Инфекционно-воспалительные заболевания вызванные чувствительными к препарату микроорганизмами: инфекции верхних отделов дыхательных путей и ЛОР-органов (фарингит тонзиллит ларингит синусит средний отит); скарлатина; инфекции нижних отделов дыхательных путей (пневмония (в т.ч. вызванная атипичными возбудителями) бронхит); инфекции кожи и мягких тканей ...
Гиперчувствительность (в т.ч. к другим макролидам) тяжелая печеночная/почечная недостаточность период лактации дети до 12 лет (с массой тела менее 45 кг).
Инструкция
Регистрационный номер
ЛСР-003652/07 от 07.11.07
Торговое название препарата
Азитромицин
Лекарственная форма
капсулы
Состав
Активное вещество: азитромицина дигидрата - 265,3 мг в пересчете на активное вещество (азитромицин) - 250,0 мг.
Состав корпуса капсулы: титана диоксид - 1,0000 %, краситель железа оксид желтый - 0,0733 %, желатин - до 100 %.
Состав крышечки капсулы: титана диоксид - 1,0000 %, краситель железа оксид желтый - 0,0733 %, желатин - до 100%.
Описание
Капсулы № 0. Корпус и крышечка капсулы желтого, со слегка коричневым оттенком цвета, непрозрачные.
Содержимое капсул - порошок белого или белого со слегка желтоватым оттенком цвета.
Фармакотерапевтическая группа
Антибиотик - азалид
Фармакологические свойства
Фармакодинамика:
Антибактериальное средство широкого спектра действия азалид действует бактериостатически. Связываясь с 50S субъединицей рибосом угнетает пептидтранслоказу на стадии трансляции подавляет синтез белка замедляет рост и размножение бактерий в высоких концентрациях оказывает бактерицидный эффект. Действует на вне- и внутриклеточных возбудителей. Активен в отношении грамположительных микроорганизмов: Streptococcus spp. (групп С F и G кроме устойчивых к эритромицину) Streptococcus pneumoniae Streptococcus pyogenes Streptococcus agalactiae Streptococcus viridans Staphylococcus epidermidis Staphylococcus aureus; грамотрицательных бактерий: Haemophilus influenzae Moraxella catarrhalis Bordetella pertussis Bordetella parapertussis Legionella pneumophila Haemophilus ducreyi Helicobacter pylori Campylobacter jejuni Neisseria gonorrhoeae и Gardnerella vaginalis; некоторых анаэробных микроорганизмов: Bacteroides bivius Clostridium perfringens Peptostreptococcus spp; а также внутриклеточных возбудителей: Chlamydia trachomatis Chlamydia pneumoniae Mycoplasma pneumoniae Mycobacterium avium complex Ureaplasma urealyticum Treponema pallidum Borrelia burgdorferi. Неактивен в отношении грамположительных бактерий устойчивых к эритромицину.
Фармакокинетика:
Абсорбция - высокая кислотоустойчив липофилен. Биодоступность после однократного приема 05 г - 37% (эффект "первого прохождения" через печень) максимальная концентрация в плазме крови после перорального приема 05 г - 04 мг/л период достижения максимальной концентрации в плазме крови - 25-29 ч; в тканях и клетках концентрация в 10-50 раз выше чем в сыворотке крови объем распределения - 311 л/кг. Легко проходит гистогематические барьеры. Хорошо проникает в дыхательные пути мочеполовые органы и ткани в предстательную железу в кожу и мягкие ткани; накапливается в среде с низким pH в лизосомах (что особенно важно для эрадикации внутриклеточно расположенных возбудителей). Транспортируется также фагоцитами полиморфно-ядерными лейкоцитами и макрофагами. Проникает через мембраны клеток и создает высокие концентрации в них. Концентрация в очагах инфекции достоверно выше (на 24-34%) чем в здоровых тканях и коррелирует с выраженностью воспалительного отека. Сохраняется в эффективных концентрациях в течение 5-7 дней после приема последней дозы. Связь с белками плазмы - 7-50% (обратно пропорциональна концентрации в крови). В печени деметилируется образующиеся метаболиты не активны. В метаболизме препарата участвуют изоферменты CYP3A4 CYP3A5 CYP3A7 ингибитором которых он является. Плазменный клиренс - 630 мл/мин. Период полувыведения между 8 и 24 ч после приема -14-20 ч период полувыведения в интервале от 24 до 72 ч - 41 ч. 50% выводится с желчью в неизмененном виде 6% - почками. Прием пищи значимо изменяет фармакокинетику (в зависимости от лекарственной формы): капсулы - максимальная концентрация в плазме крови снижается (на 52%). У пожилых мужчин (65-85 лет) фармакокинетические параметры не меняются у женщин увеличивается максимальная концентрация в плазме крови (на 30-50%) у детей в возрасте 1-5 лет снижаются максимальное содержание в плазме крови период полувыведения.
