Северная звезда ЗАО, Российская Федерация, Эссенциальная гипертензия легкой и умеренной степени тяжести
Фармакологические свойства
Лерканидипин является рацемической смесью право- (R) и левовращающих (S) стереоизомеров, производное 1,4-дигидропиридина, способен избирательно блокировать ток ионов кальция внутрь клеток сосудистой стенки, сердечные клетки и клетки гладкой мускулатуры.
Механизм гипотензивного действия обусловлен прямым релаксирующим действием на гладкомышечные клетки сосудов.
Обладает пролонгированным антигипертензивным действием.
Благодаря высокой селективности к гладкомышечным клеткам сосудов отрицательное инотропное действие отсутствует.
Лерканидипин является метаболически нейтральным препаратом и не оказывает существенного воздействия на содержание липопротеинов и аполипопротеинов в сыворотке крови, а также не изменяет липидный профиль у пациентов с артериальной гипертензией.
Терапевтический эффект достигается через 5-7 ч после приема внутрь и сохраняется в течение суток (24 ч).
Показания к применению
артериальная гипертензия 1-2 степени.
Противопоказания
повышенная чувствительность к лерканидипину, другим производным дигидропиридинового ряда или любому компоненту препарата;
нелеченная сердечная недостаточность;
нестабильная стенокардия;
обструкция выносящего тракта левого желудочка;
период в течение 1 месяца после перенесенного инфаркта миокарда;
тяжелая печеночная недостаточность;
тяжелая почечная недостаточность (КК менее 30 мл/мин);
беременность;
период грудного вскармливания;
применение у женщин детородного возраста, не пользующихся надежной контрацепцией;
возраст до 18 лет (эффективность и безопасность не установлены);
одновременное применение с субстратами изофермента CYP3A4 (терфенадин, астемизол, антиаритмические препараты III класса, например, амиодарон, хинидин);
одновременное применение с индукторами изофермента CYP3A4, например, противосудорожными средствами (фенитоин, карбамазепин) и рифампицином;
одновременное применение с бета-адреноблокаторами, дигоксином.
Применение при беременности и в период грудного вскармливания
Беременность
В исследованиях на животных лерканидипин не оказывал тератогенного действия, однако тератогенные эффекты отмечались при применении других производных дигидропиридина. Поэтому применение препарата Лерканидипин-СЗ при беременности и у женщин детородного возраста, не пользующихся надежной контрацепцией, противопоказано.
Период грудного вскармливания
Вследствие высокой липофильности лерканидипина можно предполагать его проникновение в грудное молоко, поэтому применение препарата Лерканидипин-СЗ в период грудного вскармливания противопоказано.
Способ применения и дозы
Внутрь.
Препарат Лерканидипин-СЗ назначают по 10 мг 1 раз/сут утром, не менее чем за 15 минут до еды, не разжевывая, запивая достаточным количеством воды.
Доза может быть увеличена до 20 мг (в случае, если при приеме 10 мг не достигается ожидаемый эффект). Терапевтическая доза подбирается постепенно, увеличение дозы до 20 мг осуществляется через 2 недели после начала приема препарата.
Маловероятно, что эффективность препарата будет возрастать с увеличением дозы более 20 мг/сут, в то же время повышается риск возникновения побочных эффектов.
У пациентов пожилого возраста коррекция дозы не требуется, однако при приеме препарата необходим постоянный контроль состояния пациентов.
Применение у пациентов с нарушениями функции почек или печени
При почечной или печеночной недостаточности легкой или средней тяжести, как правило, коррекции дозы не требуется, начальная доза - 10 мг, увеличение дозы до 20 мг/сут следует проводить с осторожностью. В случае, если антигипертензивный эффект будет слишком сильно выражен, следует снизить дозу.
Побочное действие
Нежелательные реакции, распределенных по системам органов и частоте возникновения (классификация ВОЗ): часто (от более 1/100 до менее 1/10), нечасто (от более 1/1000 до менее 1/100), редко (от более 1/10000 до менее 1/1000), очень редко (менее 1/10000), включая отдельные сообщения.
Со стороны нервной системы: нечасто - головная боль, головокружение; редко - сонливость.
Со стороны сердечно-сосудистой системы: нечасто - ощущение сердцебиения, тахикардия, "приливы" крови к коже лица; редко - стенокардия; очень редко - обморок, выраженное снижение АД, боль в груди, инфаркт миокарда, у пациентов со стенокардией возможно увеличение частоты, продолжительности и тяжести приступов.
Со стороны пищеварительной системы: редко - тошнота, рвота, диарея, боли в животе, диспепсия; очень редко - повышение активности печеночных ферментов (обратимое).
Со стороны кожи и подкожных тканей: редко - кожная сыпь.
Со стороны костно-мышечной системы и соединительной ткани: редко - миалгия.
Со стороны почек и мочевыводящих путей: редко - поллакиурия (увеличение частоты мочеиспускания).
Общие реакции: нечасто - периферические отеки; редко - астения, повышенная утомляемость; очень редко - гиперплазия десен.
Со стороны иммунной системы: очень редко - реакции повышенной чувствительности.
Особые указания
Следует соблюдать осторожность при назначении пациентам с нарушением функции почек, ИБС (существует риск учащения приступов стенокардии), в отношении хронической сердечной недостаточности: необходимо компенсировать перед началом применения препарата.
С особой осторожностью следует применять препарат у пациентов с синдромом слабости синусового узла (без кардиостимулятора).
