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Query: UNIPROT:Q29983 (MIC)
 21,138 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The antibacterial activity of beta-lactams against H. influenzae is difficult to evaluate as a result of the osmotic-pressure-dependent formation of filaments and spheroplasts whose viability is still under debate. We compared growth curves obtained by optic density measurements and by UFC/ml counts for H. influenzae in the presence of amoxicillin, cefaclor and cefotaxime in various concentrations. Only the early response to antibiotics, observed during the first six hours of antibiotic-culture contact, was considered. Results showed, for each of the three antibiotics: an increase in optic density with formation of abnormal organisms that correlated poorly with antibiotic concentrations; a stable number of UFC/ml for more than 90 mn, followed by a slow fall reaching at the most 1.5 Log 10 UFC/ml at the sixth hour. We conclude that amoxicillin, cefaclor and cefotaxime in active concentrations rapidly produce the formation of abnormal organisms with an increase in biomass as a result. These abnormal organisms lose their viability slowly, even with concentrations greater than 50 time the MIC. Cefaclor's MIC and MBC are underestimated when results are read only after 24 hours.
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PMID:[Growth curves and killing rate of Haemophilus influenzae exposed to amoxicillin, cefaclor and cefotaxime]. 353 10

The API ATB-MIC system was used for antibiotic sensitivity testing of H. influenzae (following addition of NAD and hemin). Results were compared to those obtained with agar dilution and disc diffusion. Eighty-four strains with a variety of resistance phenotypes (including beta-lactamase-producing strains and strains resistant to chloramphenicol, tetracycline or kanamycin) were tested. The API ATB-MIC system studies the susceptibility of H. influenzae to antibiotics by determining minimal inhibitory concentrations. Agreement between the methods ranged from 83% to 98% according to the antibiotic. Discrepancies involved ampicillin, minocycline and, to a lesser extent, chloramphenicol. These discrepancies had no influence on the interpretation of results except in one instance involving chloramphenicol. Comparison of the results obtained with each of the three methods leads to a discussion of the criteria that indicate resistance of H. influenzae and of the cutoff concentrations and diameters used for other species. Criteria indicating resistance are production of beta-lactamase for ampicillin, production of enzyme, a MIC above 2 mg/l or a diameter below 26 mm for chloramphenicol, and a diameter below 18 mm or a MIC above 4 mg/l for tetracycline and minocycline.
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PMID:[Evaluation of the API ATB-CMI system for testing the sensitivity of Haemophilus influenzae to antibiotics. Comparison with other technics and reflections on interpretation criteria]. 353 55

Cyclacillin, a new aminosalicylic semisynthetic penicillin, was compared with amoxicillin for the therapy of acute bacterial maxillary sinusitis in 80 patients (ages, 12 to 70 years) in a prospective, double-blind, randomized clinical trial. Direct sinus aspirations for quantitative culture were done for all patients before and after 10 days of therapy. Both drugs were administered at a dosage of 500 mg orally three times daily. Among culture-positive patients, clinical cure was achieved in 23 of 26 patients and 25 of 27 patients treated with cyclacillin and amoxicillin, respectively, for an overall cure rate of 91%. Bacteriologic failure occurred in 9% (4 of 44 patients); 3 of the 4 failures were in the cyclacillin group. There was no correlation between clinical or bacteriologic cure and the results of sinus transillumination (clear, dark) at follow-up. Initial direct sinus aspirates were positive in 57 of 80 cases (70%): 25 (44%) of these were the result of Streptococcus pneumoniae and 23 (40%) were the result of Haemophilus influenzae. All of these isolates were susceptible (MIC, less than or equal to 0.5 microgram/ml) to both study drugs; no ampicillin-resistant H. influenzae was recovered. On day 10 of therapy, mean concentrations of both drugs in serum were 2.5 to 2.7 micrograms/ml, but no antibiotic was detectable in 20 of 21 simultaneous sinus aspirates. Adverse effects (rash, diarrhea) were infrequent and similar in both groups. Cyclacillin appears equivalent to amoxicillin in the therapy of acute maxillary sinusitis.
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PMID:Comparison of cyclacillin and amoxicillin for therapy for acute maxillary sinusitis. 353 60

