Фармакологическое действие Противомигренозный препарат. Специфический селективный агонист серотониновых 5-НТ1D (5-гидрокситриптаминовых подтипа 1D)-рецепторов, локализованных преимущественно в кровеносных сосудах головного мозга, не действует на другие подтипы серотониновых 5-НТ-рецепторов (5-НТ2-5-НТ7). Вызывает сужение сосудов каротидного артериального ложа, которые снабжают кровью экстракраниальные и интракраниальные ткани (расширение сосудов мозговых оболочек и/или их отек является основным механизмом развития мигрени у человека), не оказывая при этом существенного влияния на мозговой кровоток. Подавляет активность рецепторов окончаний афферентных волокон тройничного нерва в твердой мозговой оболочке (в результате уменьшается выделение сенсорных нейропептидов). Оба этих эффекта могут лежать в основе противомигренозного действия суматриптана. Устраняет ассоциированную с мигренозным приступом тошноту и светобоязнь. В 50-70% случаев быстро устраняет приступ при приеме внутрь в дозе 25-100 мг. В течение 24 ч в 1/3 случаев может развиться рецидив, требующий повторного применения. Клинический эффект отмечается обычно через 30 мин после приема внутрь. Способ применения и дозы Препарат принимают внутрь. Таблетку следует проглатывать целиком, запивая водой. Лечение начинают как можно раньше после возникновения приступа мигрени (хотя препарат эффективен на любой стадии приступа). Для купирования острых приступов мигрени рекомендуемая доза взрослым - 50 мг 1 раз/сут. Некоторым пациентам может потребоваться более высокая доза - 100 мг. Если симптомы не исчезают и не уменьшаются после приема первой дозы, то для купирования этого же приступа повторно принимать препарат не следует. Однако препарат можно применять для купирования последующих приступов мигрени. Если пациент почувствовал улучшение после первой дозы, а затем симптомы возобновились, можно принять вторую дозу в течение следующих 24 ч с интервалом не менее 2 ч после приема первой дозы. Максимальная доза суматриптана - 300 мг в течение 24 ч. Противопоказания — гемиплегическая, базилярная или офтальмоплегическая формы мигрени . — ИБС (в т.ч. подозрение на нее) . — стенокардия (в т.ч. стенокардия Принцметала) . — инфаркт миокарда (в т.ч. в анамнезе) . — постинфарктный кардиосклероз . — неконтролируемая артериальная гипертензия . — окклюзионные заболевания периферических сосудов . — инсульт или транзиторное ишемическое нарушение мозгового кровообращения (в т. ч. в анамнезе) . — прием одновременно с эрготамином или его производными (включая метисергид) . — применение на фоне приема ингибиторов МАО или ранее, чем через 2 недели после отмены этих препаратов . — выраженное нарушение функции печени и/или почек . — детский и подростковый возраст до 18 лет . — пожилой возраст (старше 65 лет) . — беременность . — период лактации (в течение 24 ч после приема препарата) . — повышенная чувствительность к компонентам препарата. С осторожностью: — эпилепсия (в т.ч. любые состояния со снижением порога судорожной готовности) . — контролируемая артериальная гипертензия . — нарушение функции печени и почек . — у пациентов с повышенной чувствительностью к сульфаниламидам (возможны аллергические реакции с выраженностью от кожных проявлений до анафилаксии). Меры предосторожности Применение при нарушениях функции печени Противопоказан при выраженном нарушении функции печени. Применение при нарушениях функции почек Противопоказан при выраженном нарушении функции почек. Применение у детей Противопоказан в детском и подростковом возрасте до 18 лет. Применение у пожилых пациентов Противопоказан в пожилом возрасте (старше 65 лет). Побочное действие Общие реакции: боль, ощущение жара или покалывания, чувство сдавления или тяжести. Эти симптомы обычно являются преходящими, но могут быть интенсивными и возникать в любой части тела, включая грудную клетку и горло. Приливы, головокружение, ощущение слабости, чувство усталости, сонливость обычно выражены слабо или умеренно и носят преходящий характер. Со стороны сердечно-сосудистой системы: снижение АД, преходящее повышение АД (наблюдается вскоре после приема суматриптана), брадикардия, тахикардия (в т.