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Pharmacokinetic and pharmacodynamic interaction study between midazolam and the macrolide antibiotics, erythromycin,

R A Yeates1, H Laufen, T Zimmermann

  • 1Department of Pharmacology, Pfizer-Mack Development Center, Illertissen, Germany.

International Journal of Clinical Pharmacology and Therapeutics
|February 10, 1998
PubMed

Insights

The hypnotic midazolam

Area of Science:

  • Pharmacology and Drug Interactions

Background:

  • Midazolam is a commonly used hypnotic agent.
  • Macrolide and azalide antibiotics can affect drug metabolism.
  • Potential interactions between midazolam and these antibiotics require investigation.

Purpose of the Study:

  • To re-evaluate the pharmacokinetic and pharmacodynamic interactions between midazolam and macrolide/azalide antibiotics.
  • To compare the clinical risks associated with co-administering midazolam with erythromycin, clarithromycin, or azithromycin.

Main Methods:

  • Recalculation of pooled data from two pharmacokinetic and pharmacodynamic studies.
  • Analysis of midazolam metabolism and pharmacodynamic activity in the presence of erythromycin, clarithromycin, and azithromycin.

Main Results:

  • Erythromycin and clarithromycin significantly inhibited midazolam metabolism and increased its pharmacodynamic effects.
  • Azithromycin demonstrated minimal to no impact on midazolam's pharmacokinetics or pharmacodynamics.
  • The interaction profile differed significantly between macrolides and azithromycin.

Conclusions:

  • Coadministration of midazolam with erythromycin or clarithromycin poses a higher clinical risk due to impaired metabolism and enhanced activity.
  • Co-administering midazolam with azithromycin appears to be clinically safer compared to macrolide antibiotics.
  • Prescribers should consider antibiotic choice when co-administering with midazolam.

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