Pharmacogenetics of classical and new antipsychotic drugs.
Article Details
- CitationCopy to clipboard
Otani K, Aoshima T
Pharmacogenetics of classical and new antipsychotic drugs.
Ther Drug Monit. 2000 Feb;22(1):118-21.
- PubMed ID
- 10688273 [ View in PubMed]
- Abstract
Several classical antipsychotic drugs, i.e., chlorpromazine, haloperidol, perphenazine, thioridazine and zuclopenthixol; and some new neuroleptic drugs, i.e., risperidone and sertindole, are metabolized predominantly by cytochrome P450 (CYP) 2D6. Significant relationships have been reported between the steady state plasma concentrations (Css) of some classical neuroleptics and the CYP2D6 activity or genotype. Several of these drugs also potently inhibit the CYP2D6 activity. These facts explain several drug metabolic interactions of the classical drugs. Two studies failed to show that the CYP2D6 activity predicts the therapeutic effects of haloperidol or perphenazine. Some studies have suggested that the poor metabolizer phenotype is associated with the development of oversedation during treatment with the classical drugs, but other studies have been inconsistent or negative. The CYP2D6 phenotyping and genotyping appear to be useful in predicting the Css of some classical drugs, but their usefulness in predicting clinical effects must be further explored.
DrugBank Data that Cites this Article
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Chlorpromazine Cytochrome P450 2D6 Protein Humans UnknownSubstrateInhibitorDetails Haloperidol Cytochrome P450 2D6 Protein Humans UnknownSubstrateInhibitorDetails Perphenazine Cytochrome P450 2D6 Protein Humans UnknownSubstrateInhibitorDetails Thioridazine Cytochrome P450 2D6 Protein Humans UnknownSubstrateInhibitorDetails