Japanese Journal of Chemotherapy
Online ISSN : 1884-5886
Print ISSN : 1340-7007
ISSN-L : 1340-7007
Volume 45, Issue 2
Displaying 1-5 of 5 articles from this issue
  • Koichi Deguchi, Yumiko Suzuki, Rika Ishihara, Yukiko Ishii, Arisa Naka ...
    1997 Volume 45 Issue 2 Pages 69-77
    Published: February 25, 1997
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    The drug susceptiblity pattern and frequency of detection of β-lactamases-producing strains were investigated in probable causative organisms among clinical isolates obtained in our laboratory in 1995 mainly cases of from community-acquired pneumonia and aspiration pneumonia. The results are summarized as follows;
    1. The detection frequency of β-lactamase-producing strains were high against methicillinresistant Staphylococcus aureus (MRSA) of S. aureus subsp. aureus, penicillin-resistant Streptococcus pneumoniae (PRSP) of S. pneumoniae, Haemophilus influenzae, and Moraxella subgenus Branhamella catarrhlis, and multiple drug resistant strains of Pseudomonas aeruginosa were a large. When the drug susceptiblity pattern was antibacterial spectrum of Empiric therapy against mainly community-acquired pneumonia, sulbactam/ampicillin (SBT/ABPC) appeared to be high effective. Because, the MIC90 of SBT/ABPC was low against S. pneumoniae including PRSP, β-lactamase-producing H. influenzae and M.(B.) catarrhalis.
    2. The drug susceptiblity pattern of microaerophilus gram-positive cocci (Streptococcus milleri group, Gemella morbillorum), Peptostreptococcus spp., Bacteroides spp. and Prevotella spp. suggested that the detection frequency of cephem (CEP)-, erythromycin (EM)-and clindamycin (CLDM)-resistant strains was high against in the S. milleri group, Peptostreptococcus spp. and Bacteroides spp., and that the detection on ferquency of CEP-and EM-resistant strains were high among G. morbillorum and Prevotella spp. The detection frequency of II -lactamase-producing strains was 80.0 % among Bacteroides spp. and Prevotella spp., and the MIC90 of SBT/ABPC and sulbactam/cefoperazone was lowest among Bacterioides spp. and Prevotella spp. When the MIC90 of the test drugs against those bacterial species made the drug susceptiblity pattern, the distribution of SBT/ABPC was low.
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  • Yoshimi Matsumoto, Kaori Ishiguro, Shuichi Tawara, Yukio Yoshizawe
    1997 Volume 45 Issue 2 Pages 78-84
    Published: February 25, 1997
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    A simple and rapid method to detect target enzymes of β-lactams the penicillin-binding proteins (PBPs), using 125 I-labeled penicillin V ([125I] PCV) was constructed.[125 I] PCV was easily synthesized by incubation of p-trimethylstannyl PCV with [125 I] Na.[125 I] PCV was detected by radioluminography (RLG) using an imaging plate (IP) which is more sensitive than an X-ray film. Use of [125I] based RLG in combination with a preparation of a membrane fraction withoutultracentrifugation, and use of a 96-well microtiter plate and a mini-gel electrophoresis system made it possible to determine the affinity of β-lactams for PBPs easily in a short time (less than 3 days). Electrophoretic patterns of PBPs detected by simil PCV were similar to those detected by [14C] penicillin G ([14C] PCG). Binding affinities of cefoselis (FK037) and imipenem/cilastatin for PBPs from MRSA and Escherichia coli, determined with [125I] PCV were similar to those determilled with [125 I] PCG. In conclusion, using [125 I] PCG instead of [14C] PCG provides a useful alternative for assay of binding affinity of β-lactams for PBPs.
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  • Shinji Iwakura, Hiroshi Tanimura, Minoru Ochiai, Masami Oka, Takeshi K ...
    1997 Volume 45 Issue 2 Pages 85-91
    Published: February 25, 1997
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    Patients treated with DU-6859a developed liver dysfunction more often than patients given any other fluoroquinolone, and the rates of occurrence of liver dysfunction differ according to sex, with males occurrence more common in more than females. The causes of liver dysfunction are thought to be hepatic cell obstruction by DU-6859a, changes in intestinal bacteria as a result of the high antibacterial potency of DU-6859a, increases in cheno-deoxycholic acid in the enterohepatic circulation as a result of blocking conversion of primary bile acids to secondary bile acids, or related to female hormones. Accordingly, to determine whether intestinal bacteria cause the liver dysfunction we administered low and high doses of DU-6859a to germ-free mice, carried out serum biochemistry tests, measured concentrations of bile acids in the gallbladder and bile acid components, and assessed whether that sufferred from liver dysfunction or not. The GOT values of the male mice averaged 598± 158 IU/1 in the controls and 283± 56 IU/1 in the high-dose DU-6859a group, and in female mice, 598±124 IU/1 in the controls and 283±56 IU/1 in high-dose DU-6859a group and the difference between these groups. GPT values in the male mice were 96± 22 IU/1 in the controls and 42± 2 IU/1 in the high-dose DU-6859 group and in the female mice, 177± 45 IU/1 in the controls and 165± 40 IU/1 in the high-dose DU-6859a group. There was no significant differences between these groups, and there were no significant differences between the bile acids in the gallbladder or bile acids components in the four groups. Liver dysfunction caused by DU-6859a proved to be strongly related to intestinal bacteria.
