Apple juice greatly reduces systemic exposure to atenolol. (14th December 2012)

• Record Type: Journal Article
• Authors: Jeon, Hyewon; Jang, In‐Jin; Lee, SeungHwan; Ohashi, Kyoichi; Kotegawa, Tsutomu; Ieiri, Ichiro; Cho, Joo‐Youn; Yoon, Seo Hyun; Shin, Sang‐Goo; Yu, Kyung‐Sang; Lim, Kyoung Soo
• Is Part Of: British journal of clinical pharmacology. Volume 75:Number 1(2013:Jan.)
• Page Start: 172
• Page End: 179
• Publication Date: 2012-12-14
• Subjects: Pharmacology -- Periodicals; Drugs -- Periodicals; 615.1
• DOI: 10.1111/j.1365-2125.2012.04324.x
• Languages: English
• ISSNs: 0306-5251

Abstract

<abstract abstract-type="main" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <p> <bold>WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT</bold> </p> <p> Atenolol is an antihypertensive drug, of which negligible amounts are metabolized.</p> <p> Fruit juices may decrease the oral absorption of drugs by inhibiting intestinal drug transporters, as demonstrated <italic>in vitro</italic> and <italic>in vivo</italic>.</p> <p> <bold>WHAT THIS STUDY ADDS</bold> </p> <p> The pharmacokinetic characteristics of atenolol were determined according to the <italic>SLCO2B1</italic> genotype after apple juice administration in healthy Korean volunteers.</p> <p> Apple juice ingestion markedly reduced the systemic exposure to atenolol, but genetic variations in <italic>SLCO2B1</italic> were unlikely to contribute substantial variability to the pharmacokinetics of atenolol.</p> <p> <bold>AIM</bold> Fruit juice reduces the plasma concentrations of several β‐adrenoceptor blockers, likely by inhibiting OATP2B1‐mediated intestinal absorption. The aim of this study was to investigate the effects of apple juice on the pharmacokinetics of atenolol.</p> <p> <bold>METHODS</bold> Twelve healthy Korean volunteers with genotypes of <italic>SLCO2B1</italic> c.1457C> T (*<italic>1/</italic>*<italic>1</italic> (<italic>n</italic>= 6) and *<italic>3/</italic>*<italic>3</italic> (<italic>n</italic>= 6)) were enrolled in this study. In a three‐phase, one‐sequence crossover study, the pharmacokinetics (PK) of atenolol was evaluated after administration of 50 mg atenolol. Subjects received atenolol with either 300 ml water, 1200 ml apple juice or 600 ml apple juice.</p> <p> <bold>RESULTS</bold> Apple juice markedly reduced the systemic exposure to atenolol. The geometric mean ratios (95% confidence intervals) of apple juice : water were 0.18 (0.13, 0.25, 1200 ml) and 0.42 (0.30, 0.59, 600 ml) for the AUC(0, <italic>t</italic><sub>last</sub>). In this study, the PK parameters of atenolol responded in a dose‐dependent manner to apple juice.</p> <p> <bold>CONCLUSIONS</bold> Apple juice markedly reduced systemic exposure to atenolol. The genetic variation of <italic>SLCO2B1</italic> c.1457C>T had a minimal effect on the pharmacokinetics of atenolol when the drug was administered with water or apple juice.</p> </abstract>