
Homograft aortic valve replacement: seven years' experience with antibiotic-treated valves; Khanna SK et al.; One hundred and sixty-five patients had their aortic valve replaced with antibiotic-sterilised homograft . In all cases, a two-layered freehand technique of valve implantation was used . Tailoring (narrowing) of the annulus was required in 29 cases, and an aortic root gusset was used to enlarge the non-coronary sinus in 68 cases . There was an early mortality of 1.8% and late mortality of 2.4% . The actuarial survival rate was 95% at a maximum follow-up of seven years . The incidence of valvar regurgitation (early diastolic murmur) was 11.5% up to six months after operation and an additional 7.2% subsequent to this . Overall, it was trivial in 10.3%, mild in 7.8%, and moderate in 0.6% . Most valve regurgitation was non-progressive and actuarial analysis showed 74% regurgitation-free valves at the end of seven years . The age of the donor and the valve storage time showed some relationship to valve deterioration . Special attention has been paid to the control of hypertension to prevent accelerated graft degeneration . The results suggest that this has been successful . Anticoagulant therapy was not used and thromboembolism has not been seen in patients undergoing isolated aortic valve replacement . There was one case of miliary tuberculosis after homograft valve replacement but no pyogenic or fungal endocarditis occurred . No haemolysis, calcification, or valvar stenosis were observed . This series, followed for a maximum of seven years, shows excellent sustained valve performance and a very low incidence of important postoperative regurgitation, with 91.8% of the survivors symptom-free.

Am J Hosp Pharm, 1981 May, 38(5), 692 - 5
Computer-assisted antibiotic use review; Klapp D et al.; The use of a computer system for an antibiotic review program is described . A commercial system was selected as the software base for the development of the antibiotic use review (AUR) program . The AUR system is composed of three parts: (1) editing and verifying data from the patient's pharmacy profile card, (2) updating the data base, and (3) generation of reports . The system is flexible in its reporting capabilities . Potential functions of the system include identifying patterns of bacterial resistance . The computer system is an efficient tool for the clinical review of antibiotic use in a quality assurance program.

Am J Otolaryngol, 1981 May, 2(2), 123 - 8
The effects of cricoid cartilage injury and antibiotics in cricothyroidotomy; Koopmann CF Jr et al.; Until recent years cricothyroidotomy has been condemned as an elective surgical procedure because of reports of a high incidence of subglottic stenosis . In this study of cricothyroidotomy the effects of trauma, denudation of the mucous membrane of the anterior half of the cricoid cartilage, and the prophylactic administration of antibiotics (ampicillin) on the development of subglotttic airway narrowing were evaluated in 40 mongrel dogs . Two of the dogs developed minimal anterior narrowing of the airway . None of the dogs developed clinically important stenosis.

Antibiotiki, 1981 May, 26(5), 345 - 9
{Sensitivity of actinomycetes of the genus Actinomadura to antibiotics}; Terekhova LP et al.; Sensitivity of 46 strains of Actinomadura representing 27 species was studied with respect to 7 antibiotics . The minimum inhibitory concentrations of the antibiotics with respect to various species of Actinomadura varied within wide ranges, i . e . from 0.1 to 100 micrograms/ml, except levorin, and antifungal antibiotic which did not inhibit the growth of any of the strains even in the highest concentration (100 micrograms/ml) . The cultures of the "dassonvillei" type proved to be the most sensitive to the antibiotics . Their sensitivity spectra were very close to those of Norardiopsis dassonvillei . A . carminata, an organism producing carminomycin, was most resistant to the antibiotics . Kanamycin, streptomycin, rifampicin, olivomycin and bruneomycin inhibited the growth of some Actinomadura species even in very low concentrations (1/2 g/ml) and thus may be used for selective screening only of definite Actinomadura species . The Actinomadura cultures were most resistant to rubomycin . All of the Actinomadura strains produced satisfactory growth on media containing this antibiotic in concentrations up to 10 micrograms/ml . Rubomycin in concentrations nor higher than 10 micrograms/ml is recommended to be used for isolation of Actinomadura cultures from soil samples.

Methods Find Exp Clin Pharmacol, 1981 May-Jun, 3(3), 173 - 7
Inhibition of the pendular movements of the intestine by aminoglycoside antibiotics; Paradelis AG; In the present study the inhibitory effect of eight aminoglycoside antibiotics on the motility of the rabbit's intestine was investigated . We found that all the antibiotics tested exert inhibitory effect on the motility of the intestine and only quantitative differences exist between them . The inhibitory potency of the antibiotics appears to be as follows: gentamicin greater than amikacin greater than streptomycin greater than sisomicin greater than kanamycin greater than kanendomycin greater than dibekacin greater than tobramycin . The inhibitory effect of the above antibiotics is not exerted through the adrenergic receptors because this effect is also observed after the previous administration of alpha and beta adrenergic receptor blocking agents . Neostigmine is not able to restore the normal motility of the relaxed intestine . The normal pendular movements of the intestine are restored by calcium.

Br J Surg, 1981 May, 68(5), 314 - 5
Penetration of a prophylactic antibiotic into peritoneal fluid; Corbett CR et al.; The ability of an antibiotic, given for prophylaxis, to enter the peritoneal fluid was measured in 40 patients having abdominal operations . Cefuroxime, the antibiotic studied, attained a satisfactory level (4 mg/1) in the peritoneal fluid of 34 of the 40 patients (85 per cent) . There was no difference between emergency and elective operations, suggesting that peritoneal inflammation does not enhance the penetration of cefuroxime into peritoneal fluid.

Antimicrob Agents Chemother, 1981 May, 19(5), 891 - 900
Murein synthesis and beta-lactam antibiotic susceptibility during rod-to-sphere transition in a pbpA(Ts) mutant of Escherichia coli; Botta GA et al.; The conditional morphology mutant of Escherichia coli SP45 grows as a rod at 30 degrees C and assumes a spherical shape after 90 min of incubation at 42 degrees C . The rod-to-sphere morphological transition has been found to be associated with the disappearance of penicillin-binding protein 2 (PBP-2), the progressive reduction (as much as 50%) of murein synthesis, as measured both in intact cells and ether-permeabilized bacteria, and alterations in the structure of the cell envelope, including detachment of the outer membrane from the underlying structures . The detachment was initially localized at the poles of the cells and then spread over the entire surface . Shape transition was also linked to increased susceptibility to beta-lactam antibiotics which preferentially bound to PBP-1A (cephalothin, cephaloridine) or to PBP-3 (furazlocillin, piperacillin) . Treatment with beta-lactams possessing a high affinity for PBP-1A, although inducing a low degree of peptidoglycan synthesis inhibition (5 to 10%), was associated with a marked loss of cell viability and massive lysis . On the other hand, the simultaneous absence of PBP-2 and inhibition of PBP-3 causes a significant reduction of peptidoglycan synthesis, yet only slightly affected cell viability . Whereas PBP-1A inhibition during shape transition had no effect on morphology, addition of antibiotics binding to PBP-3 30 min after the temperature shift-up caused formation of elongated cells with a centrally located bulge, not observed in similarly treated cells grown at 30 degrees C . Inhibition of PBP-3 in round cells 90 min after temperature shift caused formation of giant cells, indicating complete loss of elongation ability . The different effects of the simultaneous inhibition of two PBPs, combining mutational loss with specific binding in vivo of another PBP by beta-lactams, provide new insight into the role of these proteins and the killing mechanisms of this class of antibiotics.

Jpn J Antibiot, 1981 May, 34(5), 734 - 46
{General pharmacological studies on a new macrolide antibiotic, miokamycin (MOM) . 1 . Effects on the central nervous system (author's transl)}; Shibata U et al.; Behavioral and electroencephalographic (EEG) effects on a new macrolide antibiotic miokamycin (MOM), 9,3"-diacetylmidecamycin, were investigated in mice, rats and rabbits after oral administration . MOM caused a decrease in the spontaneous motor activity, a slight increase in the effect of megibal seizure at a dose of 1,000 mg (Potency)/kg, and an increase in the number of deaths on the maximal electroshock seizure after administration of doses more than 100 mg (Potency)/kg . Even at a dose of 1,000 mg (Potency)/kg, however, MOM showed no effects on general behavior, rectal temperature, traction test, inclined screen test, rotarod performance, thiopental-induced sleep, pentetrazol seizure, fighting behavior induced by electric stimulation and conditioned avoidance response . EEG effects in unanesthetized rabbits with permanent electrode implants were studied . MOM showed no effects on spontaneous EEG, arousal response to mesencephalic reticular stimulation, photic driving response, evoked cortical response by ventralis posterolateralis stimulation and afterdischarge elicited by hippocampal stimulation at a dose of 1,000 mg (Potency)/kg . Consequently, it can be concluded that MOM has no specific pharmacological effects on the central nervous system . Behavior effects of MOM metabolisms, Mb-1, Mb-2, Mb-6 an Mb-12, were almost the same as those of MOM in the mode of action.

Hosp Med Staff, 1981 May, 10(5), 19 - 24
A blueprint for antibiotic utilization review; Leist ER; Antibiotic usage recently has come under careful scrutiny because of its impact upon hospital costs and its effect upon patient care . This article describes the antibiotic utilization review program developed at Norton-Children's Hospitals, Louisville, to improve antibiotic prescribing and to meet the requirements of the Joint Commission on Accreditation of Hospitals.

J Biol Chem, 1981 Apr 10, 256(7), 3175 - 7
Spectrophotometric and kinetic studies on the interaction of antibiotic X5108, the N-methylated derivative of kirromycin, with elongation factor Tu from Escherichia coli; Eccleston JF; The absorption spectrum of antibiotic X5108, the N-methylated derivative of kirromycin, has been found to be decreased in intensity on binding to elongation factor (EF)-Tu . GDP, EF-Tu . GTP, and nucleotide-free EF-Tu . This has allowed the binding of X5108 to be studied directly . In agreement with previous studies, a 1:1 stoichiometry is observed, with a dissociation constant of less than 1 microM . Identical results were obtained with all three EF-Tu species . The absorption spectrum of X5108 in increasing concentrations of isopropyl alcohol first intensifies and then decreases, 80% isopropyl alcohol giving the same spectrum as that of X5108 bound to EF-Tu . This result is interpreted as showing that the chromophoric moiety of X5108 is bound in a highly hydrophobic environment on EF-Tu . The rate of binding of X5108 to EF-Tu . GDP was measured using a stopped flow spectrophotometer . This rate was proportional to the concentration of X5108, giving a second order binding rate constant of 4.8 X 10(3) M-1 s-1 . Since this is several orders of magnitude too slow for a diffusion-controlled reaction, the results are interpreted based on a two-step binding process . A half-time of about 10 min is calculated for the dissociation of X5108 from EF-Tu . GDP . The fact that X5108 bound to EF-Tu is not in rapid equilibrium with X5108 free in solution needs to be considered in studies on the effect of X5108 and kirromycin on partial reactions of protein biosynthesis.

J Antibiot (Tokyo), 1981 Apr, 34(4), 390 - 402
Glysperin, a new antibiotic complex of bacterial origin . II . Structures of glysperins A, B and C; Tsuno T et al.; Structures of glysperins A, B and C were determined on the basis of chemical degradation studies in conjunction with spectroscopic analyses . Glysperin A consisted of L-alanine, p-hydroxybenzoic acid, a C11-alkyl tetramine and four sugar moieties, three of which were identified as D-ribose, D-galactose and 2,4-diamino-2,4,6-trideoxy-D-galactose . The fourth sugar was a novel exoenose, 6-deoxy-D-xylo-hex-5-enose . Structural difference between glysperins A and B resided solely in the terminal polyamine moiety which was spermidine in glysperin B . Glysperin C contained D-glucose in place of the exoenohexose moiety of glysperin A . Glysperins A, B and C are, in some respects, structurally related to the glycocinnamoylspermidine antibiotics, LL-BM 123 beta, gamma 1 and gamma 2.

J Antibiot (Tokyo), 1981 Apr, 34(4), 359 - 66
Studies on neplanocin A, new antitumor antibiotic . I . Producing organism, isolation and characterization; Yaginuma S et al.; Neplanocin A . C11H13N5O3, is a novel carbocyclic analog of adenosine with cyclopentene . It was isolated from the culture filtrate of Ampullariella regularis A11079 by means of ion-exchange, carbon, silica gel adsorption, or partition chromatography . Neplanocin A forms crystals, and is stable at acidic or alkaline pH . Neplanocin A has cytotoxicity against L5178Y cells in culture and showed a remarkable effect on the life prolongation of mice infected with L1210 leukemia.

Can J Comp Med, 1981 Apr, 45(2), 113 - 5
A comparison of the in vitro activity of two antibiotics against bovine ureaplasmas; Truscott RB; A comparison of the in vitro activity of rosaramicin and minocin against 52 bovine Ureaplasma sp . strains, 20 of which were isolated from semen, 23 from vaginal swabs, and nine from preputial washings, has shown that both antibiotics have good inhibitory action against the strains tested . Rosaramicin was ureaplasmacidal in most instances at, or close to the inhibitory level while for most strains studied a ureaplasmacidal level of minocin was not found.

