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Study of effects of prolonged administration of emtricitabine on expression of ABC efflux transporters in maternal and fetal organs
Havlová, Ivana ; Červený, Lukáš (advisor) ; Hofman, Jakub (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Ivana Havlová Supervisor: PharmDr. Lukáš Červený, Ph.D. Title of diploma thesis: Study of effects of prolonged administration of emtricitabine on expression of ABC efflux transporters in maternal and fetal organs The aim of this thesis was to evaluate the effect of chronic administration of antiretroviral substance emtricitabine (FTC) on expression of drug efflux ABC-binding cassette (ABC) transporters in the placenta, maternal and fetal organs (brain, liver, kidney, small intestine) of pregnant rats. We focused on two most important representatives of drug efflux ABC transporters, P-glycoprotein (MDR1) and Breast Cancer Resistance Protein (BCRP). Knowledge of FTC effects on gene expression of these transporters is crucial especially when using FTC in combination therapy, known as Highly Active Antiretroviral Therapy (HAART). Changes in MDR1/BCRP expression may lead to significantly altered pharmacokinetics of concomitantly administered drugs. First, bioavailability was analyzed. AUC of FTC (3,5 mg/kg) following i.m. administration was comparable to that one after i.v. administration allowing us to use i.m. application as a route of FTC administration to rats. Subsequently,...
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