- Язвенная болезнь желудка и двенадцатиперстной кишки (в фазе обострения и противо- рецидивное лечение) в т.ч. ассоциированные с Helicobacter pylori (в составе комбинированной терапии);
Желатиновые капсулы № 2 с белым корпусом, желтой крышкой. Содержимое капсул - белые или почти белые пеллеты сферической формы.
Фармакотерапевтическая группа
Желез желудка секрецию понижающее средство - протоно¬вого насоса ингибитор
Фармакологические свойства
Фармакодинамика:
Омепразол - противоязвенный препарат ингибитор фермента Н+/К+-аденозинтрифосфат (АТФ)-фазы. Тормозит активность Н+/К+ - аденозинтрифосфат (АТФ) - фазы (Н+/К+- аденозинтрифосфат (АТФ) - фазы она же - "протонный насос" или "протоновый насос") в париетальных клетках желудка тем самым блокирует перенос ионов водорода и заключительную стадию синтеза соляной кислоты в желудке. Омепразол является пролекарством. В кислой среде канальцев париетальных клеток омепразол превращается в активный метаболит сульфенамид который ингибирует мембранную Н+/К+- аденозинтрифосфат (АТФ) - фазу соединяясь с ней за счет дисульфидного мостика. Этим объясняется высокая избирательность действия омепразола именно на париетальные клетки где имеется среда для образования сульфенамида. Биотрансформация омепразола в сульфенамид происходит быстро (через 2-4 мин). Сульфенамид является катионом и не подвергается абсорбции.
Омепразол подавляет базальную и стимулированную любым раздражителем секрецию соляной кислоты на заключительной стадии. Снижает общий объем желудочной секреции и угнетает выделение пепсина. У омепразола обнаружена гастропротекторная активность механизм которой не ясен. Не влияет на продукцию внутреннего фактора Касла и на скорость перехода пищевой массы из желудка в двенадцатиперстную кишку. Омепразол не действует на ацетилхолиновые и гистаминовые рецепторы.
Капсулы Омепразола содержат микрогранулы покрытые оболочкой постепенное высвобождение и начало действия омепразола начинается через 1 час после приема достигает максимума через 2 часа сохраняется в течение 24 часов и более. Ингибирование 50 % максимальной секреции после однократного приема 20 мг препарата продолжается 24 часа.
Однократный прием в сутки обеспечивает быстрое и эффективное угнетение дневной и ночной желудочной секреции достигающее своего максимума через 4 дня лечения. У больных с язвенной болезнью двенадцатиперстной кишки прием 20 мг омепразола поддерживает рН=3 внутри желудка в течение 17 часов. После прекращения приема препарата секреторная активность полностью восстанавливается через 3-5 сут.
Фармакокинетика:
Абсорбция - высокая. Биодоступность 30-40 % (при печеночной недостаточности возрастает практически до 100 %) увеличивается у людей пожилого возраста и у больных с нарушениями функций печени недостаточность почечной функции влияния не оказывает. Время необходимое для достижения максимальной концентрации (ТСmах) - 05-35 часа. Обладая высокой липофильностью легко проникает в париетальные клетки желудка. Связь с белками плазмы - 90-95 % (альбумин и кислый альфа1-гликопротеин).
Период полувыведения (T1/2) - 05-1 час (при печеночной недостаточности - 3 часа) клиренс - 500-600 мл/мин. Практически полностью метаболизируется в печени с участием ферментной системы CYP2C19 с образованием 6 фармакологически Неактивных метаболитов (гидроксиомепразол сульфидные и сульфоновые производные и др.). Является ингибитором изофермента CYP2C19. Выведение почками (70-80 %) и с желчью (20-30 %) в виде метаболитов.
При хронической почечной недостаточности выведение снижается пропорционально снижению клиренса креатина. У пожилых пациентов выведение уменьшается.