Cefuzoname (CZON, L-105) a newly developed cephalosporin, has broad spectrum on Gram-positive or -negative bacteria and may also be effective against Staphylococcus aureus against which third generation cephalosporins are largely ineffective. We studied the pharmacokinetics and clinical effects of CZON on infectious disease of children. The diseases we studied included 2 cases of bacterial meningitis and 1 case each of viral meningitis, enterocolitis, upper respiratory infection, pneumonia, and mycoplasmal pneumonia. CZON was administered by drip infusion. Dose levels were 20-53 mg/kg/30-60 minutes, 3 times a day. For 5 cases, was studied time course of concentrations of CZON in plasma. Median T 1/2 was 0.96 hour. Concentrations in cerebrospinal fluid (CSF) were studied in cases of pneumonia and bacterial meningitis. In the case of pneumonia the CSF concentration of CZON was 0.272 microgram/ml after 45 minutes, in the case of meningitis they were 0.155 microgram/ml after 5 hours. Both of these values were higher than MIC of 0.025 microgram/ml against Haemophilus influenzae which was isolated from a case of bacterial meningitis. This MIC was lower than that of cefotiam and cefazolin, as well as of cefmenoxime. Clinical effects were excellent on pneumonia, good on upper respiratory infection, fair on mycoplasmal pneumonia. CZON, however, was ineffective in the treatment of a case of bacterial meningitis from which a susceptible strain of H. influenzae was isolated.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Studies on cefuzoname in the field of pediatrics]. 361 97

The concentration of antibiotics in cerebrospinal fluid is of great interest in therapeutics, especially for the treatment of the central nervous system. We studied the penetration of mezlocillin (MZPC) in 3 cases with V-P shunt and 7 cases after neurosurgical operation. After intravenous injection of 4 g MZPC in the 3 cases with V-P shunt, a peak concentration (0.26-3.6 micrograms/ml) of MZPC in the cerebrospinal fluid was reached in 2-4 hours. In the 7 cases after neurosurgical operation, cerebrospinal fluid was sampled at 4 hours after the intravenous injection of 4 g MZPC by spinal tap. Concentrations of MZPC in cerebrospinal fluid ranged from 1.1 to 17.5 micrograms/ml. The mean maximum concentration of MZPC was 5.85 micrograms/ml, which exceeded 90% MIC (minimal inhibitory concentration) against S. epidermidis, E. faecalis, H. influenzae. It is concluded MZPC can be useful for the prophylaxis of meningitis.
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PMID:[A study on penetration of mezlocillin into the cerebrospinal fluid]. 376 53

Cefminox (CMNX, MT-141) was studied both fundamentally and clinically in the field of pediatrics with following results. The MIC of CMNX for Bordetella pertussis was 0.10 micrograms/ml in inoculum size 10(6) cells/ml. Following administration of 10 and 20 mg/kg of CMNX as drip infusion over 1 hour, the blood levels of the drug were 49.0 +/- 18.1 and 69.1 micrograms/ml at completion of infusion, 28.8 +/- 7.7 and 61.6 micrograms/ml at 1.5 hours, 23.6 +/- 9.3 and 44.1 +/- 3.8 micrograms/ml at 2 hours and 1.4 +/- 1.4 and 4.0 +/- 0.6 micrograms/ml at 7 hours, with T1/2 of 1.03 and 1.41 +/- 0.03 hours, respectively. Within the first 7 hours after administration, 61.4 +/- 8.2 and 55.9 +/- 0.8% of the drug dosed were excreted at active form in urine. In child with encephalitis, drug considered to be good as a cephem antibiotic was achieved in the cerebrospinal fluid (the ratio of the level in the cerebrospinal fluid to that in the serum was 7.3%). In addition, in the pus in empyema also high level was reached (its ratio against blood level was 53%). In the treatment of 31 cases of acute infections of pediatric field including upper and lower airway infections, empyema, whooping cough, acute urinary tract infections and phlegmon, CMNX was administered intravenously either as one shot injection as drip infusion. The clinical results obtained were rated as good or more in 93% of the cases and as fair or more in 100% of the cases. The main dosage of CMNX in these cases was about 60 to 70 mg/kg per day in 2 or 3 divided doses. S. aureus, S. pyogenes, S. pneumoniae, H. influenzae and ABPC resistant strain of E. coli demonstrated in various materials could be eradicated after intravenous injection of CMNX. CMNX was administrated for a period of 2 to 16 days to a total amount of 1.5 to 26.5 g. In none of these cases side effects developed nor any abnormality was revealed by hematological findings or results of renal or liver function.
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PMID:[Study on a new cephamycin preparation cefminox in the field of pediatrics]. 383 61

