The influence of P-glycoprotein on the transport of anticonvulsants in the brain
Abstract
Pharmacoresistance to antiepileptic drugs (AEDs) is one of the major problems in the treatment of epilepsy. According to one of the current hypotheses, this pharmacoresistance may be associated with the reverse transport of AEDs by drug efflux transporters such as P-glycoprotein (Pgp) through the blood-brain barrier. However, so far there is no unequivocal opinion regarding the involvement of P-gp in the resistance to carbamazepine, one of the most important AEDs. The objective of the present study was to investigate the influence of verapamil, which is known to be P-gp inhibitor, on the anticonvulsive effect of carbamazepine in rat epilepsy induced by isoniazid. A significant enhancement of the anticonvulsive effect of carbamazepine in the presence of verapamil (30% decrease of the effective dose - from 30 mg/kg to 20 mg/kg) suggests that P-glycoprotein may considerably limit the transport of carbamazepine to the brain.
About the Authors
A. M. Zybina
Московский государственный университет имени М.В. Ломоносова, Москва
Russian Federation
Russian Federation
K. N. Kulichenkova
Московский государственный университет имени М.В. Ломоносова, Москва
Russian Federation
Russian Federation
V. Yu. Balaban`yan
ООО «Технология лекарств», г. Химки Московской обл
Russian Federation
Russian Federation
S. E. Gel`perina
ООО «Технология лекарств», г. Химки Московской обл
Russian Federation
Russian Federation
K. R. Abbasova
Московский государственный университет имени М.В. Ломоносова, Москва
Russian Federation
Russian Federation
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Review
For citations:
Zybina A.M., Kulichenkova K.N., Balaban`yan V.Yu., Gel`perina S.E., Abbasova K.R. The influence of P-glycoprotein on the transport of anticonvulsants in the brain. Journal Biomed. 2016;(4):77-85. (In Russ.)
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