Иресса обладает противоопухолевой активностью благодаря угне... Инструкция
Показания к применению
местно-распространенный или метастатический немелкоклеточный рак легкого с наличием активирующих мутаций тирозинкиназного домена рецептора эпидермального фактора роста в первой линии терапии; - местно-распространенный или метастатический немелкоклеточный рак легкого, рефрактерный к режимам химиотерапии, содержащим производные платины.
Противопоказания
Беременность; период лактации; детский и подростковый возраст (безопасность и эффективность у данной группы пациентов не оценена); повышенная чувствительность к гефитинибу или другим компонентам препарата.
В 100 г крема содержится изоконазола нитрата 1 г Вспомогательные вещества: полисорбат 60 - 3.5 г, сорбитана стеарат - 1 г, цетилстеариловый спирт (цетиловый спирт 60%, стеариловый спирт 40%) - 5 г, парафин жидкий - 10 г, вазелин белый - 10 г, вода очищенная - 69.5 г.
Фармакологические свойства
Иресса обладает противоопухолевой активностью благодаря угнетению тирозинкиназы – рецепторов фактора, стимулирующего рост эпидермиса, характерного для большинства опухолей больших размеров. Действие лекарственного средства направлено на замедление роста опухоли, препятствие образованию и распространению метастазов, замедление ангиогенеза и ускорение апоптоза сформированного новообразования. Препятствуя росту опухоли, Иресса также усиливает эффективность препаратов лучевой, гормональной и химиотерапии.
Показания к применению
местно-распространенный или метастатический немелкоклеточный рак легкого с наличием активирующих мутаций тирозинкиназного домена рецептора эпидермального фактора роста в первой линии терапии; - местно-распространенный или метастатический немелкоклеточный рак легкого, рефрактерный к режимам химиотерапии, содержащим производные платины.
Противопоказания
Беременность; период лактации; детский и подростковый возраст (безопасность и эффективность у данной группы пациентов не оценена); повышенная чувствительность к гефитинибу или другим компонентам препарата.
Применение при беременности и в период грудного вскармливания
Применение препарата Иресса противопоказано при беременности и в период лактации. Мужчинам и женщинам детородного возраста в период приема Ирессы и, как минимум, в течение 3 месяцев после лечения следует использовать надежные методы контрацепции.
Способ применения и дозы
Иресса предназначена для внутреннего употребления. Таблетки следует пить в одно и то же время, независимо от употребления пищи. Иресса назначают по 1 таблетке (250 мг) 1 р./сутки. Если очередной прием медикамента пропущен, его нужно провести не позже 12 часов до следующего приема. Запрещено принимать 2 таблетки за один прием. Если пациент не в состоянии проглотить таблетку целиком обычным способом, ее растворяют в 100 мл питьевой воды без газа, выпивают или вводят через зонд. Для получения полной дозы, выпив содержимое стакана, в него повторно, омыв стенки, наливают воду и выпивают. У пациентов с интерстициальной пневмонией, аллергическими реакциями, выраженной диареей и прочими побочными проявлениями на фоне лечения, допускается перерыв в употреблении Иресса до 2-х недель. Дальнейшее лечение проводят по стандартной схеме.
