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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