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Macrolides versus azalides: a drug interaction update

G W Amsden1

  • 1Clinical Drug Research Center, Saint Vincent Hospital, Worcester, MA 01604, USA.

The Annals of Pharmacotherapy
|September 1, 1995
PubMed
Summary
This summary is machine-generated.

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Macrolide and azalide antimicrobials can cause drug interactions, primarily through CYP3A enzyme inhibition. Azithromycin (an azalide) shows fewer interactions than older macrolides.

Area of Science:

  • Pharmacology
  • Microbiology

Background:

  • Macrolide and azalide antimicrobials are widely used.
  • Drug interactions with macrolides, particularly erythromycin, are well-documented.
  • These interactions are often mediated by the inhibition of the CYP3A enzyme system.

Purpose of the Study:

  • To review drug interaction profiles of macrolide and azalide antimicrobials.
  • To assess the clinical significance of these interactions.
  • To provide guidance for healthcare practitioners.

Main Methods:

  • Literature search of MEDLINE (1975-1995) for studies, reviews, and case reports.
  • Inclusion of manufacturer data when literature was insufficient.
  • Unbiased review of all available data on drug interactions.

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Main Results:

  • Erythromycin exhibits significant drug interactions due to CYP3A inhibition.
  • Newer macrolides show variable success in reducing interactions; 16-membered rings are improved.
  • Azalides, like azithromycin, demonstrate a significantly improved interaction profile, with azithromycin showing none of the classic macrolide interactions.

Conclusions:

  • Newer macrolides have a variable impact on drug interaction incidence.
  • Azithromycin, an azalide, exhibits fewer clinically significant CYP3A-mediated drug interactions compared to other macrolides and azalides.