Показания к применению
Инфекционно-воспалительные заболевания вызванные чувствительными к препарату микроорганизмами: инфекции верхних отделов дыхательных путей и ЛОР-органов (фарингит тонзиллит ларингит синусит средний отит); скарлатина; инфекции нижних отделов дыхательных путей (пневмония (в т.ч. вызванная атипичными возбудителями) бронхит); инфекции кожи и мягких тканей (рожа импетиго вторично инфицированные дерматозы); инфекции мочевыводящих путей (гонорейный и негонорейный уретрит цервицит); болезнь Лайма (начальная стадия - erythema migrans) язвенная болезнь желудка и 12-перстной кишки ассоциированная с Helicobacter pylori (в составе комбинированной терапии).
Противопоказания
Гиперчувствительность (в т.ч. к другим макролидам) тяжелая печеночная/почечная недостаточность период лактации дети до 12 лет (с массой тела менее 45 кг).
С осторожностью
Аритмия (возможны желудочковые аритмии и удлинение интервала Q-T) детям с нарушениями функции печени или почек беременность.
Применение при беременности и в период грудного вскармливания
Может применяться в тех случаях когда польза от его применения значительно превышает риск существующий всегда при использовании любого препарата в течение беременности. При необходимости назначение препарата в период лактации следует прекратить грудное вскармливание.
Способ применения и дозы
Внутрь за 1 ч до или через 2 ч после еды 1 раз в сутки.
Взрослым при инфекциях верхних и нижних отделов дыхательных путей - 500 мг/сут за 1 прием в течение 3 дней (курсовая доза - 1500 мг). При инфекциях кожи и мягких тканей - 1000 мг/сут в первый день за 1 прием далее по 500 мг/сут ежедневно с 2 по 5 день (курсовая доза - 3000 мг). При острых инфекциях мочеполовых органов (неосложненный уретрит или цервицит) - однократно 1 г. При болезни Лайма (боррелиоз) для лечения I стадии (erythema migrans) - 1000 мг в первый день и 500 мг ежедневно с 2 по 5 день (курсовая доза - 3 г). При язвенной болезни желудка и 12-перстной кишки ассоциированной с Helicobacter pylori - 1 г/сут в течение 3 дней в составе комбинированной антихеликобактерной терапии.
Детям старше 12 лет (с массой тела более 45 кг) при инфекциях верхних и нижних дыхательных путей кожи и мягких тканей назначают по 500 мг 1 раз в сутки в течение 3 дней.
При лечении erythema migrans у детей (старше 12 лет) препарат назначают 1 раз в сутки в дозе 1000 мг в первый день и по 500 мг со 2 по 5 день.
Побочное действие
Со стороны желудочно-кишечного тракта: диарея (5%) тошнота (3%) боль в животе (3%); 1% и менее - метеоризм рвота мелена холестатическая желтуха повышение активности "печеночных" трансаминаз; у детей - запоры снижение аппетита гастрит; кандидамикоз слизистой оболочки полости рта изменение вкуса (1% и менее).
Со стороны сердечно-сосудистой системы: сердцебиение боль в грудной клетке (1% и менее).
Со стороны нервной системы: головокружение головная боль сонливость; у детей - головная боль (при терапии среднего отита) гиперкинезия тревожность невроз нарушения сна (1% и менее).
Со стороны мочеполовой системы: вагинальный кандидамикоз нефрит (1% и менее). Аллергические реакции: сыпь крапивница зуд кожи ангионевротический отек у детей - конъюнктивит.
