Антагонист лейкотриеновых рецепторов. Монтелукаст с высокой... Инструкция
Показания к применению
Профилактика и длительное лечение бронхиальной астмы, включая: предупреждение дневных и ночных симптомов заболевания; лечение бронхиальной астмы у пациентов с повышенной чувствительностью к ацетилсалициловой кислоте; предупреждение бронхоспазма, вызванного физической нагрузкой.
Купирование дневных и ночных симптомов сезонных аллергических ринитов.
Противопоказания
Повышенная чувствительность к монтелукасту; детский возраст - в зависимости от лекарственной формы.
Антагонист лейкотриеновых рецепторов. Монтелукаст с высокой избирательностью и химическим сродством связывается с CysLT1-рецепторами (вместо других фармакологически важных рецепторов дыхательных путей, таких как простагландиновые, холинергические или β-адренергические рецепторы).
Монтелукаст ингибирует физиологическое действие цисгеинил-лейкотриенов LTC4, LTD4 и LTE4 путем связывания с CysLT1-рецепторами, не оказывая стимулирующего действия на данные рецепторы. Монтелукаст ингибирует CysLT1-рецепторы эпителия дыхательных путей, обладая тем самым одновременно способностью ингибировать бронхоспазм, обусловленный вдыханием LTD4 у пациентов с бронхиальной астмой.
Дозы 5 мг достаточно для купирования бронхоспазма, индуцированного LTD4.
Монтелукаст вызывает бронходилатацию в течение 2 ч после приема внутрь и может дополнять бронходилатацию, вызванную бета2-адреномиметиками.
Фармакокинетика
После приема внутрь монтелукаст быстро и практически полностью всасывается из ЖКТ. У взрослых при приеме в дозе 5-10 мг Cmax в плазме крови достигается через 2-3 ч. Биодоступность при приеме внутрь составляет 64-73%.
Связывание монтелукаста с белками плазмы составляет более 99%. Vd в среднем составляет 8-11 л.
При однократном приеме в дозе 10 мг 1 раз/сут наблюдается умеренная (около 14%) кумуляция активного вещества в плазме.
Монтелукаст активно метаболизируется в печени. При применении в терапевтических дозах концентрация метаболитов монтелукаста в плазме в равновесном состоянии у взрослых и детей не определяется.
Предполагается, что в процессе метаболизма монтелукаста участвуют изоферменты CYP3А4 и CYP2С9, при этом в терапевтических концентрациях монтелукаст не ингибирует изоферменты CYP3А4, 2С9, 1А2, 2А6, 2С19 и 2D6.
T1/2 монтелукаста у молодых здоровых взрослых составляет от 2.7 до 5.5 ч. Клиренс монтелукаста составляет у здоровых взрослых в среднем 45 мл/мин. После перорального приема монтелукаста 86% выводится с калом в течение 5 дней и менее 0.2% - с мочой, что подтверждает то, что монтелукаст и его метаболиты выводятся почти исключительно с желчью.
Фармакокинетика монтелукаста сохраняет практически линейный характер при приеме внутрь в дозах более 50 мг.
Показания к применению
Профилактика и длительное лечение бронхиальной астмы, включая: предупреждение дневных и ночных симптомов заболевания; лечение бронхиальной астмы у пациентов с повышенной чувствительностью к ацетилсалициловой кислоте; предупреждение бронхоспазма, вызванного физической нагрузкой.
Купирование дневных и ночных симптомов сезонных аллергических ринитов.
Противопоказания
Повышенная чувствительность к монтелукасту; детский возраст - в зависимости от лекарственной формы.
Применение при беременности и в период грудного вскармливания
При беременности монтелукаст можно применять только в том случае, когда потенциальная польза для матери превышает возможный риск для плода, только под контролем врача и только в минимальных дозах.
Сообщалось о развитии врожденных дефектов конечностей у новорожденных, матери которых принимали монтелукаст в период беременности. Большинство этих женщин также принимали другие препараты для лечения бронхиальной астмы в период беременности. Причинно-следственная связь между приемом монтелукаста и развитием врожденных дефектов конечностей не установлена.
Неизвестно, выделяется ли монтелукаст с грудным молоком. Не следует применять монтелукаст в период лактации (грудного вскармливания).