Avian Dis, 1981 Apr-Jun, 25(2), 395 - 403
Resistance and cross-resistance studies with narasin, a new polyether antibiotic anticoccidial drug; Jeffers TK; The Wisconsin (Wis) strain and a field strain (FS-196) of Eimeria tenella were propagated in the presence of 80 ppm narasin in an attempt to select for narasin resistance . Comparisons of the narasin sensitivity of the selected strains (Wis-NR and FS-196-NR) and of the parent strains (Wis and FS-196) from which they were derived revealed no resistance development . These findings agree with the results of similar studies with the polyether antibiotic anticoccidial drugs monensin and lasalocid and support the conclusion that chicken coccidia do not readily develop resistance to this class of anticoccidial drugs . In a separate series of experiments, the efficacy of narasin was evaluated against five E . tenella field strains, one each resistant to amprolium, clopidol, decoquinate, nicarbazin, and robenidine . Narasin effectively controlled infections that were inadequately controlled by the anticoccidial drugs to which the strains were resistant . There was no evidence of cross-resistance to narasin.

Antibiotiki, 1981 Apr, 26(4), 243 - 6
{A new antibiotic, corallomycin, from an Act . longispororuber}; Frolova VI et al.; A new antibiotic named corralomycin (C34H28O9) was isolated from the mycelium of culture 6795-38 classified as belonging to Act . longispororuber . The maximum UV absorption spectra of the antibiotic in an alcohol solution were observed at the wavelengths of 228, 268 and 420 nm, the absorption bonds of 3400, 2980, 2865, 1710, 1625, 1595, 1165, 880 and 780 cm(-1) were recorded in the IR spectrum . Two acetyl derivatives of corallomycin, i.e . diacetate (C38H32O11) and tetraacetate (C42H36O13) were prepared.

Dis Colon Rectum, 1981 Apr, 24(3), 198 - 200
Antibiotic-associated colitis with normal-appearing rectum; Burbige EJ et al.; A patient was recently seen with pseudomembranous colitis . He had severe disease of the proximal colon, with normal-appearing rectum and distal sigmoid, three weeks after administration of prophylactic antibiotics for surgery . The patient improved after discontinuing the antibiotics . Fiberoptic colonoscopy should be performed in patients suspected of having pseudomembranous colitis, even when sigmoidoscopy results are normal.

Ann Emerg Med, 1981 Apr, 10(4), 187 - 92
Use of antibiotics in the initial management of soft tissue hand wounds; Haughey RE et al.; A prospective, randomized study was undertaken to determine the efficacy of prophylactic antibiotics in the treatment of various types of soft tissue hand wounds . A total of 394 patients were randomly assigned to one of two treatment groups, those receiving cephalexin (250 mg orally q.i.d . x 5 days), and the control group receiving no antibiotic . Patients were followed closely during the healing phase of their wounds . There was no statistical difference in the incidence of infection in the two groups.

Arch Dermatol . 1981 Apr;117(4):189.
Antibiotics and oral contraceptives; Rubin DF; PIP: Dermatologists often prescribe oral tetracycline for the control of acne, primarily, and to a much lesser extent, for the treatment of cutaneous infections . A number of the patients taking tetracycline are also taking birth control pills . A recent article in the British Medical Journal (1980;1:293) indicates that this combination can lead to a failure of the (OC) oral contraceptive . Such failure had been associated with ampicillin as well . It is believed that the mechanism for this was the disturbance in normal gut flora, with consequent effects on bacterial hydrolysis of steroid conjugates . This would interrupt the enterohepatic circulation of contraceptive steroids, resulting in a less than normal concentration of circulating steroids . It was recommended that women taking low-dose OCs take extra precautions against pregnancy during any cycle in which antibiotics are given . In regard to our care of and responsibilities to our patients, and in an era when malpractice suits for all types of reasons are more common, it certainly behooves dermatologists to recognize and be concerned about this potential consequence of prescribing oral antibiotics .

Ugeskr Laeger, 1981 Mar 30, 143(14), 881 - 3
{Prophylactic antibiotic therapy in induced abortion . A cost benefit analysis}; Sonne-Holm S et al.; PIP: The Danish national social expense/annum of 25,000 terminations of pregnancy was calculated to equal 135 million Danish crowns in 1979 (11 million pounds) . If prophylactic penicillin/ampicillin treatment is introduced in the treatment of women who had previously had genital infections, 7 million Danish crowns could be saved annually (approximately 580,000 pounds) based on a clinically controlled investigation of the effect of prophylactic antibiotic therapy . To this must be added the savings in expenses for treating secondary infertility and other sequelae of postabortion infection . These calculations are associated with considerable uncertainty because of poorly defined information on the basic economy . (author's)

Am J Obstet Gynecol, 1981 Mar 15, 139(6), 693 - 6
Prophylactic antibiotics in first-trimester abortions: a clinical, controlled trial; Sonne-Holm S et al.; PIP: The efficacy of prophylactic antibiotic therapy in induced first trimester abortions was investigated in a double-blind study . Of the 493 women in the study, 254 received dosed of 2 million IU of penicillin G intermuscularly 1/2 hour before and 3 hours after the procedure, followed by 350 mg of pivampicillin 3 times daily for 4 days, and 239 women received corresponding doses of placebo . The incidence of pelvic infectious complications was 5.5% in the treated group and 10.9% in the control group (P=0.05) . The difference could be attributed to a selective prophylactic effect in women who had earlier suffered from (PID) pelvic inflammatory disease (N=105) . The rate of infection in this group was 22.4% among those receiving placebo and 2.1% among those receiving antibiotics (P=0.006) . Prophylactic administration of antibiotics for first trimester abortions should be used in women who have earlier had PID .

JAMA, 1981 Mar 13, 245(10), 1055 - 6
Prophylactic antibiotics in simple hand lacerations; Grossman JA et al.; A randomized prospective study of 265 patients with hand lacerations was carried out to define the role of prophylactic antibiotics in the management of simple, sutured wounds of the hand . Two hundred sixty-five patients were followed up until suture removal or satisfactory wound healing . There were a total of three infections (1.1%) . There was no noticeable differences in the incidence of infection in the antibiotic and placebo treatment groups . It is concluded that prophylactic antibiotics are an unnecessary adjunct in the treatment of simple lacerations of the hand and no replacement for meticulous wound management.

J Biol Chem, 1981 Mar 10, 256(5), 2162 - 7
Binding of saframycin A, a heterocyclic quinone anti-tumor antibiotic to DNA as revealed by the use of the antibiotic labeled with {14C}tyrosine or {14C}cyanide; Ishiguro K et al.; Saframycin A is antitumor antibiotic structurally characterized by twin heterocyclic quinone skeletons and alpha-cyanoamine moiety . The binding of saframycin A to DNA was investigated using the antibiotic labeled at different positions . Heterocyclic quinone skeletons were biosynthetically labeled with {14C}tyrosine . The cyano residue of saframycin A was specifically labeled as a result of the reaction of {14C}cyanide with a derivative of saframycins, decyanosaframycin A, in the culture filtrate . When calf thymus DNA was incubated with {14C}tyrosine-labeled saframycin A in the presence of dithiothreitol, radioactivities were progressively recovered from DNA fraction . In contrast, saframycin A in the absence of dithiothreitol was completely devoid of reactivity toward DNA . When {14C}cyanide-labeled saframycin A was reacted with DNA, however, none of the radioactivity was associated with DNA . The release of cyano residue from the antibiotic was triggered by the reduction . Thus, conversion of quinone to hydroquinone skeletons as well as conversion of alpha-cyanoamine to immonium or alpha-carbinolamine is the consequence of the reduction . The fact that dithiothreitol-inducible binding of saframycin A to DNA was blocked by the addition of excess cyanide indicates that immonium or alpha-carbinolamine is the actual species involved in the interaction with DNA . The striking similarities between saframycin A and anthramycin in regard to the mode of binding to DNA are discussed.

Biochemistry, 1981 Mar 3, 20(5), 1111 - 9
Pyrrol{1,4}benzodiazepine antibiotics . Proposed structures and characteristics of the in vitro deoxyribonucleic acid adducts of anthramycin, tomaymycin, sibiromycin, and neothramycins A and B; Petrusek RL et al.; The pyrrol{1,4}benzodiazepine antibiotics anthramycin, tomaymycin, sibiromycin, and neothramycins A and B are potent antitumor agents that bind to DNA in a unique manner, resulting in some unusual biological consequences . This paper describes results on which the points of covalent linkage between the drugs (carbinolamine carbon atom) and DNA (N-2 of guanine) are deduced, as well as Corey-Pauling-Koltun (CPK) models for the various drug-DNA adducts . Predictions based upon these CPK models have been tested, and the results are reported in this paper . These tested experimental predictions include (1) instability of the drug-DNA adducts to denaturation of DNA, (2) saturation binding limits, (3) effect of drug binding on the structure of DNA, (4) lack of unwinding and in vitro strand breakage of closed-circular supercoiled simian virus 40 (SV-40) DNA, (5) sensitivity of the secondary structure of DNA to drug binding, (6) hydrodynamic properties of the drug-DNA adducts, (7) hydrogen bonding of the 9-phenolic proton in anthramycin to DNA, (8) structure-activity relationships, and (9) biological consequences of DNA damage, including cumulative damage and slow excision repair, double-strain breaks in DNA in repair-proficient cells, and the selective inhibition of H-strand DNA synthesis in mitochondria . The results are completely in accord with our postulated space-filling models.

Quad Sclavo Diagn, 1981 Mar, 17(1), 22 - 30
{Comparison of the results of antibiotic sensitivity tests made with the ABAC method and the agar diffusion method}; Orsi A et al.; The sensitivity of 200 bacterial strains, recently isolated from pathological products, has been determined in relation to 16 antibiotics both with the ABAC system and the agar diffusion method (Barry) . Furthermore, the interference of the variation of inoculum in the ABAC system (controlled by numbering in Petri dishes) has been evaluated . This study presented a good general agreement of the results between both methods . Results of studies on the variation of inoculum (10(6)--10(7) CFU/ml) performance with the ABAC system, gave a very weak interference in the accuracy of the results (with the exception of a few bacterial species in relation to some antibiotics).

J Antibiot (Tokyo), 1981 Mar, 34(3), 271 - 5
Gilvocarcins, new antitumor antibiotics . 2 . Structural elucidation; Takahashi K et al.; Gilvocarcin V(1), C27H28O9, m.p . 264 approximately 267 degrees C (dec.), and gilvocarcin M(2), C26H26O9, m.p . 245 approximately 248 degrees C (dec.), are new antitumor antibiotics produced by Streptomyces gilvotanareus . The structure of gilvocarcins has been determined by chemical degradation, nmr and mass spectra . They have a benzonaphtopyran-one system, to which the furanose moiety is linked through a C-C glycosyl bond.

Antibiotiki, 1981 Mar, 26(3), 130 - 2
{Use of an express method in studying the cytotoxic action of antitumor antibiotics}; Makukho LV et al.; The cytostatic effect of some antitumor antibiotics such as carminomycin, olivomycin, bruneomycin, rubomycin C and adriamycin was studied with a rapid method based on measurement of 3H-thymidine and 14C-adenine incorporation into the tumor cells of suspended primary cultures of mouse lymphadenosis NK/Ly . The method is recommended for screening of antitumor antibiotics.

Ann Thorac Surg, 1981 Mar, 31(3), 211 - 3
Prophylactic antibiotics in pediatrics cardiovascular surgery: current practices; Faden H; A survey of 23 pediatric cardiovascular surgery programs demonstrated uniform use of prophylactic antibiotics for open-heart operations . Only 65% of the programs used prophylaxis for repair of patent ductus arteriosus . Cephalosporins were the most frequently used antibiotics, but aminoglycosides in combination with penicillins were used in approximately 25% of the operations . Antibiotics were most often started prior to operation (89.7%) and continued for less than five days . These data demonstrate that the use of prophylaxis in pediatric cardiovascular operations conforms to current guidelines.

J Clin Microbiol, 1981 Mar, 13(3), 598 - 600
Effect of antibiotics on the dynamics of color change in Ureaplasma urealyticum cultures; Bloomster TG et al.; Color change of pH indicators in broth medium is commonly used to quantify growth of ureaplasmas . These organisms differ from other members of the Mollicutes by their ability to hydrolyze urea to CO2 and NH3 . This study describes a method which continuously monitors color change in ureaplasmal broth cultures . Using this technique we found: (i) there was a pH-dependent absorbance at 554 nm in ureaplasmal broth medium containing phenol red, (ii) a sigmoidal-shaped color changing curve (absorbance at 554 nm versus time) was produced by metabolizing organisms whereas a linear curve was generated by antibiotic-inhibited ureaplasmas, and (iii) the minimum cell density which elicited a growth-inhibited color change was 1.25 x 10(4) colony-forming units per ml . Other have shown that apparently dead ureaplasmas can cause a color change in broth media . This color change is probably due to the presence of an active urease . This study graphically and quantitatively assesses growth-inhibited color change.

