The effect of grapefruit juice on drug disposition.
The effect of grapefruit juice on drug disposition.
复制标题
柚子汁对药物处置的影响。
DOI：
10.1517/17425255.2011.553189
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发表时间：
2011-03
影响因子：
4.3
通讯作者：
Greenblatt DJ
中科院分区：
文献类型：
--
作者：
Hanley MJ;Cancalon P;Widmer WW;Greenblatt DJ
自1989年首次发现以来，葡萄柚汁-药物相互作用受到了科学，医学，监管和非专业团体的广泛关注。尽管关于葡萄柚汁对药物处置影响的知识不断扩展，但在临床环境中研究的药物列表仍然相对有限。本文综述了葡萄柚汁及其成分对细胞色素P450酶、有机阴离子转运多肽、P-糖蛋白、酯酶和磺基转移酶活性的体外影响。翻译适用性的体外研究结果的临床环境进行了讨论，为每个药物代谢酶和转运。还提供了可用葡萄柚汁-药物相互作用研究的血浆浓度-时间曲线下面积比。通过检索1989年至2010年的Pubmed电子数据库，确定了相关研究。葡萄柚汁可以提高一些口服药物的生物利用度，这些药物通过CYP 3A代谢，通常会经过大量的系统前提取。此外，葡萄柚汁可以减少一些药物的口服吸收，这些药物依赖于胃肠道中的有机阴离子转运多肽来吸收。在体外与葡萄柚汁相互作用的药物数量远远大于临床相关的葡萄柚汁-药物相互作用的数量。对于大多数患者来说，完全避免葡萄柚汁是没有必要的。
Since their initial discovery in 1989, grapefruit juice-drug interactions have received extensive interest from the scientific, medical, regulatory, and lay communities. Although knowledge regarding the effects of grapefruit juice on drug disposition continues to expand, the list of drugs studied in the clinical setting remains relatively limited. This article reviews the in vitro effects of grapefruit juice and its constituents on the activity of cytochrome P450 enzymes, organic anion-transporting polypeptides, 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 area under the plasma concentration-time curve ratios for available grapefruit juice-drug interaction studies are also provided. Relevant investigations were identified by searching the Pubmed electronic database from 1989 to 2010. Grapefruit juice increases the bioavailability of some orally-administered drugs that are metabolized by CYP3A and normally undergo extensive presystemic extraction. In addition, grapefruit juice can decrease the oral absorption of a few drugs that rely on organic anion-transporting polypeptides in the gastrointestinal tract for their uptake. The number of drugs shown to interact with grapefruit juice in vitro is far greater than the number of clinically relevant grapefruit juice-drug interactions. For the majority of patients, complete avoidance of grapefruit juice is unwarranted.
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影响因子：
6.7
作者：
Culm-Merdek, KE;von Moltke, LL;Greenblatt, DJ
通讯作者：
Greenblatt, DJ
影响因子：
3.7
作者：
Dahan, Arik;Amidon, Gordon L.
通讯作者：
Amidon, Gordon L.
影响因子：
6.7
作者：
Charbit, B;Becquemont, L;Funck-Brentano, C
通讯作者：
Funck-Brentano, C
影响因子：
2.9
作者：
Clifford, CP;Adams, DA;Davies, DS
通讯作者：
Davies, DS
影响因子：
6.7
作者：
Bailey, D. G.;Dresser, G. K.;Kim, R. B.
通讯作者：
Kim, R. B.