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Cefmetazole: clinical evaluation of efficacy and safety in Japan

J Shimada, Y Hayashi, K Nakamura

    Drugs Under Experimental and Clinical Research
    |January 1, 1985
    PubMed

    Insights

    Cefmetazole (CMZ) demonstrated high efficacy across all age groups for various bacterial infections. It also elucidated the mechanism behind disulfiram-like reactions caused by certain cephalosporins, linked to acetaldehyde dehydrogenase inhibition.

    Area of Science:

    • Pharmacology
    • Clinical Medicine
    • Microbiology

    Background:

    • Antibiotics are crucial for treating bacterial infections.
    • Cephalosporins with specific side chains can cause disulfiram-like reactions.
    • Understanding drug efficacy and adverse reactions is vital for patient safety.

    Purpose of the Study:

    • To evaluate the clinical efficacy of cefmetazole (CMZ) in a large patient cohort.
    • To investigate the mechanism of disulfiram-like reactions induced by certain cephalosporins.
    • To compare the reaction-inducing potential of cefmetazole (CMZ), cefoperazone (CPZ), and latamoxef (LMOX).

    Main Methods:

    • Clinical evaluation of 23,855 patients treated with cefmetazole (CMZ) across 3,916 centers in Japan.
    • In vivo and in vitro experiments to study the disulfiram-like reaction mechanism.
    • Measurement of blood acetaldehyde concentrations and urinary mercaptomethyltetrazole (Me-TZ) excretion.

    Main Results:

    • Cefmetazole (CMZ) showed superior efficacy in treating infections caused by Gram-positive cocci, Gram-negative bacilli, and anaerobic bacteria sensitive to the drug.
    • The disulfiram-like reaction is caused by inhibition of acetaldehyde dehydrogenase, leading to increased blood acetaldehyde levels.
    • The severity of the reaction correlated with the urinary excretion rate of mercaptomethyltetrazole (Me-TZ), with CPZ > LMOX > CMZ.

    Conclusions:

    • Cefmetazole (CMZ) is an effective antibiotic for a wide range of bacterial infections in all age groups.
    • The methyltetrazolylthiomethyl side chain in certain cephalosporins is responsible for inhibiting acetaldehyde dehydrogenase.
    • Differences in biliary excretion and tissue stability influence the varying potential for disulfiram-like reactions among these antibiotics.

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