Antibiotiki, 1981 Mar, 26(3), 88 - 92
{Hydrolase activity characteristics of actinomycetes during antibiotic biosynthesis}; Baskakova AA et al.; The activity of the main extracellular hydrolytic enzymes, such as protease, nuclease and amylase was studied in the process of the development of the actinomycetes producing streptomycin, novobiocin, levorin and oleandomycin . It was found that the enzymatic activity significantly changed during the development of the cultures depending on their individual properties . Comparative study of the enzymatic activity of the streptomycin-producing organisms differing in the antibiotic production levels and the use of special nutrient media providing the increased biosynthesis of DNAases allowed a definite relationship to be disclosed between the activity level of extracellular hydrolases and antibiotic production.

Infect Control, 1981 Mar-Apr, 2(2), 107 - 9
Prophylactic antibiotics in pediatric orthopedic surgery: current practices; Faden H; A limited survey of 90 orthopedic surgery programs throughout the U.S.A . was conducted to determine the use of prophylactic antibiotics in pediatric orthopedic operations . Prophylaxis was used most often in the Harrington rod procedure (80.7%); less often in hip (64.2%) and knee (44.7%) reconstructive surgery; rarely in meniscus repairs (8.0%) and in lengthening of Achilles tendons (2.3%) . Cephalosporins (85%) were the antibiotics prescribed most frequently . The first dose was administered before surgery in 89.6% of the operations . Prophylaxis was discontinued within five days in 96% of the operations . These data provide a pattern of the use of prophylaxis in pediatric orthopedic surgery.

Antibiotiki, 1981 Mar, 26(3), 99 - 105
{Antibiotic behavior of Ps . aeruginosa strains isolated from various types of clinical material}; Savitskaia KI et al.; Altogether 158 strains of P . aeruginosa isolated from the material of open and close cavities and blood of patients with bronchopulmonary diseases were studied . It was found that the majority of the virulent (92.6 per cent) and avirulent (70.3 per cent) cultures were characterized by multiple resistance to tetracycline, streptomycin, monomycin, kanamycin, levomycetin and polymyxin B with preserved sensitivity to gentamicin and carbenicillin . The source of the P . aeruginosa isolation had a significant influence on its relation to the effect of antibiotics: the highest number of the resistant cultures was isolated from the blood . No differences in the antibiotic effect on P . aeruginosa depending on the serotype were observed . No differences in the antibiotic effect on P . aeruginosa depending on the serotype were observed . Virulent cultures of P . aeruginosa typed with group agglutinating sera and isolated from the material of the open and close cavities were characterized by a higher resistance level to tetracycline, kanamycin, monomycin and levomycetin than the virulent not-typed strains.

J Antibiot (Tokyo), 1981 Mar, 34(3), 313 - 6
Selective antiviral activity of the antibiotic 2'-amino-2'-deoxyribofuranosyl adenine; Taguchi F et al.; The effect of new anti-mycoplasmal antibiotic, 2'-amino-2-deoxy-9-beta-D-ribofuranosyl adenine (2-AA) on virus multiplication was investigated . The 2-AA inhibited only the multiplication of measles virus among the viruses tested; i.e., herpes simplex virus, BK virus, vesicular stomatitis virus, measles virus and Echo virus . At a concentration of 5 micrograms/ml of 2-AA, the inhibition of measles virus replication was complete, i.e., no infectious virus nor viral antigen detected . In contrast, 9-beta-D-arabinofuranosyl adenine (50 micrograms/ml) was active to herpes simplex virus and BK virus, and was inactive to measles virus, vesicular stomatitis virus and Echo virus . Results described herein may suggest that 2-AA affects the late function (perhaps the translation step) of the replication of measles virus.

J Hosp Infect, 1981 Mar, 2(1), 55 - 61
Correlation of antibiotic usage with an antibiotic policy in a urological ward; Casewell MW et al.; An antibiotic policy for a urological ward was largely implemented by restrictive antibiotic sensitivity reporting, and indications for prophylaxis were derived from the feature of 40 episodes of bacteraemia associated with urological procedure . Of 510 patients admitted to this ward, 30-8 per cent received antibiotics . Of 187 antibiotic courses, 53 per cent were for treatment and 43 per cent for prophylaxis . The stated indications were considered dubious in 28 per cent of courses of treatment and irrational in 13 per cent of courses of prophylaxis . Of 1368 days of antibiotic use, co-trimoxazole and amoxycillin/ampicillin accounted for 84.6 per cent, and gentamicin for 5.6 per cent . The modal duration of courses of co-trimoxazole, amoxycillin/ampicillin, and gentamicin were 5, 5 and 1 days respectively . Antibiotics whose sensitivities were not reported were rarely used, and there was no prescription of cephradine, cefoxitin, cefuroxime or amikacin . In general, antibiotic administration corresponded well with policy guidelines.

JAMA, 1981 Feb 27, 245(8), 842 - 6
Antibiotic use among medical specialties in a community hospital; Jogerst GJ et al.; Antibiotic use in a community hospital was evaluated to demonstrate specialty variations . A chart review was performed using the Veterans Administration's "Guidelines for Peer Review" to determine appropriate antibiotic use . Of the 1,054 patients discharged in August 1977, three hundred ten (29.4%) received 479 courses of antibiotics of which two hundred eighty-seven (60%) were considered appropriate . Seventy-two percent of the therapeutic courses and 36% of the prophylactic courses were appropriate . Prophylactic antibiotics were used in 12% of the hospitalized patients and accounted for 33% of the total antibiotics . No notable difference in appropriate antibiotic use was found among general surgeons (73%), internists (72%), orthopedists (71%), and family practitioners (67%) . Substantially lower levels were found among urologists (54%), otolaryngologists (44%), and obstetricians (36%) . Continued education in proper antibiotic use is needed especially for prophylaxis . Educational programs directed at specific specialties may be the most fruitful way to effect improved overall antibiotic use.

Biochemistry, 1981 Feb 17, 20(4), 919 - 24
Biosynthesis of the macrolide antibiotic chlorothricin; Mascaretti OA et al.; Feeding experiments with 13C-labeled precursors followed by 13C NMR analysis of the antibiotic and its aglycon have established a polyketide mode of biosynthesis for chlorothricin, a metabolite of Streptomyces antibioticus . The acyl moiety is a substituted 6-methylsalicylic acid derived from four acetate units and a methyl group of methionine . The aglycon is comprised of ten acetate and two propionate units, leaving three carbon atoms, C-22, -23, and -24, unaccounted for . The two 2-deoxy-D-rhamnose moieties are derived from glucose with retention of the hydrogens at C-1, C-2, and C-6 and loss of H-3 and H-5 . The hydrogen at C-4 of glucose is transferred intramolecularly to C-6 of the hexose, replacing the hydroxyl group at C-6 in an inversion mode, a result which implicates the thymidine 5'-diphosphate-glucose oxidoreductase reaction in this transformation.

Biochemistry, 1981 Feb 3, 20(3), 546 - 52
Affinity labeling of Escherichia coli ribosomes with a covalently binding derivative of the antibiotic pleuromutilin; Hogenauer G et al.; Reaction of an alkylating pleuromutilin derivative with E . coli ribosomes led to the binding of the compound to both proteins and RNA . If ribosomes of the E . coli strain MRE600 were used, mainly S18 and L2 became labeled . Ribosomes from E . coli D10 bound the reagent to S18 and frequently to L27 instead of L2 . Possibly at slight difference in the structure of these ribosomes exposes different, although closely neighboring, L proteins to the reagent . The simultaneous labeling of L and S proteins seems to reflect the presence of two binding sites for the antibiotic and indicates that the binding sites are located at the interphase region between large and small ribosomal subunits . Analysis of the RNA showed that the affinity label is mainly attached to the 23S species . These data are in good agreement with the known effects of pleuromutilin derivatives on ribosomal functions.

Antimicrob Agents Chemother, 1981 Feb, 19(2), 238 - 47
Repair of membrane alterations induced in baby hamster kidney cells by polyene macrolide antibiotics; Malewicz B et al.; We studied the correlation between chemical characteristics of 13 polyene macrolide antibiotics and the ability to repair the membrane permeability changes induced by polyenes in BHK-21 cells grown in shaker culture . It had been demonstrated that large-macrolide-ring polyenes with rigid molecules (heptaenes) induced specific membrane permeability pathways which were repaired by the eucaryotic cells under the proper conditions . The influence of environmental conditions on the repair process was examined . Aureofacin trimethylammonium methyl ester derivative was used as a selected representative of polyene macrolides inducing specific pathways . The factors influencing the repair process, monitored by measuring the ability of BHK-21 cells to control K+ membrane transport, were examined during and after cell contact with the antibiotic . We found that the repair process was dependent upon the temperature, the concentration of the antibiotic, time of its contact with cells, potassium concentration in the medium, and availability of an energy source . The repair process occurred in the presence of cycloheximide, which inhibited protein synthesis in BHK-21 cells . Results showed that the repair process plays an important role in mammalian cell recovery from the toxic effects of polyenes.

J Antibiot (Tokyo), 1981 Feb, 34(2), 148 - 59
BBM-928, a new antitumor antibiotic complex . III . Structure determination of BBM-928 A, B and C; Konishi M et al.; Structures of antitumor antibiotics BBM-928 A, B and C have been determined . They are cyclic decadepsipeptides containing 3-hydroxy-6-methoxyquinaldic acid as a chromophore . Two amino acids, not found in nature, L-beta-hydroxyl-N-methylvaline and trans-(3S,4S)-4-hydroxy-2,3,4,5-tetrahydropyridazine-3-carboxylic acid, were identified as structural constituents of the antibiotic . In gross structure, BBM-928 resembles the echinomycin group of antibiotics which are cyclic octadepsipeptides having a quinoxaline chromophore, but BBM-928 differs from the latter group by virtue of the lack of a sulfur-containing cross linkage.

Biophys Chem, 1981 Feb, 13(1), 1 - 14
Aspects of specific DNA-protein interaction; local bending of DNA molecules by in-register binding of the oligopeptide antibiotic distamycin; Reinert KE; Distamycin A binds strongly/moderately to DNA below/above r = 0.08 molecules bound per DNA phosphate . Titration viscometric measurements for high and low molecular weight DNA yielded the relative changes of DNA persistence length, delta alpha/alpha 0, and contour length, delta L/L0 (Nucl . Acids Res . 7 (1979) 1375) . delta L/L0 is negligible/positive in the range below/above r = 0.09 at 0.2 M Na+! A two-line covering of the small groove by ligand molecules explains the increase of contour length . The characteristic delta alpha/alpha 0 drop is quantitatively interpreted by local DNA bending (kinking) . The underlying theoretical basis is presented in two appendices and applied, in a third one, to literature data for the DNA-actinomycin system . The angle gamma of local DNA bending as induced by complex formation with different distamycin derivatives is presented for DNA species of different base composition . By means of appropriate model, a length mismatch per dinucleotide of (0.03(2) +/- 0.01)nm {or (0.04(3) +/- 0.01)nm} was derived from the experimentally obtained bending angle per dinucleotide of (1.6 +/- 0.4)0 {or (2.1 +/- 0.05)0}, independent of DNA base composition and distamycin chain length.

Mol Biochem Parasitol, 1981 Feb, 2(3-4), 235 - 55
Inhibitory effects of chloramphenicol isomers and other antibiotics on protein synthesis and respiration in procyclic Trypanosoma brucei brucei; Spithill TW et al.; The effects of various antibiotics on protein synthesis systems in procyclic trypomastigotes of Trypanosoma brucei brucei LUMP 1026 have been determined in an attempt to identify a mitochondrial translation system . The function of cytoplasmic ribosomes in T . b . brucei in vivo is sensitive to inhibition not only by cycloheximide but also by high concentrations of D-chloramphenicol, L-chloramphenicol, erythromycin and tetracycline as a possible secondary consequence of a primary inhibition of mitochondrial respiration in vivo by these latter four compounds . In support of this conclusion, antimycin A inhibits mitochondrial respiration and, secondarily, cytoplasmic protein synthesis in vivo, suggesting that mitochondrial phosphorylation is necessary for cytoplasmic translation in T . b . brucei . Tetracycline inhibition of cytoplasmic protein synthesis in vivo may also be due to a direct effect on cytoplasmic ribosomes, since this drug inhibits ribosome function in vivo . Low concentrations of D-chloramphenicol, erythromycin and tetracycline do not inhibit cycloheximide-insensitive protein synthesis in vivo, implying the presence of permeability barriers to these drugs in T . b . brucei . Mitochondrial fractions isolated from T . b . brucei possess a ribosomal translation system, the function of which is insensitive to cycloheximide but sensitive to inhibition by low concentrations of D-chloramphenicol should only be used with caution in studies of mitochondrial biogenesis in T . b . brucei.

Infusionsther Klin Ernahr, 1981 Feb, 8(1), 44 - 6
{Electrolyte content of antibiotics}; Wiener H et al.; The sodium and potassium content of frequently used antibiotics was calculated . Whenever high dose intravenous chemotherapy is used the amounts of sodium or potassium must be taken in consideration in the electrolyte balance . Special attention must be given to patients on restricted sodium diet . In these cases, the additional sodium resulting from intravenous chemotherapy may exceed the daily administered amount of sodium . The summary of electrolyte content of antibiotics may be useful in balancing electrolytes during infusion therapy.

