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 147,016 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

During the 10-year period from 1980 through 1989 using gonococci isolated in Sapporo, we studied beta-lactamase production capacity and the sensitivity of various antibacterial agents and obtained the following results. 1. The frequency of isolating beta-lactamase producing gonococci (PPNG) displayed a gradual tendency to increase during the first half of the 80's and reached a peak in 1985 of 23.9% (61/255). However, thereafter it tended to decline and in 1989 it was 6.3% (2/32). 2. The sensitivity to penicillin-type antibacterial agents was higher against PPNG than non-PPNG against PCG, ABPC, and AMPC displaying about a 7 level MIC90 so that it was quite sensitive. Against CVA/AMPC, SBTPC it showed a relatively favorable MIC90. Also, the sensitivity of PPNG against AMPC with 1984 as the boundary, thereafter the MIC distribution was observed to decline somewhat. 3. Against the monobactam-type injectable drug, AZT, both non-PPNG and PPNG showed a low MIC distribution and against SPCM both showed a relatively high MIC distribution of 3.13-25 micrograms/ml. 4. In regard to the sensitivity to cephem-type antibacterial agents, against such 3rd generation injectables as CZX, CFTM-PI, etc. it displayed a particularly low MIC distribution. 5. Against tetracycline and macrolide antibacterial agents, it displayed a relatively high MIC distribution. 6. Against new quinolone type antibacterial agents, regardless of being non-PPNG or PPNG, it showed a low MIC.
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PMID:[A study on the beta-lactamase production for Neisseria gonorrhoeae and the sensitivity to various antibacterial agents]. 190 78

The efficacy of BRL28500, a formulation of ticarcillin (TIPC, 15 parts) and clavulanic acid (CVA, 1 part), against TIPC-resistant strains of Staphylococcus aureus, Escherichia coli and Klebsiella pneumoniae was studied both in vitro and in vivo. The MICs of BRL28500 against these beta-lactamase producing strains were lower than those of TIPC or CVA alone against such strains. When BRL28500 was added during the logarithmic growth phase of bacteria at a concentration equivalent to the MIC, it demonstrated marked lytic activity. Cells treated with BRL28500 underwent morphological change, becoming filament-like, similar to those treated with TIPC alone. With CVA alone at concentrations above the MIC the cells assumed a stable round form. In bacterial cultures of the beta-lactamase-producing strains, TIPC was protected from hydrolysis by the presence of CVA. The in vivo activity of BRL28500 against experimental infections in mice caused by beta-lactamase-producing strains of bacteria was superior to that of TIPC alone. TIPC and CVA were found to be well distributed in peritoneal fluid following subcutaneous administration of BRL28500 into mice with peritoneal infections. The residual TIPC concentrations achieved were higher than when TIPC alone was administered. These results suggest that BRL28500 will be effective in the treatment of human infections due to TIPC-resistant bacteria.
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PMID:The antibacterial activity of ticarcillin/clavulanic acid (BRL28500) against ticarcillin-resistant bacteria. 353 27

BRL 25000, granules preparation containing 2 parts of amoxicillin (AMPC) and 1 part of clavulanic acid (CVA, beta-lactamase inhibitor) as its potassium salt, has been investigated fundamentally and clinically. An in vitro study of the antibacterial activity of BRL 25000 against clinically isolated S. aureus (34 strains) showed higher activity than for AMPC alone and demonstrated that CVA potentiated the activity of AMPC, showing a synergistic effect against beta-lactamase producing organisms. A total of 27 pediatric patients aged between 6 months and 13 years 8 months (23 with respiratory infections and 4 with urinary tract infections) were treated with a daily dose ranging from 31.7 to 54.5 mg/kg, divided into 3 or 4 doses a day for periods of 4-18 days. The clinical effect was evaluated as excellent in 26 cases, poor in 1 case and the efficacy ratio was therefore 96.3% (26/27). The bacteriological effect against 12 organisms isolated from 9 patients was studied and all were eradicated (12/12). A drug-related side effect was observed in only 1 patient who developed diarrhea on the 4th day of treatment which continued during the treatment for 10 days. However, no severe side effect and no abnormality related to the drug in laboratory findings were observed. From these results it is concluded that BRL 25000 will be a clinically effective drug in the treatment of mild and moderate infections in the pediatric field.
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PMID:[Experimental and clinical studies on BRL 25000 (clavulanic acid-amoxicillin) granules in pediatric infections]. 384 20