Способ применения и дозы
Внутрь. Дозу и схему применения устанавливают индивидуально, в зависимости от показаний, возраста пациента и применяемой лекарственной формы.
Монтелукаст можно добавлять к лечению бронходилататорами и ингаляционными ГКС.
Побочное действие
Инфекционные заболевания: очень часто - инфекции верхних дыхательных путей.
Со стороны системы кроветворения: редко - повышенная склонность к кровотечениям; частота неизвестна -тромбоцитопения.
Со стороны иммунной системы: нечасто - реакции гиперчувствительности, в т.ч. анафилаксия; очень редко - эозинофильная инфильтрация печени.
Со стороны психики: нечасто - ажитация, в т.ч. агрессивное поведение или враждебность, тревожность, депрессия, дезориентация, патологические сновидения, бессонница, психомоторная активность (включая раздражительность, беспокойство и тремор), сомнамбулизм, тик; редко - нарушение внимания, нарушения памяти; очень редко - галлюцинации, суицидальные мысли и поведение (суицидальность).
Со стороны нервной системы: нечасто - головная боль, головокружение, сонливость, парестезия/гипестезия, судороги.
Со стороны сердечно-сосудистой системы: редко - учащенное сердцебиение.
Со стороны дыхательной системы: нечасто - носовое кровотечение; очень редко - легочная эозинофилия.
Со стороны пищеварительной системы: часто - диарея, тошнота, рвота; нечасто - диспепсия, сухость во рту; частота неизвестна - боль в животе, панкреатит.
Со стороны печени и желчевыводящих путей: часто - увеличение активности АЛТ и ACT; очень редко - гепатит (включая холестатические, гепатоцеллюлярные и смешанные поражения печени).
Со стороны кожи и подкожных тканей: часто - сыпь; нечасто - зуд, крапивница, склонность к формированию гематом; редко - ангионевротический отек; очень редко - узловатая эритема, многоформная эритема.
Со стороны костно-мышечной системы: нечасто - артралгия, миалгия, включая мышечные судороги.
Со стороны мочевыделительной системы: частота неизвестна - энурез у детей.
Прочие: часто - лихорадка; нечасто - астения (слабость)/повышенная утомляемость, отеки, жажда; у пациентов с бронхиальной астмой редко - развитие синдрома Черджа-Стросса.
Взаимодействие с другими лекарственными средствами
При одновременном применении с фенобарбиталом AUC монтелукаста уменьшалась примерно на 40% (коррекция режима монтелукаста не требуется).
В исследованиях in vitro установлено, что монтелукаст ингибирует изофермент CYP2C8, однако при исследовании лекарственного взаимодействия in vivo монтелукаста и росиглитазона (метаболизируется с участием изофермента CYP2C8 ) не получено подтверждения ингибирования монтелукастом изофермента CYP2C8. Поэтому в клинической практике не предполагается влияние монтелукаста на CYP2С8-опосредованный метаболизм ряда лекарственных препаратов, в т.ч. паклитаксела, росиглитазона, репаглинида.
Исследованияinvitroпоказали, что монтелукаст является субстратом изоферментов CYP2C8, 2С9 и 3А4. Данные клинического исследования лекарственного взаимодействия в отношении монтелукаста и гемфиброзила (ингибитора как изофермента CYP2C8, так и изофермента 2С9) демонстрируют, что гемфиброзил повышает эффект системного воздействия монтелукаста в 4,4 раза.
Совместный прием итраконазола, мощного ингибитора изофермента CYP3A4, вместе с гемфиброзилом и монтелукастом не приводил к дополнительному повышению эффекта системного воздействия монтелукаста.
Монтелукаст является обоснованным дополнением к монотерапии бронходилататорами, если последние не обеспечивают адекватного контроля бронхиальной астмы. По достижении терапевтического эффекта от лечения монтелукастом можно начать постепенное снижение дозы бронходилататоров.
Применение монтелукаста обеспечивает дополнительный терапевтический эффект у пациентов, получающих ингаляционные ГКС. По достижении стабилизации состояния, можно начать постепенное снижение дозы ГКС под наблюдением врача. В некоторых случаях допустима полная отмена ингаляционных ГКС, однако резкая замена ингаляционных кортикостероидов на монтелукаст не рекомендуется.