Побочное действие
Наиболее распространенными побочными эффектами, наблюдаемыми более чем в 20% случаев, являлись диарея, кожная и угревая сыпь, зуд, сухость кожи. Обычно неблагоприятные реакции проявляются в течение первого месяца применения препарата и, как правило, обратимы. Приблизительно у 10% пациентов отмечались серьезные нежелательные реакции (3-4 степень тяжести согласно общим критериям токсичности). Однако только у 3% пациентов терапия была прекращена вследствие побочных реакций. Наблюдавшиеся нежелательные реакции представлены ниже. Определение частоты побочных реакций: очень часто (≥10%); часто (≥1% - <10%); нечасто (≥0.1% - <1%); редко (≥0.01% - < 0.1%). Со стороны свертывающей системы крови: часто - гематурия и носовое кровотечение; нечасто - гипокоагуляция и/или повышение частоты кровотечений на фоне приема варфарина. Со стороны пищеварительной системы: очень часто - диарея (в отдельных случаях - выраженная), тошнота (в основном, слабой степени выраженности), рвота (в основном, слабой или умеренной степени выраженности), стоматит (в основном, слабой степени выраженности), анорексия (слабой или умеренной степени выраженности), повышение активности АЛТ (в основном, слабой или умеренной степени выраженности); часто - дегидратация (вследствие диареи, тошноты, рвоты и анорексии), сухость во рту (в основном, слабой степени выраженности), повышение активности ACT (в основном, слабой или умеренной степени выраженности), повышение уровня билирубина (в основном, слабой или умеренной степени выраженности); нечасто - панкреатит, гепатит (сообщалось об единичных случаях развития печеночной недостаточности, в некоторых случаях с летальным исходом). Со стороны органа зрения: часто - конъюнктивит, блефарит, ксерофтальмия (в основном, слабой степени выраженности); нечасто - обратимая эрозия роговицы, нарушение роста ресниц. Со стороны дыхательной системы: часто - интерстициальная пневмония (3-4 степени токсичности, вплоть до летального исхода). Со стороны мочевыделительной системы: часто - бессимптомное повышение уровня креатинина в крови, протеинурия. Дерматологические реакции: очень часто - сыпь (пустулезная), зуд, сухость кожи, включая образование трещин на фоне эритемы; часто - изменения ногтей, алопеция; редко - буллезные изменения кожи, включая токсический эпидермальный некролиз, синдром Стивенса-Джонсона и многоформная экссудативная эритема, кожный васкулит. Аллергические реакции: нечасто – ангионевротический отек, крапивница. Прочие: очень часто - астения (преимущественно слабой степени выраженности), часто - повышение температуры тела.
Передозировка
Симптомы: увеличение частоты и тяжести некоторых побочных реакций, главным образом, диареи и кожной сыпи. Лечение: проводят симптоматическую терапию. Антидот не известен.
Особые указания
При решении вопроса о назначении препарата Иресса в первой линии терапии местно-распространенного или метастатического немелкоклеточного рака легкого рекомендуется определение мутации EGFR (рецептора эпидермального фактора роста) в опухолевой ткани у всех больных. Для определения мутаций важно, чтобы была выбрана валидированная и надежная методика, позволяющая минимизировать возможные как ложноотрицательные, так и ложноположительные результаты. В первой линии терапии Иресса не может быть применена вместо химиотерапии у больных с отсутствием мутации EGFR . Иногда у пациентов, принимающих препарат Иресса, отмечалось интерстициальное поражение легких, в некоторых случаях с летальным исходом. При нарастании таких симптомов как одышка, кашель, лихорадка применение препарата должно быть прекращено и незамедлительно проведено обследование. Если у пациента подтверждается наличие интерстициального легочного заболевания, прием препарата Иресса прекращают и пациенту назначается соответствующее лечение. Наиболее часто развитие интерстициальных поражений легких наблюдалось в Японии (приблизительно в 2% случаев у 27000 пациентов, принимающих препарат Иресса) по сравнению с другими странами (в 0.3% случаев среди 39000 пациентов). Среди факторов, повышающих риск развития интерстициального поражения легких были отмечены: курение, тяжелое общее