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Related Experiment Videos

Cyclosporine-phenytoin interaction.

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

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

Drug Metabolism and Disposition: the Biological Fate of Chemicals
|March 1, 1988
PubMed
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Phenytoin significantly increases the metabolism of cyclosporine (CsA) in the body. This drug interaction may affect cyclosporine levels in transplant patients taking anti-convulsants.

Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Transplantation Medicine

Background:

  • Cyclosporine (CsA) is a vital immunosuppressant for preventing organ transplant rejection.
  • CsA undergoes extensive liver metabolism via hydroxylation and demethylation.
  • Phenytoin is a common anti-convulsant used post-transplant.

Purpose of the Study:

  • To investigate the effect of chronic phenytoin treatment on cyclosporine (CsA) disposition.
  • To determine if phenytoin alters CsA metabolism and clearance.

Main Methods:

  • CsA disposition was assessed before and after 5 days of phenytoin treatment (30 mg/kg, orally).
  • CsA concentrations were quantified using High-Performance Liquid Chromatography (HPLC).

Main Results:

Related Experiment Videos

  • Cyclosporine clearance (CL) was significantly increased after chronic phenytoin treatment (25.3 +/- 3.11 ml/min/kg) compared to pre-treatment values (15.46 +/- 0.76 ml/min/kg).
  • No significant alterations were observed in the volume of distribution of CsA.

Conclusions:

  • Phenytoin likely induces the hepatic metabolism of cyclosporine (CsA).
  • This interaction highlights a potential clinical concern for transplant recipients requiring both medications.