rpcardioRational Pharmacotherapy in CardiologyРациональная Фармакотерапия в Кардиологии1819-64462225-3653«SILICEA-POLIGRAF» LLC10.20996/1819-6446-2011-7-2-227-230rpcardio-754Research ArticleCURRENT QUESTIONS OF CLINICAL PHARMACOLOGYАКТУАЛЬНЫЕ ВОПРОСЫ КЛИНИЧЕСКОЙ ФАРМАКОЛОГИИCONTEMPORARY SIGHT AT AMLODIPINE AND NEW DRUGS OF S-AMLODIPINEСОВРЕМЕННЫЙ ВЗГЛЯД НА АМЛОДИПИН И НОВЫЕ ПРЕПАРАТЫ S-АМЛОДИПИНАЛеоноваМ. В.LeonovaM. V.

д.м.н., профессор кафедры клинической фармакологии

anti23@mail.ruРоссийский государственный медицинский университетРоссияRussian State Medical UniversityRussian Federation20111401201672227230Copyright © Leonova M.V., 20162016Леонова М.В.Leonova M.V.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://www.rpcardio.online/jour/article/view/754

Contemporary scientific data about mode of action of calcium channel blocker — amlodipine, its pleiotropic effect (influence on endothelial function and antiatherogenic action) is presented. Amlodipine reduces proliferation of vascular smooth muscle cells and extracellular matrix, improves the vasodilating function of endothelial cells although they have no L-type calcium channels. It puts into action through stimulation of nitric oxide (NO) secretion in endothelium. Results of experimental studies on the role of S- and R-isomers of amlodipine in hemodynamic and pleiotropic effects are presented. S-isomer is pharmacologically active blocker of L-type calcium channel while the R-isomer is responsible for NO release. Drugs based on S-amlodipine have been developed. Bioequivalence of the S-amlodipine and amlodipine in doses of 5 and 10 mg, respectively , is shown. Mean values of systolic and diastolic blood pressure, heart rate were not different significantly according to pharmacodynamic studies of S-amlodipine 5 mg and amlodipine 10 mg. S-amlodipine demonstrated better tolerability and lower incidence of ankle edema than amlodipine. Further long-term studies on S-amlodipine effect on hard endpoints are needed.

Представлены современные научные данные о механизме действия антагониста кальция амлодипина, его плейотропном эффекте (влияние на функцию эндотелия) и антиатерогенном действии. Амлодипин уменьшает пролиферацию гладкомышечных клеток сосудов и внеклеточного матрикса, а также улучшает вазодилатирующую функцию эндотелия, несмотря на отсутствие в них кальциевых каналов L-типа. Это происходит через стимуляцию секреции оксида азота (NO) в эндотелии. Приведены результаты экспериментальных исследований о роли S- и R-изомеров амлодипина в гемодинамическом и плейотропном эффектах. S-изомер является фармакологически активным блокатором кальциевых каналов L-типа, R-изомер отвечает за высвобождение NO. Разработаны препараты на основе S-амлодипина. Показана биоэквивалентность S-амлодипина и амлодипина в дозах 5 и 10 мг , соответственно. По результатам фармакодинамического исследования средние значения систолического и диастолического артериального давления, частоты сердечных сокращений достоверно не различались при использовании 5 мг S-амлодипина и 10 мг амлодипина. S-амлодипин показал лучшую переносимость и меньшую частоту развития отеков голеней. Вместе с тем, необходимы дальнейшие долгосрочные исследования по изучению влияния S-амлодипина на твердые конечные точки.

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