Fundamental and clinical studies on BRL 25000 granules were carried out in the pediatric field. BRL 25000 is a formulation comprising 1 part of clavulanic acid (CVA) and 2 parts of amoxicillin (AMPC). The MICs of BRL 25000 and AMPC were assessed against 24 clinically isolated strains of S. aureus (including 23 beta-lactamase producing strains), 22 S. pyogenes, 20 E. coli (8 beta-lactamase producing strains), 24 K. pneumoniae (24 beta-lactamase producing strains), 20 H. influenzae (6 beta-lactamase producing strains). BRL 25000 showed MIC80 (cumulatively 80% of strains were inhibited) at 6.25 micrograms/ml against S. aureus, less than or equal to 0.10 micrograms/ml against inst S. pyogenes, 12.5 micrograms/ml against E. coli, 6.25 micrograms/ml against K. pneumoniae and 0.39 micrograms/ml against H. influenzae. BRL 25000 showed no improvement in MIC terms against beta-lactamase nonproducing strains compared with AMPC. However, BRL 25000 was markedly more effective against beta-lactamase producing strains. Thus BRL 25000 was up to 8 fold more active against S. aureus, 2 to 64 fold against E. coli, 4 to 128 fold against K. pneumoniae, 4 to 16 fold against H. influenzae than AMPC. Following oral administration of BRL 25000 granules (at a dose level of 12.5 mg/kg) to 2 children aged 9 and 11 years, the mean peak serum concentrations of AMPC and CVA were 8.33 +/- 2.43 micrograms/ml and 4.44 +/- 1.65 micrograms/ml respectively 1 hour after dosing. The half-lives of AMPC and CVA were 1.35 +/- 0.42 hours and 0.91 +/- 0.05 hour, respectively. The urinary excretion was 48.21 +/- 3.83% for AMPC and 16.90 +/- 7.06% for CVA in the first 6 hours after administration. In clinical studies, 23 pediatric patients aged 2 months to 12 years with bacterial infections were treated with BRL 25000 granules and the clinical effectiveness, bacteriological response and side effects were evaluated. The clinical response was assessed in 23 cases, 3 with acute rhinitis, 6 with acute purulent tonsillitis, 5 with acute bronchitis, 4 with acute pneumonia, 3 with impetigo, 1 with furunculosis and 1 with periproctal abscess. Results were excellent in 13 cases, good in 7, fair in 3 and hence the efficacy rate (excellent and good cases) was 87.0% (20/23). In particular the clinical response in 9 cases with infections due to beta-lactamase producing organisms was excellent in 6, good in 2, fair in 1 and the efficacy rate was 88.9% (8/9).(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Experimental and clinical studies on BRL 25000 (clavulanic acid-amoxicillin) in the pediatric field]. 384 22

