FUNDAMENTAL AND CLINICAL STUDIES ON BRL 25000 (CLAVULANIC ACID-AMOXICILLIN)

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  • KUNII OTOHIKO
    Department of Internal Medicine, Institute of Medical Science, University of Tokyo
  • KOMATSU TAKASHI
    Department of Internal Medicine, Institute of Medical Science, University of Tokyo
  • WATABE YOSHIO
    Department of Internal Medicine, Institute of Medical Science, University of Tokyo
  • NISHITANI HAJIME
    Department of Internal Medicine, Institute of Medical Science, University of Tokyo
  • NAKATSUJI SATOKO
    Department of Internal Medicine, Institute of Medical Science, University of Tokyo
  • OHARA HIROSHI
    Department of Internal Medicine, Institute of Medical Science, University of Tokyo
  • HIRAYAMA MASAKIYO
    Department of Internal Medicine, Institute of Medical Science, University of Tokyo
  • MIWA SHIRO
    Department of Internal Medicine, Institute of Medical Science, University of Tokyo

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Other Title
  • BRL25000 (Clavulanic acid-Amoxicillin) に関する基礎的・臨床的研究
  • BRL25000 Clavulanic acid Amoxicillin ニ

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Description

BRL 25000, a formulation comprising the antibiotic amoxicillin and the β-lactamase inhibitor potassium clavulanate, was studied bacteriologically and therapeutically.<BR>MIC's were measured to determine the sensitivities of 101 strains of gram-negative bacteria to BRL25000 and amoxicillin. The MIC's of amoxicillin for 12 of 49 strains of E. coli were 12.5μg/ml while MIC's for 28 strains were in excess of 200μg/ml. However, MIS's of BRL 25000 were 12.5-25μg/ml for 28 strains, 25-50μg/ml for 6 strains and in excess of 200μg/ml for only 2 strains.<BR>Thus, most of the strains which were resistant to amoxicillin were susceptible to BRL25000. Similar results were obtained with 16 strains of Klebsiella, BRL 25000 showing MIC's of 12.5μg/ml or less for 10 of 14 strains which showed AMPC MIC's greater than 200μg/ml.<BR>Similar results were obtained with P.vulgaris however, against P. aeruginosa the majority of both the AMPC and BRL 25000 MIC's were 200μg/ml or greater.<BR>Using a BRL 25000 solution it was possible to determine AMPC and CVA by HPLC. AMPC and CVA were detected in urine and serum after administration of BRL 25000 but accurate measurement was not possible. A further study will therefore be required.<BR>BRL 25000 was administered to 2 cases of acute pyelonephritis, 1 case of acute cystitis, 1 case of chronic cystitis and 1 case of bronchopneumonia.<BR>The response to theraphy was assessed as exellent in 3 (60%), good in 1 (20%), and fair in 1 (20%). Overall the clinical efficacy was good to excellent in 80%(4/5) of the cases. In terms of bacteriological response, eradication was observed in 3 cases, a decrease in 1, and it was not possible to evaluate the response in the other. Laboratory abnormalities were observed in one patient consisting of temporary slightly elevated GOT and Al-P, but no severe side effects were found.

Journal

  • CHEMOTHERAPY

    CHEMOTHERAPY 30 (Supplement2), 191-197, 1982

    Japanese Society of Chemotherapy

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