Ондансетрон является селективным антагонистом рецепторов 5НТз (серотонина). Лекарственные средства для цитостатической химиотерапии и радиотерапия могут вызвать повышение уровня серотонина который путем активации вагусных афферентных волокон содержащих рецепторы 5- НТз вызывает рвотный рефлекс. Ондансетрон тормозит появление рвотного рефлекса путем блокады рецепторов 5-НТз на уровне нейронов как центральной так и периферической нервной системы.
По-видимому на этом механизме действия основано предупреждение и лечение послеоперационной и вызванной цитостатической химио- и радио-терапией рвоты и тошноты.
Фармакокинетика:
При внутримышечном введении пиковая концентрация в плазме достигается в течение 10 минут. Препарат подвергается метаболизму в печени. Связывание с белками плазмы составляет 70-76%. С мочой в неизмененном виде выделяется менее 5% препарата.
Период полувыведения составляет около 3 ч. у пожилых больных может достигать 5 часов а при выраженной печеночной недостаточности - 15-20 часов. При поражении почек (почечный клиренс меньше 15 мл/мин) период полувыведения увеличивается на 4-5 часов но это увеличение не имеет клинического значения.
Показания к применению
Предупреждение и устранение тошноты и рвоты обусловленных цитостатической химиотерапией и радиотерапией а также послеоперационной тошноты и рвоты.
Противопоказания
- Повышенная чувствительность к ондансетрону или любому другому компоненту препарата
- Беременность и лактация.
- Детский возраст до 2-х лет (отсутствие достаточного опыта применения).
Применение при беременности и в период грудного вскармливания
противопоказано
Способ применения и дозы
Вводят препарат внутривенно или внутримышечно.
Цитостатическая терапия
Выбор режима дозирования определяется эметогенностью противоопухолевой терапии.
Для взрослых суточная доза как правило составляет 8-32 мг рекомендуются следующие режимы При умеренной эметогенной химиотерапии или радиотерапии:
- 8 мг внутривенно струйно медленно или внутримышечно непосредственно перед началом терапии;
При высокоэметогенной химиотерапии:
- 8 мг внутривенно струйно медленно непосредственно перед началом химиотерапии а затем еще две внутривенные инъекции по 8 мг каждая из которых осуществляется через 2-4 часа;
непрерывная 24-часовая инфузия препарата в дозе 24 мг со скоростью 1 мг/час;
- 16-32 мг разведенные в 50-100 мл соответствующего инфузионного раствора в виде 15- минутной инфузии непосредственно перед началом химиотерапии.
Эффективность препарата может быть увеличена путем разового внутривенного введения глюкокортикоида (например 20 мг дексаметазона) до начала химиотерапии.
Дети
Детям старше 2-х лет препарат назначается в дозе 5 мг/м2 поверхности тела внутривенно непосредственно перед началом химиотерапии.
Предупреждение послеоперационной тошноты и рвоты
Взрослым вводят разовую дозу 4 мг внутримышечно или внутривенно струйно медленно в начале наркоза.
Для купирования возникшей тошноты и рвоты рекомендуется внутримышечное или медленное внутривенное введение 4 мг препарата.
Внутримышечно в один и тот же участок тела ондансетрон может быть введен в дозе не превышающей 4 мг!
Детям для предотвращения послеоперационной тошноты и рвоты ондансетрон применяется парентерально в разовой дозе 01 мг/кг (максимально до 4 мг) в виде медленной внутривенной инъекции до или после анестезии.
Для лечения развившейся послеоперационной тошноты и рвоты у детей рекомендуется медленное внутривенное введение разовой дозы препарата 01 мг/кг (максимально до 4 мг).
В отношении предотвращения и лечения послеоперационной тошноты и рвоты у детей в возрасте до 2 лет достаточного опыта нет.
Пожилые больные
Изменения дозировки не требуется.
Больные с поражениями почек и печени
При поражении почек изменять обычную суточную дозу и частоту введения препарата не требуется.
При поражении печени в значительной степени уменьшается клиренс ондансетрона причем увеличивается время полувыведения его из плазмы поэтому необходимо снизить дозу до 8 мг в день.
Для разведения инъекционного раствора могут применяться следующие растворы:
09% раствор натрия хлорида
5% раствор декстрозы раствор Рингера
03% раствор калия хлорида и 09% раствор натрия хлорида
Со стороны пищеварительной системы: икота сухость во рту диарея запор иногда бессимптомное преходящее повышение уровня аминотрансфераз в сыворотке крови.