Взаимодействие с другими лекарственными средствами
Антациды (алюминий- и магнийсодержащие) этанол и пища замедляют и снижают абсорбцию азитромицина.
При совместном назначении варфарина и азитромицина (в обычных дозах) изменения протромбинового времени не выявлено однако учитывая что при взаимодействии макролидов и варфарина возможно усиление антикоагуляционного эффекта пациентам необходим тщательный контроль протромбинового времени.
Повышает концентрацию дигоксина за счет ослабления его инактивации кишечной флорой.
Эрготамин и дигидроэрготамин: усиление токсического действия (вазоспазм дизестезия). Триазолам: снижение клиренса и увеличение фармакологического действия триазолама. Замедляет выведение и повышает концентрацию в плазме и токсичность циклосерина непрямых антикоагулянтов метилпреднизолона фелодипина а также лекарственных средств подвергающихся микросомальному окислению (карбамазепин терфенадин циклоспорин гексобарбитал алкалоиды спорыньи вальпроевая кислота дизопирамид бромокриптин фенитоин пероральные гипогликемические лекарственные средства теофиллин и др. ксантиновые производные) за счет ингибирования микросомального окисления в гепатоцитах азитромицином.
Линкозамиды ослабляют а тетрациклин и хлорамфеникол усиливают эффективность азитромицина.
Особые указания
Не принимать с пищей.
В случае пропуска приема дозы пропущенную дозу следует принять как можно раньше а последующие - с интервалом в 24 ч.
Необходимо соблюдать перерыв 2 ч при одновременном применении антацидов.
После отмены лечения реакции гиперчувствительности у некоторых пациентов могут сохраняться что требует специфической терапии под наблюдением врача.
Форма выпуска
Капсулы по 250 мг.
Условия хранения
Хранить в защищенном от света месте при температуре не выше 25 °С.
Хранить в недоступном для детей месте.
Срок годности
4 года. Не использовать после истечения срока годности.
Условия отпуска
По рецепту
Производитель
Общество с ограниченной ответственностью "Озон" (ООО "Озон"), 445351, Самарская обл., г. Жигулёвск, ул. Гидростроителей, д. 6, Россия
Организация, принимающая претензии потребителей
ООО "Озон"
Для описания товара использована информация от партнера 36.6
Мобильное приложение «Все аптеки»
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100%."}}]},{"id":5,"name":"Описание","slug":"common_description","body":[{"type":"paragraph","data":{"text":"Капсулы № 0. Корпус и крышечка капсулы желтого, со слегка коричневым оттенком цвета, непрозрачные."}},{"type":"paragraph","data":{"text":"Содержимое капсул - порошок белого или белого со слегка желтоватым оттенком цвета."}}]},{"id":6,"name":"Фармакотерапевтическая группа","slug":"","body":[{"type":"paragraph","data":{"text":"Антибиотик - азалид"}}]},{"id":7,"name":"Фармакологические свойства","slug":"pharmacologic_effects","body":[{"type":"header","data":{"text":"Фармакодинамика:","level":3}},{"type":"paragraph","data":{"text":"Антибактериальное средство широкого спектра действия азалид действует бактериостатически. Связываясь с 50S субъединицей рибосом угнетает пептидтранслоказу на стадии трансляции подавляет синтез белка замедляет рост и размножение бактерий в высоких концентрациях оказывает бактерицидный эффект. Действует на вне- и внутриклеточных возбудителей. Активен в отношении грамположительных микроорганизмов: Streptococcus spp. (групп С F и G кроме устойчивых к эритромицину) Streptococcus pneumoniae Streptococcus pyogenes Streptococcus agalactiae Streptococcus viridans Staphylococcus epidermidis Staphylococcus aureus; грамотрицательных бактерий: Haemophilus influenzae Moraxella catarrhalis Bordetella pertussis Bordetella parapertussis Legionella pneumophila Haemophilus ducreyi Helicobacter pylori Campylobacter jejuni Neisseria gonorrhoeae и Gardnerella vaginalis; некоторых анаэробных микроорганизмов: Bacteroides bivius Clostridium perfringens Peptostreptococcus spp; а также внутриклеточных возбудителей: Chlamydia trachomatis Chlamydia pneumoniae Mycoplasma pneumoniae Mycobacterium avium complex Ureaplasma urealyticum Treponema pallidum Borrelia burgdorferi. Неактивен в отношении грамположительных бактерий устойчивых к эритромицину."