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J Antibiot (Tokyo), 1980 Dec, 33(12), 1417 - 24 C-19393 S2 and H2, new carbapenem antibiotics . I . Taxonomy of the producing strain, fermentation and antibacterial properties; Imada A et al.; C-19393 S2 and H2 are new carbapenem antibiotics produced by a streptomycete . The producing strain was taxonomically studied and named Streptomyces griseus subsp . cryophilus . Cobaltous compounds were necessary for production of the antibiotics . C-19393 S2 and H2 showed a broad spectrum of antibacterial activities with C-19393 H2 being 8 approximately 120 times more active than C-19393 S2 . They also exhibited beta-lactamase-inhibiting activities and acted synergistically with ampicillin and cefotiam against clinical isolates resistant to beta-lactam antibiotics. S Afr Med J, 1980 Nov 22, 58(21), 846 - 8 Medicine compliance in paediatric outpatients; de Wet B et al.; In a study of children attending the outpatient department of the Red Cross War Memorial Children's Hospital it was found that less than one-quarter of the medicines dispensed were correctly taken . Antibacterials, the most frequently ordered medications, had the poorest compliance rates . Furthermore, in this group the parent least understood the purpose of the prescribed preparation . The best compliance was obtained when the purpose was well understood. Experientia, 1980 Nov 15, 36(11), 1325 - 6 The synthesis of antibacterial proteins in isolated fat body from Cecropia silkmoth pupae; Faye I et al.; Fat body from previously immunized diapausing pupae of the silkmoth, Hyalophora cecropia (Saturniidae), incubated in vitro, released antibacterial activity into the medium and incorporated 3H-leucine into the immunity proteins P1-P9 . The release of antibacterial activity from fat body was also induced to some extent by injection of Ringer solution and, after 20 h in culture, by the injury of dissection. Biochim Biophys Acta, 1980 Nov 5, 593(1), 1 - 10 Relation of aerobiosis and ionic strength to the uptake of dihydrostreptomycin in Escherichia coli; Campbell BD et al.; Aminoglycoside antibiotics exhibit a markedly reduced antibacterial activity under anaerobic conditions . Anaerobiosis or inhibitors of electron transport produced an extensive decrease in the uptake of dihydrostreptomycin in Escherichia coli K-12 . Uptake of proline or putrescine were only slightly impaired under anaerobic conditions in the presence of glucose . Both the susceptibility to and the uptake of dihydrostreptomycin under anaerobic conditions were partially restored by addition of the alternative electron acceptor, nitrate . This stimulation required functional nitrate reductase activity . Abolition of uptake by 2,4-dinitrophenol under both aerobic and anaerobic conditions indicates that streptomycin uptake requires electron transport as well as a sufficient membrane potential . In addition, the initial rate of dihydrostreptomycin uptake was competitively and reversibly inhibited by added salts . The inhibition was relatively nonspecific with respect to the identity of salt added, being approximately dependent on the ionic strength . Although dihydrostreptomycin and polyamines mutually inhibited each other's uptake, several conditions (polyamine limitation, streptomycin uptake-deficient mutants) were found in which uptake of these two substrates was oppositely affected . Amino-glycosides thus do not appear to enter on one of the usual cellular transport systems, but perhaps utilize a component of the electron transport system. Pediatr Res, 1980 Nov, 14(11), 1212 - 5 Pulmonary nonspecific defense mechanisms in cystic fibrosis . I . Phagocytic capacity of alveolar macrophages and neutrophils; Cassino RJ et al.; Cystic fibrosis (CF) is the commonest cause of chronic obstruction lung disease within the first three decades of life . Because patients suffer from repeated pulmonary infections, we were interested in studying the nonspecific antibacterial mechanisms of the lungs of CF children . Fifteen CF children, 13 nontuberculous pulmonary-infected (I) children and 4 noninfected (N-I) children, who were diagnosed as having a foreign body in the air passages, were submitted to a bronchopulmonary washing . The absolute number, viability, and differential count of the cells were determined, and the phagocytic assay using the Lehrer's technique was carried out on the harvested cells . The materials obtained from CF and I patients were mucopurulent, whereas the ones from the N-I patients were not mucopurulent . The number of cells retrieved from CF and I patients was higher than that from the N-I patients . This was attributed to an increase in the absolute number of polymorphonuclear leukocytes . The phagocytic capacity of polymorphonuclear leukocytes was not different for the three groups studied, whereas that of alveolar macrophages was higher for the CF and the I patients than for the N-I ones . Inasmuch as there was no significant difference between the CF and the I patients, we conclude that the nonspecific phagocytic behavior of alveolar macrophages and pulmonary polymorphonuclear leukocytes of CF patients might be similar to the one coming from other bacterial infectious states of the lung. J Pharm Sci, 1980 Nov, 69(11), 1313 - 7 Synthesis and evaluation of substituted quinazolone derivatives for antibacterial, antifungal, and antiacetylcholinesterase activities; Gupta AK et al.; The synthesis of new 6-bromo- and 6,8-dibromo-2-{N-(2'-alkyl-1',3',4'-thiadizol-5'-yl)carbamoylmethylthio} -3-aryl/cyclohexyl-4-(3H)-quinazolones is described . The synthesis derivatives were screened for antibacterial, antifungal, and antiacetylcholinesterase activities in vitro . Most of the compounds exhibited significant biological activity . The relation between their biological activity and chemical structure was studied. Ann Thorac Surg, 1980 Nov, 30(5), 427 - 32 Clinical evaluation of bronchopulmonary lavage using the flexible fiberoptic bronchoscope; Garvey J et al.; Thirty-three patients had segmental and lobar bronchopulmonary lavage using three types of flexible fiberoptic bronchoscopes . A maximum volume of 300 ml of normal saline solution at room temperature was used . Lavage was effective for removing large numbers of alveolar macrophages (mean, 17 million) and proteinaceous material (mean, 0.18 mg per milliliter) that helped enhance the antibacterial properties of the macrophages . Transient shunting (mean fall in partial pressure of arterial oxygen, 65 mm Hg) and alveolar filling that reverted to normal in 3 hours were noted . The procedure averaged 45 minutes and was as simple as bronchoscopy . The larger the internal diameter of the bronchoscope (> 2.6 mm) the better suited it was for lavage . Sequential segmental lavage seems to offer the advantages of simplicity and technical ease over isolated lobar lavage with a balloon-tipped bronchoscope . It also has the advantage of simplicity over whole-lung lavage. Br J Anaesth, 1980 Nov, 52(11), 1097 - 100 Do neostigmine and 4-aminopyridine inhibit the antibacterial activity of antibiotics? Booij LH, van der Ploeg GC, Crul JF, Muytjens HL. Neostigmine and 4-aminopyridine are used to antagonize the neuromuscular blockade induced by antibiotics or an antibiotic-non depolarizing blocker combination . They may also counteract the antibacterial activity of antibiotics . It was found that neostigmine and 4-aminopyridine do not interfere with antibacterial activity of antibiotics in bacterial cultures using an agar solution method . It is concluded that neostigmine and 4-aminopyridine may bae used to antagonize neuromuscular blockade induced by antibiotics alone or in combination with non-depolarizing agents. J Antibiot (Tokyo), 1980 Nov, 33(11), 1352 - 6 Synthesis and biological activity of a new semisynthetic cephalosporin, CN-92,982; Mich TF et al.; A new broad spectrum semisynthetic cephalosporin (CN-92,982) was prepared from the condensation of an acetylaminoacylaminophenyl pyridone with trans-7-{(D-2-phenylglycyl) amino}-3-{{(1-methyl-1H-tetrazol-5-yl)thio}methyl}-delta 3-cephem-4-carboxylic acid . The new cephalosporin displayed an in vitro antibacterial spectrum similar to other cephaloglycine types such as cefoperazone and SM-1652 . The compound produced a high and prolonged blood level following a single intramuscular dose in a dog. J Antibiot (Tokyo), 1980 Nov, 33(11), 1231 - 5 A new antibiotic K-82 A and minor components, produced by Streptomyces lavendulae, strain No . K-82; Shibata M et al.; From the results of taxonomic studies, Streptomyces sp . strain No . K-82 isolated from a soil sample collected in Kumamoto city, was identified as a strain belonging to Streptomyces lavendulae WAKSMAN & HENRICI 1948 . The strain produced an active new antibiotic called K-82 A and minor components named the B complex . Antibiotic K-82 A was isolated as dark reddish needles by silica gel column chromatography and found to have both antibacterial activity and high phage induction activity . The K-82 B complex was found to consist of at least five components, among which K-82 B2 and B3 were isolated as crystals . Substances K-82 B2 was identified as benzoic acid from its physicochemical properties . Substance B3 like B2 had only marginal antibiotic activity. J Med Chem, 1980 Nov, 23(11), 1205 - 12 Quantitative structure-selectivity relationships . Comparison of the inhibition of Escherichia coli and bovine liver dihydrofolate reductase by 5-(substituted-benzyl)-2,4-diaminopyrimidines; Dietrich SW et al.; A quantitative structure-activity relationship (QSAR) has been formulated for the inhibition of purified E . coli dihydrofolate reductase by 23 5-(substituted benzyl)-2,4-diaminopyrimidines: log 1/C = 1.14MR'3,4,5 + 5.73; r = 0.887; s = 0.285 . In this expression, MR'3,4,5 refers to the sum of MR values for X in the 3, 4 and 5 positions of the phenyl moiety . MR' signifies that the effective value of MR is limited to 0.79 . Comparison of the QSAR for E . coli enzyme inhibition with that previously obtained for bovine enzyme offers the first general explanation for the great selectivity of the important antibacterial agent trimethoprim . Such QSSR promise to be of value in devising more selective drugs. Nouv Presse Med, 1980 Oct 25, 9(39), 2909 - 14 {Current trends in antibacterial chemotherapy (author's transl)}; Bergogne-Berezin E; Antibiotics account for about 15% of world pharmaceutical consumption, but with the rapid development of antibacterial agents capable of reaching most bacterial cell target structures, many bacterial species have become resistant, including S . pneumoniae, H . influenzae and N . gonorrhoeae, which until recently had remained susceptible to penicillin . Moreover, intrinsically resistant species have been selected and are now responsible for nosocomial infections . These shortcomings of chemotherapy, as well as the toxicity and side-effects of a number of drugs, have prompted a search for antibiotics with wider spectrum, lesser sensitivity to bacterial enzymes, reduced toxicity and improved pharmacokinetic properties . During the last 20 years, attempts to extract new antibiotics from natural sources have met with little success, but considerable progress has been achieved in the hemisynthesis of known molecules, such as 6-aminopenicillanic acid or 7-aminocephalosporanic acid, and various changes in these molecules have yielded a variety of new beta-lactam compounds, some of which being still under study and other in clinical use . Changes in the original aminoglycoside molecules have also produced compounds that are less toxic and less susceptible to inactivating enzymes . Among macrolides and sulfonamides, recent developments, although limited, have led to new products or to synergistic combinations . Finally, the search for new compounds which would inhibit two successive steps in the bacterial metabolic pathways constitutes a modern, rational and promising approach to antibacterial chemotherapy. S Afr Med J, 1980 Oct 11, 58(15), 598 - 9 Xylose absorption in infants with severe prolonged diarrhoea; Mann MD et al.; Energy supply may be a limiting factor in tissue repair when infants with severe prolonged diarrhoea are fed orally . Xylose tolerance tests were done on 8 female infants who had had severe dehydrating diarrhoea requiring treatment in hospital for 7 days . Seven infants had flat xylose tolerance curves, 5 of these being at very low levels . Very early intervention with hyperalimentation, elemental diets or antibacterial agents and basic anion exchange resins may reduce morbidity. J Med Chem, 1980 Oct, 23(10), 1108 - 13 Synthesis and antibacterial activity of new 1-oxa-1-dethiacephalosporins; Hagiwara D et al.; A series of 3-(deacetoxymethyl)-1-oxa-1-dethiacephalosporins (1) bearing the 7-(alpha-alkoxyimono)acyl side chain were synthesized and their antibacterial properties were examined in comparison with that of FK-749 (2) . (Z)-2-(Ethoxyimino)-2-(2 aminothiazol-4-yl)acetic acid was found to be a prefered side chain in the 1-oxa series, and the derivative 18b with this side chain proved to be a potential broad-spectrum antibiotic not at all inferior to 2. J Pharm Sci, 1980 Oct, 69(10), 1180 - 3 Antibacterial and antifungal activity of liriodenine and related oxoaporphine alkaloids; Hufford CD et al.; Liriodenine was evaluated for its antibacterial and antifungal activity against several microorganisms . Other related oxoaporphine alkaloids also were evaluated . Attempts to prepare oxoaporphine alkaloids from N-acetylnoraporphines were unsuccessful, but an unexpected phenanthrene alkaloid was obtained . A novel N-demethylation reaction was noted when oxogaucine methiodide and liriodenine methiodide were treated with alumina. Int J Clin Pharmacol Ther Toxicol, 1980 Oct, 18(10), 431 - 6 Role of antibacterial chemotherapy in the management of chronic bronchial obstructive disease; Gialdroni-Grassi G; Some aspects of antibiotic treatment in chronic bronchial obstructive disease are taken into consideration . The importance which can be attributed to the levels that antibiotics attain in bronchial secretions is discussed particularly as well as the factors which can influence them . The relevance of their adequate concentrations in bronchial secretions to the therapeutic results also is considered . The role which, in different ways, the behaviour of bacteria responsible for bronchial infections can play in conditioning the activity of antibacterial agents is another point that has attracted attention . The assessment of the importance that each one of these factors can have both in the development and in the treatment of the disease, as well as the integration of chemotherapy with other pharmacological and physiotherapic means, are the basis that will allow a more rational treatment of chronic bronchial obstructive disease. Arch Dis Child, 1980 Oct, 55(10), 817 - 9 Barrier properties of vernix caseosa; Joglekar VM; Experiments are described which show that vernix caseosa has a mechanical barrier effect if it is deposited in an unbroken layer . Specific antibacterial properties were not detected in vernix . It is suggested that vernix is best left on a newborn infant because of its mechanical obstruction to bacterial passage. J Antibiot (Tokyo), 1980 Oct, 33(10), 1177 - 82 Semisynthetic beta-lactam antibiotics . III . Cephalosporin derivatives in the furyl series . Chemical and microbiological properties; Tinti MO et al.; The synthesis of a series of 7-acylamido cephalosporins having a substituted furyl moiety in the side chain is described . These new cephalosporins were examined in vitro for antibacterial activity and evaluated for resistance to inactivation by beta-lactamases. Antimicrob Agents Chemother, 1980 Oct, 18(4), 604 - 9 Animal model distinguishing in vitro from in vivo carbenicillin-aminoglycoside interactions; Pieper JA et al.; Aminoglycosides and carbenicillin are frequently co-administered to patients with serious gram-negative infections . Aminoglycosides are inactivated by carbenicillin in vitro, and a loss of antibacterial activity of both antibiotics results . Although these interactions are presumed to occur in vivo, previous studies have not used assay methodology that can distinguish inactivation occurring prior to and during microbiological assay from inactivation in vivo . To address this problem, we gave seven bilaterally nephrectomized mongrel dogs doses designed to achieve simultaneous therapeutic serum concentrations of aminoglycosides and carbenicillin . Serum samples were tested by radioimmunoassay on three occasions: immediately, to determine in vivo interactions, and at 24 h and 1 week to assess the time course of in vitro inactivation . In comparison with immediate radioimmunoassay, gentamicin and tobramycin concentrations decreased by 39 and 53%, respectively, when assayed at 24 h (P < 0.05) and by 75 and 82% when assayed at 7 days (P < 0.001) . In contrast, amikacin concentrations were reduced by only 9 and 30% at 24 h and 7 days . Tobramycin concentrations were also determined by immediate microbiological assay and were found to be similar to those in samples stored for 24 h before radioimmunoassay . Immediate radioimmunoassay demonstrated that carbenicillin reduced in vivo serum half-lives of gentamicin and tobramycin by 40% (P < 0.05) . The half-life of amikacin in vivo was not significantly altered . In the presence of carbenicillin, amikacin was the most stable aminoglycoside both in vivo and in vitro, and it is the aminoglycoside of choice in patients with renal failure who require this combination. Arch Sci Med (Torino), 1980 Oct-Dec, 137(4), 767 - 74 {Experimental studies on the bactericidal activity of formaldehyde}; Finzi G et al.; A modified version of the contact test was used to assess the activity of a 1.2% and a 2.4% aqueous solution of formaldehyde against 14 hospital and standard bacterial strains . Generally speaking, there was average antibacterial activity for contact times in the 15-30 min range, while excellent activity was observed when longer periods were employed. J Pharmacol, 1980 Oct-Dec, 11(4), 411 - 25 {Clofoctol binding by the bacteria (author's transl)}; Combe J et al.; Clofoctol is an antibacterial agent which is active only on Gram + bacteria . The clofoctol binding on bacteria is fast and the number of molecules bound is about 10(6) to 1,5 10(7) molecules per bacteria . Bacteria sensitivity towards clofoctol is the result of their ability to bind with it . Gram negative and Gram + protoplasts of bacteria bind the clofoctol . Binding of clofoctol by B . subtilis is obtained with viable cells and also with thermal inactivated cells . Binding of clofoctol by the cells is reversible and we showed that the 14C clofoctol used for the experiments and the unlabelled clofoctol have the same behaviour . ions as K+, Mg++, Ca++, Mn++, and Fe++, pH variation between 2 to 9, and urea have no influence on the binding of clofoctol by the bacteria, but, sodium lauryl sulfate is an inhibitor of the binding . These results mean that clofoctol bounds are made by hydrophobic links. Vet Rec, 1980 Sep 20, 107(12), 277 - 80 A comparison of the antibacterial action of five udder washes; Davies ME et al.; Five commercially available udder washes were tested for antibacterial action . Four contained iodine and one chlorhexidine . Each product was used exclusively for 10 days and its bactericidal action compared with that of water . Bactericidal activity was demonstrated in all five washes but the chlorine based product performed better than the iodine washes . However, the results suggested that the skin of cows' teats can be cleansed with water as effectively as with an added product. Boll Soc Ital Biol Sper, 1980 Sep 15, 56(17), 1758 - 64 {In vitro and in vivo antibacterial activity of cephapirin-dicloxacillin combination in the ratio 1:1}; Di Sipio L et al.; Studies were carried out on the combination, 1:1 ratio, of two antibiotics: cephapirin and dicloxacillin . After the analysis of the activity spectrum "in vitro" of each antibiotics, the synergism of this combination against the Gram-negative bacteria strains was clearly demonstrated . This combination demonstrated a particular activity against the beta-lactamases producing strains "in vitro" as well in protection tests "in vivo" in experimental infections in mice. Can J Microbiol, 1980 Sep, 26(9), 1104 - 13 The formation of microcolonies by rumen bacteria; Cheng KJ et al.; When rumen fluid is fixed for electron microscopy, without centrifugation, a large amount of material sediments spontaneously and ruthenium red staining shows this material to be partially composed of bacterial microcolonies in which morphologically similar sister cells are enclosed in an extensive fibrous exopolysaccharide glycocalyx . The exopolysaccharide matrix condenses, to variable degrees, during the dehydration steps of specimen preparation for electron microscopy but some fibers are stabilized by their attachment to solid surfaces at multiple points and the extent of this matrix can be deduced from morphological data . Even after condensation, the glycocalyces of rumen bacteria occupy more space than the cells themselves and they completely surround most cells with a fibrous matrix, whose chemical composition dictates an ion-exchange function, that must be assumed to be protective against some bacteriophage and antibacterial agents. J Antibiot (Tokyo), 1980 Sep, 33(9), 931 - 9 Tetronic acid derivatives from Aspergillus panamensis . Production, isolation, characterization and biological activity; Anke H et al.; When Aspergillus panamensis, CBS 120.45, was grown on a medium with high carbon and low nitrogen content, it was found to produce six antibiotically active metabolites . All compounds were identified as tetronic acid derivatives; three of them were found to be identical with gregatins A, B, and D, previously reported as metabolites of Cephalosporium gregatum . The other three compounds are new . All six compounds show antibacterial activity towards Gram-negative and Gram-positive bacteria . Five of the antibiotics exhibit inhibitory effects on the macromolecular syntheses in cells of the ascitic form of EHRLICH carcinoma (ECA) of mice. Plast Reconstr Surg, 1980 Sep, 66(3), 361 - 8 Clinical evaluation of the Hydron burn dressing; Warren RJ et al.; Hydron, a synthetic barrier dressing composed of polyhydroxyethyl methacrylate (PHEMA) and polyethylene glycol (PEG), was applied to the burn wounds of 15 hospitalized patients . Application of the dressing was found to be time-consuming to the doctor and tedious for the patient . Dressing integrity was frequently broken by cracking, peeling, or ineffectual drying . Burn-wound colonization occurred beneath Hydron no more frequently than observed in other patients whose wounds had been treated with topical antibacterial agents . In general, the application of Hydron caused a reduction in burn-wound pain . In its present form, Hydron did not produce results superior to those observed in our other hospitalized burn patients . Due to technical difficulties, it is no longer being used in our unit. Ann Parasitol Hum Comp, 1980 Sep-Oct, 55(5), 605 - 13 {Mycetomas originated from South-East Bulgaria (author's transl)}; Balabanoff VA; According to investigations by the author, Bulgaria occupies a major position by the number of mycomas in European countries with temperate climate and small area . From 18 cases of mycomas, 10 cases, whom 7 were maduromycetomas or eumycetomas, originated from South-East Bulgaria, near Black Sea and Asia Minor, with warm and dry climate . This confirms that the climate has a definite influence on the disease . 6 maduromycetomas with black granules were caused by Madurella mycetomi and the only white granules mycetoma was caused by Monosporium apiospermum . Actinomycetomas were caused by Nocardia species and Actinomadura madurae . Despite the favorable effect of antibacterial compound (with special reference to Nibiol/Nitroxoline), in vitro, the actinomycetomas are more resistant to the therapy and they show a more rapid evolution . It is necessary to make a quick and early diagnosis to avoid an invasion of the underlying bones and the necessity of an amputation. Ann Plast Surg, 1980 Sep, 5(3), 186 - 90 Evaluation of biological dressings; Wolf DL et al.; The use of biological dressings in the treatment of burns is reviewed . Many theoretical advantages were initially proposed, but time and controlled studies have disproved some of them . Biological dressings are nevertheless helpful in relieving pain, protecting exposed vital structures, reducing exudative protein and erythrocyte loss and evaporative water loss, protecting granulation tissue, antibacterial activity, and testing a recipient bed's readiness for grafting . They probably offer no benefit in final wound debridement and primary dressings for partial thickness burns or split skin donor sites . There is no conclusive evidence that biological dressings alter epithelialization or the rate of formation of granulation tissue . A review of our last 100 cases at the Bothin Burn Center generally supports these conclusions with evidence of the superiority of homografts over heterografts. J Nutr, 1980 Sep, 110(9), 1914 - 21 Effects of iron on the anti-coli capacity of sow's milk in vitro and in ligated intestinal segments; Klasing KC et al.; The effect of iron on the ability of sow's milk to suppress Escherichia coli was examined both in vitro and in ligated intestinal segments of neonatal pigs . Sow's milk from day 7 of lactation was diluted with NaHCO3/KH2PO4 and divided into four treatment groups: (1) diluted milk; (2) diluted milk + ferric citrate; (3) diluted milk heated at 100 degrees for 20 minutes, and (4) treatment 3 + ferric citrate . Treatment groups were tested for antibacterial activity in vitro after inoculation of 10(4) Escherichia coli (strain 263); counts after a 3-hour incubation were: 721, 9,290, 11,400 and 9,680 for treatments 1-4, respectively . The same four treatments were tested in ligated intestinal segments of 9-day-old pigs with or without the addition of 10(4) E . coli . The average total E . coli count (+10(5)) per centimeter of intestine for 16 pigs after 3 hours of incubation were: 11, 50, 84 and 249 for treatments 1-4, respectively, without additional E . coli and 14, 110, 314 and 535 with additional E . coli . The effects of exogenous iron on the in vitro anti-coli capacity of sow's milk were also examined at 3-day intervals throughout the first 21 days of lactation . Iron had a significant detrimental effect on the anti-coli capacity of sow's milk from days 6 to 18 of lactation . Iron did not have an effect on the anti-coli capacity of colostrum, which exhibited bactericidal activity, or on milk from the 21st day of lactation, which allowed good E . coli growth . Results from these studies suggest that iron reduces the capacity of sow's milk to repress E . coli concentrations both in vitro and in vivo. Clin Exp Immunol, 1980 Aug, 41(2), 281 - 9 Measurement of intestinal antibody by radioimmunoassay; La Brooy JT et al.; The study of antibody responses in the intestine has been greatly hampered by lack of reproducible sensitive assays . An assay for measuring antibody against bacteria capable of regularly detecting gut antibody in gastroenteritis is described . It is based on absorption of antibody onto bacteria and measurement of the amount of antibody bound using radiolabelled anti-immunoglobulin antibody . Anti-light chain antibody is used to detect all classes of antibody as well as partially degraded antibody which retains the capacity to bind; anti-alpha and anti-gamma antibody is used to measure IgA and IgG antibody . The sensitivity of the assay depends on the use of anti-immunoglobulin antibody purified by affinity chromatography and allows measurement of nanogram amounts of antibody . Its specificity and kinetics are described and the particular advantages it provides in the measurement of antibacterial antibody in the intestine are discussed. Pharmazie, 1980 Aug, 35(8), 484 - 8 {Microbiological purity of pharmaceutical preparation . Part 1: External remedies; and effects of type of cream, container, storage, temperature and application (author's transl)}; Melichar M et al.; A fractional factorial experiment of the 2n type was carried out, to follow the effects of eight factors affecting simultaneously the microbiological purity of creams (Oleocremor leniens, Hydrocremor stearini) during the manufacturer-consumer chain . The effects of these factors (antibacterial substances, container (collapsible tube, pot), type of cream, storage (open, closed), number of takeouts, manner of taking-out (spatula, finger), temperature of storage, consumer (dermatological clinic, household) and interactive and interdependent . The microbiological purity of the creams is mostly impaired by the number of take-outs and the manner of taking-out . Collapsible tubes and, perhaps even better, one-dose packings are considered a solution of this problem . It is recommended to investigate creams individually with reference to their composition and structure, contents of antibacterial substances, technology and application . The tentative specification for the microbiological purity criteria of ointments and creams, designed for the Czechoslovak Pharmacopoeia, 4th Edition, is acceptable. J