The MDR1 (ABCB1) Gene Polymorphism and its Clinical Implications

被引:0
作者
Ichiro Ieiri
Hiroshi Takane
Kenji Otsubo
机构
[1] Tottori University,Department of Hospital Pharmacy, Faculty of Medicine
来源
Clinical Pharmacokinetics | 2004年 / 43卷
关键词
Digoxin; Acute Myeloid Leukaemia; Grapefruit Juice; Fexofenadine; MDR1 Gene;
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学科分类号
摘要
There has been an increasing appreciation of the role of drug transporters in the pharmacokinetic and pharmacodynamic profiles of certain drugs. Among various drug transporters, P-glycoprotein, the MDR1 gene product, is one of the best studied and characterised. P-glycoprotein is expressed in normal human tissues such as liver, kidney, intestine and the endothelial cells of the blood-brain barrier. Apical (or luminal) expression of P-glycoprotein in these tissues results in reduced drug absorption from the gastrointestinal tract, enhanced drug elimination into bile and urine, and impeded entry of certain drugs into the central nervous system. The clinical relevance of P-glycoprotein depends on the localisation in human tissues (i.e. vectorial or directional movement), the therapeutic index of the substrate drug and the inherent inter- and intra-individual variability.
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页码:553 / 576
页数:23
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