состояние (PS > 2), нормальная легочная ткань по данным компьютерной томографии < 50%, продолжительность болезни (немелкоклеточный рак легкого) < 6 месяцев, интерстициальная пневмония в анамнезе, пожилой возраст ( > 55 лет), сопутствующие сердечно-сосудистые заболевания. На фоне приема препарата Иресса было отмечено бессимптомное повышение активности печеночных трансаминаз и уровня билирубина, нечасто развивался гепатит. Сообщалось об единичных случаях развития печеночной недостаточности, в некоторых случаях с летальным исходом. В связи с чем рекомендуется периодически оценивать печеночную функцию. При выраженном повышении активности трансаминаз и уровня билирубина прием препарата должен быть прекращен. В клинических исследованиях препарата Иресса были отмечены сердечно-сосудистые осложнения. Связь с приемом препарата Иресса не была установлена. У пациентов, принимающих варфарин, необходимо регулярно контролировать протромбиновое время. При появлении любых симптомов со стороны органов зрения или при развитии тяжелой или продолжительной диареи, тошноты, рвоты или анорексии пациент должен незамедлительно обратиться к врачу. При применении препарата Иресса в комбинации с лучевой терапией в качестве терапии первой линии у детей с глиомой ствола мозга или нерадикально удаленной глиомой супратенториальной локализации сообщалось о 4 случаях (один летальный) кровоизлияний в головной мозг. Еще один случай кровоизлияния в головной мозг отмечен у ребенка с эпендимомой при монотерапии препаратом Иресса. У взрослых пациентов с немелкоклеточным раком легкого при лечении препаратом Иресса подобные побочные явления не зафиксированы ни в одном случае. Сообщалось об единичных случаях развития перфорации органов ЖКТ у пациентов с такими факторами риска, как одновременный прием стероидов, НПВП, язвенная болезнь в анамнезе, пожилой возраст, курение, наличие метастазов в толстую кишку в месте перфорации. Однако, причинно-следственной связи между перечисленными явлениями и приемом препарата Иресса не установлено. Пациентам с редкими наследственными заболеваниями, такими как непереносимость лактозы, дефицит лактазы или синдромом мальабсорбции препарат Иресса следует назначать с осторожностью, в связи с наличием в составе лактозы. Влияние на способность управлять транспортными средствами и другими механизмами, требующими повышенной концентрации внимания Поскольку во время проведения терапии препаратом Иресса могут развиться такие побочные действия как астения, тошнота и рвота, необходимо соблюдать осторожность при вождении автомобиля и занятиях другими потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций.
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г крема содержится изоконазола нитрата 1 г Вспомогательные вещества: полисорбат 60 - 3.5 г, сорбитана стеарат - 1 г, цетилстеариловый спирт (цетиловый спирт 60%, стеариловый спирт 40%) - 5 г, парафин жидкий - 10 г, вазелин белый - 10 г, вода очищенная - 69.5 г."}}]},{"id":2,"name":"Фармакологические свойства","slug":"pharmacologic_effects","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Иресса обладает противоопухолевой активностью благодаря угнетению тирозинкиназы – рецепторов фактора, стимулирующего рост эпидермиса, характерного для большинства опухолей больших размеров. Действие лекарственного средства направлено на замедление роста опухоли, препятствие образованию и распространению метастазов, замедление ангиогенеза и ускорение апоптоза сформированного новообразования. Препятствуя росту опухоли, Иресса также усиливает эффективность препаратов лучевой, гормональной и химиотерапии."}}]},{"id":3,"name":"Показания к применению","slug":"indications","displayInMenu":true,"body":[{"type":"list","data":{"style":"unordered","items":["местно-распространенный или метастатический немелкоклеточный рак легкого с наличием активирующих мутаций тирозинкиназного домена рецептора эпидермального фактора роста в первой линии терапии; - местно-распространенный или метастатический немелкоклеточный рак легкого, рефрактерный к режимам химиотерапии, содержащим производные платины."]