Clin Pharmacol, 1980 Aug-Sep, 20(8-9), 518 - 25 Dibekacin intrarenal distribution characteristics and renal cortical elution kinetics . Comparison with gentamicin and tobramycin; Whelton A et al.; Dibekacin (3',4-dideoxykanamycin B) is a new semisynthetic aminoglycoside developed in Japan and one which has found wide clinical acceptance in that country . The antibacterial activity of this compound indicates that it is relatively similar to gentamicin . Since it appears that the intrarenal distributional characteristics and renal cortical kinetics of aminoglycosides provide some predictive information concerning the clinical incidence of nephrotoxicity, we designed a series of pharmacokinetic studies in healthy mongrel dogs which would define such kinetic information for dibekacin and would contrast the results with similar studies for gentamicin and tobramycin . The renal cortical kinetics of dibekacin, as developed in these studies, show that in a canine model the behavior of dibekacin is similar to that of gentamicin and significantly different from tobramycin . Dibekacin and gentamicin show reproducibly higher renal cortical tissue concentrations than tobramycin in both the acute infusion studies and multiple dosing studies . The results suggest that dibekacin may possess the same inherent nephrotoxic potential as that of gentamicin . In order to show any difference in clinical toxicity between gentamicin and dibekacin, a very extensive randomized, double-blind, prospective clinical trial of efficacy and toxicity will be needed. J Antibiot (Tokyo), 1980 Aug, 33(8), 810 - 8 synthesis of 2-deoxyfortimicins and 1-deamino-2-deoxy-2-epi-aminofortimicins via 2-O-methanesulfonylfortimicin B; Martin JR et al.; The synthesis of 2-deoxyfortimicins A (15) and B (11) and 1-deamino-2-deoxy-2-epi-amino-fortimicins A (18) and B (12) is described . Two routes have been developed for synthesis of the key intermediate 2-O-methanesulfonylfortimicin B (7) . One route involves selective blocking of fortimicin B with B-benzyloxycarbonyl groups followed by formation of a 4,5-salicylaldehyde oxazolidine derivative . Subsequent mesylation followed by deblocking gave 7 . A more efficient route to 7 involves concomitant salicylaldehyde Schiff base and 4,5-oxazolidine formation followed by mesylation and hydrolysis . The formation of 1,2(R)-epiminofortimicin B (8) from 7 followed by RANEY nickel reduction gave 2-deoxyfortimicin B and 1-deamino-2-deoxy-2-epi-aminofortimicin B, which were converted to the corresponding fortimicin A derivative by selective N-blocking, N-acylation and subsequent deblocking . The antibacterial activities of the new fortimicin A derivatives are presented. J Antibiot (Tokyo), 1980 Aug, 33(8), 804 - 9 Synthesis and biological activities of 7-alkoxymitosanes; Urakawa C et al.; A facile alcoholysis of 7-methoxymitosanes and 5-methoxyindolequinone under basic conditions was discovered and a series of 7-alkoxymitosanes were synthesized from mitomycins A and B using this reaction . They showed strong antibacterial activity against various Gram-positive and Gram-negative bacteria and were potent inhibitors of cultivating HeLa S-3 cells in vitro . Among them, 7-n-propoxy-7-demethoxymitomycin A (2) showed the strongest antitumor activity against solid type Sarcoma-180 in mice. Obstet Gynecol, 1980 Aug, 56(2), 222 - 5 Cefoxitin sodium: double-blind vaginal hysterectomy prophylaxis in premenopausal patients; Mickal A et al.; Cefoxtin sodium is a new semisynthetic cephamycin antibiotic derivative of cephamycin-C . It has a broad antibacterial spectrum in vivo and in vitro that includes all strains of cephalosporin-sensitive bacteria and the majority of cephalosporin-resistant bacteria . A double-blind (cefoxitin and placebo) study was instigated in premenopausal women undergoing vaginal hysterectomy at Louisiana State University Gynecologic Service . There were 152 patients, of whom 125 completed the study . The objective of the study was to determine the clinical effectiveness of cefoxitin as a safe prophylactic antibiotic . Both placebo and cefoxitin groups were from the authors' clinic, and thus there were no major clinical differences among patients . The cefoxitin-treated group had a 10.3% major morbidity as compared to 29.8% in the placebo group . Cefoxitin was well tolerated and there were no adverse reactions in any of the patients. Drugs, 1980 Aug, 20(2), 137 - 54 The cephalosporins: activity and clinical use; Weinstein AJ; The cephalosporin antibiotics have been employed with increasing frequency since their introduction into clinical practice in the early 1960s . With the exception of cephaloridine, cephalosporin compounds are not associated with the production of significant untoward effects . The availability of newer cephalosporins, both oral and parenteral, with enhanced antibacterial activity, has expanded the clinical indications for administration of these antibiotics. J Antibiot (Tokyo), 1980 Aug, 33(8), 878 - 84 Comparative antibacterial properties in vitro of seven olivanic acid derivatives: MM 4550, MM 13902, MM 17880, MM 22380, MM 22381, MM 22382 and MM 22383; Basker MJ et al.; Streptomyces olivaceus ATCC 31365 produces a family of novel beta-lactam antibiotics collectively referred to as the olivanic acids . Seven such compounds, MM 4550, MM 13902, MM 17880, MM 22380, MM 22381, MM 22382 and MM 22383 have been identified which have the same carbapenem nucleus but with different side chains attached to the nucleus . The compounds with an (8S) hydroxyethyl substituent and cis-orientated beta-lactam protons, MM 22380 and MM 22382, and their sulphate esters, MM 17880 and MM 123902, are potent antibiotic with MIC values against Gram-positive and Gram-negative bacteria in the range 0.1 3.1 microgram/ml . The corresponding (8S) hydroxyethyl compounds with trans-beta-lactam protons, MM 22381 and MM 22383, also have broad-spectrum activity but are rather less potent than the cis-compound . In addition to their antibiotic activity, the olivanic acids inhibit a number of beta-lactamases and enhance the activity of beta-lactams such as amoxycillin against beta-lactamase-producing bacteria . Significant differences are observed both in antibacterial activities and in beta-lactamase inhibition properties when the olivanic acids are compared with the related thienamycin antibiotics which have (8R) rather than (8S) stereochemistry and trans-beta-lactam protons. Farmaco {Sci}, 1980 Jul, 35(7), 563 - 72 Synthesis and antibacterial activity of some ureido cephalexin and cefadroxil derivatives; Valcavi U et al.; The antibacterial activity of some ureido, acylureido and carbamoylureido derivatives of cephalexin and cefadroxil, prepared in our laboratories, as compared to parent compounds is reported . Only the 7-{D-alpha-(imidazolidin-2-one-1-ylcarbonylamino)-alpha-phenylacetamido}-3-methyl-3-cephem-4-carboxylic acid (IV d) and the 7-{D-alpha-(imidazolidin-2-one-1-ylcarbonylamino)-alpha-p-hydroxyphenylacetamido}-3-methyl-3-cephem-4-carboxylic acid (V c) showed some antibiotic activity . However we found no activity improvement against Pseudomonas strains (contrary to the results obtained in similar penicillin derivatives) and a lower beta-lactamase resistance. J Antibiot (Tokyo), 1980 Jul, 33(7), 683 - 9 New antibiotics, carbazomycins A and B . I . Fermentation, extraction, purification and physico-chemical and biological properties; Sakano K et al.; An unidentified Streptomyces, designated as Strain H 1051-MY 10, was proved to produce viomycin and two new antibiotics . The new antibiotics were extracted from the cultured mycelia with acetone and transferred to ethyl acetate after acetone was removed in vacuo . The extracted antibiotics were separated into two components by alumina column chromatography and named carbazomycins A and B, because both antibiotics were proved to contain a carbazole nucleus . The molecular formulae of carbazomycins A and B were determined to be C16H17NO2 and C15H15NO2, respectively . Further, carbazomycin B was methylated with diazomethane to give carbazomycin A . Carbazomycins inhibited the growth of phytophathogenic fungi and further showed weak antibacterial and antiyeast activities. Antimicrob Agents Chemother, 1980 Jul, 18(1), 171 - 5 Radiometric prescreen for antitumor activity with Saccharomyces cerevisiae mutant strain; Speedie MK et al.; After modification, a technique for radiometrically measuring bacterial growth has been applied to a mutant strain of Saccharomyces cerevisiae . The assay is based on inhibition of 14CO2 release from {14C}glucose, which provides an extremely sensitive measure of cellular respiratory activity and growth . The criterion for antitumor activity is the differential inhibition of wild-type and mutant (distorted cell membrane) strains of the yeast . The system was optimized for medium, time of incubation, temperature, and size of inoculum . Known antitumor agents, including bleomycin, actinomycin D, adriamycin, and ellipticine were tested in the system, and differential inhibition was observed . Vincristine showed no inhibitory effects at the concentrations tried . The sensitivity for 20% inhibition ranged from 0.8 micrograms of adriamycin per ml to 0.14 mg of ellipticine per ml . Antifungal agents such as amphotericin B exhibited no differential inhibition . Antibacterial agents were inactive . This method may provide a rapid, sensitive, in vitro quantitative assay for antitumor agents which could be applied to a variety of assay needs and which can be run with facilities and equipment available in most laboratories. Acta Paediatr Scand, 1980 Jul, 69(4), 517 - 23 The effect of digestive enzymes on the binding and bacteriostatic properties of lactoferrin and vitamin B12 binder in human milk; Samson RR et al.; Human milk contains unsaturated lactoferrin and vitamin B12 binding protein . It has been suggested that these proteins may exert antibacterial effects in the intestine of the breast fed infant, but the effect of the intestinal environment on the antibacterial effect of these proteins has not been described . In this study human milk was treated with pepsin and trypsin and the influence of digestion on iron and vitamin B12 binding capacity, bacterial uptake of iron and vitamin B12 from milk and bacteriostatic effect was studied . Pepsin digestion had no effect on vitamin B12 binding capacity, or the ability of bacteria to take up vitamin B12, or the growth inhibitory effect on a vitamin B12 dependent strain . In contrast, trypsin digestion did not affect iron binding or bacteriostatic effects attributable to lactoferrin . The . findings support an in vivo bacteriostatic role for lactoferrin in the breast fed neonate's intestine but do not support a similar role for the vitamin B12 binding protein. J Dent Res, 1980 Jul, 59(7), 1127 - 31 The effect of EDTA-containing surface-active solutions on the morphology of prepared dentin: an in vivo study; Brannstrom M et al.; The capacities of EDTA-containing and surface-active antibacterial solutions and their combinations for removing amorphous smear layers produced by cutting of dentin were studied in vivo on 132 human dentin surfaces ground at high speed with a diamond point . A combination of 0.2% EDTA and surface-active antibacterial solutions removed most of the smear layers without opening too many tubule apertures or removing peritubular dentin . No difference was found between the cleaning capacity on surfaces ground under water cooling compared to air cooling. Antibiotiki, 1980 Jul, 25(7), 483 - 8 {Isolation and physicochemical study of the components of the new antibacterial antibiotic 2562}; Lysenkova LN et al.; An antibacterial antibiotic complex consisting of 2 components designated as 2562 A and 2562 B is produced by Streptomyces griseovarabilis . The antibiotic was isolated from the mycelium and purified chromatographically on a column with aqueous silicic acid . The study of the components showed that component 2562 A was chlorbiocin, while component 2562 B differed from the known antibiotics of this group . Physicochemical assays demonstrated that component 2562 B differed from chlorbiocin by the absence of the methyl group in pyrrol, which is probably attached to sugar at beta-position . It was found that component 2562 B is a new representative of the antibiotic cumero-glycoside group. J Pharmacokinet Biopharm, 1980 Jun, 8(3), 297 - 309 An experimental assessment of the Wagner-Sedman extraction theory for the intestinal absorption of antibacterial sulfonamides; Pla-Delfina JM et al.; The chromatographic parameters in a reverse-phase partition system and the rat gut in situ absorption rate constants for 18 antibacterial sulfonamides are highly correlated values . The correlation is logarithmic-logistic in nature, being in accordance with the Wagner-Sedman extraction theory for a constant pH value . Parabolic correlations did not satisfactorily fit the experimental data . This behavior, not frequently reported in regard to the intestinal absorption of drugs, is discussed in connection with other apparently contradictory available data. Vestn Khir Im I I Grek, 1980 Jun, 124(6), 70 - 2 {Obturating thrombophlebitis as a complication of prolonged subclavian vein catheterization}; Shuvalov IuA et al.; Catheterization of subclavian veins was performed in 2800 patients including 18 children in order to fulfil infusion-transfusion massive antibacterial therapy . The article gives a detailed clinical picture of the complication and recommendations for the treatment of this dangerous complication . The outcomes of the obturating thrombosis with catheterized subclavian veins are described . The employed active conservative therapy contributed to recovery of all the patients having this complication. Antimicrob Agents Chemother, 1980 Jun, 17(6), 980 - 7 Some chemical and physical characteristics of pantomycin, and antiobiotic isolated from Streptomyces hygroscopicus; Gurusiddaiah S et al.; The production, isolation, and some structural studies of an antifungal, antibacterial, and antiviral substance from cultures of Streptomyces hygroscopicus are described . This material, designated pantomycin, appears to be a polypeptide antibiotic with inclusion of fatty acids and carbohydrate residues . Amino acid analysis of pantomycin acid hydrolysates indicates that it contains threonine, serine, proline, glycine, alanine, valine, alloisoleucine, and an as-yet-unidentified amino acid which appears to be different from types encountered in proteinaceous materials . In addition to the aforementioned compounds, the antibiotic was shown to contain alpha-aminobutyric acid after hydrogenation . Analysis of ether extracts of the hydrolysate mixture indicated the presence of several fatty aicds; myristic, isotridecanoic, lauric, and undecylic acids . The amino and fatty acid composition of pantomycin is similar to the known antibiotic stendomycin . Pantomycin appears to also have at least one carbohydrate-like residue incorporated into its structure . The presence of carbohydrate was indicated by periodic acid-Schiff base staining of electrophoretic patterns as well as positive color formation in the phenol-sulfuric and Molisch tests, but the carbohydrate did not appear to be either a hexose or a pentose . The antibiotic, which appears to be dissociated in alcoholic solution, forms stable aggregates under aqueous conditons. Urology, 1980 Jun, 15(6), 599 - 600 Accessory urethral channel communicating with the seminal vesicle; Canham J et al.; A rare variety of accessory urethra communicating with the left seminal vesicle is reported . Communication was demonstrated between the prostatic urticle and the right seminal vesicle, but not the left . Infection of the accessory channel was managed conservatively with antibacterial therapy . The classification, diagnosis, and treatment for this anomaly are discussed. Vestn Khir Im I I Grek, 1980 Jun, 124(6), 79 - 82 {Effect of antibiotics and antiseptics on the fibrinolytic activity of proteases}; Chepcheruk GS et al.; A table of compatibility of proteases and antibacterial drugs was developed on the basis of investigation of fibrinolytic effect of proteolytic enzymes (fibrinolysine, chimotrypsin, streptokinase, terrilitin) and their combinations with most popular antibiotics and antiseptic solutions . According to the data of the authors, terrilitin and streptokinase are most efficient of the proteolytic enzymes studied and less dependent upon antibiotics and antiseptic solutions when used in combinations. Scand J Dent Res, 1980 Jun, 88(3), 210 - 3 Plaque inhibition by guanidino propyl piperazine (CKO 569A); Melsen B et al.; The plaque inhibiting effect of the antibacterial substance, guanidino propyl piperazine (CKO 569A) has been analized in a clinical study of 10 adults . Plaque formation was enhanced by three daily rinses with 15% sucrose . Normal hygiene was performed . The effects of a twice daily mouthwash of 30 s duration with 0.2, 0.1 and 0.05% CKO 569A, 0.05% chlorhexidine and a placebo on plaque formation were compared through a registration of plaque scores . Each solution was tested over a period of 5 days . As a result of this study it could be concluded that in humans CKO 569A is an effective inhibitor of plaque, and that lingual plaque scores appear to be a good indicator of plaque inhibiting activity. J Med Chem, 1980 Jun, 23(6), 607 - 13 Quantitative structure-pharmacokinetic relationships derived on antibacterial sulfonamides in rats and its comparison to quantitative structure-activity relationships; Seydel JK et al.; Quantitative structure-pharmacokinetic relationships have been derived for a series of substituted 2-sulfapyridines . Pharmacokinetic parameters, such as elimination rate constant (ke), clearance (Cl), and protein-binding constant (Kassoc), have been determined in rats . The observed variation is statistically significant, explained by changes in the lipophilic (deltaRm), electronic (pKa), and steric effects (I, ES) of the substituents . The obtained correlations are discussed with respect to the previously derived correlations for the antibacterial activity of these compounds . A scale up of the results opens up the possibility of a rational synthesis of highly active sulfonamides with special pharmacokinetic properties because lipophilicity influences strongly the pharmacokinetic properties, whereas no influence on the degree of antibacterial effect is observed . Steric substituent influence is opposite on specific binding to bacterial enzymes and unspecific binding to serum proteins. J Pediatr, 1980 Jun, 96(6), 1081 - 7 Trimethoprim-sulfamethoxazole compared with ampicillin in the treatment of acute otitis media; Shurin PA et al.; We treated 132 children with acute otitis media in a randomized trial comparing trimethoprim-sulfamethoxazole and ampicillin . The antibacterial efficacy of the drugs was assessed primarly from the results of cultures of middle ear aspirates obtained during or after the course of therapy; persistent, recurrent, and new infections of the middle ear were documented in both groups of patients but did not differ significantly . Both drug regimens were well accepted by the patients and were not associated with serious side effects or toxicity . TMP-SMZ is an effective alternate to AMP or to other accepted regimens for initial treatment of acute otitis media. Contact Dermatitis, 1980 Jun, 6(4), 241 - 5 Merthiolate hypersensitivity and vaccination; Forstrom L et al.; Epicutaneous tests with 0.1% merthiolate in petrolatum showed hypersensitivity in 96 of 4647 eczema patients (2.0%) and in seven of 105 healthy recruits (7%) . There was a marked preponderance of young age classes in the eczema group . Twelve of 41 merthiolate-positive patients tested reacted to mercury alone, three to thiosalicylic acid alone and one to both . The remaining 25 patients reacted to neither of the individual components although the merthiolate complex as a whole gave a positive test result . Forty-five of the merthiolate-positive patients were tested subcutaneously with 0.5 ml of a 0.01% merthiolate solution, i.e . a dose equal to that contained in one shot of tetanus toxoid, for example . Nine patients developed a local reaction at the site of the injection, and the area became eczematous in four cases . In one of the patients the eczema spread over the body, causing fever . Since merthiolate-sensitive patients also react to merthiolate administered intracutaneously, the vaccinator should avoid the use of a needle whose outer surface has been contaminated when the vaccine was aspirated from the bottle . However, even when this precautionary measure is taken, local reactions can be expected in such a high percentage of merthiolate-sensitive persons that merthiolate in vaccines should be replaced by another antibacterial agent. J Am Vet Med Assoc, 1980 May 15, 176(10 Spec No), 1122 - 8 Availability and usage of new antibacterial drugs in Europe; Ziv G; The present-day availability and usage of established and new antibacterial drugs approved for clinical and therapeutic purposes in food-producing animals and poultry in the United States and Europe were compared . Presently, 42 such drugs are approved in Europe, 13 of which were approved since Dec 31, 1974 . In the United States, 17 such drugs are currently approved, only four were approved since Dec 31, 1974 . Most drug products approved in Europe contain two or more antibacterial agents, whereas most of the products approved in the United States are single drug entities . Drugs approved in Europe but not in the United States include sulfonamide and trimethoprim combinations, nafcillin, oxacillin, metampicillin, cephoxazole, cephalonium, cephacetrile, cephalexin, gentamicin, rifamycin SV, nifuroquine, tiamulin, chloramphenicol, colistin, and polymyxin B . Pharmacologic and clinical features of several of these drugs are briefly described. J Am Vet Med Assoc, 1980 May 15, 176(10 Spec No), 1109 - 15 Drug selection and use in mastitis: systemic vs local therapy; Ziv G; The optimal properties of antibacterial drugs, (administered parenterally or intracisternally during clinical mastitis) required for achieving and maintaining effective drug concentrations at the site of infection are reviewed . The in vitro sensitivity of the udder pathogen, expressed as the minimal inhibitory concentration (MIC) of the drug, and the physicochemical properties of the antibiotic are major determinants in the duration of effective drug concentrations in the udder . Injectable oxytetracycline and chloramphenicol possess limited IM bioavailability properties, and therefore, should be administered IV . Effective passage of drug from blood into the udder is best achieved with the macrolide antibiotics, but the antibacterial spectra of these drugs are limited to gram-positive pathogens . For intramammary treatment, drugs that are distributed throughout the udder and are quickly absorbed into the general blood circulation should be preferred . A second priority should be given to those drugs possessing more limited distribution characteristics . Some of the most active drugs in vitro are poorly and unevenly distributed in the udder and are absorbed only to a limited extent. Jpn J Antibiot, 1980 May, 33(5), 558 - 73 {The distribution of aminoglycoside antibiotics into the lymph and pancreatic fluid in dogs (author's transl)}; Lee YG; 1 . Serum, peripheral and thoracic lymph concentrations of tobramycin, dibekacin and amikacin were determined at various time intervals up to 6 hours following intramuscular administration of 4 mg/kg to dogs . Peak serum concentrations of each antibacterial agents occurred within one hour after administration . The peak lymphatic concentrations occurred in 1.5 approximately 2 hours after administration . Following peak peripheral lymph concentration, the concentration in peripheral lymph exceeded than that of serum . The concentrations of each antibacterial agent in thoracic lymph were nearly equal to serum concentration . Peak peripheral lymph concentrations were always lower than the peak serum concentrations . 2 . Serum and pancreatic fluid concentrations of tobramycin, dibekacin and amikacin were determined at various time intervals up to 6 hours following intramuscular administration of 4 mg/kg to dogs . Peak pancreatic fluid concentrations of each antibacterial agents occurred within 1.5 hours after administration . The concentrations rate of tobramycin to the pancreatic fluid was superior to those of dibekacin and amikacin. Int J Dermatol, 1980 May, 19(4), 221 - 2 Peganum harmala: its use in certain dermatoses; El-Saad El-Rifaie M; The extract of Peganum harmala (Rutaceae) was used topically to treat certain dermatoses of inflammatory nature . Results were encouraging and proved the antibacterial, antifungal, antipruritic and probably antiprotozoal effects of the extract. J Antibiot (Tokyo), 1980 May, 33(5), 463 - 7 Antibiotics from basidiomycetes . X . Scorodonin, a new antibacterial and antifungal metabolite from Marasmius scorodonius (Fr.) Fr; Anke T et al.; Scorodonin (1), a novel biologically active metabolite, was isolated from submerged cultures of the mushroom Marasmius scorodonius (FR.) FR . Its structure has been determined by chemical and physical methods . The antibiotic inhibits the growth of bacteria, yeasts, and filamentous fungi . In cells of the ascitic form of EHRLICH carcinoma the incorporation of thymidine and uridine into DNA and RNA is strongly inhibited by scorodonin whereas the incorporation of leucine into protein is not affected. J Med Chem, 1980 May, 23(5), 535 - 41 2,4-Diamino-5-benzylpyrimidines as antibacterial agents . 4 . 6-Substituted trimethoprim derivatives from phenolic Mannich intermediates . Application to the synthesis of trimethoprim and 3,5-dialkylbenzyl analogues; Roth B et al.; The preparation of a wide variety of 6-substituted trimethoprim analogues was readily accomplished by the reaction of 2,4-diamino-6-substituted-pyrimidines with 2,6-dimethoxy-4-{(N,N-dimethylamino)methyl}phenol at 120--160 degrees C . The less reactive 2,6-dialkyl-4-{(N,N-dimethylamino)methyl}phenols reacted successfully with 2,4-diamino-6-(alkylthio)pyrimidines to give 5-(substituted benzyl)pyrimidines . The phenolic groups of the products were alkylated in high yield when a nonreactive 6-substituent was present in the pyrimidine ring . 6-(Alkylthio) groups were easily removed with Raney nickel . Trimethoprim was thus obtained in high yield from its 6-(methylthio) counterpart . The 6-substituted trimethoprim analogues all had low activity as inhibitors of Escherichia coli dihydrofolate reductase and as antibacterial agents. Minerva Stomatol, 1980 May-Jun, 29(3), 159 - 62 {Use of hexetidine as an oral cavity antiseptic}; Menghini P et al.; Of the many products recommended for topical use in the prevention and control of odontostomatological diseases, those containing hexetidine have proved to combine detergent properties with a true, specific activity . Reference is made to the abundant literature in an account of the composition, antibacterial spectrum, pharmacokinetics, mechanism and action time of this molecule . The conclusion is reached that, with proper support in the form of general drug management, hexetidine is effective in the treatment of odontostomatological and ORL sepsis. Clin Pharmacol Ther, 1980 May, 27(5), 677 - 85 Cefotaxime kinetics after intravenous and intramuscular injection of single and multiple doses; Neu HC et al.; The kinetics of cefotaxime, a cephalosporin with an unusually broad antibacterial spectrum, were examined in humans after intravenous bolus injection, intravenous infusion every 6 hr for 14 days, and intramuscular injection every 8 hr for 10 days . Mean peak serum level after bolus injection of 500 mg was 37.9 microgram/ml; after 1 gm, 102.4 microgram/ml; and after 2 gm, 214.1 microgram/ml . The half-life (t1/2) was 1 hr for the 3 doses . Total serum clearance was the same for all doses . Overall excretion was 50% to 60%; part of the drug was excreted as the desacetyl derivative . After multiple intravenous infusion the elimination rate constants and t1/2 were the same on days 1 and 15 . Assayable levels were present on all days 5 min before injection of a dose . Multiple intramuscular injections of 500 mg produced serum levels of 9.2 to 11.9 microgram/ml . The t1/2 was 0.93 hr . Mean serum levels at 8 hr ranged from 0.08 to 0.55 microgram/ml . Serum levels produced by intravenous infusion or intramuscular injection were inhibitory for most (90%) aerobic gram-positive and gram-negative organisms susceptible to cefotaxime. J Antibiot (Tokyo), 1980 Apr, 33(4), 404 - 7 Syntheses of corliolin, 1-deoxy-1-ketocoriolin and 1,8-dideoxy-1,8-diketocoriolin from coriolin B; Nishimura Y et al.; Hydrolysis of 5,8-di-O-tetrahydropyranyl-5-deoxo-5-hydroxycoriolin which was prepared from coriolin B, followed by oxidation of the hydroxy groups at C-5, or C-1 and C-5, or C-1, C-5 and C-8 afforded coriolin (2), 1-deoxy-1-ketocoriolin (3) and 1,8-dideoxy-1,8-diketocoriolin (4) . All three ketones were found to have antitumor activity, whereas antibacterial activity was observed in 2 and 3 but not in 4. J Antibiot (Tokyo), 1980 Apr, 33(4), 393 - 403 Chemical modification of the ester group of diketocoriolin B; Nishmura Y et al.; 5,8-Di-O-tetrahydropyranylcoriolin B (2) was synthesized and its two expoxide groups were found to be resistant to alkaline hydrolysis to give di-O-tetrahydropyranldihydrocoriolin (3) . Acylation or alkylation of the free hydroxyl group at C-1 of 3 followed by hydrolysis of the tetrahydropyranylether groups and oxidation of the hydroxyl groups at C-5 and C-8 afforded a numer of 1-O-acyl or alkyl analogs of diketocoriolin B . All of them showed antibacterial and antitumor activities. Chest, 1980 Apr, 77(4), 552 - 4 Desquamative interstitial pneumonitis . Characterization of free intraalveolar cells; Fromm GB et al.; There is some disagreement concerning the nature of the free intraalveolar cells in desquamative interstitial pneumonitis, although the greatest weight of evidence suggests them to be alveolar macrophages . We have obtained these cells by bronchoalveolar lavage from two patients with desquamative interstitial pneumonitis and studied their in vitro antibacterial activity and their ultrastructural morphology . Our results indicate that the free intraalveolar cells in these two patients were alveolar macrophages with normal antibacterial function. J Med Chem, 1980 Apr, 23(4), 384 - 91 2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents . 