Bactericidal

Antimicrob Agents Chemother, 1990 Oct, 34(10), 1932 - 7
Comparative study of the effects of four cephalosporins against Escherichia coli in vitro and in vivo; van Ogtrop ML et al.; A thigh muscle infection induced with Escherichia coli in irradiated mice was used as a model to compare the in vivo pharmacodynamics of the antibacterial effect of four cephalosporins (i.e., cefepime, ceftriaxone, ceftazidime, and cefoperazone) with the in vitro antibacterial pharmacodynamics of these drugs . The following in vitro pharmacodynamic parameters were determined: the maximum effect as a measure for efficacy, the 50% effective concentration as a parameter for potency, and the slope of the concentration-effect relationship . For analysis of the in vivo antibacterial pharmacodynamics, the same parameters were applied for the dose instead of the concentration . For the detection of a relationship between concentration and antibacterial effect in vivo, we determined the pharmacokinetics of the four cephalosporins in the plasma of mice . The results showed that, in general, there is a direct relationship between the in vivo and in vitro pharmacodynamics of these cephalosporins . The maximum effects of cefepime, ceftazidime, and cefoperazone were approximately similar in vivo and in vitro . The sequence of potency of these drugs was, in descending order, cefepime, ceftazidime, and cefoperazone . Ceftriaxone differed from the other three cephalosporins in that it displayed unexpected in vivo pharmacodynamics . Ceftriaxone was just as efficacious as the other three in vitro, but its maximum effect in vivo was much lower . This relatively low maximum effect of ceftriaxone in vivo was not explained by the pharmacokinetic characteristics of the drug . From the present results it can be concluded that the in vitro efficacy of cephalosporins does not necessarily have a predictive value for the in vivo efficacy.

Akush Ginekol (Mosk), 1990 Oct, (10), 11 - 5
{Abortion as a cause of maternal mortality}; Volgina VF et al.; PIP: The medical documents of 342 women who died as a result of abortion (induced, self-induced, and outside of hospitals) were analyzed . 24.2% of the women were under 24 years of age, 51.3% were 25-34 years old, and the rest were 35 or older . 69.9% of the women died after abortion outside of hospitals and the rest after self-induced and induced abortions . 65.8% of the women were pregnant at 13-27 weeks of gestation . The death of 186 of 238 women was due to abortions performed outside of hospitals . Most of these were the result of invasive methods (the introduction of the catheter, solutions, rupture of the amniotic sac) . These women subsequently received medical assistance . 93.3% of them were hospitalized with delay, and only 2.6% were admitted in satisfactory condition . In a significant proportion of patients the examination was belated and inadequate . Various laboratory hematological tests that were essential for diagnosis and determination of the severity of the process were not done . The bacteriological tests to select the appropriate antibacterial drug were rarely performed--the tests were done for only 19.8% of women who had died of sepsis and for 14.3% of those who had died of peritonitis . Inadequate care manifested itself in the fact that diagnosis was established for only 46.8% of patients . Sepsis and peritonitis were the cause of death for 73.9% of all women and for 88.6% of those who died of abortion outside the hospital . Hemorrhage was the second most frequent cause, with 42 women dying because of it . Other causes were anaphylactic shock and thromboembolism of the pulmonary arteries . The elimination of such causes of death mandate goal-oriented preventive measures accompanied by diagnosis and therapy and the raising of the knowledge level of the medical personnel about purulent-septic infections . A radical improvement in bacteriological care also must be effected .

Nihon Kyobu Shikkan Gakkai Zasshi, 1990 Oct, 28(10), 1305 - 13
{Long-term therapeutic effects of erythromycin and newquinolone antibacterial agents on diffuse panbronchiolitis}; Yamamoto M et al.; The present study reviewed and summarized the long-term therapeutic effects of erythromycin or newquinolone antibacterial agents on diffuse panbronchiolitis . Various parameters before and after the treatment were analyzed in 101 patients selected from 227 diffuse panbronchiolitis patients gathered from 26 institutes in Japan . Patients had been treated with either erythromycin or newquinolone antibacterial agent for more than 3 months . Patients treated with erythromycin showed significant improvement of dyspnea on exertion, findings of chest X-ray, data on blood gas analysis, rate of ESR, titer of cold coagulation and amount of sputum, compared with patients treated with the newquinolone antibacterial agent . Among the patients treated with erythromycin, those patients with the initial high cold coagulation titer showed better improvement following treatment . However, there was no significant difference in improvement, depending upon either the duration between the time of onset of the disease, the initiation of treatment, and the initial severity of the disease.

Br J Clin Pract, 1990 Oct, 44(10), 404 - 8
Comparison of oral erythromycin ethylsuccinate and ciprofloxacin in the treatment of acute respiratory tract infections; Feld MS et al.; A total of 619 patients with acute upper or lower respiratory tract infection were randomised to receive either erythromycin ethylsuccinate tablets at a dose of 1 g twice daily, or ciprofloxacin tablets 500 mg twice daily in a single-blind, multicentre study . The efficacy of each antibacterial was similar, with close to 90% of patients on each treatment being reported as either cured or improved . Gastrointestinal symptoms were the most commonly reported side-effects, being similar in overall incidence for both agents . Nausea, vomiting, dizziness and headache occurred more frequently in the ciprofloxacin group, while abdominal pain and diarrhoea occurred more frequently in the erythromycin ethylsuccinate group . In each group, the number of patients failing to complete treatment was similar and the main reasons cited for discontinuation were gastrointestinal symptoms . This study indicates that both erythromycin ethylsuccinate and ciprofloxacin are well tolerated and are equally effective for routine empirical treatment of acute respiratory tract infections.

Rozhl Chir, 1990 Oct, 69(10), 668 - 73
{Cefuroxime axetil (Zinnat)--laboratory and clinical study}; Vyhnanek F et al.; The authors investigated the antibacterial action of cefuroxim in vitro and proved its relatively broad spectrum of action . Administration of the esterified form, Zinnat, produced very satisfactory therapeutic concentrations of cefuroxim in serum, bile tissue of operated gallbladders . The prophylactic administration of the combined parenteral and oral form of cefuroxim proved excellent in biliary surgery in twenty patients.

J Antimicrob Chemother, 1990 Oct, 26 Suppl B, 167 - 72
Prospective randomized comparison of pefloxacin and ampicillin plus gentamicin in the treatment of bacteriologically proven biliary tract infections; Chacon JP et al.; One hundred and eighty-nine patients with acute cholecystitis or cholangitis requiring antibacterial therapy and surgery were randomly allocated in a prospective open study to receive either iv or oral pefloxacin (800 mg per day) or a combination of iv or oral ampicillin (4 g per day) and gentamicin (240 mg per day im) . Ninety-two patients had to be withdrawn from the efficacy analysis, mainly because of negative baseline culture, but occasionally because of isolation of bacteria resistant to the study drugs . In the 97 evaluable patients (90 with cholecystitis and 7 with cholangitis) the clinical cure rates were excellent and similar for both groups: 49/50 (98%) for pefloxacin and 45/47 (95.7%) for the combination; the respective bacteriological success rates were 100% and 91.5% . Three patients in the pefloxacin group and six patients in the ampicillin-gentamicin group reported mild and transient side effects.

J Trauma, 1990 Oct, 30(10), 1267 - 72
Splenectomy influences endotoxin-induced bacterial translocation; Spaeth G et al.; To determine whether splenectomy affects the antibacterial defenses of the gut, experiments were performed using bacterial translocation (BT) as a marker of intestinal barrier failure . The incidence of BT was measured 8 days after splenectomy or sham-splenectomy in mice receiving or not receiving endotoxin (0.1 mg IP) . Splenectomy does not appear to promote BT from the gut, since the incidence of bacterial translocation after splenectomy or sham-splenectomy (5%) were not different . A second experiment was performed to determine whether the resistance to endotoxin-induced BT was modified after splenectomy . The incidence of endotoxin-induced BT was 73% in the unoperated control group, 59% in the sham-splenectomy group, but 23% in the splenectomy group (p less than 0.002) . Thus, splenectomy but not sham-splenectomy increased the resistance of otherwise healthy mice to endotoxin-induced BT.

Am J Hum Genet, 1990 Oct, 47(4), 686 - 97
Alleles at the PRB3 locus coding for a disulfide-bonded human salivary proline-rich glycoprotein (Gl 8) and a null in an Ashkenazi Jew; Azen EA et al.; From electrophoretic analysis, we identified in the saliva of an Ashkenazi Jew a disulfide-bonded major glycoprotein variant (Gl 8) that is a product of the proline-rich protein (PRP) locus PRB3 . A previous study of this variant protein misidentified it as Pa 2 and as a product of a different PRP locus . The other PRB3 allele in this individual is an apparent null . To identify the mutations, we sequenced the tandemly repetitious exon 3 (the major protein-coding portions) of both alleles . A CGT----TGT (Arg----Cys) mutation was found in one allele (PRB3Scys), which accounts for the disulfide-bonded and peroxidase-modifying properties of Gl 8 . A single nucleotide insertion was found in the other allele (PRB3Mnull) that leads to a frameshift with a premature termination codon that causes an apparent lack of gene expression . Null alleles are frequent at PRP loci coding for basic and glycosylated PRPs, and the mechanism described might explain other null phenotypes among PRPs . From nucleotide comparisons, a model of intragenic unequal crossing-over is proposed to explain, in part, the generation of the PRB3Mnull allele . The Gl 8 protein variant is found in Ashkenazi Jews (gene frequency around .008) but not in the general white, black, or Japanese populations . It is interesting that products of different PRP genes, Gl 8 from PRB3 and Pa 1 from PRH1, are both disulfide bonded and probably modify salivary peroxidase (part of an important intraoral antibacterial system) through formation of disulfide-bonded heterodimers.

Scand J Dent Res, 1990 Oct, 98(5), 422 - 7
Further in vivo studies on the plaque-inhibiting effect of chlorhexidine and its binding mechanisms; Waaler SM; The aim of the present study was to investigate the relative importance of chemical groups in the oral cavity which bind chlorhexidine of clinical significance . This was performed by clinical experiments where a test panel of 11 individuals rinsed with chlorhexidine at pH 7, pH 5.5, and pH 3 . Rinsing with 0.02 M EDTA was performed prior to the chlorhexidine rinse, because this procedure has been shown to enhance the antibacterial effect of chlorhexidine in vitro . However, pre-rinses with EDTA did not increase the clinical effect of chlorhexidine . Bacteriologic tests showed comparable antibacterial effect of chlorhexidine at pH 7 and pH 3 . Mouthrinses of pH 7 and pH 5.5 had comparable plaque-inhibiting effects, whereas the effect of a rinse of pH 3 was not different from that of the placebo . This finding is interpreted to suggest that primary phosphate (pK about 2) is an important receptor site for chlorhexidine, whereas secondary phosphate (pK = 7.0) is of negligible importance . Previous studies have clearly shown that phosphate binds chlorhexidine . The lack of clinical effect at pH 3 is probably due to precipitation of salivary proteins by hydrogen ions, making primary phosphate groups unavailable for interaction with chlorhexidine.

J Antibiot (Tokyo), 1990 Oct, 43(10), 1278 - 85
Synthesis and antibacterial activity of 7 beta-{1-(2-aminothiazol-4-yl)-1-cyclopropanecarboxyamido}cephem derivatives; Nishimura S et al.; The synthesis and antibacterial activity of several 7 beta-{1-(2-aminothiazol-4-yl)-1-cyclopropanecarboxyamido}cep hem derivatives (1) are described . The structure-activity relationships of 1 are also presented.

Vestn Khir Im I I Grek, 1990 Oct, 145(10), 70 - 2
{Prevention of suppurative complications after closure of formed intestinal fistulas in children}; Biriukov AV et al.; The problem of prophylactics of postoperative infectious complications in the surgery of digestive tract is discussed . A comparative analysis of efficiency of two methods of antibacterial prophylactics during operations of closing the formed intestinal fistulas in children is given . High efficiency of the method of preoperative subtotal decontamination of the intestine according to individually selected schemes is shown.

Antimicrob Agents Chemother, 1990 Oct, 34(10), 1955 - 60
Inhibitory effects of quinolones on pro- and eucaryotic DNA topoisomerases I and II; Moreau NJ et al.; As a means of gaining information on the selectivity of quinolone antibacterial agents, we examined their effect on four topoisomerases, topoisomerases I and II purified from Escherichia coli and calf thymus . The inhibition of supercoiling and relaxation activities was monitored by using the classical gel electrophoresis assay . Eight quinolones were assayed by using the four enzymes . Gyrase was much more sensitive to quinolones than the other topoisomerases which can therefore be inhibited by moderate concentrations of certain quinolones . No good correlation was observed between the activity on gyrase and on the other enzymes, since the ratio varied from 15 to more than 8,500 . On the contrary, there was a good correlation between early inhibition of DNA synthesis, inhibition of gyrase, and MICs.

FEBS Lett, 1990 Sep 3, 269(2), 413 - 20
1H nuclear magnetic resonance study of the solution conformation of an antibacterial protein, sapecin; Hanzawa H et al.; The solution conformation of an antibacterial protein sapecin has been determined by 1H nuclear magnetic resonance (NMR) and dynamical simulated annealing calculations . It has been shown that the polypeptide fold consists of one flexible loop (residues 4-12), one helix (residues 15-23), and two extended strands (residues 24-31 and 34-40) . It was found that the tertiary structure of sapecin is completely different from that of rabbit neutrophil defensin NP-5, which is homologous to sapecin in the amino acid sequences and also has the antibacterial activity . The three-dimensional structure determination has revealed that a basic-residue rich region and the hydrophobic surface face each other on the surface of sapecin.

Pol Tyg Lek, 1990 Sep 3-10, 45(36-37), 749 - 51
{Netilmicin in the treatment of bacterial respiratory tract infections}; Wandzilak M et al.; Netilmicin - a semisynthetic aminoglycoside - was administered to 33 patients with the acute or chronic lower respiratory tract or pulmonary infections in a daily dose of 5 mg/kg body weight for 10 days . A principle criterium of patients classification to netilmicin therapy were sensitive bacterial strains either in sputum or in BAL liquid . A significant clinical improvement was noted in 88% of the treated patients . However, elimination of pathogens from the sputum was achieved only in 52% of these patients . No improvement was observed in 4% of the treated patients . No adverse reactions were noted . Netilmicin proved safe and effective antibacterial agent in patients with respiratory infections.

Equine Vet J Suppl, 1990 Sep, (10), 18 - 21
Peripheral corneal ulcers in the horse; Dice PF et al.; This report involves a retrospective study of five horses with an unusual form of progressive peripheral corneal ulcers . These ulcers were located at the perilimbal region of the cornea and spread both centripetally to mid periphery and circumferentially . Lipping of the epithelial edge was observed often . The depth ranged from superficial to mid stroma . Patients ranged from two and a half to eight years, both sexes, and were referred after a variety of antibacterial therapy . Histories were similar in that all ulcers were initially located adjacent to the limbus in one or more quadrants . No trauma was known to antedate the corneal disease and the patients were in good general health . Conjunctivectomy was performed in three patients which revealed an abundance of plasma cells and lymphocytes . All five cases were negative for a specific bacterial pathogen . Patients responded to a variety of treatment modalities: topical corticosteroid, surgical debridement, therapeutic soft contact lens (TSCL), and/or conjunctivectomy.

Anesteziol Reanimatol, 1990 Sep-Oct, (5), 66 - 7
{A case of the successful treatment of an 11-year-old child with a fulminating form of tetanus}; Egorov VM et al.; A case of a successful treatment of a patient with an extremely severe tetanus form is described . The management of the patient included massive specific antibacterial and infusion therapy, hemoperfusion, standard and high frequency controlled lung ventilation . The problems of patient activation and respiration recovery have arisen in the course of treatment . They were dealt with, using hemoperfusion that reduced the residual effect of sedative agents and myorelaxants, as well as high frequency jet ventilation, which accelerated respiration recovery.

Antimicrob Agents Chemother, 1990 Sep, 34(9), 1637 - 41
In vitro selection of resistant Helicobacter pylori; Haas CE et al.; Four strains of Helicobacter pylori were subjected to an in vitro serial passage technique to compare the propensity of the organisms to develop resistance to seven classes of antibacterial agents . The passages were made on serially doubling concentrations of antibacterial agents incorporated into agar starting at one-half the base-line MIC . The frequency of spontaneous resistance was also determined for each strain at four and eight times the MIC of each antibacterial agent . Strains resistant to ciprofloxacin, metronidazole, erythromycin, and tobramycin were isolated . The experiments failed to select organisms resistant to bismuth subsalicylate, furazolidone, or amoxicillin, although the MIC of amoxicillin was increased 4- to 16-fold . With the exception of erythromycin, organisms with the selected resistance were stable after at least three passages on antibacterial agent-free medium . Spontaneous resistance rates were generally of a low magnitude and were not predictive of the serial passage results.

Vrach Delo, 1990 Sep, (9), 51 - 3
{The diagnostic significance of the test for spontaneous blood neutrophil damage in acute myeloid forms of leukemia}; Guseva SA; Spontaneous lesioning of neutrophils (SLN) cultured in a saline solution was studied in 75 patients with acute myeloid leucosis . Results indicate a significant increase of the SLN number in the group of patients with the presence of infectious complications . It is recommended to use the SLN test as a criterion of diagnosis and efficacy of antibacterial treatment of infectious complication in patients with acute myeloid leucosis.

Pharmazie, 1990 Sep, 45(9), 688 - 9
{Synthesis and action of 1-n-hexyl-2-phenyl-3-(n-alkoxymethyl)- and 1-n-hexyl-2-phenyl-3-(6-n-alkylthiomethyl)imidazolium chlorides}; Pernak J et al.; The synthesis of quaternary imidazolium chlorides was performed by reaction of 1-n-hexyl-2-phenyl-imidazole with chloromethylalkyl ether or chlormethylalkyl sulfide . The antibacterial properties of the compounds obtained was tested on 13 strains of bacteria and fungi . Chlorides with octyl- and decylthiomethyl moiety indicated the best antibacterial activity.

Stomatologiia (Mosk), 1990 Sep-Oct, (5), 24 - 6
{The use of an ortofen-containing paste in the combined treatment of periodontal diseases}; Dotsenko EV et al.; A periodontal dressing for the treatment of gingivitis and periodontitis, characterized by antiinflammatory and antibacterial action, was developed and clinically tried . Application of this dressing cut down the periods of treatment of chronic gingivitis and periodontitis, shortens the period of preparation to surgery, and provides a smooth course of the postoperative period.

Antibiot Khimioter, 1990 Sep, 35(9), 40 - 2
{Antibiotic binding by leukocytes from brucellosis patients}; Nigmatulin AZ et al.; Antibiotic binding by leukocytes from patients with chronic brucellosis was studied in vitro . The pathogens were located intracellularly . The specimens were collected during the disease aggravation prior to the treatment and at the beginning of the remission after the routine therapy . It was found that during the disease aggravation at the intoxication peak and accumulation of a large number of Brucella in the cells binding of methacycline, rifampicin and gentamicin somewhat increased . After completion of the treatment course when the number of Brucella in the leukocytes markedly lowered, up to disappearance, the antibiotic binding decreased and reached the control figures . Penetration of erythromycin into the cells infected with Brucella lowered at the disease peak and remained at that level with an insignificant tendency to normalization at the beginning of the clinical remission after the treatment . The facts suggested that intracellular localization of the bacteria would change the quantitative characteristics of interaction of the cells, i.e . human leukocytes with antibacterial chemotherapeutic agents . The direction of the shifts must depend on the particular proportion of various types of mechanisms for penetration of drugs into the intracellular medium.

Antibiot Khimioter, 1990 Sep, 35(9), 14 - 7
{Taxonomic spectrum of pathogens of mixed infections in oncology patients and principles of their antibacterial therapy}; Smolianskaia AZ et al.; Mixed infections were observed in oncological patients irrespective of the tumor or infectious process localization . 25-30 per cent of the pathological materials from such patients were contaminated with bacterial associations . The number of the associates ranged from 2 to 5 depending on the pathological material tested . Therapy of infectious complications due to pathogen associations should stem from analysis of many factors, i.e . properties of the isolated or likely pathogens, individual characteristics of the patients, compatibility of the drugs used and their pharmacokinetic features.

J Antimicrob Chemother, 1990 Sep, 26 Suppl A, 1 - 10
Serum protein binding and extravascular diffusion of methoxyimino cephalosporins . Time courses of free and total concentrations of cefotaxime and ceftriaxone in serum and pleural exudate; Scaglione F et al.; A new approach to the study of the distribution pharmacokinetics of variably bound beta-lactams is to plot the concentration time course of their free (dialysable) and total (free and bound) forms . In the present study, the 6-h concentration time course was plotted of the total and free concentrations of cefotaxime and ceftriaxone in serum and pleural exudate in 12 patients per group, after iv dosing with 1 g of either cefotaxime or ceftriaxone . Samples were taken at 0.5, 1, 1.5, 2, 3, 4 and 6h after dosing . The results of a study of similar design, but conducted over 24 h in ten patients per group, following iv dosing with either cefotaxime 1 g 12-hourly or ceftriaxone 1 g daily are also reported . Samples were taken at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 14, 16 and 24 h after dosing . Areas under the curve of free cefotaxime in pleural fluid were greater than those of free ceftriaxone, in both the 6 h (+54.6%) and 24 h studies (+29.8% after 12 h and +71.0% after 24 h) . The free cefotaxime/free ceftriaxone Cmax ratio was 1.75 in the 6 h study . Cefotaxime was superior to ceftriaxone in terms of the diffusion of the free (antibacterially active) fraction into a typical inflammatory exudate . Assessment of the effects of protein binding must be taken into account in antibiotic pharmacokinetic profiles.

J Antibiot (Tokyo), 1990 Sep, 43(9), 1160 - 8
Synthesis and biological activity of 3-vinylthio- and 3-vinylthiomethylcephem derivatives; Nishimura S et al.; The synthesis and biological properties of some 3-vinylthio- and 3-vinylthiomethylcephem derivatives are described . Both series possess potent antibacterial activity . Among them, 3-{(Z)-2-cyanovinylthiomethyl}cephem derivative was found to have an expanded antibacterial spectrum.

J Antibiot (Tokyo), 1990 Sep, 43(9), 1137 - 49
Synthesis and antibacterial activity of C-2 alkenylthio-carbapenem derivatives; Corbett DF et al.; A number of C-2 aminoalkenylthio-carbapenem derivatives possessing both the (5R,6R, 8S)- and the (5R,6S,8R)-stereochemistries have been prepared from the olivanic acids MM 22382 and MM 22383, respectively . Certain members of this new class of compounds displayed potent, broad spectrum antibacterial activity as well as improved stability to human kidney homogenate.

J Antibiot (Tokyo), 1990 Sep, 43(9), 1089 - 97
Synthesis and biological activity of some amide derivatives of the lantibiotic actagardine; Malabarba A et al.; A series of basic carboxamides of actagardine (1), a lantibiotic possessing good antistreptococcal activity, were synthetized . Some physico-chemical characteristics, in particular charge and lipophilicity, that influence water solubility were determined . The in vitro and in vivo activity was evaluated . The monocarboxamides were generally more active than actagardine against selected Gram-positive bacteria . The 3,3-dimethylamino-1-propylamide hydrochloride (4) showed good water solubility, bactericidal action and favourable antibacterial activity and it appears to be a suitable drug for further investigation.

J Antibiot (Tokyo), 1990 Sep, 43(9), 1059 - 63
Simaomicin (LL-D42067), a novel antibiotic from Actinomadura madurae . I . Taxonomy, fermentation and biological activity; Maiese WM et al.; A new antibacterial antibiotic, designated simaomicin alpha (LL-D42067 alpha) was isolated from the fermentation broth of an actinomycete strain . Based on cultural, physiological, morphological and chemical characteristics, culture LL-D42067 was identified as a new subspecies of Actinomadura madurae . Simaomicin alpha demonstrated potent activity against Gram-positive bacteria and was active in vivo against a variety of Eimeria species causing coccidiosis in chickens.

Int J Lepr Other Mycobact Dis, 1990 Sep, 58(3), 503 - 11
Sequential monitoring of leprosy patients with serum antibody levels to phenolic glycolipid-I, a synthetic analog of phenolic glycolipid-I, and mycobacterial lipoarabinomannan; Meeker HC et al.; Sequential serum samples from leprosy patients at various stages of antibacterial treatment were tested by an ELISA for antibodies to phenolic glycolipid I (PGL-I), a synthetic PGL-I analog (ND-BSA), and lipoarabinomannan (LAM) from Mycobacterium tuberculosis to determine if these antibodies could be useful in monitoring response to therapy . Among patients with positive initial anti-PGL-I IgM, a significant decrease in this antibody was seen over time (p less than 0.01), whether assayed by PGL-I or ND-BSA . The two antigens showed good agreement in the detection of decrease in anti-PGL-I IgM . The greatest decrease was seen in patients with a high initial anti-PGL-I IgM and a high bacterial index (BI) . Patients with a declining BI were seen to have generally declining antibody levels to PGL-I and to LAM; in those patients with a fluctuating BI, antibody levels were less predictable . We conclude that antibodies to PGL-I and LAM can be useful in following response to therapy in leprosy patients and that either the native PGL-I or ND-BSA can serve as antigen for the ELISA.

Chem Pharm Bull (Tokyo), 1990 Sep, 38(9), 2459 - 62
Studies on antibacterial agents . II . Synthesis and antibacterial activities of substituted 1,2-dihydro-6-oxo-6H-pyrrolo{3,2,1-ij}quinoline-5-carboxylic acids; Ishikawa H et al.; A series of substituted 1,2-dihydro-6-oxo-pyrrolo{3,2,1-ij}quinoline-5-carboxylic acids for the treatment of systemic infections was synthesized via 7-bromo-3-ethylthio-4,5-difluoro-2-methylindole (3), which was prepared by Gassman's indole synthesis in excellent yield . The synthesized pyrroloquinolines were tested for their antibacterial activities . 8-Fluoro-1,2-dihydro-2-methyl-9-(4-methyl-1-piperazinyl)-6-oxo-6H- pyrrolo{3,2,1-ij}quinoline-5-carboxylic acid showed a potent antibacterial activity against gram-positive and gram-negative bacteria.

Haematologica, 1990 Sep-Oct, 75(5), 454 - 63
Haematologic abnormalities in the acquired immunodeficiency syndrome; Brizzi MF et al.; During the clinical history of HIV infection, haematological abnormalities represent a common finding which not only contributes to worsening the clinical condition but also limit the use of antibacterial as well as antiviral agents . On the basis of the regulatory role played by the immune system on haemopoiesis, in the present review the foremost derangements of the immunoregulatory circuits are first discussed . The main functional and quantitative defects of peripheral blood erythrocytes, granulocytes, platelets and monocytes are then analysed, and the different bone marrow pictures observed during the progression of the disease are described . To elucidate the physiophatogenetic mechanisms responsible for bone marrow and peripheral cytopenia, the most relevant in vitro studies are reported and discussed . These studies suggest that both a direct cytopathic effect of HIV on haemopoietic progenitors and an immune system mediated mechanism are involved . In view of the HIV selective tropism for lymphocytes and macrophages, which are a major source of haemopoietic growth factors, the new therapeutical strategies for the treatment of cytopenias based on exogenous administration of these cytokines, alone or in combination with antiviral drugs, are briefly reported.

Am J Dent, 1990 Sep, 3 Spec No, S7 - 14
Antiplaque effects of dentifrices containing triclosan/copolymer/NaF system versus triclosan dentifrices without the copolymer; Gaffar A et al.; A dentifrice containing triclosan/PVM/MA, Colgate Gum Protection Formula Toothpaste (GPF), was found to be highly effective against oral bacteria with minimal inhibitory concentration ranging from 0.3 to 5.35 micrograms/ml . A variety of in vitro model systems simulating oral environment were used to compare dentifrices containing triclosan/PVM/MA versus the dentifrices containing triclosan without PVM/MA, such as Crest Gum Health Toothpaste (CGH) and Neo-Mentadent P Toothpaste (N-MP) . The uptake of triclosan on saliva-coated hydroxyapatite (HA) disks and buccal epithelial cells was significantly higher from the GPF versus the other dentifrices . Uptake on HA disks was 132 micrograms/disk versus 11 micrograms/disk from CGH; on buccal epithelial cells the uptake was 59 micrograms/2 x 10(5) cells with GPF versus 30.0 micrograms with CGH per same number of cells . The retained triclosan on the surfaces provided a sustained and higher antibacterial effect up to 4 hours post-treatment with GPF, but not with N-MP and CGH . In dynamic plaque model systems such as the chemostat or the controlled saliva flow system, GPF was significantly (P = 0.05) more effective than N-MP or CGH in reducing plaque thickness, protein and carbohydrate contents of plaque films . Collectively, the results of these microbiological and biochemical investigations indicate that the GPF has the potential to provide superior clinical efficacy versus the dentifrices without the copolymer.

