cardiovascularКардиоваскулярная терапия и профилактикаCardiovascular Therapy and Prevention1728-88002619-0125«SILICEA-POLIGRAF» LLC10.15829/1728-8800-2011-4-117-120cardiovascular-1907Research ArticleМНЕНИЕ ПО ПРОБЛЕМЕOPINION ON A PROBLEMСовременный взгляд на амлодипин и новые препараты S-амлодипинаModern views on amlodipine and new S-amlodipine medicationsЛеоноваМ. В.LeonovaM. V.

профессор кафедры клинической фармакологии

Москва

Moscow

anti23@mail.ruРоссийский государственный медицинский университетRussian State Medical University201120082011104117120Copyright © Леонова М.В., 20112011Леонова 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://cardiovascular.elpub.ru/jour/article/view/1907

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/сут., соответственно. По результатам фармакодинамического исследования средние значения систолического и диастолического артериального давления, частоты сердечных сокращений достоверно не различались при использовании 5 мг/сут. S-амлодипина и 10 мг/сут. 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.

The review presents the latest evidence on the calcium antagonist amlodipine, summarizing its mechanisms of action, its pleiotropic, endothelial function-related effects, and its anti-atherogenic activity. Amlodipine suppresses the proliferation of vascular smooth myocytes and extracellular matrix and improves endothelial vasodilatation, despite the absence of L-type calcium channels in these cells. This mechanism is related to an increase in endothelial nitric oxide (NO) release. The results of experimental studies on the role of S and R amlodipine isomers in its hemodynamic and pleiotropic activity are presented. While S-amlodipine is a pharmacologically active blocker of L-type calcium channels, R-amlodipine increases endothelial NO release. New medications have been developed, based on S-amlodipine. It has been shown that S-amlodipine 5 mg/d is bioequivalent to amlodipine 10 mg/d. The pharmacodynamics analysis demonstrated that S-amlodipine 5 mg/d and amlodipine 10 mg/d did not differ significantly in terms of mean levels of systolic and diastolic blood pressure, or mean heart rate. S-amlodipine was better tolerated and characterised by a lower incidence of peripheral edema than amlodipine. However, the effects of S-amlodipine on hard end-points should be investigated in the long-term prospective studies.

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