Показания к применению
- Язвенная болезнь желудка и двенадцатиперстной кишки (в фазе обострения и противо- рецидивное лечение) в т.ч. ассоциированные с Helicobacter pylori (в составе комбинированной терапии);
Гиперчувствительность детский возраст беременность период лактации.
С осторожностью
Почечная и/или печеночная недостаточность.
Применение при беременности и в период грудного вскармливания
Противопоказан во время беременности и в период лактации.
Способ применения и дозы
Внутрь капсулы обычно принимают утром не разжевывая запивая небольшим количеством воды (непосредственно перед едой).
При обострении язвенной болезни рефлюкс-эзофагите и гастропатии вызванной приемом нестероидных противовоспалительных препаратов - 20 мг 1 раз в сутки. Пациентам с тяжелым течением рефлюкс-эзофагита дозу увеличивают до 40 мг 1 раз в сутки.
Курс лечения при язвенной болезни двенадцатиперстной кишки - 2-4 недели при необходимости - 4-5 недель; при язвенной болезни желудка при рефлюкс-эзофагите при эрозивно-язвенных поражениях желудочно-кишечного тракта (ЖКТ) вызванных приемом нестероидных противовоспалительных препаратов - в течение 4-8 недель.
Уменьшение симптомов заболевания и рубцевание язвы в большинстве случаев происходит в пределах 2 недель. Пациентам у которых не произошло полного рубцевания язвы после двухнедельного курса лечение следует продолжить еще 2 недели.
Больным резистентным к лечению другими противоязвенными лекарственными средствами назначают по 40 мг в сутки. Курс лечения при язвенной болезни двенадцатиперстной кишки - 4 недели при язвенной болезни желудка и рефлюкс-эзофагите - 8 недель.
При синдроме Золлингера - Элиссона - обычно по 60 мг 1 раз в сутки; при необходимости дозу увеличивают до 80-120 мг/сутки (дозу делят на 2 приема).
Для профилактики рецидивов язвенной болезни - 10 мг 1 раз в сутки.
Для эрадикации Helicobacter pylori используют "тройную" терапию (в течение 1 недели: омепразол 20 мг амоксициллин 1 г кларитромицин 500 мг - по 2 раза в сутки; либо омепразол 20 мг кларитромицин 250 мг метронидазол 400 мг - по 2 раза в сутки; либо омепразол 40 мг 1 раз в сутки амоксициллин 500 мг и метронидазол 400 мг - по 3 раза в сутки) или "двойную" терапию (в течение 2 недель: омепразол 20-40 мг и амоксициллин 750 мг по 2 раза в сутки либо омепразол 40 мг - 1 раз в сутки и кларитромицин 500 мг - 3 раза в сутки или амоксициллин 075-15 г - 2 раза в сутки).
В особых ситуациях. При печеночной недостаточности назначают по 10-20 мг 1 раз в сутки (при тяжелой печеночной недостаточности суточная доза не должна превышать 20 мг); при нарушении функции почек и у пожилых пациентов коррекции режима дозирования не требуется.
Побочное действие
Со стороны органов пищеварения: диарея или запоры боль в животе тошнота рвота метеоризм; в редких случаях - повышение активности "печеночных" ферментов нарушения вкуса в отдельных случаях - сухость во рту стоматит у больных с предшествующим тяжелым заболеванием печени - гепатит (в т.ч. с желтухой) нарушение функции печени.
Со стороны нервной системы: у больных с тяжелыми сопутствующими соматическими заболеваниями - головная боль головокружение возбуждение депрессия у больных с предшествующим тяжелым заболеванием печени - энцефалопатия.
Со стороны опорно-двигательного аппарата: в отдельных случаях - артралгия миастения миалгия.
Со стороны системы кроветворения: в отдельных случаях - лейкопения тромбоцитопения агранулоцитоз панцитопения.
Со стороны кожных покровов: редко - кожная сыпь и/или зуд в отдельных случаях фотосенсибилизация мультиформная экссудативная эритема алопеция.