Vopr Med Khim, 1990 Sep-Oct, 36(5), 21 - 4
{Guanylate cyclase from human platelets in pulmonary tuberculosis}; Riaposova IK et al.; Activity of soluble guanylate cyclase and activating effect of sodium nitroprusside were studied in thrombocytes of patients with infiltrative form of pulmonary tuberculosis before treatment (as soon as patients entered the hospital) and within various periods of the antibacterial therapy course: during the first month, 1.5-2, 2.5-3.5 and more than 4 months of treatment . Before treatment activity of guanylate cyclase in the patients thrombocytes was similar to that of donors independently on severity of the process in lungs (impairment of more or less two lung segments) . During the antibacterial therapy the enzyme activation was detected, which reached 160% of the normal level within 2 months course and decreased down to the control rate within 4 months of treatment . The activating effect of sodium nitroprusside was distinctly decreased (by 70%) in thrombocytes of patients with infiltrative form of pulmonary tuberculosis before the treatment course, while the pattern was restored to the normal level, comparable with control values in donors, within 4 months of the treatment . The stimulating effect of sodium nitroprusside on guanylate cyclase activity in thrombocytes of patients with infiltrative form of pulmonary tuberculosis may be used as an additional criterion for evaluation of the therapeutic course efficiency.

Schweiz Rundsch Med Prax, 1990 Aug 21, 79(34), 976 - 82
{Typhoid fever}; Losse H; The second part of this review accounts on a patient with classic symptoms of typhoid fever . The case history is commented in the light of todays knowledge . The case was taken from the clinical notes of Schonlein one of the most famous clinicians of the first part of the 19th century . It reveals the difficulties of the physician to cope with such a disease without our present diagnostic and therapeutic possibilities . It is surprising to realize that 150 years ago therapy of typhoid fever was not substantially different from that in use up to the recent introduction of specific antibacterial therapy . Since the typical course of typhoid fever is only rarely encountered nowadays the case seems suitable to recall this clinical picture to our generation of physicians.

J Med Chem, 1990 Aug, 33(8), 2270 - 5
Quinolone antibacterial agents substituted at the 7-position with spiroamines . Synthesis and structure-activity relationships; Culbertson TP et al.; A series of fluoroquinolone antibacterials having the 7-position (10-position of pyridobenzoxazines) substituted with 2,7-diazaspiro{4.4}nonane (4b), 1,7-diazaspiro{4.4}nonane (5a), or 2,8-diazaspiro{5.5}undecane (6b) was prepared, and their biological activities were compared with piperazine and pyrrolidine substituted analogues . Most exhibited potent Gram-positive and Gram-negative activity, especially when side chain 4b was N-alkylated.

EMBO J, 1990 Aug, 9(8), 2507 - 15
Insect immunity: expression of the two major inducible antibacterial peptides, defensin and diptericin, in Phormia terranovae; Dimarcq JL et al.; Injections of low doses of bacteria into larvae of Phormia terranovae induce the appearance of potent bactericidal peptides in the blood, among which predominate the anti-Gram positive insect defensins and the anti-Gram negative diptericins . Insect defensins show significant homologies to mammalian (including human) microbicidal peptides present in polymorphonuclear leukocytes and macrophages . We report the molecular cloning of cDNAs and primer extension studies which indicate that insect defensin is produced as a prepro-peptide yielding mature defensin A (40 residues) after cleavage of a putative signal peptide (23 residues) and a prosequence (34 residues) . Previous studies have established that diptericin (82 residues) is matured from a pre-peptide by cleavage of a putative signal peptide (19 residues) and C-terminal amidation . Using oligonucleotide probes complementary to the sequences of the mRNAs for defensin and diptericin, we show by in situ hybridization that both antibacterial peptides are concomitantly synthesized by the same cells: thrombocytoids, a specialized blood cell type, and adipocytes . Transcriptional studies based on hybridization of RNAs to cDNAs of defensin and diptericin indicate that the transcription of both genes is induced regardless of the nature of the stimulus (injection of Gram positive or Gram negative bacteria, lipopolysaccharides) . Even a sterile injury applied to axenically raised larvae is efficient in inducing the transcription of both genes suggesting that the local disruption of the integument aspecifically initiates a signalling mechanism which the thrombocytoids and the adipocytes are able to interpret . The transcription of immune genes is relatively short lived and a second challenge yields a response similar to that of the first stimulus, indicating that the experimental insects do not keep a 'memory' of their first injection.

Antibiot Khimioter, 1990 Aug, 35(8), 37 - 9
{Rapid evaluation of the effectiveness of antibacterial drugs in experimental tularemia}; Oborin VA et al.; Rapid estimation of the protective effect of antibacterial drugs on Fransiella tularensis for not more than 2 days was shown possible in experiments on albino mice infected with tularemia . High efficacy of aminoglycosides (kanamycin, gentamicin, streptomycin, amikacin, netilmicin, tobramycin, sagamycin, ribostamycin and sisomicin), tetracyclines (tetracycline, doxycycline, minocycline and methacycline), rifampicin, phosphomycin and oxolinic acid was determined with the recommended rapid method . Amoxycillin, ampicillin, piperacillin, carbenicillin, erythromycin, levomycetin, cefradine, cefmetazole, cefatrizine, cefoxitin, cefsulodin and bactrim (biseptol) proved to be inefficient against the tularemia causative agent.

Antibiot Khimioter, 1990 Aug, 35(8), 35 - 7
{Comparative study of the effectiveness of amikacin and streptomycin in experimental tularemia}; Tynkevich NK et al.; In vitro study on antibacterial activity of amikacin in comparison to that of streptomycin revealed a high sensitivity of tularemia microbes of three geographical races to it . Amikacin showed a high therapeutic activity in treatment of albino mice infected with tularemia . The prospects of amikacin use in prophylaxis and treatment of tularemia are defined by its antibiotic activity against streptomycin-resistant forms of the tularemia causative agent.

Dan Med Bull, 1990 Aug, 37(4), 375 - 7
Prescribing in hospital outpatient departments and rural health facilities in Uganda: some clinical and educational implications; Christensen RO et al.; A comparison of prescribing patterns in hospital outpatient departments (OPD) and rural health units (RHU) in Uganda revealed an average of 2.45 and 1.66 drugs prescribed per treatment episode in OPD and RHU respectively . 40.1% of the OPD and 57.3% of the RHU prescriptions included antibacterials . It is argued that in view of the relevant morbidity pattern, an average of 1.4-1.5 drug/treatment episodes, as well as 15-20% receiving antibacterials would seem appropriate, thus leaving scope for considerable cost reductions . A successful strategy for achieving rational prescribing is likely to include a variety of educational approaches aimed at all present and future prescribers.

Planta Med, 1990 Aug, 56(4), 364 - 7
Growth, terpenoid production and antibacterial activity of an in vitro culture of the liverwort Fossombronia pusilla; Sauerwein M et al.; In vitro cultures of the liverwort, Fossombronia pusilla, have been ititiated from spores . They grew well on Gamborg B5 medium supplemented with 2% saccharose and 12.5 micrograms/l vitamin B12 . Undifferentiated cultures were obtained on Knop mineral solution with 4% glucose . The cultures produced the same constituents as collected material . Perrottetianal A and B, known substances from liverworts were isolated and characterized by spectroscopic methods as well as alpha-(-)-santonin . A hitherto unknown diterpene dialdehyde-8-hydroxy-9-hydroperrottetianal A--could also be characterized . Furthermore, 7 terpenes were identified by GC/MS . A petrol ether extract and the isolated terpenes exerted antibacterial activity.

Nippon Hinyokika Gakkai Zasshi, 1990 Aug, 81(8), 1240 - 6
{Follow-up of 104 children with "primary" VUR . Incidence of unstable bladder, its impact on resolution of VUR and progression of renal scar}; Kakizaki H et al.; One hundred and four children (48 boys and 56 girls, ranging in age from 3 months to 15 years, and follow-up period of more than 2 years in all) with "primary" vesicoureteral reflux (VUR) were retrospectively analyzed with particular emphasis on resolution of VUR and occurrence of renal scar . All underwent cystoscopic examinations which failed to demonstrate any organic vesicourethral obstruction, and all were neurologically normal . The patient population was divided into 2 groups based on cystometric findings . Group 1 consisted of 74 patients with unstable bladder and Group 2 consisted of 30 patients without unstable bladder . Although both groups were initially kept under antibacterials, in Group 1 frequent voiding and anticholinergics were maintained until the bladder stabilized by itself . There was no difference in the grade of reflux between the two groups . The rate of spontaneous resolution of reflux was 18% in group 1 in which more than 60% of the patients were with high grade reflux, while in Group 2 it was 17%, similarly to Group 1, but all were with low grade reflux . The presence or absence of renal scar and its subsequent evolution were determined in 73 patients in whom serial urograms were available enough to evaluate nephrographic renal outline . The incidence of renal scar at the first visit was 26% in Group 1 and 36% in Group 2 . New formation of renal scar was not found in either group . The progression of preexisting renal scar was seen only in Group 1 (5/55 patients, 9%), and not in Group 2 (0/18 patients, 0%).(ABSTRACT TRUNCATED AT 250 WORDS)

FEMS Microbiol Lett, 1990 Aug, 58(3), 311 - 6
Simultaneous exploitation of different peptide permeases by combinations of synthetic peptide smugglins can lead to enhanced antibacterial activity; Smith MW et al.; Various synthetic, peptide prodrugs (smugglins) were tested alone and in combination for activity against Escherichia coli . The smugglins may be transported through any of three peptide permeases, and once inside the bacteria are activated by intracellular peptidase action to release their intrinsically impermeant, antibacterial moieties . When each such antibiotic peptide present in a mixture was accumulated via a different permease, synergistic effects could be observed . Synergy was also found when smugglins were combined with other non-peptide antibiotics . The principle of using smugglin combinations could extend the scope of their application, and should minimise the potential problem that can arise from the occurrence of resistant, transport mutants . The smugglin interactions were studied using a modified microtitre plate assay.

Antimicrob Agents Chemother, 1990 Aug, 34(8), 1512 - 4
Bactericidal effect of doxycycline associated with lysosomotropic agents on Coxiella burnetii in P388D1 cells; Raoult D et al.; There is no consistently reliable treatment for endocarditis resulting from chronic Coxiella burnetii infection, the causative agent of Q fever . Although certain antibiotics are recommended on the basis of their in vitro bactericidal activities, results of therapy with these antibiotics are often disappointing . To evaluate whether the currently recommended antibiotic susceptibility tests for C . burnetii give misleading results because of continued division of uninfected cells, thereby resulting in the dilution of infected cells and, hence, a false picture of antibiotic efficacy, we blocked cell division during antibiotic susceptibility testing with cycloheximide . Using this new method, we found that the currently recommended antibiotics for the treatment of Q fever, doxycycline, pefloxacin, and rifampin, did not reduce the ratio of infected to noninfected cells (either L929 or P388D1) by 9 days postinfection . To test the hypothesis that this lack of antibacterial activity is due to antibiotic inactivation by the low pH of the phagolysosomes in which C . burnetii is found, we used alkalinizing lysosomotropic agents (chloroquine or amantadine) concurrently with doxycycline . This resulted in the sterilization of C . burnetii infection in P388D1 cells . This finding seems to confirm our suspicion that the acidic conditions of the phagolysosomes in which C . burnetii is located inhibit antibiotic activity . This inhibition can be reversed in vitro when lysosomotropic alkalinizing agents are used.

Dtsch Tierarztl Wochenschr, 1990 Aug, 97(8), 307 - 13
{A review of the diagnostic possibilities of illegal drug administration in slaughtered animals and meat inspection}; Ellerbroek L; A review of possible residues of selected antibacterial substances, hormones, beta-agonists, thyreostatics and tranquillizers in meat is given in this paper . Showing their application mode and the few clinical effects and pathological findings, the collection of samples becomes very important . For each group of substances tissues or body-fluids are proposed as samples . With modern analytical detection methods residues in food of animal origin can be demonstrated at levels of micrograms/kg . The detection of the above mentioned substances could be supported by a well-aimed sampling and the illegal use can be diminished.

Biopharm Drug Dispos, 1990 Aug-Sep, 11(6), 533 - 41
Pharmacokinetics of aditoprim in goats using a radioassay; Iqbal MP et al.; A simple, highly sensitive radioassay was developed for the activity of a newly discovered inhibitor of dihydrofolate reductase (DHFR), aditoprim . The procedure is based on the inhibition of binding of {3H}-methotrexate ({3H}MTX) with bacterial dihydrofolate reductase by the antifolate, aditoprim . The analytic sensitivity using this binding inhibition method was less than 5 ng in plasma . The procedure developed requires no extraction of the drug from the plasma . The variation of simultaneous duplicate determinations was 6.3 per cent, whereas the variability of plasma samples assayed on different days was less than 11 per cent . The assay developed was applied to study the pharmacokinetics of aditoprim in the goat . In comparison with trimethoprim (TMP), the new inhibitor of DHFR, aditoprim, had a longer half-life and a larger volume of distribution, suggesting enhanced and prolonged antibacterial activity of aditoprim over TMP.

J Periodontol, 1990 Aug, 61(8), 536 - 41
Susceptibility of oral bacteria to phenoxyethanol and phenoxyethanol/chlorhexidine combinations; Wilson M et al.; A total of 57 bacterial strains (26 different species) which may be isolated from subgingival plaque were tested for their in vitro susceptibility to phenoxycthanol, a commonly-used antiseptic and preservative . Ninety-five percent of the strains, including those associated with chronic inflammatory periodontal disease, were susceptible to concentrations of phenoxyethanol used topically (2% w/v) . Phenoxyethanol at a concentration of 1% (w/v) was also found that to have a rapid bactericidal effect achieving a 99.9% kill in 5 minutes or less for species such as Bacterodides gingivalis, Fusobacterium nucleatum, Eikenella corrodens, and Wolinella recta . Addition of chlorhexidine to phenoxyethanol resulted in a mixture with increased antibacterial activity . For most bacterial strains, the presence of chlorhexidine resulted in at least a four-fold decrease in the concentration of pheoxyethanol required for inhibition of growth . These results imply that phenoxyethanol may be useful in the treatment of chronic inflammatory periodontal disease either by itself or in combination with chlorhexidine.

Biochem Pharmacol, 1990 Aug 1, 40(3), 431 - 6
Relevance of ionic effects on norfloxacin uptake by Escherichia coli; Valisena S et al.; The uptake of the quinolone drug norfloxacin by Escherichia coli was investigated at initial rate kinetics at different pH and monovalent/divalent metal ion concentration . The results support a simple diffusion mechanism for quinolone incorporation into cells . The uptake process decreases under acidic conditions . The presence of Na+ or K+ ions does not affect the results to an appreciable extent, whereas divalent ions cause a dramatic decrease in drug incorporation . The antibacterial activity, evaluated under identical experimental conditions, shows a direct relationship with the uptake data . As a general explanation for the above results it is suggested that the ability of the drug to penetrate into cells is a function of its net charge . The molecule in the zwitterionic form exhibits maximum permeation properties, whereas the uptake is remarkably reduced when the drug bears a net charge as a result of ionization or complex formation with bivalent ions . These results allow further insight into the mechanism of quinolone access to the intracellular compartment.

Vestn Khir Im I I Grek, 1990 Aug, 145(8), 20 - 2
{Lysosomal-cation test in the control of treatment of acute proctological diseases}; Minchin SIu et al.; An express evaluation of the functional state of neutrophil granulocytes by the indications of the lysosomal-cationic test are thought to be a necessary addition to routine clinico-laboratory methods of assessment of the wound process in patient with the suppurating epithelial coccygeal canal and acute paraproctitis . Use of cytochemical indices allow the antibacterial therapy to be optimized in patients with suppurating epithelial coccygeal canal and thus substantially decrease the amount of complications in the postoperative period.

Ther Umsch, 1990 Aug, 47(8), 670 - 4
{Acne and its drug treatment}; Buchner SA; The most common disease of the pilosebaceous follicle is acne vulgaris . The primary detectable pathologic defect in acne is abnormal keratinization of the follicular epithelium, resulting in a retention hyperkeratosis . The primary lesion produced by this process, the comedo, ist the precursor of most other acne lesions . These include inflammatory papules, pustules and nodules . Treatment principles are directed against known pathogenic factors . The major topical modalities that are currently being used include tretinoin, benzoyl peroxide and topical antibiotics . Benzoyl peroxide is a powerful antibacterial agent . Topical erythromycin and clindamycin appear to have equivalent efficacy . A major treatment advance has been heralded by the use of oral 13-cis retinoic acid (isotretinoin) in the management of patients with severe nodulocystic acne, acne conglobata and acne fulminans . Isotretinoin is teratogenic and should not be given to women of childbearing age.

Chem Pharm Bull (Tokyo), 1990 Aug, 38(8), 2271 - 3
Synthetic cephalosporins . VI . Synthesis and antibacterial activity of 7-{(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methyl) ethoxyiminoacetamido}- 3-(3-hydroxy-4-pyridon-1-yl)methyl-3-cephem-4-carboxylic acid and related compounds; Sakagami K et al.; Synthesis and antibacterial activity of 7-{(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methyl)ethoxyimin oacetamido}- 3-(3-hydroxy-4-pyridon-1-yl)-3-cephem-4-carboxylic acid (12) and its related compounds are described . Compound 12 exhibited excellent antibacterial activity against gram-negative bacteria, and its anti-pseudomonal activity was ten to fifteen times greater than that of ceftazidime.

Chem Pharm Bull (Tokyo), 1990 Aug, 38(8), 2190 - 6
Synthesis of 7-thio-substituted 4-oxoquinoline-3-carboxylic acids with antibacterial activity; Nishimura Y et al.; A series of C-7 thio-substituted 1-cyclopropyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids were prepared and tested for their antibacterial activity . Structure-activity relationships associated with the C-5 and C-7 substituents were discussed . Among the C-7 substituents including alkylthio, arylthio, heteroarylthio, and cyclic aminothio groups, a 2-aminoethylthio group was the best for enhancing in vitro antibacterial activity . The C-5 variants increased activity in the order OH less than F less than H less than NH2 . Of compounds prepared in this work, 5-amino-7-(2-aminoethyl)thio-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4 -oxo-quinoline-3-carboxylic acid (18) was the most active.

J Antibiot (Tokyo), 1990 Aug, 43(8), 931 - 7
MM 47761 and MM 49721, glycopeptide antibiotics produced by a new strain of Amycolatopsis orientalis . Isolation, purification and structure determination; Box SJ et al.; Two glycopeptide antibiotics MM 47761 and MM 47921 have been isolated from Amycolatopsis orientalis NCIB 12608 . Fermentation conditions for their production, and methods for their isolation are described . The metabolites have been characterised by physio-chemical and biological properties and the structure determined by a combination of chemical degradation, COSY and NOE NMR studies . Both metabolites showed good antibacterial activity against Gram-positive organisms.

Vet Rec, 1990 Jul 28, 127(4), 86 - 90
Bovine endometritis: comparative efficacy of alfaprostol and intrauterine therapies, and other factors influencing clinical success; Murray RD et al.; A comparative study of the treatment of 306 severe, moderate, or mild cases of bovine endometritis was carried out over two calving seasons . The cases were treated with alfaprostol, or an intrauterine antibacterial preparation, or with a combination of both therapies . There was no significant difference between the efficacies of these treatments, and a single injection of alfaprostol was effective in 74 per cent of the cases treated . The effectiveness of the treatments was related to the degree of self-cure of the endometritis after parturition, the luteal activity at the time of treatment, and farm management factors affecting the health and condition of the calving cows.

Cas Lek Cesk, 1990 Jul 20, 129(29), 914 - 6
{Dual cephalosporins--a return of fixed combinations of antibiotics?}; Krcmery V Sr; The author submits information on the preparation and properties of new molecules of "tailored antibiotics"--dual cephalosporins . They are formed by esterification of cephalosporins of the third generation (so far only cephotaxim) with fleroxacine or another fluoroquinolone chemotherapeutic agent . The author discusses the aptness and advantage of this new approach to the innovation of the existing spectrum of antibacterial agents.

J Biol Chem, 1990 Jul 5, 265(19), 11333 - 7
A potent antibacterial protein in royal jelly . Purification and determination of the primary structure of royalisin; Fujiwara S et al.; A new potent antibacterial protein, for which we propose the name royalisin, was found in royal jelly of the honeybee Apis mellifera L . and purified to homogeneity for the first time by acid extraction, gel filtration, and reverse-phase high pressure liquid chromatography . The primary structure of royalisin was determined to consist of 51 residues, with three intramolecular disulfide linkages, having a calculated molecular mass of 5523 Da . Royalisin is an amphipathic protein, with the C-terminal half of the molecule being rich in charged amino acids; and it showed extensive sequence homology to two other antibacterial proteins, sapecin from embryonic Sarcophaga peregrina cells and phormicins from Phormia terranovae larvae . Royalisin was found to have potent antibacterial activity against Gram-positive bacteria at low concentrations, but not against Gram-negative bacteria . Royalisin may be involved in a defense system active against bacterial invasion of the honeybee.

Br J Clin Pharmacol, 1990 Jul, 30(1), 1 - 11
Screening for aminoglycoside auditory toxicity in the old; Cheung R et al.; 1 . We have investigated 22 patients receiving gentamicin, mean (s.d.) age 78 (6) years for auditory toxicity, using a standard audiometric technique in a sound-treated room (Study 1) . 2 . Use of a portable audiometer might allow a larger and more representative proportion of patients treated with aminoglycosides to be screened for ototoxicity . A method for detecting high frequency loss suitable for use in the ward was evaluated in 12 volunteers aged 27 (4) years (Study 2) . 3 . The error inherent in taking hearing at the start of treatment as a reference point was measured in 16 patients, aged 81 (8) years, prescribed non-ototoxic antibacterials (Study 3) . 4 . A significant (P = 0.05) reduction in hearing threshold was detected in Study 1, although psychometric tests revealed unchanged or improved ability to co-operate . This occurred only at 4000 Hz, the highest frequency used . The magnitude of this loss, mean 2.5 dB, was similar to that of the improvement in threshold detected (P = 0.0004) early in the course of treatment in Study 3 . Thus, underestimation of ototoxicity is likely . 5 . If a change of threshold of 10 dB or more is taken arbitrarily to represent a real change in hearing, then there was a significant excess of patients in Study 1 with losses at 4000 Hz only (P = 0.032) . The six with such losses at this frequency were older than the rest . However, there was a significant (P less than 0.02) positive correlation between log mean predose serum gentamicin concentration and age . Thus, it remains to be determined whether presbyacusis sensitizes those hair cells which it does not destroy to toxic damage . 6 . The cumulative dose of gentamicin (for a course of the duration given) was calculated according to published prescribing aids . There was no systematic reduction in the ratio of the dose recommended by a given aid to the dose prescribed in the six with hearing losses as defined above . 7 . In Study 2, thresholds obtained at 6000 Hz in the open ward were, on average, 0.9 dB higher than in the sound treated room, but the effect of venue did not reach statistical significance . In the morning thresholds were marginally, but significantly (P = 0.04), lower than in the afternoon . Precision, as measured by the standard deviation of replicate determination, was independent of test conditions . Using multiple (ten) threshold determinations appeared to improve resolution.(ABSTRACT TRUNCATED AT 400 WORDS)

J Periodontol, 1990 Jul, 61(7), 393 - 8
A new degradable controlled release device for treatment of periodontal disease: in vitro release study; Steinberg D et al.; The substantivity of a drug in the periodontal pocket is an important factor determining its effect on the subgingival flora . Therefore, one of the predominant factors in the development of a sustained release delivery device is the ability to control the rate of release of the drug . Previous studies have demonstrated the advantages of the local sustained release of chlorhexidine from nondegradable devices in the treatment of periodontal diseases . The aim of this study was to develop a degradable sustained release device composed of a cross-linked protein containing chlorhexidine as the therapeutic agent . The in vitro release profile of chlorhexidine from the degradable films was altered by the amount of chlorhexidine incorporated into the film, by the cross-link density of the polymer, and by the chlorhexidine salt used . The chlorhexidine in the final pharmaceutical preparation did not lose its antibacterial activity as was shown in an in vitro antibacterial test . This work demonstrates that the release of chlorhexidine from a degradable delivery system and the degradation of the matrix can be controlled by variation in the formulation . This presents a new dental drug delivery system that can be used as an adjunct in the treatment of periodontal diseases in the future . These studies enable us to choose the pharmaceutical formulations for clinical trials to be conducted testing the efficacy of this treatment modality.

J Antibiot (Tokyo), 1990 Jul, 43(7), 858 - 72
Amikacin analogs with a fluorinated amino acid side chain; Hoshi H et al.; The synthesis and biological activity of kanamycin A derivatives with an omega-amino-alpha-fluoroalkanoyl side chain on the 1-amino group are described . The fluorinated amino acids (4) for the side chain were prepared by fluorination of the alpha-hydroxy esters (2) with diethylaminosulfur trifluoride (DAST) with accompanying the Walden inversion . The reaction products varied with the amino protective groups employed, chain length of the alkanoic acids and the presence or absence of base . The fluorinated side chain was introduced to 1-free-NH2 kanamycin A (12) by the conventional active ester method and subsequent deblocking reactions afforded the desired final products (13-17) . Of the derivatives prepared, 1-N-{(S)-4-amino-2-fluorobutyryl}kanamycin A (2'''-deoxy-2'''-fluoroamikacin, 14) showed the best overall activity profile, nearly the same as that of amikacin . Preparation and antibacterial activity of several aminoglycoside antibiotics with the 1-N-(S)-4-amino-2-fluorobutyryl side chain are also discussed.

Antibiot Khimioter, 1990 Jul, 35(7), 25 - 7
{Physiologic model of NY-198 pharmacokinetics using a new method of determining tissue/blood distribution coefficient}; Manuilov KK; A 10-compartment physiological model of pharmacokinetics of NY-198, a new pyridone carboxylic acid, with antibacterial activity is described . In its construction an original rapid method based on measuring xenobiotic concentration in one particular time point was used for determining the tissue/blood distribution coefficients . The results of simulating the antibiotic pharmacokinetic profiles by the Kd values known from the literature and the values estimated with the proposed method were compared.

Stomatologiia (Mosk), 1990 Jul-Aug, (4), 29 - 33
{The pathogenetic aspects of the effect of hypoxia on the trigger mechanisms of suppurative-inflammatory complications in patients with combined maxillofacial and craniocerebral trauma}; Zuev VP et al.; Study of the relationship between the time course of secondary tissue hypoxia development and changes in the neutrophilic phagocytic activity, which was carried out in 65 patients with combined maxillofacial and craniocerebral injury, has revealed a detrimental effect of hypoxia on antibacterial defense factors of the body, this effect being conductive to development of pyoinflammatory complications; this should be borne in mind when planning treatment strategy.

Hinyokika Kiyo, 1990 Jul, 36(7), 801 - 6
{Clinical studies on chronic prostatitis and prostatitis-like syndrome (4) . The kampo treatment for intractable prostatitis}; Ikeuchi T; Kampo treatment was attempted in cases of chronic nonbacterial prostatitis and prostatitis-like syndrome which was intractable or recurred when treated with western medicine . The clinical effects of Kampo treatment were excellent in 21.3% with an efficacy rate of 67.2% for the cases with chronic non-bacterial prostatitis, and excellent in 19.5% with an efficacy rate of 52.4% in the cases with prostatitis-like syndrome . When the clinical effects were compared with those of western therapy performed in the cases which had recurrence, Kampo treatment showed more excellent effects (p less than 0.1) for both types of disease, and the treatment with Chinese medicine was suggested useful . In a comparison of the effects between the cases given only Kampo treatment and those given both Kampo treatment and western treatment using anti-inflammatory agents, no difference was seen in the cases with the prostatitis-like syndrome, but in the cases with chronic non-bacterial prostatitis, the effects were better in the concomitant treatment group than in the group given only Kampo treatment (p less than 0.1) . The response to the Kampo treatment differed depending on the type of disease . Among the antibacterial agents used concomitantly in the cases of chronic non-bacterial prostatitis, new-quinolones showed better results than ST compounds or tetracyclines, but no statistically significant differences were seen among the drugs . Of the Kampo drugs used, Keisibukuryogan and Simotuto showed high clinical usefulness in both types of disease and there was no statistically significant difference among the other drugs . The incidence rate of side effects (Goji) due to Kampo treatment was 6.3% and was higher in patients administered Keisibukuryogan.

