The Effect of Apple Juice and OATP2B1 Polymorphism on the Pharmacokinetics and Tolerability of Atenolol in Healthy Volunteers

apple juice;atenolol;pharmacokinetics;SLCO2B1;615

의과대학 협동과정임상약리학전공 ;

University:서울대학교 대학원

关键词: apple juice;    atenolol;    pharmacokinetics;    SLCO2B1;    615;   

Others  :  http://s-space.snu.ac.kr/bitstream/10371/132319/1/000000002896.pdf

美国|英语

来源: Seoul National University Open Repository

【 摘 要 】

Introduction: Fruit juice reduces the plasma concentrations of several beta-blockers likely by inhibiting their OATP2B1-mediated intestinal absorption. The aim of this study was to investigate the effects of apple juice on the pharmacokinetics of atenolol. Twelve healthy Korean volunteers were enrolled in this study based on the genotype of SLCO2B1 c.1457C> T (*1/*1 (n=6) and *3/*3 (n=6)). Methods: In a three-phase, one-sequence cross-over study, the pharmacokinetics (PK) of atenolol was evaluated after administration of 50 mg of atenolol. Each subject received atenolol with 300 mL of water, 1,200 mL and 600 mL of apple juice. Apple juice markedly reduced the systemic exposure of atenolol. Results: The geometric mean ratios (95% confidence intervals) of apple juice to water phase for AUClast were 0.18 (0.13-0.25, 1,200 mL) and 0.42 (0.30-0.59, 600 mL). In this study, the PK parameters of atenolol responded in a dose-dependent manner to apple juice. Conclusions: Apple juice markedly reduced systemic exposure of atenolol. The genetic variation of SLCO2B1 c.1457C>T had a minimal effect on the pharmacokinetics and tolerability of atenolol when the drug was administered with water or apple juice.