ISSN: 1305-3876
Dil: Türkçe
Hakkında: Özel sayılar şeklinde yayınlanır.
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The Role Of P-glycoprotein In Pharmacokinetics And Toxicokinetic
Dr. Y. Cem KAPLAN,a Dr. Ayşe GELALa
aFarmakoloji AD, Dokuz Eylül Üniversitesi Tıp Fakültesi, İZMİR
P-glycoprotein (P-gp) is an ATP driven transmembrane protein which functions as the transporter of various drugs. Beside its expression and role in multidrug resistance in tumor cells, it is also expressed in normal tissues like liver, kidney, small intestine, colon, brain, heart, peripheric nerves, placenta, adrenal glands and in tissue barriers like blood-brain barrier and blood-testis barrier. Due to the presence of P-gp in the tissues like small intestine, central nervous system, liver and kidney, it can play a critical role in pharmacokinetics and toxicokinetics of its substrates some of which are among the most frequently used drugs in daily clinical practice like antineoplastic agents, HIV protease inhibitors, immunsuppressants, cardiovascular drugs, antimicrobial agents etc. Daily food constituents and the xenobitics which we are enviromentally exposed to, may be the substrates, activators or inhibitors of P-gp, as well. Therefore, it is possible that P-gp activity may be affected by these compounds causing changes in pharmacokinetic and toxicokinetics of the substrate drug which may result in serious clinical outcomes like a decrease in the therapeutic effect or an increase in the toxicity of the medication. Without any doubt, further studies exploring the structure and the activity of P-gp will teach us more about drug pharmacokinetics and toxicokinetics. These studies will also make it possible to overcome the multidrug resistance which is one of the major problems in cancer therapy, and can be of great help to us in developing new therapeutic strategies to increase the therapeutic effects of drugs by inhibiting P-gp.Keywords: P-glycoprotein, MDR1, ABCB1, drug interactionTurkiye Klinikleri J Surg Med Sci 2006, 2(46):33-38
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