Со стороны сердечнососудистой системы: боли в грудной клетке в ряде случаев с депрессией сегмента ST аритмии брадикардия снижение артериального давления.
Со стороны нервной системы: головная боль головокружение спонтанные двигательные расстройства и судороги.
Местные реакции: боль жжение и покраснение в месте введения
Прочие: прилив крови к лицу чувство жара временное нарушение остроты зрения гипокалиемия
Передозировка
В случаях предполагаемой передозировки показана симптоматическая терапия.
Специфический антидот не известен.
Взаимодействие с другими лекарственными средствами
Так как ондансетрон метаболизируется ферментной системой (цитохром Р450) печени требуется осторожность при совместном применении:
- с ферментативными индукторами Р450 (CYP2D6 и CYP3A) (барбитураты карбамазепин каризопродол глютетимид гризеофульвин динитроген оксид папаверин фенилбутазон фенитоин (вероятно и другие гидантоины) рифампицин толбутамид);
У пациентов у которых ранее при применении других селективных антагонистов 5НТз- рецепторов наблюдались реакции повышенной чувствительности при применении ондансетрона также могут развиться аналогичные реакции.
Так как ондансетрон может вызывать запор больные с признаками непроходимости кишечника после применения препарата требуют регулярного наблюдения.
Инфузионный раствор должен быть приготовлен непосредственно перед использованием. В случае необходимости готовый инфузионный раствор может храниться до использования максимально в течение 24 часов при температуре 2-8°С.
Во время проведения инфузии защиты от света не требуется; разведенный инъекционный раствор сохраняет свою стабильность как минимум в течение 24 часов при естественном свете или нормальном освещении.
Влияние на способность управлять автомобилем и движущимися механизмами
Сведения отсутствуют.
Форма выпуска
Раствор для внутривенного и внутримышечного введения 2 мг/мл. По 2 мл или 4 мл в ампулы нейтрального стекла.
Условия хранения
При температуре от 15°Сдо25°С в защищенном от света месте.
Хранить в недоступном для детей месте.
Срок годности
3 года
Не использовать после истечения срока годности указанного на упаковке.
Условия отпуска
По рецепту
Производитель
Акционерное общество "Новосибхимфарм" (АО "Новосибхимфарм"), 630028, г. Новосибирск, ул. Декабристов, д. 275, Россия
Организация, принимающая претензии потребителей
АО "Новосибхимфарм"
Для описания товара использована информация от партнера 36.6
Мобильное приложение «Все аптеки»
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селективным антагонистом рецепторов 5НТз (серотонина). Лекарственные средства для цитостатической химиотерапии и радиотерапия могут вызвать повышение уровня серотонина который путем активации вагусных афферентных волокон содержащих рецепторы 5- НТз вызывает рвотный рефлекс. Ондансетрон тормозит появление рвотного рефлекса путем блокады рецепторов 5-НТз на уровне нейронов как центральной так и периферической нервной системы."}},{"type":"paragraph","data":{"text":"По-видимому на этом механизме действия основано предупреждение и лечение послеоперационной и вызванной цитостатической химио- и радио-терапией рвоты и тошноты."}},{"type":"header","data":{"text":"Фармакокинетика:","level":3}},{"type":"paragraph","data":{"text":"При внутримышечном введении пиковая концентрация в плазме достигается в течение 10 минут. Препарат подвергается метаболизму в печени. Связывание с белками плазмы составляет 70-76%. С мочой в неизмененном виде выделяется менее 5% препарата."}},{"type":"paragraph","data":{"text":"Период полувыведения составляет около 3 ч. у пожилых больных может достигать 5 часов а при выраженной печеночной недостаточности - 15-20 часов. При поражении почек (почечный клиренс меньше 15 мл/мин) период полувыведения увеличивается на 4-5 часов но это увеличение не имеет клинического значения."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"Предупреждение и устранение тошноты и рвоты обусловленных цитостатической химиотерапией и радиотерапией а также послеоперационной тошноты и рвоты."}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"paragraph","data":{"text":"- Повышенная чувствительность к ондансетрону или любому другому компоненту препарата"}},{"type":"paragraph","data":{"text":"- Беременность и лактация."}},{"type":"paragraph","data":{"text":"- Детский возраст до 2-х лет (отсутствие достаточного опыта применения)."