Khirurgiia (Mosk), 1990 Jul, (7), 50 - 6
{Pathogenetic aspects of the treatment of diffuse suppurative peritonitis}; Lutsevich OE et al.; Experience with the treatment of 130 patients with generalized purulent peritonitis is analysed . The complex of therapeutic measures included intraoperative cleansing of abdominal cavity with ultrasound; postoperative prolonged laparoscopic cleansing with the use of rational antibacterial therapy and laser irradiation of the abdominal cavity . The cell immunity values in patients with peritonitis were studied and the principles of immunocorrective therapy substantiated . It is shown that detoxification measures are necessary in the treatment of this category of patients . A complex approach to the treatment of purulent peritonitis led to a decrease in mortality to 13.8%.

Eur J Clin Microbiol Infect Dis, 1990 Jul, 9(7), 510 - 6
Significance of tissue levels for prediction of antibiotic efficacy and determination of dosage; Carbon C; Determination of tissue levels is widely thought to provide useful information in the investigation of a new antibiotic, however this assumption is not fully justified . In this paper the following questions are covered . Firstly, the methodological problems encountered in the measurement of antibiotic levels in solid tissues and extravascular fluids are described . Secondly, the difficulties encountered in interpreting tissue concentrations are discussed, given the heterogeneity of distribution of drugs, potential intracellular penetration, binding to tissue proteins and local factors reducing antibacterial activity . Thirdly, the respective importance of animal and human data on tissue levels for prediction of efficacy is analysed . In some animal models it is possible to study the conditions affecting antibacterial activity and to obtain data relevant to the clinical situation . However, the inoculum effect, the metabolism of bacteria, the mechanism of the bactericidal action of drugs and the type of infected tissue are important factors to be taken into account . In humans, data obtained from infected tissue is sparse and contributes little to knowledge . Knowledge of tissue levels may be important for establishing whether data obtained in animals can be applied to humans or not . Fourthly, the importance of tissue levels in determining antibiotic dosages is evaluated . In humans, tissue levels are of limited value in the determination of unitary dose and dosage intervals in relation to the clinical response . Trough serum levels of free drug, half-life at the beta-phase and rate of in vitro killing are the most important parameters to be considered . Their relative importance depends mainly on the mode of action of the drug.(ABSTRACT TRUNCATED AT 250 WORDS)

Eur J Clin Microbiol Infect Dis, 1990 Jul, 9(7), 479 - 87
Correlation between pharmacokinetics, pharmacodynamics and efficacy of antibacterial agents in animal models; Dalhoff A et al.; On the basis of a review of published literature it is demonstrated that pharmacokinetic parameters of antibacterial agents correlate well with therapeutic efficacy in animal models, provided pharmacodynamic parameters are taken into account . The time that serum levels exceed the MIC is the most significant parameter determining efficacy of beta-lactams, whereas the efficacy of aminoglycosides is dependent on serum concentrations and the area under the curve . The efficacy of quinolones tends to be correlated to the doses administered or drug levels achieved . However, specific pharmacodynamic properties contribute significantly to the therapeutic efficacy of a few quinolones only whereas other quinolones lack these specific pharmacodynamic attributes . Thus, the correlation of pharmacokinetic parameters with therapeutic efficacy provides important basic concepts for the design of preclinical and clinical studies in the course of which additional pharmacodynamic properties will become apparent.

Transpl Int, 1990 Jul, 3(2), 113 - 5
Disseminated tuberculosis after renal transplantation . A report of two cases; Schorn TF et al.; Disseminated mycobacterial infections occurred in two female renal graft recipients late after transplantation . In the first patient, initially presenting with fever, diagnosis was made at autopsy . Temporary defervescence following antibiotic therapy with ofloxacin possibly contributed to the fatal diagnostic delay . In the second case, body temperature was normal throughout the protracted course of the patient's illness . Her presenting symptom was rapidly increasing ascites, attributed initially to chronic liver disease . These cases demonstrate that tuberculosis remains a serious complication after renal transplantation, in particular due to its sometimes atypical clinical manifestations . Response to antibacterial therapy has to be critically evaluated in order to avoid fatal diagnostic delay.

J Antibiot (Tokyo), 1990 Jul, 43(7), 847 - 57
Synthesis and antibacterial activity of C-2 carboxyethenylthio-carbapenem derivatives; Basker MJ et al.; A number of C-2 carboxyethenylthio-carbapenem derivatives possessing either the (5R,6R,8S)- or the (5R,6S,8R)-stereochemistries have been prepared from the olivanic acids MM 22382 (1) and MM 22383 (4), respectively . Their in vitro antibacterial activities and stabilities to human kidney homogenate are superior to those of the parent compounds, particularly in the latter series.

Br J Ophthalmol, 1990 Jul, 74(7), 433 - 6
Endogenous Nocardia asteroides endophthalmitis in a patient with systemic lupus erythematosus; Ishibashi Y et al.; We report a case of endogenous Nocardia endophthalmitis in a patient with systemic lupus erythematosus (SLE) . He developed a parafoveal lesion in the right fundus while on systemic corticosteroid and antibiotic treatment . Initially we suspected a fungal origin and treated him with antifungal drugs . The intraocular disease progressed without improvement and advanced to the vitreous cavity . Nocardia asteroides was found in a specimen obtained at pars plana vitrectomy and was also cultured from the same specimen . The intraocular infection was controlled by antibacterial drugs, though the visual acuity of the right eye was reduced to only light perception owing to heavy vitreous opacity and secondary cataract . This case is the first report of endogenous Nocardia endophthalmitis in Japan and also the first case of this disease reported from outside the United States of America.

Med Clin North Am, 1990 Jul, 74(4), 1025 - 37
Medical and surgical complications of renal transplantation: diagnosis and management; Yoshimura N et al.; Renal transplantation is a common modality of therapy in end-stage renal failure, but it has the potential of developing many complications, both surgical and medical in nature . In transplantation surgery, more than in any other type of surgery, prevention of these complications is essential . This includes attention to many details, including optimum organ salvage, preservation, implantation, and postoperative care . Although infection has decreased in frequency and severity with the advent of antiviral and antibacterial agents, prevention, early diagnosis, and suitable treatment with appropriate antibiotic(s) will be necessary to obtain desirable results and to reduce morbidity and mortality . It should be stressed that although careful attention to the patients and adjustment of the immunosuppressive regimen may mitigate much of the gastrointestinal, hematologic, and osteogenic complications, high incidence of cancer of the skin and mucous membrane continues.

Pediatr Rev, 1990 Jul, 12(1), 15 - 21
Peptic ulcer disease in children; Gryboski JD; Chronic gastroduodenal ulceration is the end product of an imbalance between acid levels, peptic hostile factors, and mucosal defenses . This condition differs significantly from stress ulceration, in which the primary factor is decreased mucosal blood flow, and from nonsteroidal anti-inflammatory drug-induced injury, in which there is local vascular injury and inhibition of prostaglandin synthesis . The identification of H pylori as a cause of chronic gastritis, duodenitis, and peptic ulcer is required for specific antibacterial therapy.

J Biochem (Tokyo), 1990 Jul, 108(1), 128 - 32
Mode of action of sapecin, a novel antibacterial protein of Sarcophaga peregrina (flesh fly); Matsuyama K et al.; Sapecin is an antibacterial protein purified from the culture medium of NIH-Sape-4, an embryonic cell line of Sarcophaga peregrina {Matsuyama, K . & Natori, S . (1988) J . Biol . Chem . 236, 17112-17116} . As this protein inhibited the growth of Gram-positive bacteria better than that of Gram-negative bacteria, we studied its mode of action with special reference to its effects on S . aureus and Escherichia coli . Results showed that sapecin had high affinity for cardiolipin, which is a major phospholipid of S . aureus . Moreover, a mutant of E . coli with a defect in cardiolipin synthesis was more resistant to sapecin than wild type E . coli, suggesting that cardiolipin is a target for sapecin . Lipopolysaccharide of E . coli was also found to be a barrier for the antibacterial activity of sapecin.

J Med Chem, 1990 Jul, 33(7), 2012 - 5
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo{3,2-a}{1,8}naphthyridinecarboxylic acids; Kondo H et al.; It is known that thiazolo{3,2-a}{1,8}naphthyridine derivatives (3a) exhibit good antibacterial activity . Accordingly, several analogues of 3a, viz . oxazolo- and imidazolo{3,2-a}{1,8}naphthyridine derivatives 3b and 3c, were synthesized and evaluated for antibacterial activity in vitro and for inhibitory activity against DNA gyrase of Escherichia coli K-12 C600 . Compound 3a exhibited antibacterial activity comparable to that of ofloxacin and enoxacin against Gram-positive and Gram-negative bacteria and displayed antibacterial activity superior to that of 3b and 3c . The antibacterial activities of 3b and 3c decreased in that order . DNA gyrase inhibitory activities of 3a-c in E . coli K-12 C600 paralleled their in vitro antibacterial activity . It was found that enhancement of the DNA gyrase inhibitory activity of 3a was dependent on a certain feature of the sulfur atom of the thiazole ring.

Antibiot Khimioter, 1990 Jul, 35(7), 44 - 7
{Optimal control of the microflora environment in suppurative foci}; Menshikov DD et al.; The informative capacity of various statistic parameters characterizing the ecology of pathogens of purulent processes was studied . Many-years' results of the routine bacteriological tests of the materials from purulent wounds in patients from surgical, traumatological and burn departments served as the study subjects . The frequency, persistence and contamination capacity of the pathogens were investigated . Data on the changes in the frequency parameter with respect to the main pathogens of wound infections in various contingents of patients were collected . In relation to the observation period and contingent of the patients, various microorganisms were found to be permanent, supplementary and casual . The use of the ecological parameters was shown to provide integrated information on the etiological role of the pathogens in the development of purulent processes . The information characterized the microbial properties which should be considered in planning the use of antibacterial drugs and estimating the efficacy of the epidemiological control.

In Vivo, 1990 Jul-Aug, 4(4), 221 - 3
Lignified materials as potential medicinal resources . II . Prevention of pathogenic bacterial infections in mice; Oh-Hara T et al.; Antibacterial activity was demonstrated when ddY mice were intraperitoneally infected with E . coli or P . aeruginosa two days after a single ip-injection of a hot-water or alkaline extract obtained from lignified materials, such as chips of slash pine, Douglas fir, tallow wood, and two shelf fungi . Lignified material is a promising medicinal resource for the prevention and/or treatment of pathogenic microbial infection.

Quintessence Int, 1990 Jul, 21(7), 589 - 98
Apexification: review of the literature; Morse DR et al.; Five methods for the treatment of teeth with an incompletely formed apex (open apex) and a necrotic pulp are discussed . The methods discussed include the use of (1) a customized cone (blunt-end, rolled cone); (2) a short-fill technique; (3) periapical surgery (with or without a retrograde seal); (4) apexification (apical closure induction); and (5) one-visit apexification . The apexification techniques, which use various formulations of calcium hydroxide to induce closure, are stressed . Based on the review of the literature and clinical experience of the authors, it was concluded that successful treatment of an immature pulpless tooth can partly result from the antibacterial and calcification-inducing action of calcium hydroxide.

Mol Pharmacol, 1990 Jul, 38(1), 20 - 5
Inhibition of human immunodeficiency virus-1 reverse transcriptase activity by rubromycins: competitive interaction at the template.primer site; Goldman ME et al.; Rubromycins, a class of quinone antibacterials, were discovered to selectively inhibit human immunodeficiency virus-1 (HIV-1) RNA-directed DNA polymerase (reverse transcriptase) (RT) activity more potently than cellular DNA polymerase alpha . beta- and gamma-rubromycin each inhibited equipotently HIV-1 RT and avian myeloblastosis virus RT, in a concentration-dependent manner, and were significantly weaker as inhibitors of calf thymus DNA polymerase alpha . These agents inhibited HIV-1 RT reversibly, were competitive with respect to template.primer, and were noncompetitive with respect to TTP . Dixon analyses yielded HIV RT Ki values of 0.27 +/- 0.014 and 0.13 +/- 0.012 microM for beta- and gamma-rubromycin, respectively . Similarly, using DNA polymerase alpha, the Ki values were 25.1 +/- 4.3 and 3.9 +/- 0.6 microM for beta- and gamma-rubromycin, respectively . Because these agents were toxic to noninfected human T lymphoid cells using concentrations at or above 6 microM, HIV-1 infectivity studies were carried out at 0.8-6 microM . At these concentrations, which are below the range expected to provide protection, no significant antiviral activity was observed . Although beta- and gamma-rubromycins did not possess sufficient HIV RT inhibitory potency or selectivity versus mammalian DNA polymerase to demonstrate antiviral activities, these studies support the hypothesis that specific molecules containing quinone functional groups can selectively inhibit viral polymerase activities over cellular polymerase activities . In addition, these studies suggest that rubromycins may be lead structures for the development of more potent and selective agents.

Vet Rec, 1990 Jun 30, 126(26), 635 - 7
Cephalexin in ponies: a preliminary investigation; Lees P et al.; The administration of a single dose of the antibacterial agent cephalexin intramuscularly to six ponies at a dose rate of 7 mg/kg was well tolerated . No reactions at the injection site were apparent . It was absorbed rapidly and reached a mean peak plasma concentration of 6.77 micrograms/ml after a mean of 1.41 hours; plasma concentrations above 2.0 and 0.5 micrograms/ml were maintained for 3.8 and 9.8 hours, respectively.

J Biol Chem, 1990 Jun 25, 265(18), 10438 - 42
A synthetic 13-residue peptide corresponding to the hydrophobic region of bovine seminalplasmin has antibacterial activity and also causes lysis of red blood cells; Sitaram N et al.; Seminalplasmin (SPLN), a 47-residue peptide present in bovine seminal plasma, is one of the few proteins isolated from mammalian sources having potent antibacterial activity . SPLN also interacts with sperm acrosomal and plasma membranes . On the basis of analysis of the primary structure of SPLN with respect to its relative hydrophobicity and hydrophilicity, a region comprising of 13-amino acids, Pro-Lys-Leu-Leu-Glu-Thr-Phe-Leu-Ser-Lys-Trp-Ile-Gly, has been delineated . It is demonstrated that a synthetic peptide corresponding to this 13-residue region inhibits growth of Escherichia coli like SPLN and also has the ability to lyse red blood cells.

Ned Tijdschr Geneeskd, 1990 Jun 23, 134(25), 1227 - 9
{Inefficacy of oral contraception during use of minocycline}; de Groot AC et al.; A healthy woman aged 21 years who used the oral contraceptive Trigynon became pregnant while being treated with Minocin (minocycline; 100 mg per day) for acne conglobata . While the risk of use of antibiotics such as this one reducing the efficacy of oral contraceptives is small, patients should nevertheless be informed that the risk existsPIP: A 21-year old woman using an oral contraceptive, the combination preparation Trigynon containing levonorgestrel (LNG) and ethinyl estradiol (EE), since June 1987 had experienced pain in the groin . In September 1988 she had a single occurrence of bleeding, a sign of lessened effectiveness of the OC . She was treated with 50 mg of minocycline/day as of April 1989, and for inguinal acne conglobata with locally applied clindamycine (10 mg/ml of clindamycine hydrochloride lotion) . She switched to another OC, and the next month timely, normal menstruation ensued . A few days later the dose of minocycline was raised to 100 mg/day . Subsequently she had a regular breakthrough bleeding followed by a missed cycle and a positive pregnancy test . There have been several recent reports about the interaction between antibiotics and OCs (breakthrough bleeding and contraceptive failure) . Rifampicin and griseofulvin are known to reduce the activity of OCs via induction of liver enzymes . Between 1968-84 there was a total of 62 failures of OCs (15 using OCs with 50 mcg of EE) reported in the UK . The suspected cause was the combined use with antibiotics (70% penicillin and tetracycline) . In the Netherlands 6 cases of possible interactions were reported during 1980-86: 2 cases caused by nitrofurantoin and/or trimethoprim, and 1 case by sulfamethoxazol with trimethoprim . The interference of minocycline with the intestinal flora can occur as 34% of it is excreted in feces, and its antibacterial spectrum corresponds to that of tetracycline hydrochloride (reduction of beta-glucuronidase in the feces) . The failure of Trigynon cannot be irrefutable ascribed to minocycline as unintended pregnancy also occurs while using OCs without antibiotics . Clindamycine could have also influenced the intestinal flora percutaneously .

Hosp Pract (Off Ed), 1990 Jun 15, 25(6), 181 - 94
Antibacterial therapy: problems and promises, Part II; Neu HC; Numerous antibacterial agents recently or soon to be available are reviewed: new quinolones, macrolides, aminoglycosides, glycopeptides, and lipopeptides . Overall, these agents do much to improve antibacterial activity against problem organisms, overcome resistance, and reduce toxicity and frequency of administration . Many are orally administered and will shorten hospital stays.

Antibiot Khimioter, 1990 Jun, 35(6), 34 - 7
{Increasing the effectiveness of ampicillin in combination with lysozyme}; Shcherbakova EG et al.; The effect of lysozyme (2 mg/kg) on pharmacokinetics of ampicillin (60 mg/kg) and the lymph nodes was studied in a model of experimental diffuse peritonitis in 52 dogs . The drugs were administered intramuscularly in single doses simultaneously with simulation of the pathological process . Under such conditions, lysozyme promoted an increase in the ampicillin concentration in the lymphatic system, blood and tissues and prolonged the antibacterial activity to 18 hours of the experiment . This resulted in retarding lympho- and hematogenic dissemination of the infection from the primary focus and lowered the infectious and toxic affection of the regional lymph nodes, thus securing their barrier and immunological function . With lysozyme used in combination with the antibiotic the immunomorphological zones of the lymph nodes appeared to be preserved and the volumetric proportion of macrophages increased . Then the volumetric proportion of the blast cells and the frequency of macrophagal and lymphocytic interactions also increased . The most pronounced cell interactions were observed in the distal (tracheobronchial) lymph nodes whose functions before the infection generalization were mainly immunological.

Antimicrob Agents Chemother, 1990 Jun, 34(6), 1160 - 4
Pharmacokinetics of cephem antibiotics in exudate of pelvic retroperitoneal space after radical hysterectomy and pelvic lymphadenectomy; Ito K et al.; Many cephalosporin antibiotics have recently been invented and attempts have been made to use them clinically . The choice of which of these drugs should be used has been difficult in gynecology . The efficacies of these drugs depend on their antibacterial spectra, potencies, and concentrations in tissues . This study was designed to investigate the pharmacokinetics of various cephem antibiotics in the exudate of the retroperitoneal space that is formed after radical hysterectomy and pelvic lymphadenectomy . These cephem antibiotics were cefoxitin, cefotiam, cefotetan, cefpiramide, cefminox, cefotaxime, ceftizoxime, cefoperazone, cefmenoxime, cefbuperazone, ceftazidime, cefpimizole, flomoxef, and cefuzonam . The maximum concentrations after administration of a 1-g dose in the exudate of the pelvic retroperitoneal space were 37.9 micrograms/ml with cefminox, 30.3 micrograms/ml with cefpimizole, 21.6 micrograms/ml with flomoxef, 21.5 micrograms/ml with ceftazidime, and 17.6 micrograms/ml with cefbuperazone, which were relatively high . When selecting antibiotics for prophylactic use against infections in the retroperitoneal space after radical hysterectomy and pelvic lymphadenectomy, on the basis of drug transfer, flomoxef, cefminox, cefbuperazone, ceftazidime, and cefpimizole were considered to be the drugs of first choice at a dose of 1 g.

Analyst, 1990 Jun, 115(6), 797 - 9
Determination of antibacterial agents in microbiological cultures by high-performance liquid chromatography; Taylor RB et al.; A general high-performance liquid chromatographic (HPLC) procedure is described which allows the assay of several antibacterial drugs in combination in a matrix of bacterial cell cultures . The drugs assayed were dibromopropamidine, trimethoprim, sulphadiazine and sulphamerazine . It is also shown that p-aminobenzoic acid, which is an essential metabolite of many micro-organisms, does not interfere and can itself be quantified . The method uses solid-phase extraction on a cyclohexyl-bonded silica with subsequent separation of the analytes by reversed-phase HPLC . Tetrabutylammonium is used in order to reduce the retention of trimethoprim and dibromopropamidine and quantification is by ultraviolet detection at 254 nm . The analytical characteristics of the proposed method are shown for certain drug combinations.

J Chemother, 1990 Jun, 2(3), 167 - 70
In-vitro sensitivity of amoxicillin/clavulanic acid (Augmentin) to isolated beta-lactamases and in-vitro antibacterial activity; Esposito S et al.; The in vitro sensitivity of amoxicillin alone and combined with clavulanic acid (ratio 4:1) as been studied by a spectrophotometric method utilizing crude extract of the following enzymes: TEM1, TEM2, SHV1, SHV2, TLE1, HMS1, LXA, P99, ENT208 . The in-vitro antibacterial activity of ampicillin, amoxicillin alone and associated with clavulanic acid was also determined by an agar dilution method . Clavulanate protects amoxicillin from the hydrolytic activity of plasmid mediated beta-lactamase, conferring a stability on the beta-lactam comparable with that of cefotaxime . The protection of amoxicillin by means of clavulanic acid reduces the minimal concentration of antibiotic necessary to inhibit most bacterial species and allows bacteria to remain sensitive to the drug which might otherwise be resistant.

J Antibiot (Tokyo), 1990 Jun, 43(6), 594 - 600
A54145, a new lipopeptide antibiotic complex: isolation and characterization; Fukuda DS et al.; A54145 is a complex of acidic lipopeptide antibiotics which are produced by Streptomyces fradiae and are active against Gram-positive bacteria . The A54145 complex was isolated by adsorption on Diaion HP-20 nonfunctionalized macroreticular resin and/or ion exchange on Amberlite IRA-68 anion exchange resin . Antibacterial factors A, A1, B, B1, C, D, E, and F were obtained in purified form by repeated preparative reverse phase HPLC on C8 and/or C18 bonded-phase supports . The molecular formulae of the factors are C72H109N17O27 (factors A and A1), C73H111N17O27 (factors B, B1, C, and D), C74H113N17O27 (factor E), and C71H107N17O27 (factor F) . The identities of the acyl side chains were established as 8-methylnonanoyl (factors F, A, and B1), n-decanoyl (factors A1 and B), and 8-methyldecanoyl (factors C, D, and E).

J Pediatr Surg, 1990 Jun, 25(6), 669 - 71
The role of videourodynamic studies in diagnosis and treatment of vesicoureteral reflux; Scholtmeijer RJ et al.; From January 1986 to January 1988, 63 children with 95 refluxing ureters have been studied in a prospective study with videourodynamic examination . All children with reflux grades I, II, and III received antibacterial treatment . Surgical treatment was adopted for reflux grades IV and V, provided detrusor instability had been excluded . However, if there was detrusor instability, anticholinergic drugs and antibacterial treatment were given in all grades of reflux and videourodynamic examination was repeated after 3 to 6 months and after 12 months of therapy . Bilateral reflux was found in 22 of 38 patients with a stable bladder, and reimplantation was performed in 11 patients with 18 refluxing ureters . In 25 children with 35 refluxing ureters of various grades of reflux, detrusor instability was found and unilateral reflux was noted more frequently than bilateral reflux . Surgery was necessary for only five children, because in the majority of the patients detrusor instability and reflux could be treated by anticholinergic drugs and antibacterial treatment . For the decision as to which treatment should be given in vesicoureteral reflux, a videourodynamic study is mandatory.

J Med Chem, 1990 Jun, 33(6), 1645 - 56
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency; Miyamoto T et al.; A series of 5,7-disubstituted 1-cyclopropyl-6,8-difluoro-4(1H)-oxoquinoline-3-carboxylic acids (10-36) were prepared; the C-5 substituent in these compounds comprised halo, hydroxy, mercapto, and amino groups and the C-7 functional group included variously substituted piperazines . In vitro antibacterial screening results indicated that the amino group was optimal among the C-5 substituents . A combination of the C-5 amino group and the C-7 3,5-dimethylpiperazinyl appendage in this series conferred the best overall antibacterial property with lack of adverse drug interactions . Compound 36k {named sparfloxacin, originally AT-4140, 5-amino-1-cyclopropyl-6,8-difluoro-7-(cis-3,5-dimethyl-1-piperazinyl)- 4(1H)-oxoquinoline-3-carboxylic acid} was superior to ciprofloxacin in both in vitro and in vivo potency and hence was selected as a promising candidate for an improved therapeutic agent.

Semin Respir Infect, 1990 Jun, 5(2), 111 - 22
Invasive pulmonary aspergillosis in patients with neoplastic diseases; Walsh TJ; Invasive pulmonary aspergillosis is an important cause of morbidity and mortality in granulocytopenic patients . The purpose of this article is to review the current understanding of the microbiology, hospital epidemiology, clinical manifestations, diagnosis, prevention, and treatment of invasive pulmonary aspergillosis . Aspergillus conidia (spores) are inhaled from environmental sources into the paranasal sinuses and lower respiratory tract . Persistent fever, pulmonary infiltrates, and pleuritic pain in granulocytopenic patients receiving antibacterial antibiotics is a common manifestation of invasive pulmonary aspergillosis . Computerized tomographic scans of the chest often reveal characteristic peripheral nodules that also may progress to characteristic cavitary lesions . Hemoptysis may develop due either to hemorrhagic infarction during granulocytopenia or to the rupture of mycotic aneurysms during recovery from granulocytopenia . Aspergillus organisms may extend locally from the lung to involve other thoracic structures, including the heart and chest wall, and may disseminate to extrapulmonary sites, such as the brain, where focal neurological deficits ensue . Early diagnosis of invasive pulmonary aspergillosis may be difficult . Isolation of Aspergillus organisms from respiratory secretions of a persistently febrile granulocytopenic patient is usually indicative of invasive pulmonary aspergillosis and should not be dismissed as a contaminant or saprophyte . Amphotericin B is the treatment of choice; however, high dosages (1.0 to 1.5 mg/kg/day) are often necessary . Aspergillosis may develop in granulocytopenic patients who are already receiving empirical amphotericin B in lower doses (0.5 to 0.6 mg/kg/day) . It is hoped that further investigation directed toward an understanding of pathogenesis, improving diagnostic methodology, and developing new therapeutic and preventive strategies will improve the outcome of this life-threatening infection.

Rev Fr Endod, 1990 Jun, 9(2), 31 - 9
{In vitro evaluation of the antibacterial activity of endodontic drugs}; Lardinois ML et al.; The antibacterial activity of camphorated phenol, iodine-potassium iodide, aqueous 2% glutaraldehyde, Rockles 4, Cresophene and Terra-Cortril has been tested in vitro against 21 species of bacteria . After 2 minutes of contact between medication and bacteria, Rockles 4, Cresophene, IKI and camphorated phenol inhibited completely all the tested bacteria . Terra-Cortril and aqueous glutaraldehyde 2% even pures were ineffective against all the bacteria species . Only Cresophene remained effective against 4 bacteria species when diluated 100 times.

Chem Pharm Bull (Tokyo), 1990 Jun, 38(6), 1672 - 4
New fatty monoesters of erythromycin A; Philippe M et al.; New fatty polyenic (linoleic, linolenic, arachidonic, linoelaidic) mono esters of erythromycin A have been synthesized by using various reagents such as acyl chloride, carboxylic acid anhydride, and mixed carbonic anhydride . These different ways of activating the fatty acid allowed a regioselectivity of esterification at position 2' of the desosamine ring or position 4" of the cladinose ring of erythromycin A . The in vitro antibacterial properties of these new esters against members of the resident flora of the human skin were determined and compared with those of erythromycin A . The number and the stereochemistry of the double bonds seem to play a crucial role in the expression of the in vitro antibacterial activity.

