EFFECT OF A COMBINED ORAL CONTRACEPTIVE ON THE ACTIVITY AND EXPRESSION OF P-GLYCOPROTEIN

DOI: https://doi.org/None
Issue: 
4
Year: 
2015

E.N. Yakusheva, MD; A.A. Kotlyarova; A.V. Shchulkin, PhD; I.Yu. Vinogradov, PhD; N.M. Popova, PhD Acad. I.P. Pavlov Ryazan State Medical University; 9, Vysokovoltnaya St., Ryazan

The effect of a combined oral contraceptive containing ethinylestradiol and gestodene on the functional activity of the efflux poly-specific transporter protein P-glycoprotein and its expression in the liver and small intestine was investigated in Chinchilla rabbits. The activity of the transporter protein was assessed from the pharmacokinetics of its marker substrate fexofenadine after its single intragastric administration. The expression of P-glycoprotein was determined immunohistochemically and estimated semiquantitatively. Radioimmunoassay was used to measure the serum levels of estradiol, progesterone, and testosterone in the rabbits. The 21-day administration of the agent was found to inhibit P-glycoprotein functional activity at the whole-organism level. Correlations were found between the activity of P-glycoprotein, its expression in hepatocytes, and the serum level of estradiol after administration of the agent.

Keywords: 
P-glycoprotein
ABCB1 protein
functional activity
expression
lindinet
ethinylestradiol
gestodene
fexofenadine

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