ч. желудочковая), аритмии, стенокардия . нарушения сердечного ритма, преходящие изменения ЭКГ по ишемическому типу, инфаркт миокарда, спазм коронарных артерий . в единичных случаях - синдром Рейно. Со стороны пищеварительной системы: тошнота, рвота, ишемический колит (связь этих побочных эффектов с суматриптаном не установлена), дисфагия, ощущение дискомфорта в животе. Двигательные расстройства: чувство скованности (эти симптомы обычно являются преходящими, но могут быть интенсивными и возникать в любой части тела, включая грудную клетку и горло) . тремор, ригидность мышц затылка. Со стороны нервной системы: сенсорные нарушения, включая парестезию . судорожные приступы (в ряде случаев они наблюдались у пациентов с судорогами в анамнезе или при состояниях, предрасполагающих к возникновению судорог . у части пациентов предрасполагающих факторов выявлено не было), дистония. Со стороны органов чувств: диплопия, мелькание "мушек" перед глазами, нистагм, скотома, снижение остроты зрения. Крайне редко развивается частичная преходящая потеря зрения. Однако следует иметь в виду, что нарушения зрения могут быть связаны с приступами мигрени. Аллергические реакции: кожная сыпь (в т.ч. крапивница и эритематозные высыпания), зуд кожи, анафилактические реакции. Со стороны лабораторных показателей: незначительные изменения активности печеночных трансаминаз. Со стороны дыхательной системы: одышка, носовое кровотечение. Передозировка Симптомы: при приеме внутрь в дозе до 400 мг не наблюдается каких-либо других побочных реакций, кроме ранее перечисленных. Лечение: симптоматическая терапия, наблюдение за состоянием больного не менее 10 ч. Нет данных о влиянии гемодиализа или перитонеального диализа на концентрацию суматриптана в плазме. Применение при беременности и кормлении грудью Противопоказано применение препарата при беременности и в период лактации (грудного вскармливания). Тип: Лекарственное средство Количество в упаковке, шт: 1 Срок годности: 36 мес Сфера применения: Анальгетики, Противомигренозные, Неврология Действующее вещество: Суматриптан (Sumatriptan) Путь введения: Перорально Порядок отпуска: По рецепту Форма выпуска: По рецепту Условия хранения: В защищенном от солнца помещении, Беречь от детей Максимальная допустимая температура хранения, °С: 30 Фармакологическая группа: N02CC01 Суматриптан Нозологическая классификация (МКБ-10): G43 Мигрень
Фармакокинетика Всасывание После приема внутрь быстро абсорбируется из ЖКТ. Через 45 мин концентрация суматриптана в плазме достигает 70% от Cmax. Биодоступность составляет 14% (за счет пресистемного метаболизма и неполного всасывания). После приема внутрь суматриптана в дозе 100 мг Cmax в плазме крови составляет 54 нг/мл. Распределение Связывание с белками плазмы составляет 14-21%. Общий Vd - 170 л (2.4 л/кг). Метаболизм Метаболизируется путем окисления при участии МАО (преимущественно изофермента А) с образованием основного метаболита - индолуксусного аналога суматриптана, не обладающего фармакологической активностью в отношении серотониновых 5-НТ1- и 5-НТ2-рецепторов. Выведение T1/2 суматриптана - около 2 ч. Плазменный клиренс - 1160 мл/мин, почечный клиренс - 260 мл/мин . внепочечный клиренс - 80% от общего клиренса. Выводится почками, преимущественно в виде метаболитов (97% после приема внутрь) - свободной кислоты или глюкуронидного конъюгата.
Побочное действие
мигрень (купирование приступов, с аурой или без нее).
