scbmtБИОМЕДИЦИНАJournal Biomed2074-59822713-0428Scientific center of biomedical technologies of Federal Medical and Biological Agencyscbmt-53Research ArticleМЕТОДЫ БИОМЕДИЦИНСКИХ ИССЛЕДОВАНИЙMETHODS OF BIOMEDICAL RESEARCHESВлияние Р-гликопротеина на транспорт противосудорожных средств в головной мозгThe influence of P-glycoprotein on the transport of anticonvulsants in the brainЗыбинаА. М.ZybinaA. M.noemail@neicon.ruКуличенковаК. Н.KulichenkovaK. N.noemail@neicon.ruБалабаньянВ. Ю.Balaban`yanV. Yu.bal.pharm@mail.ruГельперинаС. Э.Gel`perinaS. E.ООО «Технология лекарств». г.Химки Московской облАббасоваК. Р.AbbasovaK. R.noemail@neicon.ruМосковский государственный университет имени М.В. Ломоносова, МоскваRussian FederationООО «Технология лекарств», г. Химки Московской облRussian Federation201625022019047785Copyright © Зыбина А.М., Куличенкова К.Н., Балабаньян В.Ю., Гельперина С.Э., Аббасова К.Р., 20192019Зыбина А.М., Куличенкова К.Н., Балабаньян В.Ю., Гельперина С.Э., Аббасова К.Р.Zybina A.M., Kulichenkova K.N., Balaban`yan V.Y., Gel`perina S.E., Abbasova K.R.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://journal.scbmt.ru/jour/article/view/53

Резистентность к антиэпилептическим препаратам (АЭП) является серьезной клинической проблемой. Среди факторов, обуславливающих устойчивость к АЭП, определенную роль играет гиперэкспрессия P-гликопротеина (P-gp) - одного из основных транспортеров, ограничивающих поступление ксенобиотиков в мозг. В настоящее время нет единого мнения о взаимодействии карбамазепина (КБЗ) с P-gp. Целью настоящего исследования явилось изучение влияния верапамила - ингибитора P-gp на противосудорожный эффект КБЗ на модели эпилепсии у крыс, вызванной изониазидом. Показано, что применение верапамила позволяет значительно усилить противосудорожное действие КБЗ и обеспечивает снижение его эффективной дозы не менее, чем на 30% (с 30 мг/кг до 20 мг/кг). Полученные данные свидетельствуют о том, что P-gp существенно ограничивает поступление КБЗ в мозг.

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.

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The authors declare that there are no conflicts of interest present.