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Involvement of CYP3A4 and CYP2D6 in the metabolism of haloperidol.
Cell Mol Neurobiol. 1997 Apr; 17(2):227-33.CM

Abstract

1. Human cytochrome P450 (CYP) isoenzymes expressed in a human cell line were used to elucidate their involvement in the metabolism of haloperidol (HAL). 2. It was found that CYP3A4 catalyzes the metabolism of HAL to HAL 1,2,3,6-tetrahydropyridine (HTP). HTP is further metabolized to HAL pyridinium (HP+) by both CYP3A4 and CYP2D6. 3. CYP3A4 and CYP2D6 are also responsible for the N-dealkylation of HAL. The N-dealkylation of reduced HAL (RH) was observed, which is catalyzed by CYP3A4. In addition, CYP3A4 also catalyzes the oxidation of RH back to HAL. 4. These results are discussed in terms of the metabolic interactions of HAL with other drugs and how this knowledge may be used to reduce the movement disorders induced by HAL.

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Authors+Show Affiliations

Fang J
Department of Psychiatry, University of Alberta, Edmonton, Canada.
Baker GB
No affiliation info available
Silverstone PH
No affiliation info available
Coutts RT
No affiliation info available

MeSH

BiotransformationCell LineCytochrome P-450 CYP2D6Cytochrome P-450 CYP3ACytochrome P-450 Enzyme SystemCytochrome ReductasesDrug InteractionsHaloperidolHumansKineticsMixed Function OxygenasesMovement DisordersOxidation-Reduction

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

9140699

Citation

Fang, J, et al. "Involvement of CYP3A4 and CYP2D6 in the Metabolism of Haloperidol." Cellular and Molecular Neurobiology, vol. 17, no. 2, 1997, pp. 227-33.
Fang J, Baker GB, Silverstone PH, et al. Involvement of CYP3A4 and CYP2D6 in the metabolism of haloperidol. Cell Mol Neurobiol. 1997;17(2):227-33.
Fang, J., Baker, G. B., Silverstone, P. H., & Coutts, R. T. (1997). Involvement of CYP3A4 and CYP2D6 in the metabolism of haloperidol. Cellular and Molecular Neurobiology, 17(2), 227-33.
Fang J, et al. Involvement of CYP3A4 and CYP2D6 in the Metabolism of Haloperidol. Cell Mol Neurobiol. 1997;17(2):227-33. PubMed PMID: 9140699.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Involvement of CYP3A4 and CYP2D6 in the metabolism of haloperidol. AU - Fang,J, AU - Baker,G B, AU - Silverstone,P H, AU - Coutts,R T, PY - 1997/4/1/pubmed PY - 1997/4/1/medline PY - 1997/4/1/entrez SP - 227 EP - 33 JF - Cellular and molecular neurobiology JO - Cell Mol Neurobiol VL - 17 IS - 2 N2 - 1. Human cytochrome P450 (CYP) isoenzymes expressed in a human cell line were used to elucidate their involvement in the metabolism of haloperidol (HAL). 2. It was found that CYP3A4 catalyzes the metabolism of HAL to HAL 1,2,3,6-tetrahydropyridine (HTP). HTP is further metabolized to HAL pyridinium (HP+) by both CYP3A4 and CYP2D6. 3. CYP3A4 and CYP2D6 are also responsible for the N-dealkylation of HAL. The N-dealkylation of reduced HAL (RH) was observed, which is catalyzed by CYP3A4. In addition, CYP3A4 also catalyzes the oxidation of RH back to HAL. 4. These results are discussed in terms of the metabolic interactions of HAL with other drugs and how this knowledge may be used to reduce the movement disorders induced by HAL. SN - 0272-4340 UR - https://www.unboundmedicine.com/medline/citation/9140699/Involvement_of_CYP3A4_and_CYP2D6_in_the_metabolism_of_haloperidol_ L2 - http://ovidsp.ovid.com/ovidweb.cgi?T=JS&PAGE=linkout&SEARCH=9140699.ui DB - PRIME DP - Unbound Medicine ER -