3 . C-Benzylation of aminopyridines with phenolic Mannich bases . Synthesis of 1- and 3-deaza analogues of trimethoprim; Rauckman BS et al.; Electrophilic substitution of 2,4-diaminopyridine by 2,6-disubstituted -4-{(N,N-dimethylamino)methyl}phenols and by halogens (bromine and fluorine) produces 3-benzyl and 3-halo derivatives, plus a small amount of disubstitution at the 3,5 positions . Treatment of a 2,4-diamino-3-halopyridine with phenolic Mannich bases gives 5- and N-benzylation . 2,4-Diamino-3-bromo-5-(4-hydroxy-3,5-dimethoxybenzyl)pyridine was methylated on the phenolic group in good yield and dehalogenated to produce 3-deazatrimethoprim {2,4-diamino-5-(3,4,5-trimethoxybenzyl)pyridine} . This compound is about 300-fold less active as an inhibitor of Eschericia coli dihydrofolate reductase than is trimethoprim . 2,6-Diaminopyridine is very readily dibenzylated at the 3,5 positions as well as on an amino group, by a phenolic Mannich base; use of a fourfold excess of the pyridine provided a 3-benzylated 2,6-diaminopyridine in 50% yield; this was inactive as an inhibitor of dihydrofolate reductase at 10(-4) M . 2-Amino- and 4-aminopyridines do not produce C-benzylated products under the conditions reported here. J Med Chem, 1980 Apr, 23(4), 379 - 84 2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents . 2 . C-Alkylation of pyrimidines with Mannich bases and application to the synthesis of trimethoprim and analogues; Roth B et al.; A new route to 5-(p-hydroxybenzyl)pyrimidines has been developed which utilizes phenolic Mannich bases plus pyrimidines containing at least two activating groups . The products can be alkylated on the phenolic oxygen or on the pyrimidine N-1 atom, depending on conditions . This method has been used to prepare trimethoprim, a broad-spectrum antibacterial agent, starting from 2,4-diaminopyrimidine and 2,6-dimethoxyphenol. Acta Pathol Microbiol Scand {B}, 1980 Apr, 88(2), 103 - 6 Effects of some antibacterial agents on the phagocytosis of 32P-labelled Escherichia coli by human polymorphonuclear cells; Melby K et al.; Gentamicin, trimethroprim, cephalothin, colistin, erythromycin, oxytetracycline and chloramphenicol were studied in a phagocytic system . A radiolabelled strain of E . coli was used as test bacterium and human polymorphonuclear cells were used as phagocytes . Except for trimethoprim and cephalothin, there was a tendency towards depression of the process of phagocytosis in the presence of high concentrations of the various antibiotics . Colistin in a high concentration (83 micrograms/ml) exerted the most significant effect. J Infect Dis, 1980 Mar, 141(3), 326 - 30 A study of cephalothin and desacetylcephalothin in cerebrospinal fluid in therapy for experimental pneumococcal meningitis; Nolan CM et al.; One explanation for the failure of cephalothin to cure patients with bacterial meningitis is that desacetylcephalothin, as in vivo metabolite that has less antibacterial activity than the parent drug, penetrates more efficiently into cerebrospinal fluid (CSF); In experimental pneumococcal meningitis in rabbits, the peak levels of cephalothin and desacetylcephalothin in CSF after an intramuscular injection of 250 mg of cephalothin/kg were, respectively, 1.43 +/- 4.9 microgram/ml (2.8% of peak serum level) and 1.69 +/- 0.57 microgram/ml (2.2% of peak serum level) . The observed half-life of desacetylcephalothin in CSF (3.32/hr) was longer (P less than 0.01) than that of cephalothin (0.72/hr) . Choroid plexuses isolated from the lateral cerebral ventricles of rabbits with meningitis took up cephalothin in vitro more avidly than desacetylcephalothin (P less than 0.05), and metabolism of cephalothin to desacetylcephalothin by isolated choroid plexuses was demonstrated directly . Thus, intrathecal metabolism of cephalothin by the choroid plexus may contribute to the unsatisfactory performance of cephalothin in bacterial meningitis. Zentralbl Bakteriol A, 1980 Mar, 246(3), 329 - 35 Antibacterial action of quinolones on Escherichia coli . I . Structure/activity relationship; Mahmood F et al.; Quinolones, a large group of substituted heterocyclic compounds synthesized by ICI (U.K.), showed antibacterial activity both in vivo and in vitro studies . In the present work an attempt was made to evaluate their antibacterial activity in relation to their chemical structure . Active compounds possess carboxylic and nitroside groups . Regarding the pattern of growth inhibition quinolone with carboxylic side group showed a different behaviour than quinolone possessing nitro side group. Acta Otolaryngol, 1980 Mar-Apr, 89(3-4), 214 - 21 IgA transport mechanism through the human nasal mucosa: an immunoenzymatic ultrastrutural study; Crifo S et al.; The role of secretory IgA antibodies in the antiviral and antibacterial defense of the higher respiratory tract has been widely demonstrated, and the IgA determination in the nasal secretion has become of the highest value in the clinical study . The mechanism by which IgA reaches nasal secretion through the mucosa is still a matter of discussion and neither hypothesis put forward by Tomasi (i.e . free filtration through the epithelic-connectival interstitium or transcellular transport plus active secretion) has so far been fully demonstrated . By using a horseradish peroxidase labeled IgG directed against human IgA we have performed, with suitable controls, a semi-quantitative study on semi-thin and thin section of the IgA behaviour at the level of human nasal mucosa . We have shown that IgA, made up and secreted in the connectival interstitium by specific plasma cells, would be taken up by endocytosis by epithelial cells, where it can be seen especially in the Golgi apparatus and in the large secretion granules . Since in the intracellular transport of pinocytic vesicles actin microfilaments and microtubules undoubtedly play a major role, with ATP utilisation, further studies using either physical factors (e.g . exposure to cold) effecting ATP utilisation or chemical ones (e.g . cytochalasin B and colchicine) depolymering respectively microfilaments and microtubules, should be performed in order to bring further proofs in favor of the active transport IgA mechanism suggested by our present investigations. Int J Lepr Other Mycobact Dis, 1980 Mar, 48(1), 18 - 29 Mechanism of action of the folate blocker diaminodiphenylsulfone (dapsone, DDS) studied in E . coli cell-free enzyme extracts in comparison to sulfonamides (SA); Seydel JK et al.; The antibacterial activity of DDS has been studied in whole cell (E . coli), cell-free folate synthesizing enzyme extracts and compared to effects obtained for sulfonamides (SA) . It is shown that DDS acts as a synthetase inhibitor in the folate synthesizing enzyme system . DDS reacts with the substrate 7,8-dihydro-6-hydroxymethylpterinopyrophosphate to form a 7,8-dihydropteroic acid analog . Bacterial growth kinetic studies were performed to test for possible synergistic activity of the analog in combination with DDS . Possible reasons for the extremely large inhibitory power of DDS against M . leprae are discussed. Antibiotiki, 1980 Mar, 25(3), 218 - 22 {Gentamycin sulfate in the therapy of acute and chronic pneumonias}; Zamotaev IP et al.; Clinical efficacy of gentamicin in treatment of acute and chronic pneumonia was shown . The wide antibacterial spectrum of the antibiotic provided its use in therapy of mixed bacterial infections . Satisfactory results were observed in 47 (93.7 per cent) out of 51 patients . The adverse reactions, such as proteinuria, hematuria, and polymorphous eruption were recorded in 5 patients and vanished after discontinuation of the drug . On the basis of the experience acquired the drug may be recommended for use in pulmonology. Blood, 1980 Mar, 55(3), 501 - 4 The effect of trimethoprim/sulfamethoxazole on Friend erythroleukemia cells; Steinberg SE et al.; Cultures of Friend erythroleukemia cells were subjected to the antibiotics trimethoprim (T) and sulfamethoxazole (S) at levels equal to or below the usual therapeutic range . At T 8 microgram/ml and S 40 microgram/ml, cell growth was arrested, cells appeared megaloblastic, and the examination of cell-cycle distribution by flow microfluorimetry revealed arrest in S phase . With a tenfold reduction in drug levels (T, 08 microgram/ml; S, 4 microgram/ml) cell growth was less markedly inhibited, morphology remained megaloblastic, and S-phase block was still dramatic . A further tenfold reduction (T, 0.08 microgram/ml; S, 0.4 microgram/ml), well below effective antibacterial levels, allowed normal cell growth and morphology but DNA synthesis was still inhibited . Additions of folinic acid at 100 ng/ml averted all drug effects . Thus T/S can affect cell replication even at levels well below those usually employed and could prolong the rate of recovery of hematopoietic cells in the myelosuppressed patient. J Antibiot (Tokyo), 1980 Mar, 33(3), 259 - 66 FR-900148, a new antibiotic . I . Taxonomy, fermentation, isolation and characterization; Kuroda Y et al.; A strain of Streptomyces, isolated from a soil sample and identified as Streptomyces xanthocidicus, has been found to produce FR-900148, a new antibiotic containing chlorine in its molecule . The antibiotic inhibits both Gram-positive and negative bacteria . However, it is not effective against wild type of Pseudomonas aerguinosa . Its antibacterial action is considered to result from cell wall synthesis inhibition since it causes spheroplast formation from susceptible cells. Laryngol Rhinol Otol (Stuttg), 1980 Mar, 59(3), 170 - 5 {Antibacterial substances in tamponades after tympanoplasties - an "in-vitro"-study (author's transl)}; Pau HW et al.; This "in-vitro"-study is concerned with the efficiency of antibacterial agents used in packings after tympanoplasties . For this purpose, gel-foam-material was impregnated either with rolitetracyclin (mostly used in German ENT-clinics), or comparatively with a combination of bacitracin and neomycin or with antiseptics like phenylmercuriborate and povidon-iodine . It is tested, how these impregnated "packings" behave in the presence of pathogenic germs (Staph . aureus, Ps . aeruginosa) . Antibacterial effects and alterations of the material were judged . It is shown, that in some regards the rolitetracyclin - very successful in clinical use - is superior to the other substances tested. Zh Mikrobiol Epidemiol Immunobiol, 1980 Mar, (3), 72 - 5 {Immune response of guinea pigs to combined action of brucella vaccine and homologous lysed antigen}; Rementsova MM et al.; Experiments on guinea-pigs have shown the synergetic effect of the lyzed, low-molecular Brucella component (glucopeptide) and live brucellosis vaccine prepared from Br . abortus 82 on the antibacterial immunity index . After the injection of these preparations in succession (glucopeptide and then the vaccine) at an interval of 72 hours the number of immune animals increased 1.5-2 times in comparison with the animals receiving only one of these preparations. Mycopathologia, 1980 Feb 29, 70(1), 43 - 7 Comparison of gentamicin with other antibacterials and variation of incubation temperature on growth of trichophyton mentagrophytes from skin scales; Sinski JT et al.; Neutral (Emmons modification) Sabouraud medium, Dermatophyte Test Medium and Littman oxgall agar, with substitutions in type of antibacterial antibiotic, were quantitatively evaluated by colony counts for ability to support growth when suspensions of trypsintreated guinea pig skin scales, infected with Trichophyton mentagrophytes, were used as inocula . Both liquid and powder form of gentamicin sulfate were used separately in place of other routinely used antibacterial antibiotics . Also evaluated were three isolation temperatures . No differences in ability to support growth were noted among media . No difference was noted between the two forms of gentamicin . No data were available on the antibacterial activities of the antibiotics because no bacterial growth was produced on any of the media . Room temperature (24 degrees-26 degrees C), 30 degrees C and 37 degrees C were found to support growth similarly as primary isolation temperatures for this fungus. Br Med J, 1980 Feb 16, 280(6212), 442 - 4 Sulphasalazine in rheumatoid arthritis; McConkey B et al.; Seventy-four patients with rheumatoid arthritis were treated with sulphasalazine . There was a significant improvement in clinical score, with substantial falls in serum C-reactive protein concentrations and erythrocyte sedimentation rate four weeks after starting the drug . Improvement was maintained in the 38 patients who remained on the durg for one year . The mean Rose-Waaler titre did not change . There was little difference between the results in seropositive and seronegative patients . The commonest adverse effect was dyspepsia, but five patients developed a megaloblastic anaemia and one patient neutropenia; all made a complete recovery . The results suggest that the drug has a disease-modifying action not attributable to its "salicylate" content . The mode of action might be by an antibacterial effect on gut flora. Dtsch Med Wochenschr, 1980 Feb 8, 105(6), 194 - 201 {Acquired agammaglobulinaemia: clinical and immunological aspects (author's transl)}; Ludwig H et al.; Chronic recurrent bacterial infections, especially sinusitis, bronchitis and pneumonia, frequently taking a fulminating course, were the characteristic leading clinical symptoms of acquired agammaglobulinaemia in three women . This abnormally increased susceptibility to infection had previously caused numerous hospitalisations, operations and punctures as well as high-dosage antibiotic treatments . Analysis for immunological defects provided evidence of a lymphocyte-inherent defect in two patients, while in the third there was an abnormally increased suppressor-cell activity as a cause for the humoral immunodefect . Gammaglobulin substitution was tried in all three patients, but in one it had to be discontinued because of severe intolerance to homologous serum proteins . In the other two a high dosage substitution regimen, undertaken at 14-day intervals, has resulted in almost complete normalisation of antibacterial defences and of the clinical state. Farmaco {Sci}, 1980 Feb, 35(2), 161 - 6 Synthesis of derivatives of 3,5-dinitropyridine aldehydes; Achremowicz L; Mono- and dimethyl-3,5-dinitropyridines were oxidized with SeO2, yielding hemiacetals of new 3,5-dinitropyridine aldehydes . Some of their oximes showed antibacterial activity. Poult Sci, 1980 Feb, 59(2), 274 - 81 A new poultry semen extender . 4 . Effect of antibacterials in control of bacterial contamination in chicken semen; Sexton TJ et al.; Forty antibacterials were qualitatively and quantitatively tested for controlling aerobic bacterial contamination without affecting viability of semen . Semen samples were collected aseptically, diluted 1:4 with the Beltsville poultry semen extender containing one of 40 antibiotics and held for 0, 24, 48, and 72 hr at 5 C . Semen samples were monitored at each storage interval for bacterial counts, sperm motility, sperm counts, and fertilizing capacity . Gentamicin (2.5 microgram/ml), kanamycin (31.2 microgram/ml), neomycin (62.5 microgram/ml), and tobramycin (2.5 microgram/ml) were the only antibacterials tested which controlled microbial growth without affecting sperm viability for up to 24 hr storage at 5 C . Tobramycin maintained fertility equal to that of the non-antibiotic control up to 24 hr storage . Neomycin maintained higher levels of fertility in semen stored for 48 and 72 hr than in semen of controls to all other treatments for the same storage periods and to undiluted, unstored semen . The conclusion from these studies is that the control of aerobic microbial growth in chicken semen has little influence on the maintenance of sperm viability during low temperature storage. Ann Plast Surg, 1980 Feb, 4(2), 166 - 9 Perifolliculitis capitis: successful control with alternate-day corticosteroids; Adrian RM et al.; A case of perifolliculitis capitis is reported in which the patient was initially treated with high-dose intravnous antibiotics and topical antibacterial agents without success . Systemic corticosteroids were instituted, with rapid subsidence of disease activity . One year later, the patient remains on 5 mg of prednisone on alternate days, and is free of disease activity . In view of other more aggressive treatments reported in the literature for this disease, high-dosage prednisone with rapid change to alternate-day dosage is a reasonable initial course of action. Drugs, 1980 Feb, 19(2), 119 - 34 Topical corticosteroids: clinical pharmacology and therapeutic use; Miller JA et al.; The development of topical corticosteroids has enabled many dermatoses to be more effectively treated than previously, but there is also no doubt that misuse of these preparations can lead to troublesome local effects and potentially serious systemic problems . The most effective assay for comparing different compounds has been their vasoconstrictive activity, and this on the whole correlates well with clinical effect . To be effective, corticosteroid must be absorbed and the importance of concentration, occlusion, the type of vehicle, added penetrants such as urea and the anatomical site, on the amount of absorption and therefore on clinical activity has been demonstrated . Ointments have been shown to be more effective than creams but because of the considerable choice of potencies now available most dermatologists tend to prescribe the different formulations according to the wishes of the patient . For the same reason, dilution of the commercially marketed preparations is now not generally recommended . The main therapeutic activity of topical corticosteroids is their nonspecific anti-inflammatory effect, thought to be primarily a result of their action on the chemical mediators of inflammation . They have also been shown to be antimitotic which may well be relevant not only to the treatment of scaling dermatoses but also to their dermal thinning effect resulting from inhibition of fibroblasts . Combinations of corticosteroids with antibacterial and antifungal agents have been shown to be very effective in flexural eruptions and secondarily infected dermatoses . As a general rule, the use of topical corticosteroids in outpatients, unless badly misused, is not associated with any significant risk of adrenal axis suppression, but care must be exercised as to the amount prescribed, especially if large areas of the body are to be treated with highly potent preparations . Certain groups such as young children and patients with liver failure, and certain anatomical sites such as the flexures and face appear much more prone to side effects, and in these cases mild or moderate compounds should be used in preference to the stronger preparations. Carbohydr Res, 1980 Feb, 79(1), 91 - 102 4-N-acylfortimicins B and the preparation of fortimicin A from fortimicin B; Tadanier J et al.; Selective 4-N-acylation of fortimicin B (2) has been accomplished by 4-N-acylation of 1,2',6'-tri-N-benzyloxycarbonylfortimicin B (4) followed by hydrogenolysis of the N-protecting benzyloxycarbonyl groups . In this manner, fortimicin B was converted into fortimicin A (1), and a series of 4-N-acylfortimicins B (3) was prepared for antibacterial assay . The key intermediate, 1,2',6'-tri-N-benzyloxycarbonylfortimicin B, was prepared either directly from fortimicin B or by converting fortimicin A into 1,2',6',2''-tetra-N-benzyloxycarbonylfortimicin A (6a), followed by selective hydrolysis of the 4-N-(N-benzyloxycarbonyl)glycyl group of the latter. Infect Immun, 1980 Feb, 27(2), 302 - 8 Bacteriostatic effect of serum: role of antibody to lipopolysaccharide; Fitzgerald SP et al.; Previous work has shown that antibody and transferrin, acting together, exert a bacteriostatic effect on certain pathogenic Escherichia coli . This effect may be due to the ability of the antibody to interfere with the release of the iron chelator, enterochelin, from the bacterial cell . Enterochelin is essential for the transport of iron from transferrin to the bacterial cell . The nature of the bacterial antigen against which the antibody is directed has now been determined by means of adsorption experiments . It was found that absorption of serum either with hear-killed cells of E . coli O111 or with Boivin antigen abolished the bacteriostatic effect . A monosaccharide, which proved to be colitose (3,6-dideoxy-L-galactose), was isolated after acetic acid hydrolysis of the Boivin antigen . Colitose is the terminal monosaccharide of the O-specific side chain of the lipopolysaccharide from E . coli O111 . This monosaccharide abolished the bacteriostatic effect of both whole serum and mixtures of antibody and iron-binding proteins . When administered by the intraperitoneal route, it reduced the resistance of mice to subsequent infection with E . coli O111 . This ability of colitose to interfere with antibacterial mechanisms is in accord with published immunochemical studies. Drugs, 1980 Feb, 19(2), 107 - 18 Acute otitis media: diagnosis and drug therapy; Schwartz RH et al.; Diagnostic criteria for acute otitis media have become more precise with recent improvements in the otoscope and emphasis on meticulous aural toilet and careful observation of the ossicular landmarks, contour and mobility of the tympanic membrane . The treatment of the acute phase of the disease poses few therapeutic difficulties . There are many alternative antibacterial agents which have proven effective against the common middle ear pathogens . However, each drug or combination has indications and associated problems . Middle ear effusion is the most frequent sequelae of acute otitis media occurring after approximately 50% of cases in younger children . Between 5 to 10% of these effusions persist in excess of 3 months . There is intense interest in the prevention of recurrent acute otitis media (in otitis-prone children) by chemoprophylaxis, immunisation or assuring continuous middle ear ventilation by tympanostomy tube insertion . Several major projects are underway to evaluate the role of decongestants in acute middle ear disease. Oral Surg Oral Med Oral Pathol, 1980 Feb, 49(2), 166 - 70 Antibacterial properties of dilute formocresol and eugenol and propylene glycol; Thomas PA et al.; Formocresol and eugenol are the two nonspecific intracanal medicaments commonly used in endodontic practice . Both have high tissue irritation potential when used in conventional strength . Propylene glycol is an alcohol that is injectable and itself possesses significant antibacterial action . It is a popular vehicle and hence was used to modify the two drugs . Standard bacteriologic methods were employed to test the antibacterial action of these lower concentrations of the two drugs against four test organisms . The investigations indicate that formocresol at as low as 10 to 20% and eugenol at 75% are bactericidal in action and hence may be useful at these concentrations for clinical use . Evaluation of these lower concentrations is warranted for possible clinical use . Propylene glycol, which possesses antibacterial action and is remarkably innocuous to tissues, appears to be a suitable vehicle for dilution of formocresol and eugenol. Surg Clin North Am, 1980 Feb, 60(1), 65 - 81 Common adverse effects of antibacterial agents on major organ systems; Calderwood SB et al.; Antibiotics contribute significantly to the management of the surgical patient . However, their potential for adverse effects, both toxic and allergic, must always be kept in mind . We have reviewed the major adverse reactions to antibiotics, so that side effects may be promptly recognized and treated . Armed with this information, the surgeon can more effectively utilize this valuable class of drugs for the benefit of the patient. Boll Soc Ital Biol Sper, 1980 Jan 30, 56(2), 133 - 9 {Evaluation of the antibacterial activity in vitro of various cephalosporins on different gram-negative bacterial species of recent clinical isolation}; Piccolomini R et al.; The Authors have compared the antibacterial activity "in vitro" of new cephalosporines (cephuroxim, cephoxitin and cephaclor) with other cephalosporines having an action which is already known (cephaloridine, cephazoline and cephalexine) on the Gram-negative bacterial strains of recent clinical isolation . The results show that the cephalosporines of last generation, having in their molecular nucleus a methoximinic group, realize a greater antibacterial protection than those cephalosporines of antecedent preparation. Vet Rec, 1980 Jan 19, 106(3), 48 - 52 Investigation of factors affecting superovulation and non-surgical embryo recovery from lactating British Friesian cows; Newcomb R; Factors affecting the success of superovulation and embryo recovery were examined in two groups of 16 lactating Friesian cows which were superovulated twice at five to six week intervals in a 24 factorial experiment . There were no differences in ovarian response using pregnant mare serum gonadotrophin or human menopausal gonadotrophin . A total of 3000 iu human chorionic gonadotrophin given intravenously at the first insemination significantly (P less than 0.01) affected embryo recovery rate . A single intramuscular treatment with releasing hormone had no effect . A lower proportion of unfertilised eggs was recovered after insemination with semen from a bull of above average fertility than with semen from a bull of below average fertility (P less than 0.03) . Insemination routines affected both the proportion of unfertilised eggs (P = 0.06) and embryo recovery rate (P less than 0.03) . Antibacterial treatment given when insemination was carried out after the end of oestrus did not affect success . The three-way circulation system of embryo and fluid recovery was significantly (P less than 0.01) more efficient than the two-way to-and-fro system at day 7 after oestrus, but this appeared to alter at day 8 in favour of the two-way system . A more efficient fluid recovery was achieved with the three-way system (P less than 0.001) . Catheter location, catheter size, interval from calving and condition of the donor did not affect success, but embryo recovery rate from younger cows (less than 4.5 years) was lower than from older animals (4.5 to 7 years) (P less than 0.05). Mikrobiyol Bul, 1980 Jan, 14(1), 53 - 64 {Interactions between antibiotics (author's transl)}; Ata H; Combined antibiotic therapy has been used frequently to obtain broader antibacterial spectrum because of increased antibiotic resistance in microorganisms . However, antibiotics should not be combined for purposes of synergy except in certain serious infections or in infections which cannot be treated with a single drug . Other than antagonism, potential deleterious effects of combined therapy such as broader suppression of normal bacterial flora, greater risk of secondary infections and increased adverse reactions may occur during the treatment . The results of in vivo and in vitro studies in the use of combinations may be different and sometimes good clinical results can be observed with a combined therapy which is antagonistic in vitro . But, this antagonistic interaction will no be sufficient . Therefore, at the beginning of the antibiotic therapy pathogenicity of the infectious agent, defence mechanisms of the patient and the type of interaction between antibiotics must be carefully considered. Scand J Infect Dis, 1980, 12(3), 227 - 30 Cefuroxime in soft tissue infections and septicaemia; Hugo H et al.; Data are presented on the absorption, antibacterial activity, clinical efficacy and side effects of cefuroxime in 33 cases with proven bacterial infection in soft tissues and in patients with septicaemia . The drug was administered mainly intramuscularly (i.m.) but also intravenously (i.v.) . Peak serum concentrations 1 h after an injection of 750 mg cefuroxime i.m . were between 16-25 mug/ml . After 8 h the levels were mostly < 4 mug/ml in patients with normal renal function . I.v . injection gave only slightly higher maximum serum level obtained was approximately 40 mug/ml . No