Bacteriological and clinical evaluations of BRL 25000 (1 part clavulanic acid plus 2 parts amoxicillin) granules in the pediatric field have been performed. The MICs of BRL 25000 against 25 clinically isolated strains of S. aureus, 40 E. coli, and 14 K. pneumoniae were compared with those of AMPC. Against beta-lactamase non-producing strains of S. aureus and E. coli, the MICs of both drugs were nearly equal, however, against beta-lactamase producing strains of these species and K. pneumoniae, BRL 25000 was superior to AMPC. The blood levels of AMPC and CVA after single oral administration of approximately 15 mg/kg of BRL 25000 granules to fasted children were studied in 3 subjects. The mean levels of AMPC and CVA peaked about 1 hour after administration at values of 11.40 and 5.49 micrograms/ml, respectively, with half-lives of 0.91 and 1.02 hours, and AUCs of 23.52 and 12.66 hr X micrograms/ml, respectively. The 6-hour urinary recovery of AMPC ranged from 30.59% to 52.03% and for CVA from 16.31% to 45.18%. There was no significant difference between the blood level of AMPC following single oral administration of approximately 10 mg/kg AMPC granules and that of AMPC following single oral administration of approximately 15 mg/kg BRL 25000 granules to the same children. Clinical evaluation of BRL 25000 granules administered orally 3-4 times a day at total daily doses of between 42.9-52.9 mg/kg resulted in improvement, judged excellent or good, in all 7 cases of tonsillitis and 2 cases of pyelonephritis. In particular, the clinical effect was excellent in the case of tonsillitis where a beta-lactamase producing H. influenzae was isolated. In the total 11 cases treated, including 2 cases of mycoplasmal pneumonia excluded from the clinical evaluation, 1 case of rash and eosinophilia was observed. No other adverse reactions or abnormal laboratory findings were observed. The taste and flavor of the drug were well accepted by the children. It was concluded that BRL 25000 granules are promising new drug which should be markedly useful in the treatment of infections in pediatric outpatients.
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PMID:[Bacteriological and clinical evaluation of BRL 25000 (clavulanic acid-amoxicillin) granules in the pediatric field]. 384 23

BRL 25000 granules (containing 2 parts amoxicillin and 1 part clavulanic acid) have been studied fundamentally and clinically. The MICs of BRL 25000 against strains of S. aureus, E. coli, K. pneumoniae which were resistant to CEZ and beta-lactamase producing strains of H. influenzae were determined. The MICs of BRL 25000 at an inoculum of 10(6) cells/ml were 1/4 to 1/128 of those of AMPC and, in particular, the MICs of BRL 25000 were especially reduced against the organisms for which those of AMPC were more than 100 micrograms/ml. The pharmacokinetics of BRL 25000 were studied in 46 children at dose levels of 7.5 mg (8 fasting children, 7 non-fasting children), 10 mg/kg (4 fasting, 4 non-fasting), 15 mg/kg (4 fasting, 4 non-fasting), 20 mg/kg (8 fasting, 7 non-fasting). The peak serum concentrations in fasting children were marginally higher than those in non-fasting subjects. Values for AMPC and CVA from BRL 25000, dosed at 7.5, 10, 15 and 20 mg/kg to fasting children, 0.5-1 hour after dosing were 4.86 and 2.36 micrograms/ml, 5.20 and 1.69 micrograms/ml, 7.50 and 3.27 micrograms/ml, 9.38 and 6.30 micrograms/ml, respectively. In non-fasting subjects, corresponding values were 2.84 and 1.01 micrograms/ml, 4.53 and 2.10 micrograms/ml, 7.29 and 4.08 micrograms/ml, 6.83 and 2.96 micrograms/ml, respectively. The biological half-lives of AMPC and CVA, following the administration of BRL 25000, show no significant difference between the fasting and non-fasting states. Values for AMPC and CVA in fasting children were 0.85-1.15 hours and 0.64-1.03 hours, and in non-fasting children, 1.18-1.79 hours and 0.78-1.02 hours, respectively. The time to reach the peak serum concentration and half-lives were similar for AMPC and CVA when dosed as BRL 25000. Peak urinary concentrations for BRL 25000 (AMPC and CVA) at dose levels of 7.5, 10, 15, 20 mg/kg to fasting children were 681.8 and 148.2 micrograms/ml, 247.1 and 66.3 micrograms/ml, 484.2 and 149.1 micrograms/ml, 1,796.5 and 372.0 micrograms/ml, whilst in the non-fasting state the values were 496.3 and 83.2 micrograms/ml, 991.1 and 156.7 micrograms/ml, 2,397.5 and 460.7 micrograms/ml, 1, 896.3 and 323.4 micrograms/ml, respectively. The peak urinary concentration in the fasting state was observed at 0-2 hours after dosing, and in non-fasting individuals it occurred at 2-4 hours after dosing.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Experimental and clinical studies on BRL 25000 (clavulanic acid-amoxicillin) granules in the pediatric field]. 384 24