Eur Respir J, 1990 Jun, 3(6), 725 - 7
The airways effects of inhaled chlorbutol in asthmatic subjects; Windom H et al.; Chlorbutol is an antibacterial and antifungal agent incorporated in terbutaline (Bricanyl) nebulizer solution . Ten stable atopic asthmatic subjects undertook bronchial challenge testing, according to a double-blind protocol . Patients inhaled doubling concentrations of either methacholine (0.13-4.0 mg.ml-1) or chlorbutol (0.16-5.0 mg.ml-1) for 2 min until the forced expiratory volume in one second (FEV1) had fallen by 20% from baseline . If this had not occurred following the administration of the final concentration, then this highest concentration was repeated for 4 min . The nine subjects completing the study had a geometric mean provocation concentration producing a 20% fall from baseline FEV1 (PC20) methacholine of 0.16 mg.ml-1 (range less than 0.125-0.475 mg.ml-1) . After inhalation of 2.5 mg.ml-1 chlorbutol one subject experienced a fall in FEV1 greater than 20% . In the remaining eight subjects, inhalation of chlorbutol did not affect airway calibre . We conclude that chlorbutol, in the concentration present in Bricanyl nebulizer solution, has no clinically significant effect on airway calibre.

Khirurgiia (Mosk), 1990 Jun, (6), 59 - 63
{Quantitative evaluation of humoral and cellular factors of antibacterial protection in patients with postoperative hernia complicated by suppurative process}; Usenov DA et al.; The article presents material on the study of the dynamics of humoral factors of the organism's antibacterial protection in correlation with factors of cellular immunity in 78 patients with postoperative ventral hernias complicated by a pyoinflammatory process . Factors of cellular immunity were studied in 33 patients, humoral factors of the organisms' antibacterial protection, in 45 patients . A distinct relation of the character of disorders of these factors to the type of the operation was revealed and their prognostic significance for clinical medicine was determined.

Hell Period Stomat Gnathopathoprosopike Cheir, 1990 Jun, 5(2), 53 - 8
{The use of prophylactic antibiotics in oral and maxillofacial surgery}; Antoniadis K et al.; Cultures of postoperative wounds after head and neck surgery reveal a variety of oropharyngeal anaerobic and aerobic flora, aerobic gram negative rods and fungi . Control clinical trials have shown that preoperative antibacterial prophylaxis reduces the incidence of postoperative wound infections . When an antibiotic is used prophylactically, it must be active against the micro-organisms known to cause the infection which the patient is supposed to be protected from . Antibacterial prophylaxis should begin just before the operation beginning, earlier is unnecessary and beginning later is less effective . It is indicated for a variety of surgical procedures that high risk of wound sepsis, superinfection and the emergence of resistance has not been shown to occur if antibacterial agents are used only "perioperatively".

Actual Odontostomatol (Paris), 1990 Jun, 44(170), 237 - 56
{Periodontal diseases and antibacterial drug treatment}; Huynh C et al.; Recent data concerning the bacteriology of periodontal diseases justify the use of antibacterial drugs . In advanced or resistant forms of the disease, the standard treatments are in fact insufficient . The antibacterial agents advocated include systemic antibiotics and local antiseptics . These products may be used separately or in combination . But, this antibacterial treatment remains a complementary option and cannot replace conventional treatments.

Proc Natl Acad Sci U S A, 1990 Jun, 87(12), 4761 - 5
All-D amino acid-containing channel-forming antibiotic peptides; Wade D et al.; The D enantiomers of three naturally occurring antibiotics--cecropin A, magainin 2 amide, and melittin--were synthesized . In addition, the D enantiomers of two synthetic chimeric cecropin-melittin hybrid peptides were prepared . Each D isomer was shown by circular dichroism to be a mirror image of the corresponding L isomer in several solvent mixtures . In 20% hexafluoro-2-propanol the peptides contained 43-75% alpha-helix . The all-D peptides were resistant to enzymatic degradation . The peptides produced single-channel conductances in planar lipid bilayers, and the D and L enantiomers caused equivalent amounts of electrical conductivity . All of the peptides were potent antibacterial agents against representative Gram-negative and Gram-positive species . The D and L enantiomers of each peptide pair were equally active, within experimental error . Sheep erythrocytes were lysed by both D- and L-melittin but not by either isomer of cecropin A, magainin 2 amide, or the hybrids cecropin A-(1-13)-melittin-(1-13)-NH2 or cecropin A-(1-8)-melittin-(1-18)-NH2 . The infectivity of the bloodstream form of the malaria parasite Plasmodium falciparum was also inhibited by the D and L hybrids . It is suggested that the mode of action of these peptides on the membranes of bacteria, erythrocytes, plasmodia, and artificial lipid bilayers may be similar and involves the formation of ion-channel pores spanning the membranes, but without specific interaction with chiral receptors or enzymes.

Minerva Chir, 1990 May 15, 45(9), 677 - 81
{The use of a topical antibacterial agent (silver sulfadiazine) on soft-tissue wounds}; Bocchiotti G et al.; Reducing the quantitative level of bacterial contamination in an open, acute or chronic, soft tissue wound below the critical level of 10(5) bacteria per gram of viable tissue is essential to delayed primary closure . First step in the management of the contaminated or infected wound is accurate local debridement, preferably with pulsating jet irrigation . Topical antibacterial agents, specifically silver sulfadiazine cream, are then usefully employed to reduce the bacterial count . Contrary to systemic antibiotics, these agents penetrate adequately into the open, granulating wound with a direct bacteriostatic or bactericidal action on a wide spectrum of gram positive and negative organisms, without the effect of local tissue injury typical of topical antiseptics . The use of topical antibacterials, traditionally confined to the treatment of the burn wound, the open "difficult" wound for excellence where control of local infection is first priority, provides a rapid local reduction of the bacterial level and paves the way to the final goal of primary delayed closure of the wound, either direct or with the use of grafts or local, distant, or free flaps.

Hosp Pract (Off Ed), 1990 May 15, 25(5), 63 - 74, 77-8
Antibacterial therapy: problems and promises, Part I; Neu HC; Agents approved for clinical use in the past five years and others most likely to be available in the near future are evaluated in this two-part review . This installment is devoted entirely to the beta-lactam antibiotics--penicillins, cephalosporins, monobactams, and carbapenems . There are more similarities than differences among them, but the variations give each agent a range of appropriate uses.

Cesk Farm, 1990 May, 39(3), 109 - 12
{Preparation of derivatives of 3-(3,4-dimethoxyphenyl)propanic acid and a study of its biological activity}; Novacek L et al.; From 3-(3,4-dimethoxyphenyl)propenic acid chloride and substituted amines and hydrazides, the appropriate amides and hydrazides (Table 1) were synthesized at 60-80 degrees C in the medium of benzene or toluene . The reaction of this chloride with benzaldehyde hydrazone at 70-80 degrees C yielded N,N'-bis{3-(3,4-dimethoxyphenyl)propenoyl}hydrazine (VIII) . At ambient temperature the benzylidene hydrazide of 3-(3,4-dimethoxyphenyl)propenic acid (VII) and a small amount of compound VIII were isolated . In the reaction of 3-(3,4-dimethoxyphenyl)propenic acid chloride with benzylidene hydrazide (VII) at 70-80 degrees C, compound VIII was obtained (Scheme 1) . Compounds I, VII, VIII and IX possessed higher indices of increase in fortnight tests of the first degree in the roosters of meat hybrides compared to the negative control, but the indices of conversion were unfavourable . The compounds did not reach the efficacy of the avoparcin standard . Derivatives II and VI possessed 67.5 and 63.5%, respectively, of anthelmintic activity of levamisol against Nippostrongylus brasiliensis . The prepared compounds were not antibacterially effective and they were not mutagenic in the tests following the method of Ames, either.

Klin Med (Mosk), 1990 May, 68(5), 77 - 81
{The first experience with using autologous macrophages in the complex treatment of patients with destructive pulmonary tuberculosis}; Chuchalin AG et al.; To correct local immunity, a suspension of autologous macrophages (AM) produced by culturing peripheral blood monocytes has been introduced in combined treatment of 15 patients with infiltrative, local disseminated, cavernous, fibrocavernous tuberculosis and tuberculoma (8, 1, 1, 4 and 1 case, respectively) . AM treatment was added to the standard antibacterial and pathogenetic therapy . AM were introduced into the subsegmental bronchus at fibrobronchoscopy via a catheter inserted into the cavern-draining bronchus . The trial showed AM-promoted resolution of pulmonary tissue infiltrates and more intensive repair processes . The best results were obtained in 11 new-onset cases of pulmonary tuberculosis.

Jpn J Antibiot, 1990 May, 43(5), 890 - 4
{Clinical study on norfloxacin in children}; Okada K et al.; Norfloxacin (NFLX, AM-715), a new synthetic antibacterial agent, was administered to 18 child patients with infectious diseases . The patients included 5 boys and 13 girls from 3 to 14 years of ages . They were given orally dosage ranging 5.2-17.9 mg/kg/day for 4 to 14 days . Clinical efficacies were excellent in 1 case, good in 16 cases, unknown in 1 case, hence the total efficacy rate was determined to be 100% . There were no cases which showed side effects of the drug and no abnormal laboratory test values were observed during the treatment.

Arzneimittelforschung, 1990 May, 40(5), 614 - 7
Evaluation of ibuprofen dimethyl aminoethanol octyl bromide and related active metabolites in biological samples; Marzo A et al.; AF 150 is ibuprofen dimethyl aminoethanol octyl bromide, endowed with antibacterial and antiinflammatory activities . An indirect HPLC analytical method for AF 150 with UV detection, to be used for pharmacokinetic studies, has been validated in terms of linearity, reproducibility, specificity and sensitivity . Using this method the bioavailability of AF 150 and its active metabolite ibuprofen was investigated following parenteral administration and topical application.

Pharmacol Toxicol, 1990 May, 66(5), 329 - 34
Comparison of the sensitivity of human and rat hepatocytes to the genotoxic effects of metronidazole; Martelli A et al.; Metronidazole (MNZ), an antiprotozoan and antibacterial agent, has been shown to yield DNA-damaging reactive species after nitroreductive biotransformation . The genotoxic effect of MNZ was studied in primary cultures of both rat and human hepatocytes . In millimolar concentrations MNZ produced DNA fragmentation, as measured by the alkaline elution technique, and unscheduled DNA synthesis, as evaluated by quantitative autoradiography, in rat hepatocytes . The amount of DNA damage was directly related to the dose and the length of exposure, was increased by hypoxia and GSH depletion, and was markedly reduced by inhibition of cytochrome P-450 activity . In the same experimental conditions human hepatocytes resulted constantly more resistant than rat hepatocytes to the genotoxic activity of MNZ . These findings suggest that the rat hepatocyte model might be an inappropriate predictor of nitroimidazoles genotoxicity.

J Antibiot (Tokyo), 1990 May, 43(5), 544 - 9
Chemical modification of erythromycins . IV . Synthesis and biological properties of 6-O-methylerythromycin B; Morimoto S et al.; 6-O-Methylerythromycin B has been synthesized from erythromycin B via regioselective methylation of the 6-hydroxyl group in 71% overall yield . This compound shows in vitro antibacterial activity comparable to erythromycins A and B and exhibits superior in vivo activity with improved pharmacokinetic properties.

J Antibiot (Tokyo), 1990 May, 43(5), 519 - 32
A novel carbapenem antibiotic, SM-7338 structure-activity relationships; Sunagawa M et al.; A series of new carbapenem compounds, which have a pyrrolidin-3'-ylthio group substituted with various aminocarbonyl group at C-5' position as C-2 side chain, have been prepared . The antibacterial activity and the stability to renal dehydropeptidase-I of these compounds were investigated, and the structure-activity relationships were discussed . In this series, SM-7338; (1R,5S,6S)-2-{(3S,5S)-5-dimethylaminocarbonylpyrrolidin-3-ylthi o}-6-{(R)-1-hydroxyethyl}-1-methylcarbapen-2-em-3-carboxylic acid (5a) was the most interesting compound.

J Antibiot (Tokyo), 1990 May, 43(5), 504 - 12
Citreamicins, novel antibiotics from Micromonospora citrea: isolation, characterization, and structure determination; Carter GT et al.; A new family of antibacterial antibiotics has been isolated from Micromonospora citrea . The compounds, designated citreamicins alpha, beta, gamma, zeta and eta are of the polycyclic xanthone structure type . Their isolation, characterization and structure determination are presented.

Br J Plast Surg, 1990 May, 43(3), 307 - 11
The management of exposed cardiac pacemaker pulse generator and electrode using restricted local surgical interventions; subcapsular relocation and vertical-to-horizontal bow transposition techniques; Har-Shai Y et al.; This paper describes an approach to the treatment of exposed pacemaker generator and electrode . Local infection is controlled by the administration of systemic antibiotics and topical antibacterial solutions . Because the generator and lead are enveloped by an inert synthetic coating, it is possible to eradicate an infection without their removal if it is due to a weak opportunist pathogen fully sensitive to antibiotics . Thereafter, subcapsular relocation of the exposed generator or vertical-to-horizontal transposition of the exteriorised lead is carried out . These surgical interventions are designed to overcome the vertical force which tends to cause the extrusion of the pacing hardware.

J Med Chem, 1990 May, 33(5), 1470 - 6
Synthesis and biological activity of some derivatives of rifamycin P; Cavalleri B et al.; A series of derivatives of rifamycin P, an antibiotic produced by fermentation of a mutant strain of Nocardia mediterranea or by chemical modification of rifamycin S, have been prepared . The structures of these compounds were determined by 1H NMR, IR, UV, and LC/MS . Their in vitro and in vivo antibacterial activities in comparison with rifampicin and two other rifamycins under investigation were evaluated . The derivatives were more active than rifamycin P against Mycobacterium avium complex and other slowly and rapidly growing nontuberculous mycobacteria which frequently cause systemic infection in patients with AIDS . 2'-(Diethylamino)rifamycin P (P/DEA) appears suitable for further investigation.

J Med Chem, 1990 May, 33(5), 1344 - 52
Fluoronaphthyridines and quinolones as antibacterial agents . 2 . Synthesis and structure-activity relationships of new 1-tert-butyl 7-substituted derivatives; Bouzard D et al.; A number of 7-substituted-1-tert-butyl-6-fluoroquinolone-3-carboxylic acids and 7-substituted-1-tert-butyl-6-fluoro-1,8-naphthyridine-3-carboxylic acids have been prepared and tested for antibacterial activities . Among those the 7-aminopyrrolidinyl 20b and the 7-diazabicyclo naphthyridine 18b are the most potent compounds in vitro and in vivo . Physicochemical data and acute toxicity are also discussed . Compound 18b, BMY 40062, exhibits the most favorable overall properties, considering in vitro and in vivo microbiological activity, its low toxicity, and pharmacokinetic profile, and was selected for clinical evaluation.

J Biomed Mater Res, 1990 May, 24(5), 573 - 80
Effect of vacuum mixing on the mechanical properties of antibiotic-impregnated polymethylmethacrylate bone cement; Askew MJ et al.; Polymethylmethacrylate bone cement, containing either no added antibiotic, 0.5 g of Vancomycin, 1.0 g of Vancomycin, or 1.0 g of Tobramycin, was mixed either in air or a vacuum chamber . Following storage in a water bath at 37 degrees C for 48 h, the specimens were tested in four-point bending . The porosity of the specimens was assessed radiographically, and their antibacterial activity was monitored for 21 days . The bending strength of the vacuum mixed specimens containing no antibiotic was 40% greater than that of similar air-mixed specimens . However, there were no significant differences in the bending strength of either the air- or vacuum-mixed specimens when any of the antibiotic dosages were added . The bending modulus of the vacuum-mixed specimens, containing no antibiotic, was significantly greater than the moduli of all the other specimen groups which did not differ from each other . Vacuum mixing reduced the apparent porosity of the specimens fivefold, and while the addition of antibiotic did not effect porosity of the air-mixed specimens, that of the vacuum-mixed specimens was doubled . Although initial rapid decreases were seen, leaching of antibiotic from the cement and antibacterial activity continued through the 21-day monitoring period.

Kansenshogaku Zasshi, 1990 May, 64(5), 630 - 5
{A case of Pneumocystis carinii pneumonia with hyperinfection of Strongyloides stercoralis complicated with smoldering adult T-cell leukemia}; Udaka M et al.; A 43-year-old woman visited a clinic for an attack of bronchial asthma which she had been suffering since her childhood . She was treated with prednisolone which was used for the first time . Two weeks later, she had a fever and her chest X-ray showed diffuse reticulonodular shadows on both middle to lower lung fields . In spite of the use of antibacterial drugs, her symptoms such as cough, dyspnea, malaise and fever increased . It was revealed that she had Stronglyoides sterocoralis in the stool . She was referred to our department for treatment and further examination . Transbronchial lung biopsy (TBLB) was performed, and cyst of Pneumocystis carinii were histologically detected in the lung specimen . Anti-human T-lymphotropic virus type 1 (HTLV-1) antibody in the serum was 1:4,096 less than . Typical adult T-cell leukemia (ATL) cells were also observed in the peripheral blood smear at the rate of 10-15% of leukocytes . The parasite was observed in the sputum too . We diagnosed her as having Pneumocystis carinii pneumonia with hyperinfection of Strongyloides stercoralis complicated with smoldering ATL, and the pneumonia might have been induced by steroid therapy (total doses of 500 mg, for 25 days) . After sulfamethoxazole-trimethoprim (ST compound) was used for the Pneumocystis carinii pneumonia, her symptoms markedly subsided, and the chest X-ray findings turned to normal by 45 days after the treatment . Thiabendazole was initially administered for the Strongyloidiasis and the parasite temporarily disappeared from both sputum and stool . Then pyrvinium pamoate and mebendazole were used, but the parasite could not be completely eradicated in the stool . We did not treat the smoldering ATL because there were no symptoms . We have been looking after her as an outpatient now, and she has neither symptoms nor signs.

Zh Mikrobiol Epidemiol Immunobiol, 1990 May, (5), 3 - 7
{The effect of the cationic proteins of human blood cells on the growth of Escherichia coli}; Rybakova LP et al.; The antibacterial effect of cationic proteins (CP) on donor leukocytes and thrombocytes with respect to the growth of E . coli has been demonstrated in vitro, the maximum recorded inhibition being caused by the action of leukocytic CP . Differences in the inhibitory action may be linked with the presence of anomalies in the amino acid composition of leukocytic CP and thrombocytic CP, manifested by the deterioration of the basic properties of the latter, as well as by the fractional composition whose characteristic features for thrombocytic CP are the appearance of high-molecular components and a decrease in the proportion of low-molecular fractions . In patients with different forms of leukosis (chronic myeloleukemia, chronic lympholeukemia, acute myelomonoblastic leukosis) leukocytic CP retain their antibacterial activity . Under the action of blood cell CP changes in the outer and cytoplasmic membranes have been noted.

Pathol Biol (Paris), 1990 May, 38(5), 347 - 51
{Comparative antibacterial activity of ceftibuten (SH 39 720) against 150 K . pneumoniae strains producing different beta-lactamases}; Thabaut A et al.; Comparative antibacterial activity of ceftibuten (SH 39 720) on 150 K . pneumoniae strains producing different beta-lactamases . MICs of ceftibuten, cefotaxime + clavulanic acid (10 mg/l), ceftazidime and azthreonam were determined for 150 clinical isolates of K . pneumoniae: 15 "wild" type producing only the SHV-1 type beta-lactamase, 15 TEM-1 and 120 producing new "extended spectrum" beta-lactamases (48 CTX-1, 9 SHV-2, 4 SHV-3, 35 SHV-4, 24 SHV-5) . Against SHV-1 and TEM-1 strains the bacteriostatic activity of ceftibuten was close to that of the other beta-lactams tested . This activity was preserved against strains producing CTX-1, SHV-2, SHV-3 beta-lactamases and MICs were comparable to those of cefotaxime + clavulanic acid . The MICs of ceftibuten against strains producing SHV-4 and SHV-5 beta-lactamases were higher (1 to 8 mg/l) but this level of antibacterial activity was superior to that of the other beta-lactam antibiotics . The bactericidal activity of ceftibuten was evaluated by kill kinetic studies: this activity was preserved against the CTX-A and SHV-2 strains--with concentrations equal to 2 or 4 x CMI a 4 log10 reduction of the bacterial inoculum was obtained at 24 h . A such reduction was not obtained with cefotaxime . This preserved antibacterial activity of ceftibuten against K . pneumoniae producing some new "extended spectrum" beta-lactamases need further studies to state the structure-activity relation-ships of this antibiotic.

Med Hypotheses, 1990 May, 32(1), 33 - 5
Drugs from seaweeds; Abdussalam S; Extracts from seaweed are of botanical and pharmaceutical interest . They are used in traditional remedies in many parts of the world . A large number of edible seaweeds are consumed by the coastal peoples of Asia . Extracted substances from the plants have antibacterial actions and some of these substances have potential use in mosquito control . Other properties include antifungal activities and growth inhibition of other plants . Several chemical compounds have been isolated and identified.

Med Clin North Am, 1990 May, 74(3), 837 - 50
Antibacterial therapy in cystic fibrosis; Mouton JW et al.; Bacterial lung infections determine the prognosis for most cystic fibrosis patients . The antibacterial therapy is difficult because of the host-bacterium interaction and altered pharmacokinetics . The new insights in the working mechanisms of antibiotics that may lead to better treatment results have been discussed, and guidelines for treatment of lung infections in cystic fibrosis patients were given.

Dig Dis Sci, 1990 May, 35(5), 630 - 7
In vitro antibacterial effect of yogurt on Escherichia coli; Kotz CM et al.; We investigated the bactericidal and bacteriostatic effects of yogurt on three strains of Escherichia coli: human toxigenic (078:H11), rabbit pathogenic (RDEC-1) and rabbit nonpathogenic {015:K14(L):H4} . Approximately 10(6) organisms were incubated in yogurt, milk, broth, and modifications of these materials . Aliquots were removed at various intervals and plated on MacConkey's agar for enumeration of E . coli . Yogurt was bactericidal (at least 5 log10 reduction in bacterial counts) to all three strains of E . coli with less than 10 CFU/ml remaining by 9 hr . In contrast, all three strains replicated rapidly in milk and broth, reaching maximum concentrations by 9 hr . The E . coli strains survived and multiplied in milk acidified to the same pH as the yogurt . Yogurt (native pH 4.1-4.4) in which the pH was brought up to and maintained at pH 5.5 or pH 7 for 8 hr was not bactericidal to E . coli . Heat-treated yogurt and the filtered supernatant of centrifuged yogurt (both containing no yogurt bacteria) were only bacteriostatic . We conclude that both live yogurt bacteria and a pH near 4.5 are necessary for the bactericidal activity of yogurt . The possibility that yogurt ingestion could protect against infection via other foods contaminated with pathogenic E . coli merits further in vivo investigation.

Antibiot Khimioter, 1990 May, 35(5), 13 - 6
{Streptonigron--a minor component of bruneomycin complex}; Kozlova NV et al.; A mutant strain of the bruneomycin-producing culture which produced up to 10% of the minor component was selected . The component was identified as streptonigrone . It was isolated and its physicochemical properties and antibacterial activity were investigated . Trimethylsilyl derivatives of streptonigrone and bruneomycin were prepared . Their PMR spectra and electron impulse mass spectra were studied . Streptonigrone was shown to have antibacterial and cytotoxic activities which was 1 to 2 orders of magnitude lower than that of bruneomycin.

J Antibiot (Tokyo), 1990 May, 43(5), 550 - 5
MM 45289, a potent glycopeptide antibiotic which interacts weakly with diacetyl-L-lysyl-D-alanyl-D-alanine; Good VM et al.; MM 45289 (A82846A, eremomycin), a glycopeptide antibiotic of the vancomycin type, was confirmed to have improved antibacterial activity over vancomycin . However its affinity (Ka) for the target site peptide mimetic diacetyl-L-lysyl-D-alanyl-D-alanine (DALAA) was 23-fold lower . Concentrations of DALAA required to reverse the antibacterial activity of MM 45289 were in the order of 10 to 50-fold higher than for vancomycin . These results have implications for both mode of action studies and mechanism-based screening strategies for this class of antibiotic.

Mutat Res, 1990 May, 244(1), 21 - 5
Different effect of hyperthermia and heat shock on the action of quinolone drugs versus some mutagens against chloroplasts of Euglena gracilis; Krajcovic J et al.; Hyperthermia (37 degrees C permanently) and heat shock (42 degrees C for 10 min, and then 27 degrees C) retarded the elimination of chloroplasts from the flagellate Euglena gracilis induced by quinolone antibacterial chemotherapeutics (OA, NA, Cnx, Ofx, Cpfx, Enx, Nfx) in comparison with their action at 27 degrees C . In the case of OA, NA, and Cnx those hyperthermic conditions completely blocked their action against chloroplasts . On the other hand, both temperature regimes accelerated the antichloroplast activity of the mutagens/carcinogens nitrosoguanidine and furylfuramide.

Res Microbiol, 1990 May, 141(4), 499 - 510
Antibacterial activity of phenolic compounds and aromatic alcohols; Lucchini JJ et al.; The antibacterial properties of phenolic compounds and aromatic alcohols (growth inhibition, lethal effect and cytological damage) were investigated . The role of protein and RNA synthesis in the bactericidal action was also determined . All compounds tested demonstrated lethal properties and the ability to alter membranes, especially in Gram-negative bacteria . Efficacious concentrations, however, varied greatly among the compounds . These data corroborate previous findings which suggest that the mechanism of action of these compounds is related to their lipophilia . Moreover, since it was demonstrated that the lethal effect of two aromatic alcohols (phenethyl alcohol and benzyl alcohol) stops when protein synthesis is inhibited, it is likely that both possess specific mechanisms of action.

Antibiot Khimioter, 1990 Apr, 35(4), 20 - 1
{Chemistry of galtamycin . Specification of the aglycone structure . Synthesis of the amino analog}; Murenets NV et al.; The structure of galtamycin aglycone was elucidated . Synthesis of its amino analog with higher antitumor activity and antibacterial activity is described.

Pathol Biol (Paris), 1990 Apr, 38(4), 261 - 6
{Influence of some antibiotics on eicosanoid production by human macrophages in vitro}; Garraffo R et al.; Non antibacterial effects of antibiotics are presently investigated by several authors . They estimate the effects of different molecules on polynuclear chemotaxis, cytokine production or macrophage activity . In this experiment we have studied the effects of two betalactams, two macrolides, a fluoroquinolone and a tetracycline on eicosanoid production by stimulated human macrophages in vitro . All evaluated antibiotics are able to modify the prostaglandin and/or leukotriene production . Taking into account the immunomodulative and inflammatory properties of the eicosanoids, the variation of their production could be relevant in clinical practice.

J Can Dent Assoc, 1990 Apr, 56(4), 325 - 7
Efficacy of chlorhexidine and sanguinarine mouthrinses on selected salivary microflora; Hoover JN et al.; The antibacterial effects of chlorhexidine and sanguinarine on selected salivary microflora were evaluated in 15 healthy young adults . The experiment was performed in a cross-over manner enabling both mouthrinses and the saline control to be tested on all 15 subjects for periods of one week separated by three week intervals . The total bacterial count and selected bacterial genera were followed in saliva samples taken just before the first rinse, and on three occasions after the last rinse . Statistically significant reductions in the salivary levels of S . mutans and S . salivarius were obtained with chlorhexidine but not with sanguinarine, and rinsing twice a day with sanguinarine, according to the manufacturer's instructions, did not significantly reduce the total bacterial count . Additional well controlled, longer-term studies are required before any firm conclusions can be drawn regarding the effect of sanguinarine on salivary microorganisms.

J Biochem (Tokyo), 1990 Apr, 107(4), 514 - 8
Determination of the disulfide array in sapecin, an antibacterial peptide of Sarcophaga peregrina (flesh fly); Kuzuhara T et al.; Sapecin is a 40-residue peptide containing 6 half-cystine residues . The disulfide structure of sapecin was determined by sequencing cystine-containing peptides obtained by digesting sapecin with thermolysin . Results showed that sapecin has a vortical structure fixed by 3 disulfide bonds between cysteine residues 3 and 30, 16 and 36, and 20 and 38, respectively, and that these disulfide bonds are essential for its antibacterial activity.

J Antibiot (Tokyo), 1990 Apr, 43(4), 357 - 71
Synthesis and antibacterial activity of novel 2-methyl-1-oxacephalosporins; Okonogi T et al.; New 2-methyl-1-oxacephem compounds having 2-(2-aminothiazol-4-yl)-2-(alkoxyimino)acetamido substituents at C-7 and various C-3 side chains were synthesized starting from (3R,4S)-phenyloxazolinoazetidinone (8) . Introduction of the 2 beta-methyl group into the 1-oxacephem nucleus increased the stability to beta-lactamases . OCP-9-176 (7b) having the (1-methylpyridinium-4-yl)thiomethyl group at C-3 showed potent antibacterial activity and a broad spectrum.

