Суматриптан - специфический селективный агонист 5-НТ1-серотониновых рецепторов, локализованных преимущественно в кровеносных сосудах головного мозга и их стимуляция приводит к сужению этих сосудов. Не влияет на другие подтипы 5-НТ-серотониновых рецепторов (5-НТ2-7). Активирует чувствительность рецепторов тройничного нерва. Терапевтический эффект обычно наступает через 30 мин после приема.
Фармакологические свойства
После приема внутрь быстро всасывается. 70% от максимальной плазменной концентрации достигается через 45 мин. Cmax в плазме крови составляет 54 нг/мл. Биодоступность - 14% (за счет пресистемного метаболизма и неполного всасывания). Связывание с белками плазмы составляет 14-21%.
Метаболизируется путем окисления при участии моноаминоксилазы (преимущественно изофермента А) с образованием метаболитов, основными из которых являются индолуксусный аналог суматриптана, не обладающий фармакологической активностью в отношении 5-НТ1-серотониновых рецепторов, и его глюкуронид. Выводится почками, преимущественно в виде метаболитов.
Показания к применению
Приступ мигрени с аурой или без нее.
Противопоказания
Гемиплегическая, базилярная или офтальмоплегическая формы мигрени;
ИБС или наличие симптомов, позволяющих предположить ее наличие;
повышенная чувствительность к любому из компонентов препарата.
С осторожностью
Эпилепсия (в т.ч. любые состояния со сниженным эпилептическим порогом), фармакологически контролируемая артериальная гипертензия, нарушения функции печени или почек, повышенная чувствительность к сульфаниламидам (введение суматриптана может вызвать аллергические реакции, выраженность которых варьируется от кожных проявлений до анафилаксии).
Применение при беременности и в период грудного вскармливания
Противопоказан во время беременности и в период грудного вскармливания (грудное вскармливание возможно не ранее чем через 24 ч после приема препарата).
Противопоказан в возрасте до 18 лет.
Способ применения и дозы
Внутрь, таблетку следует проглатывать целиком, запивая водой. Начинать лечение следует как можно раньше при возникновении приступа мигрени. Рекомендуемая доза - 50 мг, при необходимости - 100 мг.
Если симптомы мигрени не исчезают и не уменьшаются после приема первой дозы, то повторно для купирования этого же приступа препарат не применяют.
Для купирования последующих приступов (при уменьшении или исчезновении симптомов, а затем возобновлении) можно принять вторую дозу в течение следующих 24 ч при условии, что интервал между приемом составляет не менее 2 ч.
Максимальная суточная доза - 300 мг.
Побочное действие
Частота побочных реакций, приведенных ниже, определялась соответственно следующему: очень часто - более 1/10; часто - от более 1/100 до менее 1/10; иногда - от более 1/1000 до менее 1/100; редко - от более 1/10 000 до менее 1/1000; очень редко - от менее 1/10 000, включая отдельные случаи.
Со стороны нервной системы: часто - головокружение, сонливость, нарушения чувствительности, включая парастезии и снижение чувствительности.
Со стороны сердечно-сосудистой системы: часто - преходящее повышение АД (наблюдается вскоре после приема препарата), «приливы».
Со стороны дыхательной системы и органов группой клетки: часто – диспноэ, легкое, преходящее раздражение слизистой оболочки или чувство жжения в носовой полости или горле, носовое кровотечение.
Со стороны ЖКТ: часто - тошнота, рвота.
Со стороны опорно-двигательного аппарата и соединительной ткани: часто - чувство тяжести (обычно преходящее, может быть интенсивным и возникать в любой части тела, включая грудную клетку и горло).
Общие и местные реакции: часто - болевые ощущения, чувство холода или жара, чувство давления пли стягивания (обычно преходящее, могут быть интенсивными и возникать в любой части тела, включая грудную клетку и горло), слабость, утомляемость (обычно слабо или умеренно выражены, преходящи).
Лабораторные показатели: очень редко - незначительные отклонения показателей печеночных проб.
Постмаркетинговое наблюдение
Со стороны иммунной системы: очень редко - реакции гиперчувствительности, включая кожные проявления, а также анафилаксию.
