Abstract
Objective: The objective of this study was to determine CYP2D6 phenotype in a Javanese and Sundanese healthy subject in Indonesia.Methods: Ninety unrelated healthy Indonesian subjects from Java and Sunda were studied. Metoprolol was used as phenotyping substrate. A 100 mgoral tablet of metoprolol was administered to all the subjects. Urinary metoprolol and α-hydroxymetoprolol were determined to calculate metoprololmetabolic ratio (MR). Determination of metoprolol and α-hydroxymetoprolol was carried out by high performance liquid chromatography method.Results: Metoprolol MR varied widely (from 0.08 to 72.75). One subject (1.11%) in the study was classified as poor metabolizer (PM), one subject(1.11%) as ultrarapid metabolizer, and the remaining 88 subjects (97.78%) were classified as extensive metabolizers.Conclusion: The frequencies of PM for the CYP2D6 phenotype (1.11%) in the Javanese and Sundanese population are in concordance with mostresults of oxidation metabolizers in other Asian populations.
Highlights
CYP2D6, a minor form of CYP isoforms is only about 2% of the total CYP but has an important contribution in the metabolism of approximately 20– 25% of drugs used in the clinic, including β-blockers and antiarrhythmic agents
Phenotyping study of CYP2D6 enzyme activity can be measured in vivo after oral administration of a single dose of the drug which is a substrate of the enzyme
As shown in the histogram, the distribution of metabolic ratio (MR) showed the presence of three different phenotypes
Summary
CYP2D6, a minor form of CYP isoforms is only about 2% of the total CYP but has an important contribution in the metabolism of approximately 20– 25% of drugs used in the clinic, including β-blockers and antiarrhythmic agents. This enzyme activity catalyzes the Phase I reaction of drug metabolism which may determine the effects of the drug. CYP2D6 along with CYP2C9 and CYP2C19 has a high polymorphism approximately 40% of Phase I hepatic metabolism. The urinary metabolic ratio (MR) between the parent drug and its metabolites was determined as an indicator of polymorphism [1,2,3]
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