Burns, 1990 Apr, 16(2), 137 - 43
Histological and bacteriological studies of burn wounds treated with boiled potato peel dressings; Keswani MH et al.; Histological and clinical studies have been made on comparable burn wounds covered with either boiled potato peels affixed to gauze bandages or gauze dressings alone; both dressings were applied over a thin layer of 5 per cent silver sulphadiazine . Compared with treatment with plain gauze dressings, the application of the potato peel dressing reduced or eliminated dessication, permitted the survival of superficial skin cells and hastened epithelial regeneration . Bacteriological studies showed that the potato peels had no intrinsic antibacterial activity, the wounds beneath both dressings showing either no growth or, on most occasions, the same bacterial species . The easy availability of potato peels and gauze bandages on to which they can be affixed, the simplicity of the preparation of this dressing, the ease of sterilization and its low cost of production make this the dressing of choice for burn wounds in our developing country.

J Med Chem, 1990 Apr, 33(4), 1246 - 52
The synthesis and antibacterial activities of quinolones containing five- and six-membered heterocyclic substituents at the 7-position; Cooper CS et al.; A series of 6-fluoro-7-substituted-1-ethyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids were prepared . The substituents at the 7-position included five- and six-membered heterocyclic rings such as oxazoline and oxazine as well as five-membered heteroaromatic rings such as oxazoles and imidazoles . The structure--activity relationships (SAR) of these compounds indicated that oxazole substituents containing a 2-methyl group had the greatest in vitro potency . The compounds showed greater in vitro antibacterial activity against Gram-positive organisms than against Gram-negative organisms.

J Am Acad Dermatol, 1990 Apr, 22(4), 583 - 6
The antibacterial efficacy of econazole nitrate in interdigital toe web infections; Kates SG et al.; Twenty-four patients with severe interdigital toe web infections and no evidence of dermatophyte colonization received randomized treatment with either econazole nitrate (Spectazole) or its vehicle . Of the patients treated with econazole nitrate, 88% had good to excellent responses, whereas no patient treated with the vehicle showed improvement . The total aerobic flora in the econazole group decreased 93%, with decreases in the large-colony diphtheroids, lipophilic diphtheroids, and gram-negative bacteria . The results of this study demonstrate that the antibacterial activity of econazole nitrate makes it an effective agent for the treatment of severe interdigital bacterial infections uncomplicated by dermatophyte colonization.

Rev Argent Microbiol, 1990 Apr-Jun, 22(2), 68 - 72
{Isolation of ALteromonas putrefaciens from secondary-recovery water in the petroleum industry}; Pucci OH; Eight strains obtained from injection water for secondary recovery of oil were isolated and characterized as alteromonas . This species has been reported in a relatively great number in the system, after its treatment with cresylic acid (used as antibacterial agent) . It has the property of forming important viscous sediments which are related to biofouling of the injection system.

Minerva Anestesiol, 1990 Apr, 56(4), 127 - 31
{The activity of the "Hygrobac DAR 352" filter in resuscitation patients}; Grondona G et al.; The Authors clinically evaluated the efficacy of the "Hygrobac DAR 352" filter as an antibacterial barrier in a group of patients during mechanical ventilation . After 24 hours of IPVV, a cultural sample has been taken on both sides of the filter introduced in the breathing circuit (patient's side; ventilator's side) . While bacteria has been isolated on "the patient's side" of the filter, they were not present on the surface of the "ventilator's side" of the filter . Therefore, the Authors emphasize that the Hygrobac DAR 352 filter represents a good barrier against the passage of bacteria, as it avoids the contamination of the mechanical ventilator by keeping pathogenic organisms coming from patient's airways inside the filter itself.

Biophys Chem, 1990 Apr, 35(2-3), 287 - 300
Ambazone as a membrane active antitumor drug; Lober G et al.; Ambazone (1,4-benzoquinone guanylhydrazone thiosemicarbazone) was found to be active against various transplantable tumors in mice as well as rats . When administered orally for 4-9 days, the effective therapeutic dose ranged between 60 and 125 mg/kg . The antineoplastic effect of ambazone appeared to be mediated, at least in part, by the immune system . In order to characterize the drug, biophysical and biophysicochemical studies were carried out using thin-layer chromatography, absorption spectroscopy and polarographic measurements . The distribution of ambazone in an n-octanol/water system indicated low hydrophobicity, thereby excluding the possibility of a preferential contribution from hydrophobic forces to the mode of action of ambazone . Ambazone undergoes three protonation reactions with pK values at 10.69 (equilibrium between the negatively charged and neutral forms), 7.39 (equilibrium between the neutral and singly positively charged form) and 6.22 (equilibrium between the singly and doubly positively charge form) . Interaction of the drug with model membrane system was monitored by spectrophotometric and fluorescence measurements . Using the fluorescence label 1-anilino-8-naphthalenesulfonic acid (ANS) as a probe pointed to the interaction of ambazone with the inner area of the phospholipid bilayer matrix of liposomes as being nonspecific . Ambazone induces an overall increase in the cellular cAMP content of leukemia cells and macrophages . So far, membrane interaction has provided a molecular basis for both immunological and antineoplastic activities of the drug . By performing DNA melting experiments, it was shown that neutral or singly positively charged ambazone species stabilize the secondary structure of DNA, while the doubly positively charged form binds more strongly and destabilizes the DNA . After oral administration to rats and mice, ambazone was found to be incompletely absorbed from the gastrointestinal tract, to an extent of about 35-50% . Absorbed ambazone binds only weakly to plasma proteins, whereas its binding to red blood cells is relatively strong . The mutagenic potential of ambazone shown in bacterial systems and human lymphocytes corresponds to its relatively weak interaction with DNA . The toxic action of ambazone on the intestine is believed to be due to inhibition by the drug of bacterial DNA, RNA and protein syntheses . It is assumed that the reported affinity of ambazone for different cellular targets, i.e., membranes, nucleic acids and proteins, contributes to the overall antibacterial effect . The weak antiviral activity of ambazone in the Sendai virus/chicken embryo fibroblast system is probably the result of the interaction with Sendai virus NH glycoprotein.

Yakugaku Zasshi, 1990 Apr, 110(4), 258 - 67
{Studies on quinolone antibacterials . I . Synthesis and antibacterial activity of 7-(2-aminoethoxy)-, 7-(2-aminoethylthio)-, and 7-(2-aminoethylamino)-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo qui noline -3-carboxylic acids and their derivatives}; Yoshida T et al.; 7-(2-Aminoethoxy)-, 7-(2-aminoethylthio)-, and 7-(2-aminoethylamino)-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoq uin oline-3- carboxylic acids and their derivatives (11a--f, h, j, k, 12a--f, and 13a--f) were synthesized and their antibacterial activities were tested . Among them, compounds (13a, d) having a primary amino group at the terminal position of alkoxy and alkylthio groups were found to have excellent in vitro and in vivo antibacterial activity comparable to those of ciprofloxacin (5) . Structure-activity relationship of these compounds was also stated.

Minerva Chir, 1990 Mar 15, 45(5), 307 - 8
{Clinical use of ceftriaxone in short-term prophylaxis in general surgery . A case load contribution}; Brigli G et al.; The results obtained after short-term surgical prophylaxis with ceftriaxone in 443 patients of whom 361 operated of choice are reported . In all, only 3 failures were encountered . The drug also proved to be well tolerated and there were no noteworthy side-effects in the treated patients . The effectiveness of prophylactic treatment is attributed to the long half-life of the molecule (about 8 hours) guaranteeing efficient antibacterial cover with just one administration for the whole period that is critical for surgical infections, during and after operation.

Presse Med, 1990 Mar 10, 19(9), 405 - 6
{Optimal length of antibiotic therapy in aspirated cerebral abscess}; Lepresle E et al.; Between 1983 and 1988, 22 patients with brain abscess were admitted to our neurosurgery department; 2 patients deeply comatose on admission and who died on the first day were excluded from this study . Treatment consisted of needle aspiration of the abscess and antibacterial therapy initially using a broad-spectrum antibiotic later replaced, in all cases, by an antibiotic found to be active in vitro against the organism(s) isolated . The portal of entry was eradicated as early as possible . The duration of antibiotic therapy was determined according to the changes observed on computerized tomography images classified as cavitary, nodular, hypodense or normal . Nodular images were taken as reflecting an inflammatory state in the healing process, and hypodense images as sequelae, so that antibiotics were withdrawn in patients with such images . Altogether, 62 per cent of the patients received antibiotics for 60 days and 95 per cent for 90 days . There was no recurrence . In some patients with deep or, chiefly, multiple abscesses, treatment was pursued . In any case, antibiotics should not be given for more than 90 days if the initial treatment has proved effective, since cure is achieved in 45 to 60 days on average.

Farmaco, 1990 Mar, 45(3), 313 - 30
Chemometric approach in a QSAR study: the antibacterial and antimicotic activities of benzofused heteroaromatic derivatives; De Meo G et al.; In order to establish quantitative relationships between the antibacterial activities of a number of thienyl- and furyl-benzimidazoles and benzoxazoles, the biological data were measured homogeneously for a selected set of 16 representative compounds of the available set of 103 . The data were analyzed by the PLS method . The results of linear PLS modelling and PLS response surface modelling permitted a straightforward interpretation of the structural features relevant to the activities and the prediction of a possible optimal structure.

Int J Artif Organs, 1990 Mar, 13(3), 169 - 75
Computer simulation of ciprofloxacin pharmacokinetics in patients on CAPD; Mrhar A et al.; Continuous ambulatory peritoneal dialysis (CAPD) has become an accepted alternative to chronic hemodialysis in the treatment of end-stage renal disease . The method utilizes the diffusion of drugs from the blood through the peritoneal membrane to the peritoneal cavity if administered intravenously (IV) and perorally (PO) and in the opposite direction if applied intraperitoneally (IP) . The present work uses an open, two-compartment pharmacokinetic model reversibly linked with the compartment representing the peritoneal cavity and an analog-hybrid computer to simulate drug levels in sampled and unsampled compartments under conditions of various routes of administration (IV, IP and sequential IV, IP and PO) and different clinical status (presence and absence of peritonitis) . The drug chosen for simulation was ciprofloxacin (CIP), a new synthetic antibacterial agent of the 4-quinolone group . Eight patients were included in the study, and CIP concentrations in plasma and dialysate were obtained by HPLC analysis to assess the reliability of the model and the efficiency of the sequential dosing scheme . CIP plasma and dialysate levels were adequate for the majority of microbes causing CAPD peritonitis . The proposed regimen was efficient in 85% of cases.

J Antimicrob Chemother, 1990 Mar, 25(3), 353 - 9
Microcalorimetric studies of the initial interaction between antimycobacterial drugs and Mycobacterium avium; Hoffner SE et al.; To further our understanding of the mechanisms by which ethambutol potentiates the effect of other antimycobacterial drugs on mycobacteria we have studied the initial physico-chemical interaction between ethambutol and the Mycobacterium avium cell envelope using batch reaction microcalorimetry . When strains of M . avium were exposed to ethambutol an immediate endothermic reaction was recorded . When the M . avium cells were pre-treated with ethambutol this strongly affected the initial interaction between streptomycin and the bacterial cell surface . When the M . avium cells were simultaneously exposed to a combination of ethambutol and streptomycin an altered initial interaction with streptomycin was seen . These data suggest that ethambutol may potentiate the effect of other antibacterial drugs on M . avium by increasing cell wall permeability.

J Antibiot (Tokyo), 1990 Mar, 43(3), 286 - 94
Chemical modification of erythromycins . II . Synthesis and antibacterial activity of O-alkyl derivatives of erythromycin A; Morimoto S et al.; A series of O-alkyl erythromycin A derivatives have been synthesized and their antibacterial activities compared with those of erythromycin A (1) and 6-O-methylerythromycin A (3) . Methylation of the hydroxyl groups of erythromycin A analogue proceeded stepwise by the two main pathways beginning at the C-6 and C-11 positions, individually . O-Alkylation, other than methylation, took place at the C-11 hydroxyl group exclusively . Among O-alkyl derivatives, 6,12-di-O-methylerythromycin A (5) showed comparable in vitro antibacterial activity to those of 1 and 3 . 11-O-Methylerythromycin A (8) was slightly less active than 1 . O-Methylation at the C-4" position resulted in a decrease of antibacterial activity.

J Antibiot (Tokyo), 1990 Mar, 43(3), 306 - 13
Synthesis and structure-activity relations in the class of 2-(pyridyl)penems; Bedeschi A et al.; The isosteric CH----N substitution in the class of 2-arylpenems results in improved antibacterial activity, with retention of the favorable characteristic of stability towards renal dehydropeptidase . High therapeutic efficacy was demonstrated in experimental mice septicemias with the 2-(3-pyridyl) derivative 2b and its orally absorbed acetoxymethyl ester prodrug 4n.

Gan To Kagaku Ryoho, 1990 Mar, 17(3 Pt 2), 517 - 23
{DNA damage and anticancer effect}; Kanamaru R et al.; In a sense, cancer chemotherapy is similar to antibacterial chemotherapy . The main target for both chemotherapies is on DNA and its precursors . Whenever anticancer drugs exhibit its activity on cancer cells, damage or metabolic abnormality of DNA is usually accompanied . Among various anticancer drugs, the main cellular target of alkylating agents or anticancer antibiotics is DNA strand, and many of newly introduced anticancer drugs exert effect on DNA strand or DNA synthesis . The mechanism of action of quinocarmycin, KT 6149, which is a derivative of mitomycin C, YM534, which shows thrombocyte agglutination activity, and MCNU, a nitrosourea, were studied for their antitumor action and damage to DNA strand . It was found that there was a close relationship between anticancer effect and single strand scission of DNA in all the agents tested.

Nurs Clin North Am, 1990 Mar, 25(1), 205 - 22
Wound healing in the patient with burns; Bayley EW; The burn wound presents many unique challenges to the nurse who promotes optimal wound healing . Nursing care includes meticulous attention to the prevention of infection, wound cleansing and debridement, and application of topical antibacterial agents . Preparation of graft recipient sites, care of graft and donor sites, and use of various biologic and synthetic wound coverings are required . An interdisciplinary approach that provides for adequate nutrition, fosters physical function, and supports psychologic adjustment to altered self-concept is required for holistic healing of the burn wound.

Gan To Kagaku Ryoho, 1990 Mar, 17(3 Pt 1), 330 - 4
{Inhibitors of DNA topoisomerases}; Andoh T; DNA topoisomerases participate in various aspects of DNA metabolism by their unique catalytic activity of changing DNA topology . Inhibitors of bacterial topoisomerases are antibacterial agents and those inhibiting mammalian counterparts are antitumor agents . What kinds of antitopoisomerase chemicals we have, how they act on topoisomerases, and what is known about the resistance against those agents are briefly reviewed . Furthermore, future problems to be solved in cancer chemotherapy were mentioned.

Am Rev Respir Dis, 1990 Mar, 141(3 Pt 2), S141 - 4
Receptors on airway gland cells; Basbaum CB et al.; Airway submucosal glands are by volume the most important source of macromolecules in airway secretions . These secretions, containing gel-forming mucins, antibacterial proteins, and antiproteases, comprise the major defensive barrier protecting the host against airborne pathogens . The identification of the mechanisms regulating secretion from the submucosal glands is key to understanding the genesis of this barrier and how it is altered by disease processes . Using a variety of methods, we and others have identified on the gland cells of several species receptors specific for ACh, norepinephrine, substance P, VIP, PGE1, PGE2, PGA1, PGD2, histamine and bradykinin . These receptors all participate in modulating the secretory activity of the airway submucosal glands . Studies of homogeneous cultures of bovine airway serous cells have yielded detailed information regarding the beta-adrenergic receptor on these cells . Using radioligand binding techniques, we found evidence for the presence of a single high affinity beta receptor of beta-2 subtype . Occupancy of this receptor by isoproterenol causes an elevation in the concentration of intracellular cAMP, which in turn stimulates the phosphorylation of a subset of cytoplasmic and membrane proteins . Based on the kinetics and pharmacology of these effects, it is likely that cAMP functions as a second messenger in the serous cell secretory pathway, probably acting through protein kinases . Current efforts are directed at identification of those phosphoproteins whose phosphorylation and dephosphorylation times are consistent with their possible roles in secretion.

J Antimicrob Chemother, 1990 Mar, 25(3), 319 - 33
The accumulation of five quinolone antibacterial agents by Escherichia coli; Diver JM et al.; The accumulation of five radiolabelled quinolone antibacterial agents by Escherichia coli KL16 was examined using a vacuum filtration method . Preliminary experiments were performed to determine the optimum quinolone concentration, inoculum of cells, filter washing regimen and filter type . All five quinolones showed a similar biphasic pattern of accumulation with high radioactive counts cell-associated during the first ten seconds of the assay, followed by steadily increasing accumulation over 30 min . Analysis of the mean accumulation after 30 min for each quinolone showed that there was no direct relationship between quinolone accumulation and antibacterial activity (as quantified by the MIC or bactericidal activity) . Mechanistic investigations showed that accumulation was decreased by low reaction temperatures, acid pH and the presence of the metabolic inhibitors 2,4-dinitrophenol, potassium cyanide and sodium azide . These results suggest that quinolone accumulation by E . coli KL16 is partly dependent on cell metabolism and may proceed by an active transport mechanism . Treatment of cells with EDTA was found not to increase quinolone accumulation, suggesting that the outer membrane of E . coli KL16 does not act as a permeability barrier to these quinolones . The implication of these results in terms of possible mechanisms of bacterial resistance to quinolones is discussed.

Drug Metab Dispos, 1990 Mar-Apr, 18(2), 245 - 52
Physiologically based pharmacokinetics of a new penem, SUN5555, for evaluation of in vivo efficacy; Tsuji A et al.; SUN5555, (5R,6S)-6-{(R)-1-hydroxyethyl}-7-oxo-3-{(R)-2- tetrahydrofuryl}-4-thia-1-azabicyclo-{3.2.0}-hept-2-ene-carboxylic acid, is a newly developed and orally effective penem with a broad antibacterial spectrum . SUN5555 was degraded in rat tissue homogenates and serum, and its degradations in the kidney and lung homogenates were significantly inhibited by cilastatin, an inhibitor of dehydropeptidase I . The pulmonary extraction was evaluated to be 0.033 by comparing the AUCs resulting from iv and intra-arterial administration of 10 mg/kg . From the arterial-to-venous concentration differences under steady state conditions in rats, extraction ratios of SUN5555 across the kidney, hind leg, gut, and liver were determined to be 0.333, 0.104, 0.071 and 0.053, respectively, whereas no appreciable extraction across the brain was observed . Therefore, organ clearances of SUN5555 are limited by the product of plasma unbound fraction and organ intrinsic clearances in various tissues . Using a physiologically based pharmacokinetic model, unbound concentrations of SUN5555 in the tissue interstitial fluids, which are the measure of in vivo antibacterial efficacy, were estimated to be almost identical with, or higher than, those in plasma in rats . Similarly, serum concentration-time profiles of SUN5555 after iv administration in other animal species were predicted and found to be in good agreement with the observed data in dogs . A preliminary prediction of the pharmacokinetics of SUN5555 in a human subject was also attempted by animal scale-up technique.

J Membr Biol, 1990 Mar, 114(1), 79 - 95
Formation of ion channels by colicin B in planar lipid bilayers; Bullock JO et al.; The gene for the antibacterial peptide colicin B was cloned and transformed into a host background where it was constitutively overexpressed . The purified gene product was biologically active and formed voltage-dependent, ion-conducting channels in planar phospholipid bilayers composed of asolectin . Colicin B channels exhibited two distinct unitary conductance levels, and a slight preference for Na+ over Cl- . Kinetic analysis of the voltage-driven opening and closing of colicin channels revealed the existence of at least two conducting states and two nonconducting states of the protein . Both the ion selectivity and the kinetics of colicin B channels were highly dependent on pH . Excess colicin protein was readily removed from the system by perfusing the bilayer, but open channels could be washed out only after they were allowed to close . A monospecific polyclonal antiserum generated against electrophoretically purified colicin B eliminated both the biological and in vitro activity of the protein . Membrane-associated channels, whether open or closed, remained functionally unaffected by the presence of the antiserum . Taken together, our results suggest that the voltage-independent binding of colicin B to the membrane is the rate-limiting step for the formation of ion channels, and that this process is accompanied by a major conformational rearrangement of the protein.

BMJ, 1990 Feb 17, 300(6722), 441 - 4
Antibiotic prescribing: the need for a policy in general practice; Wyatt TD et al.; OBJECTIVE--To see whether changes in prescribing of oral antibacterials in Northern Ireland show the need for a community antibiotics policy . DESIGN--Analysis of prescribing totals for several oral antibiotics obtained retrospectively from the prescription pricing bureau for the years 1983-7 . SETTING--Audit of anti-infective prescribing in general practice in Northern Ireland over five years . MAIN OUTCOME MEASURE--Respective usage of agents defined as "common" and "occasional" in 1983 . RESULTS--There was a gradual decrease in the relative use of common agents from 82% of the total in 1983 to 77% in 1987 together with a complementary increase in the use of occasional agents from 5% to 10% . Pronounced changes were noted in the use of amoxycillin, ampicillin, erythromycin, minocycline, doxycycline, and amoxycillin-clavulanic acid . CONCLUSION--Though this survey found reasonably conservative prescribing, the trend towards increased use of occasional agents has both clinical and cost implications which could be addressed by the use of a prescribing formulary.

Klin Med (Mosk), 1990 Feb, 68(2), 91 - 4
{Use of decamethoxine in the complex treatment of chronic bronchitis}; Iukhimets VA et al.; Seventy-two patients with chronic bronchitis were examined and divided into 3 groups . Group I consisted of patients with chronic catarrhal bronchitis (CCB) group II of those with chronic purulent bronchitis (CPB), group III of subjects with bronchitis associated with purulent destructive pulmonary diseases . All the patients received combined treatment with decamethoxin as an antibacterial modality . It was found that decamethoxin promotes elimination of the infection of the bronchial secretion in 60% of chronic bronchitis suffers, the incidence of microorganisms resistent to several antibiotics reduced 2-fold . Local use of decamethoxin as an antibacterial and antiinflammatory drug in multimodality treatment of chronic purulent bronchitis proved highly effective.

Khirurgiia (Mosk), 1990 Feb, (2), 97 - 100
{Treatment of peritonitis of appendicular etiology}; Shurkalin BK et al.; The authors had 475 patients with appendicular peritonitis under observation . All of them underwent emergency operation and were given antibacterial therapy with metronidazole and agents of the aminoglycoside series . Among 223 patients, the operation on whom was completed by traditional drainage of the abdominal cavity and complete closure of the operative wound, 148 patients developed postoperative complications . Five patients died . In 252 patients, primarily delayed sutures were applied to the wound and drainage of the abdominal cavity was limited . The abdominal cavity was inspected repeatedly in 24 patients with generalized peritonitis and clinical signs of anaerobic nonclostridial infection . Postoperative complications occurred in 87 patients and were limited to suppuration of the wound . One patient died.

Clin Otolaryngol, 1990 Feb, 15(1), 59 - 61
Do patients with otitis externa produce biochemically different cerumen?
Osborne JE, Baty JD.
As polyunsaturated fatty acids have better antibacterial properties than saturated fatty acids, the cerumen of seven patients with recurrent otitis externa and seven unaffected subjects was analysed to determine their ratio . There was no significant difference in either the overall ratio of unsaturated/saturated fatty acids or in the amounts of the individual fatty acids from the cerumen of either group.

Dig Dis Sci, 1990 Feb, 35(2), 231 - 5
Complement levels in patients with hepatic dysfunction; Ellison RT 3rd et al.; Total hemolytic complement activity and serum complement protein concentrations were compared in 17 hospitalized patients with normal hepatic function and 16 patients with liver disease due to alcohol (15 patients) or acetaminophen toxicity (one patient) . In contrast to the control patients, individuals with hepatic dysfunction had decreased total CH50 levels and low concentrations of total C3, C4, C5, factor B, and the regulatory proteins factor I and beta-1H . These patients also had increased C4d/C4 ratios, indicating classical pathway activation . The level of complement deficiency appears to correlate with either prolongation of the prothrombin time or depression of serum albumin concentration . These results indicate that patients with hepatic disease have severe complement depletion that is probably multifactorial in origin . This impairment in complement function will contribute to the impaired antibacterial host defense of the patient with chronic hepatic disease.

J Med Chem, 1990 Feb, 33(2), 765 - 71
Lipophilic 1,3-xylyl-21-crown-6 macrocyclic polyether 2-carboxylic acids as biological mimics of the ionophore antibiotics; Urban FJ et al.; Twelve lipophilic 1,3-xylyl-21-crown-6 macrocyclic polyether 2-carboxylic acids, two lariat ether 1,3-xylyl-21-crown-6 macrocyclic polyether 2-carboxylic acids, and two 1,3-xylyl-28-crown-8 macrocyclic polyether 2-carboxylic acids were synthesized and tested for in vitro antibacterial activity, in vitro stimulation of rumen propionic acid production, and in vivo anticoccidial activity in chickens . These are biological screens relevant to animal health areas where the ionophore antibiotics such as monensin have found application . While the parent structure 1 without lipophilic substituents was biologically inactive, the lipophilic macrocycles were active in the two in vitro tests but not against chicken coccidiosis . One compound was tested in cattle and was found to increase levels of propionic acid in the rumen fermentation . This effect is considered an important factor for increasing the efficiency of feed utilization in cattle exhibited by the ionophore antibiotic monensin . The alkali ion salts of these lipophilic macrocyclic polyether carboxylic acids are very soluble in organic solvents and insoluble in water . These compounds are proposed to act as ion-transport agents and functional mimics of the ionophore antibiotics in the biological systems described above.

J Med Chem, 1990 Feb, 33(2), 552 - 60
Hypolipidemic activity of rifamycin derivatives; Traxler P et al.; Series of 3-piperidinyl- and 3-piperazinylrifamycins and to a certain extent 3-hydrazonorifamycins all bearing lipophilic side chains were found to exert potent hypolipidemic activity in lowering both serum cholesterol and LDL-cholesterol in rats . Starting from 3-{N'-(2,4,6-trimethylbenzyl)-N-piperazinyl}rifamycin SV (compound 25), a series of derivatives were synthesized with the aim of dissociating the hypolipidemic from the antibacterial activity, leading to the 8-O,N-dipivaloyl derivative of 25 (compound 48), which is devoid of any antibacterial activity but shows about 50-60% reduction of LDL-cholesterol and 20-30% reduction of serum cholesterol at a dose of 10 mg/kg . Compound 48 was selected for further pharmacological evaluation.

Arzneimittelforschung, 1990 Feb, 40(2 Pt 1), 190 - 2
Ofloxacin treatment of nongonococcal urethritis . A multi-center study in Asia; Kawada Y et al.; Ofloxacin, a new quinolone antibacterial agent, is active in vitro against gonococcal and nongonococcal urogenital pathogens . Chlamydia trachomatis infection is the most common cause of nongonococcal urethritis . In a multicenter study in seven Asian countries, 105 mal patients with chlamydial urethritis and 46 male patients with nongonococcal and nonchlamydial urethritis were treated with oral ofloxacin at a dosage of 200 mg twice daily for 5 to 10 days . The evaluation performed at day 5 and/or day 10 after treatment revealed good results in 58.2% and 96.8% of the chlamydial urethritis group, and 73.1% and 79.4% of the nongonococcal, nonchlamydial urethritis group, respectively . No severe side effects were observed . Ten-day treatment with ofloxacin showed good clinical efficacy on nongonococcal urethritis.

Med Hypotheses, 1990 Feb, 31(2), 99 - 103
Sulfapyridine and sulfones decrease glycosaminoglycans viscosity in dermatitis herpetiformis, ulcerative colitis, and pyoderma gangrenosum; Stone OJ; Shortly after the introduction of sulfa drugs, sulfapyridine was found to have unique therapeutic properties, unrelated to antibacterial activity . Later, sulfones were found to share the same properties . The disorders initially improved were dermatitis herpetiformis, pyoderma gangrenosum, subcorneal pustular dermatosis, acrodermatitis continua, impetigo herpetiformis and ulcerative colitis . They were also sometimes helpful in many other disorders . They are effective in select disorders characterized by edema followed by granulocytic inflammation or edema followed by vesicle or bullae formation . The sulfones work in low doses in leprosy and their mode of action is not fully understood . Several pieces of experimental information are available . It is proposed that these drugs are entering or influencing the protein moiety of glycosaminoglycans and decreasing tissue viscosity . This decreased tissue viscosity prevents edema and dilution of tissue fluid and decreases acute inflammation and vesicle and bullae formation.