}}]},{"id":4,"name":"Противопоказания","slug":"contraindications","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Беременность; период лактации; детский и подростковый возраст (безопасность и эффективность у данной группы пациентов не оценена); повышенная чувствительность к гефитинибу или другим компонентам препарата."}}]},{"id":5,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Применение препарата Иресса противопоказано при беременности и в период лактации. Мужчинам и женщинам детородного возраста в период приема Ирессы и, как минимум, в течение 3 месяцев после лечения следует использовать надежные методы контрацепции."}}]},{"id":6,"name":"Способ применения и дозы","slug":"dosage","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Иресса предназначена для внутреннего употребления. Таблетки следует пить в одно и то же время, независимо от употребления пищи. Иресса назначают по 1 таблетке (250 мг) 1 р./сутки. Если очередной прием медикамента пропущен, его нужно провести не позже 12 часов до следующего приема. Запрещено принимать 2 таблетки за один прием. Если пациент не в состоянии проглотить таблетку целиком обычным способом, ее растворяют в 100 мл питьевой воды без газа, выпивают или вводят через зонд. Для получения полной дозы, выпив содержимое стакана, в него повторно, омыв стенки, наливают воду и выпивают. У пациентов с интерстициальной пневмонией, аллергическими реакциями, выраженной диареей и прочими побочными проявлениями на фоне лечения, допускается перерыв в употреблении Иресса до 2-х недель. Дальнейшее лечение проводят по стандартной схеме."}}]},{"id":7,"name":"Побочное действие","slug":"side_effects","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Наиболее распространенными побочными эффектами, наблюдаемыми более чем в 20% случаев, являлись диарея, кожная и угревая сыпь, зуд, сухость кожи. Обычно неблагоприятные реакции проявляются в течение первого месяца применения препарата и, как правило, обратимы. Приблизительно у 10% пациентов отмечались серьезные нежелательные реакции (3-4 степень тяжести согласно общим критериям токсичности). Однако только у 3% пациентов терапия была прекращена вследствие побочных реакций. Наблюдавшиеся нежелательные реакции представлены ниже. Определение частоты побочных реакций: очень часто (≥10%); часто (≥1% - \u003c10%); нечасто (≥0.1% - \u003c1%); редко (≥0.01% - \u003c 0.1%). Со стороны свертывающей системы крови: часто - гематурия и носовое кровотечение; нечасто - гипокоагуляция и/или повышение частоты кровотечений на фоне приема варфарина. Со стороны пищеварительной системы: очень часто - диарея (в отдельных случаях - выраженная), тошнота (в основном, слабой степени выраженности), рвота (в основном, слабой или умеренной степени выраженности), стоматит (в основном, слабой степени выраженности), анорексия (слабой или умеренной степени выраженности), повышение активности АЛТ (в основном, слабой или умеренной степени выраженности); часто - дегидратация (вследствие диареи, тошноты, рвоты и анорексии), сухость во рту (в основном, слабой степени выраженности), повышение активности ACT (в основном, слабой или умеренной степени выраженности), повышение уровня билирубина (в основном, слабой или умеренной степени выраженности); нечасто - панкреатит, гепатит (сообщалось об единичных случаях развития печеночной недостаточности, в некоторых случаях с летальным исходом). Со стороны органа зрения: часто - конъюнктивит, блефарит, ксерофтальмия (в основном, слабой степени выраженности); нечасто - обратимая эрозия роговицы, нарушение роста ресниц. Со стороны дыхательной системы: часто - интерстициальная пневмония (3-4 степени токсичности, вплоть до летального исхода). Со стороны мочевыделительной системы: часто - бессимптомное повышение уровня креатинина в крови, протеинурия. Дерматологические реакции: очень часто - сыпь (пустулезная), зуд, сухость кожи, включая образование трещин на фоне эритемы; часто - изменения ногтей, алопеция; редко - буллезные изменения кожи, включая токсический эпидермальный некролиз, синдром Стивенса-Джонсона и многоформная экссудативная эритема, кожный васкулит. Аллергические реакции: нечасто – ангионевротический отек, крапивница. Прочие: очень часто - астения (преимущественно слабой степени выраженности), часто - повышение температуры тела."