Nefazodone and cyclosporine drug-drug interaction

J Heart Lung Transplant. 1999 Sep;18(9):913-5. doi: 10.1016/s1053-2498(98)00036-9.

Abstract

Depression is a significant post-transplant complication often necessitating drug therapy. Many of the newer selective serotonin reuptake inhibitor (SSRI) antidepressants are metabolized by the same cytochrome P450IIIA isoenzyme system that is responsible for the metabolism of cyclosporine, and these agents pose an interactive risk in transplant patients. We have observed nearly a 10-fold increase in whole blood cyclosporine concentrations in a cardiac transplant patient shortly after the addition of nefazodone antidepressant therapy. We suggest there is a clinically significant drug-drug interaction between nefazodone and cyclosporine due to inhibition of cytochrome P-450 IIIA4 isoenzymes by nefazodone.

Publication types

  • Case Reports

MeSH terms

  • Antidepressive Agents, Second-Generation / pharmacology*
  • Antidepressive Agents, Second-Generation / therapeutic use
  • Aryl Hydrocarbon Hydroxylases*
  • Cyclosporine / pharmacokinetics*
  • Cytochrome P-450 CYP3A
  • Cytochrome P-450 Enzyme Inhibitors
  • Drug Interactions
  • Enzyme Inhibitors / pharmacology
  • Female
  • Heart Transplantation*
  • Humans
  • Immunosuppressive Agents / pharmacokinetics*
  • Middle Aged
  • Oxidoreductases, N-Demethylating / antagonists & inhibitors
  • Piperazines
  • Triazoles / pharmacology*
  • Triazoles / therapeutic use

Substances

  • Antidepressive Agents, Second-Generation
  • Cytochrome P-450 Enzyme Inhibitors
  • Enzyme Inhibitors
  • Immunosuppressive Agents
  • Piperazines
  • Triazoles
  • nefazodone
  • Cyclosporine
  • Aryl Hydrocarbon Hydroxylases
  • Cytochrome P-450 CYP3A
  • Oxidoreductases, N-Demethylating