Со стороны нервной системы: очень редко - судорожные припадки (в ряде случаев наблюдавшиеся у пациентов с судорожными приступами в анамнезе или при сопутствующих состояниях, предрасполагающих к возникновению судорог; у части пациентов факторов риска не было выявлено), тремор, дистония, нистагм, скотома.
Со стороны органов зрения: очень редко - мелькание, диплопия, снижение остроты зрения, слепота (обычно преходящая). Однако, расстройства зрения могут быть обусловлены собственно приступом мигрени.
Со стороны сердечно-сосудистой системы: очень редко - брадикардия, тахикардия, трепетание, аритмии, транзиторные изменения на ЭКГ, коронарный вазоспазм, стенокардия, инфаркт миокарда, гипотония, синдром Рейно.
Со стороны ЖКТ: очень редко - ишемический колит, дисфагия, ощущение дискомфорта в животе.
Передозировка
Симптомы: при приеме внутрь до 400 мг не наблюдается каких-либо других побочных реакций, кроме перечисленных выше.
Лечение: промывание желудка, наблюдение за больным в течение 10 ч, симптоматическая терапия.
Взаимодействие с другими лекарственными средствами
При одновременном введении с эрготамином и эрготаминсодержащими лекарственными средствами возможен длительный спазм сосудов.
Возможно взаимодействие между суматриптаном и ингибиторами МАО (снижение интенсивности метаболизма суматриптана, повышение его концентрации).
При одновременном применении суматриптана и лекарственных средств из группы селективных ингибиторов обратного захвата серотонина возможно развитие слабости, гиперрефлексии и нарушения координации движений.
Не отмечено взаимодействия суматриптана с пропранололом, флуниризином, пизотифеном и этанолом.
Особые указания
Не применять для профилактики приступа мигрени.
Больным группы риска со стороны сердечно-сосудистой системы терапию не начинают без предварительного обследования (женщины в постклимактерическом периоде, мужчины в возрасте старше 40 лет, лица с факторами риска развития ИБС). Перед назначением суматриптана пациентам с впервые выявленной или атипичной мигренью, следует исключить другие потенциально опасные неврологические заболевания. После приема суматриптана могут возникать боль и чувство стеснения в груди. Боль может быть интенсивной и иррадиировать в шею. Если есть основания полагать, что эти симптомы являются проявлением ИБС, необходимо провести и соответствующее обследование.
Влияние на способность к вождению автотранспорта и управлению механизмами.
В период лечения необходимо соблюдать осторожность при вождении автотранспорта и занятии др. потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций.
Условия отпуска
По рецепту.
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Не влияет на другие подтипы 5-НТ-серотониновых рецепторов (5-НТ2-7). Активирует чувствительность рецепторов тройничного нерва. Терапевтический эффект обычно наступает через 30 мин после приема."}}]},{"id":7,"name":"Фармакологические свойства","slug":"","body":[{"type":"paragraph","data":{"text":"После приема внутрь быстро всасывается. 70% от максимальной плазменной концентрации достигается через 45 мин. C\u003csub\u003emax\u003c/sub\u003e в плазме крови составляет 54 нг/мл. Биодоступность - 14% (за счет пресистемного метаболизма и неполного всасывания). Связывание с белками плазмы составляет 14-21%."}},{"type":"paragraph","data":{"text":"Метаболизируется путем окисления при участии моноаминоксилазы (преимущественно изофермента А) с образованием метаболитов, основными из которых являются индолуксусный аналог суматриптана, не обладающий фармакологической активностью в отношении 5-НТ1-серотониновых рецепторов, и его глюкуронид. Выводится почками, преимущественно в виде метаболитов."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"Приступ мигрени с аурой или без нее."}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"paragraph","data":{"text":"Гемиплегическая, базилярная или офтальмоплегическая формы мигрени;"}},{"type":"paragraph","data":{"text":"ИБС или наличие симптомов, позволяющих предположить ее наличие;"}},{"type":"paragraph","data":{"text":"инфаркт миокарда в анамнезе;"}},{"type":"paragraph","data":{"text":"фармакологически неконтролируемая артериальная гипертензия;"}},{"type":"paragraph","data":{"text":"окклюзионные заболевания периферических сосудов;"}},{"type":"paragraph","data":{"text":"инсульт или преходящее нарушение мозгового кровообращения (в т.