Несмотря на то, что контролируемые исследования гемодинамики не выявили нарушений со стороны функции левого желудочка, лечение блокаторами кальциевых каналов пациентов с признаками дисфункции левого желудочка должно осуществляться с особой осторожностью.
Существует также мнение о том, что пациенты с ИБС, получающие короткодействующие дигидропиридины, представляют собой группу высокого риска по заболеваниям сердечно-сосудистой системы.
Особую осторожность следует соблюдать на начальных стадиях лечения пациентов с легкой и средней степенью выраженности недостаточности функции печени.
Влияние на способность к управлению транспортными средствами и механизмами
В период лечения следует соблюдать осторожность при выполнении работ, требующих повышенного внимания, при управлении транспортными средствами, особенно в начале лечения и при повышении дозы препарата (риск развития сонливости, головной боли и головокружения).
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Терапевтическая доза подбирается постепенно, увеличение дозы до 20 мг осуществляется через 2 недели после начала приема препарата."}},{"type":"paragraph","data":{"text":"Маловероятно, что эффективность препарата будет возрастать с увеличением дозы более 20 мг/сут, в то же время повышается риск возникновения побочных эффектов."}},{"type":"paragraph","data":{"text":"У пациентов пожилого возраста коррекция дозы не требуется, однако при приеме препарата необходим постоянный контроль состояния пациентов."}},{"type":"paragraph","data":{"text":"Применение у пациентов с нарушениями функции почек или печени"}},{"type":"paragraph","data":{"text":"При почечной или печеночной недостаточности легкой или средней тяжести, как правило, коррекции дозы не требуется, начальная доза - 10 мг, увеличение дозы до 20 мг/сут следует проводить с осторожностью. В случае, если антигипертензивный эффект будет слишком сильно выражен, следует снизить дозу."}}]},{"id":12,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Нежелательные реакции, распределенных по системам органов и частоте возникновения (классификация ВОЗ): часто (от более 1/100 до менее 1/10), нечасто (от более 1/1000 до менее 1/100), редко (от более 1/10000 до менее 1/1000), очень редко (менее 1/10000), включая отдельные сообщения."}},{"type":"paragraph","data":{"text":"Со стороны нервной системы: нечасто - головная боль, головокружение; редко - сонливость."}},{"type":"paragraph","data":{"text":"Со стороны сердечно-сосудистой системы: нечасто - ощущение сердцебиения, тахикардия, \"приливы\" крови к коже лица; редко - стенокардия; очень редко - обморок, выраженное снижение АД, боль в груди, инфаркт миокарда, у пациентов со стенокардией возможно увеличение частоты, продолжительности и тяжести приступов."}},{"type":"paragraph","data":{"text":"Со стороны пищеварительной системы: редко - тошнота, рвота, диарея, боли в животе, диспепсия; очень редко - повышение активности печеночных ферментов (обратимое)."}},{"type":"paragraph","data":{"text":"Со стороны кожи и подкожных тканей: редко - кожная сыпь."}},{"type":"paragraph","data":{"text":"Со стороны костно-мышечной системы и соединительной ткани: редко - миалгия."}},{"type":"paragraph","data":{"text":"Со стороны почек и мочевыводящих путей: редко - поллакиурия (увеличение частоты мочеиспускания)."}},{"type":"paragraph","data":{"text":"Общие реакции: нечасто - периферические отеки; редко - астения, повышенная утомляемость; очень редко - гиперплазия десен."}},{"type":"paragraph","data":{"text":"Со стороны иммунной системы: очень редко - реакции повышенной чувствительности."}}]},{"id":15,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"Следует соблюдать осторожность при назначении пациентам с нарушением функции почек, ИБС (существует риск учащения приступов стенокардии), в отношении хронической сердечной недостаточности: необходимо компенсировать перед началом применения препарата."}},{"type":"paragraph","data":{"text":"С особой осторожностью следует применять препарат у пациентов с синдромом слабости синусового узла (без кардиостимулятора)."}},{"type":"paragraph","data":{"text":"Несмотря на то, что контролируемые исследования гемодинамики не выявили нарушений со стороны функции левого желудочка, лечение блокаторами кальциевых каналов пациентов с признаками дисфункции левого желудочка должно осуществляться с особой осторожностью."}},{"type":"paragraph","data":{"text":"Существует также мнение о том, что пациенты с ИБС, получающие короткодействующие дигидропиридины, представляют собой группу высокого риска по заболеваниям сердечно-сосудистой системы."}},{"type":"paragraph","data":{"text":"Особую осторожность следует соблюдать на начальных стадиях лечения пациентов с легкой и средней степенью выраженности недостаточности функции печени."}},{"type":"paragraph","data":{"text":"Влияние на способность к управлению транспортными средствами и механизмами"}},{"type":"paragraph","data":{"text":"В период лечения следует соблюдать осторожность при выполнении работ, требующих повышенного внимания, при управлении транспортными средствами, особенно в начале лечения и при повышении дозы препарата (риск развития сонливости, головной боли и головокружения)."}}]}],"source":{"title":"ЗдравСити","url":"https://zdravcity.ru"}},"description_toggle":false,"short_description":"Лерканидипин является рацемической смесью право- (R) и левовращающих (S) стереоизомеров, производное 1,4-дигидропиридина, способен избирательно блокировать ток ионов кальция внутрь клеток сосудистой стенки, сердечные клетки и клетки гладкой мускулатуры. 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