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 ...
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.
Способ применения и дозы
мигрень (купирование приступов, с аурой или без нее).
Побочное действие
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).
Особые указания
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).
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