}}]},{"id":11,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","body":[{"type":"paragraph","data":{"text":"противопоказано"}}]},{"id":12,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Вводят препарат внутривенно или внутримышечно."}},{"type":"paragraph","data":{"text":"Цитостатическая терапия"}},{"type":"paragraph","data":{"text":"Выбор режима дозирования определяется эметогенностью противоопухолевой терапии."}},{"type":"paragraph","data":{"text":"Для взрослых суточная доза как правило составляет 8-32 мг рекомендуются следующие режимы При умеренной эметогенной химиотерапии или радиотерапии:"}},{"type":"paragraph","data":{"text":"- 8 мг внутривенно струйно медленно или внутримышечно непосредственно перед началом терапии;"}},{"type":"paragraph","data":{"text":"При высокоэметогенной химиотерапии:"}},{"type":"paragraph","data":{"text":"- 8 мг внутривенно струйно медленно непосредственно перед началом химиотерапии а затем еще две внутривенные инъекции по 8 мг каждая из которых осуществляется через 2-4 часа;"}},{"type":"paragraph","data":{"text":"непрерывная 24-часовая инфузия препарата в дозе 24 мг со скоростью 1 мг/час;"}},{"type":"paragraph","data":{"text":"- 16-32 мг разведенные в 50-100 мл соответствующего инфузионного раствора в виде 15- минутной инфузии непосредственно перед началом химиотерапии."}},{"type":"paragraph","data":{"text":"Эффективность препарата может быть увеличена путем разового внутривенного введения глюкокортикоида (например 20 мг дексаметазона) до начала химиотерапии."}},{"type":"paragraph","data":{"text":"Дети"}},{"type":"paragraph","data":{"text":"Детям старше 2-х лет препарат назначается в дозе 5 мг/м\u003csup\u003e2\u003c/sup\u003e поверхности тела внутривенно непосредственно перед началом химиотерапии."}},{"type":"paragraph","data":{"text":"Предупреждение послеоперационной тошноты и рвоты"}},{"type":"paragraph","data":{"text":"Взрослым вводят разовую дозу 4 мг внутримышечно или внутривенно струйно медленно в начале наркоза."}},{"type":"paragraph","data":{"text":"Для купирования возникшей тошноты и рвоты рекомендуется внутримышечное или медленное внутривенное введение 4 мг препарата."}},{"type":"paragraph","data":{"text":"Внутримышечно в один и тот же участок тела ондансетрон может быть введен в дозе не превышающей 4 мг!"}},{"type":"paragraph","data":{"text":"Детям для предотвращения послеоперационной тошноты и рвоты ондансетрон применяется парентерально в разовой дозе 01 мг/кг (максимально до 4 мг) в виде медленной внутривенной инъекции до или после анестезии."}},{"type":"paragraph","data":{"text":"Для лечения развившейся послеоперационной тошноты и рвоты у детей рекомендуется медленное внутривенное введение разовой дозы препарата 01 мг/кг (максимально до 4 мг)."}},{"type":"paragraph","data":{"text":"В отношении предотвращения и лечения послеоперационной тошноты и рвоты у детей в возрасте до 2 лет достаточного опыта нет."}},{"type":"paragraph","data":{"text":"Пожилые больные"}},{"type":"paragraph","data":{"text":"Изменения дозировки не требуется."}},{"type":"paragraph","data":{"text":"Больные с поражениями почек и печени"}},{"type":"paragraph","data":{"text":"При поражении почек изменять обычную суточную дозу и частоту введения препарата не требуется."}},{"type":"paragraph","data":{"text":"При поражении печени в значительной степени уменьшается клиренс ондансетрона причем увеличивается время полувыведения его из плазмы поэтому необходимо снизить дозу до 8 мг в день."}},{"type":"paragraph","data":{"text":"Для разведения инъекционного раствора могут применяться следующие растворы:"}},{"type":"paragraph","data":{"text":"09% раствор натрия хлорида"}},{"type":"paragraph","data":{"text":"5% раствор декстрозы раствор Рингера"}},{"type":"paragraph","data":{"text":"03% раствор калия хлорида и 09% раствор натрия хлорида"}},{"type":"paragraph","data":{"text":"03% раствор калия хлорида и 5% раствор декстрозы."}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Аллергические реакции: крапивница бронхоспазм ларингоспазм ангионевротический отек анафилаксия."}},{"type":"paragraph","data":{"text":"Со стороны пищеварительной системы: икота сухость во рту диарея запор иногда бессимптомное преходящее повышение уровня аминотрансфераз в сыворотке крови."}},{"type":"paragraph","data":{"text":"Со стороны сердечнососудистой системы: боли в грудной клетке в ряде случаев с депрессией сегмента ST аритмии брадикардия снижение артериального давления."