Influence of the CYP2D6*10 allele on the metabolism of mexiletine by human liver microsomes.

Article Details

Citation

Senda C, Yamaura Y, Kobayashi K, Fujii H, Minami H, Sasaki Y, Igarashi T, Chiba K

Influence of the CYP2D6*10 allele on the metabolism of mexiletine by human liver microsomes.

Br J Clin Pharmacol. 2001 Jul;52(1):100-3. doi: 10.1046/j.0306-5251.2001.01411.x.

PubMed ID
11453897 [ View in PubMed
]
Abstract

AIMS: To study the influence of CYP2D6*10 on the formation of p-hydroxymexiletine (PHM) and hydroxymethylmexiletine (HMM) using microsomes from human liver of known genotypes. METHODS: Microsomes from human livers of genotype CYP2D6*1/*1 (n = 5), *1/*10 (n = 6) and *10/*10 (n = 6) were used in this study. The formation of PHM and HMM was determined by high-performance liquid chromatography. RESULTS: The formation rates of PHM and HMM were decreased by more than 50% and 85% in CYP2D6*1/*10 and *10/*10 microsomes, respectively, compared with *1/*1 microsomes. CONCLUSIONS: The metabolism of mexiletine to form PHM and HMM appears to be impaired to a significant extent in human liver microsomes from hetero- and homozygotes of CYP2D6*10.

DrugBank Data that Cites this Article

Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
MexiletineCytochrome P450 2D6ProteinHumans
Unknown
Substrate
Details