Lack of interaction between citalopram and the CYP3A4 substrate triazolam

Pharmacotherapy. 2000 Jul;20(7):750-5. doi: 10.1592/phco.20.9.750.35198.

Abstract

Study objectives: To determine the effect of the selective serotonin reuptake inhibitor citalopram on plasma levels of triazolam, and to determine the effect of a single dose of triazolam on steady-state levels of citalopram and its major metabolites.

Design: Open-label, multidose study.

Setting: Clinical Studies, Ltd., Fort Lauderdale, Florida.

Participants: Eighteen healthy male and female volunteers.

Interventions: Subjects received triazolam 0.25 mg alone and another 0.25-mg dose after 4 weeks of citalopram 20 mg/day for 1 week, followed by 3 weeks of citalopram 40 mg/day

Measurements and main results: Pharmacokinetic parameters were determined after single-dose administration of triazolam alone, after administration of citalopram alone at steady state, and after coadministration of the drugs. The pharmacokinetics of triazolam and its metabolite alpha-hydroxytriazolam were unchanged by citalopram coadministration. Triazolam appeared to be absorbed slightly more quickly during coadministration. Citalopram kinetics were unaffected by coadministration.

Conclusion: No pharmacokinetic interaction between the drugs was observed, suggesting that triazolam and other cytochrome P450 3A4 substrates can be coadministered safely with citalopram.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Antidepressive Agents / adverse effects*
  • Area Under Curve
  • Citalopram / adverse effects*
  • Cytochrome P-450 CYP3A
  • Cytochrome P-450 Enzyme System / metabolism*
  • Drug Interactions
  • Female
  • Humans
  • Hypnotics and Sedatives / blood
  • Hypnotics and Sedatives / pharmacokinetics*
  • Male
  • Mixed Function Oxygenases / metabolism*
  • Triazolam / blood
  • Triazolam / pharmacokinetics*

Substances

  • Antidepressive Agents
  • Hypnotics and Sedatives
  • Citalopram
  • Triazolam
  • Cytochrome P-450 Enzyme System
  • Mixed Function Oxygenases
  • CYP3A protein, human
  • Cytochrome P-450 CYP3A
  • CYP3A4 protein, human