Fundamental and clinical studies of aspoxicillin (ASPC, TA-058), a new penicillin antibiotic, were performed in pediatric field. Antimicrobial activity MIC of ASPC was compared with that of piperacillin (PIPC), ampicillin (ABPC) and carbenicillin (CBPC) for clinical isolates of S. aureus (24 strains), S. pyogenes (22 strains), H. influenzae (18 strains), E. coli (21 strains) and K. pneumoniae (23 strains). MIC of ASPC against S. pyogenes was distributed in less than 0.39 microgram/ml and this numerical value of MIC was very superior. MIC distributions of ASPC against S. aureus, H. influenzae and E. coli had 2 peaks respectively. It was presumed that the results are due to an existence of beta-lactamase producing strains. The sensitive strains in those were distributed in less than 1.56-12.5, less than or equal to 0.10 and 0.78-3.13 micrograms/ml, respectively, and those numerical value of MIC was superior. While against K. pneumoniae, all strains were distributed in more than 12.5 micrograms/ml and the antimicrobial activity of ASPC was very inferior. ASPC was as active as PIPC and ABPC against S. pyogenes, but more active then CBPC, ASPC was less active against S. aureus than PIPC and ABPC, but more active than CBPC. And ASPC was less active against H. influenzae and E. coli than PIPC, but more active than ABPC and CBPC. Against K. pneumoniae, strains that showed somewhat low numerical value of MIC at only PIPC were observed, but antimicrobial activities of ABPC and CBPC, as well as ASPC were very inferior. Absorption and excretion Serum level and urinary excretion of ASPC in 6 pediatric patients of 4 months to 12 years of age after one shot intravenous injection of 20 mg/kg were examined. The serum mean levels were 51.7 micrograms/ml at 1/4 hour, 38.2 micrograms/ml at 1/2 hour, 22.9 micrograms/ml at 1 hour, 3.0 micrograms/ml at 4 hours and 1.0 microgram/ml at 6 hours after injection, respectively. The mean half-life of serum level was 1.03 hours. The mean urinary levels were 4,646 micrograms/ml for 0-2 hours, 1,773 micrograms/ml for 2-4 hours and 299 micrograms/ml for 4-6 hours. The mean urinary recovery rate within 6 hours after injection was 64.7%. Clinical studies In order to evaluate clinical response, bacteriological response and side effects, ASPC was applied to 28 cases, i.e., 5 cases of acute purulent tonsillitis, 2 cases of acute purulent otitis media, 2 cases of acute bronchitis and 19 cases of acute pneumonia.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Fundamental and clinical studies on aspoxicillin in the pediatric field]. 385 60

Susceptibilities in various types of clinical isolates to cefmetazole (CMZ) were determined by the disk method and the serial agar dilution method for MIC measurement. CMZ showed high antibacterial activity for all Gram-positive cocci except E. faecalis, and for H. influenzae, E. coli, Klebsiella sp. and Proteus sp.. CMZ was administered on 33 patients with infections, mainly biliary tract infections, in the field of internal medicine. The clinical efficacy of the drug was 86.7% for infections of the biliary tract, 80.0% for respiratory tract infections, 100% for urinary tract infections and 76.7% for all cases. There were no adverse reaction or changes in laboratory findings caused by CMZ in any of the patients.
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PMID:[Experimental and clinical studies on cefmetazole in the field of internal medicine]. 385 74

The tendency for bacteria to develop resistance to enoxacin (Cl-919, AT-2266), a new oxyquinolone derivative, was investigated in vitro and in vivo. The mutation frequencies of Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli, Salmonella sp., and Haemophilus influenzae to enoxacin, norfloxacin, nalidixic acid, tobramycin, cephalexin, cefotaxime, ampicillin, azlocillin, oxacillin, and ticarcillin were determined by plating large numbers of organisms onto antibiotic-containing agar. Enoxacin resistance developed infrequently. For example, the mutation frequency of Ps. aeruginosa in the presence of enoxacin was 1 in 2.8 X 10(9) cells as compared to 1 in 1.1 X 10(6) for nalidixic acid. The increase in MIC after serial transfer through increasing concentrations of enoxacin ranged from 8-fold for Ps. aeruginosa and Staph. aureus to 256-fold for H. influenzae. Rats with chronic Ps. aeruginosa pneumonia were given subtherapeutic doses of enoxacin daily for ten weeks. Two rats were sacrificed weekly and the homogenized lungs were cultured on agar containing 5 mg/l of enoxacin and on antibiotic-free agar. No organisms resistant to 5 mg/l of enoxacin were recovered. No increase in the minimum inhibitory concentration of enoxacin for the infecting organism was seen.
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PMID:Low frequency of bacterial resistance to enoxacin in vitro and in experimental pneumonia. 386 24


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