accumulation of the drug occurred in patients with normal renal function . Cefuroxime was active against all the gram-positive bacteria isolated from our patients as well as most of the gram-negatives . The clinical effect was satisfactory in 96% . The drug was well tolerated . Side effects were slight and relatively few. Pharmazie, 1980, 35(9), 550 - 2 A study of the effect of some drugs on the dissolution rate of nitrofurantoin; Naggar VF et al.; Determination of the effect of some drugs on the dissolution rate of 70 mg nitrofurantoin was carried out at 37 degrees C in 500 ml dissolution medium . Hexamine, formamol, sodium salicylate, sodium benzoate, nicotinamide, aminophylline, aminophenazone, phenazone and paracetamol were studied . Hexamine was found to increase the dissolution of nitrofurantoin in either water of Sorensen's phosphate buffer (pH = 5) . Nicotinamide and sodium salicylate enhanced, as well, the dissolution of the antibacterial agent . However, aminophenazone, formamol, phenazone, paracetamol, sodium benzoate, and aminophylline retarded the dissolution rate of the drug . Spectral studies performed on mixtures of either nitrofurantoin-hexamine or nitrofurantoin-aminophenazone, suggested a possible interaction . Further in-vivo studies are needed to determine the effect of these co-administered drugs on the bioavailability of nitrofurantoin. Acta Med Scand, 1980, 207(6), 469 - 73 Methenamine-hippurate and bacteriuria in the geriatric patient with a catheter; Wibell L et al.; Oral treatment with methenamine-hippurate (MH) in patients with an indwelling catheter has been found to reduce the need of frequent catheter exchange and the number of symptomatic infections . Bacteriuria, however, persists during MH treatment . The hypothesis that the therapeutic effect is due to a reduction in the number of bacteria, or a change in the pattern of strains was tested in a crossover study (2 x 6 weeks) . MH treatment, 1 g twice daily, was compared to control periods in 52 patients . The majority of quantitative and qualitative bacterial cultures at 2-week intervals yielded 2--4 strains . Of the bacterial isolates, 50% were found on 4--6 occasions out of 6 possible . MH treatment had no significant influence on the pattern of various strains . A 30% decrease in the mean total bacterial count during MH treatment did not reach statistical significance (p approximately 0.07) . It is suggested that prevention of catheter complications during MH treatment may be due to a physiochemical action on salt formation rather than a direct antibacterial effect. Infection, 1980, 8(3), 101 - 3 Cerebrospinal fluid concentrations of metronidazole, tinidazole and ornidazole in rabbits; Jokipii AM et al.; The penetration of metronidazole, tinidazole and ornidazole into the cerebrospinal fluid (CSF) of rabbits was determined using a bioassay based on the antibacterial activity of the drugs . After an intravenous dose of 50 mg, the CSF levels of each drug exceeded previously reported minimum bactericidal concentrations against Bacteriodes fragilis . Low serum levels of each drug, produced by intramuscular administration of low doses, resulted in CSF/serum ratios ranging from 0.63--0.73. Zentralbl Chir, 1980, 105(2), 87 - 93 {Processing of surgical material with antibacterial and anticoagulant properties (author's transl)}; Smailys AJ et al.; The impregnation of surgical suture material, drainage systems, and implants (rubber, plastic, and metallic objects) with antibiotics and anticoagulants by means of ultrasound in an electric field are discussed . The impregnated objects acquire antibacterial properties which they retain when stored for several months and for 5 to 10 days when implanted into the body . Impregnation with heparin by the same method prevents plugging of the system in long-term intravenous infusion. Curr Med Res Opin, 1980, 6(9), 585 - 8 Tissue levels of cephradine in ischaemic limbs following a single intravenous injection; Bullen BR et al.; A single dose of 2g cephradine was administered intravenously at the time of anaesthetic induction to 20 patients with occlusive arterial disease . Concentrations of cephradine were measured in serum, subcutaneous fat from the groins of 10 patients underdoing arterial reconstruction and in the subcutaneous fat and skeletal muscle of 10 legs amputated for severe arterial ischaemia . Concentrations of cephradine were adequate for antibacterial prophylaxis at the time of operation in all serum samples, 9 out of 10 samples of subcutaneous fat from reconstruction cases, all muscle and 8 of 10 fat samples from the level of section of amputated limbs, and in 8 of 10 muscle and fat samples from the distal parts of amputated limbs . These results confirm that a single intravenous dose of 2 g cephradine given with anaesthetic provides adequate serum and tissue concentrations for antibacterial prophylaxis during vascular surgery. Chir Forum Exp Klin Forsch . 1980;:67-71. {Antibacterial therapy of purulent peritonitis: a prospective randomized study on the effects of antibiotics and taurolin, a new chemotherapeutic and antiendotoxic agent (author's transl)}; Linder MM et al.; A prospective randomized study on the value of additional antibacterial therapy in surgically treated, purulent peritonitis (69 patients) is presented . A new chemotherapeutic agent Taurolin with antiendotoxin activity is tested against conventional antibiotic therapy . There was an increased rate of secondary wound healing and overall complications in the Taurolin group (especially bronchopneumonia) . Local complications and lethality due to peritonitis occur similarly frequently in both groups . The bactericidal and antiendotoxic effects of Taurolin, its lacking toxicity (possibility of higher dosage), and the choice of combination with antibiotics make it a most interesting substance for additional antibacterial therapy for purulent peritonitis following surgical treatment. Br J Clin Pharmacol, 1980 Jan, 9(1), 51 - 5 Factors determining the passage of drugs from blood into saliva; Stephen KW et al.; 1 . Following single oral dosing of ampicillin, cephalexin, tetracycline, erythromycin estolate, clindamycin and rifampicin to six normal volunteers, antibacterial activity was measured at 1, 3 and 6 h in serum, gingival fluid and minor gland saliva from all subjects and in parotid and submandiabular saliva from three . 2 . pH values of all gingival fluid and saliva specimens were noted . 3 . Partition coefficients between n-octanol and water were measured for erythromycin, clindamycin and rifampicin . Published data were used for ampicillin, cephalexin and tetracycline . 4 . All antibiotics, but particularly rifampicin, were detected in gingival fluid . Only rifampicin and to a lesser degree, clindamycin were present in the other salivary constituents . 5 . In studies of secretion of drugs in saliva, both the physico-chemical characteristics of the drugs and the physiological differences between individual salivary components should be considered . 6 . Parotid saliva samples are likely to be of greatest value. Acta Vitaminol Enzymol, 1980, 2(1-2), 27 - 45 Drugs producing vitamin deficiencies; Montenero AS; Many drugs produce vitamin deficiencies . They belong to the most important and common therapeutical classes: analgesics, antianemics, antibacterial and antiblastic agents, antibiotics, antidiabetics, antimalarials, antiphlogistics, antipyretics, diuretics, laxatives and purgatives, tranquilizers and anticonvulsives, radiomimetics, hormones and vitamins themselves . The vitamin deprivation processes may be produced by a variety of mechanisms and may involve all vitamins . Recent experiments indicate that there is a competition for binding sites on proteins between vitamin C and salicylate and between dicoumarol and vitamin K . Usually a drug exerts a "devitaminizing" action with respect to only one vitamin . However there are examples of multiple vitamin deficiencies induced by a single drug, like salicylate which deprives the organism of vitamins C, K and pantothenate . These deficiencies may develop either all at the same time or successively . A direct and concomitant vitamin depriving action occurs when an antibiotic blocks the production of vitamins by the enteric flora . A different mode of action occurs in the drug induced folic acid deficiency, which in turn induces a deficiency of vitamin B12 . It has been reported that a vitamin deficiency may result from intake of high pharmacological doses of other vitamins . These data need confirmation in patients treated with high doses of nicotinic acid . The drug induced vitamin deficiencies are studied with the same methodology employed for avitaminoses in general; hence they can be diagnosed using the same criteria. Scand J Urol Nephrol, 1980, 14(3), 233 - 8 Vesico-ureteral reflux in non-paediatric patients; Erichsen C et al.; In the period 1968-1975 we treated 55 female and 19 male adolescent or adult patients for vesico-ureteral reflux (v . u . r.) to a total of 116 renal units . The reflux was primary in 69 units, secondary in 20 and or mixed type in 27 units . It was of moderate degree in 50 units, 31 (62%) of which showed radiologic nephropathy . Of the 18 units with gross reflux, 16 (89%) showed nephropathy . Re-implantation of 75 ureters in the bladder ad modum Politano-Leadbetter was followed by cessation of reflux in 66 units (88%), with cure of symptoms and bacteriuria in a corresponding number of patients . Infravesical surgery or antibacterial medication were less effective when used alone . Two patients with severely impaired renal function (serum creatinine greater than 440 mumol/l) failed to improve, despite technically successful surgery . Primary v . u . r . in adolescents and adults has often been present since childhood, and many of these patients show radiologic evidence of nephropathy . Effective antireflux treatment should be given early, in order to prevent progressive renal damage. Arzneimittelforschung, 1980, 30(12), 2087 - 90 Antiviral, antibacterial and antitumor activity of the hydrazide and the ethyl ester of 2,2'-anhydro-1-(beta-D-arabinofuranosyl)-orotic acid; Golovinsky E et al.; It has been demonstrated that the hydrazide and the ethyl ester of 2,2'-anhydro-1-(beta-D-arabinofuranosyl) orotic acid inhibit selectively the multiplication of some DNA-containing viruses (PsRV, VV, AdV5), suppress the growth of E . coli and St . aureus in vitro and exhibit an antitumor effect with Lewis lung carcinoma and sarcoma 298. Scand J Infect Dis, 1980, 12(4), 307 - 9 Antibiotic assays in muscle: are conventional tissue levels misleading as indicator of the antibacterial activity? Ryan DM, Cars O. Concentrations of ampicillin and cefuroxime in serum and muscle were studied in rabbits following a single intramuscular injection of 25 mg/kg . Simultaneous measurements were performed in whole muscle tissue pieces and in muscle tissue fluid obtained by implantation of cotton threads under the muscle fascia . The concentrations in the tissue fluid showed only a short time lag to thea serum levels . However, levels in whole muscle were substantially lower than the corresponding concentrations in muscle tissue fluid, indicating that the antibiotics were not evenly distributed within the tissue . The whole muscle tissue levels seriously underestimated, by a factor of approximately 5 times, the actual antibiotic concentrations in the extracellular fluid, where the microorganisms causing soft tissue infections are most likely to be found. Tsitol Genet, 1980 Jan-Feb, 14(1), 60 - 5 {Nature of the mutagenic action of dioxidine on bacteria}; Fonshtein LM et al.; Lethal and mutagenic action of the antibacterial drug dioxidine was studied in bacteria . The mutagenic action of dioxidine is related to rec A-dependent repair process . The effect of the drug was increased due to mutation of rfa in S . typhimurium causing a destruction of the cell wall polyliposaccharide complex . The mutagenic action of dioxidine was studied as applied to isogenic strains of S . typhimurium bearing the pKM-101 plasmid and to strains lacking the plasmid. Zentralbl Bakteriol A, 1980, 247(2), 221 - 8 Antibacterial action of quinolones on Escherichia coli . IIa . Conditions required for lethality: effect of anaerobiosis, inoculum size and media composition; Mahmood F et al.; Quinolones with carboxylic or nitroside groups behaved differently in vitro under various physiological conditions tested . CarboxyQ was not active during the lag phase of E . coli and its activity was proportional to the growth rate under anaerobic conditions . NitroQ was immediately active on the cells soon after the inoculum was introduced under similar conditions . High cell density did not change the typical behaviour of these drugs . Only nitroQ was active in nitrogen-free medium while both were inactive in glucose-free medium . Chloramphenicol, reduced the activity of carboxyQ while that of nitroQ was unaffected. Infection, 1980, 8 Suppl 3, S 313 - 20 Therapeutic drug monitoring of aminoglycoside antibiotics; Reeves DS; Aminoglycosides are widely used antibacterial agents, particularly for serious infections . They have a narrow therapeutic margin of efficacy over toxicity relative to many other agents, a disadvantage which can be obviated to some extent by precise dosing regulated by blood concentration monitoring . The relationships of efficacy and toxicity to concentrations are discussed, as are the practical aspects of clinical indications for monitoring and specimen collection . Dosing by predictive methods is useful but not always of sufficient precision . A large number of methods for assay are now available . With care, microbilogical plate assays can give results of adequate accuracy and selectivity, and with sufficient speed . Immunoassays give more accurate, specific and rapid answers; EMIT, in particular, seems the best method available at the present time . Whichever method is used, control of its accuracy is essential. Histochemistry, 1980, 66(3), 285 - 91 Distribution of lactoferrin in human salivary glands; Reitamo S et al.; An immunoperoxidase technique was used to study the distribution of lactoferrin (LF) in human salivary glands from autopsy tissues fixed in Carnoy's fluid for the optimal preservation of LF antigenicity . Specific LF staining was seen in the intralobular ducts of all salivary glands but never in the interlobular ducts; acinar LF was detected in most serous demilunes of the mixed glands and in some but not all acinar cells of the pure serous glands . No LF was detected in the acinar cells of the pure mucous glands . In the oral tissues studied the only additional cells containing LF were polymorphonuclear leucocytes . Whether LF in the salivary glands is synthesized locally and/or ultrafiltrated from the blood is at present unclear . Present evidence indicates that the biological role of salivary LF is antibacterial. Chemotherapy, 1980, 26(5), 361 - 71 Bacterial growth kinetics of E . coli in the presence of various trimethoprim derivatives alone and in combination with sulfonamides; Seydel JK et al.; Bacterial growth kinetic experiments have been performed to study the potentiating effect of trimethoprim (TMP) AND TMP derivatives on the antibacterial action of sulfonamides (SA) . The TMP derivatives showed different inhibitory effects when used alone . Derivatives with decreased inhibitory activity excerted 'bactericidal' effects only at high concentrations . A rather fast development of bacteria with lower sensitivity against these derivatives has also been observed . In the combined action with SA, however, the same maximal 'kill' rate was observed for TMP derivatives as tetroxoprim or derivative IV (TABLE I) at low concentrations of these inhibitors . Under the experimental conditons there is no significant difference between the studied TMP derivatives and various SA in the combined action. Chemotherapy, 1980, 26(4), 297 - 300 Comparison of sulphadiazine-trimethoprim and sulphamethoxazole-trimethoprim in the treatment of acute respiratory tract infections . Randomized double-blind trial; Salmi HA; The combination of sulphadiazine 225 mg (SD) and trimethoprim 75 mg (TMP) was compared with the combination of sulphamethoxazole 400 mg (SM) and trimethoprim 80 mg (TMP) in the treatment of acute respiratory tract infection using a randomized double-blind clinical trial . The dose of both preparations was two tablets twice daily for 7-14 days . The patients were 200 conscripts hospitalized for an acute respiratory infection warranting antibacterial treatment . The most frequent diagnoses were pneumonia, bronchitis and tonsillitis . The combination SD/TMP was statistically significantly (p less than 0.001) superior to the combination of SM/TMP regarding overall efficacy of all indications . Especially pneumonia and bronchitis responded more favourably to SD/TMP than to SM/TMP . The duration of fever was also shorter (p less than 0.001) with SD/TMP than with SM/TMP . The occurrence of side effects was 2% in both treatment groups. J Bone Joint Surg Am, 1980, 62(4), 620 - 7 Escherichia coli infections in knee joints . The pharmacological and antibacterial effects of intramuscular antibiotics; Schurman DJ et al.; Using a standardized strain of Escherichia coli 06 and a rabbit knee-joint model, we determined the following values: (1) the effective concentrations of amikacin and carbenicillin in vitro against Escherichia coli 06 when used singly or in combination; (2) the levels of each of these antibiotics in serum and synovial fluid after an intramuscular injection; (3) the effectiveness of amikacin in preventing intra-articular infection when it is administered thirty minutes before and six hours after an intra-articular inoculation of the same strain of Escherichia coli; and (4) the synergistic effects of amikacin and carbenicillin in combination both in vitro and in vivo when used together as a single dose six hours after intra-articular bacterial inoculation . Amikacin was much more effective when administered before joint inoculation and the minimum effective (inhibitory) concentrations of amikacin in vitro and in vivo were approximately the same . A synergistic effect of amikacin and carbenicillin in combination was more clearly evident in vitro than in vivo . CLINICAL RELEVANCE: In vitro tests such as determinations of the minimum inhibitory concentration and the minimum bactericidal concentration, and the serum bactericidal test, can provide valuable guides for the determination of minimum goals for antibiotic therapy . These in vitro tests were related to concentrations of antibiotics in tissue assessed by in vivo bacterial challenge tests and were found to be predictive of efficacy in vivo. Scand J Infect Dis, 1980, 12(1), 49 - 53 Antibacterial activity of cefuroxime in human bone; Dornbusch K et al.; Bone samples were taken at orthopaedic surgery from 12 patients, who had been treated with 2 doses of 750 mg cefuroxime by intravenous infusion . After grinding, extraction and assay by the agar diffusion method the levels of cefuroxime ranged between 0.4--1.9 micrograms/g bone . Using an electrophoretic method followed by microbiological assay, higher levels of cefuroxime were measured, possibly because of a diminution in the binding capacity of the bone. J Clin Invest, 1980 Jan, 65(1), 82 - 94 Influence of the Escherichia coli capsule on complement fixation and on phagocytosis and killing by human phagocytes; Horwitz MA et al.; To define mechanisms by which polysaccharide capsules confer enhanced virulence on gram-negative bacteria, we examined the effect of the Escherichia coli capsule on complement fixation to the bacterial surface and on phagocytosis and killing of these bacteria by mouse macrophages and human polymorphonuclear leukocytes (PMN) and monocytes . When E . coli were attached to mouse macrophages with concanavalin A, the macrophages readily phagocytosed unencapsulated but not encapsulated bacteria even in the presence of fresh mouse serum; macrophages did not phagocytose encapsulated E . coli unless antibacterial or anti-Con A antibody was added . Similarly, when these bacteria were attached to human PMN with Con A, PMN ingested unencapsulated but not encapsulated E . coli . PMN phagocytosed and killed encapsulated serum-resistant E . coli only in the presence of both complement and antibacterial antibody; PMN phagocytosed and killed unencapsulated E . coli of the same strain in the presence of complement alone . Fluorescence microscopy showed that antibody had to be present for encapsulated but not unencapsulated E . coli to fix complement to its surface . To examine the role of the complement receptors of human PMN and monocytes in phagocytosis and killing of encapsulated E . coli, we used human and rabbit antibacterial immunoglobulin (Ig)M to fix complement to the bacteria . PMN and monocytes phagocytosed and killed encapsulated E . coli in the presence of both IgM and complement, but not in the presence of either serum opsonin alone . In the presence of antibacterial IgG, PMN and monocytes required complement to effectively phagocytose and kill the E . coli . We conclude that (a) attachment by itself results in ingestion of unencapsulated but not encapsulated E . coli; (b) under physiologic conditions, E . coli are not phagocytosed or killed the absence of antibody, the E . coli capsule blocks complement fixation to the bacterial surface probably by masking surface components, such as lipopolysaccharide, capable of activating the complement pathway; (d) the E . coli capsule imposes a requirement for specific antibacterial antibody for complement fixation; and (e) the complement receptor of human PMN and monocytes mediates phagocytoses of complement-coated encapsulated bacteria and is the primary mediator of phagocytosis and killing of these bacteria. Scand J Infect Dis Suppl, 1980, Suppl 23, 104 - 13 The ototoxic potential of netilmicin compared with amikacin . An animal study in guinea pigs; Wersall J; The potential ototoxicity of netilmicin and amikacin was compared in guinea pigs . When the toxicity in animals is determined two parameters should be discussed: Dose related comparison of ototoxicity and a comparison related to the antibacterial potency . None of the netilmicin test groups (50-100 mg/kg body weight) showed a higher percentage of degenerated hair cells than the control group . Even the individual animals showed a sensory cell damage within the control animal range . With the antibacterial potency taken into account, a dose three times higher was given to the animals treated with amikacin than to those treated with netilmicin . The amikacin group of animals showed a high percentage of degenerated hair cells under these conditions. Microbios, 1980, 28(113-114), 133 - 47 Effect of irgasan on bacterial growth and its adsorption into the cell wall; Meincke BE et al.; Isolated cell walls and whole cells of E . coli, S . aureus and P . aeruginosa were shown to adsorb irgasan, with P . aeruginosa adsorbing the greatest amount of irgasan per microgram of cell wall and whole cell tested . The drug uptake displayed by both cell walls and whole cells appears to be by diffusion . Although P . aeruginosa revealed the highest affinity for the bisphenol of the three organisms tested, it was most resistant to its antibacterial action . These results indicated that the lipid content of the cell wall may be responsible for the degree of adsorption and resistance since P . aeruginosa showed the most adsorption, resistance and the highest cell wall lipid content of the three micro-organisms tested. Zentralbl Bakteriol A, 1980, 248(3), 414 - 21 High-pressure liquid chromatography and microbiological assay in the determination of serum levels using cefradine and cefaclor; Ullmann U; A method for the identification of cefradine and cefaclor by high-pressure liquid chromatography is described in detail . The antibacterial activity in the serum of ten subjects was determined by microbiological methods and by the HPLC method . No statistically significant difference exists between the values obtained by the two procedures . No decomposition of antibiotic occurs in the preparation of the serum sample for HPLC . The recovery rate was 94-105% . With the HPLC method 10 samples can be analysed within 70 min . The advantages and disadvantages of the method are discussed. Folia Microbiol (Praha), 1980, 25(4), 289 - 94 Isolation, characterization and biological activities of verotetrone from a mutant strain of Streptomyces aureofaciens; Prikrylova V et al.; A new metabolite denoted as verotetrone was isolated from the mycelium of the mutant strain Streptomyces aureofaciens NMG-2 . Interpretations of physical data concerning verotetrone and its triacetate and, the determination of its degradation product indicate that verotetrone belongs to pretetramide-type metabolites . Verotetrone exhibits neither antibacterial nor antifungal activity . In vitro it inhibits the synthesis of nucleic acids as well as proteins in Ehrlich ascites carcinoma cells . Both verotetrone and its triacetate interfere in vivo with the metabolism of tumour and lymphoid cells, exhibiting antitumour or immunosuppressive activity . This activity, which is more intense with verotetrone than with its triacetate, is detectable in a dose which is already toxic in some animals. Infection, 1980, Suppl 1, 14 - 20 Dose-activity relationships in chemotherapy; Stille W; The in vitro antibacterial effects of subinhibitory and suprainhibitory concentrations of a number of beta-lactam antibiotics and aminoglycosides on microbial growth are presented . The type and extent of the subinhibitory activity of a drug can be well defined by means of growth curves obtained with different subinhibitory concentrations; from these values one can deduce and define the minimal active concentration (MAC) as the concentration at which morphological alterations or inhibition of growth of the bacteria can be seen . The effect of suprainhibitory concentrations can be evaluated by studying the kinetics of the bactericidal activity of a drug . Different types of bactericidal dose-activity relationships can be observed; in many cases a minimal optimal concentration (MOC) can be defined as the lowest concentration of a drug which causes no further appreciable enhancement of efficacy on increasing the concentration . Usually chemotherapy is carried out at subinhibitory drug levels--with decreasing and increasing concentrations--and at present it would appear difficult to assess these constant changes in an in vitro test . Bacteriologists should thus take into account the clinicians' demands for more precise bacteriological data on antibacterial agents. Infection, 1980, Suppl 1, 096 - 10 An in vitro model for monitoring bacterial responses to antibiotic agents under simulated in vivo conditions; Bergan T et al.; A new in vitro model for the study of bacterial responses to antibacterial agents at exponentially varying concentrations, i . e . at given elimination half-life values simulating in vivo conditions, is described . The initial concentrations and elimination rates of the agents, composition of bacterial milieu, and commencing density of the bacterial population may be altered . The principal responses of key gram-negative and gram-positive species to bactericidal and bacteriostatic agents and experimental variation are described. Derm Beruf Umwelt, 1980, 28(6), 175 - 81 {Aminopenicillin rashes - a multicentric prospective study (author's transl)}; Scherzer W et al.; 538 patients, admitted to the hospitals participating in this study for a variety of indications for antibacterial therapy, were treated by the ampicillin-analogue Epicillin . 42 patients (7.8%) who developed exanthem underwent detailed clinical and immunological investigation . Exanthems were scored according to the form of application and doses of Epicillin as well as to the morphology and time of onset of the exanthem . A variety of serological tests were performed: 1 . total IgE (RIST), 2 . presence of penicilloyl-specific IgE (RAST), 3 . penicilloyl-reactive antibodies using an antiglobulin-haemagglutination-tests . In addition, PHA-induced lymphocyte transformation was studied in 10 patients with exanthems . 38/42 patients developed transient monomorphic morbiliform or scarlatiniform exanthems . 