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Effect of CYP3A53 genotype on the pharmacokinetics and pharmacodynamics of amlodipine in healthy Korean subjects by KIM, K; PARK, P; LEE, O; CHOI, S; MIN, B; SHIN, K; CHUN, B; SHIN, J; PARK, J is a Medicine article available to read on EtoBox.

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## Background and objective: 1,4-dihydropyridine calcium channel blockers, including amlodipine, are mainly metabolized by cytochrome p450 (cyp) 3a. we investigated the effect of cyp3a5\*3 genotype on the pharmacokinetics and pharmacodynamics of amlodipine in healthy korean male subjects. ## Methods: Forty healthy male participants were enrolled and genotyped for the cyp3a5\*3 gene. each subject ingested a 5-mg dose of amlodipine, and plasma amlodipine concentrations were measured for 144 hours after dosing. blood pressure and pulse rate were also measured for pharmacodynamic analysis. ## Results: Among the 40 volunteers, 24 were cyp3a5\*3/\*3 carriers and 16 were cyp3a5\*1 carriers (cyp3a5\*1/\*1 in 2 and cyp3a5\*1/\*3 in 14). the difference in the oral clearance of amlodipine approached statistical significance between the 2 major genotype groups, with cyp3a5\*1 carriers (27.0 +/- 8.2 l/h) showing 20% lower clearance than cyp3a5\*3/\*3 carriers (32.4 +/- 10.2 l/h) (p = .063). however, the mean area under the plasma concentration-time curve of amlodipine was 200.9 +/- 61.9 ng . h/ml for cyp3a5\*1 carriers and 167.6 +/- 45.0 ng . h/ml for cyp3a5\*3/\*3 carriers (p = .029). moreover

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Author

KIM, K; PARK, P; LEE, O; CHOI, S; MIN, B; SHIN, K; CHUN, B; SHIN, J; PARK, J

Publisher

Nature Publishing Group; Wiley (Blackwell Publishing); Wiley-Blackwell; Wiley; Springer Science and Business Media LLC; Research Square (ISSN 0009-9236)

Published

2006

Language

EN

Field

Medicine (Health Sciences)