Прочие: редко - нарушения зрения недомогание периферические отеки усиление потоотделения гинекомастия образование желудочных гландулярных кист во время длительного лечения (следствие ингибирования секреции соляной кислоты носит доброкачественный обратимый характер).
Передозировка
Симптомы: спутанность сознания нечеткость зрения сонливость сухость во рту тошнота тахикардия аритмия головная боль.
Специфического антидота не существует. Лечение симптоматическое.
Взаимодействие с другими лекарственными средствами
Может снижать абсорбцию эфиров ампициллина солей железа итраконазола и кетоконазола (омепразол повышает pH желудка).
Являясь ингибиторов цитохрома Р450 может повышать концентрацию и снижать выведение диазепама антикоагулянтов непрямого действия фенитоина (лекарственные средства которые метаболизируются в печени посредством цитохрома CYP2C19) что в некоторых случаях может потребовать уменьшения доз этих лекарственных средств. Может повышать концентрацию кларитромицина в плазме крови.
В тоже время длительное применение омепразола в дозе 20 мг 1 раз в сутки в комбинации с кофеином теофиллином пироксикамом диклофенаком напроксеном метопрололом пропранололом этанолом циклоспорином лидокаином хинидином и эстрадиолом не приводило к изменению их концентрации в плазме.
Усиливает ингибирующее действие на систему кроветворения и других лекарственных средств.
Не отмечено взаимодействия с одновременно принимаемыми антацидами.
Особые указания
Перед началом терапии необходимо исключить наличие злокачественного процесса (особенно при язве желудка) так как лечение маскируя симптоматику может отсрочить постановку правильного диагноза.
Прием одновременно с пищей не влияет на его эффективность.
Форма выпуска
Капсулы 20 мг.
Условия хранения
В сухом защищенном от света месте при температуре не выше 25°С.
Хранить в местах недоступных для детей.
Срок годности
3 года. Не использовать по истечении срока годности указанного на упаковке
Условия отпуска
По рецепту
Производитель
Открытое акционерное общество "Акционерное Курганское общество медицинских препаратов и изделий "Синтез" (ОАО "Синтез"), 640008, Курганская обл., г. Курган, проспект Конституции, д. 7, Россия
Организация, принимающая претензии потребителей
ОАО "Синтез"
Для описания товара использована информация от партнера 36.6
Мобильное приложение «Все аптеки»
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оболочки пеллет: метакриловой кислоты и этилакрилата сополимер (акриловое покрытие L30D)."}},{"type":"paragraph","data":{"text":"Состав капсулы желатиновой: титана диоксид, желатин, краситель хинолиновый желтый (желтый хинолиновый), краситель солнечный закат желтый (закатно-желтый), метилпара- гидроксибензоат (метилгидроксибензоат), пропилпарагидроксибензоат (пропилгидроксибензоат), уксусная кислота."}}]},{"id":5,"name":"Описание","slug":"common_description","body":[{"type":"paragraph","data":{"text":"Желатиновые капсулы № 2 с белым корпусом, желтой крышкой. Содержимое капсул - белые или почти белые пеллеты сферической формы."}}]},{"id":6,"name":"Фармакотерапевтическая группа","slug":"","body":[{"type":"paragraph","data":{"text":"Желез желудка секрецию понижающее средство - протоно¬вого насоса ингибитор"}}]},{"id":7,"name":"Фармакологические свойства","slug":"pharmacologic_effects","body":[{"type":"header","data":{"text":"Фармакодинамика:","level":3}},{"type":"paragraph","data":{"text":"Омепразол - противоязвенный препарат ингибитор фермента Н\u003csup\u003e+\u003c/sup\u003e/К\u003csup\u003e+\u003c/sup\u003e-аденозинтрифосфат (АТФ)-фазы. Тормозит активность Н\u003csup\u003e+\u003c/sup\u003e/К\u003csup\u003e+\u003c/sup\u003e - аденозинтрифосфат (АТФ) - фазы (Н\u003csup\u003e+\u003c/sup\u003e/К\u003csup\u003e+\u003c/sup\u003e- аденозинтрифосфат (АТФ) - фазы она же - \"протонный насос\" или \"протоновый насос\") в париетальных клетках желудка тем самым блокирует перенос ионов водорода и заключительную стадию синтеза соляной кислоты в желудке. Омепразол является пролекарством. В кислой среде канальцев париетальных клеток омепразол превращается в активный метаболит сульфенамид который ингибирует мембранную Н\u003csup\u003e+\u003c/sup\u003e/К\u003csup\u003e+\u003c/sup\u003e- аденозинтрифосфат (АТФ) - фазу соединяясь с ней за счет дисульфидного мостика. Этим объясняется высокая избирательность действия омепразола именно на париетальные клетки где имеется среда для образования сульфенамида. Биотрансформация омепразола в сульфенамид происходит быстро (через 2-4 мин). Сульфенамид является катионом и не подвергается абсорбции."}},{"type":"paragraph","data":{"text":"Омепразол подавляет базальную и стимулированную любым раздражителем секрецию соляной кислоты на заключительной стадии. Снижает общий объем желудочной секреции и угнетает выделение пепсина. У омепразола обнаружена гастропротекторная активность механизм которой не ясен. Не влияет на продукцию внутреннего фактора Касла и на скорость перехода пищевой массы из желудка в двенадцатиперстную кишку. Омепразол не действует на ацетилхолиновые и гистаминовые рецепторы."}},{"type":"paragraph","data":{"text":"Капсулы Омепразола содержат микрогранулы покрытые оболочкой постепенное высвобождение и начало действия омепразола начинается через 1 час после приема достигает максимума через 2 часа сохраняется в течение 24 часов и более. Ингибирование 50 % максимальной секреции после однократного приема 20 мг препарата продолжается 24 часа."}},{"type":"paragraph","data":{"text":"Однократный прием в сутки обеспечивает быстрое и эффективное угнетение дневной и ночной желудочной секреции достигающее своего максимума через 4 дня лечения. У больных с язвенной болезнью двенадцатиперстной кишки прием 20 мг омепразола поддерживает рН=3 внутри желудка в течение 17 часов. После прекращения приема препарата секреторная активность полностью восстанавливается через 3-5 сут."}},{"type":"header","data":{"text":"Фармакокинетика:","level":3}},{"type":"paragraph","data":{"text":"Абсорбция - высокая. Биодоступность 30-40 % (при печеночной недостаточности возрастает практически до 100 %) увеличивается у людей пожилого возраста и у больных с нарушениями функций печени недостаточность почечной функции влияния не оказывает. Время необходимое для достижения максимальной концентрации (ТС\u003csub\u003emах\u003c/sub\u003e) - 05-35 часа. Обладая высокой липофильностью легко проникает в париетальные клетки желудка. Связь с белками плазмы - 90-95 % (альбумин и кислый альфа1-гликопротеин)."}},{"type":"paragraph","data":{"text":"Период полувыведения (T\u003csub\u003e1/2\u003c/sub\u003e) - 05-1 час (при печеночной недостаточности - 3 часа) клиренс - 500-600 мл/мин. Практически полностью метаболизируется в печени с участием ферментной системы CYP\u003csub\u003e2C19\u003c/sub\u003e с образованием 6 фармакологически Неактивных метаболитов (гидроксиомепразол сульфидные и сульфоновые производные и др.). Является ингибитором изофермента CYP\u003csub\u003e2C19\u003c/sub\u003e. Выведение почками (70-80 %) и с желчью (20-30 %) в виде метаболитов."}},{"type":"paragraph","data":{"text":"При хронической почечной недостаточности выведение снижается пропорционально снижению клиренса креатина. У пожилых пациентов выведение уменьшается."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"- Язвенная болезнь желудка и двенадцатиперстной кишки (в фазе обострения и противо- рецидивное лечение) в т.