J Antibiot (Tokyo), 1981 Feb, 34(2), 206 - 11
C-19393 S2 and H2, new carbapenem antibiotics . III . Mode of action; Nozaki Y et al.; Biochemical activities of new carbapenem antibiotics, C-19393 H2(H2) and C-19393 S2(S2), were examined in comparison with those of mecillinam using Escherichia coli . H2 showed remarkably high affinity for penicillin-binding protein (PBP) 2, and high affinity for PBPs 1 and 3 . S2 showed high affinity for PBP 2, moderate affinity for PBP 1 and low affinity for PBP 3 . They induced ovoid cells at lower concentrations and cell lysis at higher concentrations . The inhibitory potency of H2 for peptidoglycan synthesis was similar to that of mecillinam at lower concentrations up to 0.1 micrograms/ml . At concentrations higher than 0.1 micrograms/ml, the inhibition rate by H2 gradually increased up to 100%, whereas that by mecillinam remained at 60% level . The MICs of H2, S2 and mecillinam corresponded to the lowest concentrations giving 60% of inhibition of peptidoglycan synthesis at which concentrations the function of PBP 2 seemed to be prevented completely . These findings indicate that the primary targets of H2 and S2 are PBP 2 involved in cell shape determination in E . coli.

J Urol, 1981 Feb, 125(2), 151 - 2
The value of intraoperative antibiotics in preventing renal transplant wound infections; Novick AC; In a 3-year period 179 renal transplant operations were performed, during which time a uniform regimen for preventing wound infections was used . The incidence of primary renal transplant wound infections was reduced to 1 per cent by administering a single high dose of broad-spectrum antibiotics intraoperatively as an adjunct to this regimen . Intraoperative antibiotic coverage has been a safe and effective measure for preventing primary transplant wound infections.

Antimicrob Agents Chemother, 1981 Feb, 19(2), 349 - 51
Mode of action of Myxococcus xanthus antibiotic TA; Zafriri D et al.; Antibiotic TA inhibited incorporation of diaminopimelic acid and uridine diphosphate-N-acetylglucosamine into Escherichia coli cell walls without altering the ratio of cross-linked to uncross-linked peptidoglycan . Formation of the lipid intermediate was not blocked by TA, suggesting that TA interferes with polymerization of the lipid-disaccharide-pentapeptide.

Proc Natl Acad Sci U S A, 1981 Feb, 78(2), 1233 - 6
Effects of amphotericin B, nystatin, and other polyene antibiotics on chitin synthase; Rast DM et al.; The effects of amphotericin B (AmB), nystatin, filipin, and pimaricin were tested chitin synthase (EC 2.4.1.16) (chitosomes from yeast cells of Mucor rouxii) . AmB and nystatin inhibited the enzyme at concentrations greater than or equal to 10 micrograms/ml, filipin was weakly inhibitory, and pimaricin had no effect . The inhibition of chitin synthase by AmB appears to be noncompetitive, with a Ki value of about 0.13 mM . the effect of nystatin was more complex and included a sharp stimulation of chitin synthase activity at approximately 50 micrograms/ml . Our findings suggest the existence of binding sites (sterols?) on the chitosome that are selective for certain polyenes and that play a role in the operation of chitin synthase . Because the minimal growth inhibitory concentrations of AmB or nystatin are lower than the concentrations that inhibit chitin synthase in vitro, the possibility of chitosomal chitin synthase being a primary target for the antifungal action of these polyenes seems unlikely.

Lancet, 1981 Jan 3, 1(8210), 31 - 3
Marketing of obsolete antibiotics in Central America; Gustafsson LL et al.; In 1977 the World Health Organisation published a list of essential drugs that would provide the basis for rational drug utilisation in developing countries . Only 16 antibiotics were included . A review of antibiotics marketed in Central America revealed that in only two of eight countries were less than 200 antibiotic drug products sold . At least a third of these were drug combinations of questionable value . Adequate information about adverse drug effects was frequently not provided to doctors in the manufacturers' drug descriptions . Furthermore compounds could be obtained without prescription . Thus there is a high potential risk for misuse of antibiotics in the countries studied which might be reduced by adhering to the principles outlined in the W.H.O . report on essential drugs.

Postgrad Med, 1981 Jan, 69(1), 96 - 100, 103, 105-7
Potential pitfalls in antibiotic prescribing; DeHaan RM; The ever-increasing number of antibiotics on the market, coupled with the uncanny ability of pathogens to develop resistance, makes choosing an agent for a given patient a complex task for even the most skilled clinician . A rational plan for making this choice, as well as a number of potential problems in prescribing the drugs, is discussed.

Surg Gynecol Obstet, 1981 Jan, 152(1), 36 - 8
Operations on the colon without preoperative oral antibiotic therapy; Menaker GJ et al.; The ideal preparation of the intestine prior to elective colonic resection has been a controversial subject . With the development of new and more effective antibiotics, many modalities of intestinal preparation preoperatively have been used in an effort to reduce the number of infectious complications . Mechanical cleansing of the intestine, when accompanied by perioperative parenteral antibiotics, is adequate preparation prior to resection of the intestine . One hundred consecutive operations upon the colon by one surgeon were the subject of this retrospective study . Approximately 70 per cent of the operations were for carcinoma and the remainder for inflammatory disease . Preparation consisted of the administration of cathartics and saline solution enemas combined with a liquid diet for 48 hours prior to operation . Perioperative parenteral antibiotic therapy was given for 48 to 72 hours or as long as intravenous fluids were administered . All anastomoses were the open, two layer type, using nonabsorbable suture material . All abdominal incisions were closed primarily . There were no operative deaths, anastomotic leaks, intra-abdominal abscesses or fistulas . There were six instances of wound infection . Our results with this type of management compare favorably with those of other surgeons using various modes of preoperative oral antibiotic therapy and suggest that oral preoperative antibiotic therapy may not be necessary in elective operations on the colon.

Drug Chem Toxicol, 1981, 4(4), 383 - 96
The toxicological evaluation of carminomycin - an antineoplastic anthracycline antibiotic; Buroker RA et al.; Carminomycin, an anthracycline antibiotic discovered in the Soviet Union, possesses antitumor activity and is chemically related to adriamycin and daunorubicin . The toxic effects of carminomycin observed in single-dose toxicologic studies in mice iv (4.5-13.5 mg2) and po (18.9-52.2 mg/m2), rats iv (6.0-21.0 mg/m2), dogs iv (1.0-16.0 mg/m2) and po (16.0-80.0 mg/m2), Rhesus monkeys po (24.0-144.0 mg/m2); and in multiple-dose studies in dogs iv (18 doses 0..6-5.0 mg/m2, 2X/week) and rats sc (9 doses 3.0-12.0 mg/m2, 3X/week), were dose-related and primarily manifested as suppression of hematopoiesis . Other toxicities observed included nephrotoxicity, gastrointestinal toxicity, decreased spermatogenesis, decrease in size and activity of the prostate and seminal vesicles, and ovarian alterations . In general, these toxicities were reversible in surviving animals during recovery periods . Cardiotoxicity, similar to that seen with adriamycin sc (13 doses 12.0 mg/m2, 1X/week) was not observed with carminomycin sc (13 doses 6.0 mg/m2, 1X/week).

Rev Fr Mal Respir, 1981, 9(6), 453 - 60
{The cost of antibiotics in respiratory disease (author's transl)}; Leophonte P et al.; The most common prescriptions for antibiotics in France are those used in the treatment of respiratory infections, both in hospital and in general practice . They represent 10% of the total drug bill and about 1.5 to 2% of the total expenses of medical care . Antibiotics are often presented excessively or irrationally either because the proper indications were not firmly established or because unnecessarily powerful preparations were used . This is illustrated by two examples (among others), namely uncomplicated pneumococcal pneumonia and chronic bronchitis . More economic solutions are not easy and the current lack approach should not be replaced by a dogmatic one . Two immediate measures would hold the attention of respiratory physicians: the publication of a guide to antibiotic therapy in respiratory disease and periodic audits of antibiotic usage.

Scand J Gastroenterol, 1981, 16(4), 465 - 8
Colonoscopy in the diagnosis of antibiotic-associated colitis . A prospective study; Seppala K et al.; Colonoscopic findings among 16 patients with histologically proved antibiotic-associated pseudomembranous colitis (PMC) were analyzed . The characteristic endoscopic changes of PMC with pseudomembranes were observed in only 5 (31%) out of 16 patients by sigmoidoscopy but in 11 (85%) out of 13 patients in whom colonoscopy was also performed . The findings suggest the importance of colonoscopy in the early diagnosis of PMC and indicate that the typical endoscopic changes of PMC are limited to the colon above the rectosigmoid area in most patients with antibiotic-associated colitis . It is emphasized that colonoscopy should be performed at least in clinically suspected PMC cases, in which the early diagnosis of PMC might be missed if sigmoidoscopy alone is performed.

Zentralbl Bakteriol Mikrobiol Hyg {B}, 1981, 173(3-4), 173 - 9
Acute toxicity testing of some herbicides-, alkaloids-, and antibiotics-metabolizing soil bacteria in the rat; Kaiser A et al.; Seven strains of soil bacteria with the ability to metabolize herbicides, alkaloids or antibiotics were tested in rats for acute toxicity . 1 . Upon oral administration of 9.0 x 10(8) to 6.6 x 10(10) cells daily during 7 d no adverse reactions were observed . 2 . Exposure by air did not lead to specific pulmonary changes . 3 . Intracutaneous injection of 7.5 x 10(6) to 1.4 x 10(8) cells did not lead to adverse skin reactions . 4 . Intraperitoneal injections up to 10(8) cells per animal did not kill rats although bacteria entered blood . At higher concentrations some mortality occurred partly due to unspecific stress reactions . 5 . Animal data and observations on 20 humans being exposed to these strains for 2 months up to 15 years support the view that the bacteria tested are essentially harmless for health.

Eur Surg Res, 1981, 13(4), 290 - 8
Defects in hemostasis produced by antibiotics . An in vivo study in the rat; Bengmark S et al.; The effect of preoperative infusion of benzylpenicillin, carbenicillin, ampicillin, chloramphenicol and doxycycline on hemostasis after standardized liver resection was studied in the rat . Plasma levels of each antibiotic were within the range of those found after administration of therapeutic doses in man . Bleeding time was prolonged and blood loss was increased in all cases of antibiotic administration compared with controls . APT time after liver resection was prolonged in the carbenicillin- and chloramphenicol-treated groups . Platelet function, assayed by ADP- and collagen-induced platelet aggregation was impaired in benzylpenicillin-, carbenicillin- and chloramphenicol-treated animals.

Z Exp Chir, 1981, 14(3), 128 - 38
{Intra-arterial antibiotic therapy in the management of chronic post-traumatic osteomyelitis of the extremities (experimental and clinical studies}; Laky R et al.; Authors examined the changes of antibiotic concentration in the inflammatory focus after administering Gentamycin and Cephalothin intravenously or intraarterially in case of experimentally induced osteomyelitis in the tibia of rabbit . Administering Gentamycin i . v . no therapeutic level could be measured, while Cephalothin showed a therapeutic level of antibiotic concentration just for a short period . When the same doses of these antibiotics were administered in the femoral artery, effective local antibiotic concentration could be detected for 3 hours . Authors' clinical studies also support these experimental results . Performing 43 i . a . treatments in 38 patients with osteomyelitis 39 was rated as effective.

J Antibiot (Tokyo), 1981 Jan, 34(1), 103 - 13
Binding of aminocyclitol antibiotics to kidney and intestinal brush border membranes; Kardos N et al.; Binding of aminocyclitol antibiotics to intestinal and kidney brush border membranes has been studied in vitro by means of vesicular preparations . The binding is rapid, reversible, specific, saturable and has a high affinity . To both tissues, gentamicin and sisomicin bind to a single binding site or receptor . These antibiotics demonstrate increased binding under conditions of increasing pH . Membrane binding disappears when the vesicle proteins are denatured with TCA . A significant reduction in aminocyclitol binding after treatment of vesicles with papain indicates that a portion of the binding receptor protein is exposed to the outer surface of the brush border membrane . The accumulated evidence suggests that the nature of the binding mechanism is not a simple electrostatic interaction between the antibiotic's charged amino groups and the polyanions of the membrane . Alternatively, a specific membrane structure is required for binding whose characteristics reflect a drug-receptor interaction . Receptor binding is characterized as being saturable, reversible, and specific; all of which have been demonstrated for aminocyclitols and brush border membranes.

Int J Health Serv, 1981, 11(2), 283 - 301
Adverse reactions to antibiotic drugs: the present scope of the problem in outpatient care and possibilities for improvement; Hemminki E; This study provides estimates of the frequency of adverse reactions due to antibiotic therapy and the effectiveness of two approaches in reducing them . Calculations were made of the extent of decrease in adverse reactions if physicians prescribed the drug of choice, and if antibiotics were prescribed only when necessary . The risks of adverse reactions and the estimates of unnecessary prescribing were obtained from the published medical literature . The number of prescriptions and the diseases treated were obtained from a commercial data source (IMS America) . It was estimated that on average one antibiotic prescription per inhabitant was prescribed in outpatient care, that 7.6 percent of the population had adverse reaction due to antibiotic therapy, and that 1.4 percent had a serious reaction in 1974 in the United States . If physicians had prescribed the drug of choice, the number of adverse reactions would have been reduced by 37 percent . If antibiotics had been prescribed only when necessary, but the pattern of prescribing different antibiotics had been the same, one third of the adverse reactions would have occurred . If physicians had prescribed the drug of choice and only when necessary, about one fifth of the adverse reactions would have occurred . The actual number of avoidable adverse reactions may be larger or smaller than these estimates, but the magnitude of the effect indicates an area for concern.