}}]},{"id":8,"name":"Передозировка","slug":"overdose","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Симптомы: увеличение частоты и тяжести некоторых побочных реакций, главным образом, диареи и кожной сыпи. Лечение: проводят симптоматическую терапию. Антидот не известен."}}]},{"id":9,"name":"Особые указания","slug":"cautions","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"При решении вопроса о назначении препарата Иресса в первой линии терапии местно-распространенного или метастатического немелкоклеточного рака легкого рекомендуется определение мутации EGFR (рецептора эпидермального фактора роста) в опухолевой ткани у всех больных. Для определения мутаций важно, чтобы была выбрана валидированная и надежная методика, позволяющая минимизировать возможные как ложноотрицательные, так и ложноположительные результаты. В первой линии терапии Иресса не может быть применена вместо химиотерапии у больных с отсутствием мутации EGFR . Иногда у пациентов, принимающих препарат Иресса, отмечалось интерстициальное поражение легких, в некоторых случаях с летальным исходом. При нарастании таких симптомов как одышка, кашель, лихорадка применение препарата должно быть прекращено и незамедлительно проведено обследование. Если у пациента подтверждается наличие интерстициального легочного заболевания, прием препарата Иресса прекращают и пациенту назначается соответствующее лечение. Наиболее часто развитие интерстициальных поражений легких наблюдалось в Японии (приблизительно в 2% случаев у 27000 пациентов, принимающих препарат Иресса) по сравнению с другими странами (в 0.3% случаев среди 39000 пациентов). Среди факторов, повышающих риск развития интерстициального поражения легких были отмечены: курение, тяжелое общее состояние (PS \u003e 2), нормальная легочная ткань по данным компьютерной томографии \u003c 50%, продолжительность болезни (немелкоклеточный рак легкого) \u003c 6 месяцев, интерстициальная пневмония в анамнезе, пожилой возраст ( \u003e 55 лет), сопутствующие сердечно-сосудистые заболевания. На фоне приема препарата Иресса было отмечено бессимптомное повышение активности печеночных трансаминаз и уровня билирубина, нечасто развивался гепатит. Сообщалось об единичных случаях развития печеночной недостаточности, в некоторых случаях с летальным исходом. В связи с чем рекомендуется периодически оценивать печеночную функцию. При выраженном повышении активности трансаминаз и уровня билирубина прием препарата должен быть прекращен. В клинических исследованиях препарата Иресса были отмечены сердечно-сосудистые осложнения. Связь с приемом препарата Иресса не была установлена. У пациентов, принимающих варфарин, необходимо регулярно контролировать протромбиновое время. При появлении любых симптомов со стороны органов зрения или при развитии тяжелой или продолжительной диареи, тошноты, рвоты или анорексии пациент должен незамедлительно обратиться к врачу. При применении препарата Иресса в комбинации с лучевой терапией в качестве терапии первой линии у детей с глиомой ствола мозга или нерадикально удаленной глиомой супратенториальной локализации сообщалось о 4 случаях (один летальный) кровоизлияний в головной мозг. Еще один случай кровоизлияния в головной мозг отмечен у ребенка с эпендимомой при монотерапии препаратом Иресса. У взрослых пациентов с немелкоклеточным раком легкого при лечении препаратом Иресса подобные побочные явления не зафиксированы ни в одном случае. Сообщалось об единичных случаях развития перфорации органов ЖКТ у пациентов с такими факторами риска, как одновременный прием стероидов, НПВП, язвенная болезнь в анамнезе, пожилой возраст, курение, наличие метастазов в толстую кишку в месте перфорации. Однако, причинно-следственной связи между перечисленными явлениями и приемом препарата Иресса не установлено. Пациентам с редкими наследственными заболеваниями, такими как непереносимость лактозы, дефицит лактазы или синдромом мальабсорбции препарат Иресса следует назначать с осторожностью, в связи с наличием в составе лактозы. 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