ч. ассоциированные с Helicobacter pylori (в составе комбинированной терапии);"}},{"type":"paragraph","data":{"text":"- Рефлюкс-эзофагит (в т. ч. эрозивный)."}},{"type":"paragraph","data":{"text":"- Гиперсекреторные состояния (синдром Золлингера - Эллисона стрессовые язвы желудочно-кишечного тракта полиэндокринный аденоматоз системный мастоцитоз)."}},{"type":"paragraph","data":{"text":"- Гастропатия вызванная приемом нестероидных противовоспалительных препаратов."}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"paragraph","data":{"text":"Гиперчувствительность детский возраст беременность период лактации."}}]},{"id":10,"name":"С осторожностью","slug":"cautions","body":[{"type":"paragraph","data":{"text":"Почечная и/или печеночная недостаточность."}}]},{"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 лактации."}}]},{"id":12,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Внутрь капсулы обычно принимают утром не разжевывая запивая небольшим количеством воды (непосредственно перед едой)."}},{"type":"paragraph","data":{"text":"При обострении язвенной болезни рефлюкс-эзофагите и гастропатии вызванной приемом нестероидных противовоспалительных препаратов - 20 мг 1 раз в сутки. Пациентам с тяжелым течением рефлюкс-эзофагита дозу увеличивают до 40 мг 1 раз в сутки."}},{"type":"paragraph","data":{"text":"Курс лечения при язвенной болезни двенадцатиперстной кишки - 2-4 недели при необходимости - 4-5 недель; при язвенной болезни желудка при рефлюкс-эзофагите при эрозивно-язвенных поражениях желудочно-кишечного тракта (ЖКТ) вызванных приемом нестероидных противовоспалительных препаратов - в течение 4-8 недель."}},{"type":"paragraph","data":{"text":"Уменьшение симптомов заболевания и рубцевание язвы в большинстве случаев происходит в пределах 2 недель. Пациентам у которых не произошло полного рубцевания язвы после двухнедельного курса лечение следует продолжить еще 2 недели."}},{"type":"paragraph","data":{"text":"Больным резистентным к лечению другими противоязвенными лекарственными средствами назначают по 40 мг в сутки. Курс лечения при язвенной болезни двенадцатиперстной кишки - 4 недели при язвенной болезни желудка и рефлюкс-эзофагите - 8 недель."}},{"type":"paragraph","data":{"text":"При синдроме Золлингера - Элиссона - обычно по 60 мг 1 раз в сутки; при необходимости дозу увеличивают до 80-120 мг/сутки (дозу делят на 2 приема)."}},{"type":"paragraph","data":{"text":"Для профилактики рецидивов язвенной болезни - 10 мг 1 раз в сутки."}},{"type":"paragraph","data":{"text":"Для эрадикации Helicobacter pylori используют \"тройную\" терапию (в течение 1 недели: омепразол 20 мг амоксициллин 1 г кларитромицин 500 мг - по 2 раза в сутки; либо омепразол 20 мг кларитромицин 250 мг метронидазол 400 мг - по 2 раза в сутки; либо омепразол 40 мг 1 раз в сутки амоксициллин 500 мг и метронидазол 400 мг - по 3 раза в сутки) или \"двойную\" терапию (в течение 2 недель: омепразол 20-40 мг и амоксициллин 750 мг по 2 раза в сутки либо омепразол 40 мг - 1 раз в сутки и кларитромицин 500 мг - 3 раза в сутки или амоксициллин 075-15 г - 2 раза в сутки)."}},{"type":"paragraph","data":{"text":"В особых ситуациях. При печеночной недостаточности назначают по 10-20 мг 1 раз в сутки (при тяжелой печеночной недостаточности суточная доза не должна превышать 20 мг); при нарушении функции почек и у пожилых пациентов коррекции режима дозирования не требуется."}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Со стороны органов пищеварения: диарея или запоры боль в животе тошнота рвота метеоризм; в редких случаях - повышение активности \"печеночных\" ферментов нарушения вкуса в отдельных случаях - сухость во рту стоматит у больных с предшествующим тяжелым заболеванием печени - гепатит (в т.