In vitro antimicrobial activity of biapenem and its therapeutic efficacy in the treatment of respiratory infections

Yoshihiro Honda, Junichi Saito, Yushi Nakai, Akira Watanabe, Satoshi Shoji, Hiroshi Takahashi, Hiroaki Kikuchi, Toshihiro Nukiwa, Masakichi Motomiya, Tsuneo Sayama, Kiyoshi Konno, Masahumi Masuda, Kenichi Takeuchi, Mitsunobu Honma, Kousaku Nagai, Kazunao Niizuma, Yoshiyuki Anzai

    Research output: Contribution to journalArticlepeer-review

    2 Citations (Scopus)

    Abstract

    Biapenem (BIPM), a newly developed carbapenem antibiotic agent, was evaluated by in vitro tests and by in vivo trials. The minimum inhibitory concentrations (MICs) of BIPM, imipenem (IPM) and ceftazidime (CAZ) against methicillin-sensitive Staphylococcus aureus (MSSA) and methicillinresistant Staphylococcus aureus (MRSA), Haemophilus influenzae, Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Serratia marcescens, Pseudomonas aeruginosa and Branhamella (Moraxella) catarrhalis were determined by the microbroth dilution method. BIPM showed the strongest antimicrobial activity against P. aeruginosa, B. catarrhalis and E. cloacae. The MIC values of BIPM against MRSA, MSSA and gram-negative bacteria were equal to those of IPM. Penetration of BIPM into the lung tissue was studied in nine patients who had undergone chest surgery. The lung tissue levels of BIPM after intravenous administration of 0.3g ranged from 0.08 to 3.32μg/g and the lung/plasma concentration ratio ranged from 0.92 to 40.2%(mean 18.0%). BIPM concentration in plasma and sputum was studied in six patients with respiratory infections. The peak plasma concentration which ranged from 11.3 to 25.4μg/ml was observed immediately after infusion. The peak sputum concentration ranged from 0.43 to 2.72μg/ml at 1 to 4 hours after infusion. The sputum/plasma concentration ratio of 1.89∼∼12.48%(mean 6.3%) suggested that BIPM penetrated rapidly into the lung. Adaily dose of 0.3∼12g of BIPM was given intravenously for 15∼15 days to a total of 38 patients: 30 with pneumonia, 4 with pulmonary abscess, 2 with bronchiectasis, 1 with chronic bronchitis, 1 with infection supervening on pulmonary emphysema. Clinical effects were excellent in 12, good in 21, fair in 2 cases. No side effect was observed. From the above results, we conclude that BIPM is one of the most useful carbapenem agents for parenteral use as a first choice in the treatment of respiratory tract infections.

    Original languageEnglish
    Pages (from-to)301-313
    Number of pages13
    JournalChemotherapy
    Volume42
    DOIs
    Publication statusPublished - 1994 Jan 1

    Keywords

    • Biapenem

    ASJC Scopus subject areas

    • Pharmacology (medical)
    • Infectious Diseases
    • Pharmacology
    • Drug Discovery
    • Oncology

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