J Antibiot (Tokyo), 1990 Feb, 43(2), 199 - 206
A screening method for antifungal substances using Saccharomyces cerevisiae strains resistant to polyene macrolides; Etienne G et al.; Strains of Saccharomyces cerevisiae FL200 capable of growing on a solid medium containing a mixture of polyene macrolide antibiotics (nystatin, 40 micrograms/ml, amphotericin B, 40 micrograms/ml, pimaricin, 150 micrograms/ml and RP9971 antibiotic, 10 micrograms/ml) have been isolated after successive selection steps . The mutant strains, PR13 and PRC24, are 10 to 100 times more resistant than the polyene macrolide antibiotics . When 4% Tween 80 is added to the medium, resistance to these antifungal drugs is further increased . In addition, strain PRC24, derived from strain PR13, is resistant to a non-polyene macrolide antifungal antibiotic, cycloheximide . In contrast, PR13 and PRC24 are both highly susceptible to a large range of compounds, including non-polyenic antifungal, antitumor and antibacterial agents . These particular characteristics make these strains useful for the rapid detection of antifungal compounds of the polyene macrolide and cycloheximide types, as well as for the recognition of antimitotic substances.

J Antibiot (Tokyo), 1990 Feb, 43(2), 189 - 98
New aminothiazolylglycylcephalosporins with a 1,5-dihydroxy-4-pyridone-2-carbonyl group . II . Synthesis and antibacterial activity of MT0703 and its diastereomers; Ogino H et al.; A practical synthetic method for large scale production of MT0703, (6R,7R)-7-{(RS)-2-(2-aminothiazol-4-yl)-2-(1,5-dihydroxy-4-pyridon e-2- carboxamido)acetamido}-3-{{1-(2-hydroxyethyl)pyridinium-4- yl}thiomethyl}ceph-3-em-4-carboxylate, was established . Its two diastereomers on configuration of the aminothiazolylglycyl moiety were synthesized using chemico-enzymatic method . The S-isomer of MT0703 was found to be more active against Gram-positive and Gram-negative bacteria including beta-lactamase-producing strains than the R-isomer.

J Antibiot (Tokyo), 1990 Feb, 43(2), 174 - 88
New aminothiazolylglycylcephalosporins with a 1,5-dihydroxy-4-pyridone-2-carbonyl group . I . Synthesis and biological activity of cephalosporin derivatives leading to MT0703; Ogino H et al.; A series of new aminothiazolylglycylcephalosporins with a mono- or dihydroxypyridonecarbonyl group at the alpha-amino group of the C-7 substituent have been prepared and antibacterial activity of these compounds was investigated . Among them, the compounds having a 1,5-dihydroxy-4-pyridone-2-carbonyl group showed excellent anti-pseudomonal activity . In particular, (6R,7R)-7-{(RS)-2-(2-aminothiazol-4-yl)-2-(1,5-dihydroxy-4- pyridone-2-carboxamido)- acetamido}-3-{{1-(2-hydroxyethyl)pyridinium-4-yl}thiomethyl}ceph-3 -em- 4-carboxylate (MT0703, 7g) was found to be a well balanced compound with respect to antibacterial activity.

J Antibiot (Tokyo), 1990 Feb, 43(2), 129 - 34
Resorthiomycin, a novel antitumor antibiotic . I . Taxonomy, isolation and biological activity; Suzuki H et al.; Resorthiomycin, a novel antitumor antibiotic, was isolated from the fermentation broth of a strain of Streptomyces collinus by ethyl acetate extraction, silica gel chromatography and HPLC . Resorthiomycin exhibited an in vitro cytotoxic activity against mouse leukemia L5178Y cells (IC50, 15.5 micrograms/ml) and also inhibited the clonogenic activity of a multidrug-resistant mutant of human hepatoma PLC/PRF/5 cells to a greater extent than that of the parental cells . On the other hand, this antibiotic does not possess any antibacterial or antifungal activity.

J Med Chem, 1990 Feb, 33(2), 849 - 54
New quinolone antibacterial agents . Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids; Hagen SE et al.; A series of 7-(3-amino- or 3-aminomethyl-1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-o xo-3-quinolinecarboxylic acids was synthesized and tested for antibacterial activity . Unique to these quinolones was the presence of a methyl or phenyl group in the pyrrolidine ring . Although the in vitro activity of these agents was usually equal to or less than that of their unsubstituted counterparts, one quinolone, 7-{3-(aminomethyl)-3-methyl-1-pyrrolidinyl}-1-cyclopropyl-6,8-difluoro-1 ,4-dihydro-4-oxo-3-quinolinecarboxylic acid, displayed exceptional potency both in vitro and in vivo, particularly against Gram-positive organisms.

Z Gesamte Hyg, 1990 Feb, 36(2), 86 - 8
{Antibacterial mechanism of action of hydrogen peroxide preparations}; Tschernjawskaja MA et al.; Whereas the effectivity of H2O2 can be influenced only little through the acidulation (to pH 2.7) its combination with chinosole are distinctly superior to H2O2 in their effectivity . The most increase of effectivity is attainable with the admixture of anionic and cationic detegents . Ideas about different character of effectivity of combinations partner were discussed by reason of the influence of ATPase activity and optical dencity of E . coli cells.

J Antibiot (Tokyo), 1990 Jan, 43(1), 92 - 9
Antibacterial properties of the bicyclic pyrazolidinones; Allen NE et al.; LY173013 and LY186826 are bicyclic pyrazolidinones containing a novel aza-gamma-lactam ring structure . The antibacterial properties of these compounds appear to be related to those of beta-lactam antibiotics in that both classes of compounds share certain common binding molecules such as beta-lactamases and penicillin-binding proteins.

J Antibiot (Tokyo), 1990 Jan, 43(1), 76 - 82
6-(substituted methylene)penems, potent broad spectrum inhibitors of bacterial beta-lactamase . II . Racemic furyl and thienyl derivatives; Broom NJ et al.; A series of racemic 6-(substituted methylene)penems have been prepared . These compounds contain a 5-membered monoheteroaromatic ring at C-8 . The antibacterial/synergistic and beta-lactamase inhibitory activities of both E- and Z-isomers and 2-substituted derivatives are compared.

J Antibiot (Tokyo), 1990 Jan, 43(1), 62 - 9
A new aminothiazolylcephalosporin having 1-carboxyethoxyimino group, ME1228; Shibahara S et al.; Aminothiazolylacetamidocephalosporins having 1-carboxyethoxyimino groups were synthesized and found to have excellent antibacterial activities including anti-pseudomonal activity and low toxicities . Among these cephalosporins, ME1228 having (S)-1-carboxyethoxyimino substituent and being combined with an (N-ethyl-4-pyridinio)thiomethyl group at C-3 showed marked therapeutic effects against systemic infections in mice and was selected as the best candidate for further evaluation.

Vet Clin North Am Small Anim Pract, 1990 Jan, 20(1), 47 - 65
Bandages and topical agents; Swaim SF; Bandages are included in the regimen of therapy of superficial wounds . Bandages have varying functions depending upon the type of wound to which they are applied . When bandaging recently inflicted open wounds, the primary bandage layer may be dry-to-dry, wet-to-dry, or wet-to-wet, depending upon the type of tissue and exudate present on the wound . These bandages aid in debriding and cleansing a wound . The secondary layer of such bandages serves primarily to absorb material from the wound, and the tertiary bandage layer serves to hold the other bandage layers in place . Once an open wound is well into the repair stage of healing, an occlusive bandage may be considered to help enhance epithelialization of the wound . Bandages for wounds associated with compound fractures must include some form of fixation for the fracture . Other types of bandages are designed to (1) cover closed wounds, (2) provide pressure over a wound, and (3) relieve pressure over wounds or impending wounds . Bandages for closed wounds provide protection and allow for absorption of exudate that may be present . Pressure bandages are used to control minor hemorrhage, edema, and excess granulation tissue . With impending decubital ulcers, actual decubital ulcers, or repaired decubital ulcers, it is necessary to have a bandage designed to relieve pressure over the lesion . Many substances have been described for topical application to wounds . This section presents information on some substances available to or commonly used by veterinarians . It includes information on the wound lavage solutions chlorhexidine diacetate, povidone-iodine, hydrogen peroxide, and sodium hypochlorite solutions . Topical antibacterial agents are used to help prevent wound infection . The triple antibiotics, silver sulfadiazine, nitrofurazones, and gentamicin sulfate are some commonly used antibacterial agents . Hydrophilic agents are used to diffuse fluids through the wound tissues to bathe the tissues from the inside . Dry starch copolymer flakes and dextran polymer beads are two substances that help bathe the wound with the body's own fluids . Other topical medications are used to selectively act upon various wound tissues and exudates to aid in cleansing the wound; these include organic acid preparations and enzymatic debriding agents . In addition, a live yeast-cell derivative has been described for enhancing tissue oxygen consumption, epithelialization, and collagen synthesis in wounds.

Am Rev Respir Dis, 1990 Jan, 141(1), 79 - 83
Effects of orally administered drugs on dynamic viscoelasticity of human nasal mucus; Majima Y et al.; The effects of orally administered drugs on rheologic properties of nasal mucus were investigated in adult chronic sinusitis patients . The elastic modulus G' and the dynamic viscosity eta' of nasal mucus were determined by an oscillating sphere magnetic rheometer . Both G' and eta' values of the mucus before drug administration were much higher than optimal viscoelasticity for mucociliary transport . Norfloxacin, an antibacterial agent, reduced the G' but not the eta' of nasal mucus . Serratiopeptidase, a proteolytic enzyme, reduced eta' but did not reduce G' . S-carboxymethylcysteine, a blocked thiol derivative of cysteine, did not change either G' or eta' . L-cysteine ethyl ester hydrochloride, a sulfhydryl type of agent, reduced both G' and eta' . The results indicate that some of the orally administered mucokinetic agents can improve the abnormal rheologic properties of nasal mucus in chronic sinusitis.

J Med Chem, 1990 Jan, 33(1), 434 - 44
Antifolate and antibacterial activities of 5-substituted 2,4-diaminoquinazolines; Harris NV et al.; A series of 5-substituted 2,4-diaminoquinazolines (3) has been synthesized and evaluated as inhibitors of the enzyme dihydrofolate reductase (DHFR) from both bacterial and mammalian sources . The best compounds (e.g . 53) show good activity against Escherichia coli DHFR, but there is no significant selectivity for the bacterial over the mammalian enzyme . The structure-activity relationships for enzyme inhibition appear to be complex and not amenable to simple analysis; a hypothesis to explain the observed qualitative structure-activity relationships is proposed . The inhibitory activities of the compounds against the growth of intact bacterial cells in vitro closely parallel those for the inhibition of the isolated bacterial enzymes, suggesting that their antifolate action is responsible for their antibacterial effects . Five of the compounds were tested for their ability to cure a systemic E . coli infection in the mouse, but they showed no therapeutic effects at their maximum tolerated doses.

J Med Chem, 1990 Jan, 33(1), 291 - 7
Cephalosporins to carbapenems: 1-oxygenated carbapenems and carbapenams; Rosati RL et al.; The photo "Wolff" rearrangement of readily available 2-diazoceph-3-em oxides (1) directly affords carbapen-2-ems, allowing a facile entry into a ring system previously accessible only by total synthesis, lengthly semisynthesis or fermentation . The chirality of the cephalosporin is accurately translated into the corresponding carbapenem . The resulting 1-oxocarbapenems (2) were selectively transformed through reduction into 1-oxygenated carbapenems and carbapenams (3 and 4, respectively) . On microbiological screening, a carbapenem (3c) was found to possess a broad spectrum of activity . An interesting antibacterial profile was discovered for a carbapenam (26).

Pediatriia, 1990, (3), 23 - 8
{Clinical variants of pneumococcal pneumonia and the characteristics of its course and outcome}; Manerov FK et al.; The authors relate the results of examining 92 patients with acute pneumococcal pneumonia (APP) . The bacteriological methods of studying the tracheal contents and pleural exudate, performed before treatment turned out highly informative . As regards the course of APP, the bacteremic , classic (infiltrative) and pleurisy-complicated varieties were distinguished . It was established that the bacteremic variety of APP may be accompanied by bactericidal shock eventuating in a lethal outcome which is not observed in other varieties . 19.6% of patients with APP demonstrated abacterial fever and 27.1% severe pleuropulmonary complications . The development of the latter ones is predictable according to the presence of pleurisy and fever lasting over 5 days . An opinion is advanced that the continuance of antibacterial therapy over 5 days is not desirable whatever the APP variety.

Ter Arkh, 1990, 62(3), 75 - 8
{The effect of adequate therapy on the indices of external respiratory function in patients with arterial hypertension combined with obstructive lung diseases}; Katiukhin VN et al.; In patients with associated arterial hypertension and obstructive lung diseases, external respiratory function was established to return to normal thanks to adequate hypotensive therapy and administration of the cholinolytic agents combined with antibacterial and antiinflammatory treatment.

Trans R Soc Trop Med Hyg, 1990 Jan-Feb, 84(1), 129 - 31
Diagnosis of typhoid fever in Nigeria: misuse of the Widal test; Onuigbo MA; In the last 2 years, there has been public panic across Nigeria about an epidemic of a 'killer' febrile disease, purportedly typhoid fever . The evidence for this epidemic is reviewed in the light of appropriate diagnosis of typhoid fever . All the patients were diagnosed as typhoid fever, primarily based on Widal test results . Investigations in the hospital of 15 patients confirmed malaria in 70% who, though failing to respond to chloroquine, promptly responded to treatment with Fansidar (sulfadoxine + pyrimethamine) . Fever in the remaining 30%, without evidence of malaria and who failed to respond to chloroquine, Fansidar and antibacterials including chloramphenicol, remitted spontaneously . The merits and limitations of the Widal test are discussed . It is concluded that diagnosis of typhoid fever by the Widal test alone is prone to error, and that any claims of a typhoid fever epidemic in Nigeria remain mere conjecture . Misuse of the Widal test and, subsequently, misuse of the antibiotic chloramphenicol, should be very strongly condemned.

Probl Tuberk, 1990, (2), 41 - 3
{Use of laser therapy in combined treatment of pulmonary tuberculosis in children and adolescents}; Badalov RK et al.; The effect of 0.89 micron wave gallium arsenide laser radiation was studied on 19 patients with various forms of pulmonary tuberculosis . Laser therapy was conducted in combination with antibacterial drugs . Laser skin radiation was projected into the pathologic process . The regimen included 15 sessions at 7-day intervals . The use of laser energy in the complex management of pulmonary tuberculosis patients makes it possible to reduce lung destruction healing and to accelerate normalization of biochemical indices and their hemogram.

Toxicon, 1990, 28(3), 275 - 83
Effect of antibacterial plant flavanones on the intracellular calcium compartment involved in the first cleavage of sea urchin eggs; Biyiti L et al.; Two plant flavanones, (Sigmoidin A and B) having noticeable antibacterial activity, were assayed using a preparation for the study of sea urchin egg cleavage . When added after insemination, both toxins inhibit egg division with a half maximal dose of 7.5 microM for Sigmoidin A and 12 microM for Sigmoidin B . The first Ca2+ signal following fertilization was not modified by the molecules, however, the intracellular storage of calcium in isolated non-mitochondrial compartments was reduced in a dose-dependent manner by Sigmoidin A and Sigmoidin B . Both trigger a complete discharge of the sequestered calcium . In vivo the flavanones dramatically reduced the capacity of storage of non-mitochondrial intracellular calcium compartments necessary to the cyclical elevation of cytosolic free calcium during the cell cycle.

Chem Pharm Bull (Tokyo), 1990 Jan, 38(1), 116 - 22
Synthesis and antibacterial activity of lactivicin derivatives; Tamura N et al.; The chemical modification of the 4-acetylamino group on the cycloserine moiety of lactivicin (1a) was carried out . The lactivicin derivatives (1d, k--p and w) having heterocyclic acylamino groups which have been often utilized in beta-lactam antibiotics showed potent antibacterial activities . Ester prodrugs (7a--d) of lactivicin derivatives were also prepared in order to improve the bioavailability on oral administration . The pivaloyloxymethyl (POM) esters (7a and 7b) and 1-ethoxycarbonyloxyethyl (EOE) ester (7c) were found to have slightly improved protective effect in vivo compared with their parent compounds 1c and 1k.

Urol Nefrol (Mosk), 1990 Jan-Feb, (1), 59 - 62
{A comparative evaluation of surgical methods for treating hydrocele}; Dunaevskii IaL et al.; The authors analysed the results of the surgical treatment of 167 patients with hydrocele who were operated on with the use of Winkelmann's or Bergmann's technique (group I), the same but modified by Grebenshchikov-Shevtsov's (group II), and Lord's method (group III) . Sclerotherapy was employed in the group IV patients . A high percentage of complications was associated with Winkelmann and Bergmann's techniques (scrotal edema, hematoma, wound purulence) when the hydropic sac was isolated from the adjacent tissues . Postsurgical staying-in-bed time for those operated on with Winkelmann's and Bergmann's technique was mean 8.6 +/- 1.2 days and 9.4 +/- 1.3 days, respectively . When the same surgery was performed according to the Grebenshchikov-Shevtsov's modification a mean staying-in-bed time reduced to 7.2 +/- 0.9 days due to a lower incidence of postsurgical complications . Analysis of 42 surgeries performed with the Lord's method which avoided the isolation of the hydropic sac from the adjacent tissues demonstrated its efficacy and simplicity . No hematomas, suppurations or relapses were documented . The staying-in-bed time was 3.4 +/- 0.6 days . The pronounced changes in tunica propria and the multilocular character of hydrocele were the contradictions to this pattern of the treatment . In case the performance of the surgery was impossible, sclerotherapy with administration of 2-10 ml of 2.5 per cent of tetracycline solution was performed for the sclerosing and antibacterial effect . A mean staying-in-bed time was 2.1 +/- 0.9 days . Seven out of 8 patients recovered after 1-3 sessions of sclerotherapy.

J Inorg Biochem, 1990 Jan, 38(1), 57 - 67
Coordination behavior and antifungicidal, antibacterial, and antifertility activities of dioxomolybdenum(VI) complexes of biologically active heterocyclic benzothiazolines; Kanoongo N et al.; Synthesis, characterization, and structural aspects of a new class of dioxomolybdenum(VI) complexes with biologically active benzothiazolines, 2-(2-pyridyl) benzothiazoline, 2-(2-thienyl) benzothiazoline, 2-(2-furyl) benzothiazoline, 2-(3-indolyl) benzothiazoline, glyoxal benzothiazoline, biacetylbenzothiazoline, benzil benzothiazoline, and terphthaldehyde benzothiazoline have been described . The newly synthesized complexes, {MoO2(Bzt)2} and {MoO2(Bzt')} (where BztH and Bzt'H2 represent benzothazoline molecules) have been characterized by elemental analysis, conductance measurements, molecular weight determinations, and magnetic studies . Based on IR, 1H NMR, 13C NMR, and electronic spectral studies, distorted octahedral geometry with cis-MoO2 group has been indicated for the resulting complexes . Two benzothiazolines and their corresponding metal complexes were screened for their antifungicidal and antibacterial activity on several fungi and bacteria and found to be quite active in this respect . In addition, antifertility activity of representative ligands and their molybdenum complexes was also evaluated and discussed in male mice.

Comp Biochem Physiol B, 1990, 95(1), 71 - 5
Antibacterial activity of Eisenia fetida andrei coelomic fluid: transcription and translation regulation of lysozyme and proteins evidenced after bacterial infestation; Hirigoyenberry F et al.; 1 . After bacterial infestation lysozyme and antibacterial activities are enhanced, peaking at 4 hr and 3 days, respectively . 2 . Both humoral defenses require RNA and protein de novo synthesis in response to pathogenic bacteria injection (actinomycin D and cycloheximide experiments) . 3 . Antibacterial activity exists naturally at some basic level, involving regular translation of stable RNAs . 4 . When antibacterial activity reaches its maximum after bacterial injection, proteins responsible for it undergo a turn-over . 5 . Lysozyme and antibacterial proteins cannot account for the whole response to bacterial infestation; some cellular defense mechanisms like phagocytosis are involved at the same time.

Microbios, 1990, 61(248-249), 181 - 4
Antibacterial activity of the essential oil of Thymus serpylloides subspecies gadorensis; Crespo ME et al.; The in vitro antibacterial activity of the essential oil obtained from the flowering apex of Thymus serpylloides ssp . gadorensis against various micro-organisms is reported . Moreover, the main chemical groups found in this essential oil are described.

Stomatologiia (Mosk), 1990 Jan-Feb, 69(1), 35 - 6
{A method for treating acute serous lymphadenitis by the action of novocaine block of the cervical autonomic ganglia}; Timofeev AA et al.; Thirty-five patients with acute inflammations of the soft tissues were treated with procain blockages of the cervical sympathetic ganglia . This treatment modality has helped cut down the patients' hospitalization period by 3-4 days and did not involve therapy with other drugs, this being an important factor for patients with antibacterial drug allergies, contributing to improvement of the efficacy of the suggested method.

J Antimicrob Chemother, 1990 Jan, 25(1), 175 - 81
Predictive value of susceptibility tests for the outcome of antibacterial therapy; Lorian V et al.; A total of 510 charts of patients who received antibacterial agents were examined for clinical outcome and microbiology findings . A total of 382 patients (75%) had one or more specimens submitted for culture and susceptibility tests before the administration of the drugs; 298 (78%) of these had positive cultures and susceptibility tests were done . A total of 18 species were isolated . Of the 298 patients with organisms of known susceptibilities, 271 (91%) received antibacterial agents to which the respective organisms were susceptible and 219 of these patients (81%) improved (P less than 0.05) . This high rate of good infectious diseases practice is probably due to two factors: (1) susceptibility tests results were available in most cases the next day after the submission of a specimen; (2) the medical board distributed guidelines for the use of antibiotics and monitored the compliance closely . The patients treated with antibacterial agents to which the bacteria were resistant improved in 3% and did not improve in 82% (P less than 0.05) of the patients . This study shows that choosing an antibacterial agent in accordance to the susceptibility test resulted in a high rate of improvement . When the choice of agent disregarded bacterial resistance in vitro, therapy almost always ended in failure . Therefore, susceptibility tests in vitro have a good predictive value for the outcome of antibacterial therapy.

J Periodontol, 1990 Jan, 61(1), 30 - 4
In vitro release of doxycycline from bioabsorbable materials and acrylic strips; Larsen T; Treatment of marginal periodontitis may include use of local antibiotics . In the present in vitro study the bioabsorbable materials Surgicel, Tissell, and CollaCote and acrylic strips were examined for release of doxycycline into liquids and residual antibacterial activity of the materials . Pieces of material were incubated in 1 ml of water or human serum which was exchanged every day for 9 days . The concentration of doxycycline in the liquids was measured spectrophotometrically while the residual antibacterial activity of the materials was determined microbiologically . Surgicel constantly showed very high concentrations and level of residual activity . The acrylic strip and CollaCote decreased to low levels of both concentration and residual activity in a few days . Tissell was intermediate with a continuous decrease in concentration but rather high level of residual activity throughout the study . In serum the acrylic strip was partly dissolved and Surgicel was totally dissolved after 2 days . Left undisturbed in serum Surgicel was not dissolved for 2 weeks . These results indicate that Surgicel and Tissel may be capable of prolonged release of doxycycline in vivo.

J Clin Chem Clin Biochem, 1990 Jan, 28(1), 19 - 23
Antibodies from colostrum in oral immunotherapy; Stephan W et al.; An immunoglobulin preparation for oral use was prepared from pooled bovine colostrum from more than 100 animals . The preparation has high antibacterial antibody titres, and a high capacity for the neutralization of bacterial toxins . It is well tolerated and highly effective in the treatment of severe diarrhoea, e.g . in AIDS patients . The preparation is spray-dried and stable at 2-8 degrees C.

Dtsch Tierarztl Wochenschr, 1990 Jan, 97(1), 5 - 10
{Metaphylaxis and therapy of the MMA syndrome of sows with Baytril}; Schoning G et al.; The efficiency of antibacterial metaphylaxis and therapy on the control of the MMA-syndrome has been investigated in a large breeding-herd with a total of 828 sows in the study . For this the recently developed quinolone-derivate Baytril was used . Feed medication with furazolidone and sulfadimidine reduced the incidence of disease to 29.7% (control 41.3%), injection of Baytril on the day of parturition reduced it to 10.8% (using a dosage of 1.25 mg/kg body weight) respectively 6.8% (dosage 5 mg/kg) . Treatment also resulted in a lower incidence of elevated milk-pH (greater than 6.7) . The development of piglets was good in all groups of metaphylaxis . Litters of sows which had been treated with Baytril as prophylaxis or therapy had no low extremes in the weight gains of the piglets . In the treatment of MMA-affected animals Baytril was significantly superior as compared to Trimethoprim-Sulfonamide, if a dosage of 5 mg/kg body weight was used . Using a dosage of 1.25 mg/kg body weight both drugs had the same effect . Even at the end of the five month of the study there was no isolation of bacteria resistant against Baytril.

Ther Drug Monit, 1990 Jan, 12(1), 65 - 71
Single oral dose pharmacokinetics of erythromycin and roxithromycin and the effects of chronic dosing; Birkett DJ et al.; Roxithromycin is a semisynthetic macrolide antibiotic having similar in vitro antibacterial profile and potency to erythromycin but possibly greater in vivo potency . The single and multiple oral dose pharmacokinetics of roxithromycin and erythromycin were studied in 12 healthy volunteers . Plasma concentrations of the two compounds were measured by a sensitive and specific high-performance liquid chromatographic method using electrochemical detection . After single doses, roxithromycin 150 mg gave a Cmax 3.3-fold higher and an area under the curve (AUC) 16.2-fold higher than erythromycin 250 mg . The half-life for roxithromycin was 12.42 +/- 3.94 h compared with 1.53 +/- 0.42 h for erythromycin . On multiple dosing, the AUC over a dosing interval for erythromycin (250 mg, six hourly doses) was increased 2.3-fold compared with the single dose, whereas that for roxithromycin (150 mg, 12 hourly) was decreased by 25.4% . Because of these opposing changes during chronic dosing, the average plasma roxithromycin concentration over the dosing interval was 2.6-fold higher than that for erythromycin, which was a smaller excess than would have been predicted from the single dose data . The results suggest that roxithromycin exerts less inducing and inhibiting effects on human cytochrome P450 than erythromycin . Roxithromycin has a favorable pharmacokinetic profile suitable for twice daily dosing and may have a lower potential than erythromycin for cytochrome P450-mediated drug interactions.

Intensive Care Med, 1990, 16 Suppl 3, S229 - 34
Impact of dosage schedule of antibiotics on the treatment of serious infections; Bakker-Woudenberg IA et al.; Experimental studies suggest that the importance of the antibiotic dosage schedule for therapeutic efficacy in severe infection and when host defences are impaired is related to the class of antibiotic . The efficacy of beta-lactams is mainly dependent on the maintenance of adequate antibiotic concentrations in plasma during the entire treatment interval, and not on high peak concentrations . The efficacy of aminoglycosides is related to the total dose administered, i.e., the area under the concentration-time curve, irrespective of the frequency of administration . This difference in efficacy between beta-lactams and aminoglycosides in relation to the dosage schedule correlate well with differences between both classes of antibiotics in kinetics of antibacterial activity in vitro and in vivo . Another factor relevant in this respect is the post-antibiotic effect (PAE) which means the suppression of bacterial regrowth at the end of the period of exposure to antibiotic.

Pediatr Radiol, 1990, 21(1), 23 - 6
Pre-suppurative phase of retropharyngeal infection: contribution of ultrasonography in the diagnosis and treatment; Ben-Ami T et al.; Pre-suppurative phase of retropharyngeal infection can't be differentiated from retropharyngeal abscess clinically or radiographically . Ultrasound, however, can diagnose this common infection in early phase . Early antibacterial treatment prevents the suppurative phase, obviates surgery and shortens the hospitalization phase.