Circ Shock, 1981, 8(1), 41 - 7
Graded intestinal vascular obstruction . II . Effects of antibiotic pretreatment in the rat; Haglind E et al.; This study was performed to elucidate whether bacteria, or products of bacterial origin, could account for the circulatory collapse following a 1-hour intestinal vascular obstruction in the rat . Animals pretreated with clindamycin, in a way previously shown to induce characteristics otherwise found only in germ-free rats, were compared to controls pretreated with saline . Graded intestinal vascular obstruction was applied and four different pressure levels were used . Mortality increased with the applied pressure but there was no difference between the clindamycin-pretreated rats and controls . Hematocrit increased equally in all pressure levels and was not influenced by pretreatment . The amount of fluid lost from the serosal surface of the intestines was not correlated to the pretreatment used, the increase in hematocrit, or mortality . In the higher pressure levels, characteristic microscopic intestinal mucosal lesions were found in both series and the degree of mucosal damage correlated with increase mortality.

Acta Chir Scand, 1981, 147(1), 33 - 6
Local antibiotic irrigation in the treatment of arterial graft infections; Almgren B et al.; A retrospective study was made of 7 patients with infected vascular grafts treated by local debridement, drainage and continuous antibiotic irrigation in combination with systemic antibiotics . The long-term results were excellent in 4 patients in whom infection had occurred along Dacron grafts without involvement of anastomoses but involved a risk of rebleeding . Some general principles in the management of patients with infected vascular grafts are suggested.

In Vitro, 1981 Jan, 17(1), 71 - 6
Effects of antibiotics on protein synthesis and degradation in primary cultures of rat hepatocytes; Schwarze PE et al.; In primary hepatocyte cultures, maintained in a protein-free medium, streptomycin, penicillin, and Garamycin (gentamicin) all inhibited protein synthesis at concentrations above 0.1 mM . Some inhibition was also observed with the fungicide Mycostatin at 100 U/ml . Hepatocytic protein degradation was markedly inhibited by penicillin fat concentrations above 0.1 mM, whereas streptomycin and Garamycin only showed slight inhibition at concentrations in excess of 1 mM . None of the antibiotics had any detectable effect on the structural integrity (viability) of the cells.

Antibiotiki, 1981 Jan, 26(1), 24 - 8
{Use of the aliphatic amine reaction with 2,5-dinitrophenol in antibiotic analysis}; Bronov LV et al.; Possible use of dinitrophenol reaction with amines in quantitative determination of amines and amino sugars in various antibiotics was investigated . It was found that the reaction with 2,5-dinitrophenol (2,5-DNP) in dimethylsulfoxide (DMSO) providing the highest batochromic shift in the electron spectra was most suitable . Selectivity of the 2,5-DNP reaction with respect to mycosamine contained in polyenic antibiotics was shown . With the method of PMR it was demonstrated that DMSO formed a complex with 2,5-DMP . The electron spectral of the complexes of glucosamine, N-methylgycosamine and levorin with 2,5-DNP were used for calculation of the complex stability constants, which were practically the same . This provided the use of glucosamine as a standard for plotting the calibration curves . A quantitative method for determination of amines in polyenic antibiotics based on the above reaction was developed.

Antibiotiki, 1981 Jan, 26(1), 19 - 23
{Aglycone structure of the polyene antibiotic, gannibamycin}; Shenin IuD et al.; Functional analysis of gannibamycin, a new macrolide pentaenic antibiotic was performed . It was found that the antibiotic contained carbonyl, carboxyl group and one molecule of nitrogen and no isolated double bonds . The antibiotic did not participate in the reaction of retroaldol splitting . Ozonization of the antibiotic followed by reduction of the ozonolysis products at first by catalytic hydrogenation and then by lithium aluminohydride resulted in formation of polyols, such as 14-hydroxymethyloctadecanhexaol-1, 6, 13, 15, 17, 18 and 2-methyl-1, 4, 6-trihydroxyoctane . Their structures were proved with mass spectrometry of peracetates . 3-Methyl-tetradecanedicarboxylic acid was isolated from the oxidation products of perhydrogannibamycin . Partial structure of the aglycone, i . e . 1, 30 (or 1, 32)-lactone 13, 15, 17, 30, 32-pentohydroxy-28-methyl-6-ketotetratricontane-18, 20, 22, 24, 26-pentaen-1, 14-dicarboxylic acid was suggested . It was confirmed by the analysis of the mass spectra of the antibiotic permethoxy derivative and its deutero analog.

Arzneimittelforschung, 1981, 31(6), 974 - 6
Influence of ambroxol on the bronchopulmonary level of antibiotics; Wiemeyer JC; Antibiotic levels in bronchopulmonary tissue following oral administration of ampicillin, erythromycin and amoxycillin dosed 50 mg/dg were compared with those obtained by the same treatments n0 mg/dg p.o of trans-4-{(2-amino-3,5-dibromo-benzyl)amino}cyclohexanol (ambroxol, Mucosolvan) in several groups of rats . The addition of ambroxol was correlated with an increase of 234% in the pulmonary average concentration of ampicillin, 27% in that of erythromycin 27% in that of amoxycillin; the statistical evaluation of these differences resulted in less than 0.05 in each case . It may be concluded that ambroxol, through a mechanism still unclear, can increase the antibiotic levels in the lungs of the rat.

Klin Padiatr, 1981 Jan, 193(1), 39 - 40
{Identification of bacterial antigens in patients pretreated with antibiotics using counter-current immunoelectrophoresis (author's transl)}; Storm W; The article describes the method of counter-current immunoelectrophoresis as a rapid and safe technique for the identification of bacterial antigens in body fluids . This technique has proved very useful especially in patients who had been pretreated with antibiotics, since the culture yields are usually negative in such patients, as experience has shown.

Mikrobiyol Bul, 1981, 15(3-4), 189 - 206
{Aminoglycoside antibiotics: chemistry, modifying enzymes, present therapeutic values and recent developments}; Berkman E; This review article outlines the chemical structures and the location of the enzymatic inactivation sites which are sensitive to bacterial enzymes of aminoglycoside antibiotics . The distribution of these enzymes in different bacterial genera are also discussed . It is also noted that ineffectiveness of a new antibiotic may be due to the presence of preexisting inactivating enzymes . The great importance of these must be taken into an account before deciding to introduce a new drug into the therapy of local pathogens . Some new methods, like chemical alterations, are now available which renders aminoglycoside antibiotics to be resistant against these enzymes.

Vet Med Nauki, 1981, 18(8), 47 - 54
{Antibiotic relationship of streptomycin-dependent and streptomycin-resistant Escherichia coli mutants pathogenic for poultry}; Cherneva E et al.; Studied was the reaction streptomycin-dependent and streptomycin-resistant mutants and their revertants of the Escherichia coli strains 078:K80, 02:K1, and 0111:K58 to the following, practically important antibiotics: rifampicin, novobiocin, chloramphenicol, and penicillin . The study made use of mutants of both smooth (S) and rough (R) form obtained through induced mutagenesis effected by means of nitrosoguanidine and nitrous acid . The method of serial dilution of antibiotics and that of dynamic recording of their action through automatic biophotometry were employed . Negligible differences were established in the behaviour of the various groups of organisms . The streptomycin - dependent mutants retained unchanged the reaction of the initial strains to the antibiotics . The revertants showed high level of of resistance to streptomycin and by their behaviour they were closer to the streptomycin - resistant mutants than to the initial strains . In connection with this the probability is discussed of the "suppressor" origin of the streptomycin-dependent mutants.

Mol Gen Genet, 1981, 184(2), 224 - 9
An antibiotic dependent conditional lethal mutant with a lesion affecting transcription and translation; Dabbs ER et al.; A conditioned lethal mutant of E . coli was isolated which required the presence of either the RNA polymerase targeted antibiotic, rifampicin, or the ribosomally targeted antibiotic, kasugamycin, for survival . This mutant was characterised . The locus of the mutation responsible for the antibiotic dependent phenotype, ridA, was mapped at about 70.5 min on the chromosomal linkage map, between argR and fabE . The mutant was investigated as a candidate for a strain with a lesion in some cellular component acting on both RNA polymerase and the ribosome . A close interaction with RNA polymerase was evident from the interplay arising from the combination of ridA and various rpoB mutations as manifested in the phenotype . The ability of kasugamycin, but not other ribosomally targeted aminoglycoside antibiotics, to relieve the lethality due to the ridA mutation was an indication of the specificity in the interaction of the ridA gene product with the ribosome.

Experientia, 1981, 37(8), 828 - 31
Flow microcalorimetric bioassay of polyene antibiotics: interaction with growing Saccharomyces cerevisiae; Beezer AE et al.; Microcalorimetric investigation of the interaction of polyene antibiotics with mid-exponential cells of a growing culture of Saccharomyces cerevisiae has been used as the basis of a bioassay procedure . The assay is rapid, sensitive and reproducible . The results are compared to classical assays and potency ranking orders.

Rev Infect Dis, 1981 Jan-Feb, 3(1), 45 - 66
Pharmacokinetics of tissue penetration of antibiotics; Bergan T; Past efforts to characterize the ability of antibiotics to penetrate into tissues is reviewed, particularly the results of models that reflect the concentration of antibiotics in interstitial fluid (i.e., skin blisters, tissue chambers, skin chambers, wound exudates, implanted fibrin clots, and peripheral lymph) . The preferable sources of such fluid appear to be skin chambers, suction-induced skin blisters, and peripheral lymph . Extent of penetration of antibiotics into tissue fluid is related to the amount of antibiotic not bound to protein . Protein binding is particularly inhibitory to penetration when greater than 80% of the antibiotic is bound . It is preferable to follow the extravascular concentrations of antibiotic for longer periods than is usually done . The ability of antibiotics to penetrate is best evaluated by use of the ratio of the area under the concentration curve (AUC) for antibiotic in the peripheral locus to the AUC for serum . Pharmacokinetic analysis should be done with data from each individual, not with data derived from curves using mean values . Penetration into fibrin, lymph, and chambers implanted in tissues follows Fick's law of diffusion . Lag times indicate the interval before penetration of antibiotic in serum to the peripheral locus may be observed . First-order, one-compartment, open models are applicable to the characterization of extravascular concentrations of antibiotics . The AUC for antibiotic in serum during a time interval is the factor determining the amount of agent that passes into an extravascular focus . Concentrations of drug in tissues are lower than those in serum; the peaks occur simultaneously or shortly after the maximal levels are reached in serum, and for most antibiotics the elimination of antibiotics from extravascular parts of the body is slower than from serum, particularly for agents with a half-life in serum of less than 4-5 hr.

J Med Chem, 1981 Jan, 24(1), 33 - 8
Permethyl analogue of the pyrrolic antibiotic distamycin A; Gendler PL et al.; The synthesis of an analogue of distamycin A, a pyrrolic oligopeptide possessing antiviral and antibiotic activity, is described in which each of the three pyrrole rings is fully methylated . This structural modification results in pyrrole rings which are extraordinarily electron rich and required the development of a new synthetic approach to these polypyrrolic amides . The key reactions involved development of a general method for the synthesis of 3-aminopyrroles and for formation of an amide bond between a pyrrole-2-carboxylic acid and these 3-aminopyrroles . Since the acid is hindered, a poor electrophile, and acid sensitive, while the amine is unstable and a hindered, weak nucleophile, amide bond formation under the usual conditions was poor . A very efficient method, however, was developed involving the isolation of 1-hydroxybenzotriazole active ester prepared in situ from another active ester . Neither the mono-, di-, nor tripyrrolic permethyl analogues were effective antimalarials, and none showed anticancer activity.

J Bacteriol, 1981 Jan, 145(1), 632 - 7
Effects of furazlocillin, a beta-lactam antibiotic which binds selectively to penicillin-binding protein 3, on Escherichia coli mutants deficient in other penicillin-binding proteins; Schmidt LS et al.; Furazlocillin binds selectively to penicillin-binding protein 3 (PBP-3), prevents septation of Escherichia coli, and allows the cells to form long filaments without lysis . The effect of furazlocillin on the morphology, autolysis, and murein synthesis of E . coli mutants deficient in either PBP-1A, PBP-1Bs, or PBP-2 was studied . The results reveal that PBP-1A and PBP-1Bs functions are not equivalent since furazlocillin affects the morphology, autolysis, and murein synthesis of PBP1A- mutants quite differently from that of PBP-1Bs mutants . Different "PBP-2-" mutants were found to respond to furazlocillin in dramatically different ways: strain LS-1 cells formed elongated rods with a central bulge which eventually lysed, whereas SP6 cells formed stable "barbells" in which the two daughter cells were well separated but remained connected by a thick central region.