4 . exanthems were classified as urticarial or polymorphic . In contrast to the 38 patients, the latter also were positive in the serological tests as it is observed in patients with IgE-mediated penicillin allergy. Am J Ind Med, 1980, 1(3-4), 349 - 57 Toxicity of metal ions to alveolar macrophages; Castranova V et al.; Significant concentrations of metals are found in the respirable particulate effluents associated with metallurgical smelters . In this investigation the effects of the metallic ions lead, cadmium, iron, mercury, aluminum, chromium, and nickel on various aspects of alveolar macrophage function were studied . The production of antibacterial substances (ie, reactive forms of oxygen) by these cells and oxygen consumption are very sensitive to the metals . Particle uptake displays moderate sensitivity, while lysosomal enzyme activity and membrane integrity are fairly resistant to metals . In addition, the effects of the organic solvents carbon tetrachloride, toluene, and xylene on alveolar macrophage function were tested . These solvents were found to inhibit oxygen consumption and the release of antibacterial substances while not greatly affecting membrane integrity . The results of these experiments indicate that some metals and some organic substances are toxic to alveolar macrophage function. Int J Fertil, 1980, 25(4), 281 - 6 Evaluation of ten potential organic spermicides; Chow PY et al.; PIP: In vitro studies were conducted with 10 potential organic spermicides to test their ability to decrease sperm motility . The organic substances tested were: cytochalasins A and B, N-cetylpyridinium chloride (CPC), N-cetyl-N,N,N-trimethylammonium bromide (CTAB), sodium deoxycholate (SDC), quinine and emetine hydrochlorides, 4-nitrophenyl-4-guanidinobenzoate hydrochloride, n-hexanal, and 6-amidino-2-(4-amidinophenyl) dilactate . The 1st 2 substances are antibiotics secreted by at least 4 different orders of fungi; the next 3 substances are soaps or detergents; quinine derives from the bark of the cinchoa tree and emetine derives from ipecac . The most effective spermicide was the antibacterial cytochalasin A which severely reduced the percentage of motile sperm even at quite low concentrations and caused an instantaneous loss of motility at higher concentrations . The rapidity of the effect and the low concentrations required make this agent a potentially useful spermicide . 2 of the detergent agents, CPC and CTAB, were also very potent, instantly immobilizing sperm at a .1% concentration . All the other agents tested had some spermicidal effect except cytochalasin B which had no effect on sperm motility even at .1% concentration . Genetika, 1979 Dec, 15(12), 2204 - 9 {Sulfalene pharmacogenetics . I . The genetic determination of the pharmacokinetic indices}; Lil'in ET et al.; Genetic determination of pharmacokinetics of sulfalen, a new antibacterial drug, has been studied in 28 twin pairs of Moscow Russian population . In order to determine the degree of heritability of such pharmacokinetic parameters of sulfalen as t 1/2 (half-life); Vd and delta (apparent and specific volumes of distribution) and Co (apparent initial concentration) Holtsinger H-statistics values have been calculated, which are 0.891, 0.866, 0.766 and 0.797 respectively . Possible causes of discrepancies between these values and the coefficients of genetic determination G, calculated by decomposition of general phenotypical dispercion of the parameters via the main equation of quantitative traits of genetics are given (0.913, 0.762, 0.828, 0.856 in that order) . The data obtained make it possible to assume that genetic determination t 1/2 of sulfalen is carried out within the system of monogenous interaction (HD = 0.91, HA = 0), that of Vd and Co--within the system of additive-polygenous interaction, while linear and non-linear effects contribute to delta determination (HD = 0.232, HA = 0.596). J Antibiot (Tokyo), 1979 Dec, 32(12), 1311 - 8 Semisynthetic beta-lactam antibiotics . II Cephalosporin derivatives in the naphthalene series . Chemical and microbiological properties; Quaresima E et al.; A seris of new 7-acylamidocephalosporins, containing a substituted naphthalene moiety in the side chain, has been prepared and tested for their in vitro antibacterial activity . Some observations are made on the structure-activity relationships. Hosp Pract, 1979 Dec, 14(12), 89 - 100 Acute diarrheal infections in infants . I . Epidemiology, Treatment, and prospects for immunoprophylaxis; Levine MM et al.; PIP: Diarrheal disease is bacterial in much of the Third World and viral elsewhere . In the poorest underdeveloped country, as many as 15% of children die from diarrheal disease before their third birthday . This association with geographical or climatic areas of the world, however, is actually a reflection of low socioeconomic levels and poor sanitation for practically all of diarrhea's infectious agents are in fact ubiquitous worldwide . Clinical problems associated with acute diarrhea, irrespective of etiology, relate to dehydration that results from abnormal loss of water and electrolytes in stools . Because an infant's total body weight is 70% water (as opposed to 60% in adults), diarrhea is a particular threat . During diarrheal disease, the major event is the disruption of the recycling of electrolyte-rich digestive fluids, which are nomally secreted into the gastrointestinal tract and then 99% reabsorbed . Treatments include preventive methods, such as public health improvements, and rehydration with glucose-water solutions, either orally or intravenously, depending on extent of dehydration . Vaccine development against rotavirus infection has been stymied by inability to cultivate the organism . However, immunoprophylaxis of bacterial diarrheas has made progress in developing vaccines against enterotoxigenic Escherichia coli . The role of immunity transmitted by breastfeeding is also emphasized . Genetika, 1979 Dec, 15(12), 2210 - 4 {Sulfalene pharmacogenetics . II . The population genetic aspect}; Kholodov LE et al.; Half-life of sulfalen, a new antibacterial drug, with the biotransformation, performed by means of microsomal acetyltransferase, has been studied in 53 individuals of Moscow Russian population . The absence of sex dimorphism for the trait studied is demonstrated . Distribution of individuals according to values of the pharmacokinetic parameter mentioned within the population is bimodal with the correlation of phenotypic frequencies of "rapid" and "slow" inactivators--72 and 28% . Possible causes of discrepancies between the observed sulfalen inactivator frequencies and similar data on isoniazid are discussed. Antimicrob Agents Chemother, 1979 Dec, 16(6), 695 - 700 Enhancement of leukocyte activity against Escherichia coli after brief exposure to chloramphenicol; Pruul H et al.; The effect of brief exposure of Escherichia coli to chloramphenicol on the antibacterial activity of normal human leukocytes was studied by following changes in viability of the bacteria in the presence of leukocytes and serum . Growth was suppressed, and the extent of suppression was directly related to the period of exposure and the concentration of chloramphenicol . When exposed to clinically achievable levels of the drug for 10 min, E . coli failed to resume normal growth for 1 to 4 h in the presence of leukocytes and serum after removal of the drug . The post-antibiotic leukocyte enhancement effect required the presence of antibody and complement . This effect demonstrates the importance of early events in the encounter between antibiotic and microorganism in determining the subsequent activity of host defense components. Am J Med, 1979 Dec, 67(6), 1049 - 57 The contaminated small bowel syndrome; Isaacs PE et al.; Contamination of the small bowel with an abnormal microflora causes a variety of disturbances of intraluminal digestion and of mucosal function resulting in malabsorption of fat, protein, carbohydrate, electrolytes and vitamin B12 . Indirect clinical tests for the presence of small bowel bacterial overgrowth must be supported by careful roentgenologic examination of the small intestine and intestinal aspiration studies to establish a firm pretreatment diagnosis . However, the reversal of absorptive defects by antibacterial therapy is valuable confirmatory evidence. J Antibiot (Tokyo), 1979 Dec, 32(12), 1280 - 7 1-N-Alkyl analogs of butirosin; Hayashi T et al.; Butirosin (Ia), 5''-amino-5''-deoxy-(Ic), 3',4'-dideoxy-(Ie), and 5''-amino-3',4',5''-trideoxy-butirosin A (If) were converted into the corresponding 1'''-deoxo derivatives, Ib, Id, Ig, and Ih by borane reduction . In addition, xylostasin (IIIa) was converted into its 1-N-ethyl derivative (IIIb) by reductive ethylation . Their antibacterial activities were discussed. Biochem J, 1979 Nov 15, 184(2), 427 - 30 Cell-free conversion of delta-(L-alpha-aminoadipyl)-L-cysteinyl-D-valine into an antibiotic with the properties of isopenicillin N in Cephalosporium acremonium; Konomi T et al.; Cell-free extracts of antibiotic-negative mutants of Cephalosporium acremonium converted delta-(L-alpha-aminoadipyl)-L-cysteinyl-D-valine (LLD-tripeptide) into an antibiotic that was destroyed by penicillinase . The enzymic activity of the extracts was destroyed by boiling, but was not inhibited by cycloheximide . LLL-Tripeptide was totally inactive as substrate . The product resembled isopenicillin N, but not penicillin N, in its antibacterial spectrum . We propose that isopenicillin N is the first product of cyclization of LLD-tripeptide. Farmaco {Sci}, 1979 Nov, 34(11), 923 - 35 Synthesis of 7-acylamidodesacetoxycephalosporanic acids and corresponding pivaloyloxymethyl esters . Chemical and microbiological properties; Tinti MO et al.; A series of 7-acylamidodesacetoxycephalosporanic acids and analogous pivaloyloxymethyl esters have been prepared and tested in vitro for antibacterial activity . Those acids which exhibited a significant in vitro activity, were also studied in vivo and compared with the corresponding esters . Experiments performed on laboratory animals showed that, after oral administration, the esters were absorbed more efficiently than the corresponding acids. Antimicrob Agents Chemother, 1979 Nov, 16(5), 533 - 9 Affinities of penicillins and cephalosporins for the penicillin-binding proteins of Escherichia coli K-12 and their antibacterial activity; Curtis NA et al.; The affinities of a range of penicillins and cephalosporins for ther penicillin-binding proteins of Escherichia coli K-12 have been studied, and the results were compared with the antibacterial activity of the compounds against E . coli K-12 and an isogenic permeability mutant . Different penicillins and cephalosporins exhibited different affinities for the "essential" penicillin-binding proteins of E . coli K-12, in a manner which directly correlated with their observed effects upon bacterial morphology . Furthermore, the affinities of the compounds for their "primary" lethal penicillin-binding protein targets showed close agreement with their antibacterial activities against the permeability mutant. Antimicrob Agents Chemother, 1979 Nov, 16(5), 549 - 53 Antibacterial activity of ceftizoxime (FK 749), a new cephalosporin, against cephalosporin-resistant bacteria, and its stability to beta-lactamase; Kojo H et al.; Antibacterial activity of FK 749 against ampicillin-resistant clinical isolates of Escherichia coli was compared with those of other newly developed cephalosporins . FK 749 was the most active against strains possessing R-plasmids specifying ampicillin resistance and those whose resistance was chromosomally determined . The susceptibility of ampicillin-susceptible E . coli to FK 749 was not decreased by transduction of ampicillin resistance-specifying plasmids . However, most of the transconjugants acquired a high level of resistance to cefoperazone and cefamandole and a moderate level of resistance to cefoperazone and cefamandole and a moderate level to cefotiam . FK 749 was highly stable to both penicillinase- and cephalosporinase-type beta-lactamases, including R-plasmid-mediated beta-lactamase . Its level of resistance to beta-lactamases was comparable to those of cefoxitin, cefmetazole, and cefotaxime, slightly superior to that of cefuroxime, and much superior to those of cefotiam, cefamandole, and cefoperazone. Chir Ital, 1979 Oct, 31(5), 696 - 701 {Primary closure of the perineum after Miles's abdominoperineal amputation for carcinoma of the rectum (author's transl)}; Catania G et al.; In view of the results obtained in 32 cases of primary closure of the perineum after amputation of the rectum for cancer, the authors believe that this policy is best after removal of the malignancy by the abdominoperineal approach . Unquestionable advantages are shortening of the patient's hospital stay and a more rapid recovery; the possible disadvantages are relatively rare, from an uncommonly severe dysmetabolic situation to local disorders such as poor hemostasis, contamination of the operation site, inadequate preoperative antibacterial protection, or an unusually large tumor. J Antibiot (Tokyo), 1979 Oct, 32(10), 973 - 7 Synthesis and antibacterial activity of 1-N-(1,3-dihydroxy-2-propyl)kanamycin B (UK-31,214); Richardson K et al.; 1-N-(1,3-Dihydroxy-2-propyl)kanamycin B was prepared and its in vitro activity against aminoglycoside-sensitive and aminoglycoside-resistant organisms was compared with that of kanamycin B and gentamicin . This kanamycin B derivative (code No . UK-31,214) demonstrated potent activity in all of these tests and gave good protection in experimental infections in mice. Clin Plast Surg, 1979 Oct, 6(4), 541 - 3 Difficult wounds: radiation wounds; Krizek TJ; In an era of modern radiotherapy, problems associated with the indiscriminate treatment of benign disease have largely disappeared . Skin sparing effects of super voltage radiation equipment make the problems previously seen with orthovoltage equipment less frequent . Vigilance on the part of the workers in the field, in general, protects from the disasters that befell Thomas Edison's laboratory assistant . Despite these modern advances, the reconstructive surgeon often faces problems of managing acute local radiation injury from accident following planned therapeutic radiation or the ulcerations and breakdowns seen months or years after radiation therapy . The single most serious hazard to surgery in radiated tissue is the lodgment of bacteria in this tissue rendered avascular by the radiation and secondary necrosis from the infection itself . The principles of management are no different from those used for other chronic granulating wounds: local wound care, appropriate topical antibacterial therapy, systemic antibiotics during the perioperative period and, most importantly, adequate soft tissue coverage. Aust Fam Physician, 1979 Oct, 8(10), 1069 - 74 A shortcut to rational prescribing . Matching the bug and the drug; Heffernan M; The rational use of antibacterial chemotherapy in the clinical setting is a necessary objective, but a difficult task . This article presents a particular interpretation of history that links bacteria, conditions and chemotherapy in a prescribing rule that applies to much of the bacterial infection seen in clinical practice . Whilst retaining a rational basis, use of the rule simplifies day-to-day prescribing of antibacterial chemotherapy. Br J Ophthalmol, 1979 Oct, 63(10), 687 - 9 The intraocular penetration of cefuroxime after parenteral administration; Richards AB et al.; Cefuroxime (Zinacef) is a new second generation cephalosporin which is resistant to beta-lactamases produced by both Gram-negative and Gram-positive organisms, with an antibacterial spectrum that includes practically all likely ocular pathogens except pseudomonas . It is shown to penetrate into the eye after intravenous (1.5g) or intramuscular (1 g) injection and achieve therapeutic concentrations, with absence of side effects . Cefuroxime is therefore a useful antibiotic for ophthalimic infections and should have a role in combination with gentamicin in intraocular infections, particularly those of unknown aetiology. Int J Dermatol, 1979 Oct, 18(8), 639 - 44 Sporotrichosis; Segal RJ et al.; Five cases of cutaneous sporotrichosis were seen at the Stanford University Department of Dermatology from 1966 to 1977, where the disease was previously unreported . The possibility of sporotrichosis should be considered when suppurative cutaneous lesions do not respond to antibacterial agents . Skin biopsy of sporotrichotic lesion is often nonspecific, while culture is the best method of diagnosis. Farmaco {Sci}, 1979 Oct, 34(10), 869 - 75 The bromination of 6-methyl-4-methoxy-2H-thiopyran-2-one; Caputo O et al.; The bromination of 6-methyl-4-methoxy-2H-thiopyran-2-one was studied under ionic and radical conditions . The 6-bromomethyl, respectively 6-dibromomethyl derivatives were hydrolyzed to the corresponding 6-hydroxymethyl and 6-formyl derivatives . The antibacterial and antimycotic activities of the new compounds were tested. Farmaco {Sci}, 1979 Oct, 34(10), 858 - 68 A reanalysis of the structure-activity relationships of sulfonamide derivatives; Silipo C et al.; A reanalysis of correspondence between electronic distribution of sulfonamides and their antibacterial activity is proposed . Correlation equations show that the rate limiting steps for sulfonamide action on E . coli cell-free system and whole cell system have similar dependence on the negative logarithm of the ionization constant . The existence of a "bilinear relationship" demonstrates that the whole class of compounds has a single mechanism of action and that permeability factors are unimportant in both biological processes. Zentralbl Bakteriol {B}, 1979 Oct, 169(3-4), 287 - 94 {Studies to investigate the ecological importance of the mass development of Hydrodictyon reticulatum in infiltration basins for drinking water . III . Identification of the active components by the use of spectroscopic methods and gas chromatography (author's transl)}; Olfers-Weber R et al.; Antibacterial substances from H . reticulatum, that was harvested from its natural habitat or grown under culture conditions, could be isolated by extraction with ethanol or by steam destillation from cells as well as from culture filtrate . The active substances were tested by gas chromatography, infrared spectroscopy and mass spectrometry and characterized as a fraction of saturated fatty acids . Its composition seems to depend on external circumstances or culture conditions, respectively, because it differed from experiment to experiment even in samples, harvested at the same day . The most effective acids, active, however, only against grampositive strains are the long chain unsaturated ones with 16 or 18 C-atoms, as shown by bioassay detection (Fig . 3) . The C16 = 3-acid was only found in the strain LB236-1b. Postgrad Med J, 1979 Sep, 55(647), 619 - 21 Aspergillus sinusitis; Grigoriu D et al.; Since 1969, 79 cases of fungal maxillary sinusitis have been diagnosed . Forty-nine were due to Aspergillus fumigatus . There were no underlying diseases which depressed cellular immunity and no patient was receiving immunosuppressive drugs or corticosteroids . Most patients had received antibacterial therapy before the appearance of FMS . Treatment was by surgery, nystatin and econazole. J Clin Pathol, 1979 Sep, 32(9), 944 - 50 A survey of the sensitivity of fresh clinical isolates to cefuroxime and other antibiotics; Potaschmacher LO et al.; The sensitivities to cefuroxime and cephradine of potentially pathogenic bacteria isolated in two British general hospitals comprising 900 beds have been assessed . In a three-month period 2537 strains were studied; 30 microgram cefuroxime discs were used with 2511 strains, and cephradine discs of the same strength were used with 2525 strains . The organisms were also examined routinely for sensitivity to other antibiotics . Overall, 91.7% of the isolates were sensitive to cefuroxime and 85.8% were inhibited by cephradine, the differences in percentage strain susceptibility to cefuroxime and cephradine being mainly a result of the greater activity of cefuroxime against the Gram-negative bacteria . The wide antibacterial effectiveness of cefuroxime should make it a useful antibiotic for the treatment of serious infections including those conditions in which the causative organism has not been identified. J Antibiot (Tokyo), 1979 Sep, 32(9), 868 - 73 Fortimicins C, D and KE, new aminoglycoside antibiotics; Sugimoto M et al.; From the fermentation broth of Micromonospora olivoasterospora CS-26 that produced fortimicins A and B three new aminoglycoside antibiotics, fortimicins C, D and KE, were isolated . Fortimicins C and D exhibited potent, broad spectrum antibacterial activities against Gram-positive and negative bacteria, while fortimicin KE was only weakly active. Clin Orthop, 1979 Sep, (143), 266 - 70 Silver polymethyl methacrylate antibacterial bone cement; Spadaro JA et al.; An improved antibacterial bone cement was sought based on the addition of low concentrations of inorganic silver compounds to polymethyl methacrylate . Composites with AgCl, Ag-AgCl, Ag2O, Ag2SO4 and Ag3PO4 in concentrations of 0.05% to 1% by weight, were tested in vitro against bacterial cultures . All were effective, but Ag2SO4 was especially so, even after 7 weeks of incubation in normal saline . Compressive strength of the cement was not affected by these additions, except in the case of Ag2O . Biocompabibility tests in rabbit muscle for up to 12 weeks showed no significant difference between the Ag -PMM and plain PMM in tissue reactivity, both being minimal . These features, coupled with the broad spectrum of antibacterial activity and low allergic potential of silver, make Ag-PMM an attractive alternative to conventional organic antibiotic/bone cement composites. J Pharm Sci, 1979 Sep, 68(9), 1081 - 4 Quantitative structure-selectivity relationships: selective drug design; Garzia A et al.; The concept of complex selectivity (Scn) permits the investigation of quantitative structure--selectivity relationships in the presence of n side effects; Scn permits differentiation of the most selective molecules rather than the most active ones in a congener series . Selectivity quantification in the presence of n side effects facilitates molecular comparisons . The information provided by Scn and its changes with increasing n is discussed . The proposed mathematical model is applied to the study of the selectivity of some antibiotics and antibacterial agents. Rev Infect Dis, 1979 Sep-Oct, 1(5), 807 - 12 Interactions between antibacterial drugs below the minimal inhibitory concentration; Greenwood D; Interaction between antibacterial agents is often assessed in chessboard titrations, in which bacteriostatic synergy is detected as a mutual reduction in the minimal inhibitory concentrations (MICs) of the agents being tested . If MIC titrations are continually monitored turbidimetrically, the conventionally determined "end point" is seen to reflect the final outcome of a series of events that have occurred during the incubation period . One factor that influences the end point is the emergence, during overnight incubation, of a bacterial population with slightly increased drug resistance . A frequent component of the synergy recorded in chessboard titrations is the mutual suppression of such adaptive resistance . Synergy can also be expressed in terms of the minimal antibiotic concentration (MAC), i.e., the lowest concentration needed to produce an observable antibacterial effect . Antibacterial agents that exhibit true biochemical synergy interact to cause a mutual reduction in the MAC, but the degree of synergy recorded in this way is substantially lower than that determined by conventional chessboard titration . The benefits of antibacterial synergy in therapy cannot be predicted based on chessboard titrations alone . Dramatic synergy of the trimethoprim-sulfamethoxazole type may be of limited clinical use, whereas other drug combinations may be more useful than the results of cross-titration suggest. Cancer Lett, 1979 Sep, 7(5), 289 - 98 Reduction in the formation of carcinogen-induced transformed foci by pencillin G sodium in the C3H/10T1/2 CL8 cell lines; Bertram JS; The C3H/10T1/2 CL8 cell line is being widely used to study mechanisms of malignant transformation in vitro . As currently employed, the standard assay system uses a combination of penicillin (100 I.U./ml) and streptomycin (50 micrograms/ml) to reduce the occurrence of bacterial contamination . The penicillin component of this mixture has been discovered to cause a reduction in the number of transformed foci which develop after exposure of cells to MCA, DMBA and X-rays . This reduction is dose dependent; 500 I.U./ml virtually eliminates transformation, while 100 I.U./ml causes an approximate 50% decrease in the number of foci . This effect does not appear to be due to overt toxicity and is largely reversible on removal of the antibiotic . Gentamicin (25 micrograms/ml) causes no reduction in the formation of transformed foci when compared to cultures maintained in antibiotic-free medium and offers the advantages of chemical stability, a wider spectrum of antibacterial activity in comparison with penicillin/streptomycin and, in addition, is active against many mycoplasma . It is suggested that future studies with this cell line should ideally be performed without antibiotics or should employ Gentamicin for antibacterial protection. Wien Klin Wochenschr, 1979 Aug 10, 91(15), 521 - 4 {Mixed infection after renal transplantation (author's transl)}; Zazgornik J et al.; Severe mixed infection was observed in 9 out of 101 renal transplant recipients over a period of 6 years and was characterized by the simultaneous incidence of bacterial, fungal and viral infections . Severe septicaemia was clinically evident in all cases . The critical clinical situation called for a rapid assessment of the differential diagnosis and relevant bacterial, fungal and viral investigations . Antibacterial and antimycotic therapy must be instituted as soon as possible on account of the high mortality from mixed infection in renal transplant recipients . The reduction or discontinuation of immunosuppressive therapy during infection did not impair renal transplant function. JAMA, 1979 Aug 3, 242(5), 442 - 4 Improved life expectancy for children with exstrophy of the bladder; Macfarlane MT et al.; Life-table techniques demonstrate a 98% ten-year survival, a 96% 20-year survival, and 91% 35-year survival of children with exstrophy of the bladder . These figures represent a vast improvement over the earlier figures, due in large part to technical advances that have been made in areas of surgery, anesthesia, and antibacterial and metabolic therapy. Appl Environ Microbiol, 1979 Aug, 38(2), 311 - 3 Microbial transformations of natural antitumor agents: conversion of lapachol to dehydro-alpha-lapachone by Curvularia lunata; Otten S et al.; Microbial transformation of lapachol, a naturally occurring naphthoquinone, was carried out by Curvularia lunata (NRRL 2178) . The fungus brings about oxidative cyclization of the substrate to dehydro-alpha-lapachone, which was isolated and characterized by nuclear magnetic resonance and mass spectral analyses; its structure was verified by chemical synthesis . The metabolite is a naturally occurring chromene possessing antibacterial and antitumor activities. J Med Chem, 1979 Aug, 22(8), 977 - 80 Antileukemic activity of derivatives of 1,2-dimethyl-3,4-bis(hydroxymethyl)-5-phenylpyrrole bis(N-methylcarbamate); Anderson WK et al.; A series of phenyl-substituted derivatives of 1,2-dimethyl-3,4-bis(hydroxymethyl)-5-phenylpyrrole bis(N-methylcarbamate) (1) were synthesized and tested for antileukemic activity against P388 lymphocytic leukemia in the mouse . All of the compounds tested, 1a--r, showed significant activity in this assay . Selected derivatives of 1 were tested against several bacteria and were found to have little or no antibacterial activity in the systems examined. Boll Soc Ital Biol Sper, 1979 Jul 30, 55(14), 1348 - 54 {"In vitro" and "in vivo" antibacterial activity of a new synthetic antibiotic cinoxacin}; Ravagnan G et al.; The Authors have conducted the experimental studies tending to valuate the antibacterial activity in vitro and in vivo of cinoxacin versus that demonstrated by nalidixic acid . The obtained results demonstrate the cinoxacin presents a similar antibacterial activity to that of nalidixic acid. J Biol Chem, 1979 Jul 25, 254(14), 6392 - 6 Synthesis of a peptide form of N-delta-(phosphonoacetyl)-L-ornithine . Its antibacterial effect through the specific inhibition of Escherichia coli L-ornithine carbamoyltransferase; Penninckx M et al.; N-delta-(Phosphonoacetyl)-L-ornithine is a potent inhibitor of the Escherichia coli L-ornithine carbamoyltransferase (Ki = 0.77 microM, pH 8.0, 37 degrees C) . Nevertheless, the analog does not cross the bacterial membrane . Therefore we have designed a tripeptide, glycylglycyl-N-delta-(phosphonoacetyl)-L-ornithine, to take advantage of the broad specificity of the oligopeptide permease system of the bacterium . A lag effect, related to the tripeptide concentration, was observed in the growth of the wild type P4X strain . At high concentration (greater than or equal to 0.75 mM) the peptide appears to be bacteriostatic and the cells which escape this action were characterized gentically as mutants devoid of the oligopeptide transport system . It was shown that the in vivo cellular target of the toxic tripeptide is solely restricted to L-ornithine carbamoyl-transferase and that the tripeptide is probably split in the cell to permit an effective inhibition by N-delta-(phosphonoacetyl)-L-ornithine . Resistance of the wild type cells to moderate levels (less than 0.75 mM) of the phosphonic analog is accompanied by a derepression of the L-ornithine carbamoyltransferase activity . The P4XB2 strain, which is an arg R regulatory mutant, has a reduced lag effect in the presence of the tripeptide and appears to react to the intoxication by a further adjustment of the L-ornithine carbamoyltransferase cellular level. Mol Gen Genet, 1979 Jul 24, 174(3), 317 - 25 Suppressor mutations causing partial reversion in the amiA region of