Biomater Artif Cells Artif Organs, 1990, 18(4), 555 - 68
Peroral application of synthetic activated charcoal in USSR; Nikolaev VG; This work presents a review of the enterosorption procedure, spheres of its application, the results achieved and prospects for use in the future . This technique was developed by the author in the late 1970's and is based on peroral administration of high doses of synthetic activated carbons . This review also summarises new experimental and clinical reports by Soviet researchers who studied the use of enterosorption procedure in liver and biliary tract diseases, endogenous intoxications, acute intestinal infections, renal pathologies and immuno-dependent diseases, metabolism in aged animals, in oncologic patients, abstinence syndrome in alcohol and drug-abuse patients . The peroral application of activated carbons has been known for a long time . The most extensive list of usage of activated carbons has been presented by Adler in the first quarter of this century . The powdery activated charcoal usually was prescribed in doses of 2-10 g per day, since larger doses caused nausea, vomiting and constipation, and that demanded simultaneous usage of cathartics . The Carbon sorption therapy, soon became neglected owing to development of potent antibacterial preparations, and probably due to depleted enteric content of the components which are necessary for the organism . Later, carbon sorption therapy was investigated for use in uremia . In 1979, the author of this article proposed the use of oral administration of high doses (up to 100-150 g/day) of synthetic activated carbons with diameters 0.2-1.0 mm, derived through pyrolysis of various polymeric resins . The reasons for this approach which we termed enterosorption, were good adsorptive properties, smooth surface, strength and uniformal nature of synthetic carbon adsorbents, causing practically no symptoms of enteropathy which are typical for high doses of powdery carbons . We have described our earlier clinical results of this approach . Since that time the number of studies has substantially increased in the USSR . Accordingly, the author deemed it expedient to attempt a review of the results.

Pediatriia, 1990, (10), 33 - 8
{Sensitization of lymphocytes from newborn infants and young children to pathogenic and opportunistic microflora}; Gavrilova LO et al.; The nucleolar test was used to study sensitization of peripheral blood lymphocytes from the newborn and infants . The test is based on the counting of cells with a clarification area around nucleoli after incubation with antigens and microbial bodies of the pathogenic and opportunistic microflora . It has been established that the peripheral blood from children with infectious-inflammatory diseases and from those vaccinated with BCG shows an increase in the sensitized lymphocyte count which is influenced by child's trophicity at birth and by administration of antibacterial therapy . The use of the nucleolar test as a diagnostic aid is advisable to identify the disease etiology.

J Int Med Res, 1990, 18 Suppl 4, 48D - 57D
Overcoming enzymatic resistance in bacteria: impact on future therapy; Labia R et al.; Resistance of bacteria to antibiotics often involves inactivating enzymes . One approach developed to overcome this mechanism of resistance consists of combining an efficient but possibly unstable antibiotic with a powerful inhibitor of the inactivating enzyme . Attempts have been made with different antibiotics but significant success has only been obtained with the beta-lactams, clavulanic acid and sulbactam being the only compounds currently being used clinically . Sulbactam, a time-dependent irreversible inhibitor of plasmid-mediated penicillinases and of chromosomally mediated penicillinases and cephalosporinases, potentiates the antibacterial activity of beta-lactams but only exhibits a moderate antibacterial activity, which is related to its affinity for the lethal targets of the beta-lactams--the penicillin-binding proteins . In bacterial strains that produce either low amounts of beta-lactamase, or none at all, a synergistic effect can be observed when sulbactam is associated with a beta-lactam antibiotic that has a complementary affinity for the target sites.

Ter Arkh, 1990, 62(9), 111 - 6
{The immunomodulating effect of sodium nucleinate in chronic infectious-allergic urticaria}; Zemskov VM et al.; Based on clinical, laboratory, bacterial, allergologic and immunologic studies a group of patients with infectious allergic urticaria (IAU) was distinguished . The immunologic examination of 30 patients with IAU identified a decrease in phagocytosis . Sodium nucleinate (SN) was employed as an immunomodulator as compared to placebo . SN was noted to produce an optimal immunomodulating effect, provided it was combined with antibacterial drugs . The use of SN in patients with IAU produced a good clinical effect elucidated for 6 months . It is recommended that SN be used as an immunomodulator in the multimodality therapy of IAU and introduced into the practice of the allergological rooms.

Ter Arkh, 1990, 62(9), 100 - 5
{The clinical aspects of using plasmapheresis in sepsis}; Gorshkov MP et al.; The rise of the sepsis incidence at therapeutic hospitals, the emergence of new forms and evolutionally new mechanisms of infection, insufficient efficacy of antibacterial therapy necessitate the search of novel approaches to the treatment of sepsis . The use of plasmapheresis (PP) in 27 sepsis patients allowed a two-fold reduction of the lethality as compared to that in the control group . The main mechanisms by which PP acts may involve deblockade of the system of phagocytosing mononuclears, enhancement of the efficacy of antibacterial therapy, protective action on the system of natural detoxication of the body.

Scand J Plast Reconstr Surg Hand Surg, 1990, 24(3), 199 - 205
Antibacterial activity of rosin and resin acids in vitro; Soderberg TA et al.; The antibacterial effects of rosins and resin acids were studied in vitro using three methods, disc diffusion on agar, agar dilution, and broth dilution . Rosin and some resin acids had antibacterial effects that were restricted to Gram-positive bacteria . The abietic type of acids had a more pronounced antibacterial activity than the pimaric and labdane acids when the disc diffusion method was used but there was no inhibition of growth of Gram-negative bacteria . Among the individual resin acids, dehydroabietic acid was generally the most potent, when disc diffusion on agar was used, and prediffusion increased the inhibitory effect . The composition of the pure resin acids dehydroabietic, neoabietic, and isopimaric acid did not change during the experiment, but abietic and levopimaric acid were converted into dehydroabietic acid by the addition of Muller-Hinton agar . In conclusion the old tradition of treating wounds with pitch, sap, rosin, or rosin containing tapes might therefore have some antibacterial relevance.

Klin Khir, 1990, (10), 30 - 2
{Treatment of acute nonspecific empyema}; Safarov IS et al.; The experience with treatment of 104 patients with non-specific pleural empyema without bronchial fistula is summarized . The local use of antibacterial agents in combination with proteolytic enzymes against the background of rational general immunocorrective therapy permitted to cure without operative intervention 124 patients . Four patients were operated on . They underwent decortication of a lung with pleurectomy . One patient died.

Klin Khir, 1990, (10), 17 - 8
{Pharmacodynamics of antibiotics in their preventive use in heart surgery with general artificial circulation}; Krastin OA et al.; Pharmacodynamics of antibiotics in their prophylactic use was studied in 100 operations with artificial circulation, which were performed in patients with rheumatic heart defects . It was established that at the time of operation and after it, the antibiotic excreted via the kidneys insignificantly++, within the whole period of intracardiac stage of the operation, the myocardium remained without the antibacterial protection, and required the local use of an antibiotic.

Probl Tuberk, 1990, (9), 32 - 4
{Follow-up studies of children who had postvaccination lymphadenitis}; Gaitnietse RIa et al.; Analysis of the examination findings from of 80 children who had postvaccination lymphadenitis in their early childhood was made . The observation period covered 8-10 years . Regional lymphadenitis in the infiltration stage was detected in 23 (28.8% of the children); in the abscess formation stage in 42 (52.5%); and in the calcification stage in 15 (18.7%) . The children were treated with antibacterial drugs for 2-4 months, thus producing positive results . However, 1 or 2 years after recovery there were 5 recurrent cases . During 8-10 years which followed BCG vaccination none of the 80 children had tuberculosis . The study proves the fact the cured postvaccination lymphadenitis does not affect the formation of antituberculous immunity.

Klin Khir, 1990, (9), 12 - 5
{Comprehensive therapy of obstructive jaundice with neoplastic origin}; Buianov VM et al.; The authors treated 67 patients with jaundice on the ground of biliopancreatoduodenal tumors . Of them, 49 underwent the palliative operations . In 31 patient, the conventional two-stage treatment was employed . The postoperative complications occurred in 28.6% of the patients . The lethality was 20.8% . Examination for 1-3 days, intensive preoperative preparation, antibacterial prophylaxis, regional chemotherapy were performed in 18 patients . The incidence of postoperative complications in these patients was 11.2%, the lethality--5.6%.

Grud Serdechnososudistaia Khir, 1990, (10), 59 - 61
{Effectiveness of therapeutic and surgical treatment after delayed detection of destructive pulmonary tuberculosis}; Kariev TM et al.; The authors studied the results of antibacterial therapy in 647 and the results of surgical treatment in 837 patients . Complex modern antibacterial therapy led to recovery of only 65% of patients, in 20-25% of patients tuberculosis progressed with the formation of chronic forms, lethality was up to 13.0% . Timely undertaken surgical treatment after an ineffective course of antibacterial therapy facilitated stable recovery of 98% of patients with complete restoration of working capacity in 93.2%.

Stomatol DDR, 1990 Jan, 40(1), 9 - 11
{Effect of helium-neon-laser radiation on microbes}; Zimmermann M; In a well-defined in-vitro experiment the effects of a He-Ne-laser of 6 mW output on some dominating microbes in the oral cavity were studied by using a scanning electron microscope . No changes on the surface in the irradiated colonies could be seen even after an exposition lasting for 60 minutes (continuous or pulsated wave) . Therefore an antibacterial effect of softlaser-irradiation sometimes described in literature in questionable.

Scand J Infect Dis, 1990, 22(5), 581 - 4
Fungemia with Saccharomycetaceae . Report of four cases and review of the literature; Nielsen H et al.; Invasive fungal disease with Saccharomycetaceae is very rarely reported and these fungi are usually considered nonpathogenic . We report here 4 cases of positive blood cultures with fungal species belonging to this family . Severe neutropenia, permanent central venous catheter, ongoing antibacterial chemotherapy, and major abdominal surgery were identified as risk factors for fungemia in patients . In the immunocompromised host isolation of such species from sterile fluids cannot be ignored but should be considered an opportunistic infection and treated as such.

Chemotherapy, 1990, 36(4), 251 - 3
Penetration of aminoglycosides into human peritoneal tissue; Serour F et al.; Each of 30 patients underwent elective laparotomy following administration of a single intravenous dose of amikacin, netilmicin or tobramycin . Therapeutic concentrations of amikacin were achieved in peritoneal tissue in 10/10 patients . Only 13/20 samples from patients receiving the other two antibiotics showed antibacterial activity . Our data suggest that the penetrability of tobramycin (53%) and amikacin (39%) into the uninflamed peritoneal tissue is superior to that of netilmicin (16%).

Vet Res Commun, 1990, 14(5), 403 - 10
A comparison of some of the pharmacokinetic parameters of three commercial sulphadiazine/trimethoprim combined preparations given orally to pigs; Soli NE et al.; Three sulphadiazine/trimethoprim preparations were administered orally during feeding to pigs . Six male and six female pigs were used . Clinically important pharmacokinetic parameters of the two drugs in the three preparations were determined and compared . The plasma concentrations of sulphadiazine and trimethoprim increased rapidly in the pigs followed by a quite rapid decrease from 4 to 12 h after oral administration . The mean values of the absorption half-lives of sulphadiazine and trimethoprim were 0.9-1.6 h and 0.5-0.8 h, respectively . The corresponding values for the elimination half-lives of sulphadiazine and trimethoprim were 3.1-4.3 h and 3.4-6.0 h, respectively . There were no significant differences between the pharmacokinetic parameters of the two compounds in the three preparations with the exception of Tmax for sulphadiazine and t 1/2 beta for trimethoprim . Comparative bioavailability calculations showed no statistically significant differences between sulphadiazine and trimethoprim in the three preparations . The weight increase of the pigs during the experimental period (mean = 37.3-64.9 kg) did not cause differences in the kinetics of the two drugs which could have consequences for the use of the three combined preparations in clinical practice . No unacceptable or antibacterial residues of sulphadiazine or trimethoprim were found in the kidneys of pigs slaughtered at 5, 7 and 10 days after administration.

Parasitology, 1990, 100 Suppl, S53 - 61
The evolution of inducible defence; Harvell CD; Defences against parasites are characterized by inducible, amplifiable responses, often with a memory component . Inducible defences with similar properties are common in a variety of other types of interactions, for example many aquatic invertebrates produce inducible structural defences against their predators and competitors . Most inducible defences have the following properties: (1) a threshold of activation; (2) an amplification of response with increasing stimulus; (3) a memory component . Specificity, amplification and memory are the basis for defining a defence as 'immune' (Klein, 1982), and these properties are present in both the vertebrate and invertebrate internal defence responses to pathogens . Invertebrates differ in the absence of immunoglobulins and therefore in reduced specificity . Although the reduced specificity of invertebrate internal defence systems is often viewed as proof of their 'primitiveness', the differences in defence systems of vertebrates and invertebrates may be more related to their respective selection regimes than to phylogeny . The syngeneic recognition system of vertebrates functions to recognize small departures from self, such as would arise from neoplasia . Are vertebrates under more intense selection from neoplasia, perhaps due to a greater incidence of hormonal imbalance or hypersensitivity reactions? The invertebrate internal defence systems are all less discriminating than the vertebrate, but there are marked differences in degree of discrimination depending on whether the group is colonial or not . Even the phyla of colonial animals with quite simple body plans, the sponges and cnidarians, have a more discriminating recognition system than the phyla of solitary animals with more complex body plans, such as the molluscs and arthropods . The primary effectors of all invertebrate responses to parasites are encapsulation and phagocytosis, although in some phyla there are specific antibacterial proteins than can also be induced.(ABSTRACT TRUNCATED AT 250 WORDS)

Vestn Akad Med Nauk SSSR, 1990, (6), 44 - 7
{Anti-inflammatory effects of liposomes}; Kreines VM et al.; Studies of antiexudative, antialterative, and antibacterial effects of lecithin-cholesterol liposomes suggest their possible use as antiinflammatory agents . It is shown that incubation of liposomes with opportunistic microorganisms is attended with a pronounced antibacterial effect, while subcutaneous injection of liposomes significantly reduces the soft tissue edema caused by administration of formalin, and prevents pronounced alteration in response to acetic acid solution . A conclusion is derived on the possibility to use the membranotropic properties of liposomal membranes to alleviate manifestations of inflammation.

Vestn Akad Med Nauk SSSR, 1990, (6), 40 - 4
{Ectericide as a dispersion medium for the preparation of prospective clinical liposomal drug forms}; Dikii IL et al.; The possibility of using ectericide, having antibacterial, detergent, antioxidative, and reparative effects, as a dispersion medium for liposome production has been studied . Its application allows for elaboration of a simplified liposome production technique simultaneously imparting them stability against oxidation, heating, and pH changes . A technology to produce multivesicular liposomes with ectericide++, containing rifampicin in the membranous envelope and gentamicin in the inner volume, has been developed . Liposomal antibiotics proved to be effective in clinical trials.

Prog Med Chem, 1990, 27, 235 - 95
The fluoroquinolone antibacterial agents; Rosen T; In summary, the last decade has been a highly fertile and productive period in quinolone medicinal chemistry, resulting in major improvements in potency, antibacterial spectra, oral absorption and pharmacokinetic properties as well as an increased knowledge of the molecular features important to conferring these various properties . Very recent discoveries concerning replacements for the 3-carboxylic acid moiety, previously thought to be uniquely essential for activity, to give highly potent antibacterials such as (83) illustrate the potential for new breakthroughs in this field . Among the major goals for future research remains the understanding of the potential cartilage toxicity associated with this class of agents, such that an agent useful for pediatric indications may be developed . Future studies can also be expected to further enhance and refine the level of current insight into the manner by which these agents inhibit the target enzyme on a molecular level.

Probl Tuberk, 1990, (6), 52 - 6
{The state of the liver in rabbits during combination chemotherapy of experimental disseminated tuberculosis}; Mozhokina GN; Functional and morphologic changes in the liver condition of experimental rabbits were studied in the process of the disseminated tuberculosis development and treatment . Medication of the animals was started 2 weeks after the infection at the peak of the process and continued for 60 days . In Group 1 of the rabbits, isoniazid and rifampicin were administered enterally in combination with intramuscular streptomycin, and in Group 2, isoniazid and rifampicin were given intravenously plus intramuscular streptomycin . The doses of the antibacterial drugs were adequate, as compared to the clinical ones . It was shown that an intravenous administration of isoniazid and rifampicin supplemented by intramuscular streptomycin resulted in more pronounced normalization of processes in the liver morphologic and functional changes caused by tuberculosis than an enteral route of administration of the drugs.

Probl Tuberk, 1990, (6), 38 - 41
{The results of antibacterial therapy combined with prodigiozan in children with tuberculosis}; Makhamatov KM et al.; The paper presents the findings of a clinico-roentgenologic and immunologic follow-up of 100 children aged 3-14 years . The efficacy of the antibacterial treatment of children with different forms of intrathoracic tuberculosis supplemented by prodigiosan as well as that of prodigiosan alone were analysed by means of clinical, X-ray, laboratory and immunologic methods . By increasing the body reactivity, prodigiosan can promote higher rates of resolution of pathologic changes in the lungs . The data of this study permit one to recommend prodigiosan as an effective non-specific impact method in the combined treatment of tuberculosis in children.

Probl Tuberk, 1990, (6), 11 - 5
{The use of argon laser coagulation in the combination treatment of patients with tuberculous chorioretinitis}; Ustinova EI et al.; The outcomes of argon laser coagulation (ALC) of active tuberculous chorioretinal foci (mainly of exudative and hemorrhagic nature, macular and paramacular localization) in 26 patients are illustrated . The coagulation was performed concurrently with a combined general and local antituberculosis therapy (with 48 patients as controls) . The developed direct ALC technique was used together with antibacterial therapy of the total surface of the inflammation focus itself . The examination findings prove that the effectiveness of the above technique is high, since the disappearance of the clinical signs of the inflammatory activity is achieved in a relatively short time (45 days); acute conditions and relapses are prevented; complications are excluded; and an evident economic effect is produced (the shorter period of hospitalization, less duration of the main therapeutic regimen and lower frequency of relapses).

Arzneimittelforschung, 1990 Jan, 40(1), 69 - 75
In vitro and in vivo experiments with the new inhibitor of mycobacterium leprae brodimoprim alone and in combination with dapsone; Seydel JK et al.; The antibacterial effect of brodimoprim alone and in combination with dapsone has been studied in vitro in cell-free systems and in whole mycobacterial cells as well as in vivo in mice and humans . The obtained inhibitory effects in vitro and in vivo against model mycobacterial strains and M . leprae, the pharmacokinetic properties in human and its synergistic effect with the most used drug in the chemotherapy of leprosy, dapsone, make brodimoprim a promising candidate in the therapy of leprosy.

Comp Biochem Physiol B, 1990, 95(3), 551 - 4
Isolation and structure of cecropins, inducible antibacterial peptides, from the silkworm, Bombyx mori; Morishima I et al.; 1 . Cecropins, inducible antibacterial peptides, were purified by simple two step chromatography from immunized larval hemolymph of the silkworm, Bombyx mori . 2 . The cecropins were further separated into four major and two minor forms by reverse-phase HPLC . 3 . The four major cecropins were sequenced and divided into two types, A and B, whose structures were quite similar to cecropins A and B of Hyalophora cecropia . 4 . Three of them contained an unusual amino acid, delta-hydroxylysine . 5 . No remarkable difference in antibacterial activity against E . coli was detected among these cecropins.

Probl Tuberk, 1990, (9), 54 - 7
{Determination of the activity of broad-spectrum antibiotics against Mycobacterium fortuitum by the agar diffusion method}; Otten TF; Rapidly growing M . fortuitum bring about such conditions in man, like mycobacterioses . Management of patients presents a problem since potentially pathogenic mycobacteria are highly resistant to most antituberculous drugs . To find effective antibacterial drugs for the treatment of human patients, the definition of sensitivity of M . fortuitum to broad--spectrum antibiotics by agar disk-diffusion method on Soton's medium was carried out . Sensitivity of 53 strains of mycobacteria to 13 drugs was investigated . It was demonstrated that the aminoglycoside group (gentamicin, kanamycin and monomycin inhibiting the growth of 96, 98 and 76% % of the strains, respectively) had been the most active . Tetracycline, ristomycin and erythromycin actively affected 35-15% of the tested strains . The agar disk-diffusion method is easy to handle and use in laboratory conditions.

Curr Med Res Opin, 1990, 11(10), 661 - 7
Comparative efficacy and tolerability of two antibacterial/anti-inflammatory formulations ('Otomize' spray and 'Otosporin' drops) in the treatment of otitis externa in general practice; Smith RB et al.; An open, multi-centre study was carried out in general practice to compare the efficacy, tolerability and acceptability of a neomycin/dexamethasone preparation administered by spray ('Otomize') and neomycin/polymyxin B/hydrocortisone administered as drops ('Otosporin') in the treatment of 187 patients with otitis externa . Patients were allocated at random to receive one or other preparation 3-times daily for 10 days irrespective of response and were followed up again 14 days after cessation of therapy . Assessments were made on entry and at Days 10 and 24 of the severity of erythema, swelling and debris . A global assessment of clinical outcome was made by the doctor on Day 10 . There were no significant differences between the two groups at the start of treatment . Significant improvement occurred in both groups from Day 0 to Day 10 and from Day 10 to Day 24 in all symptoms, but no statistically significant differences were recorded between the two drugs . However, significantly more patients in the 'Otomize' group were rated as having a good clinical outcome by the physicians, and a highly significant number of patients, with previous experience of the use of ear drops, expressed a preference for the spray preparation . Few side-effects were reported by either treatment group, none necessitating discontinuation of therapy.

J Med Chem, 1990 Jan, 33(1), 77 - 86
Cephalosporin 3'-quinolone esters with a dual mode of action; Albrecht HA et al.; According to the generally accepted mechanism by which bacterial enzymes react with cephalosporins, opening of the beta-lactam ring can lead to the expulsion of a 3'-substituent . A series of dual-action cephalosporins was prepared in which antibacterial quinolones were linked to the cephalosporin 3'-position through an ester bond in the expectation that, in addition to exerting their own beta-lactam activity, these cephalosporins would act as prodrugs for the second antibacterial agent . Compared to parent cephalosporins in which the 3'-substituent was acetoxy, the bifunctional cephalosporins exhibited a broadened antibacterial spectrum, suggesting that a dual mode of action may indeed be operative.

Zahn Mund Kieferheilkd Zentralbl, 1990, 78(5), 403 - 6
{The clinical significance of bacteremia following tooth extraction}; Pavek V et al.; A group of 61 patients underwent conservative and surgical dental treatment in general anesthesia and their blood was sampled for bacteremia before and after treatment . The antibiotic antibacterial prophylaxis was administered in 21 patients one hr . before treatment (both in conservatively and surgically treated patients) . Immediately after the treatment the prevalence of bacteremia amounted to 80% in a group of ATB-free patients . In patients with ATB prophylaxis the prevalence of bacteremia after the treatment amounted to 17%.

Arkh Patol, 1990, 52(1), 66 - 8
{Primary hemochromatosis with cardiac involvement}; Mel'nik SG et al.; An autopsy case is described of a primary hemochromatosis in a 33-year-old man which was not diagnosed clinically . The peculiar feature of the disease was the absence of skin discolorations, definite symptoms of diabetes mellitus and a hepatic cirrhosis against the background of pigment cardiomyopathy . It's suggested that the progression of the heart pathology was due to the use of certain antibacterial preparations.

J Periodontal Res, 1990 Jan, 25(1), 1 - 5
Local ofloxacin delivery using a controlled-release insert (PT-01) in the human periodontal pocket; Higashi K et al.; PT-01, a controlled-release insert, was developed for topical chemotherapy in periodontal disease . It is a soluble insert that consists of fast-release and sustained-release parts containing ofloxacin (OFLX) as an antibacterial agent . In this study, the release profile of OFLX from PT-01 was investigated in vitro . Twelve adult volunteers were administered OFLX as PT-01 or as an aqueous solution into their periodontal pockets, OFLX concentrations in gingival crevicular fluid (GCF) were evaluated from the viewpoint of pharmacokinetics . The in vitro release profile of OFLX from PT-01 showed a biphasic pattern . The release rate of OFLX was relatively rapid in the early phase and slow thereafter . When OFLX aqueous solution was administered into periodontal pockets, the OFLX level in GCF rapidly decreased to be about 1/100 after 30 minutes . When PT-01 was inserted into the pockets, the OFLX level in GCF immediately reached a peak (about 12 mg/ml), and gradually decreased until the 3rd day, and maintained a constant level above 2 micrograms/ml, the effective minimum antibacterial concentration for periodontopathic microorganisms, from the 3rd to 7th day after insertion . No side-effects were observed in the volunteers who received the PT-01 insert . The above results suggest that PT-01 is a suitable pharmaceutical preparation for periodontal chemotherapy.

Arch Dermatol, 1990 Jan, 126(1), 37 - 42
Toxic epidermal necrolysis (Lyell syndrome) . Incidence and drug etiology in France, 1981-1985; Roujeau JC et al.; We looked retrospectively for all cases of toxic epidermal necrolysis that occurred in France over a 5-year period to appreciate the incidence of this disorder and its drug etiology . Of the 399 cases identified, we obtained detailed information on 344 cases and validated 253 cases . From response rates (66% to 98%), we estimated the actual total number of cases to be 333, and the incidence of toxic epidermal necrolysis in France to 1.2 cases per million per year . An independent estimation derived from death certificates gave a figure of 1.3 cases per million per year . When the number of cases with a given drug present were related to the defined daily doses of that drug sold over the 5-year period, the highest ratios were for sulfadiazin (230.10(-8}, isoxica (41.10(-8}, oxyphenbutazone (18.10(-8}, phenytoin (14.10(-8}, fenbufen (13.10(-8}, and cotrimoxazole (12.10(-8} . This first nationwide study confirmed the rarity of toxic epidermal necrolysis . Within the two main classes of responsible drugs (antibacterial sulfonamides and nonsteroidal anti-inflammatory agents) the risks linked to different drugs appeared quite different, even for closely chemically related products.

Andrologia, 1990, 22 Suppl 1, 185 - 92
Functions of the seminal vesicle; Clavert A et al.; The seminal vesicle is a gland which appeared late in the evolution of placental mammals . Vesiculectomy leads to very serious subfertility demonstrating the important role of this gland . Secretions of the seminal vesicle act during coitus and the maturation of the spermatozoon, on its mobility, its freezing capacity and the condensation of chromatin . These secretions also act on the female genital tract because they possess immunodepressive capacity . Due to their high concentration of prostaglandins, they can modify the contraction of smooth muscle . As shown by the animal model, they have an antibacterial role in the male genital tract . This explains the relatively low frequency of purely vesicular infections in human pathology.

Yao Xue Xue Bao, 1990, 25(9), 670 - 6
{Synthesis and antibacterial activity of 1-substituted benzyl quinolone acid derivatives}; Zhou SQ et al.; The compounds of quinolone class, which were studied extensively and developed very quickly in the last decades, showed high activity, low toxicity and broad antibacterial spectrum . About thirty new compounds of 1,7-disubstituted-6-fluoro-1, 4-dihydro-4-oxoquinoline-3-carboxylic acids were synthesised and evaluated in vitro against S . aureus 25923, E . coli-25922 and P . aeruginosa . Their activities were low . The minimum inhibitory concentrations (MIC microgram/ml) of these compounds against Gram-positive bacteria were higher than those against Gram-negative bacteria . The relative in vitro activity contributed by 1-benzyl was: benzyl greater than p-chlorobenzyl greater than p-nitrobenzyl groups.

Probl Tuberk, 1990, (7), 41 - 3
{The course and outcome of tuberculous meningitis in cases of detection of Mycobacterium tuberculosis in the cerebrospinal fluid}; Gasparian AA et al.; The cases of M . tuberculosis detected in cerebrospinal fluid of the patients with tuberculous meningitis being under observation during 1968-1987, are analysed . The second decade (1978-1987) witnessed a greater percentage of M . tuberculosis found in the cerebrospinal fluid of the patients (including children, adolescents and adults) . Children and adolescents constituted the majority of the cases . M . tuberculosis agents were detected by means of bacterioscopy and inoculation in 33.3 and 66.7% of the patients, respectively . In 15.5% of the cases, primary resistance to antibacterial drugs was revealed . The detection of M . tuberculosis in the cerebrospinal fluid is now considered to be an unfavourable factor indicating the severity of the disease and entailing, to a certain extent, its adverse outcome . Antibacillary drug resistance of the M . tuberculosis strains isolated from cerebrospinal fluid may serve as an aggravating condition . As a rule, the disease in these cases has a serious course, making the treatment much more difficult and causing unfavourable outcomes.