Antibiotiki, 1981 Jan, 26(1), 55 - 8
{Effect of antibiotics on human lymphocyte mitogenesis}; Rachkov SM et al.; The effect of some antibiotics on in vitro blast transformation of lymphocytes of healthy donors stimulated with phytohemagglutinin was studied . The stimulation level was estimated by incorporation of 3H-thymidine into lymphocytes . It was shown that minocycline had a markedly pronounced inhibitory activity . Chloramphenicol and tetracycline also proved to be active inhibitors . Penicillin, cephalotin and carbenicillin had no effect on lymphocyte mitogenesis . Gentamicin proved to be a rather active stimulator of mitogenesis, especially with the use of a suboptimal concentration of phytohemagglutinin . The method is rather sensitive and informative . It may be used for preliminary determination of the immunotropic properties of drugs and chemical compounds with respect to immunocompetent cells of man.

Cancer Treat Rep, 1981, 65 Suppl 4, 35 - 7
Future clinical investigations with anthracycline antibiotics in relation to daunorubicin; Muggia FM et al.; Future studies with daunorubicin involve mainly comparative evaluations with other anthracycline antibiotics and related compounds . Efforts are ongoing to improve the therapeutic index of these drugs . This includes not only laboratory development but also clinical evaluation of analogs, manipulations in dose schedules, and the use of protectors of toxic manifestations, primarily of cardiomyopathy . Technological advances in the clinical area permit, for example, the exploration of daunorubicin and related compounds by continuous infusion under more precise pharmacologic and cardiologic monitoring than was possible when they were initially introduced.

Scand J Infect Dis Suppl, 1981, Suppl 27, 1 - 48
Tissue distribution of beta-lactam antibiotics . Experimental studies in rabbits; Cars O; Tissue distribution of ampicillin, dicloxacillin and cefuroxime was studied in rabbits . Different methods allowing frequent samples to be obtained from the same animal were used . Tissue fluid was obtained from subcutaneously implanted steel net cages and by implantation of thin cotton threads under the muscle fascia . A microtechnique was developed for determination of antibiotic concentrations in small muscle samples . The concentration time course in serum and tissue was followed after a single intravenous or intramuscular injection of the antibiotic . In tissue cage fluid, levels of ampicillin and dicloxacillin were low as compared to the serum concentrations . Also, maximum levels occurred later than in serum and elimination was slower . In contrast, rapid peak levels were achieved in muscle tissue with all three investigated antibiotics and the muscle concentrations declined parallel to the serum levels . The results also indicated that beta-lactam antibiotics are not homogeneously distributed in muscle tissue but mainly confined to the extracellular fluid volume . Whole tissue levels could therefore underestimate the actual antibiotic concentrations in the tissue fluid where the bacteria causing soft tissue infections are most likely to be found . Serum levels, however, seemed to be a good indicator for the concentration time course in tissue fluid.

Antibiotiki, 1981 Jan, 26(1), 28 - 33
{Isolation and purification of the chloramphenicol-acetyltransferase from Y . pestis EV cells with extrachromosomal resistance to the antibiotic by affinity chromatography}; Korobeinik NV et al.; Purification of chloramphenicol acetyltransferase isolated from the cells of Y . pestis EV-R with extrachromosomal resistance to chloramphenicol included ultrafiltration on the microporous membranes Diaflo-XM 300 and biospecific chromatography on columns with cepharose 4B covalently bound with the reduced chloramphenicol . Elution of chloramphenicol acetyltransferase was achieved by means of addition of native chloramphenicol to the buffer solution . Such native chloramphenicol had higher affinity to the enzyme than the reduced antibiotic . As a result the enzyme preparations with 250 times higher purity levels and 70 per cent of the initial activity were obtained . The disc electrophoresis of the sample in polyacrylamide gel produced a single protein zone capable of chloramphenicol acetylation in the presence of Ac approximately CoA.

Immun Infekt, 1981, 9(3), 99 - 105
{Bacterial penicillin-binding proteins as specific targets of beta-lactam-antibiotics and as factors of resistance to antibiotics (author's transl)}; Martin HH et al.; Bacteria contain several isofunctional, beta-lactam sensitive membrane enzymes engaged in the synthesis of cell wall peptidoglycan (peptidoglycan-DD-carboxypeptidases, -transpeptidases, -endopeptidases) as members of sets of even more numerous membrane proteins with specific, high binding-affinity for beta-lactam antibiotics (penicillin-binding proteins, PBPs) . Effective inhibition of bacterial growth by beta-lactam antibiotics requires simultaneous inactivation of the essential functions of several PBPs by formation of stable enzyme-antibiotic complexes . Failure to achieve permanent inactivation of all essential targets by a given beta-lactam appears to be another cause of bacterial beta-lactam resistance, in addition to known resistance mechanisms based on action of beta-lactamases and on screening off targets from antibiotic by a penetration barrier . Different groups of beta-lactam antibiotics vary characteristically in their affinity for specific essential PBPs . Combined application of two beta-lactams which complement each other in the inactivation to essential targets is a possibility to overcome resistance of single antibiotics.

Chemotherapy, 1981, 27(2), 89 - 94
A comparison of the myocardial depressant effects of several aminoglycoside antibiotics; Descotes J et al.; The myocardial depressant action of aminoglycosides has been known for a number of years but there was no available data on newer derivatives . We have thus studied the contractile responses of isolated guinea pig left atria to increasing concentrations of gentamicin, tobramycin, lividomycin and amikacin (0.02, 0.04, 0.08, 0.13, 0.17 and 0.22 mM) . Our results are consistent with those of previous workers and show that newer aminoglycosides do exert a similar depressant action . As gentamicin and tobramycin are more depressant than lividomycin, then amikacin at similar concentrations, no clear-cut difference was obtained when respecting a relative range of concentrations mimicking that of clinical situations . However, these depressant effects were attained using concentrations far exceeding those reached in man.

Rev Infect Dis, 1981 Jan-Feb, 3(1), 121 - 4
Levels of antibiotic in human blood and interstitial fluid after oral administration of bacampicillin or phenoxymethyl penicillin and intravenous administration of amoxicillin or ampicillin; Tan JS et al.; Levels of antibiotic in the serum and interstitial fluid were determined for 11 volunteers who received conventional doses of either phenoxymethyl penicillin (penicillin V) or bacampicillin orally and for 11 volunteers who received either amoxicillin or ampicillin intravenously . The levels of antibiotic achieved in both blood and interstitial fluid were higher in the volunteers who received bacampicillin than in those who received penicillin V . The levels of antibiotic in serum and interstitial fluid of participants in the study who received amoxicillin or ampicillin intravenously were comparable with those achieved with equivalent doses of oral bacampicillin . The lowest levels of antibiotic in serum and interstitial fluid were obtained in volunteers who received oral penicillin V, whereas the highest levels were obtained in those given ampicillin and amoxicillin intravenously.

Arzneimittelforschung, 1981, 31(11), 1972 - 6
Antibiotic concentrations in blood and tissue . Intraoperative ischemia as a model for the determination of tissue concentrations using mezlocillin and oxacillin as examples; Adam D et al.; Blood present in the tissue distorts the results obtained during measurement of antibiotic tissue levels . The greater the blood supply to the tissue, the bigger the error when tissue levels are measured . The examination of tissue removed during temporary intraoperative ischemia is an alternative to the indirect mathematical method of correcting errors of blood level measurement . This technique was tested by determining tissue concentrations after i.v . injection of 4 g mezlocillin and 2 g oxacillin . The tissue was removed during operations on limbs after the application of an Esmarch's bandage . Determination of hemoglobin in ischemic tissue confirmed exsanguination so that the 6-((R)-2-{3-methylsulfonyl-2-oxo-imidazolidine-1-carboxamido}-2-phenylacetamido )-penicillanic acid-Na (mezlocillin) and 5-methyl-3-phenyl-4-isoxazolylpenicillin (oxacillin) concentrations determined corresponded to the actual tissue levels . The concentrations of mezlocillin and oxacillin in fat, skin, tendon, muscle, ganglion, aponeurosis, tumour, ligament, subcutis, synovial fluid, epineurium and serum are given in the text.

Cancer Chemother Pharmacol, 1981, 5(4), 243 - 9
A pharmacokinetic simulation model for chemotherapy of brain tumor with an antitumor protein antibiotic, neocarzinostatin . Theoretical considerations behind a two-compartment model for continuous infusion via an internal carotid artery; Maeda H et al.; A pharmacokinetic two-compartment model for the treatment of brain tumors in man was simulated with the aid of a computer . The parameters necessary for the simulations such as inactivation rate constant, elimination rate constant, distribution volume, blood volume, cerebral blood flow, and cytotoxic drug concentration were either determined in this study or obtained from the literature . A proteinaceous antitumor antibiotic, neocarzinostatin (NCS), was utilized as a prototype drug because it has features making it advantageous in the treatment of brain tumor . In particular, NCS has an extremely short half-life in serum (t 1/2 less than or equal to 3 s), while it is relatively stable in the cerebrospinal fluid (CSF) (t 1/2 approximately 50 s) . Therefore, the drug level in the cerebral compartment can be made adequately high with an appropriate infusion velocity into the cerebral compartment; however, it was possible to keep the plasma level of the drug much lower than the toxic level . Thus, few side-effects should result . In an in vitro study, NCS was found to exhibit its cytotoxicity to glioblastoma cells at a concentration as low as 0.005 microgram/ml . In contrast, the cytotoxicity was not apparent for the normal glia cells at 0.1 microgram/ml . The model being considered in this investigation is a two-compartment model, which consists of the cerebral compartment and the rest of the circulatory system of the body . In this case the drug is infused via an internal carotid artery . The results of pharmacokinetic simulation and dose regimens for NCs are presented, based on the effective concentration of the drug to glioblastoma cells in culture and the available pharmacological parameters.

Prostate Suppl, 1981, 1, 119 - 23
Fundamental studies on a new antitumor antibiotic peplomycin; Matsuda A; Results of testing in mice and rats revealed that peplomycin has a stronger antitumor effect than bleomycin (BLM) . Peplomycin, a BLM analogue, also has superior organ distribution characteristics and localizes in the rat prostate . Pulmonary toxicity associated with peplomycin therapy is less severe than that which accompanies BLM therapy.

Eur J Biochem, 1981 Jan, 113(3), 457 - 61
On the mechanism of interaction of N-acetylphenylalanyl-tRNAPhe with ribosomes of Escherichia coli: effect of antibiotics and Tp psi pCpGp; Ivanov YV et al.; The tetranucleotide Tp psi pCpGp acts as a specific inhibitor of the rate of AcPhe-tRNAPhe binding in the ribosomal P site . This effect is observed both in the presence and in the absence of poly(U) . In the absence of poly(U) antibiotics tetracycline and puromycin also decrease the rate of AcPhe-tRNAPhe binding . Some inhibition by tetracycline is observed with poly(U) . All these inhibitors are known to be ligands of the ribosomal A site, and their influence on the P site binding can be most naturally explained by the suggestion that AcPhe-tRNAPhe enters the ribosome via the A site, forms there an intermediate complex, and spontaneous translocation into the P site follows . In the presence of poly(U) arguments in favour of this hypothesis are much weaker, but the same sequence of events is possible.

Ann Intern Med, 1981 Jan, 94(1), 51 - 2
Encephalopathy complicating Whipple's disease: failure to respond to antibiotics; Schmitt BP et al.; Progressive dementia, vertical ophthalmoplegia, and prominent hypothalamic dysfunction developed in one patient with documented intestinal Whipple's disease despite ongoing antibiotic therapy with intestinal remission . A clinical diagnosis of central nervous Whipple's disease was made on the basis of the patient's presentation . High-dose parenteral penicillin and chloramphenicol were administered for 4 1/2 weeks . There was no improvement in results of daily mental status examination or neuropsychologic testing . Deterioration was noted in the electroencephalographic findings after therapy . Vigorous antibiotic therapy with agents that cross the blood-brain barrier had no immediate beneficial effect . Irreversible neurologic damage or a slow, delayed response may account for this observation.

Reprod Nutr Dev, 1981, 21(2), 185 - 92
{Mechanism of action of the new antibiotic kirromycin}; Sander G; The discovery and the elucidation of the mechanism of action of a new family of antibiotics is described . These antibiotics, here represented by kirromycin, all inhibit bacterial protein synthesis by acting on the protein elongation factor Tu, blocking its release from the ribosome during the elongation cycle and thereby inhibiting peptide bond formation . A number of these compounds have been successfully used as feed additives.

Antibiotiki, 1980 Dec, 25(12), 909 - 11
{Determination of the sulfate ion content in antibiotic sulfate salts by a complexometric titration method}; Kartseva VD et al.; A possibility of assaying antibiotic sulfates, such as gentamicin, kanamycin, monomycin, neomycin, ristomycin, streptomycin, florimycin and polymyxin M sulfates for sulfate ions by titration with barium chloride in the presence of chlorphosphonaso-III, a metal indicator immediately in the salt solutions or after elimination of the cation by means of ion exchange (sulfocation exchange resins in H+-form) was tested . The procedure was shown to be adequate to the classical weight method.