ч. с желтухой) нарушение функции печени."}},{"type":"paragraph","data":{"text":"Со стороны нервной системы: у больных с тяжелыми сопутствующими соматическими заболеваниями - головная боль головокружение возбуждение депрессия у больных с предшествующим тяжелым заболеванием печени - энцефалопатия."}},{"type":"paragraph","data":{"text":"Со стороны опорно-двигательного аппарата: в отдельных случаях - артралгия миастения миалгия."}},{"type":"paragraph","data":{"text":"Со стороны системы кроветворения: в отдельных случаях - лейкопения тромбоцитопения агранулоцитоз панцитопения."}},{"type":"paragraph","data":{"text":"Со стороны кожных покровов: редко - кожная сыпь и/или зуд в отдельных случаях фотосенсибилизация мультиформная экссудативная эритема алопеция."}},{"type":"paragraph","data":{"text":"Аллергические реакции: крапивница ангионевротический отек лихорадка бронхоспазм интерстициальный нефрит и анафилактический шок."}},{"type":"paragraph","data":{"text":"Прочие: редко - нарушения зрения недомогание периферические отеки усиление потоотделения гинекомастия образование желудочных гландулярных кист во время длительного лечения (следствие ингибирования секреции соляной кислоты носит доброкачественный обратимый характер)."}}]},{"id":14,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"Симптомы: спутанность сознания нечеткость зрения сонливость сухость во рту тошнота тахикардия аритмия головная боль."}},{"type":"paragraph","data":{"text":"Лечение: симптоматическое. Гемодиализ недостаточно эффективен."}},{"type":"paragraph","data":{"text":"Специфического антидота не существует. Лечение симптоматическое."}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"Может снижать абсорбцию эфиров ампициллина солей железа итраконазола и кетоконазола (омепразол повышает pH желудка)."}},{"type":"paragraph","data":{"text":"Являясь ингибиторов цитохрома Р450 может повышать концентрацию и снижать выведение диазепама антикоагулянтов непрямого действия фенитоина (лекарственные средства которые метаболизируются в печени посредством цитохрома CYP\u003csub\u003e2C19\u003c/sub\u003e) что в некоторых случаях может потребовать уменьшения доз этих лекарственных средств. Может повышать концентрацию кларитромицина в плазме крови."}},{"type":"paragraph","data":{"text":"В тоже время длительное применение омепразола в дозе 20 мг 1 раз в сутки в комбинации с кофеином теофиллином пироксикамом диклофенаком напроксеном метопрололом пропранололом этанолом циклоспорином лидокаином хинидином и эстрадиолом не приводило к изменению их концентрации в плазме."}},{"type":"paragraph","data":{"text":"Усиливает ингибирующее действие на систему кроветворения и других лекарственных средств."}},{"type":"paragraph","data":{"text":"Не отмечено взаимодействия с одновременно принимаемыми антацидами."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"Перед началом терапии необходимо исключить наличие злокачественного процесса (особенно при язве желудка) так как лечение маскируя симптоматику может отсрочить постановку правильного диагноза."}},{"type":"paragraph","data":{"text":"Прием одновременно с пищей не влияет на его эффективность."}}]},{"id":18,"name":"Форма выпуска","slug":"","body":[{"type":"paragraph","data":{"text":"Капсулы 20 мг."}}]},{"id":19,"name":"Условия хранения","slug":"storage","body":[{"type":"paragraph","data":{"text":"В сухом защищенном от света месте при температуре не выше 25°С."}},{"type":"paragraph","data":{"text":"Хранить в местах недоступных для детей."