Vestn Dermatol Venerol, 1990, (5), 66 - 71
{New approaches to the combined therapy of gonorrheal infection and accelerated methods for predicting its efficacy}; Stepanenko VI et al.; The authors suggest a combined method for the treatment of new torpid and chronic gonorrheal urethritis, involving preliminary studies of the agent's cellular respiration activity, and offer the technique for predicting the efficacy of such treatment . If gonococcal cellular respiration activity is low, aerobic processes in these agents are stimulated with daily subcutaneous injections of plasmol (a biostimulant), starting from 1 ml and building up the dose by 1 ml daily, and local irrigations of the urethra with oxygen cocktails via specially designed irrigators (Authors' Certificate No . 827071 USSR); such stimulation is carried out for 4 days prior to specific therapy . This treatment modality is maintained by an Authors Certificate No . 1107867 USSR . To check up the efficacy of the antibiotic chosen for therapy, a rapid method has been developed, consisting in measurement of the patient's blood serum antibacterial activity carried out in special chambers for cell microcultivation.

Probl Tuberk, 1990, (4), 42 - 4
{Partial resection of the lungs in patients with newly detected destructive tuberculosis}; Ibragimov MA et al.; The efficacy of partial pneumonectomies in 700 patients with newly-diagnosed destructive tuberculosis preceded by an ineffective antibacterial therapy for 3-15 months was studied . Operations were performed in 411 (58.8%) patients with fibrocavernous tuberculosis, in 173 (24.7%) with cavernous tuberculosis, in 10 (1.4%) with disseminated tuberculosis and cavitation, and in 106 (15.1%) with tuberculoma . Segmental resections were carried out in 214 (30.6%) cases, lobectomies in 309 (44.1%), and combined resections in 177 (25.3%) . Immediately good and satisfactory clinical efficacy was achieved in 687 (98.1%) and 7 (1.0%) subjects respectively, the remaining 6 (0.9%) patients died . 3-15 years after the operation, the reactivation of tuberculosis was observed in 14 (2.3%) cases out of the 603 examined . An intensive antibacterial therapy as well as repeated operations made it possible to cure 6 patients, with 5 still under treatment and 3 dead . Later on a stable clinical cure was registered in 595 (98.7%) patients out of the 603 examined.

NCI Monogr, 1990, (9), 73 - 85
Infection prevention in bone marrow transplantation and radiation patients; Epstein JB; This article reviews the prevention of oral and systemic infection in bone marrow transplantation and radiation patients . Prophylaxis of herpes virus reactivation in bone marrow transplant and leukemic patients has resulted in reduced morbidity associated with their medical management . In order to reduce the risk of systemic infection, reduction in ulcerative mucositis is desirable . The use of antifungal and antibacterial agents has not been encouraging to date . Cytoprotective agents have shown some initial success in preventing mucosal breakdown . Further study is required to confirm these initial results.

J Med Chem, 1990 Jan, 33(1), 142 - 6
Synthesis and structure-activity relationships of new 7-{3-(fluoromethyl)piperazinyl}- and -(fluorohomopiperazinyl)quinolone antibacterials; Ziegler CB Jr et al.; Some novel 6-fluoro-7-substituted-1,4-dihydro-4-oxoquinoline-3-carboxylic acids have been prepared . At the N-1 position "standard" substitution was employed with the ethyl, cyclopropyl, and p-fluorophenyl groups being used . At C-7 the introduction of some novel piperazines was made . Most notably, 2-(fluoromethyl)piperazine (10) and hexahydro-6-fluoro-1H-1,4-diazepine (16, fluorohomopiperazine) at the quinolone C-7 position produced products with similar in vitro antibacterial activity as the ciprofloxacin reference . The in vivo efficacy of 1-cyclopropyl-6-fluoro-7-{3-(fluoromethyl)piperazinyl}-1,4-dihydro-4- oxoquinoline-3-carboxylic acid (20) was excellent with better oral absorption than ciprofloxacin (2).

Infect Immun, 1990 Jan, 58(1), 269 - 71
Stimulation of antibacterial macrophage activities by B-cell stimulatory factor 2 (interleukin-6); Flesch IE et al.; Mononuclear phagocytes provide the major habitat of intracellular bacteria, including Mycobacterium tuberculosis and Mycobacterium bovis . The capacity of B-cell stimulatory factor 2 (interleukin-6 {IL-6}) to activate tuberculostatic functions was investigated by using murine bone marrow-derived macrophages (BMM phi) . BMM phi stimulated with recombinant IL-6 and subsequently infected with M . bovis organisms failed to inhibit mycobacterial growth . In contrast, marked tuberculostasis was induced by IL-6 in BMM phi that were already infected with M . bovis, indicating that IL-6 has a macrophage-activating function.

Drugs Exp Clin Res, 1990, 16(9), 451 - 5
Ramoplanin: a review of its discovery and its chemistry; Parenti F et al.; Ramoplanin is a novel antibacterial agent with characteristics that make it suitable for development as a topical treatment for acne, infected wounds, and for treatment of antibiotic-associated diarrhoea . In this paper, the authors will review the discovery process and the descriptive chemistry of this novel molecular entity.

Drugs Exp Clin Res, 1990, 16(9), 435 - 43
Synthesis and biological properties of A-71497: a prodrug of tosufloxacin; Chu DT et al.; Tosufloxacin (5, A-61827 tosylate or T-3262) is currently under product development by both Abbott Laboratories and Toyama Chemical Co . Its registration as antibacterial agent has been approved in Japan . It has been found to be extremely effective in treating several bacterial infections . However, due to its inherent low water solubility, the development of an intravenous formulation will be extremely difficult and may preclude its parenteral use . In search of a more water-soluble analog of tosufloxacin for parenteral use, the 3-formyl derivative of tosulfoxacin, A-71497 (13), was synthesized for evaluation . It was found to produce high plasma levels of tosufloxacin upon both oral and subcutaneous administration to mice . High plasma levels of tosufloxacin were also obtained when 13 was administered both orally and intravenously to dogs . It possesses increased water solubility and makes the development of intravenous formulation possible . The chemical synthesis as well as biological properties of A-71497 (13) are described.

Yao Xue Xue Bao, 1990, 25(10), 739 - 44
{Synthesis of N2-aryl-triazinoylamoxicillins and N2-phenyl-N4-alkyl (aryl)-triazinoylamoxicillins and their antibacterial activity}; Zhao LX et al.; Sixteen derivatives of BL-P1908 were synthesized by reaction of 2-aryl-1, 2, 4-triazine -3, 5-dione -6-carboxylic acid, or 2-phenyl-4-alkyl (aryl) -1, 2, 4-triazine-3, 5-dione-6-carboxylic acid with amoxicillin . All of them are new compounds . Their chemical structures were determined by elemental analysis, IR and 1HNMR . Preliminary tests showed that all compounds have marked activities against standard G(+) and G(-) bacteria and five of them have certain characteristic of broad spectrum, but they have no activities against resistant strains S . aureus S1, E coli C1 and P . aeruginosa PS1 isolated from clinic.

Yao Xue Xue Bao, 1990, 25(11), 834 - 9
{Studies on antibacterial constituents from the roots of Rubia cordifolia L.}; Qiao YF et al.; Twelve compounds were isolated from the roots of Rubia cordifolia L. . Nine of them were established by chemical and spectroscopic methods to be alizarin (I),1-hydroxy-2-methyl-9,10-anthraquinone(II),1,3,6-trihydroxy-2-methyl- 9,10-anthra-quinone-3-O-(6'-O-acetyl)-alpha-L-rhamnosyl(1--- -2)-beta-D- glucoside(III),1,3,6-trihydroxy-2-methyl-9,10-anthraqueinone-3-O-a lpha- L-rhamnosyl(1----2)-beta-D-glucoside(IV),1,3,6-trihydrozy-2- methyl-9,10- anthraquinone-3-O-(6'-O-acetyl)-beta-D-glucoside(V),2-carbomethyoxy++ +-3-prenyl- 1,4-naphthohydroquinone di-beta-D-glucoside(VI),rubimallin(VII),beta- sitosterol(VIII) and daucosterol(IX), among them, V is a nwe compound and IX was obtained from this genus for the first time, III, VI and VII showed certain antibacterial activities.

Scand J Infect Dis Suppl, 1990, 74, 49 - 53
Pharmacokinetic studies of antibacterial agents using the suction blister method; Bruun JN et al.; The suction blister technique was used for pharmacokinetic studies with sulfonamides and trimethoprim . Blisters produced by suction (-0.3 kg/cm2) for 1.5 h contained approximately 0.15 ml fluid with a protein content of 40-50% of that in plasma, the main protein fractions being present in the same ratio as in plasma . 2 g sulfaisodimidine was given as bolus injection, i.v . infusion or orally to groups of 4 volunteers . The peak blister fluid concentrations after oral administration (120 +/- 18 mmol/l) was only marginally lower than the concentrations after i.v . infusion (122 +/- 28 mmol/l) and i.v . bolus injections (134 +/- 37 mmol/l) . The total drug blister fluid concentration started to decrease before the plasma level was reached . However the relative concentration increased from 53% of that in plasma at 8 h to 66% at 12 h after drug administration . Considering the protein binding of the drugs, the interstitial fluid levels of free drug were presumably higher than the plasma level after 8 h . Comparison of drug concentrations in blisters produced before and after the drugs were given showed higher concentrations in the latter for the first 2-6 h . However, after 8-12 h the concentrations of the drugs in the two types of blisters were similar . The suction blister method produces blisters of uniform size . The drug concentrations in different experiments showed the coefficient of variation for blister fluid concentrations to be no greater than for plasma levels . The consistent results of the standardized suction blister method makes this method useful for studying drug penetration to extravascular compartments in humans.

Scand J Infect Dis Suppl, 1990, 74, 218 - 34
Correlation of pharmacokinetic parameters to efficacy of antibiotics: relationships between serum concentrations, MIC values, and bacterial eradication in patients with gram-negative pneumonia; Schentag JJ; In vitro, antibiotics are known to kill bacteria in predictable relationships to their broth concentrations . It was our hypothesis that serum concentration was an important determinant of the rate of bacterial eradication in patients . This contention was reinforced by animal studies, which have clearly demonstrated concentration-related antibacterial activity . The animal models rely on reduction of bacterial colony counts as an endpoint of effect, and demonstrate that colony count reductions are related to antibiotic dose and probably to serum concentration . We adapted these methods for use in intubated patients with Gram-negative pneumonia . Briefly, each patient had extensive staging of the pneumonic process, and the Gram-negative organism was isolated and its minimal inhibitory concentration (MIC) was determined . In each patient measurement of the antibiotic serum concentrations in the interval between two doses of the drug was also performed . The pharmacokinetic profile of the drug was then superimposed on the bacterial MIC, and we then derived the patients individual peak to MIC ratio, area above MIC, and time above MIC . Each of these pharmacokinetic parameters was then related to the time required to eradicate the bacterial pathogens in the patient . For beta-lactams and quinolones, time above MIC was the most predictive of bacterial eradication times . Clearly, these methods can be used to develop dosing strategies for patients, as well as to determine clinically relevant doses and dosing strategies in clinical trials . Further work is needed, however, to assess whether these concepts hold for other types of bacteria (such as Gram-positive) or apply as accurately to other infection sites in addition to pneumonia.

Drugs Exp Clin Res, 1990, 16(8), 403 - 6
Efficacy of dactimicin plus clindamycin compared with gentamicin plus clindamycin in the treatment of experimental intra-abdominal infections in rats; Nord CE et al.; A reproducible experimental model of intra-abdominal infections in rats has been developed in order to simulate intra-abdominal sepsis in patients . A 1-cm segment of ileum was isolated on its vascular pedicle . The intestine was then divided at each end of the segment and intestinal continuity was re-established by an end-to-end anastomosis . Dactimicin is a new aminoglycoside antibiotic with a broad antibacterial spectrum including both aerobic Gram-positive and Gram-negative bacteria . The experimental model was used to compare the efficacy of dactimicin in combination with clindamycin with the combination gentamicin/clindamycin in the treatment of intra-abdominal infections . Of the untreated animals, 70% died within two days . Animals treated with dactimicin plus clindamycin or gentamicin plus clindamycin exhibited significantly decreased mortality and increased cure rates during the experimental period . Only 5% of these animals died . Thus the combination dactimicin/clindamycin seems to be useful in the treatment of intra-abdominal infections.

Arch Exp Veterinarmed, 1990, 44(5), 740 - 56
{Experimental udder infection with Escherichia coli . 2 . Morphological changes of the epithelium in the area of the glands of the milk cistern and the large milk ducts}; Sterba P et al.; Optical light, transmission, and scanning electron microscopy were used in investigations of epithelia in the glandular region of the milk cistern and greater lactiferous ducts and yielded the following findings, four and six hours from infection: degeneration and necrosis of epithelial cells, intraepithelial foreign cell infiltration (neutrophilic granulocytes, lymphocytes, macrophages), intra-epithelial oedema and locally delimited epithelial loss . The lesions differed by intensity in various regions, so that a distinction could be made among five froms of epithelial alterations . The epithelial cells revealed their capability of absorbing pathogenic material and storing it in cytoplasmic vacuoles . This was considered to reflect active involvement of epithelium in antibacterial defence, and consequently, to reflect the role played by epithelium as a defence barrier in the milk cistern and greater lactiferous ducts.

Ann Pharm Fr, 1990, 48(5), 255 - 63
{Antibacterial activity of extracts from plants used in preparation as antidiarrheals at Kinshasa, Zaire}; Kambu K et al.; A preliminary and anterior bacteriological study about 38 plant antidiarrheic traditional preparations, has demonstrated that 35 of them have bactericidal activity . Thirty inhibit the growth of all select germs and 5 exert this bactericidal effect on some germs . Some extracts proceeding of these possess a bactericidal activity, specially if they contain polyphenols (flavonoids, catechics tanins), saponins and alkaloids.

Rev Laryngol Otol Rhinol (Bord), 1990, 111(5), 503 - 5
{Cefuroxime axetil, a new oral cephalosporin for treating infections of the ORL field: clinical synthesis}; Westphal JF; Cefuroxime axetil (C.A.E.) is a broad spectrum cephalosporin, suitable for oral route . Its antibacterial activity includes all the pathogens usually responsible for E.N.T . infection, with low M.I.C.'s: H . influenzae, S . pneumoniae, S . aureus, S . pyogene . The stability of the drug against betalactamases, especially those produced by H . influenzae, associated with good bio availability (50%) and tissue penetration (30%) account for the potent in vivo bactericidal activity and clinical efficacy of cefuroxime axetil . More than 1,000 patients had been enrolled in controlled clinical trials: the success rates yielded by C.A.E . were 98%, 96% and 91%, respectively for pharingitis/tonsilitis, otitis media and acute sinusitis . C.A.E . is at least as effective as amoxycillin/clavulanic acid and safety appears to be better.

Dev Comp Immunol, 1990 Fall, 14(4), 379 - 83
Bacteriostatic and cytolytic activity of purple fluid from the sea hare; Yamazaki M et al.; A bacteriostatic factor, aplysianin P, was purified from the purple fluid of a sea hare, Aplysia kurodai, as a glycoprotein of 60 K daltons . A cytolytic glycoprotein purified from the purple fluid of Dolabella auricularia did not show antibacterial activity . Aplysianin P was half-maximally active for gram-positive and -negative bacteria at 0.2-5.8 micrograms/mL and its action was not bactericidal but bacteriostatic . Aplysianin P completely inhibited the syntheses of DNA and RNA by E . coli, but it did not induce the release of ATP from bacteria . These results suggest that aplysianin P, found in an invertebrate, the sea hare, is a new bacteriostatic protein and that it exerts its action by inhibiting nucleic acid syntheses, as a DNA-inhibiting, chemotherapeutic drug does.

Perit Dial Int, 1990, 10(2), 157 - 60
Stability of cotrimoxazole in peritoneal dialysis fluid; Holmes SE et al.; This study examines the stability of both components of the antibacterial combination, cotrimoxazole (trimethoprim and sulphamethoxazole) in peritoneal dialysis fluid stored in polyvinyl chloride bags and glass ampoules at room temperature for up to nine days . Greater than 10% loss of trimethoprim occurred within three days for admixtures stored in plastic bags, whereas the original concentration remained virtually unchanged after nine days for similar solutions stored in glass ampoules . This indicated that the loss of trimethoprim observed in solutions stored in plastic bags was associated primarily with the nature of the container, presumably due to some form of uptake by or loss through the plastic . Greater than 10% loss of sulphamethoxazole occurred within two days for all admixtures examined, stored in either glass or plastic containers . This degree of loss was achieved within 12 h for one admixture stored in plastic . There was also the time-dependent appearance of an additional peak in HPLC analyses of these solutions, indicating that loss of sulphamethoxazole was due to chemical decomposition of the drug in the peritoneal dialysis fluid . The shelf-life of such admixtures would be limited by the stability of the sulphamethoxazole component, with the available data suggesting a shelf-life of 12 h for solutions stored at room temperature.

Ter Arkh, 1990, 62(12), 14 - 7
{Blood immunoglobulin E in acute pneumonia}; Nonikov VE; The program of examination of 209 patients suffering from acute pneumonias (AP) included identification of the etiologic agents and measurement of the blood serum concentrations of immunoglobulins E (IgE) . Immunoglobulinemia E was detected in 106 patients (50.7%) . That phenomenon was noted in all the patients with eosinophilic pneumonia . Immunoglobulinemia E occurred mostly in patients (p = 0.05-0.001) with an aggravated allergological anamnesis, in those with a history of obstructive bronchitis and in cases where antibacterial therapy had been administered for a long time . The concentration of IgE in blood serum was established to agree with the intensity of antibacterial chemotherapy.

Probl Tuberk, 1990, (12), 60 - 2
{Pathomorphology of tuberculosis after the treatment with antibacterial drugs and amniocene}; Sapozhnik KG et al.; The tests on guinea pigs proved that amniocene (a tissue preparation) has a double action (antiinflammatory and potentiating repair processes in the foci of tuberculous lesions) . This action manifests itself depending on the type of tuberculous inflammation and produces an effect upon the involution of experimental tuberculosis.

Ann Pharm Fr, 1990, 48(4), 185 - 91
{Chemical and pharmacological study of Phragmites communis Trin.}; Tsitsa-Tzardi E et al.; A chemical study of the aerial parts of Phragmites communis Trin . concerning free amino-acids, fatty acids, sterols, tocopherols and polyphenols has been carried out . The amino-acids content was studied at two different periods (winter, summer) in order to elucidate differences . The isolated polyphenols were investigated for antibacteriophage properties.

Infection, 1990, 18 Suppl 3, S125 - 8
{Cefixime treatment in different bacterial infections in the ENT region}; Schlenter WW et al.; The clinical efficacy and tolerance of cefixime were evaluated in an open uncontrolled clinical trial including 37 patients suffering from ENT-infections . The MIC90 values of this new oral cephalosporin against gram-negative pathogens are less than 1 mg/l . The antibacterial activity of cefixime against gram-negative pathogens is stronger than that of other oral cephalosporins . Cefixime was administered for five to twelve days twice daily in a dose of 200 mg . In one patient the treatment with cefixime was discontinued after five days due to perioral dermatitis . In 33 of 36 patients cure or distinct improvement was observed after cefixime treatment, showing a clinical success rate of 91.7% . Causative organisms were isolated in 17 of 37 patients (47.2%) . After the cefixime therapy the causative organisms were eradicated in 13 of 17 patients (76.5%) . The tolerance of cefixime is comparable with that of other oral cephalosporins.

Klin Khir, 1990, (11), 33 - 5
{Renal syndrome in amebic lesions of the liver}; Gaibatov SP; The author observed 315 patients with the amebic liver abscess . Of them in 134 (42.5%), the renal syndrome was diagnosed . The kidney damage had the course of the secondary pyelonephritis type, or in the form of a toxic kidney . On the basis of clinico-laboratory analysis, the author distinguishes the mild, moderate and severe degrees of kidney damage, recommends an adequate transfusion-infusion, antibacterial and specific therapy.

Ital J Gastroenterol, 1990, 22 Suppl 2, 36 - 9
Long-term treatment with anti-secretory drugs: could it affect morphology and cell kinetics of gastric mucosa?
Biasco G.
Drugs reducing gastric acid output are widely used and commonly considered free from relevant side effects . However, our knowledge on the consequences of long-term anti-secretory treatment is still lacking . Several observations both, in animal models and in man, indicate that a decreased gastric acid output may lead modifications of several features of epithelial gastric cells . These alterations can be determined by different mechanisms . The drugs can raise plasma levels of gastrin, which possibly cause a proliferative stimulus on fundic mucosa . Moreover, some drugs showed a direct effect on cell proliferation . Finally, hypochlorhydria reduces the antibacterial power of gastric juice . In this environment, bacterial flora can overgrow and synthesize also the N-nitrosocompounds . These observations suggest that prolonged treatments with powerful anti-secretory drugs should be carried out taking into account the hypothetical biological risk on gastric mucosa.

Drugs Exp Clin Res, 1990, 16(5), 215 - 24
Structure-activity relationship of quinolone antibacterial agents: the effects of C-2 substitution; Chu DT et al.; Very little is known about the structure-activity relationship of quinolone antibacterials at the 2-position . Because of the loss of biological activity with 2-methyl and 2-hydroxyl substitution, modifications at C-2 were generally considered to be unfavourable . Quinolone derivatives having a ring between positions 1 and 2 were recently shown to have biological activity . The sulfur-bridged analogs such as the benzothiazolo{3,2-a}quinolone, KB-5246 and NAD-394 have been reported to be highly active in vitro . The authors have synthesized 2-methylthiociprofloxacin, 2-methylofloxacin, the 5-oxopyrrolo{1,2-a}quinoline and isothiazolonaphthyridine to assess the importance of the sulfur atom on biological activity as well as the effect of C-2 substituent on the spatial arrangements of N-1 or the 3-carboxylic group . It was found that the planarity between the 4-keto and 3-carboxylic acid groups of quinoline molecules is the most important criterion for biological activity . The syntheses of the above four compounds are also described.

Lab Delo, 1990, (5), 58 - 64
{Determination of the sensitivity to antibacterial preparations of the microflora in the sputum of patients with nonspecific lung diseases}; Smolianskaia AZ; Nonspecific pulmonary diseases (NPD) of infectious etiology often complicate and aggravate the course of various somatic diseases . Isolation, identification, and assessment of the drug sensitivities of the agents are obligatory for effective therapy . The sputum is the most frequent object of microbiologic investigation . Such investigation is fruitful if the sputum is properly collected and the quantitative method is used for inoculation in a set of nutrient media, that provide the maximum growth of the agents . A correct estimation of the role of isolated bacteria in the infectious process involves additional studies of their biological characteristics and clinical interpretation of the findings . Assessment of antibiotic sensitivity provides the most valuable information for a clinician, but these data are clinically useful only if referred to the agent and not to the contaminating flora.

Arch Monaldi Mal Torace, 1990 Jan-Feb, 45(1), 21 - 9
{Pefloxacin in the treatment of lower respiratory tract infections}; Dericoloso A et al.; Pefloxacin is an antibacterial agent belonging to the group of quinolones having a methyl-carboxylic acid which possesses a high activity as compared to other quinolonic drugs . In this study we tested the efficacy and tolerability of the drug in the treatment of 25 patients with environmental L.R.T.I . (Low Respiratory Tract Infections) . The microbiological and clinical characteristics of the drug were tested in this study . Excellent results were obtained in 96% of the patients treated and the tolerability was also very good.

Trends Biotechnol, 1990 Jan, 8(1), 26 - 30
Antibiotics from within: antibacterials from human and animal sources; Elsbach P; The isolation of potent antibacterial proteins and peptides from human and animal phagocytes has raised the possibility that these 'antibiotics from within' can be used as therapeutic agents . Problems in delivery to and toxicity towards the host must be faced, but rapid progress in defining the structural determinants of the cytotoxic action of these naturally occurring cytotoxins provides a basis for biotechnological development of new classes of antibiotics.

J Chem Technol Biotechnol, 1990, 47(3), 209 - 18
Synthesis and biological activity of some new 2-chlorophenothiazine derivatives; el-Ezbawy SR et al.; 10-(Hetero/arylthio)acetyl-2-chlorophenothiazines II have been synthesized via interaction of 10-chloroacetyl-2-chlorophenothiazine I with heterocyclic and/or aromatic potassium mercaptide in ethanol . Oxidation of II using H2O2/CH3COOH mixture was studied . Structures of the products were verified by elemental and spectral analyses . Some compounds were screened in vitro for their antibacterial activities.

Clin Ter, 1989 Dec 31, 131(6), 391 - 5
{Treatment of infection of the lower respiratory tract . Experience with a new quinolinone: pefloxacin}; Collimedaglia P et al.; Twenty-nine patients (16 females and 13 males, aged 48 to 81 years) with lower respiratory tract infections have been treated with pefloxacin 400 mg, orally and/or intravenously, every 12 hours for 3 to 13 days . No other antibacterial agent was associated . Two patients dropped out because of gastralgia and vomiting and one because of pruritus . Success was obtained in 23 (88%) out of the 26 patients who completed the study . A patient with pleural empyema was treated successfully by washing the pleural cavity with a dextrose solution of pefloxacin . In addition to the drop-outs, 4 patients complained of gastralgia which disappeared spontaneously in 2 of them or after switching from oral to parenteral administration in the other 2 . No adverse interaction was observed between pefloxacin and other drugs taken concomitantly, in particular theophylline, corticosteroids, and beta 2-adrenoceptor stimulants . Hematological tests including blood-cell count did not reveal any adverse modification.

Biochem Biophys Res Commun, 1989 Dec 15, 165(2), 637 - 43
Mass spectrometric identification of peptides present in immunized and parasitised hemolymph from honeybees without purification; Craig AG et al.; We propose that a substance, identified using mass spectrometry, present in the hemolymph of the honeybee (Apis mellifera) as a result of stimulating the insect immune system corresponds with Apidaecin I, an antibacterial peptide recently described . The plasma desorption mass spectra indicate that several other higher molecule mass substances are synthesised as a result of bacterial or parasite infection.

FEBS Lett, 1989 Dec 4, 258(2), 199 - 202
Cloning of gene cluster for sarcotoxin I, antibacterial proteins of Sarcophaga peregrina; Kanai A et al.; A genomic clone of sarcotoxin I was isolated . This clone contained four genes of structurally related proteins belonging to the sarcotoxin I family present in tandem array . One of these genes was sequenced and found to be the sarcotoxin IB gene . This gene contained a single intron of 95 bases.

Harefuah, 1989 Dec 1, 117(11), 361 - 3
{Cefaclor and trimethoprim-sulfamethoxazole for recurrent otitis media}; Fliss DM et al.; The efficacy of cefaclor and of trimethoprim-sulfamethoxazole (TMP-SMX) in the management of recurrent otitis media was evaluated in a randomized single-blind controlled trial . The median age of the patients was 12 months (range 5-37); there were 37 boys and 19 girls . All had received 1 or more courses of antibacterials for acute otitis media in the previous 2-3 weeks . 27 were treated with oral cefaclor suspension, 40 mg/kg/day in 3 divided doses, and 29 with 1 mg/kg/day of TMP-SMX (trimethoprim 8 mg, sulfamethoxazole 40 mg) in 2 divided doses, each group for 10 days . 70% of the cefaclor group and 90% of the TMP-SMX group were cured after the 10 days of therapy (0.1 greater than p greater than 0.05) . Results were not better on the 21st day as compared with the 10th . Our data indicate a mild preference for TMP-SMX (although p was not less than 0.05), since it needs to be given only twice a day and costs less than cefaclor.

Arch Pharm (Weinheim), 1989 Dec, 322(12), 847 - 52
Investigations on the antiproliferative effects of amino acid antagonists targeting for aminoacyl-tRNA synthetases . Part I--The antibacterial effect; Laske R et al.; Amino acid antagonists with proven or potentially inhibitory activities on aminoacyl-tRNA synthetases were tested for their antiproliferative effect against E . coli B . The compounds 4- and 6-fluoro-tryptophan, 5-methyltryptophan, selenocystine and beta-(2-thienyl)alanine gave strong growth inhibition in minimal medium, which disappeared after addition of structurally related natural amino acids or in an enriched broth . The inhibitory effect on amino-acyl-tRNA synthetases and the minimal inhibitory concentration for growth inhibition in minimal medium could not be correlated.

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