Antibiotiki, 1980 Dec, 25(12), 891 - 4
{Obtaining mutants that yield tobramycin in a culture of the producer of a complex of aminoglycoside antibiotics, Streptomyces cremeus var . tobramycini var . nov . 2242.}; Siniagina OP et al.; The organism producing an aminoglycoside antibiotic complex was subjected to selection with a purpose of obtaining a strain producing tobramycin . Spontaneous and gamma-radiation-induced variation of the strains obtained as a result of a step-wise selection of the tobramycin-producing organism was studied . Correlation between the antibiotic activity levels and morphological features of these strains was shown . 8 physiological groups of mutants were differentiated and characterized as dependent on the ratio of the components in the aminoglycoside antibiotic complex produced by them . A highly productive strain 3406 was selected . The level of tobramycin synthesis by this strain is 10 times higher than that of the initial culture.

Antibiotiki, 1980 Dec, 25(12), 883 - 7
{New producer of amphomycin-group antibiotics}; Gauze GF et al.; An actinomycetous culture 33 inhibiting the growth of grampositive bacteria was isolated from a soil sample . The culture was classified as belonging to Streptomyces albogriseolus . It was found that culture 33 produced antibiotics of the amphomycin group . The antibiotic complex consists of 2 components, one of which is identical to amphomycin and the other differs from it . Conditions for the complex production were also investigated . Production of amphomycin by Str . albogriseolus was observed for the first time.

Pediatrics, 1980 Dec, 66(6), 932 - 5
Antibiotic-associated pseudomembranous colitis in siblings; Schussheim A et al.; Pseudomembranous colitis induced by antibiotics is not commonly diagnosed in children . Recent developments have clarified the pathogenesis and suggested that agents such as cholestyramine are therapeutically useful . Two siblings with pseudomembranous colitis were carefully studied and may serve to alert pediatricians to an approach to this entity.

J Trauma, 1980 Dec, 20(12), 1021 - 3
Subeschar antibiotic infusion in the treatment of burn wound infection; McManus WF et al.; In a reproducible infected rat burn model, subeschar infusion of antibiotics failed to protect the animals from death via burn wound invasion excepting those animals receiving carbenicillin . Subcutaneous injection of maximal doses of carbenicillin at a distance from the burn wound protected these animals equally well . Some advantage was defined for the subeschar route of administration with suboptimal doses of carbenicillin . More important is the fact that propective selection of an effective antibiotic could not be made on the basis of in vitro antibiotic sensitivity tests.

Gann, 1980 Dec, 71(6), 900 - 6
5-Di-(2'-tetrahydropyranyl)secalonic acid D as a new antibiotic derivative with anticancer activity; Iwaguchi T et al.; A pyranyl derivative was chemically synthesized from secalonic acid D, an antibiotic obtained from culture filtrates of Penicillium oxalium, and its anticancer activity towards a highly antigenic rat bladder cancer, BC-47, implanted into inbred ACI/N rat was studied . The anticancer effect of the drug was similar to that of adriamycin . Delayed initiation of treatment, starting 5 days after the cancer implantation, was more effective than treatment starting from day 1 . In addition, it was less effective in an immunodeficient host subsequently implanted with BC-47 . This compound is thought to retard the cancer cell growth until the appearance of tumor immunity in the host.

J Antibiot (Tokyo), 1980 Dec, 33(12), 1480 - 90
Myxothiazol, an antibiotic from Myxococcus fulvus (myxobacterales) . II . structure elucidation; Trowitzsch W et al.; Myxothiazol is shown to be 4-(6-carbamoyl-3,5-dimethoxy-4-methylhexa-1E,5E-dienyl)-2'-(1,6-dimethylhepta-2 E,4E-dienyl)-2,4'-bithiazole by spectroscopic (mainly 1H NMR, 15C NMR and mass spectroscopic) and chemical methods.

J Antibiot (Tokyo), 1980 Dec, 33(12), 1510 - 4
Studies on new aminoglycoside antibiotics, istamycins, from an actinomycete isolated from a marine environment . II . Possible involvement of plasmid in istamycin production; Hotta K et al.; Acriflavine treatment of an istamycin-producing Streptomyces tenjimariensis strain designated SS-939 resulted in a high frequency of isolates with reduced istamycin production . Some of these were shown to have lost a particular plasmid present in the parent strain . Istamycin production by these isolates was largely restored by the addition of 2-deoxystreptamine (DOS) to the medium whereas the effect of DOS was small in the strain SS-939 . Sodium palmitate also stimulated production, especially when added together with DOS . These stimulative effects by DOS and palmitate, however, were not exhibited in the presence of glucose (1.0%).

J Antibiot (Tokyo), 1980 Dec, 33(12), 1502 - 9
Studies on new aminoglycoside antibiotics, istamycins, from an actinomycete isolated from a marine environment . I . The use of plasmid profiles in screening antibiotic-producing streptomycetes; Hotta K et al.; Plasmid profiles were used to screen streptomycetes for production of new antibiotics . Among about 100 strains isolated from sea muds, an isolate designated SS-939 was revealed to harbor several plasmids of different sizes, and to produce istamycins, new aminoglycoside antibiotics . Based on the characteristics of the strain, a new Streptomyces species is proposed: S . tenjimariensis.

J Antibiot (Tokyo), 1980 Dec, 33(12), 1457 - 61
New anthracycline antibiotics produced by interspecific recombinants of streptomycetes . III . Isolation and structure of iremycin; Ihn W et al.; The structure of the anthracycline antibiotic iremycin isolated from Streptomyces violaceus subspecies iremyceticus has been elucidated as 10-(alpha-L-rhodosaminyl)-gamma-rhodomycinone (I) on the basis of spectroscopic analyses and chemical reactions.

Jpn J Antibiot, 1980 Dec, 33(12), 1285 - 93
{Studies of the real state of antibiotic consumption at an university hospital . Study in the pediatric department (author's transl)}; Fujii R et al.; Antibiotic use at the Department of Pediatrics, Teikyo University Hospital was studied from 1974 to 1978, during which period a marked change was observed in the antibiotic consumption of Japan on the whole . From the view point of net weight of antibiotics consumed, beta-lactam antibiotics have been increasing up to more than 90% of antibiotic consumption and then follow macrolides and aminoglycoside substances . Chloramphenicol which was once the top antibiotic prescribed, and tetracyclines which have not been our choice, both have become very minor antibiotics in our present prescription . More than 90% of oral antibiotics were prescribed for outpatients and more than 90% of injectable antibiotics were administered to outpatients . Concerning oral penicillins, major three were ACPC, ABPC and AMPC for these years and as to oral CEPs most of them was CEX . ABPC and the fixed combination of ABPC and penicillinase resistant penicillin, were the top choice among injectable penicillins and CEZ was the top among CEPs . Concerning aminoglycoside antibiotic SM and KM were preferred as antituberculosis drug, and GM and DKB as antipseudomonas drug which took the main role in place with CBPC and SBPC since 1976 . The type of oral drug preferred by pediatricians for prescription was also investigated and dry syrup type was found to be the most important one for pediatrics use . In spite of a steady increase of our outpatients for these five years, there was observed a remarkable decrease in number of antibiotic prescriptions, namely from 8,223 in 1974 to 4,613 in 1978 . The reason is esteemed due to our policy to restrict possibly the needless use of oral antibiotics.

Jpn J Antibiot, 1980 Dec, 33(12), 1259 - 67
{Clinical evaluation of cefoxitin against intractable bronchopulmonary infections . Patients not responding to other conventional antibiotics (author's transl)}; Yaguchi S et al.; Cefoxitin was administered to a total of 17 patients with intractable bronchopulmonary infections who had failed to respond to other conventional antibiotics, and the following results were obtained . (1) The clinical response, except 1 patient classified as evaluation impossible, was excellent in 3 patients, good in 10 and fair in 3 with an efficacy rate of 81.3% . (2) An improvement rate of more than 70% was observed in the findings of body temperature, dyspnea, colour of sputum, WBC and CRP . (3) There was no subjective nor objective side effects attributable to cefoxitin . In view of the results stated above, we have concluded that cefoxitin is a useful antibiotic for the treatment of intractable bronchopulmonary infections.

Am J Gastroenterol, 1980 Dec, 74(6), 493 - 6
Modification of endoscopic retrograde cholangiopancreatography (ERCP) septic complications by the addition of an antibiotic to the contrast media . Randomized controlled investigation; Collen MJ et al.; We studied the efficacy of gentamicin or placebo to decrease the incidence of septic complications after ERCP in 61 inpatients with possible pancreatic or biliary tract disease . The antibiotic or placebo was added to the Renograffin-60 contrast media and the study was conducted in a randomized controlled fashion . There were 29 patients who received gentamicin and 32 patients who were in the placebo group . No patient received parenteral antibiotic prior to, during, or after the ERCP unless a septic complication developed and each was followed daily with complete blood counts and oral temperatures . The incidence of febrile episodes in the gentamicin group was one (3%) . All blood cultures were negative . One patient (3%) in the placebo group developed a febrile episode with subsequent blood cultures growing Escherichia coli . There was no statistical difference in the incidence of septic episodes between the two study groups . The results of this study demonstrate that the incidence of septic complications during ERCP is not modified by the addition of gentamicin to the contrast media.

J Pharmacol Methods, 1980 Dec, 4(4), 285 - 9
An animal model for assessing pain-on-injection of antibiotics; Celozzi E et al.; The paw-licking response of rats to a subplantar injection of an antibiotic was used as an indicator of the pain caused by that antibiotic . Good agreement with clinical findings was obtained with cefoxitin, cephalothin, cephradine, cefazolin, cephaloridine, and carbenicillin . Incorporation of a local anesthetic into the diluent of an irritating antibiotic reduced the number of paw-licking episodes . This rat paw model offers a simple and rapid means of estimating pain-on-injection following intramuscular injection of antibiotics to humans and may be applicable to other drugs as well.

J Antibiot (Tokyo), 1980 Dec, 33(12), 1527 - 31
In vivo and in vitro cross-resistance of kanamycin-resistant mutants of E . coli to other aminoglycoside antibiotics; Choi EC et al.; Cross resistance of kanamycin-resistant mutants of E . coli Q13 to other aminoglycosides (streptomycin, neomycin, gentamicin and dibekacin) was demonstrated in vivo (growth) and in vitro (polyphenylalanine synthesis, codon misreading and translocation on the ribosomes) . Kanamycin-resistant mutants, R1-4, R2-1, R2-2, R3-3 and R3-5 showed various degrees of cross-resistance to streptomycin, gentamicin, neomycin and dibekacin in vivo . In vitro, polyphenylalanine synthesis was more resistant to kanamycin, streptomycin, neomycin and gentamicin on the ribosomes of the kanamycin-resistant mutants than on those of the parental strain . In the presence of kanamycin, neomycin or gentamicin, less degrees of {14C}isoleucine uptake with poly{U} (codon misreading) were observed on the ribosomes obtained from the resistant mutants than on the sensitive cell ribosomes . The N-acetyl-{14C}phenylalanyl-puromycin synthesis enhanced by an elongation factor, EF-G and GTP (translocation) was more resistant to kanamycin and dibekacin on the mutant ribosomes than on the parental ribosomes . The results indicate that the cross-resistance to other aminoglycoside antibiotics, as well as the kanamycin resistance, are attributed to mutational alterations of the ribosomes in these mutants.

Can J Microbiol, 1980 Dec, 26(12), 1465 - 72
The effect of R plasmids and antibiotics on the UV recovery of Escherichia coli strain B; LaBrie DA; A R-plasmid-containing fil mutant of Escherichia coli strain B, when exposed to chloramphenical (CMP) plus streptomycin (Sm) after irradiation, achieved 100% ultraviolet (UV) recovery from doses that otherwise kill over 90% of the cells . UV-induced filament cells with R plasmids are very UV sensitive regardless of the treatment after the filament-inducing irradiation . The exposure to CMP and Sm can be delayed after irradiation and still rescue filament cells from UV death even when grown on antibiotic-free agar . Development of UV-induced filament cells in CMP-Sm liquid medium increases the number of irradiated cells that will recover the ability to divide even when transferred to antibiotic-free agar soon after irradiation . The results suggest that the recovery of cell division by UV-induced filaments with R plasmids can be accomplished by contact with antibiotics even after extensive "unbalanced growth" or by growing in liquid medium throughout a critical period following irradiation.

Helv Chir Acta, 1980 Dec, 47(5), 659 - 62
{Antibiotic preparation of the colon or preoperative parenteral prophylaxis in colon surgery . A randomized study}; Fluckiger M et al.; A double-blind randomised trial was carried out among 72 patients undergoing elective colorectal surgery . 37 patients received Metronidazole and Kanamycin systemically, 35 patients the same medicaments orally . We could not find any difference between the two ways of application . These results are in opposition to those of a comparable study of Birmingham, where the therapy was significantly less successful in the oral group . This fact is discussed and the parenteral, short-term prophylaxis is recommended.