ч. в анамнезе);"}},{"type":"paragraph","data":{"text":"выраженные нарушения функций печени и почек;"}},{"type":"paragraph","data":{"text":"одновременный прием с эрготамином или его производными и в течение 24 ч после их приема;"}},{"type":"paragraph","data":{"text":"применение на фоне приема ингибиторов моноаминооксидазы или ранее, чем через 2 недели после отмены этих препаратов;"}},{"type":"paragraph","data":{"text":"возраст до 18 и старше 65 лет (эффективность и безопасность не установлены);"}},{"type":"paragraph","data":{"text":"беременность;"}},{"type":"paragraph","data":{"text":"грудное вскармливание (грудное вскармливание возможно не ранее чем через 24 ч после приема препарата;"}},{"type":"paragraph","data":{"text":"врожденная галактоземия, синдром мальабсорбции глюкозы/галактозы, врожденная недостаточность лактозы;"}},{"type":"paragraph","data":{"text":"повышенная чувствительность к любому из компонентов препарата."}}]},{"id":10,"name":"С осторожностью","slug":"cautions","body":[{"type":"paragraph","data":{"text":"Эпилепсия (в т.ч. любые состояния со сниженным эпилептическим порогом), фармакологически контролируемая артериальная гипертензия, нарушения функции печени или почек, повышенная чувствительность к сульфаниламидам (введение суматриптана может вызвать аллергические реакции, выраженность которых варьируется от кожных проявлений до анафилаксии)."}}]},{"id":11,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","body":[{"type":"paragraph","data":{"text":"Противопоказан во время беременности и в период грудного вскармливания (грудное вскармливание возможно не ранее чем через 24 ч после приема препарата)."}},{"type":"paragraph","data":{"text":"Противопоказан в возрасте до 18 лет."}}]},{"id":12,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Внутрь, таблетку следует проглатывать целиком, запивая водой. Начинать лечение следует как можно раньше при возникновении приступа мигрени. Рекомендуемая доза - 50 мг, при необходимости - 100 мг."}},{"type":"paragraph","data":{"text":"Если симптомы мигрени не исчезают и не уменьшаются после приема первой дозы, то повторно для купирования этого же приступа препарат не применяют."}},{"type":"paragraph","data":{"text":"Для купирования последующих приступов (при уменьшении или исчезновении симптомов, а затем возобновлении) можно принять вторую дозу в течение следующих 24 ч при условии, что интервал между приемом составляет не менее 2 ч."}},{"type":"paragraph","data":{"text":"Максимальная суточная доза - 300 мг."}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Частота побочных реакций, приведенных ниже, определялась соответственно следующему: очень часто - более 1/10; часто - от более 1/100 до менее 1/10; иногда - от более 1/1000 до менее 1/100; редко - от более 1/10 000 до менее 1/1000; очень редко - от менее 1/10 000, включая отдельные случаи."}},{"type":"paragraph","data":{"text":"Со стороны нервной системы: часто - головокружение, сонливость, нарушения чувствительности, включая парастезии и снижение чувствительности."}},{"type":"paragraph","data":{"text":"Со стороны сердечно-сосудистой системы: часто - преходящее повышение АД (наблюдается вскоре после приема препарата), «приливы»."}},{"type":"paragraph","data":{"text":"Со стороны дыхательной системы и органов группой клетки: часто – диспноэ, легкое, преходящее раздражение слизистой оболочки или чувство жжения в носовой полости или горле, носовое кровотечение."}},{"type":"paragraph","data":{"text":"Со стороны ЖКТ: часто - тошнота, рвота."}},{"type":"paragraph","data":{"text":"Со стороны опорно-двигательного аппарата и соединительной ткани: часто - чувство тяжести (обычно преходящее, может быть интенсивным и возникать в любой части тела, включая грудную клетку и горло)."