MICs of BRL 25000, a combination of a newly developed beta-lactamase inhibitor CVA and AMPC in the ratio of 1 to 2, were determined against a number of bacterial strains and compared with those of AMPC, CVA, CEX and CCL. The 98 bacterial strains tested included 2-S. aureus, 23-H. influenzae, 25-E. coli, 22-K. pneumoniae and 26-P. mirabilis. In pharmacokinetic studies, BRL 25000 medium granules were administered to groups of 3 male subjects, aged between 7 years 8 months and 9 years 5 months, at doses of 10, 15 and 20 mg/kg, 2 hours after a meal. The resultant serum and urine concentrations and drug recoveries were measured. Furthermore, BRL 25000 was administered to a total 43 patients (2-pharyngitis, 8-tonsillitis, 3-bronchitis, 2-pneumonia and 28-urinary tract infection) whom clinically evaluable. An average daily dosage of 45.3 mg/kg was given, in 3 or 4 divided doses, for a period of 8 days on average. Clinical and bacteriological effects as well as side effects were studied. In the microbiological studies on 98 clinical strains, including beta-lactamase negative bacteria, BRL 25000 showed MICs against the Gram-positive cocci (2-S. aureus) superior to the other 4 drugs at inoculum sizes of 10(8) and 10(6) cells/ml. For the Gram-negative bacilli, against H. influenzae at inoculum sizes of 10(8) and 10(6) cells/ml, BRL 25000 was inferior in the small MIC range but superior in the large MIC range to AMPC, and was superior to the other 3 drugs. Against E. coli at an inoculum of 10(8) cells/ml, BRL 25000 showed antibacterial activity next to AMPC and CCL whilst at an inoculum of 10(6) cells/ml, it was inferior in the small MIC range but superior in the large MIC range to AMPC and CEX and was inferior to CCL but superior to CVA. Against K. pneumoniae at an inoculum of 10(8) cells/ml, BRL 25000 was equal to AMPC, CVA and CEX but inferior to CCL, whilst at an inoculum of 10(6) cells/ml, it was inferior to CCL but superior to the other 3 drugs. Against P. mirabilis at inoculum sizes of 10(8) and 10(6) cells/ml, BRL 25000 was inferior in the small MIC range but equal or superior in the large MIC range to AMPC, and was superior to CVA and CEX.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Experimental and clinical trials of BRL 25000 (clavulanic acid-amoxicillin) granules in the field of pediatrics]. 389 76

The authors have carried out laboratory and clinical studies on the BRL 25000 granule (containing 2 parts amoxicillin and 1 part clavulanic acid). The antibacterial activity of BRL 25000 against 29 clinically isolated strains of S. aureus, 30 E. coli and 30 K. pneumoniae were measured by the agar dilution method using an inoculum size of 10(6) cells/ml. beta-Lactamase production was detected by the Nitrocefin method. The MICs of BRL 25000 against S. aureus ranged from 0.2 approximately 12.5 micrograms/ml, with the majority of strains being inhibited by 1.56 micrograms/ml or less. Seven beta-lactamase producing strains of S. aureus were all inhibited by less than 12.5 micrograms/ml. The range against E. coli was 1.56 approximately 100 micrograms/ml, with the majority inhibited by 6.25 micrograms/ml or less. Fifteen beta-lactamase producing strains of E. coli were inhibited by 6.25 approximately 100 micrograms/ml and the majority by 25 micrograms/ml or less. All strains of K. pneumoniae were beta-lactamase producers and the MIC distribution against K. pneumoniae was 1.56 approximately 50 micrograms/ml, with a majority inhibited by 3.13 micrograms/ml or less, 96% of strains, were inhibited by less than 6.25 micrograms/ml. Against K. pneumoniae, BRL 25000 showed a 8 to 16-fold superiority when compared with AMPC. In a pharmacokinetic study, BRL 25000 granules were orally administered to children in the fasting state at single doses of 7.5 mg/kg and 20 mg/kg. The peak serum levels of AMPC were 6.13 and 6.94 micrograms/ml approximately 1 hour after administration and decreased with half-lives of 1.08 and 0.97 hours, respectively. The corresponding serum levels of CVA were 1.16 and 1.90 micrograms/ml at 1 hour after administration, with half-lives of 0.99 and 0.87 hour, respectively. In clinical studies, the BRL 25000 granule was effective in 39 cases of bacterial infection out of a total of 41 treated. Side effects were limited to 2 cases of diarrhea and minor changes in laboratory findings were elevation of serum GOT (1 case), elevation of serum GPT (1 case), and eosinophilia (2 cases).
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PMID:[Laboratory and clinical studies of BRL 25000 (clavulanic acid-amoxicillin) granules in the pediatric field]. 400 52

