The effect of grapefruit juice on drug disposition

被引:146
作者
Hanley, Michael J. [1 ]
Cancalon, Paul [2 ]
Widmer, Wilbur W. [3 ]
Greenblatt, David J. [1 ]
机构
[1] Tufts Univ, Sch Med, Program Pharmacol & Expt Therapeut, Boston, MA 02111 USA
[2] Florida Dept Citrus, Lakeland, FL 33802 USA
[3] USDA, Winter Haven, FL 33881 USA
基金
美国国家卫生研究院;
关键词
SEVILLE ORANGE JUICE; SULFOTRANSFERASE ISOFORMS SULT1A1; INCREASES PLASMA-CONCENTRATIONS; PROTEASE INHIBITOR SAQUINAVIR; INTESTINAL CYP3A4 INHIBITION; RENAL-TRANSPLANT RECIPIENTS; CYTOCHROME-P450 3A ACTIVITY; P-GLYCOPROTEIN; FELODIPINE INTERACTION; HEALTHY-VOLUNTEERS;
D O I
10.1517/17425255.2011.553189
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Areas covered: This article reviews the in vitro effects of GFJ and its constituents on the activity of CYP enzymes, organic anion-transporting polypeptides (OATPs), P-glycoprotein, esterases and sulfotransferases. The translational applicability of the in vitro findings to the clinical setting is discussed for each drug metabolizing enzyme and transporter. Reported AUC ratios for available GFJ--drug interaction studies are also provided. Relevant investigations were identified by searching the PubMed electronic database from 1989 to 2010. Expert opinion: GFJ increases the bioavailability of some orally administered drugs that are metabolized by CYP3A and normally undergo extensive presystemic extraction. In addition, GFJ can decrease the oral absorption of a few drugs that rely on OATPs in the gastrointestinal tract for their uptake. The number of drugs shown to interact with GFJ in vitro is far greater than the number of clinically relevant GFJ--drug interactions. For the majority of patients, complete avoidance of GFJ is unwarranted.
引用
收藏
页码:267 / 286
页数:20
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