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Macrolide drug interactions: an update.

M P Pai1, D M Graci, G W Amsden

  • 1Clinical Pharmacology Research Center, Bassett Healthcare, Cooperstown, NY 13326, USA.

The Annals of Pharmacotherapy
|April 20, 2000
PubMed
Summary
This summary is machine-generated.

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Macrolide antibiotics like erythromycin can cause significant drug interactions by inhibiting cytochrome P450 enzymes. Azithromycin, however, shows a much safer interaction profile, with fewer clinically significant interactions observed.

Area of Science:

  • Pharmacology and Drug Interactions
  • Antimicrobial Agents
  • Drug Metabolism

Background:

  • Macrolide antibiotics are widely used, but their drug interaction profiles are a significant clinical concern.
  • Interactions often stem from the inhibition of cytochrome P450 enzyme systems, leading to altered metabolism of co-administered drugs.
  • Adverse events can arise from decreased drug metabolism induced by certain macrolides.

Purpose of the Study:

  • To delineate the drug interaction profiles of commonly prescribed macrolides in the US and Europe.
  • To assess the clinical implications and impact of these identified drug interactions.
  • To evaluate newer macrolides for improved safety regarding drug interactions.

Main Methods:

  • Comprehensive literature search of MEDLINE (1975-1998) for studies, reviews, and case reports on macrolide drug interactions.

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  • Inclusion of data from product manufacturers when literature information was insufficient.
  • Unbiased review of all gathered data to present a clear account of potential drug interactions.

    • Main Results:

    • Erythromycin and clarithromycin exhibit interaction profiles similar to each other, primarily due to cytochrome P450 inhibition.
    • Newer macrolides show variable success in improving interaction profiles; some remain similar to erythromycin.
    • Azithromycin, an azalide subclass member, demonstrated no significant inhibition of the cytochrome P450 system in vitro and has shown no classic macrolide drug interactions.

    Conclusions:

    • Clarithromycin's interaction profile mirrors erythromycin's, necessitating careful consideration when co-prescribing, especially given erythromycin's generic status.
    • Azithromycin exhibits a favorable profile with minimal clinically significant interactions involving drugs metabolized by the cytochrome P450 system.
    • Further clinical studies in patients on chronic medication are recommended to fully validate azithromycin's promising interaction profile.