}},{"type":"header","data":{"text":"Фармакокинетика:","level":3}},{"type":"paragraph","data":{"text":"Абсорбция - высокая кислотоустойчив липофилен. Биодоступность после однократного приема 05 г - 37% (эффект \"первого прохождения\" через печень) максимальная концентрация в плазме крови после перорального приема 05 г - 04 мг/л период достижения максимальной концентрации в плазме крови - 25-29 ч; в тканях и клетках концентрация в 10-50 раз выше чем в сыворотке крови объем распределения - 311 л/кг. Легко проходит гистогематические барьеры. Хорошо проникает в дыхательные пути мочеполовые органы и ткани в предстательную железу в кожу и мягкие ткани; накапливается в среде с низким pH в лизосомах (что особенно важно для эрадикации внутриклеточно расположенных возбудителей). Транспортируется также фагоцитами полиморфно-ядерными лейкоцитами и макрофагами. Проникает через мембраны клеток и создает высокие концентрации в них. Концентрация в очагах инфекции достоверно выше (на 24-34%) чем в здоровых тканях и коррелирует с выраженностью воспалительного отека. Сохраняется в эффективных концентрациях в течение 5-7 дней после приема последней дозы. Связь с белками плазмы - 7-50% (обратно пропорциональна концентрации в крови). В печени деметилируется образующиеся метаболиты не активны. В метаболизме препарата участвуют изоферменты CYP3A4 CYP3A5 CYP3A7 ингибитором которых он является. Плазменный клиренс - 630 мл/мин. Период полувыведения между 8 и 24 ч после приема -14-20 ч период полувыведения в интервале от 24 до 72 ч - 41 ч. 50% выводится с желчью в неизмененном виде 6% - почками. Прием пищи значимо изменяет фармакокинетику (в зависимости от лекарственной формы): капсулы - максимальная концентрация в плазме крови снижается (на 52%). У пожилых мужчин (65-85 лет) фармакокинетические параметры не меняются у женщин увеличивается максимальная концентрация в плазме крови (на 30-50%) у детей в возрасте 1-5 лет снижаются максимальное содержание в плазме крови период полувыведения."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"Инфекционно-воспалительные заболевания вызванные чувствительными к препарату микроорганизмами: инфекции верхних отделов дыхательных путей и ЛОР-органов (фарингит тонзиллит ларингит синусит средний отит); скарлатина; инфекции нижних отделов дыхательных путей (пневмония (в т.ч. вызванная атипичными возбудителями) бронхит); инфекции кожи и мягких тканей (рожа импетиго вторично инфицированные дерматозы); инфекции мочевыводящих путей (гонорейный и негонорейный уретрит цервицит); болезнь Лайма (начальная стадия - erythema migrans) язвенная болезнь желудка и 12-перстной кишки ассоциированная с Helicobacter pylori (в составе комбинированной терапии)."}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"paragraph","data":{"text":"Гиперчувствительность (в т.ч. к другим макролидам) тяжелая печеночная/почечная недостаточность период лактации дети до 12 лет (с массой тела менее 45 кг)."}}]},{"id":10,"name":"С осторожностью","slug":"cautions","body":[{"type":"paragraph","data":{"text":"Аритмия (возможны желудочковые аритмии и удлинение интервала Q-T) детям с нарушениями функции печени или почек беременность."}}]},{"id":11,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","body":[{"type":"paragraph","data":{"text":"Может применяться в тех случаях когда польза от его применения значительно превышает риск существующий всегда при использовании любого препарата в течение беременности. При необходимости назначение препарата в период лактации следует прекратить грудное вскармливание."}}]},{"id":12,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Внутрь за 1 ч до или через 2 ч после еды 1 раз в сутки."