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Prediction of in vivo drug metabolism in the human liver from in vitro metabolism data.
Scaling of in vivo metabolic clearance from in vitro data obtained using human liver microsomes or hepatocytes is described in this review, based on the large number of literature data, and it appears to be possible to predict in vivo drug metabolic clearanceFrom in vitro metabolic data. Expand
Genetic polymorphism of UDP-glucuronosyltransferase 2B7 (UGT2B7) at amino acid 268: ethnic diversity of alleles and potential clinical significance.
Although the UGT2B7 polymorphism characterized here is probably not associated with altered enzyme activity, the results highlight the need to consider ethnic variability in assessing the consequences of UGT polymorphisms. Expand
Frequencies of the defective CYP2C19 alleles responsible for the mephenytoin poor metabolizer phenotype in various Oriental, Caucasian, Saudi Arabian and American black populations.
This study examined whether the genotype predicted the phenotype in Japanese, Filipino and Saudi Arabian populations, and compared the frequencies of the defective CYP2C19 alleles in these populations with those found in European-Americans, Chinese-Taiwanese, and African-Americans from North Carolina. Expand
Influence of CYP2C19 pharmacogenetic polymorphism on proton pump inhibitor-based therapies.
For the better PPI-based treatment, doses and dosing schemes of PPIs should be optimized based on CYP2C19 genotype status, which influences the cure rates for the gastro-esophageal reflux disease and H. pylori infection by P PI-based therapies. Expand
Nomenclature for human CYP2D6 alleles.
It is proposed that alleles be designated by CYP2D6 followed by an asterisk and a combination of roman letters and arabic numerals distinct for each allele with the number specifying the key mutation and, where appropriate, a letter specifying additional mutations. Expand
Oxidative metabolism of omeprazole in human liver microsomes: cosegregation with S-mephenytoin 4'-hydroxylation.
It is suggested that S-mephenytoin 4'-hydroxylase is an enzyme primarily responsible for the 5-Hydroxylation of OPz and further metabolism of OPZ-SFN, but not for the sulfoxidation ofOPZ in human liver microsomes. Expand
Pharmacokinetics of haloperidol: an update.
In vivo pharmacogenetic studies have indicated that the metabolism and disposition of haloperidol may be regulated by genetically determined polymorphic CYP2D6 activity, however, these findings appear to contradict those from studies in vitro with human liver microsomes and from studies of drug interactions in vivo. Expand
Effects of CYP2C19 genotypic differences in the metabolism of omeprazole and rabeprazole on intragastric pH
Omeprazole is mainly metabolized in the liver by CYP2C19, a genetically determined enzyme, whereas rabeprazole is mainly reduced non‐enzymatically and partially metabolized by CYP2C19. TheExpand
Metoprolol and mephenytoin oxidation polymorphisms in Far Eastern Oriental subjects: Japanese versus mainland Chinese
The findings indicate that the two Far Eastern Oriental subject groups have a lower frequency of PM phenotype of debrisoquin/sparteine‐type oxidation and a greater incidence ofPM phenotype of mephenytoin oxidation compared with the respective frequencies reported from white subjects. Expand
Human buprenorphine N-dealkylation is catalyzed by cytochrome P450 3A4.
The demonstration of BN N-dealkylation by recombinant CYP3A4 and the agreement in the affinities (apparent KM values) of human liver microsomes and recombinant cytochrome P450 enzyme(s) provide the most supportive evidence for BNN-dealksylation being catalyzed by CYP 3A4. Expand