Особые указания
Эффективность монтелукаста для приема внутрь в отношении лечения острых приступов бронхиальной астмы не установлена. Поэтому монтелукаст для приема внутрь не рекомендуется применять для лечения острых приступов бронхиальной астмы. Пациентам должны быть даны инструкции всегда иметь при себе препараты экстренной помощи для купирования приступов бронхиальной астмы (ингаляционные бета2-агонисты короткого действия).
Не следует прекращать прием монтелукаста в период обострения астмы и необходимости применения для купирования приступов препаратов экстренной помощи (ингаляционных бета2-агонистов короткого действия).
Пациенты с подтвержденной аллергией к ацетилсалициловой кислоте и другим НПВС не должны принимать эти препараты в период лечения монтелукастом, поскольку монтелукаст, улучшая дыхательную функцию у пациентов с аллергической бронхиальной астмой, тем не менее, не может полностью предотвратить вызванную у них НПВС бронхоконстрикцию.
Дозу ингаляционных ГКС, применяемых одновременно с монтелукастом, можно постепенно снижать под наблюдением врача, однако резкой замены ингаляционных или пероральных ГКС монтелукастом проводить нельзя.
Влияние на способность управлять автомобилем и движущимися механизмами
У некоторых пациентов на фоне применения монтелукаста отмечались сонливость и головокружение. При появлении этих признаков пациентам не рекомендуется управлять транспортными средствами и заниматься другими видами деятельности, требующими концентрации внимания и быстроты психомоторных реакций.
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вещества\u003c/i\u003e: крахмал прежелатинизированный - 20 мг, лактозы моногидрат - 139.4 мг, гипролоза (гидроксипропилцеллюлоза) низкозамещенная - 4 мг, карбоксиметилкрахмал натрия (натрия крахмала гликолат) - 20 мг, кремния диоксид коллоидный безводный - 1.6 мг, магния стеарат - 2.6 мг."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСостав оболочки:\u003c/i\u003e опадрай белого цвета 03F28342 (тальк - 3.442 мг, гипромеллоза - 3.123 мг, титана диоксид - 0.765 мг, макрогол - 0.637 мг) - 7.967 мг, краситель железа оксид желтый (E172) - 0.027 мг, краситель железа оксид красный (E172) - 0.006 мг."}}]},{"id":10,"name":"Фармакологические свойства","slug":"pharmacologic_effects","body":[{"type":"paragraph","data":{"text":"Антагонист лейкотриеновых рецепторов. Монтелукаст с высокой избирательностью и химическим сродством связывается с CysLT\u003csub\u003e1\u003c/sub\u003e-рецепторами (вместо других фармакологически важных рецепторов дыхательных путей, таких как простагландиновые, холинергические или β-адренергические рецепторы)."}},{"type":"paragraph","data":{"text":"Монтелукаст ингибирует физиологическое действие цисгеинил-лейкотриенов LTC\u003csub\u003e4\u003c/sub\u003e, LTD\u003csub\u003e4\u003c/sub\u003e и LTE\u003csub\u003e4\u003c/sub\u003e путем связывания с CysLT\u003csub\u003e1\u003c/sub\u003e-рецепторами, не оказывая стимулирующего действия на данные рецепторы. Монтелукаст ингибирует CysLT\u003csub\u003e1\u003c/sub\u003e-рецепторы эпителия дыхательных путей, обладая тем самым одновременно способностью ингибировать бронхоспазм, обусловленный вдыханием LTD\u003csub\u003e4\u003c/sub\u003e у пациентов с бронхиальной астмой."}},{"type":"paragraph","data":{"text":"Дозы 5 мг достаточно для купирования бронхоспазма, индуцированного LTD\u003csub\u003e4\u003c/sub\u003e."}},{"type":"paragraph","data":{"text":"Монтелукаст вызывает бронходилатацию в течение 2 ч после приема внутрь и может дополнять бронходилатацию, вызванную бета\u003csub\u003e2\u003c/sub\u003e-адреномиметиками."}},{"type":"header","data":{"text":"Фармакокинетика","level":4}},{"type":"paragraph","data":{"text":"После приема внутрь монтелукаст быстро и практически полностью всасывается из ЖКТ. У взрослых при приеме в дозе 5-10 мг C\u003csub\u003emax\u003c/sub\u003e в плазме крови достигается через 2-3 ч. Биодоступность при приеме внутрь составляет 64-73%."}},{"type":"paragraph","data":{"text":"Связывание монтелукаста с белками плазмы составляет более 99%. V\u003csub\u003ed\u003c/sub\u003e в среднем составляет 8-11 л."