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Cyclosporine-cimetidine interaction.

M J D'Souza1, S H Pollock, H M Solomon

  • 1Department of Pharmaceutical Sciences, School of Pharmacy, Mercer University, Atlanta, GA 30312.

Drug Metabolism and Disposition: the Biological Fate of Chemicals
|January 1, 1988
PubMed
Summary
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Cimetidine, an H2 antagonist, significantly reduces cyclosporine (CsA) clearance by inhibiting its liver metabolism. This interaction impacts how the body processes CsA, crucial for transplant patients.

Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Transplantation Medicine

Background:

  • Cyclosporine (CsA) is a vital immunosuppressant to prevent organ transplant rejection.
  • CsA is primarily metabolized in the liver by the cytochrome P450 enzyme system.
  • Cimetidine, a common H2 antagonist, is known to inhibit P450 enzymes.

Purpose of the Study:

  • To investigate the effect of chronic cimetidine treatment on cyclosporine disposition.
  • To determine if cimetidine alters cyclosporine metabolism in vivo.

Main Methods:

  • Administered CsA (15 mg/kg, IV) to subjects before and after 5 days of cimetidine (60 mg/kg, PO) treatment.
  • Quantified CsA levels using High-Performance Liquid Chromatography (HPLC).
  • Calculated pharmacokinetic parameters including clearance (Cl) and volume of distribution.

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Main Results:

  • Chronic cimetidine treatment significantly reduced CsA clearance (10.36 ml/min/kg) compared to controls (15.46 ml/min/kg).
  • No significant change was observed in the volume of distribution of CsA.
  • The reduced clearance is attributed to cimetidine's inhibition of CsA metabolism.

Conclusions:

  • Cimetidine inhibits the hepatic metabolism of cyclosporine.
  • This drug interaction necessitates careful consideration in patients receiving both medications.
  • The findings highlight the role of P450 inhibition in altering CsA pharmacokinetics.