title: Apple juice greatly reduces systemic exposure to atenolol.
abstract: OBJECTIVE
  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.
  
  
  METHODS
  Twelve healthy Korean volunteers with genotypes of SLCO2B1 c.1457C> T (*1/*1 (n = 6) and *3/*3 (n = 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.
  
  
  RESULTS
  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,t(last)). In this study, the PK parameters of atenolol responded in a dose-dependent manner to apple juice.
  
  
  CONCLUSIONS
  Apple juice markedly reduced systemic exposure to atenolol. The genetic variation of SLCO2B1 c.1457C>T had a minimal effect on the pharmacokinetics of atenolol when the drug was administered with water or apple juice.
authors.affiliation: Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul, Korea.
authors.forename: Hyewon
authors.initials: H
authors.lastname: Jeon
authors.forename: In-Jin
authors.initials: IJ
authors.lastname: Jang
authors.forename: SeungHwan
authors.initials: S
authors.lastname: Lee
authors.forename: Kyoichi
authors.initials: K
authors.lastname: Ohashi
authors.forename: Tsutomu
authors.initials: T
authors.lastname: Kotegawa
authors.forename: Ichiro
authors.initials: I
authors.lastname: Ieiri
authors.forename: Joo-Youn
authors.initials: JY
authors.lastname: Cho
authors.forename: Seo Hyun
authors.initials: SH
authors.lastname: Yoon
authors.forename: Sang-Goo
authors.initials: SG
authors.lastname: Shin
authors.forename: Kyung-Sang
authors.initials: KS
authors.lastname: Yu
authors.forename: Kyoung Soo
authors.initials: KS
authors.lastname: Lim
mesh_terms: D000319:Adrenergic beta-Antagonists / Q000493:pharmacokinetics*; D000328:Adult; D001262:Atenolol / Q000493:pharmacokinetics*; D001628:Beverages; D018592:Cross-Over Studies; D018565:Food-Drug Interactions; D005838:Genotype; D006801:Humans; D008297:Male; D027845:Malus; D008875:Middle Aged; D027361:Organic Anion Transporters / Q000235:genetics; D020641:Polymorphism, Single Nucleotide
chemical_list: D000319:Adrenergic beta-Antagonists; D027361:Organic Anion Transporters; C450859:SLCO2B1 protein, human; D001262:Atenolol