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, ca