Effects of paroxetine on plasma concentrations of aripiprazole and its active metabolite, dehydroaripiprazole, in Japanese patients with schizophrenia

Ther Drug Monit. 2012 Apr;34(2):188-92. doi: 10.1097/FTD.0b013e31824a31e6.

Abstract

Background: The effects of paroxetine coadministration on plasma concentrations of aripiprazole and its active metabolite, dehydroaripiprazole, were studied in 14 Japanese patients with schizophrenia.

Methods: The patients had been treated with aripiprazole (24 mg/d in 5 cases, 12 mg/d in 5 cases, and 6 mg/d in 4 cases) for at least 2 weeks. Paroxetine 10 mg/d was coadministered during the first week, and the dose was increased to 20 mg/d during the second week. Blood samples were taken 3 times, before the start of paroxetine and then 1 and 2 weeks after paroxetine coadministration. On the same days, the severity of illness and extrapyramidal adverse effects were evaluated by the clinical global impressions and the Drug-Induced Extra-Pyramidal Symptoms Scale, respectively. Plasma concentrations of aripiprazole and dehydroaripiprazole were measured using liquid chromatography with mass spectrometric detection.

Results: Plasma concentrations of aripiprazole and the sum of aripiprazole and dehydroaripiprazole during coadministration of paroxetine 10 and 20 mg/d were significantly (P < 0.05) higher (1.5-fold and 1.7-fold; 1.4-fold and 1.5-fold) than those before paroxetine coadministration. Those values during coadministration of paroxetine 20 mg/d were also significantly (P < 0.05) higher (1.1-fold and 1.1-fold) than those during coadministration of paroxetine 10 mg/d. Plasma concentrations of dehydroaripiprazole were unchanged throughout the study period. The mean clinical global impression score was significantly (P < 0.05) higher during the paroxetine 10 mg/d than that before coadministration, whereas the Drug-Induced Extra-Pyramidal Symptoms Scale scores remained unchanged during the study.

Conclusions: This study suggests that lower doses (10-20 mg/d) of paroxetine coadministration increase plasma concentrations of aripiprazole and the sum of aripiprazole and dehydroaripiprazole.

Publication types

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

MeSH terms

  • Adult
  • Aged
  • Antipsychotic Agents / administration & dosage
  • Antipsychotic Agents / adverse effects
  • Antipsychotic Agents / pharmacokinetics*
  • Aripiprazole
  • Asian People
  • Basal Ganglia Diseases / chemically induced
  • Chromatography, Liquid
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Female
  • Humans
  • Japan
  • Male
  • Mass Spectrometry
  • Middle Aged
  • Paroxetine / administration & dosage
  • Paroxetine / adverse effects
  • Paroxetine / pharmacology*
  • Piperazines / administration & dosage
  • Piperazines / adverse effects
  • Piperazines / pharmacokinetics*
  • Psychiatric Status Rating Scales
  • Quinolones / administration & dosage
  • Quinolones / adverse effects
  • Quinolones / pharmacokinetics*
  • Schizophrenia / drug therapy
  • Schizophrenia / physiopathology
  • Selective Serotonin Reuptake Inhibitors / pharmacology
  • Severity of Illness Index
  • Young Adult

Substances

  • Antipsychotic Agents
  • Piperazines
  • Quinolones
  • Serotonin Uptake Inhibitors
  • dehydroaripiprazole
  • Paroxetine
  • Aripiprazole