}},{"type":"paragraph","data":{"text":"При однократном приеме в дозе 10 мг 1 раз/сут наблюдается умеренная (около 14%) кумуляция активного вещества в плазме."}},{"type":"paragraph","data":{"text":"Монтелукаст активно метаболизируется в печени. При применении в терапевтических дозах концентрация метаболитов монтелукаста в плазме в равновесном состоянии у взрослых и детей не определяется."}},{"type":"paragraph","data":{"text":"Предполагается, что в процессе метаболизма монтелукаста участвуют изоферменты CYP3А4 и CYP2С9, при этом в терапевтических концентрациях монтелукаст не ингибирует изоферменты CYP3А4, 2С9, 1А2, 2А6, 2С19 и 2D6."}},{"type":"paragraph","data":{"text":"T\u003csub\u003e1/2\u003c/sub\u003e монтелукаста у молодых здоровых взрослых составляет от 2.7 до 5.5 ч. Клиренс монтелукаста составляет у здоровых взрослых в среднем 45 мл/мин. После перорального приема монтелукаста 86% выводится с калом в течение 5 дней и менее 0.2% - с мочой, что подтверждает то, что монтелукаст и его метаболиты выводятся почти исключительно с желчью."}},{"type":"paragraph","data":{"text":"Фармакокинетика монтелукаста сохраняет практически линейный характер при приеме внутрь в дозах более 50 мг."}}]},{"id":11,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"Профилактика и длительное лечение бронхиальной астмы, включая: предупреждение дневных и ночных симптомов заболевания; лечение бронхиальной астмы у пациентов с повышенной чувствительностью к ацетилсалициловой кислоте; предупреждение бронхоспазма, вызванного физической нагрузкой."}},{"type":"paragraph","data":{"text":"Купирование дневных и ночных симптомов сезонных аллергических ринитов."}}]},{"id":12,"name":"Противопоказания","slug":"contraindications","body":[{"type":"paragraph","data":{"text":"Повышенная чувствительность к монтелукасту; детский возраст - в зависимости от лекарственной формы."}}]},{"id":14,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","body":[{"type":"paragraph","data":{"text":"При беременности монтелукаст можно применять только в том случае, когда потенциальная польза для матери превышает возможный риск для плода, только под контролем врача и только в минимальных дозах."}},{"type":"paragraph","data":{"text":"Сообщалось о развитии врожденных дефектов конечностей у новорожденных, матери которых принимали монтелукаст в период беременности. Большинство этих женщин также принимали другие препараты для лечения бронхиальной астмы в период беременности. Причинно-следственная связь между приемом монтелукаста и развитием врожденных дефектов конечностей не установлена."}},{"type":"paragraph","data":{"text":"Неизвестно, выделяется ли монтелукаст с грудным молоком. Не следует применять монтелукаст в период лактации (грудного вскармливания)."}}]},{"id":15,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Внутрь. Дозу и схему применения устанавливают индивидуально, в зависимости от показаний, возраста пациента и применяемой лекарственной формы."}},{"type":"paragraph","data":{"text":"Монтелукаст можно добавлять к лечению бронходилататорами и ингаляционными ГКС."}}]},{"id":16,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"\u003ci\u003eИнфекционные заболевания: \u003c/i\u003eочень часто - инфекции верхних дыхательных путей."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны системы кроветворения: \u003c/i\u003eредко - повышенная склонность к кровотечениям; частота неизвестна -тромбоцитопения."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны иммунной системы: \u003c/i\u003eнечасто - реакции гиперчувствительности, в т.ч. анафилаксия; очень редко - эозинофильная инфильтрация печени."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны психики:\u003c/i\u003e нечасто - ажитация, в т.ч. агрессивное поведение или враждебность, тревожность, депрессия, дезориентация, патологические сновидения, бессонница, психомоторная активность (включая раздражительность, беспокойство и тремор), сомнамбулизм, тик; редко - нарушение внимания, нарушения памяти; очень редко - галлюцинации, суицидальные мысли и поведение (суицидальность)."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны нервной системы: \u003c/i\u003eнечасто - головная боль, головокружение, сонливость, парестезия/гипестезия, судороги."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны сердечно-сосудистой системы: \u003c/i\u003eредко - учащенное сердцебиение."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны дыхательной системы: \u003c/i\u003eнечасто - носовое кровотечение; очень редко - легочная эозинофилия."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны пищеварительной системы: \u003c/i\u003eчасто - диарея, тошнота, рвота; нечасто - диспепсия, сухость во рту; частота неизвестна - боль в животе, панкреатит."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны печени и желчевыводящих путей: \u003c/i\u003eчасто - увеличение активности АЛТ и ACT; очень редко - гепатит (включая холестатические, гепатоцеллюлярные и смешанные поражения печени)."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны кожи и подкожных тканей: \u003c/i\u003eчасто - сыпь; нечасто - зуд, крапивница, склонность к формированию гематом; редко - ангионевротический отек; очень редко - узловатая эритема, многоформная эритема."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны костно-мышечной системы:\u003c/i\u003e нечасто - артралгия, миалгия, включая мышечные судороги."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны мочевыделительной системы: \u003c/i\u003eчастота неизвестна - энурез у детей."}},{"type":"paragraph","data":{"text":"\u003ci\u003eПрочие:\u003c/i\u003e часто - лихорадка; нечасто - астения (слабость)/повышенная утомляемость, отеки, жажда; у пациентов с бронхиальной астмой редко - развитие синдрома Черджа-Стросса."}}]},{"id":18,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"При одновременном применении с фенобарбиталом AUC монтелукаста уменьшалась примерно на 40% (коррекция режима монтелукаста не требуется)."}},{"type":"paragraph","data":{"text":"В исследованиях in vitro установлено, что монтелукаст ингибирует изофермент CYP2C8, однако при исследовании лекарственного взаимодействия in vivo монтелукаста и росиглитазона (метаболизируется с участием изофермента CYP2C8 ) не получено подтверждения ингибирования монтелукастом изофермента CYP2C8. Поэтому в клинической практике не предполагается влияние монтелукаста на CYP2С8-опосредованный метаболизм ряда лекарственных препаратов, в т.ч. паклитаксела, росиглитазона, репаглинида."}},{"type":"paragraph","data":{"text":"Исследования\u003ci\u003einvitro\u003c/i\u003eпоказали, что монтелукаст является субстратом изоферментов CYP2C8, 2С9 и 3А4. Данные клинического исследования лекарственного взаимодействия в отношении монтелукаста и гемфиброзила (ингибитора как изофермента CYP2C8, так и изофермента 2С9) демонстрируют, что гемфиброзил повышает эффект системного воздействия монтелукаста в 4,4 раза."}},{"type":"paragraph","data":{"text":"Совместный прием итраконазола, мощного ингибитора изофермента CYP3A4, вместе с гемфиброзилом и монтелукастом не приводил к дополнительному повышению эффекта системного воздействия монтелукаста."}},{"type":"paragraph","data":{"text":"Монтелукаст является обоснованным дополнением к монотерапии бронходилататорами, если последние не обеспечивают адекватного контроля бронхиальной астмы. По достижении терапевтического эффекта от лечения монтелукастом можно начать постепенное снижение дозы бронходилататоров."}},{"type":"paragraph","data":{"text":"Применение монтелукаста обеспечивает дополнительный терапевтический эффект у пациентов, получающих ингаляционные ГКС. По достижении стабилизации состояния, можно начать постепенное снижение дозы ГКС под наблюдением врача. В некоторых случаях допустима полная отмена ингаляционных ГКС, однако резкая замена ингаляционных кортикостероидов на монтелукаст не рекомендуется."