Abstract
WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT •Atenolol is an antihypertensive drug, of which negligible amounts are metabolized. •Fruit juices may decrease the oral absorption of drugs by inhibiting intestinal drug transporters, as demonstrated in vitro and in vivo. WHAT THIS STUDY ADDS •The pharmacokinetic characteristics of atenolol were determined according to the SLCO2B1 genotype after apple juice administration in healthy Korean volunteers. •Apple juice ingestion markedly reduced the systemic exposure to atenolol, but genetic variations in SLCO2B1 were unlikely to contribute substantial variability to the pharmacokinetics of atenolol. AIM 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 50mg atenolol. Subjects received atenolol with either 300ml water, 1200ml apple juice or 600ml 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, 1200ml) and 0.42 (0.30, 0.59, 600ml) for the AUC(0,tlast). 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.
| Original language | English |
|---|---|
| Pages (from-to) | 172-179 |
| Number of pages | 8 |
| Journal | British Journal of Clinical Pharmacology |
| Volume | 75 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - Jan 2013 |
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All Science Journal Classification (ASJC) codes
- Pharmacology (medical)
- Pharmacology
Cite this
Apple juice greatly reduces systemic exposure to atenolol. / 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.
In: British Journal of Clinical Pharmacology, Vol. 75, No. 1, 01.2013, p. 172-179.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Apple juice greatly reduces systemic exposure to atenolol
AU - Jeon, Hyewon
AU - Jang, In Jin
AU - Lee, Seunghwan
AU - Ohashi, Kyoichi
AU - Kotegawa, Tsutomu
AU - Ieiri, Ichiro
AU - Cho, Joo Youn
AU - Yoon, Seo Hyun
AU - Shin, Sang Goo
AU - Yu, Kyung Sang
AU - Lim, Kyoung Soo
PY - 2013/1
Y1 - 2013/1
N2 - WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT •Atenolol is an antihypertensive drug, of which negligible amounts are metabolized. •Fruit juices may decrease the oral absorption of drugs by inhibiting intestinal drug transporters, as demonstrated in vitro and in vivo. WHAT THIS STUDY ADDS •The pharmacokinetic characteristics of atenolol were determined according to the SLCO2B1 genotype after apple juice administration in healthy Korean volunteers. •Apple juice ingestion markedly reduced the systemic exposure to atenolol, but genetic variations in SLCO2B1 were unlikely to contribute substantial variability to the pharmacokinetics of atenolol. AIM 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 50mg atenolol. Subjects received atenolol with either 300ml water, 1200ml apple juice or 600ml 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, 1200ml) and 0.42 (0.30, 0.59, 600ml) for the AUC(0,tlast). 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.
AB - WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT •Atenolol is an antihypertensive drug, of which negligible amounts are metabolized. •Fruit juices may decrease the oral absorption of drugs by inhibiting intestinal drug transporters, as demonstrated in vitro and in vivo. WHAT THIS STUDY ADDS •The pharmacokinetic characteristics of atenolol were determined according to the SLCO2B1 genotype after apple juice administration in healthy Korean volunteers. •Apple juice ingestion markedly reduced the systemic exposure to atenolol, but genetic variations in SLCO2B1 were unlikely to contribute substantial variability to the pharmacokinetics of atenolol. AIM 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 50mg atenolol. Subjects received atenolol with either 300ml water, 1200ml apple juice or 600ml 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, 1200ml) and 0.42 (0.30, 0.59, 600ml) for the AUC(0,tlast). 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.
UR - http://www.scopus.com/inward/record.url?scp=84871124271&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84871124271&partnerID=8YFLogxK
U2 - 10.1111/j.1365-2125.2012.04324.x
DO - 10.1111/j.1365-2125.2012.04324.x
M3 - Article
C2 - 22574741
AN - SCOPUS:84871124271
VL - 75
SP - 172
EP - 179
JO - British Journal of Clinical Pharmacology
JF - British Journal of Clinical Pharmacology
SN - 0306-5251
IS - 1
ER -