Pneumococcus; George Y et al.; Mutants of an aminopterin-resistant strain of pneumococcus possessing four different suppressor genes have been isolated after mutagenesis with 5-BUdR . The suppressed strains exhibit a partial revertant phenotype since the parental aminopterin resistance remained unchanged but the associated sensitivity to an excess concentration of the branched chain amino acids L-isoleucine, L-valine and L-leucine was diminished almost to the level of the wild-type strain C13 . The suppressor mutations had therefore dissociated the two properties associated with a mutation in the amiA cistron, namely aminopterin resistance and isoleucine sensitivity . The suppressor genes reduced the sensitivity to isoleucine of a number of amiA mutants, but had no effect on the level of resistance to a number of unrelated genes conferring resistance to other antibacterial substances . The suppressor mutations themselves did not confer resistance to aminopterin . Mapping of the suppressor mutations by recombination analysis and by clonal analysis showed them to be intragenic lying in the region near to the amiA-r19, amiA-r23, amiA-r17 loci. Pharmazie, 1979 Jul, 34(7), 423 - 5 {The antibacterial activity of some substituted cysteine sulphonamides and peptides containing cysteine sulphonamide}; Maneva L et al.; The authors investigated the antibacterial activity of some cysteine sulphonamides substituted in the sulphonamide group as well as that of some peptides containing cysteine sulphonamide . They found that the antibacterial activity of these compounds was in part considerably stronger than that of cysteine sulphonamide. J Trauma, 1979 Jul, 19(7), 502 - 11 Fresh-frozen plasma vs . plasma protein derivative as adjunctive therapy for patients with massive burns; Alexander JW et al.; Twenty patients with burn injuries involving 45% or more total body surface area were randomly allocated to receive either fresh-frozen plasma (plasma), 200 ml/m2/d (11 patients), or an approximately equal amount of plasma protein derivative (Plasmanate) (nine patients) during the first 45 days postburn . To study the potential effects of these two adjunctive therapies on host resistance to infection, measurements were made twice weekly of the antibacterial funciton of neutrophils, the opsonic index (ability to opsonize alternative pathway dependent E . coli 075), C3(B), IgG, properdin, factor B, total protein, and albumin . The average size of burn in the plasma group was 61.5% total and 42% 3 degrees compared with 61% total and 46% 3 degrees in the Plasmanate group . Ten and 18 episodes of bacteremia occurred in the plasma and Plasmanate groups, respectively . Analysis of the results indicates only slightly better support of host resistance when plasma is administered, but this is counterbalanced by the increased risk of viral hepatitis. J Pharm Sci, 1979 Jul, 68(7), 924 - 5 Antibacterial activity of Artemisia herba-alba; Yashphe J et al.; The antibacterial activity of Artemisia herba-alba was investigated . Only its essential oil was active against some Gram-positive and Gram-negative bacteria . The essential oil was fractionated by column chromatography, and these fractions were tested for antibacterial activity . The principal component of the most active fraction was santolina alcohol. J Biomed Mater Res, 1979 Jul, 13(4), 623 - 30 Mechanical properties of antibacterial silicone rubber for hydrocephalus shunts; van Noort R et al.; In an effort to find a solution to the serious problem of bacterial colonization of cerebrospinal-fluid shunting devices, room-temperature and heat-vulcanizing silicone rubbers were impregnated with gentamicin sulphate . The effects on the mechanical properties of the two rubbers were studied . Results show that the tensile strength and extensibility of the room-temperature-vulcanizing silicone rubber reduced with increasing concentration of the drug . For the heat-vulcanizing silicone rubber, the tensile strength was also found to decrease with increasing drug content . The extensibility after an initial reduction at low concentrations was found to increase at drug concentrations in excess of 10 mg/g . Nevertheless, the changes in mechanical properties measured are considered not to be so great as to preclude the application of drug-impregnated silicone rubbers to cerebrospinal-fluid shunting devices. Antibiotiki, 1979 Jul, 24(7), 493 - 6 {Sensitivity to antibacterial preparations of the pseudotuberculosis bacteria isolated on the territory of the Ukraine}; Sakal' NN et al.; Sensitivity of 92 strains of the causative agent of pseudotuberculosis isolated in the Ukraine was studied with respect to 26 antibacterial drugs . It was found that the strains of the pseudotuberculous bacteria were sensitive to 17 drugs, i.e . benzylpenicillin, ampicillin, carbenicillin, cephaloridin, chloramphenicol, tetracycline, streptomycin, neomycin, monomycin, kanamycin, gentamicin, polymyxin, colistin, furadontin, nalidixic acid, sulfisoxazol and septrin . No differences in the sensitivity of the strains isolated in various districts of the Ukraine and from various sources were found . By their antibiotic sensitivity the strains isolated in the Ukraine did not differ from the cultures isolated in other districts of the USSR and abroad. Surgery, 1979 Jul, 86(1), 94 - 104 A comparison of immunologic profiles and their influence on bacteremia in surgical patients with a high risk of infection; Alexander JW et al.; Prospective sequential studies of the antibacterial function of neutrophils, lymphocyte responsiveness, opsonic capacity of serum and serum levels of C3(B), properdin, factor B, IgG, and albumin were made in 32 patients with severe burn injury (greater than or equal to 45%), 21 patients with severe multisystem traumatic injury, 20 high-risk, infected patients, and 22 renal transplant patients . Fifty-five episodes of bacteremia occurred in 37 of the 95 patients . Abnormal neutrophil function was clearly associated as a predisposing factor to these episodes, whereas there was no association between bacteremia and low serum levels of C3, IgG, factor B, or properdin . C3, factor B, and IgG usually rose following bacteremia as acute phase proteins, but there was evidence of a consumptive opsoninopathy in 11% of episodes . Defective opsonization was associated with a high risk of bacteremia only when there was a coexisting abnormality of neutrophil function (88% of such patients became bacteremic) . None of 27 nonburned patients tested with delayed hypersensitivity antigens responded normally, and there was regularly depression of lymphocyte responsiveness to phytohemagglutinin-A and concanavalin-A in a whole blood assay related to serum immunosuppressive factors, but poor responsiveness was not associated with bacteremia. S Afr Med J, 1979 Jun 23, 55(26), 1059 - 60 Antibacterial activity of amniotic fluid; Woods DL et al.; The antibacterial activity of amniotic fluid against Escherichia coli in the last month of pregnancy was reduced in an unselected sample of mothers delivering in Cape Town . Amniotic fluid zinc, required for normal antibacterial activity, was also reduced . These findings offer an explanation for the high incidence of amniotic fluid infection previously reported. Clin Chim Acta, 1979 Jun 15, 94(3), 211 - 7 Sulfonamide inhibition of human alkaline phosphatase; Price GH; Several sulfonamides used as antibacterial or diuretic drugs are potent alkaline phosphatase inhibitors . The mechanism of inhibition may involve binding of the zinc in the active site of the enzyme by the unbonded electron pair on the sulfonamide group nitrogen atom as well as binding of the drug to a second site . Addition of progressively larger groups to this nitrogen leads to an increasing loss of inhibitory capability . Isoenzymes from human liver, bone, kidney, granulation tissue and intestine are inhibited to a similar extent while the placenta isoenzyme is more resistant . It is suggested that some pharmacologic actions of sulfonamides may be due to inhibition of alkaline phosphatase, rather than carbonic anhydrase. Quad Sclavo Diagn, 1979 Jun, 15 Suppl 1, 803 - 8 {Environment microbiological control in a department with patients at great risk (author's transl)}; D'Antonio D et al.; Microbic flora has been studied in the Centro di Rianimazione of the Ospedali Riuniti in Chieti to control validity of the antibacterial systems and to verify efficacy of the filter systems that allow the admission into the isolation boxes, stopping great bacterial exogenous increases . These inspection have been executed by suction system Batteriological Air Pollution Detector. Quad Sclavo Diagn, 1979 Jun, 15 Suppl 1, 532 - 79 {Quantitative evaluation methods of the chemoantibiotic associations (author's transl)}; Gori E et al.; In the introductory part a new classification of joint drug actions is submitted, according which three fundamental types are distincted, named respectively interference, cooperation and true interaction . In its turn, interaction is subdivided in three classes (uni-effectual, bis-ineffectual, bis-effectual) in the last of which is placed the most relevant of the interactions, that is synergism, subclassified, at its turn, as additive, super and infra-additive . The second part is devoted to the classification of the bacteriological techniques hitherto proposed in order to evaluate in vitro and in vivo the antibacterial interaction of chemoantibiotics . The third part is devoted to the classification and critical analysis of biometrical techniques hitherto applied to above quoted bacteriological techniques in order to obtain a quantitative evaluation of interaction . Criticism versus isobolic model is pointed out . In the final part a new procedure, named isoeffectual, is proposed . According to such a procedure a close grid of single and joint concentrations of a couple of chemoantibiotics, broad enough in order to cover the whole of the effects to be explored, is tested in vitro adopting the one-center agar diffusion test or a liquid medium . The experimental data so obtained are related in a planar diagram to the log of the sum obtained by adding to the concentrations of the first the concentrations of the second agent, converted into equi-effectual concentrations of the first . By this way a series of curvilinear regressions is obtained, which may be all explained by a mathematical formula according which the data may be submitted to statistical analysis and elaborated in order to draw the parameters able to define quantitatively the interaction . The model so applied is discussed as a general model for joint drug action. Quad Sclavo Diagn, 1979 Jun, 15 Suppl 1, 517 - 22 {Practical meaning of the determination of the minimal inhibitory concentration (MIC) and the minimal bactericidal concentration (MBC) (author's transl)}; Sanfilippo A; The minimal inhibitory concentration (MIC) and the minimal bactericidal concentration (MBC) are the parameters generally used for evaluation of the activity of antibacterial agents . Particular care must be taken for the control of experimental conditions in which the MICs and the MBCs are determined (medium, inoculum, incubation, etc.) in order to obtain informations able to help in the choice and management of the dosage regimen of an antibacterial agent . The significance of MIC and MBC is discussed in connection with blood and tissue levels attainable during therapy and with the pharmacokinetic properties of a drug. J Med Chem, 1979 Jun, 22(6), 743 - 5 Synthesis and antibacterial activity of 2-oxocephalosporins; Kim CU et al.; The first reported synthesis of 2-oxocephalosporin derivatives has been achieved via ozonolysis of the corresponding 2-methylenecephalosporins . The new cephalosporin derivatives showed some antibacterial activity against Gram-positive bacteria, but the 2-oxo analogue of cephalothin was much less active than cephalothin itself. Quad Sclavo Diagn, 1979 Jun, 15 Suppl 1, 785 - 92 {Correlation between antibacterial activity of some cephalosporins and pharmacokinetic properties "in vitro" (author's transl)}; Tamassia V et al.; A new apparatus is described which can be used to investigate the in vitro antibacterial activity of antibiotics as a function of different concentration-time curves . The apparatus can be adjusted to simulate the biexponential serum level curves observed in vivo after oral or intramuscular administration . Preliminary studies were carried out with cefazolin against an E . coli strain simulating initial concentrations of 5, 10 and 20 micrograms/ml that decreased exponentially with half-lives of 30, 60 and 120 min . In all the situations tested there was an initial phase of rapid bactericidal activity followed by a phase of bacteriostatic activity, whose length depended on the drug elimination rate but was relactively independent of the initial concentrations . Bacterial regrowth occurred when the antibiotic concentration fell below the minimum inhibitory concentration (MIC) of the drug . The antibacterial activity of cefazolin, cephacetrile, and cephradine against an E . coli strains was also investigated, in a medium containing 4% human albumin, simulating the serum level curves observed in humans after an intramuscular dose of 1 g . The results obtained confirm that, for cephalosporins, the dosage schedule should be adjusted taking into account the potency of the drug (MIC) and its rate of elimination. Br J Exp Pathol, 1979 Jun, 60(3), 252 - 8 Lactoperoxidase activity in guinea-pig milk and saliva: correlation in milk of lactoperoxidase with bactericidal activity against Escherichia coli; Stephens S et al.; The lactoperoxidase (LPO) activity in guinea-pig milk and saliva has been investigated in sows suckling normal young, and young orally infected with Escherichia coli . There was a 5-fold increase in activity in milk during the 3--4 weeks of lactation; infection of the young did not alter this . There was no comparable increase in lactoperoxidase activity of saliva during this same period, either in the infected or non-infected group . The antibacterial activity of milk from sows suckling normal young increased with the lactoperoxidase, and this bactericidal activity could be reversed by LPO inhibitors such as penicillamine and cysteine but not by addition of sufficient iron to saturate the lactoferrin . In milk from sows suckling infected young, bacteriostatic activity occurring in samples from about 14 days after infection needed iron or both iron and penicillamine (or cysteine) for reversal, indicating that both the antibody-lactoferrin system and the LPO system may be involved in the infected state. Mutat Res, 1979 Jun, 67(2), 133 - 44 Action of nitrofurans on E . coli: mutation and induction and repair of daughter-strand gaps in DNA; Lu C et al.; The antibacterial and mutagenic potency of 9 nitrofurans in "treat and plate" experiments varied over almost 5 orders of magnitude . The relative toxicities were as follows: FANFT greater than AF2 greater than ANFT greather than furazolidone greater than furagin greater than nitrofurantoin greater than nitrofurazone greater than methylnitrofuroate greater than nitrofuroic acid . In general, mutagenic activity paralleled toxicity . The compounds at concentrations corresponding to their LD50's, induced mutations at frequencies which ranged from 2.5/10(6) survivors for FANFT to 130/10(6) survivors for furagin (NF416) . The observed differences in antibacterial and mutagenic activity are unlikely to be due to lack of activation of the weaker agents since the two most potent agents were reduced somewhat more slowly than many of the less active agents . The relative sensitivities to the antibacterial effects of AF2 of strains WP2, WP2 uvrA, CM561 (lexA) and CM571 (recA) were 1 : 1.6 : 3 : 7 and to nitrofurazone 1 : 1 : 25 : 50 . The wvrA strain was 6--7-fold more mutable with both these agents than was WP2 . No increase over the spontaneous mutation frequency was observed when recA or lexA strains were exposed to either AF2 or nitrofurazone in these experiments . When wild-type of wvrA bacteria containing nitrofuran-induced lesions replicated their DNA in drug-free medium in the presence of {3H}thymidine for 5 min, the label was found in low molecular weight DNA indicating that daughter-strand gaps were formed . During subsequent incubation in nonradioactive medium the molecular weight of the DNA increased to the control value . A recA strain (which was very sensitive to the lethal effects of AF2 and nitrofurazone) lacked the ability to repair daughter-strand gaps caused by nitrofuran-induced lesions. J Bacteriol, 1979 Jun, 138(3), 976 - 83 Binding of lysozyme to common pili of Escherichia coli; McMichael JC et al.; Common pili from Escherichia coli were found to bind hen egg white lysozyme . The binding was highly dependent on ionic strength, and the maximum binding occurred near an ionic strength of 0.02 . The pili were aggregated by lysozyme, and this process could be followed by optical turbidity, electron microscopy, and coprecipitation . Near the maximum saturation of binding, one lysozyme molecule was bound by two pilus protein subunits . Electron micrographs of this aggregate indicated that they were paracrystalline structures . Piliated bacteria were more readily agglutinated by lysozyme than were nonpiliated bacteria . Since lysozyme is considered to be an antibacterial humoral factor and since pili are considered to be a colonization factor, the binding of lysozyme may represent an important bacterium-host interaction Am J Surg, 1979 Jun, 137(6), 780 - 5 Intraperitoneal povidone-iodine in experimental canine and murine peritonitis; Bolton JS et al.; In dogs with appendicitis-peritonitis, intraperitoneal povidone-iodine caused death more rapidly than the instillation of saline solution . The bacterial content of canine peritoneal fluid increased with time . Although fewer bacteria were found in fluid from povidone-iodine-treated dogs, the differences were not statistically significant . Qualitative chemical analysis of peritoneal fluid revealed iodide, but not free iodine, 15 to 30 minutes after instillation of povidone-iodine . Iodine was present in the peritoneum at 2 hours but not at 3 or 6 hours . The antibacterial effect of povidone-iodine was demonstrated in mice challenged intraperitoneally with lethal doses of Escherichia coli . Povidone-iodine diminished mortality when injected immediately (p less than 0.005) but not when given 1 to 3 hours later . Immediate injection of povidone-iodine into mice lowered the number of E . coli by 3 logs . Injection of povidone-iodine 3 hours after bacterial challenge lowered the number of E . coli by only 1/3 log . This lesser bactericidal effect in mice is attributed to greater dispersal and sequestration of bacteria throughout the peritoneal cavity with time and with inactivation of povidone-iodine by reduction to iodide in vivo . In dogs with appendicitis-peritonitis, the more rapid death after treatment with povidone-iodine was not associated with differences in peritoneal microflora but with peritoneal absorption of excessive amounts of iodide. Quad Sclavo Diagn, 1979 Jun, 15 Suppl 1, 777 - 84 {Observations on antibacterial activity of thiamphenicol glycinate acetylcysteinate (author's transl)}; Marca G et al.; In vitro thiamphenicol antibacterial activity in the presence of N-acetylcysteine as sodium salt proved to be enhanced when compared with that of the antibacterial alone against both Gram-positive and Gram-negative bacterial strains . The in vitro results were confirmed in vivo in the guinea-pig, where the sera from animals previously treated by i.m . route with thiamphenicol glycinate acetylcysteinate, showed a higher antibacterial activity than sera from animals treated with thiamphenicol glycinate hydrochloride . The observation, even after allowing for differences between species might be of some interest in view of use of this chemotherapeutic agent in the treatment of respiratory infections. Minerva Ginecol, 1979 Jun, 31(6), 483 - 6 {Study of a topical antibacterial, contraceptive, antifungal and anti-venereal pharmacological combination . III . Post-coital test of the spermicidal action of a combination of oxyquinoline sulfate, copper sulfate and lactic acid}; Franchi F et al.; PIP: 30 fertile couples volunteered to test a new spermicidal vaginal cream . The cream, an association of oxyguinoline sulphate, copper sulphate, and lactic acid, was applied before and during intercourse . Postcoital tests were done with material taken from the posterior fornix and from the cervical mucus to investigate the presence and motility of spermatozoa . No mobile forms were found, while preceding spermiograms had evaluated that count, motility, and morphology of the partners' spermatozoa were perfectly normal . From these results it can be stated that the drug can be a valid alternative to oral or intrauterine contraception, being safe, easy, cheap, and without side effects . Quad Sclavo Diagn, 1979 Jun, 15 Suppl 1, 656 - 61 {Culture media for antibiotic sensitivity testing (author's transl)}; Bridson EY; The medium is undoubtedly one of the most important factors influencing the sensitivity testing techniques . The possible role of pH and different components of media, as such as the concentration of peptone, tymidine or tymine, riboflavin, cations (MG++, Ca++, Fe++), mineral salts, agar and phosphate (added eventually with buffer solutions) is discussed . The conclusions point to the need of synthetic media which are suitable for growing all common pathogens and to not interfere with the antibacterial activity of drugs. Anaesth Intensive Care, 1979 May, 7(2), 143 - 7 Intravenous erythromycin in acute chest infections in critically ill patients; Cade JF et al.; Superinfections with resistant micro-organisms have recently become an increasing problem in hospital patients and are throught to be contributed to by inappropriate use of newer, broad-spectrum antibiotics . Erythromycin exhibits a more limited spectrum of antibacterial activity and was therefore re-evaluated in the treatment of acute chest infections in critically ill patients . Twenty-one patients were given erythromycin in a dose of 1.8 g per day by continuous intravenous infusion for up to five days . A satisfactory clinical response occurred in ten patients, in all of whom erythromycin-sensitive micro-organisms were isolated from sputum . An unsatisfactory response occurred in six patients, all associated with micro-organisms insensitive to erythromycin and requiring alternative antibiotic treatment . No undesirable side-effects were noted . It is concluded that erythromycin is a safe and useful agent in the routine treatment of acute chest infections in critically ill patients. Zentralbl Bakteriol {B}, 1979 May, 168(3-4), 331 - 42 {Studies to investigate the ecological importance of the mass development of Hydrodictyon reticulatum in infiltration basins for drinking water . I . Metabolic products and their effect on various types of bacteria (author's transl)}; Olfers-Weber R et al.; Cells of the green freshwater alga H . reticulatum, harvested from their natural habitat, were found to have antibacterial activity . The active substances seem to be lipophilic, because ethanol extracts were more effective, especially against Bac . subtilis, than water extracts (Table 4) . The different effects of water extracts, which were tested after various dilution steps (Table 1--3) presume, that there must be a second active substance . We suppose, that it is correlated with chlorophyll derivatives . Culture filtrate from a strain, grown under laboratory conditions, was tested in the same way . Concentrated tenfold it was active against several grampositive strains of bacteria. Vestn Khir Im I I Grek, 1979 May, 122(5), 56 - 8 {Tuberculosis of the breast}; Zhivetskii AV; The author observed 6 cases of mammary gland tuberculosis . 3 patients showed disseminated nodular form of mammary gland tuberculosis, 2--sclerotic form and 1--ulcerative form . Contrast-free mammography is an essential aid in diagnosis . Surgical intervention with postoperative specific antibacterial therapy is a radical method of treatment . Sectoral resection of the mammary gland should be carried out in young patients and amputation--in elderly ones. J Med Chem, 1979 May, 22(5), 559 - 64 Synthesis and antibacterial activity of 2'-substituted chelocardin analogues; Garmaise DL et al.; Chelocardin (1) was condensed with numerous hydrazines, hydrazides, and anilines, yielding 2'-substituted derivatives with antibacterial spectra similar to the parent antibiotic . The hydrazone derivatives 9 and 10 and the two anilino derivatives 42 and 44 had more in vivo antibacterial activity than chelocardin. Zh Mikrobiol Epidemiol Immunobiol, 1979 May, (5), 26 - 30 {Antilymphocyte immunoglobulin with an associated antibacterial directed effect . II . The use of the preparation in the overall therapy of chronic lympholeukemia}; Shabalin VN et al.; Use in the composition of complex therapy of patients suffering from chronic lympholeukemia of antilymphocytic immunoglobulin with an associated antibacterial activity aided normalization of the leukocytic differential count and prevented development of inflammatory and septic complications in these patients. Antibiotiki, 1979 May, 24(5), 331 - 6 {Comparative experimental study of cyclacillin and ampicillin}; Rudzit EA et al.; Cyclacillin was compared with ampicillin by its bacteriostatic efficiency in vitro, chemotherapeutic efficiency in experimental infections of mice and rats and pharmacokinetic characteristics . It was found that cyclacillin was not superior to ampicillin by its antibacterial action . By a number of characteristics it was even significantly inferior . The pharmacokinetic advantages of cyclacillin were not considered significant. J Dent Res, 1979 May, 58(5), 1471 - 7 Effect of two antibacterial mouth sprays and dentifrices on dental plaque and gingivitis in beagle dogs; Compton FH et al.; Plaque inhibition by dilute mouth sprays and dentrifrices containing benzethonium chloride and chlorhexidine gluconate was compared in beagle dogs . Agents with chlorhexidine gluconate produced less plaque than their benzethonium chloride or placebo counterparts, but the differences were not significant when compared to mean control scores registered during interexperimental recovery periods. Minerva Ginecol, 1979 May, 31(5), 387 - 90 {Study of a drug combination for topical use, with contraceptive, antibacterial and antimycotic action and venereal disease preventive action . II . Optical microscopic and scanning microscopic studies of morphological changes of human spermatozoa in vitro after contact with the oxyquinoline sulfate and copper sulfate association}; Ivaldi M et al.; PIP: A new spermicidal contraceptive agent consisting of an association of oxyquinoline sulfate and copper sulfate was tested in vitro to study its morphological effects on fresh sperm . Notable changes, such as a crumpling of the head, and variations in linear geometry of spermatozoa, were noted at the optic microscope . The scanning microscope discovered further erosions at the head and at the neck membranes level . It would be advisable to further study the association of these 2 drugs, to be eventually used as a strong topical spermicidal agent, and as a valid alternative to hormonal contraception . Can Anaesth Soc J, 1979 May, 26(3), 196 - 200 Autonomic block, cardiovascular depression and histamine release produced by polymyxin B in the cat; Lee C et al.; The present study quantifies the autonomic block, the cardiovascular depression and the histamine releasing effects of polymyxin B in nine anaesthetized cats . The dose requirements for 50 per cent depression of the mean arterial blood pressure, the bradycardiac response to vagal stimulation, and the contraction of the nictitating membrane elicited by pre-ganglionic and post-ganglionic stimulation of the cervical sympathetic trunk have a narrow range of scatter, being of the order of 6--12 mg.kg-1 of the polymycin B base . The neuromuscular blocking dose (ED50), previously determined and hereby confired, also falls in the same range . Bradycardia and possibly histamine release are also observable . The relatively unremarkable effect of polymyxin B on the heart rate can be attributed to the balance between the vagal, sympathetic and ganglionic blocks, as well as the possible histamine release . All effects are long-lasting . Thus lack of tissue specificity makes it implausible to explain the neuromuscular and the cardiovascular effects of polymyxin B solely by the cholinergic mechanism of action . Ganglionic block and histamine release do not completely explain hypotension induced by polymyxin B . We propose that all biological effects of polymyxin B derive from a common mechanism of action, which may be its antimembrane antibacterial action . We would like to alert anaesthetists to the possiblity that polymyxin B may cause severe multiple organ system depression, in addition to neuromuscular block. Tijdschr Diergeneeskd, 1979 Apr 15, 104(8), suppl 115 - 7 The therapy of otitis externa; Oldenkamp EP et al.; The clinical findings following the instillation of an aqueous solution containing natamycin, neomycin and hydrocortisone into the ears of dogs exhibiting the signs of otitis externa are described . Out of a total of 143 cases, 50 were also examined microbiologically both before and after treatment in order to evaluate the antibacterial and antifungal properties of the solution . The severity of the complaint appeared to be of little significance as far as the respons is concerned . A favourable response was noted clinically in 95% and microbiologically in 86% of the cases treated. J Antibiot (Tokyo), 1979 Apr, 32(4), 371 - 8 Chemical modification of fortimicins: preparation of 4-N-substituted fortimicin B; Sato M et al.; Among the new aminoglycoside antibiotic family for fortimicins, components A, C and D have higher activity compared to their 4-N-deacylated components B and KE . Synthesis and antibacterial activities of 4-N-acyl- and 4-N-alkyl-fortimicin B derivatives are described . 