}},{"type":"paragraph","data":{"text":"Общие и местные реакции: часто - болевые ощущения, чувство холода или жара, чувство давления пли стягивания (обычно преходящее, могут быть интенсивными и возникать в любой части тела, включая грудную клетку и горло), слабость, утомляемость (обычно слабо или умеренно выражены, преходящи)."}},{"type":"paragraph","data":{"text":"Лабораторные показатели: очень редко - незначительные отклонения показателей печеночных проб."}},{"type":"paragraph","data":{"text":"Постмаркетинговое наблюдение"}},{"type":"paragraph","data":{"text":"Со стороны иммунной системы: очень редко - реакции гиперчувствительности, включая кожные проявления, а также анафилаксию."}},{"type":"paragraph","data":{"text":"Со стороны нервной системы: очень редко - судорожные припадки (в ряде случаев наблюдавшиеся у пациентов с судорожными приступами в анамнезе или при сопутствующих состояниях, предрасполагающих к возникновению судорог; у части пациентов факторов риска не было выявлено), тремор, дистония, нистагм, скотома."}},{"type":"paragraph","data":{"text":"Со стороны органов зрения: очень редко - мелькание, диплопия, снижение остроты зрения, слепота (обычно преходящая). Однако, расстройства зрения могут быть обусловлены собственно приступом мигрени."}},{"type":"paragraph","data":{"text":"Со стороны сердечно-сосудистой системы: очень редко - брадикардия, тахикардия, трепетание, аритмии, транзиторные изменения на ЭКГ, коронарный вазоспазм, стенокардия, инфаркт миокарда, гипотония, синдром Рейно."}},{"type":"paragraph","data":{"text":"Со стороны ЖКТ: очень редко - ишемический колит, дисфагия, ощущение дискомфорта в животе."}}]},{"id":14,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"Симптомы: при приеме внутрь до 400 мг не наблюдается каких-либо других побочных реакций, кроме перечисленных выше."}},{"type":"paragraph","data":{"text":"Лечение: промывание желудка, наблюдение за больным в течение 10 ч, симптоматическая терапия."}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"При одновременном введении с эрготамином и эрготаминсодержащими лекарственными средствами возможен длительный спазм сосудов."}},{"type":"paragraph","data":{"text":"Возможно взаимодействие между суматриптаном и ингибиторами МАО (снижение интенсивности метаболизма суматриптана, повышение его концентрации)."}},{"type":"paragraph","data":{"text":"При одновременном применении суматриптана и лекарственных средств из группы селективных ингибиторов обратного захвата серотонина возможно развитие слабости, гиперрефлексии и нарушения координации движений."}},{"type":"paragraph","data":{"text":"Не отмечено взаимодействия суматриптана с пропранололом, флуниризином, пизотифеном и этанолом."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"Не применять для профилактики приступа мигрени."}},{"type":"paragraph","data":{"text":"Больным группы риска со стороны сердечно-сосудистой системы терапию не начинают без предварительного обследования (женщины в постклимактерическом периоде, мужчины в возрасте старше 40 лет, лица с факторами риска развития ИБС). Перед назначением суматриптана пациентам с впервые выявленной или атипичной мигренью, следует исключить другие потенциально опасные неврологические заболевания. После приема суматриптана могут возникать боль и чувство стеснения в груди. Боль может быть интенсивной и иррадиировать в шею. Если есть основания полагать, что эти симптомы являются проявлением ИБС, необходимо провести и соответствующее обследование."}},{"type":"paragraph","data":{"text":"Влияние на способность к вождению автотранспорта и управлению механизмами."}},{"type":"paragraph","data":{"text":"В период лечения необходимо соблюдать осторожность при вождении автотранспорта и занятии др. потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций."}}]},{"id":21,"name":"Условия отпуска","slug":"release_condition","body":[{"type":"paragraph","data":{"text":"По рецепту."}}]},{"id":22,"name":"Производитель","slug":"","body":[{"type":"paragraph","data":{"text":"Велфарм"}}]}],"source":null},"description_toggle":false,"short_description":"Средство для лечения 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