Особые указания
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действие Противомигренозный препарат. Специфический селективный агонист серотониновых 5-НТ1D (5-гидрокситриптаминовых подтипа 1D)-рецепторов, локализованных преимущественно в кровеносных сосудах головного мозга, не действует на другие подтипы серотониновых 5-НТ-рецепторов (5-НТ2-5-НТ7). Вызывает сужение сосудов каротидного артериального ложа, которые снабжают кровью экстракраниальные и интракраниальные ткани (расширение сосудов мозговых оболочек и/или их отек является основным механизмом развития мигрени у человека), не оказывая при этом существенного влияния на мозговой кровоток. Подавляет активность рецепторов окончаний афферентных волокон тройничного нерва в твердой мозговой оболочке (в результате уменьшается выделение сенсорных нейропептидов). Оба этих эффекта могут лежать в основе противомигренозного действия суматриптана. Устраняет ассоциированную с мигренозным приступом тошноту и светобоязнь. В 50-70% случаев быстро устраняет приступ при приеме внутрь в дозе 25-100 мг. В течение 24 ч в 1/3 случаев может развиться рецидив, требующий повторного применения. Клинический эффект отмечается обычно через 30 мин после приема внутрь. Способ применения и дозы Препарат принимают внутрь. Таблетку следует проглатывать целиком, запивая водой. Лечение начинают как можно раньше после возникновения приступа мигрени (хотя препарат эффективен на любой стадии приступа). Для купирования острых приступов мигрени рекомендуемая доза взрослым - 50 мг 1 раз/сут. Некоторым пациентам может потребоваться более высокая доза - 100 мг. Если симптомы не исчезают и не уменьшаются после приема первой дозы, то для купирования этого же приступа повторно принимать препарат не следует. Однако препарат можно применять для купирования последующих приступов мигрени. Если пациент почувствовал улучшение после первой дозы, а затем симптомы возобновились, можно принять вторую дозу в течение следующих 24 ч с интервалом не менее 2 ч после приема первой дозы. Максимальная доза суматриптана - 300 мг в течение 24 ч. Противопоказания — гемиплегическая, базилярная или офтальмоплегическая формы мигрени . — ИБС (в т.ч. подозрение на нее) . — стенокардия (в т.ч. стенокардия Принцметала) . — инфаркт миокарда (в т.ч. в анамнезе) . — постинфарктный кардиосклероз . — неконтролируемая артериальная гипертензия . — окклюзионные заболевания периферических сосудов . — инсульт или транзиторное ишемическое нарушение мозгового кровообращения (в т. ч. в анамнезе) . — прием одновременно с эрготамином или его производными (включая метисергид) . — применение на фоне приема ингибиторов МАО или ранее, чем через 2 недели после отмены этих препаратов . — выраженное нарушение функции печени и/или почек . — детский и подростковый возраст до 18 лет . — пожилой возраст (старше 65 лет) . — беременность . — период лактации (в течение 24 ч после приема препарата) . — повышенная чувствительность к компонентам препарата. С осторожностью: — эпилепсия (в т.ч. любые состояния со снижением порога судорожной готовности) . — контролируемая артериальная гипертензия . — нарушение функции печени и почек . — у пациентов с повышенной чувствительностью к сульфаниламидам (возможны аллергические реакции с выраженностью от кожных проявлений до анафилаксии). Меры предосторожности Применение при нарушениях функции печени Противопоказан при выраженном нарушении функции печени. Применение при нарушениях функции почек Противопоказан при выраженном нарушении функции почек. Применение у детей Противопоказан в детском и подростковом возрасте до 18 лет. Применение у пожилых пациентов Противопоказан в пожилом возрасте (старше 65 лет). Побочное действие Общие реакции: боль, ощущение жара или покалывания, чувство сдавления или тяжести. Эти симптомы обычно являются преходящими, но могут быть интенсивными и возникать в любой части тела, включая грудную клетку и горло. Приливы, головокружение, ощущение слабости, чувство усталости, сонливость обычно выражены слабо или умеренно и носят преходящий характер. Со стороны сердечно-сосудистой системы: снижение АД, преходящее повышение АД (наблюдается вскоре после приема суматриптана), брадикардия, тахикардия (в т.ч. желудочковая), аритмии, стенокардия . нарушения сердечного ритма, преходящие изменения ЭКГ по ишемическому типу, инфаркт миокарда, спазм коронарных артерий . в единичных случаях - синдром Рейно. Со стороны пищеварительной системы: тошнота, рвота, ишемический колит (связь этих побочных эффектов с суматриптаном не установлена), дисфагия, ощущение дискомфорта в животе. Двигательные расстройства: чувство скованности (эти симптомы обычно являются преходящими, но могут быть интенсивными и возникать в любой части тела, включая грудную клетку и горло) . тремор, ригидность мышц затылка. Со стороны нервной системы: сенсорные нарушения, включая парестезию . судорожные приступы (в ряде случаев они наблюдались у пациентов с судорогами в анамнезе или при состояниях, предрасполагающих к возникновению судорог . у части пациентов предрасполагающих факторов выявлено не было), дистония. Со стороны органов чувств: диплопия, мелькание \"мушек\" перед глазами, нистагм, скотома, снижение остроты зрения. Крайне редко развивается частичная преходящая потеря зрения. Однако следует иметь в виду, что нарушения зрения могут быть связаны с приступами мигрени. Аллергические реакции: кожная сыпь (в т.