4-N-Acylfortimicin B's, which are relatively unstable in alkaline conditions, were converted to stable 4-N-alkyl derivatives with diborane . The activity is greatly affected by the 4-N-substituents, and the presence of hydrophilic group(s) is necessary to confer activity on the derivatives . 4-N-(2-Aminoethyl)-, 4-N-(4-amino-2-hydroxybutyl)- and 4-N-(2-hydroxy-4-methylaminobutyl)-fortimicin B are the most potent compounds among them. J Antibiot (Tokyo), 1979 Apr, 32(4), 330 - 9 Studies on auromomycin; Yamashita T et al.; A new antitumor antibiotic, named auromomycin, was isolated from the culture broth of Streptomyces macromomyceticus, a macromomycin-producing strain . The antibiotic was recovered from the culture filtrate by salting out with ammonium sulfate and further purified by successive application of ion-exchange chromatography on Amberlite IRA-93 (Cl form) and DEAE-Sephadex (OH form), Gel filtration on Sephadex G-50 and hydrophobic chromatography on Octyl-Sepharose CL-4B . The antibiotic is an acidic polypeptide with a molecular weitht of 12,500 and an isoelectric point of pH 5.4 and consists of 16 different amino acids . It has characteristic absorption maxima at 273 nm and 357 nm in the ultraviolet spectrum and two minima at 280 nm and 350 nm in the optical rotatory dispersion spectrum . Auromomycin exhibits antibacterial activity not only against Gram-positive bacteria, but also Gram-negative bacteria . Antitumor activities of auromomycin were revealed against EHRLICH ascites carcinoma, ascites sarcoma 180, L1210 leukemia and LEWIS lung carcinoma . Auromomycin was found to be converted into macromomycin by adsorption chromatography on Amberlite XAD. J Antibiot (Tokyo), 1979 Apr, 32(4), 287 - 94 Olivanic acids, a family of beta-lactam antibiotics with beta-lactamase inhibitory properties produced by Streptomyces species . I . Detection, properties and fermentation studies; Butterworth D et al.; The screening of soil actinomyces for beta-lactamase inhibitors is described . Using a plate test a number of strains of Streptomyces were found to produce beta-lactamase inhibitory activity designated olivanic acid complex . Factors affecting the production of this complex by Streptomyces olivaceus ATCC 21379 are reported . The complex showed antibacterial activity and also inhibited a number of different types of beta-lactamase in a progressive manner . Certain ampicillin-resistant bacteria are rendered sensitive to ampicillin in the presence of olivanic acid complex at a concentration which alone did not inhibit growth. J Clin Periodontol, 1979 Apr, 6(2), 83 - 92 Periodontal therapy by local delivery of tetracycline; Goodson JM et al.; The present investigation assessed the feasibility of treating periodontal disease by controlled delivery of antibacterial agents from within periodontal pockets . Tetracycline-filled hollow fibers placed in the gingival sulcus were shown to have a dramatic effect both on the periodontal microflora and clinical manifestations of disease . Furthermore, it was found that drug-filled cellulose acetate hollow fibers are biologically compatible with the environment and can be manipulated by dental personnel to provide drug therapy with less than 1/1000 the amount of tetracycline that would have been used for systemic therapy . Of theoretical importance is the observation that virtual elimination of spirochetes from the gingival sulcus is possible by a single placement of tetracycline-filled hollow fibers, and spirochetes, once eliminated from a site, do not rapidly recolonize despite the persistence of viable organisms elsewhere in the mouth. Zentralbl Bakteriol {Orig A}, 1979 Apr, 243(2-3), 372 - 80 {Microcalorimetric testing of the antibacterial activity of doxycycline, gentamicin and their combination (author's transl)}; Semenitz E; The antibacterial activity of doxycycline and gentamicin was tested by microcalorimetric methods and by finding out the MIC of these substances, the test organisms being Staph . aur . haem . (13.665) and E . coli (3.579) . The investigations were carried out with the above mentioned substances both alone and in combination . A synergistic effect was found with both methods applied, but microcalorimetry showed that the combination influences the cell metabolism in another way than the individual substances . Another remarkable finding is that doxycycline inhibits the microcalorimetric activity of our bacterial strains in doses 10 to 100 times lower than found with the standard MIC finding methods. Scand J Dent Res, 1979 Apr, 87(2), 115 - 22 Determination of fluoride and chlorhexidine from chlorhexidine/fluoride-containing dentifrices; Dolles OK et al.; The intention of the present experiment was to study the effects of a possible interaction between fluoride and chlorhexidine when both agents were incorporated in the same vehicle . The amount of fluoride extractable from dentrifrices containing 0.1% NaF and the fluoride ion activity were not reduced by the addition of 2% chlorhexidine digluconate . Less than 50% of the added chlorhexidine was available when the dentifrices were dissolved in deionized water . This was not affected by the presence of fluoride . The in vitro antibacterial activity of the chlorhexidine-containing dentifrices was not reduced by the addition of fluoride . Approximately 40% of the chlorhexidine was retained in the human oral cavity after brushing for 1 min with both the chlorhexidine- and the chlorhexidine/fluoride-containing dentifrice . Thus the binding of chlorhexidine to vehicle ingredients when dissolved in water is probably too weak to affect the retention in the mouth. S Afr Med J, 1979 Mar 31, 55(14), 544 - 7 A comparison of the antibacterial activity of sulphonamide-trimethoprim combinations; Fourie ED et al.; Sensitivity patterns of 326 clinical isolates toward sulphonamide/trimethoprim combinations were tested in vitro . The relative merits of the different combinations are discussed in their pharmacological and bacteriological contexts . It is concluded that organisms sensitive to cotrimoxazole as judged by in vitro sensitivity tests performed at 37 degrees C are also sensitive to sulphamoxole/trimethoprim. Minerva Med, 1979 Mar 24, 70(14), 973 - 6 {Antibacterial effects of 70 percent denatured ethyl alcohol on hospital bacteria strains}; Finzi G et al.; Data relating to a study of the activity of 70 percent methylated spirits on some bacterial strains isolated in a hospital environment are reported . It was found that the spirit had very little effect over times of 30'' or less, a good bactericidal power for time of 1', and an excellent bactericidal power for times of more than 1'. Am J Surg, 1979 Mar, 137(3), 381 - 3 Activity of antibiotics in contaminated wounds containing clay soil; Roberts AH et al.; Most traumatic wounds are contaminated to some degree by soil and run a high risk of infection . The presence of soil in wounds interferes with natural tissue defenses, which include phagocytosis and serum bactericidal capacity . The experimental studies reported herein clearly demonstrate that soil also limits the antibacterial effects of specific antibiotics . This inactivation appears to be the result of a chemical reaction between the charged antibiotics and the soil particles. Zh Mikrobiol Epidemiol Immunobiol, 1979 Mar, (3), 35 - 9 {Immunological reactions in the secretions of volunteers vaccinated against influenza by aerosol and intranasally}; Pershin BB et al.; Aerosol and intranasal methods of influenza vaccination were studied on volunteers . Aerosol vaccination induced intensive S-IgA-producing reaction and increase of the specific antibody titres in the saliva and nasal secretions . Intranasal vaccination led to increase of influenza antibodies in the washings from the nasopharynx . The presence of a wide spectrum of antiviral and antibacterial normal secretory antibodies was revealed in the fluids under study . Along with stimulation of specific secretory antibodies, the methods of influenza vaccination under study led to increase of the titre of antibodies nonspecific of the vaccine used. J Prosthet Dent, 1979 Mar, 41(3), 290 - 5 Bacteria and pulpal reactions under silicate cement restorations; Brannstrom M et al.; Silicate cement was inserted in deep unlined cavities in 70 human teeth; 35 cavities were cleaned with an antibacterial cleanser, and the other 35 cavities in the contralateral teeth were treated with water spray only . In all teeth, invasion of bacteria from the tooth surface was prevented with a surface seal . Histologic examinations after 4 weeks revealed bacterial growth on dentinal walls in 9 of the uncleaned and in 2 cleaned cavities . Only in these 11 teeth was an inflammatory reaction seen in the pulp . Under eight cavities without bacterial growth and with silicate cement placed directly on an exposed pulp, no serious injury and no inflammatory reactions were observed . It was concluded that silicate cement per se does not seriously irritate the pulp . Infection of cavity walls should be avoided, not only by removing grinding debris and antibacterial cleansing, but also by use of a liner to prevent invasion of bacteria from the surface of the tooth. Antibiotiki, 1979 Mar, 24(3), 182 - 5 {Participation of the antibiotics of Bac . pumilus and Bac . subtilis in the regulation of bacterial spore formation}; Lukin AA et al.; Sporulation and antibiotic production, as well as the effect of exogenic antibacterial substances on bacterial sporogenesis were studied in various strains of Bac . pumilus and Bac . pumilus and Bac . subtilis . The bacteria were grown on a solid sporulation medium with and without the antibiotics . After 5-day incubation the presence of refractyl spores was determined with a phase-contrast method . It was found that in the strains of Bac . pumilus producing antibacterial substances the sporulation was normal . The loss of the capacity for synthesizing such substances resulted in asporegenicity or oligosporogenicity . This allowed a conclusion on existence of phenomenological connection between sporulation and antibiotic production . The study of the antibiotic effect on bacterial sporogenesis showed negative results which are discussed in the paper along two directions: (1) the antibiotics did not probably participate in regulation of the bacteria cell differentiation, (2) the antibiotics regulated the bacterial sporogenesis though their effect was not as yet detected because of methodical difficulties . Therefore, the problem of the antibiotic participation in regulation of sporulation in Bac . pumilus and Bac . subtilis remains open. Biull Eksp Biol Med, 1979 Mar, 87(3), 256 - 9 {Intensification of antibacterial and antiviral nonsusceptibility and of the immune response with an officinal RNA preparation}; Zemskov VM et al.; Sodium nucleinate increased essentially the insusceptibility of mice to pathogenic escherichia, strain O26, Pr . vulgaris, Ps . aeruginosa, Ser . marcescens, and produced a total stimulating effect on the nonspecific bacterial resistance; analogous stimulating activity was found in the homologous low polymeric RNA from the liver . Sodium nucleinate intensified the insusceptibility of the animals to the tick-born encephalitis and encephalomyelitis viruses, and increased the antibody-forming cells count . The side-effect of heat-inactivated vaccine from pathogenic escherichia was reduced in animals inoculated with sodium nucleinate preliminarily. Zh Mikrobiol Epidemiol Immunobiol, 1979 Mar, (3), 99 - 102 {Antilymphocytic immunoglobulin with an associated antibacterial orientation . I . The production and experimental laboratory study of the preparation}; Shabalin VN et al.; Immunoglobulin was obtained from rabbit sera following immunization of the animals with a complex antigen composed of a suspension of human thymocytes and killed microbe polyvaccine . The preparation possessed not only antilymphocytic activity in vitro, but also protected the animals after their artificial infection. Vestn Khir Im I I Grek, 1979 Feb, 122(2), 18 - 20 {Perforation of gastroduodenal ulcers and pulmonary tuberculosis}; Likhovid NP et al.; 17 observations of the perforation of gastroduodenal ulcer in pulmonary tuberculosis cases are analysed . Most of the patients were males, aged over 50, with protracted chronic forms of tuberculosis . In all cases the suturing of perforation was carried out . 9 patients died . The conclusion has been drawn that a massive antibacterial therapy, which should be carried out in specialized medical institutions, is imperiable. Ciba Found Symp, 1979 Jan 16-18, (70), 201 - 19 Gastrointestinal host defence: importance of gut closure in control of macromolecular transport; Walker WA; An important adaptation of the gastrointestinal tract to the extrauterine environment is its development of a mucosal barrier against the penetration of harmful substances (bacteria, toxins and antigens) present within the intestinal lumen . At birth, the newborn infant must be prepared to deal with bacterial colonization of the gut, with formation of toxic byproducts of bacteria and viruses (enterotoxins and endotoxins) and with the ingestion of antigens (milk proteins) . These potentially noxious substances if allowed to penetrate the mucosal epithelial barrier under pathological conditions can cause inflammatory and allergic reactions which may result in gastrointestinal and systemic disease states . To combat the potential danger of invasion across the mucosal barrier the infant must develop an elaborate system of defence mechanisms within the lumen and on the luminal mucosal surface which act to control and maintain the epithelium as an impermeable barrier to uptake of macromolecular antigens . These defences include a unique immunological system adapted to function in the complicated milieu of the intestine as well as other non-immunological processes such as a gastric barrier, intestinal surface secretions, peristaltic movement and natural antibacterial substances (lysozyme, bile salts) which also help to provide maximum protection for the intestinal surface . Unfortunately, during the immediate postpartum period, particularly for premature and small-for-dates infants, this elaborate local defence system is incompletely developed . As a result of the delay in the maturation of the mucosal barrier newborn infants are particularly vulnerable to pathological penetration by harmful intraluminal substances . The consequences of altered defence are susceptibility to infection and the potential for hypersensitivity reactions and for formation of immune complexes . With these reactions comes the potential for developing life-threatening diseases such as necrotizing enterocolitis, sepsis and hepatitis . Fortunately, 'nature' has provided a means for passively protecting the 'vulnerable' newborn against dangers of a deficient intestinal defence system, namely human milk . It is now increasingly apparent that human milk contains not only antibodies and viable leucocytes but many other substances which can interfere with bacterial colonization and prevent antigen penetration. Arzneimittelforschung, 1979, 29(9), 1334 - 9 Investigation of the common mechanism of action of antibacterial compounds containing gamma-pyridone-beta-carboxylic acid structure by principal component; Darvas F et al.; On the basis of 576 in vitro antibacterial positive results of 99 compounds containing gamma-pyridone-beta-carboxylic acid structure conclusions have been drawn on the mechanism of action of the derivatives by principal component analysis . It has been found that the compounds exert their effect essentially by influencing two types of physiological processes or series of processes . The more important of the two "mechanisms", responsible for 50-95% of the activity of the compounds, is common for the compounds investigated, and is associated with the gamma-pyridone-beta-carboxylic acid structure. Arzneimittelforschung, 1979, 29(8), 1081 - 3 Synthesis of difuran derivatives and their biological activity; Hishmat OH et al.; Visnaginone and khellinone react with chloroacetamide and chloroacetonitrile in dimethyl formamide to give either the cyclised benzo{1,2-b : 5,4-b'}difuran or the open form depending on the heating period . The antibacterial activity of the compounds was tested. J Int Med Res, 1979, 7(5), 443 - 8 Crotamiton cream and lotion in the treatment of infants and young children with scabies; Konstantinov D et al.; Fifty hospitalized infants and small children in the age-group of 3 months to 2 years admitted with scabies were treated with 5 applications of either 10% crotamiton cream or lotion on consecutive days . In this trial, the second to be performed exclusively in infants and young children, an improvement in itching was observed in all patients within 3 days of starting the treatment and the examination on Day 7 showed absence of skin lesions in all patients . Crotamiton cream as well as lotion rendered a 100% cure rate . All patients, including those having secondary pyoderma and/or eczematization tolerated the treatment with crotamiton cream and lotion well and no adverse reactions, either due to the topical application or to the transcutaneous systemic absorption of crotamiton, were reported . Post-treatment laboratory investigations did not reveal any unwanted effect due to transcutaneous systemic absorption of crotamiton on the blood, kidneys or liver . Crotamiton is the only scabicide available today which displays not only antiprurtic but also marked antibacterial properties . It is especially indicated in the treatment of scabies in children as they are very prone to secondary bacterial infection following scratching . In view of its good efficacy and excellent tolerability the 5-application treatment schedule, with crotamiton cream applied to the whole body from the chin downward, can therefore be recommended as an optimum form of treatment for scabies in infants and young children. Z Erkr Atmungsorgane, 1979, 152(2), 153 - 65 {Antibacterial activity, place of action and mechanism of resistance of pulmonal effecting antibiotics (author's transl)}; Ellorhaoui M; Antibiotics are of high importance in iatrogenic pathology . The emergence of resistent strains is a sanitary problem of remarkable consequences particularly under hospital conditions . Modern pulmology is not imaginable without antibiotic and chemotherapeutic drugs . A rational and economic therapy is possible only if the mechanisms and sites of antibacterial action and of drug resistance in bacteria are known. Scand J Plast Reconstr Surg, 1979, 13(1), 89 - 94 Metal sulfonamides as antibacterial agents in topical therapy; Fox CL Jr et al.; The apparent efficacy of zinc and cerium sulfadiazine and the metabolic role of other trace metals suggested that sulfonamide salts of these might be of therapeutic value . There is also a possibility that metal salts of other sulfonamides might be useful . Accordingly other sulfonamide salts of zinc were prepared and studied in vitro and in vivo . Only zinc sulfathiazole and zinc methoxazole were as effective as zinc sulfadiazine in animal studies . The sulfadiazines of aluminum, chromium, cobalt, copper and iron were prepared and compared in vitro and in vivo . Only cobalt sulfadiazine appeared comparable to zinc and cerium sulfadiazine in healing burn wounds in rats . Studies on the molecular structure of silver sulfonamides disclosed the polymeric structure peculiar to silver sulfadiazine which appears to account for its unique properties . It is not yet known whether other metal sulfadiazines have this attribute. Pharmazie, 1979 Jan, 34(1), 20 - 2 {Azoles . Part 5: On halogen-nitroindazole derivatives and their antibacterial properties (author's transl)}; Wrzeciono U et al.; The authors describe a modified procedure for the synthesis of the 3-halogenindazole derivatives 1--7 and of the 1-hydroxymethylindazole derivatives 8--14 . The compounds 8--13 yield the corresponding 1-chloromethyl derivatives 15--20, and 23 is obtained from 3 . The compounds 7--23 exert slight antibacterial effects. Ann Otol Rhinol Laryngol, 1979 Jan-Feb, 88(1 Pt 1), 16 - 20 Pathogenesis of sinus empyema; Carenfelt C; The crucial event in the pathogenesis of sinus empyema is the ostial obstruction . On the basis of recent reports, some consequences of the obstruction on the local bacterial-host interrelationship have been outlined . The anaerobic gas environment of the empyema is one quality important to the selection of bacteria but probably also to the efficiency of the antibacterial activity of the granulocytes . Release of proteolytic enzymes from neutrophilic granulocytes in the sealed sinus may jeopardize the bacterial engulfment due to proteolytic degradation of opsonins . A longstanding exposure of the sinus mucosa to uninhibited proteolytic enzymes may explain the irreversible lesion of the mucosa in chronic sinusitis. Drugs, 1979 Jan, 17(1), 56 - 65 Treatment of bacterial infections in pregnancy; Weinstein AJ; Treatment of bacterial infections in pregnancy requires an understanding of the unique problems related to the administration of antibacterial agents to pregnant women . The clinician must be aware not only of the antibiotic-associated untoward effects which may develop in the mother, but also of the possibility that adverse reactions may occur in the fetus . Precise knowledge of the microbial aetiology of those infections which occur during pregnancy and an understanding of the intricacies of antibiotic administration to pregnant women will assure the greatest likelihood that bacterial infections in pregnancy will be effectively, and safely, treated. Acta Obstet Gynecol Scand, 1979, 58(1), 49 - 51 The peroxidase content and the antibacterial activity of the amniotic fluid; Feingold M et al.; A possible relationship between the antibacterial activity of amniotic fluid and its peroxidase content was examined . Antibacterial activity, assessed by counting colonies of S . aureus following 24 hour incubation, was present in 76% of the samples studied . It was not related to gestational age . Peroxidase activity, assessed by the O-dianisidine method, was not found in any of the amniotic fluid samples examined. Mikrobiyol Bul, 1979 Jan, 13(1), 9 - 12 {Antibacterial effects of arsenic on pulp necrosis using the plate diffusion method}; Guven O et al.; The microorganisms which arrive in various ways to dental pulp causes the infections of pulp . The pulp is necrotised in cases it is not possible to keep it alive . In this study arsenic which is known an available material for devitalisation of pulp and its antibacterial effects on microorganisms which are the causes of the infections of pulp have been investigated. Acta Microbiol Acad Sci Hung, 1979, 26(3), 233 - 9 Antitoxic immunity against the so-called lung toxin produced by Escherichia coli; Emody L et al.; Cross neutralization test with antisera to crude haemolysins produced by some Escherichia coli strains indicated that there were no antigenic differences among the haemolysins tested . These crude preparates showed definite cytotoxicity which could also be cross neutralized by "antihaemolysin" sera . Neutralization experiments were performed in mouse lung test with homologous and heterologous anti-haemolysin sera, and with O and OK sera to the wild type strain and its toxic R mutant . The results showed that the immunity in the mouse lung model is antitoxic and antibacterial. Czech Med, 1979, 2(1-2), 29 - 40 The bactericidal activity of sera of healthy neonates and newborns with hyperbilirubinaemia to E . coli; Miler I et al.; Cord and newborn sera were found to possess a significantly decreased in vitro bactericidal activity to E . coli as compared to sera of adults . Hyperbilirubinaemia in neonataes suffering from both Rh and ABO incompatibility results in a further significant impairment of bactericidal activity of their sera in comparison to healthy newborn infants . Exchange transfusion considerably improved this serum antibacterial activity . The possible mechanism of toxic action of unconjugated bilirubin on the cells of the immune system is discussed. Eur J Pediatr, 1979, 132(4), 239 - 52 Treatment of infantile E . coli gastroenteritis with specific bovine anti-E . coli milk immunoglobulins; Mietens C et al.; A milk immunoglobulin concentrate (MIC) containing antibodies to enteropathogenic E . coli strains was prepared by hyperimmunisation of pregnant cows and using the milk obtained during the first 6 to 8 days of lactation . The sterile concentrate contained 70 to 80% protein and 35 to 40% immunoglobulin . The antibacterial activity was measured by bacterial passive agglutination, bacteriostatic activity in vitro, phagocytic clearance in vivo, and a protection test in mice . Though differences in titers were observed, adequate immunologic activity was demonstrated by these tests . Clinical studies were performed with 60 patients (aged 10 days to 18 months) suffering from diarrhoea with isolation of enteropathogenic E . coli . They were treated for 10 days with MIC and stool cultures were done prior to, during, and 2, 3 and 4 days after termination of treatment . Among 51 patients infected with E . coli strains incorporated in the vaccine, stool cultures became negative in 43 (84.3%) after treatment with MIC and 8 remained positive . Nine patients infected with strains O 78:K80(B-) and O 114:K--(B-)--which were not included in the vaccine used for immunisation--served as controls . Only one patient in this group became negative . If all patients receiving antibiotics for non intestinal infections during the treatment period are omitted the results remained unaltered: MIC was effective in 32 out of 38 patients (84.2%) . These differences were highly significant . These results provide evidence that treatment with specific MIC is effective in eliminating enteropathogenic E . coli from the intestine. Infection, 1979, 7 Suppl 5, S434 - 7 Influence of aminopenicillins on bacterial growth kinetics in vitro in comparison with the antibacterial effect in vivo; Mattie H et al.; To quantify the relative antibacterial efficacy of beta-lactam antibiotics in vitro, a mathematical description of bacterial growth was developed . Curves of growth in the presence of the antibiotic are expressed as quadratic functions of time, with initial growth rate (ko) and rate of change of growth (a) as concentration dependant variables . For these variables the concentration-effect slopes were not parallel; therefore the potency ratio varied between 1 (at about 2 mg/l) and 2 (at higher concentrations) . The relative efficacy in vivo was expressed as a potency ratio with regard to the number of bacteria in an infected thigh muscle in mice . The potency ratio was 1.5, which is between the limits of the in vitro results. Infection, 1979, 7 Suppl 5, S425 - 33 The aminopenicillins: development and comparative properties; Reeves DS et al.; In this review we have compared and contrasted the antibacterial and pharmacological properties of the aminopenicillins currently available . It is apparent that there is little hard evidence (except in the case of thphoid fever) that either amoxycillin or the pro-drug esters of ampicillin are significantly more effective than ampicillin itself, despite their better absorption and higher serum levels . However, amoxycillin and the ampicillin pro-drug esters do cause fewer bowel side-effects than ampicillin, which may justify their use despite the extra cost involved . The problem of susceptibility to penicillinases is unlikely to be solved by modification of the aminopenicillin molecule . A more likely solution is administration of these substances with beta-lactamase inhibitors such as clavulanic acid . Trials with such combinations are already under way. G Batteriol Virol Immunol, 1979 Jan-Jun, 71(1-6), 3 - 15 {Effect of the carbon/nitrogen ratio on the antibiotic activity of prodigiosin}; Alonzo V et al.; The antibacterical activity of prodigiosin varies according to the C/N ratio in the cultural media for S . marcescens . In organic media, as nutrient agar, peptone or soytone, the optimal ratio lies between 4 and 5, and higher values are required for "mineral media" where the nitrogen source is essentially an ammonium salt . The separate C source would be probably used as "acetate source" for the synthesis of the terminal alkylpyrrole. Dermatologica, 1979, 159(1), 113 - 9 {Levuroses appearing in cases of severe burns}; Male O et al.; The preconditions for the development of systemic mycoses, mainly levuroses, caused by opportunistic organisms are particularly favorable in the severely burned patients: on the one hand as a consequence of suppression of immunity, on the other hand by the overgrowth of these fungi in the digestive tract as a side-effect of the antibacterial chemotherapy which is necessary for the treatment of the original disease . Since such mycoses are usually very severe, mostly life endangering, their prophylaxis and early diagnosis are highly important . The aspects and measurements, most important in this connection, are discussed on the basis of our experience. Rev Cubana Med Trop, 1979 Jan-Apr, 31(1), 5 - 12 {Biological evaluation of Cuban plants . I}; Jimenez Misas CA et al.; Aqueous, alcoholic and ketonic extracts from five species of superior plants of the families Papilonaceae, Euforbiaceae, Moraceae, Piperaceae and Solanaceae were assessed from an antibacterial viewpoint using the gel double-layer diffusion method with cylindric sections . Values of inhibition areas are depicted in diameter millimeters . The best results were obtained from Desmodium barbatum extracts. Rev Cubana Med Trop, 1979 Jan-Apr, 31(1), 45 - 51 {Biological evaluation of Cuban plants VI}; Jimenez Misas CA et al.; The study of the antibacterial activity of plants growing in Cuba is pursued . Aqueous, alcoholic and ketonic extracts were prepared from five species, and it was found that the best inhibitions corresponded to the species Hamelia patens, Nephrolepis acuminata, Calocarpum sapota and Colocasia antiquorum. Rev Cubana Med Trop, 1979 Jan-Apr, 31(1), 29 - 35 {Biological evaluation of Cuban plants . IV.