}},{"type":"paragraph","data":{"text":"Со стороны нервной системы: головная боль головокружение спонтанные двигательные расстройства и судороги."}},{"type":"paragraph","data":{"text":"Местные реакции: боль жжение и покраснение в месте введения"}},{"type":"paragraph","data":{"text":"Прочие: прилив крови к лицу чувство жара временное нарушение остроты зрения гипокалиемия"}}]},{"id":14,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"В случаях предполагаемой передозировки показана симптоматическая терапия."}},{"type":"paragraph","data":{"text":"Специфический антидот не известен."}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"Так как ондансетрон метаболизируется ферментной системой (цитохром Р450) печени требуется осторожность при совместном применении:"}},{"type":"paragraph","data":{"text":"- с ферментативными индукторами Р450 (CYP2D6 и CYP3A) (барбитураты карбамазепин каризопродол глютетимид гризеофульвин динитроген оксид папаверин фенилбутазон фенитоин (вероятно и другие гидантоины) рифампицин толбутамид);"}},{"type":"paragraph","data":{"text":"- с ингибиторами ферментов Р450 (CYP2D6 и CYP3A) (аллопуринол макролидные антибиотики антидепрессанты - ингибиторы МАО хлорамфеникол циметидин пероральные контрацептивы содержащие эстрогены дилтиазем дисульфирам вальпроевая кислота вальпроат натрия эритромицин флуконазол фторхинолоны изониазид кетоконазол ловастатин метронидазол омепразол пропранолол хинидин хинин верапамил)."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"У пациентов у которых ранее при применении других селективных антагонистов 5НТз- рецепторов наблюдались реакции повышенной чувствительности при применении ондансетрона также могут развиться аналогичные реакции."}},{"type":"paragraph","data":{"text":"Так как ондансетрон может вызывать запор больные с признаками непроходимости кишечника после применения препарата требуют регулярного наблюдения."}},{"type":"paragraph","data":{"text":"Инфузионный раствор должен быть приготовлен непосредственно перед использованием. В случае необходимости готовый инфузионный раствор может храниться до использования максимально в течение 24 часов при температуре 2-8°С."}},{"type":"paragraph","data":{"text":"Во время проведения инфузии защиты от света не требуется; разведенный инъекционный раствор сохраняет свою стабильность как минимум в течение 24 часов при естественном свете или нормальном освещении."}}]},{"id":17,"name":"Влияние на способность управлять автомобилем и движущимися механизмами","slug":"","body":[{"type":"paragraph","data":{"text":"Сведения отсутствуют."}}]},{"id":18,"name":"Форма выпуска","slug":"","body":[{"type":"paragraph","data":{"text":"Раствор для внутривенного и внутримышечного введения 2 мг/мл. По 2 мл или 4 мл в ампулы нейтрального стекла."}}]},{"id":19,"name":"Условия хранения","slug":"storage","body":[{"type":"paragraph","data":{"text":"При температуре от 15°Сдо25°С в защищенном от света месте."}},{"type":"paragraph","data":{"text":"Хранить в недоступном для детей месте."}}]},{"id":20,"name":"Срок годности","slug":"expiry_date","body":[{"type":"paragraph","data":{"text":"3 года"}},{"type":"paragraph","data":{"text":"Не использовать после истечения 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":"Акционерное общество \"Новосибхимфарм\" (АО \"Новосибхимфарм\"), 630028, г. Новосибирск, ул. Декабристов, д. 275, Россия"}}]},{"id":23,"name":"Организация, принимающая претензии потребителей","body":[{"type":"paragraph","data":{"text":"АО \"Новосибхимфарм\""}}]}],"source":null},"description_toggle":false,"short_description":"Ондансетрон является селективным антагонистом рецепторов 5НТз (серотонина). Лекарственные средства для цитостатической химиотерапии и радиотерапия могут вызвать повышение уровня серотонина который путем активации вагусных афферентных волокон содержащих рецепторы 5- НТз вызывает рвотный рефлекс. Ондансетрон тормозит появление рвотного рефлекса путем блокады рецепторов 5-НТз на уровне нейронов как центральной так и периферической нервной системы. По-видимому на этом механизме действия основано предупреждение и лечение послеоперационной и вызванной цитостатической химио- и радио-терапией рвоты и тошноты. При внутримышечном введении пиковая концентрация в плазме достигается в течение 10 минут. Препарат подвергается метаболизму в печени. 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