}}]},{"id":19,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"Эффективность монтелукаста для приема внутрь в отношении лечения острых приступов бронхиальной астмы не установлена. Поэтому монтелукаст для приема внутрь не рекомендуется применять для лечения острых приступов бронхиальной астмы. Пациентам должны быть даны инструкции всегда иметь при себе препараты экстренной помощи для купирования приступов бронхиальной астмы (ингаляционные бета\u003csub\u003e2\u003c/sub\u003e-агонисты короткого действия)."}},{"type":"paragraph","data":{"text":"Не следует прекращать прием монтелукаста в период обострения астмы и необходимости применения для купирования приступов препаратов экстренной помощи (ингаляционных бета\u003csub\u003e2\u003c/sub\u003e-агонистов короткого действия)."}},{"type":"paragraph","data":{"text":"Пациенты с подтвержденной аллергией к ацетилсалициловой кислоте и другим НПВС не должны принимать эти препараты в период лечения монтелукастом, поскольку монтелукаст, улучшая дыхательную функцию у пациентов с аллергической бронхиальной астмой, тем не менее, не может полностью предотвратить вызванную у них НПВС бронхоконстрикцию."}},{"type":"paragraph","data":{"text":"Дозу ингаляционных ГКС, применяемых одновременно с монтелукастом, можно постепенно снижать под наблюдением врача, однако резкой замены ингаляционных или пероральных ГКС монтелукастом проводить нельзя."}}]},{"id":20,"name":"Влияние на способность управлять автомобилем и движущимися механизмами","slug":"","body":[{"type":"paragraph","data":{"text":"У некоторых пациентов на фоне применения монтелукаста отмечались сонливость и головокружение. При появлении этих признаков пациентам не рекомендуется управлять транспортными средствами и заниматься другими видами деятельности, требующими концентрации внимания и быстроты психомоторных реакций."}}]},{"id":21,"name":"Форма выпуска","slug":"","body":[{"type":"paragraph","data":{"text":"Таблетки."}}]},{"id":24,"name":"Условия отпуска","slug":"release_condition","body":[{"type":"paragraph","data":{"text":"По рецепту."}}]}],"source":{"title":"('Эркафарм/Столетов',)","url":"https://stoletov.ru/"}},"description_toggle":false,"short_description":"Антагонист лейкотриеновых рецепторов. Монтелукаст с высокой избирательностью и химическим сродством связывается с CysLT1-рецепторами (вместо других фармакологически важных рецепторов дыхательных путей, таких как простагландиновые, холинергические или β-адренергические рецепторы). Монтелукаст ингибирует физиологическое действие цисгеинил-лейкотриенов LTC4, LTD4и LTE4путем связывания с CysLT1-рецепторами, не оказывая стимулирующего действия на данные рецепторы. Монтелукаст ингибирует CysLT1-рецепторы эпителия дыхательных путей, обладая тем самым одновременно способностью ингибировать бронхоспазм, обусловленный вдыханием LTD4у пациентов с бронхиальной астмой. Дозы 5 мг достаточно для купирования бронхоспазма, индуцированного LTD4. Монтелукаст вызывает бронходилатацию в течение 2 ч после приема внутрь и может дополнять бронходилатацию, вызванную бета2-адреномиметиками. После приема внутрь монтелукаст быстро и практически полностью всасывается из ЖКТ. У взрослых при приеме в дозе 5-10 мг Cmaxв плазме крови достигается через 2-3 ч. Биодоступность при приеме внутрь составляет 64-73%. Связывание монтелукаста с белками плазмы составляет более 99%. Vdв среднем составляет 8-11 л. При однократном приеме в дозе 10 мг 1 раз/сут наблюдается умеренная (около 14%) кумуляция активного вещества в плазме. Монтелукаст активно метаболизируется в печени. При применении в терапевтических дозах концентрация метаболитов монтелукаста в плазме в равновесном состоянии у взрослых и детей не определяется. Предполагается, что в процессе метаболизма монтелукаста участвуют изоферменты CYP3А4 и CYP2С9, при этом в терапевтических концентрациях монтелукаст не ингибирует изоферменты CYP3А4, 2С9, 1А2, 2А6, 2С19 и 2D6. T1/2монтелукаста у молодых здоровых взрослых составляет от 2.7 до 5.5 ч. Клиренс монтелукаста составляет у здоровых взрослых в среднем 45 мл/мин. После перорального приема монтелукаста 86% выводится с калом в течение 5 дней и менее 0.2% - с мочой, что подтверждает то, что монтелукаст и его метаболиты выводятся почти исключительно с желчью. 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