Drug metabolism and atypical antipsychotics.

Article Details

Citation

Prior TI, Chue PS, Tibbo P, Baker GB

Drug metabolism and atypical antipsychotics.

Eur Neuropsychopharmacol. 1999 Jun;9(4):301-9.

PubMed ID
10422890 [ View in PubMed
]
Abstract

The introduction of the atypical antipsychotics clozapine, risperidone, olanzapine, quetiapine and sertindole for the treatment of schizophrenia has coincided with an increased awareness of the potential of drug-drug interactions, particularly involving the cytochrome P450 (CYP) enzymes. The current literature describing the pharmacokinetics of the metabolism of these agents, including their potential to influence the metabolism of other medications, is reviewed. Clozapine appears to be metabolized primarily by CYP1A2 and CYP3A4, with additional contributions by CYP2C19 and CYP2D6. In addition, clozapine may inhibit the activity of CYP2C9 and CYP2C19, and induce CYP1A, CYP2B and CYP3A. Risperidone is metabolized by CYP2D6, and possibly CYP3A4. In vitro data indicate that olanzapine is metabolized by CYP1A2 and CYP2D6. Quetiapine is metabolised by CYP3A4 and sertindole by CYP2D6. There is, however, a general paucity of in vivo data regarding the metabolism of the atypical antipsychotics, indicating a need for further research in this area.

DrugBank Data that Cites this Article

Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
ClozapineCytochrome P450 1A1ProteinHumans
No
Inducer
Details
ClozapineCytochrome P450 2C19ProteinHumans
No
Substrate
Inhibitor
Details
ClozapineCytochrome P450 3A4ProteinHumans
No
Substrate
Inhibitor
Inducer
Details
SertindoleCytochrome P450 2D6ProteinHumans
Unknown
Substrate
Details