Tubercle, 1980 Dec, 61(4), 213 - 9
beta-Lactamase activity in slow-growing nonpigmented mycobacteria and their sensitivity to certain beta-lactam antibiotics; Kasik JE et al.; It has been reported that certain nonpigmented, slow-growing mycobacteria do not have a constitutive beta-lactamase and are more sensitive to benzyl penicillin than M . tuberculosis . Thirty-nine isolates of these organisms, most of them belonging to the M . avium-intracellulare complex, were found to be sensitive to less than 10 micrograms of benzyl penicillin per ml in vitro . Approximately half of these isolates were inhibited by 1 microgram per ml . By contrast of 32 isolates of M . tuberculosis, only one was inhibited by 10 micrograms of benzyl penicillin . Sensitivity studies with cephalothin yielded similar results . Analysis of beta-lactamase activity in some of these species showed no activity, confirming earlier observations of this deficit.

J Antibiot (Tokyo), 1980 Dec, 33(12), 1474 - 9
Myxothiazol, an antibiotic from Myxococcus fulvus (myxobacterales) . I . Cultivation, isolation, physico-chemical and biological properties; Gerth K et al.; Myxothiazol (AB-Mx f16-1), a new antifungal antibiotic, is produced by the myxobacterium Myxococcus fulvus strain Mx f16 . It is active against many filamentous fungi, and completely inhibits growth of Mucor hiemalis at a concentration of 2 micrograms/ml . The molecular formula of myxothiazol was determined to e C25H33N3O3S2.

Arch Microbiol, 1980 Dec, 128(2), 196 - 203
Analysis of the physiological effects of the antibiotic streptozotocin on Escherichia coli K 12 and other sensitive bacteria; Lengeler J; The antibiotic streptozotocin under a variety of growth conditions rapidly and irreversibly inactivates the capacity to divide or to form colonies of a series of sensitive bacteria, containing the phosphoenolpyruvate-dependent sugar-phosphotransferase system . Cells can be sensitized towards the drug by pregrowth in N-acetyl-glucosamine and can be protected by adding this amino-glucoside to the medium . Starvation for energy, especially for phosphoenolpyruvate, or prevention of the induction of a transport system involved in streptozotocin uptake will protect the cells, while a block in protein synthesis does not . The killed cells neither lyse, nor are they transformed into spheroplasts . At first, the capacity of such "dead" cells to respire, to swim actively or to keep the cytoplasmic membrane impermeable for small molecules remains intact . Their capacity for over-all RNA and protein synthesis, and for carbohydrate and amino acid uptake by facilitated diffusion or active transport is not affected . However, they loose rapidly their ability to take up carbohydrates by the phosphoenolpyruvate dependent process of group translocation or to synthesize inducible enzymes, e.g . the enzyme beta-galactosidase . These inhibitory effects apparently are caused by the accumulation of phosphorylated, toxic derivatives of the antibiotic and eventually lead to a pronounced bacteriostasis . Killing of the cells seems to be caused by a direct effect of the strongly mutagenic drug on replicating DNA.

Antibiotiki, 1980 Dec, 25(12), 887 - 91
{Obtaining a productive strain of Streptoverticillium griseocarneum var . bleomycini that yields the new antineoplastic antibiotic, bleomycetin}; Pogozheva VV et al.; Selection of the organism producing bleomycin, a multicomponent antitumor antibiotic, was performed . The aim was the selection of a more active strain with preferable synthesis of component A5 (bleomycetin) of the bleomycin complex . Optimal variants of the conditions for mutagensis with UV light and gamma-rays in step-wise selection of the active strain were determined and a possibility of selecting analog-resistant mutants with the use of structural analogs of the metabolites participating in synthesis of the bleomycin molecule was studied . A mutant analog-resistant strain capable of supersynthesis of bleomycin A5 (bleomycetin) was selected, the biosynthetic capacity of Streptoverticillum griseocarneum var . bleomycini being increased at least 19 times.

N Z Med J, 1980 Nov 26, 92(672), 378 - 9
Vitamin K deficiency developing in patients with renal failure treated with cephalosporin antibiotics; Reddy J et al.; Five patients developed vitamin K-related abnormalities in blood coagulation during treatment with parenteral cephalosporin or cephamycin antibiotics . All the patients had significantly impaired renal function and complicated medical problems . The coagulation defect was corrected with vitamin K therapy.

Biochemistry, 1980 Nov 25, 19(24), 5537 - 42
Interactions of a new antitumor antibiotic BBM-928A with deoxyribonucleic acid . Bifunctional intercalative binding studied by fluorometry and viscometry; Huang CH et al.; A new actinoleukin-like antitumor antibiotic, BBM-928A, has been shown to interact with isolated DNA molecules . BBM-928A contains two substituted quinolines linked by a cyclic decapeptide . Quenching effects of the covalently closed superhelical PM2 DNA on the BBM-928A fluorescence revealed a strong interaction with an apparent association constant of 1.93 x 10(7) M-1 and with 11 deoxyribonucleic acid (DNA) nucleotides per BBM-928A binding site . Viscometric studies indicated the BBM-928A induced an unwinding-rewinding process of the closed superhelical PM2 DNA typically observed for DNA intercalators . The unwinding angle (43 degrees) induced by BBM-928A was almost twice that of the ethidium bromide (26 degrees), a monofunctional intercalator . The BBM-928A-induced increase of the helix length of sonicated rodlike calf thymus DNA was approximately 1.5-fold that induced by the ethidium bromide . On the basis of these observations, we concluded that BBM-928A bifunctionally intercalated with DNA in a manner similar to the bifunctional intercalation of echinomycin.

J Pharm Sci, 1980 Nov, 69(11), 1282 - 4
Effects of antibiotics on platelet functions in human plasma in vitro and dog plasma in vivo; Genua MI et al.; The effects of 31 antibiotics on platelet aggregation in human plasma in the presence of adenosine 5'-diphosphate were studied . The marked activity of tetracycline hydrochloride led to a study of its effects on various platelet functions in vivo in dogs.

Antibiotiki, 1980 Nov, 25(11), 831 - 4
{Spectrophotometric method of determining aminoglycoside antibiotics}; Alykov NM; Azo-derivatives of chromotropic acid and azo-dyes of the stilbene series were studies as possible reagents for photometric determination of aminoglycoside antibiotics (AB) in biological materials . The complex of Pr3+ with stilbazochrome-P (Sch-P) proved to be the best precipitant of AB . P (Sch-P) with Pr3+ and AB in acetate and citrate buffer-solutions formed a precipitate with AB:Pr:Sch-P = 1 : 1 : 3 . Most of the metallic cations and anions did not prevent formation of the precipitate in the citrate buffer . A procedure for determination of 0.01--100 micrograms of AB in biological materials was developed with the use of Sch-P . The procedure is based on separation of the AB:Pr:Sch-P precipitate and photometry of the sypernatant solution at 560 nm.

Clin Pediatr (Phila), 1980 Nov, 19(11), 753 - 60
Predicting fever response of children with pneumonia treated with antibiotics; McCarthy PL et al.; In order to study predictors of fever response in children with radiologic pulmonary infiltrates treated with antibiotics, 156 children with pneumonia were evaluated with slide test C-reactive protein (CRP), white blood cell count (WBC), erythrocyte sedimentation rate (ESR), blood cultures, acute and convalescent viral and mycoplasma titers, and then followed clinically . Both CRP (+) at a serum dilution of 1:50 and WBC greater than or equal to 15,000 were better predictors of rapid resolution of fever while the patient was receiving antibiotics than were ESR greater than or equal to 30 or temperature greater than or equal to 40 C . WBC greater than or equal to 15,000 was nearly as specific but more sensitive than CRP (+) 1:50 for resolution of fever in either 8, 12 or 24 hours . Positive blood or lung bacterial cultures, but not four-fold or greater viral or mycoplasma titer increases, were also associated with rapid resolution of fever . WBC greater than or equal to 15,000 is useful in predicting rapid fever response in children with pneumonia treated with antibiotics.

J Antibiot (Tokyo), 1980 Nov, 33(11), 1316 - 22
Biosynthesis of the boron-containing antibiotic aplasmomycin . Nuclear magnetic resonance analysis of aplasmomycin and desboroaplasmomycin; Chen TS et al.; The 360 MHz 1H NMR spectra of the boron-containing macrolide antibiotic Aplasmomycin and of desboroaplasmomycin were analyzed to extract most of the parameters revealing the conformations of these compounds in CDCl3 solution . It was found than the conformation of aplasmomycin in CDCl3 solution is identical to that in the solid state and that removal of the boron atom from aplasmomycin results only in a slight conformational change of the molecule in CDCl3 . All resonances observed in the 13C NMR spectrum of the antibiotic have been assigned on the basis of chemical shift theory, multiplicity analyses, single frequency proton decoupling experiments, comparison with several derivatives and model compounds, specific deuteration experiments, and analysis of one-bond carbon-carbon couplings of pairs of carbon atoms.

J Antibiot (Tokyo), 1980 Nov, 33(11), 1220 - 3
Malioxamycin, a new antibiotic with spheroplast-forming activity . II . Structural elucidation and total synthesis; Takahashi S et al.; Malioxamycin (1) is a new antibiotic produced by Streptomyces lydicus No . 15748 . The structure of malioxamycin has been determined by nmr and mass spectra to possess a hydroxamic acid bond between L-valine and D-malic acid . This structure was confirmed by total synthesis of the antibiotic with (R)-aminooxysuccinic acid and the active ester of L-valine.

Antimicrob Agents Chemother, 1980 Nov, 18(5), 832 - 3
Susceptibility of Eikenella corrodens to newer beta-lactam antibiotics; Goldstein EJ et al.; In vitro susceptibility testing of 28 strains of Eikenella corrodens by the agar dilution technique showed that all strains were uniformly susceptible to penicillin, ticarcillin, cefoxitin, cefotaxime, N-formimidoyl thienamycin, and moxalactam and resistant to clindamycin and cefadroxil . Cefoperazone, piperacillin, and mezlocillin showed good activity, with some strains relatively resistant . Bacampicillin and cefamandole showed relatively poor activity.

Antibiotiki, 1980 Nov, 25(11), 860 - 4
{Action of the antitumor antibiotics, rubomycin and carminomycin, on the T- and B-cell population ratio in mouse lymphoid organs}; Vatin AE; Quantitative ratios of T- and B-cells in the lymphoid organs of mice were studied comparatively at various periods after administration of rubomycin and carminomycin in maximum tolerated doses, i . e . 20 and 3 mg/kg . It was found that the antibiotics decreased the total number of the cariocytes in these organs and induced irregular elimination of T- and B-cells from the spleen and lymph nodes . Comparison of the time-course of T- and B-lymphocyte population reduction suggested that the cells reduced independently of each other, the reduction rate of B-cells being higher than that of T-cells.

J Antibiot (Tokyo), 1980 Nov, 33(11), 1331 - 40
Biosynthesis of anthracycline antibiotics by Streptomyces galilaeus . I . Glycosidation of various anthracyclinones by an aclacinomycin-negative mutant and biosynthesis of aclacinomycins from aklavinone; Oki T et al.; An aclacinomycin-negative mutant strain KE303 which required aklavinone aglycone for the production of anthracycline antibiotics was derived from Streptomyces galilaeus, and employed for the glycosidation of various anthracyclinones . epsilon- gamma- and beta-Rhodomycinones, epsilon-isorhodomycinone, epsilon- and beta-pyrromycinones and chemically modified aklavinones were found to be glycosidated to the biologically active anthracyclines, when they were fed to the growing culture . However, the feeding of daunomycinone, 13-deoxydaunomycinone, adriamycinone and steffimycinone did not yield any glycoside . The bioconversion of presumptive precursor glycosides revealed that aclacinomycin A is biosynthesized by the step-wise glycosidation from aklavinone vai aklavin and MA144 S1.

J Antibiot (Tokyo), 1980 Nov, 33(11), 1323 - 30
Chemical modification of anthracycline antibiotics . I . Demethoxycarbonylation, 10-epimerization and 4-o-methylation of aclacinomycin A; Tanaka H et al.; Demethoxycarbonyl derivatives of aclacinomycin A and of its 7-epimer, 10-epi-aclacinomycin A and 4-O-methylaclacinomycin A were chemically derived from aclacinomycin A . The cytotoxicity and inhibitory effects of RNA and DNA synthesis in cultured L1210 leukemia cells of the 4-O-methyl derivative approximated that of aclacinomycin A, while the demethoxycarbonyl derivatives and 10-epi-aclacinomycin A exhibited decreased activities in comparison with the parent compound.

J Pharm Sci, 1980 Nov, 69(11), 1334 - 8
Structure-activity relationships of pyrrole amidine antiviral antibiotics III: preparation of distamycin and congocidine derivatives based on 2,5-disubstituted pyrroles; Bialer M et al.; Isomers of distamycin A and tripyrrole congocidine containing 2,5-disubstituted pyrroles were synthesized along with distamycin and congocidine homologs containing a single pyrrole ring . Selected compounds were evaluated for their cytotoxicity and antiviral activity . All of the tripyrrole derivatives tested in this series were nontoxic but were less active than distamycin A . The monopyrrole derivative, N-methyl-5-nitropyrrole-2-carboxamido-beta-propionamidine hydrochloride, was nontoxic and was almost as active antivirally as distamycin A.

Ann Intern Med, 1980 Nov, 93(5), 709 - 11
Acute meningoencephalitis after withdrawal of antibiotics in Whipple's disease; Feldman M et al.; Publication Types:

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