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  • Keiji Yamamoto, Mansho Itokazu, Naoki Kato, Kunitomo Watanabe
    1997 Volume 45 Issue 2 Pages 92-98
    Published: February 25, 1997
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    An in vitro and in vivo study was conducted to evaluate a novel tool, freeze-dried fibrin-antibiotic (FDFA) complex, for the treatment of osteomyelitis. The antimicrobial agent used was arbekacin (ABK). The in vitro elution study demonstrated that ABK was released from the FDFA complex into saline at a concentration of 37.9mg/ml on day 1 and the antibiotic was detectable at 0.4βg/ml on day 18. In experiments with rats, staphylococcus aureus (MIC of ABK, 0.2βg/ml) was inoculated into the right tibial medullary cavity along with a piece of absorbable thread. Implantation of the FDFA complex containing ABK 4 weeks after the bacterial challenge reduced the number of bacteria in the infected tibia to an undetectable level in one-third of the rats, a level which was not achieved by implantation of freeze-dried fibrin (FDF) alone or curettage alone. The roentgenographical and histopathological findings in the infected tibia showed that the FDFA complex containing ABK apparently steared the infected tibia to a curative course. These results suggest that implantation of the FDFA complex containing ABK is a promisingalternative treatment for osteomyelitis caused by S. aureus in humans.
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  • Seiji Matsuda
    1997 Volume 45 Issue 2 Pages 99-107
    Published: February 25, 1997
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    An investigation was carried out to determine the therapeutic effect of cefozopran (CZOP), a injectable cephem antibiotics on infections in pregnant women during the perinatal period. Of the 78 patients enrolled in the study, 66 were subjected to the analysis, with 3 of the subjects having been exclnded because being pregnant for less than 16 weeks, 4 because of protocol violations (regimen), and 5 because of uncertain eridence symptoms of infection or failure to undergo laboratory tests. CZOP was administered by intravenous drip infusion at doses of 0.5 to 2 g twice daily for periods of 3 to 14 days. The efficacy rate according to the evaluation of the Drug Efficacy Evaluation Committee was 83.9%(47/56). The efficacy rate in the 37 patients from whom causative pathogens were isolated was 81.1%(30/37). The bacteriological effect of CZOP could be evaluated in 30 patients. The eradication rate was 80.0%(24/30), with 42 of the 49 clinical isolates (85.7%) being eradicated. The efficacy rate determined by the attending physicians in 57 patients was 87.7%(50/57), and 81.6%(31/38) for the 38 patients from whom causative pathogens were isolated. The eradication rate was 80.6%(25/31) and 43 of the 50 clinical isolates (86.0%) were eradicated. Safety was evaluated as “safe” in 63 of the 66 assessable patients (95.5%). Moderate headache and nausea were experienced by 1 patient (1.5%) as adverse drug reactions, but the symptoms disappeared after the completion of treatment. Slight elevations of GOT, GPT, and LDH in laboratory tests were observed in one patient (1.5%), but these values returned to normal after the completion of treatment. When CZOP was administered by intravenous drip infusion in a dose of 1 g over 30 min. to pregnant women before parturition, maternal blood drug concentrations changed from 30.5-42.6μg/ml 1 hour after administration to 1.0-3.3βg/ml 6 hours after administration.Pharmacokinetic analysis in a two-compartment open model showed that the blood elimination half-life of CZOP was 1.4-5.6 hours. After intravenous administration of a 1 g dose. CZOP levels in the fetus, amniotic fluid, and breast milk were determined. The concentrations of drug in blod and tissue were determined 36 to 135 minutes after administration. The concentrations ranged from 17.4 to 74.6 βg/ml in maternal blood, from 9.0 to 21.7 βg/ml in umbilical cord blood, from 1.5 to 7.5 pglg, in the umbilical cord, from 6.0 to 27.2 βg/g in the placenta, from 8.3 to 30.6βg/g in the fetal membranes, and from 0.3 to 3.3 βg/ml in amniotic fluid. These results suggested that CZOP can be a useful drug in the treatment of bacterial infections occurring during the perinatal period. To firmly establish its safety, however, further studies are needed in larger populations.
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