Effect of fluvoxamine on the pharmacokinetics of imipramine and desipramine in healthy subjects

E. Spina, A. M. Pollicino, A. Avenoso, G. M. Campo, E. Perucca, A. P. Caputi

Research output: Contribution to journalArticlepeer-review

Abstract

The effect of the selective serotonin reuptake inhibitor fluvoxamine (100 mg/day for 10 consecutive days) on the kinetics of a single oral dose of imipramine (50 mg) and desipramine (100 mg) was investigated in 12 healthy subjects. Compared with a control session, treatment with fluvoxamine caused a significant prolongation of imipramine half-life (from 22.8 ± 6.4 to 40.5 ± 5.0 h, means ± SD, p <0.01) and a marked decrease in imipramine apparent oral clearance (from 1.02 ± 0.19 to 0.28 ± 0.06 L/h/kg, p <0.0001). No significant changes in desipramine kinetics were observed during fluvoxamine treatment. These findings indicate that, at the dosage tested, fluvoxamine markedly inhibits the demethylation of imipramine without affecting significantly the CYP2D6-mediated hydroxylation of desipramine.

Original languageEnglish
Pages (from-to)243-246
Number of pages4
JournalTherapeutic Drug Monitoring
Volume15
Issue number3
Publication statusPublished - 1993

Keywords

  • Demethylation
  • Desipramine
  • Drug interaction
  • Fluvoxamine
  • Hydroxylation
  • Imipramine

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology
  • Biochemistry, Genetics and Molecular Biology(all)
  • Biochemistry
  • Health, Toxicology and Mutagenesis
  • Public Health, Environmental and Occupational Health
  • Toxicology

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