}},{"type":"paragraph","data":{"text":"Взрослым при инфекциях верхних и нижних отделов дыхательных путей - 500 мг/сут за 1 прием в течение 3 дней (курсовая доза - 1500 мг). При инфекциях кожи и мягких тканей - 1000 мг/сут в первый день за 1 прием далее по 500 мг/сут ежедневно с 2 по 5 день (курсовая доза - 3000 мг). При острых инфекциях мочеполовых органов (неосложненный уретрит или цервицит) - однократно 1 г. При болезни Лайма (боррелиоз) для лечения I стадии (erythema migrans) - 1000 мг в первый день и 500 мг ежедневно с 2 по 5 день (курсовая доза - 3 г). При язвенной болезни желудка и 12-перстной кишки ассоциированной с Helicobacter pylori - 1 г/сут в течение 3 дней в составе комбинированной антихеликобактерной терапии."}},{"type":"paragraph","data":{"text":"Детям старше 12 лет (с массой тела более 45 кг) при инфекциях верхних и нижних дыхательных путей кожи и мягких тканей назначают по 500 мг 1 раз в сутки в течение 3 дней."}},{"type":"paragraph","data":{"text":"При лечении erythema migrans у детей (старше 12 лет) препарат назначают 1 раз в сутки в дозе 1000 мг в первый день и по 500 мг со 2 по 5 день."}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Со стороны желудочно-кишечного тракта: диарея (5%) тошнота (3%) боль в животе (3%); 1% и менее - метеоризм рвота мелена холестатическая желтуха повышение активности \"печеночных\" трансаминаз; у детей - запоры снижение аппетита гастрит; кандидамикоз слизистой оболочки полости рта изменение вкуса (1% и менее)."}},{"type":"paragraph","data":{"text":"Со стороны сердечно-сосудистой системы: сердцебиение боль в грудной клетке (1% и менее)."}},{"type":"paragraph","data":{"text":"Со стороны нервной системы: головокружение головная боль сонливость; у детей - головная боль (при терапии среднего отита) гиперкинезия тревожность невроз нарушения сна (1% и менее)."}},{"type":"paragraph","data":{"text":"Со стороны мочеполовой системы: вагинальный кандидамикоз нефрит (1% и менее). Аллергические реакции: сыпь крапивница зуд кожи ангионевротический отек у детей - конъюнктивит."}},{"type":"paragraph","data":{"text":"Прочие: астения фотосенсибилизация."}}]},{"id":14,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"Симптомы: сильная тошнота временная потеря слуха рвота диарея."}},{"type":"paragraph","data":{"text":"Лечение: промывание желудка симптоматическая терапия."}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"Антациды (алюминий- и магнийсодержащие) этанол и пища замедляют и снижают абсорбцию азитромицина."}},{"type":"paragraph","data":{"text":"При совместном назначении варфарина и азитромицина (в обычных дозах) изменения протромбинового времени не выявлено однако учитывая что при взаимодействии макролидов и варфарина возможно усиление антикоагуляционного эффекта пациентам необходим тщательный контроль протромбинового времени."}},{"type":"paragraph","data":{"text":"Повышает концентрацию дигоксина за счет ослабления его инактивации кишечной флорой."}},{"type":"paragraph","data":{"text":"Эрготамин и дигидроэрготамин: усиление токсического действия (вазоспазм дизестезия). Триазолам: снижение клиренса и увеличение фармакологического действия триазолама. Замедляет выведение и повышает концентрацию в плазме и токсичность циклосерина непрямых антикоагулянтов метилпреднизолона фелодипина а также лекарственных средств подвергающихся микросомальному окислению (карбамазепин терфенадин циклоспорин гексобарбитал алкалоиды спорыньи вальпроевая кислота дизопирамид бромокриптин фенитоин пероральные гипогликемические лекарственные средства теофиллин и др. ксантиновые производные) за счет ингибирования микросомального окисления в гепатоцитах азитромицином."}},{"type":"paragraph","data":{"text":"Линкозамиды ослабляют а тетрациклин и хлорамфеникол усиливают эффективность азитромицина."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"Не принимать с пищей."}},{"type":"paragraph","data":{"text":"В случае пропуска приема дозы пропущенную дозу следует принять как можно раньше а последующие - с интервалом в 24 ч."}},{"type":"paragraph","data":{"text":"Необходимо соблюдать перерыв 2 ч при одновременном применении антацидов."