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Oral cimetidine prolongs clarithromycin absorption

G W Amsden1, K L Cheng, C A Peloquin

  • 1Clinical Pharmacology Research Center, Bassett Healthcare, Cooperstown, New York 13326, USA. amsden@telenet.net

Antimicrobial Agents and Chemotherapy
|July 14, 1998
PubMed
Summary

Cimetidine significantly alters clarithromycin absorption, delaying its formation and increasing half-lives. This drug interaction impacts pharmacokinetic profiles without affecting overall drug clearance.

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Area of Science:

  • Pharmacology
  • Drug Interactions
  • Clinical Pharmacokinetics

Background:

  • Clarithromycin is a widely used antibiotic.
  • Cimetidine is a common medication for acid reflux.
  • Potential interactions between co-administered drugs require investigation.

Purpose of the Study:

  • To investigate the pharmacokinetic interaction between oral cimetidine and clarithromycin.
  • To determine the effect of cimetidine on clarithromycin absorption and elimination.

Main Methods:

  • A pharmacokinetic study involving 12 healthy subjects.
  • Administration of single doses of clarithromycin alone and with steady-state oral cimetidine.
  • Measurement of serum concentrations of clarithromycin and its metabolite 14-OH-clarithromycin (14OHC).

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Main Results:

  • Cimetidine significantly decreased peak serum concentrations of clarithromycin and 14OHC by 46% and 43%, respectively.
  • Cimetidine delayed the formation of 14OHC by 68% and increased the half-lives of both compounds by 75% and 82%.
  • No significant changes were observed in the total oral clearance or area under the concentration-time curve for either drug.

Conclusions:

  • Oral cimetidine alters the absorption and disposition of clarithromycin.
  • The interaction leads to prolonged absorption and elimination phases for clarithromycin and its metabolite.
  • The underlying mechanism for this observed pharmacokinetic interaction remains unidentified.