}; Jimenez Misas CA et al.; Aqueous, alcoholic and ketonic extracts from leaves and stems of plants of the families Malvaceae, Anonaceae, Punicaceae, Verbenaceae and Urticaceae were analyzed in order to prove their antibacterial proprieties . The best results were obtained from Punica granatum extracts which inhibited over a 50% of bacteria. Scand J Plast Reconstr Surg, 1979, 13(1), 131 - 5 Prospective randomized treatments for burned hands: nonoperative vs . operative . Preliminary report; Edstrom LE et al.; It has been suggested that deep partial-thickness burns of the hand which remain unhealed by 14 days should be excised and totally resurfaced . Controlled data supporting this suggestion is not available . Therefore, a prospective randomized study was performed on 222 burns of the hand to evaluate if excision and skin grafting had any advantage over conservative management . Full-thickness burns were eliminated from the series by excision and grafting them as soon as possible after the diagnosis had been made . To eliminate the very superficial burns, randomization did not take place until the wound had remained unhealed for ten days and would not heal for at least another week . In the two groups, the first ten days were managed similarly with topical antibacterials, escharotomies when necessary, and splinting in the "safe" position . Conservatively managed hands were treated with scarlet red gauze dressing as soon as all eschar had been removed . Those cases randomized into the excision and grafting group were operated upon approximately day 14 . Physical therapy was the same in both groups except for the immediate period after grafting . Results were recorded by active and passive joint measurements and photographs on predetermined days throughout the study . In this study, spontaneous healing, taking as much as five weeks, gave acceptable results, comparable to excision and grafting performed at two weeks . The use of range of motion exercises, accurate splinting and pressure allowed optimal healing and prevented stiffness and contractures in both groups . There was no significant difference between the two treatment modalities. Stomatol DDR, 1979 Jan, 29(1), 45 - 8 {New aspects of therapy for alveolitis with Grisaldon}; Frohlich M; In the GDR, Grisaldon has been used in alveolitis therapy since 1974 . The results from the bacteriological testing of this preparation and the diluting and rinsing effects of saliva and blood on it arouse doubts about its antibacterial efficiency . Thrombelastographic studies demonstrated the clotting-accelerating and the marked fibrin-stabilizing effect of pure acetylsalicylic acid . In contrast to other publications, it was stated that the p-hydroxybenzoic acid propyl ester is absolutely indifferent . Histological studies on animals have shown that Grisaldon is detectable in the alveolus as a foreign body even 28 days after application, and that it decelerates wound healing. Infection, 1979, 7(1), 30 - 4 Antibacterial efficacy of cefazolin and cephradine in neutropenic mice; Kunst MW et al.; The activity of cefazolin (CEZ) and cephradine (CED) was studied in experimentally infected neutropenic mice . Neutropenia was induced by 600 rad whole-body irradiation; an infection was induced by the injection of 5 X 10(6) Escherichia coli into the thigh on Day 5 after irradiation . Antibiotics were administered 1 h later, and antibacterial activity was estimated from bacteria counts made in the homogenized individual thighs 3 h after infection . The effect of a low dose of each of the cephalosporins on the infection was significantly lower in the absence of granulocytes than in animals with intact host defence; at higher dosages the effect of both antibiotics on the infection was the same in neutropenic and unirradiated mice . In the neutropenic mice, CEZ was 2.95 times more active than CED against E . coli in vivo, this difference in activity being similar to that found earlier in normal mice. Acta Odontol Scand, 1979, 37(6), 371 - 5 Evaluation of extrinsic tooth discoloration; Eriksen HM et al.; Extrinsic brown tooth discolorations are frequently detected in connection with antibacterial agents used for chemical plaque control . The present investigation confirmed the staining ability of an antibacterial quarternary ammonium salt, benzethoniumchloride, used as a 2% additive to a dentifrice . A weak chelator did not alter the discoloration tendency . Extrinsic discoloration was evaluated both by direct inspection, from color photographs and by using a microphotometric technique . The discoloration tendency was well demonstrated by all three techniques . Evaluation from the color photographs, however, may be preferable in epidemiological surveys while the microphotometric technique may possess certain advantages in detailed experimental discoloration studies. Ciba Found Symp, 1979, (77), 39 - 53 The genesis of amniotic fluid infections; Ross SM et al.; Amniotic fluid infections manifested by an inflammatory response in the extraplacental membranes and subchorionic plate of the placenta are a common phenomenon thought to be due in most cases to ascending bacterial infections via intact membranes . Fatal spread to the fetus is much less common and more likely to occur in underprivileged communities . The probable reasons are nutritional deprivation in the mother or both, leading to production of a liquor with diminished ability to suppress bacterial growth . Zinc is one component of the antibacterial system but liquor levels of zinc vary widely and inconsistently with antibacterial activity . Dietary supplementation with zinc did not improve antibacterial activity of liquors in a population with diminished liquor antibacterial activity and large number of fatal infections . Other factors in the genesis of amniotic fluid infections may be interference with normal defence mechanisms as a result of coitus in late pregnancy and vaginal infections with Trichomonas vaginalis . Socioeconomic factors may play a role apart from their association with maternal nutrition, through diminished hygiene associated with insufficient use of water and insufficient availability and use of medical facilities. Ciba Found Symp, 1979, (77), 17 - 38 Pathology of the placenta and cord in ascending and in haematogenous infection; Blanc WA; The two main patterns of inflammatory response in the placenta and its adnexae are: (1) amniotic infection, usually bacterial ascending, with acute chorioamnionitis and funisitis; (2) haematogenous villitis, usually viral, with early necrotizing lesions and vasculitis and, later, chronic infiltrates and obliterative vasculitis . In amniotic infection most cells in the exudate are maternal . These leucocytes participate in antibacterial defence of the amniotic cavity in conjunction with substances such as zinc polypeptide and lysozyme and may contribute directly to fetal defence . Immunoglobulins may be produced in the cord of placenta only in protracted lesions such as 'healed' funisitis . Individual variations in the resistance of the membranes to bacterial penetration are possible . In viral infections a massive multifocal production by plasmacytes of immunoglobulins M, G and A is seen in affected villi . The secretion of non-specific antiviral substances in the infected placenta is possible . In all affected villi there is an activation of fixed macrophages (Hofbauer cells) that remain partly 'immature', i.e . are lysozyme-negative . Multifocal lymphoplasmacytic villitis is uncommon and has helped to focus the diagnosis on prenatal infection . In contrast, non-specific lymphocytic villitis is common; since there is no morphological difference between cases known to be associated with an infection, e.g . varicella, and the others, many cases may well be due to silent infection, although a graft-versus-host reactions remains a distinct possibility. Scand J Plast Reconstr Surg, 1979, 13(1), 111 - 4 Considerations on early surgery in the treatment of extensive burns; Teich-Alasia S et al.; The results obtained with early surgical treatment of burns have been re-examined from various aspects . Early escharectomy, which tranforms the necrobiotic tissue into a surgical lesion, reduces the chemical factors of inflammation, lowers the lactic acid level and depresses the activity and disordered proliferation of the fibroblasts and the consequent laying down of immature collagen which is responsible for the pathological evolution of the burn scar . The removal of toxic material with proteasic activity, the reduction in the risk of sepsis, the saving of work for the immunopoietic mechanism, a reduction in the weight loss through improved nitrogen balance and an increase in the anabolic phase of muscular metabolism by early movement as well as a shortening of the period of hospitalization--all are factors in favour of the early surgical technique . Better healing is obtained by the elimination of the necrotic tissue, a reduction in the haematologic tissue inflammation mediators, an increase in the antibacterial defence following the reconstruction of the skin surface with covering materials and the rapid articular reduction; not to mention the inhibition of the formation of granulation tissue. G Batteriol Virol Immunol, 1979 Jan-Jun, 72(1-6), 134 - 42 {In vitro antibacterial activity of a halogenated derivative of D-alanine}; Viano I et al.; The "in vitro" effect of beta-chloro-D-alanine, a drug that inhibits cell-wall synthesis, was studied . We used some strains of microorganisms, mainly Gram-negative and resistant to antibiotics with the same mechanism of action . MIC and MBC values obtained show a poor efficacy of this drug . Therefore we studied the association of beta-chloro-D-alanine with ampicillin and fosfomycin . The evaluation of the results, determined by means of a graphic and a mathematical method, shows a good synergistic effect with both associations . Synergism is more marked with ampicillin. Arzneimittelforschung, 1979, 29(12a), 1916 - 20 {Antibacterial activity of mezlocillin and azlocillin/A survey (author's transl)}; Knothe H; A review of the antibacterial activity of 6-{(R)-2-{3-methylsulfonyl-2-oxo-imidazolidine-carboxamido}-2-phenyl-acetamido}-penicillanic acid sodium salt (mezlocillin, Baypen) and 6-{(R)-2-(2-oxo-imidazolidine-1-carboxamido)-2-phenyl-acetamido}-penicillanic acid sodium salt (azlocillin, Securopen) is given on the basis of extensive in vitro studies . The action of each of the preparations is compared with that of important antibiotics of other substance classes from the group of penicillins and cephalosporins. Chemotherapy, 1979, 25(6), 336 - 45 Antibiotic compatibility and stability in a parenteral nutrition solution; Reed MD et al.; Eight antibiotics, alone and in selected combinations, were evaluated for stability and compatibility in a protein hydrolysate parenteral nutrition solution . Samples were stored under varying conditions and evaluated at 12-hour intervals over a period of 24--48 h . Compatibility and stability were assessed by quantitative bacteriologic assay, pH determinations and visual inspection . In most cases, antibiotics were compatible and stable over the entire study period . Carbenicillin, methicillin in combination with gentamicin, and tobramycin in combination with cephalothin or methicillin, exhibited a gradual loss of antibacterial activity after 24 h . These results indicate that the antibiotics studied may be administered in protein hydrolysate parenteral nutrition solutions . This mode of therapy offers a means of combating infection, while maintaining a nutritional source for host defences, tissue repair, and growth. Eur J Drug Metab Pharmacokinet, 1979, 4(1), 43 - 8 Serum kinetics of doxycycline polyphosphate in dogs; Michel G et al.; Serum kinetics of Doxycycline polyphosphate (DPP) have been studied in dogs after oral administration of 10 mg.kg-1 by measurement of total serum concentration (Ct) of tetracycline derivatives by a chemical assay and active concentration (Ca) by a microbiological method . Kinetics have been studied using a one compartment open model with absorption by oral route . DPP is rapidly absorbed, the peak serum level is reached three hours after absorption and slowly eliminated (elimination half-life = 12 hours) . The main differences observed between Ct and Ca kinetics are in the values of the areas under the curves (AUC) and the peak serum level . The values obtained for these parameters for Ca kinetics were found to be 50% of those obtained for Ct, the volumes of distribution being in inverse proportion . These results are in a good agreement with the correlation and linear regression observed between Ca and Ct showing that 55% of total serum Doxycycline possesses immediate antibacterial activity . It is postulated that this difference between Ct and Ca kinetics is essentially a reflection of the ratios of bound and free drug . Similar results were obtained with the finished pharmaceutical form except for a 15% increase of AUC indicating improvement of the bioavailability of the drug. Microbios, 1979, 24(97-98), 173 - 84 Relationship between the antibacterial activity towards Escherichia coli NCTC 5933 and the physico-chemical properties of some esters of 3,4,5-trihydroxybenzoic acid (Gallic acid); Boyd I et al.; Aqueous solubilities, oleyl alcohol: water and octanol: water partition coefficients, RM values, reduction in surface tension of water, relative antioxidant activities and pKa values, were determined for gallic acid and a series of its alkyl esters . Correlations were sought between these physico-chemical measurements and MIC, MBC and killing-rate determinations against Escherichia coli . Variations in antibacterial activity generally correlated well with partition parameters, but these correlations did not accurately predict the cut-off point in antibacterial activity. Farmaco {Sci}, 1978 Dec, 33(12), 945 - 53 Conformational properties and in vitro antibacterial activity of some diarylsulphones; Pappalardo GC et al.; The 2-pyridylphenylsulphone, di-2-pyridylsulphone and its p-nitro and p,p'-dinitro derivatives were synthesized and tested for antibacterial activity against a number of gram-positive and gram-negative bacteria . The electric dipole moment of these compounds were also measured (in benzene, 25 degrees) and analyzed in terms of molecular conformation in solution . The derivative compounds bearing a 5-nitro-2-pyridine fragment were found to be the most active in the series examined . Among these the nitro-2-pyridylphenylsulphone was found to have a broad-spectrum effect on gram-positive and gram-negative bacteria . Results of the conformational study in combination with microbiological data allowed discussion on the possible inferences concerning the stereochemical aspects of the interaction of diarylsulphones with bacterial receptor sites. J Infect Dis, 1978 Dec, 138(6), 829 - 36 Bacteremic superinfections of patients with bacteremia: occurrence, bacteriology, mortality, and duration of hospitalization at Boston City Hospital during 12 selected years between 1935 and 1972; Finland M et al.; During the course of hospitalization of 6,414 patients with bacteremic infections identified at Boston City Hospital (Boston, Massachusetts) during 12 selected years between 1935 and 1972, 6.0% developed verified bacteremic superinfections with organisms not isolated or identified in the primary bacteremic infection . Analysis of these cases reemphasizes the increasing occurrence of serious hospital-acquired infections despite the successive introduction and intensive use of a large number of effective antibacterial agents . The bacteremic superinfections, like the primary hospital-acquired bacteremias, increased in incidence over the years, particularly since 1961; they were more frequent and were associated with a higher mortality rate and longer duration of hospital stay in the primary hospital-acquired cases than in the patients in whom bacteremia was considered to be community-acquired . The organisms in superinfections were similar to those in primary hospital-acquired bacteremias . Superinfection was more frequent among the patients who died than among the survivors. J Med Chem, 1978 Dec, 21(12), 1325 - 7 Electronic aspects of the antibacterial action of sulfanilamides; De Benedetti PG et al.; Intramolecular interactions in N1-substituted sulfanilamides (SA) can rationalize the trend of their antibacterial powers with the use of a resonance scheme, derived from d orbital symmetry and tested with an extensive spectroscopic investigation on amidic, imidic, and anionic SA . On quantitative grounds, a good relationship is presented between the antibacterial power and the proton chemical shift of the p-amino group . The electronic features for high activity are described. Helv Chir Acta, 1978 Dec, 45(4-5), 505 - 10 {Antibiotic prophylaxis in plastic reconstructive surgery}; Clodius L; In plastic reconstructive surgery the use of prophylactic antibiotics is considered for wounds in which tissue trauma can not exactly be delineated as in gun shot wounds, bites, contusions; for extensive surgery lasting more than three hours in the oral area, with opening of the maxillary sinuses; when large foreign bodies are implanted; if there is massive intraoperative contamination and for patients with reduced antibacterial defence mechanisms . A principal factor leading to infection is reduced tissue oxygenation, which can be reversed by the use of benzopyrones as experimentally demonstrated. J Infect Dis, 1978 Dec, 138(6), 837 - 48 Duration of hospitalization for bacteremic infections at Boston City Hospital during 12 selected years between 1935 and 1972; Finland M et al.; In survivors of both community-acquired (CA) and hospital-acquired (HA) bacteremic infections at Boston City Hospital during 12 selected years between 1935 and 1972, the mean hospital stay fluctuated widely from one selected year to the next, but it was generally shorter and early discharges were more frequent in the years when effective antibacterial agents were used . The greatest reduction in hospital stay occurred by 1941 . The size of the fluctuations and reductions also varied with the causative organism . The average duration of hospitalization of all survivors of HA bacteremic infections after the first positive blood culture was 10.5 days longer than the total hospitalization of survivors of CA infections . The reduced length of hospital stay after 1935 is attributed to the successful use of effective antibacterial drugs, and the greater effect in CA than in HA cases is attributed to more frequent infections in the latter with organisms resistant to those drugs. Appl Environ Microbiol, 1978 Dec, 36(6), 794 - 7 Improvement in the sensitivity of DNA polymerase I-deficient Escherichia coli for detecting mutagens and carcinogens; Venturini S et al.; The sensitivity of a polA strain to the antibacterial activity of mutagens and carcinogens may be increased by inserting one or both of the following characteristics, a lexA mutation or the R391 bacterial plasmid . The effects of the lexA mutation and the plasmid appear to be additive . The differential sensitivity of a polA lexA (R391) strain could be adapted as a preliminary screening test for mutagens and potential carcinogens. Immun Infekt, 1978 Dec, 6(6), 226 - 8 {Inoculum effects and bacterial resistance (author's transl)}; Greenwood D; Massive bacterial populations are frequently involved in infection . Such dense cultures may appear 'resistant' to therapeutically achievable concentrations of some antibacterial agents in vitro, but the implications of this for treatment are not always clear . A better understanding of the mechanisms responsible for inoculum effects may help in assessing their clinical significance and some possible approaches to this goal are described. Antibiotiki, 1978 Dec, 23(12), 1102 - 8 {Leukolysis reaction in the diagnosis of allergy to antibacterial preparations in pulmonology}; Gurin NG et al.; The experiment included 109 patients with non-specific pathological processes in the lungs . i.e . 21 cases with acute and 55 cases with chronic pneumonia and 33 cases with bronchial asthma with or without chronic pneumonia . Clinically intolerance of the antibacterial drugs was observed in 39 patients and increased leucolysis (above 15 per cent) was observed sometimes more frequently . Only with the use of penicillin the difference was 1.6 times . Out of 39 patients with clinical signs of allergy to antibiotics or sulphanilamide only 20 showed the signs of increased leucolysis on the use of the respective drug . No correlation between the percentage of the leucolysis cases due to antibiotics or sulphanilamides and the clinical signs of their intolerance was observed . The use of such drugs by a person or even only his presence in the hospital often induced increased leucolysis which may be considered as an indication of the person sensibilization to them. Klin Monatsbl Augenheilkd, 1978 Dec, 173(6), 842 - 5 {Concentration of minocycline in human aqueous humor after oral administration (author's transl)}; Hartwig H et al.; For antibacterial prophylaxis in intraocular surgery minocycline was administered in oral dosage in 22 cataract-patients . The concentration levels reached in the aqueous humor were determined . The detected levels ranged in some cases from 0.08 to 0.2 mcg/ml, the majority was below 0.06 mcg/ml. Cutis, 1978 Dec, 22(6), 696 - 703 Special topical approach to the treatment of acne . Suppression of sweating with aluminum chloride in an anhydrous formulation; Hurley HJ et al.; A new topical approach to acne treatment--the use of aluminum chloride hexahydrate in anhydrous ethanol (ACAE)--was studied in 141 patients . Using sequential treatment schedules, paired comparison techniques, and various concentrations of ACAE, we established maximal efficacy with minimal local irritation for the 6.25% strength solution . Clinical efficacy and lack of toxicity of this formulation were confirmed by the additional clinical study of 65 patients . The antiperspirant and antibacterial actions of 6.25% ACAE solution were then verified on acne skin areas . It is postulated that the clinical improvement in acne that follows the topical use of ACAE results from one or both of these actions. Can J Microbiol, 1978 Nov, 24(11), 1321 - 30 {Effect of fatty acids on the antibacterial activity of butylated hydroxytoluene (BHT)}; Saheb SA et al.; This study deals with the effect of the association of certain fatty acids with butylhydroxytoluene (BHT) on the antibacterial activity of this antioxidant . Evidence is drawn from the results as to an increase of the inhibitory effect of the antioxidant towards a few bacterial strains when it is associated with either lauric acid or palmitoleic acid. Ann Intern Med, 1978 Nov, 89(5 Pt 2 Suppl), 842 - 5 Clinical investigators and the pharmaceutical industry; Kunin CM; Virtually all new drugs are introduced, evaluated, and marketed under the control of the pharmaceutical industry and general supervision of the Food and Drug Administration (FDA) . The clinical investigator must look to the pharmaceutical industry for support of studies of drugs, and the industry, in turn, needs the investigator to evaluate agents before FDA approval and to present findings in the medical media . A survey of members of the infectious Disease Society of America has shown heavy dependence on the pharmaceutical industry for support of applied studies of antibacterial and other chemotherapeutic agents . More than half the respondents believed that industry support was essential, about one third felt it was useful, and about one quarter would prefer other sources of support . Several proposals are presented to clarify the relations between investigators and the pharmaceutical industry and to provide for a broad-based clinical infectious disease consortium to provide research funds and plan educational programs in the field of infectious disease. Biol Bull Acad Sci USSR, 1978 Nov-Dec, 5(6), 690 - 5 Antibacterial activity of seawater and microvibrion-predators (Microvibrio marinus Roscoffensis) in it; Gelen AM et al.; In the seawater of the Atlantic Ocean and surface waters of different points of the World Ocean, including arctic basins and equatorial regions, microvibrion-predators of bacterial cells have been discovered . The number of microvibrions in the surface waters of the English Channel reaches a thousand cells per ml, but it varies, depending on the season . In this article a method of the separation and culture of microvibrions is described . The ultrastructure of two strains of microvibrions was investigated and a similarity found between their structure and Gram-negative bacteria . The distinctive features of microvibrions are their sea derivation and the ability to reproduce only in the presence of bacteria, without penetrating bacterial cells . To a certain extent, the antibacterial activity of seawater is connected with the presence in it of microvibrions. J Clin Periodontol, 1978 Nov, 5(4), 229 - 36 Extrinsic discoloration of teeth; Eriksen HM et al.; The majority of tooth discolorations are extrinsic in nature and appear as brown integuments . Various clinical indices and photometric techniques have been used for the evaluation of extrinsic discolorations . Smoking, tea or coffee consumption and increasing age are promoting factors and such discolorations are frequently seen in connection with oral use of antibacterial plaque-inhibiting mouthrinses . Chemical alteration of the acquired pellicle appears to be the major reason for these brown integuments. Invest Urol, 1978 Nov, 16(3), 196 - 200 Bladder surface mucin . Examination of possible mechanisms for its antibacterial effect; Parsons CL et al.; We have previusly provided physiologic and histochemical data implicating the bladder surface mucin layer as an important new antibacterial defense mechanism . This mucin or its contents seems to act as an "antiadherence factor", inhibiting bacterial adherence to the bladder mucosa and thereby facilitating the removal of bacteria by the voiding process . The present study was designed to investigate three mechanisms by which the mucin might repel bacterial attachment . Our data suggest that neither IgA nor a chelating agent are anti-adherence factors . We did find, however, that pH had a significant effect on the adherence of bacteria to mucosal cells stripped of their mucin layer . This result suggest that electrochemical charge is important in bacterial adherence . We beleive that the mucin layer both provides an electrochemical coat on the bladder surface that is a poor substrate for bacterial adherence and blocks the receptor sites of the transitional cells to which the microbes might adhere. Experientia, 1978 Oct 15, 34(10), 1322 - 3 An approach for the in vitro screening of drugs for activity against leprosy; Kato L et al.; Slow growing strains of mycobacteria isolated from leprous tissues present a characteristic resistance pattern to antibacterial agents that is comparable to drug sensitivity of M . leprae in man. Sem Hop, 1978 Oct 8-15, 54(29-32), 975 - 81 {Cefoxitin, a new semi-synthetic cephamycin (author's transl)}; Stapley EO et al.; The authors review the procedure utilized for the naming of a new antibiotic . The cephamycins are taken as an example . Cefoxitin, derivative of the cephamycin C through an original chemical reaction is described . This antibiotic possesses a high degree of resistance to beta-lactamases due to the presence of a methoxy group in the 7alpha position of the beta-lactam ring . The results of extensive in-vitro trials are given, they indicate that cefoxitin has a unique antibacterial activity.
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