}},{"type":"paragraph","data":{"text":"После отмены лечения реакции гиперчувствительности у некоторых пациентов могут сохраняться что требует специфической терапии под наблюдением врача."}}]},{"id":18,"name":"Форма выпуска","slug":"","body":[{"type":"paragraph","data":{"text":"Капсулы по 250 мг."}}]},{"id":19,"name":"Условия хранения","slug":"storage","body":[{"type":"paragraph","data":{"text":"Хранить в защищенном от света месте при температуре не выше 25 °С."}},{"type":"paragraph","data":{"text":"Хранить в недоступном для детей месте."}}]},{"id":20,"name":"Срок годности","slug":"expiry_date","body":[{"type":"paragraph","data":{"text":"4 года. Не использовать после истечения срока годности."}}]},{"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":"Общество с ограниченной ответственностью \"Озон\" (ООО \"Озон\"), 445351, Самарская обл., г. Жигулёвск, ул. Гидростроителей, д. 6, Россия"}}]},{"id":23,"name":"Организация, принимающая претензии потребителей","body":[{"type":"paragraph","data":{"text":"ООО \"Озон\""}}]}],"source":null},"description_toggle":false,"short_description":"Антибактериальное средство широкого спектра действия азалид действует бактериостатически. Связываясь с 50S субъединицей рибосом угнетает пептидтранслоказу на стадии трансляции подавляет синтез белка замедляет рост и размножение бактерий в высоких концентрациях оказывает бактерицидный эффект. Действует на вне- и внутриклеточных возбудителей. Активен в отношении грамположительных микроорганизмов: Streptococcus spp. (групп С F и G кроме устойчивых к эритромицину) Streptococcus pneumoniae Streptococcus pyogenes Streptococcus agalactiae Streptococcus viridans Staphylococcus epidermidis Staphylococcus aureus; грамотрицательных бактерий: Haemophilus influenzae Moraxella catarrhalis Bordetella pertussis Bordetella parapertussis Legionella pneumophila Haemophilus ducreyi Helicobacter pylori Campylobacter jejuni Neisseria gonorrhoeae и Gardnerella vaginalis; некоторых анаэробных микроорганизмов: Bacteroides bivius Clostridium perfringens Peptostreptococcus spp; а также внутриклеточных возбудителей: Chlamydia trachomatis Chlamydia pneumoniae Mycoplasma pneumoniae Mycobacterium avium complex Ureaplasma urealyticum Treponema pallidum Borrelia burgdorferi. Неактивен в отношении грамположительных бактерий устойчивых к эритромицину. Абсорбция - высокая кислотоустойчив липофилен. Биодоступность после однократного приема 05 г - 37% (эффект \"первого прохождения\" через печень) максимальная концентрация в плазме крови после перорального приема 05 г - 04 мг/л период достижения максимальной концентрации в плазме крови - 25-29 ч; в тканях и клетках концентрация в 10-50 раз выше чем в сыворотке крови объем распределения - 311 л/кг. Легко проходит гистогематические барьеры. Хорошо проникает в дыхательные пути мочеполовые органы и ткани в предстательную железу в кожу и мягкие ткани; накапливается в среде с низким pH в лизосомах (что особенно важно для эрадикации внутриклеточно расположенных возбудителей). Транспортируется также фагоцитами полиморфно-ядерными лейкоцитами и макрофагами. Проникает через мембраны клеток и создает высокие концентрации в них. Концентрация в очагах инфекции достоверно выше (на 24-34%) чем в здоровых тканях и коррелирует с выраженностью воспалительного отека. Сохраняется в эффективных концентрациях в течение 5-7 дней после приема последней дозы. Связь с белками плазмы - 7-50% (обратно пропорциональна концентрации в крови). В печени деметилируется образующиеся метаболиты не активны. В метаболизме препарата участвуют изоферменты CYP3A4 CYP3A5 CYP3A7 ингибитором которых он является. Плазменный клиренс - 630 мл/мин. Период полувыведения между 8 и 24 ч после приема -14-20 ч период полувыведения в интервале от 24 до 72 ч - 41 ч. 50% выводится с желчью в неизмененном виде 6% - почками. Прием пищи значимо изменяет фармакокинетику (в зависимости от лекарственной формы): капсулы - максимальная концентрация в плазме крови снижается (на 52%). 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