}}]},{"id":20,"name":"Срок годности","slug":"expiry_date","body":[{"type":"paragraph","data":{"text":"3 года. Не использовать по истечении срока годности указанного на упаковке"}}]},{"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":"Открытое акционерное общество \"Акционерное Курганское общество медицинских препаратов и изделий \"Синтез\" (ОАО \"Синтез\"), 640008, Курганская обл., г. Курган, проспект Конституции, д. 7, Россия"}}]},{"id":23,"name":"Организация, принимающая претензии потребителей","body":[{"type":"paragraph","data":{"text":"ОАО \"Синтез\""}}]}],"source":null},"description_toggle":false,"short_description":"Омепразол - противоязвенный препарат ингибитор фермента Н+/К+-аденозинтрифосфат (АТФ)-фазы. Тормозит активность Н+/К+- аденозинтрифосфат (АТФ) - фазы (Н+/К+- аденозинтрифосфат (АТФ) - фазы она же - \"протонный насос\" или \"протоновый насос\") в париетальных клетках желудка тем самым блокирует перенос ионов водорода и заключительную стадию синтеза соляной кислоты в желудке. Омепразол является пролекарством. В кислой среде канальцев париетальных клеток омепразол превращается в активный метаболит сульфенамид который ингибирует мембранную Н+/К+- аденозинтрифосфат (АТФ) - фазу соединяясь с ней за счет дисульфидного мостика. Этим объясняется высокая избирательность действия омепразола именно на париетальные клетки где имеется среда для образования сульфенамида. Биотрансформация омепразола в сульфенамид происходит быстро (через 2-4 мин). Сульфенамид является катионом и не подвергается абсорбции. Омепразол подавляет базальную и стимулированную любым раздражителем секрецию соляной кислоты на заключительной стадии. Снижает общий объем желудочной секреции и угнетает выделение пепсина. У омепразола обнаружена гастропротекторная активность механизм которой не ясен. Не влияет на продукцию внутреннего фактора Касла и на скорость перехода пищевой массы из желудка в двенадцатиперстную кишку. Омепразол не действует на ацетилхолиновые и гистаминовые рецепторы. Капсулы Омепразола содержат микрогранулы покрытые оболочкой постепенное высвобождение и начало действия омепразола начинается через 1 час после приема достигает максимума через 2 часа сохраняется в течение 24 часов и более. Ингибирование 50 % максимальной секреции после однократного приема 20 мг препарата продолжается 24 часа. Однократный прием в сутки обеспечивает быстрое и эффективное угнетение дневной и ночной желудочной секреции достигающее своего максимума через 4 дня лечения. У больных с язвенной болезнью двенадцатиперстной кишки прием 20 мг омепразола поддерживает рН=3 внутри желудка в течение 17 часов. После прекращения приема препарата секреторная активность полностью восстанавливается через 3-5 сут. Абсорбция - высокая. Биодоступность 30-40 % (при печеночной недостаточности возрастает практически до 100 %) увеличивается у людей пожилого возраста и у больных с нарушениями функций печени недостаточность почечной функции влияния не оказывает. Время необходимое для достижения максимальной концентрации (ТСmах) - 05-35 часа. Обладая высокой липофильностью легко проникает в париетальные клетки желудка. Связь с белками плазмы - 90-95 % (альбумин и кислый альфа1-гликопротеин). Период полувыведения (T1/2) - 05-1 час (при печеночной недостаточности - 3 часа) клиренс - 500-600 мл/мин. Практически полностью метаболизируется в печени с участием ферментной системы CYP2C19с образованием 6 фармакологически Неактивных метаболитов (гидроксиомепразол сульфидные и сульфоновые производные и др.). Является ингибитором изофермента CYP2C19. Выведение почками (70-80 %) и с желчью (20-30 %) в виде метаболитов. При хронической почечной недостаточности выведение снижается пропорционально снижению клиренса креатина. 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