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Third-generation cephalosporins: a critical evaluation.

S L Barriere, J F Flaherty

    Clinical Pharmacy
    |July 1, 1984
    PubMed
    Summary

    This review covers six third-generation cephalosporins, detailing their chemistry, activity against bacteria like E. coli and H. influenzae, and clinical uses. These antibiotics offer broad-spectrum efficacy and cost-effectiveness for serious infections.

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    Area of Science:

    • Pharmacology
    • Infectious Diseases
    • Medicinal Chemistry

    Background:

    • Third-generation cephalosporins represent a significant advancement in antibiotic therapy.
    • Their broad spectrum of activity and improved pharmacokinetic profiles offer advantages over older agents.

    Purpose of the Study:

    • To provide a comprehensive review of six third-generation cephalosporins: cefotaxime, moxalactam, cefoperazone, ceftizoxime, ceftriaxone, and cefmenoxime.
    • To evaluate their chemistry, structure-activity relationships, mechanism of action, spectra of activity, pharmacokinetics, clinical utility, adverse effects, and cost-effectiveness.

    Main Methods:

    • Literature review and synthesis of existing data on the specified third-generation cephalosporins.
    • Comparative analysis of their pharmacological and clinical properties.

    Main Results:

    • These cephalosporins exhibit broad-spectrum activity against many Gram-negative pathogens, including E. coli and H. influenzae, but limited activity against MRSA.
    • Ceftriaxone's long half-life allows once-daily dosing; moxalactam and cefotaxime show good penetration into cerebrospinal fluid.
    • They are effective for meningitis and serious Enterobacteriaceae infections, with moxalactam showing promise in intra-abdominal infections.

    Conclusions:

    • Third-generation cephalosporins are valuable agents for treating serious Gram-negative infections, including meningitis.
    • Despite higher costs, their efficacy, dosing convenience, and safety profile often make them cost-effective.
    • Adverse effects are generally similar to other beta-lactams, with notable exceptions like coagulopathy with moxalactam and cefoperazone.

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