Serum levels of aripiprazole and dehydroaripiprazole, clinical response and side effects
- 1 January 2008
- journal article
- research article
- Published by Taylor & Francis Ltd in The World Journal of Biological Psychiatry
- Vol. 9 (3), 212-218
- https://doi.org/10.1080/15622970701361255
Abstract
Aripiprazole, a novel antipsychotic drug, is metabolized by CYP3A4 and CYP2D6 forming mainly its active metabolite dehydroaripiprazole. In this study, aripiprazole and dehydroaripiprazole serum levels of psychiatric patients were measured and related to dose, comedication, and clinical effects including therapeutic and side effects. Patients were treated with mean doses of 20±8 mg/day of aripiprazole (median 15 mg, range 7.5–60 mg). Serum levels correlated significantly with the dose (r=0.419; P<0.01), with a mean value of aripiprazole of 214±140 ng/ml. Mean concentrations of the active metabolite dehydroaripiprazole amounted to 40% of the parent compound. Comedication with CYP3A4 and CYP2D6 inducers or inhibitors changed serum levels up to 51%. Improvement was best in patients with a serum level between 150 to 300 ng/ml. No or only mild side effects were detected in patients, with aripiprazole plasma concentrations between 110 and 249 ng/ml. A total of 32% of the patients who received no other antipsychotic drug besides aripiprazole reported side effects; tension being the most frequent one. Since serum levels of aripiprazole and dehydroaripiprazole were highly variable between individuals, and distinct ranges were associated with good therapeutic response and minimal side effects, it seems likely that therapeutic drug monitoring can be helpful to improve the antipsychotic drug therapy.Keywords
This publication has 16 references indexed in Scilit:
- Pharmacokinetic Variability of Aripiprazole and the Active Metabolite Dehydroaripiprazole in Psychiatric PatientsTherapeutic Drug Monitoring, 2006
- A prospective, multicenter, randomized, parallel-group, open-label study of aripiprazole in the management of patients with schizophrenia or schizoaffective disorder in general psychiatric practice: Broad Effectiveness Trial With Aripiprazole (BETA)Schizophrenia Research, 2006
- Clinical implications of Brief Psychiatric Rating Scale scoresThe British Journal of Psychiatry, 2005
- Therapeutic Monitoring of Aripiprazole by HPLC with Column-Switching and Spectrophotometric DetectionClinical Chemistry, 2005
- The AGNP-TDM Expert Group Consensus Guidelines: Therapeutic Drug Monitoring in PsychiatryPharmacopsychiatry, 2004
- Aripiprazole, A Novel Atypical Antipsychotic Drug with a Unique and Robust PharmacologyNeuropsychopharmacology, 2003
- PM Frequencies of Major CYPs in Asians and CaucasiansDrug Metabolism Reviews, 2003
- Therapeutic Window of Serum Haloperidol Concentration in Acute Schizophrenia and Schizoaffective DisorderPharmacopsychiatry, 1998
- Novel positive inotropic agents: synthesis and biological activities of 6-(3-amino-2-hydroxypropoxy)-2(1H)-quinolinone derivativesJournal of Medicinal Chemistry, 1992
- The UKU side effect rating scale: A new comprehensive rating scale for psychotropic drugs and a cross‐sectional study of side effects in neuroleptic‐treated patientsActa Psychiatrica Scandinavica, 1987