We tested susceptibilities of 46 strains of clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) to arbekacin (ABK), tobramycin (TOB), ticarcillin (TIPC), clavulanic acid/ticarcillin (CVA/TIPC) and fosfomycin (FOM). Twelve strains had penicillinase activity. Most strains were resistant to TOB, TIPC, FOM and CVA/TIPC, but ABK inhibited 80% of the 46 MRSA strains at a concentration of 1.56 microgram/ml. The combination of ABK and FOM was indifferent. Synergism was observed, however, between FOM and TIPC against 79% of penicillinase non-producing MRSA. This synergism may mean that FOM inhibits the production of penicillin-binding protein 2' in some strains of penicillinase non-producing MRSA.
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PMID:[Activities of antibiotics against methicillin-resistant Staphylococcus aureus with particular reference to synergetic effect between ticarcillin and fosfomycin on penicillinase non-producing methicillin-resistant S. aureus]. 836 Sep 77

In order to investigate antimicrobial activities of clavulanic acid/ticarcillin (CVA/TIPC) against Escherichia coli, Enterobacter spp. and Pseudomonas aeruginosa in 1992 and 1994, beta-lactamase activities were analyzed and minimum inhibitory concentrations (MICs) were determined including those of the control drugs. The results are as follows; 1. Compared to a report in 1980, the MIC distributions of CVA/TIPC against E. coli and P. aeruginosa did not show large differences. We found, however, that CVA/TIPC-resistant strains increased among Enterobacter spp. 2. Almost all of CVA/TIPC-resistant strains of Enterobacter spp. were also resistant to cephems and new quinolones, thus they were multiple drug resistant. 3. CVA/TIPC showed strong antimicrobial activities against penicillinase producing E. coli.
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PMID:[Antimicrobial activities of clavulanic acid/ticarcillin against clinical isolates]. 858 64

In order to investigate antimicrobial activities of clavulanic acid/amoxicillin (CVA/AMPC) against freshly isolated clinical strains obtained in 1995, beta-lactamase activities and minimum inhibitory concentration (MICs) were determined including those of the control drugs. The results are summarized as follows; 1. Detection frequencies of beta-lactamase producing strains were as follows: methicillin-susceptible Staphylococcus aureus subsp. aureus (MSSA, 90.0%), Haemophilus influenzae (22.0%), Moraxella subgenus Branhamella catarrhalis (100.0%), Escherichia coli (100.0%), Klebsiella pneumoniae subsp. pneumoniae (100.0%) and Neisseria gonorrhoeae (14.0%). It appeared that beta-lactamases produced by these strains were mostly penicillinase or enzyme of similar that. 2. Antimicrobial activities of CVA/AMPC against beta-lactamase producing strains were stronger than those of AMPC, and MIC90 of CVA/AMPC against benzylpenicillin (PCG)-insensitive or resistant Streptococcus pneumoniae was lower than those of sultamicillin, cefaclor and cefpodoxime. 3. CVA showed strong beta-lactamase inhibitory effect against M.(B.) catarrhalis of direct and indirect pathogenicity. We can expect CVA/AMPC to negate or decrease the influence of indirect pathogenicity.
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PMID:[Antimicrobial activities of clavulanic acid/amoxicillin against freshly isolated clinical strains from outpatients]. 858 66


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