ч. крапивница и эритематозные высыпания), зуд кожи, анафилактические реакции. Со стороны лабораторных показателей: незначительные изменения активности печеночных трансаминаз. Со стороны дыхательной системы: одышка, носовое кровотечение. Передозировка Симптомы: при приеме внутрь в дозе до 400 мг не наблюдается каких-либо других побочных реакций, кроме ранее перечисленных. Лечение: симптоматическая терапия, наблюдение за состоянием больного не менее 10 ч. Нет данных о влиянии гемодиализа или перитонеального диализа на концентрацию суматриптана в плазме. Применение при беременности и кормлении грудью Противопоказано применение препарата при беременности и в период лактации (грудного вскармливания). Тип: Лекарственное средство Количество в упаковке, шт: 1 Срок годности: 36 мес Сфера применения: Анальгетики, Противомигренозные, Неврология Действующее вещество: Суматриптан (Sumatriptan) Путь введения: Перорально Порядок отпуска: По рецепту Форма выпуска: По рецепту Условия хранения: В защищенном от солнца помещении, Беречь от детей Максимальная допустимая температура хранения, °С: 30 Фармакологическая группа: N02CC01 Суматриптан Нозологическая классификация (МКБ-10): G43 Мигрень"}}]},{"id":2,"name":"Показания к применению","slug":"indications","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Состав 1 таб. суматриптана сукцинат 140 мг, что соответствует содержанию суматриптана 100 мг Вспомогательные вещества: лактозы моногидрат - 140 мг, кроскармеллоза натрия - 12 мг, лактоза безводная (Pharmatose DCL 21) - 211.4 мг, целлюлоза микрокристаллическая (Авицел PH 102) - 90.6 мг, магния стеарат - 6 мг. Состав оболочки: лактозы моногидрат - 8.64 мг, маннитол - 5.52 мг, титана диоксид - 4.8 мг, тальк - 3.6 мг, триацетин - 1.44 мг."}}]},{"id":3,"name":"Способ применения и дозы","slug":"dosage","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Фармакокинетика Всасывание После приема внутрь быстро абсорбируется из ЖКТ. Через 45 мин концентрация суматриптана в плазме достигает 70% от Cmax. Биодоступность составляет 14% (за счет пресистемного метаболизма и неполного всасывания). После приема внутрь суматриптана в дозе 100 мг Cmax в плазме крови составляет 54 нг/мл. Распределение Связывание с белками плазмы составляет 14-21%. Общий Vd - 170 л (2.4 л/кг). Метаболизм Метаболизируется путем окисления при участии МАО (преимущественно изофермента А) с образованием основного метаболита - индолуксусного аналога суматриптана, не обладающего фармакологической активностью в отношении серотониновых 5-НТ1- и 5-НТ2-рецепторов. Выведение T1/2 суматриптана - около 2 ч. Плазменный клиренс - 1160 мл/мин, почечный клиренс - 260 мл/мин . внепочечный клиренс - 80% от общего клиренса. Выводится почками, преимущественно в виде метаболитов (97% после приема внутрь) - свободной кислоты или глюкуронидного конъюгата."}}]},{"id":4,"name":"Побочное действие","slug":"side_effects","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"мигрень (купирование приступов, с аурой или без нее)."}}]},{"id":5,"name":"Особые указания","slug":"cautions","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"мигрень (купирование приступов, с аурой или без нее)."}}]}],"source":{"title":"36.6","url":"https://366.ru"}},"description_toggle":false,"short_description":"Фармакологическое действие Противомигренозный препарат. Специфический селективный агонист серотониновых 5-НТ1D (5-гидрокситриптаминовых подтипа 1D)-рецепторов, локализованных преимущественно в кровеносных сосудах головного мозга, не действует на другие подтипы серотониновых 5-НТ-рецепторов (5-НТ2-5-НТ7). Вызывает сужение сосудов каротидного артериального ложа, которые снабжают кровью экстракраниальные и интракраниальные ткани (расширение сосудов мозговых оболочек и/или их отек является основным механизмом развития мигрени у человека), не оказывая при этом существенного влияния на мозговой кровоток. Подавляет активность рецепторов окончаний афферентных волокон тройничного нерва в твердой мозговой оболочке (в результате уменьшается выделение сенсорных нейропептидов). Оба этих эффекта могут лежать в основе противомигренозного действия суматриптана. Устраняет ассоциированную с мигренозным приступом тошноту и светобоязнь. В 50-70% случаев быстро устраняет приступ при приеме внутрь в дозе 25-100 мг. В течение 24 ч в 1/3 случаев может развиться рецидив, требующий повторного применения. Клинический эффект отмечается обычно через 30 мин после приема внутрь. Способ применения и дозы Препарат принимают внутрь. Таблетку следует проглатывать целиком, запивая водой. Лечение начинают как можно раньше после возникновения приступа мигрени (хотя препарат эффективен на любой стадии приступа). Для купирования острых приступов мигрени рекомендуемая доза взрослым - 50 мг 1 раз/сут. Некоторым пациентам может потребоваться более высокая доза - 100 мг. Если симптомы не исчезают и не уменьшаются после приема первой дозы, то для купирования этого же приступа повторно принимать препарат не следует. Однако препарат можно применять для купирования последующих приступов мигрени. Если пациент почувствовал улучшение после первой дозы, а затем симптомы возобновились, можно принять вторую дозу в течение следующих 24 ч с интервалом не менее 2 ч после приема первой дозы. Максимальная доза суматриптана - 300 мг в течение 24 ч. Противопоказания — гемиплегическая, базилярная или офтальмоплегическая формы мигрени . — ИБС (в т.ч. подозрение на нее) . — стенокардия (в т.ч. стенокардия Принцметала) . — инфаркт миокарда (в т.ч. в анамнезе) . — постинфарктный кардиосклероз . — неконтролируемая артериальная гипертензия . — окклюзионные заболевания периферических сосудов . — инсульт или транзиторное ишемическое нарушение мозгового кровообращения (в т. ч. в анамнезе) . — прием одновременно с эрготамином или его производными (включая метисергид) . — применение на фоне приема ингибиторов МАО или ранее, чем через 2 недели после отмены этих препаратов . — выраженное нарушение функции печени и/или почек . — детский и подростковый возраст до 18 лет . — пожилой возраст (старше 65 лет) . — беременность . — период лактации (в течение 24 ч после приема препарата) . — повышенная чувствительность к компонентам препарата. С осторожностью: — эпилепсия (в т.ч. любые состояния со снижением порога судорожной готовности) . — контролируемая артериальная гипертензия . — нарушение функции печени и почек . — у пациентов с повышенной чувствительностью к сульфаниламидам (возможны аллергические реакции с выраженностью от кожных проявлений до анафилаксии). Меры предосторожности Применение при нарушениях функции печени Противопоказан при выраженном нарушении функции печени. Применение при нарушениях функции почек Противопоказан при выраженном нарушении функции почек. Применение у детей Противопоказан в детском и подростковом возрасте до 18 лет. Применение у пожилых пациентов Противопоказан в пожилом возрасте (старше 65 лет). Побочное действие Общие реакции: боль, ощущение жара или покалывания, чувство сдавления или тяжести. Эти симптомы обычно являются преходящими, но могут быть интенсивными и возникать в любой части тела, включая грудную клетку и горло. Приливы, головокружение, ощущение слабости, чувство усталости, сонливость обычно выражены слабо или умеренно и носят преходящий характер. Со стороны сердечно-сосудистой системы: снижение АД, преходящее повышение АД (наблюдается вскоре после приема суматриптана), брадикардия, тахикардия (в т.ч. желудочковая), аритмии, стенокардия . нарушения сердечного ритма, преходящие изменения ЭКГ по ишемическому типу, инфаркт миокарда, спазм коронарных артерий . в единичных случаях - синдром Рейно. Со стороны пищеварительной системы: тошнота, рвота, ишемический колит (связь этих побочных эффектов с суматриптаном не установлена), дисфагия, ощущение дискомфорта в животе. Двигательные расстройства: чувство скованности (эти симптомы обычно являются преходящими, но могут быть интенсивными и возникать в любой части тела, включая грудную клетку и горло) . тремор, ригидность мышц затылка. Со стороны нервной системы: сенсорные нарушения, включая парестезию . судорожные приступы (в ряде случаев они наблюдались у пациентов с судорогами в анамнезе или при состояниях, предрасполагающих к возникновению судорог . у части пациентов предрасполагающих факторов выявлено не было), дистония. Со стороны органов чувств: диплопия, мелькание \"мушек\" перед глазами, нистагм, скотома, снижение остроты зрения. Крайне редко развивается частичная преходящая потеря зрения. Однако следует иметь в виду, что нарушения зрения могут быть связаны с приступами мигрени. Аллергические реакции: кожная сыпь (в т.ч. крапивница и эритематозные высыпания), зуд кожи, анафилактические реакции. Со стороны лабораторных показателей: незначительные изменения активности печеночных трансаминаз. Со стороны дыхательной системы: одышка, носовое кровотечение. Передозировка Симптомы: при приеме внутрь в дозе до 400 мг не наблюдается каких-либо других побочных реакций, кроме ранее перечисленных. Лечение: симптоматическая терапия, наблюдение за состоянием больного не менее 10 ч. Нет данных о влиянии гемодиализа или перитонеального диализа на концентрацию суматриптана в плазме. Применение при беременности и кормлении грудью Противопоказано применение препарата при беременности и в период лактации (грудного вскармливания). 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