Оланзапин является антипсихотическим средством (нейролептико... Инструкция
Показания к применению
Шизофрения у взрослых, биполярное аффективное расстройство у взрослых, терапевтически резистентная депрессия.
Противопоказания
Повышенная чувствительность к любому из компонентов препарата, при риске развития глаукомы, закрытоугольная глаукома, возраст до 18 лет (эффективность и безопасность не доказаны), период грудного вскармливания.
Оланзапин является антипсихотическим средством (нейролептиком) с широким фармакологическим спектром влияния на ряд рецепторных систем. Установлено сродство оланзапина к серотониновым, дофаминовым, мускариновым, адренергическим альфа1 и гистаминовым H1-рецепторам. В экспериментах на животных было выявлено наличие антагонизма оланзапина по отношению к 5НТ, дофаминовым и холинергическим рецепторам. В условиях in vitro и in vivo оланзапин обладает более выраженным сродством и активностью в отношении серотониновых рецепторов, в сравнении с дофаминовыми D2 рецепторами. Оланзапин снижает условный защитный рефлекс (тест, характеризующий антипсихотическую активность) в дозах более низких, чем дозы, вызывающие каталепсию (расстройство, отражающее побочное влияние на моторную функцию). В отличие от других нейролептиков, оланзапин усиливает противотревожный эффект при проведении "анксиолитического" теста. Оланзапин обеспечивает статистически достоверную редукцию как продуктивных (бред, галлюцинации и др.), так и негативных расстройств.
Показания к применению
Шизофрения у взрослых, биполярное аффективное расстройство у взрослых, терапевтически резистентная депрессия.
Противопоказания
Повышенная чувствительность к любому из компонентов препарата, при риске развития глаукомы, закрытоугольная глаукома, возраст до 18 лет (эффективность и безопасность не доказаны), период грудного вскармливания.
Применение при беременности и в период грудного вскармливания
Противопоказано.
Способ применения и дозы
Внутрь, независимо от приема пищи. Рекомендуемая терапевтическая доза препарата Оланзапин Канон составляет от 5 мг до 20 мг в сутки. Суточную дозу необходимо подбирать индивидуально в зависимости от клинического состояния пациента.
Побочное действие
Нарушения со стороны крови и лимфатической системы: часто - эозинофилия, нечасто - лейкопения, нейтропения, редко: тромбоцитопения. Нарушения со стороны иммунной системы: очень редко - аллергические реакции (анафилактический шок, ангионевротический отек, кожный зуд, крапивница). Нарушения со стороны обмена веществ: очень редко - развитие или декомпенсация сахарного диабета, в некоторых случаях сопровождающейся кетоацидозом и диабетической комой, в том числе с летальным исходом, после отмены терапии, спустя 9-12 месяцев лечения, возможно снижение концентрации глюкозы в крови. Нарушения со стороны обмена веществ и питания: очень часто - увеличение массы тела, часто - повышение концентрации холестерина, триглицеридов, глюкозурия, повышение аппетита. Изменение концентрации глюкозы от нормальных значений натощак (<5,56 ммоль/л) до повышенных (≥7 ммоль/л) наблюдается часто. Изменение концентрации глюкозы от пограничных значений (≥5,56 ммоль/л - <7 ммоль/л) до повышенных (≥7 ммоль/л) наблюдается очень часто, очень редко: гипертриглицеридемия, гиперхолистеринемия, частота не известна - вздутие живота. Нарушения со стороны нервной системы: очень часто - сонливость, часто - головокружение, акатизия, паркинсонизм, дискинезия, нечасто: судороги (чаще на фоне судорожного синдрома в анамнезе), очень редко - злокачественный нейролептический синдром, дистония (включая окулогирный криз), поздняя дискинезия, синдром "отмены" (потливость, бессонница, тремор, тревога, тошнота или рвота). Нарушения со стороны сердца: нечасто - брадикардия, удлинение интервала QT, очень редко - желудочковая тахикардия/ фибрилляция желудочков, внезапная смерть. Нарушения со стороны сосудов: часто - ортостатическая гипотензия, очень редко - тромбоэмболия легочной артерии, тромбоз глубоких вен. Нарушения со стороны желудочно-кишечного тракта: часто - транзиторные антихолинергические эффекты, в том числе сухость во рту, запор, редко: панкреатит, Нарушения со стороны печени и желчевыводящих путей: часто - преходящее повышение активности "печеночных" трансфераз (аланинаминотрансферазы (АЛТ), аспартатаминотрансферазы (ACT)), особенно в ранний период исследования, редко: гепатит (включая печеночно-клеточный, гепатоцеллюлярный или смешанный). Нарушения со стороны колеи и подкожных тканей: часто - кожная сыпь, нечасто - реакции фотосенсибилизации, очень редко - алопеция. Нарушения со стороны скелетно-мышечной и соединительной ткани: редко - рабдомиолиз, частота не известна: артралгия. Нарушения со стороны почек и мочевыводящих путей: нечасто - недержание мочи, редко: задержка начала мочеиспускания, частота неизвестна: повышение мочевой кислоты. Нарушения со стороны половых органов и молочной железы: редко - приапизм. Общие расстройства и нарушения в месте введения: часто - астения, усталость, отеки, редко - гипотермия, частота не известна - лихорадка. Лабораторные и инструментальные данные: очень часто - увеличение концентрации пролактина в плазме, по клинические проявления (например, гинекомастия, галакторея и увеличение молочных желез) редко. У большинства пациентов уровень пролактина спонтанно нормализовался без отмены препарата, часто - увеличение активности креатинфосфокиназы (КФК), общего билирубина, очень редко - увеличение активности щелочной фосфатазы.
Передозировка
Частые симптомы: тахикардия, возбуждение/агрессивность, расстройство артикуляции, различные экстрапирамидные расстройства и нарушения сознания разной степени тяжести (от седативного эффекта до комы). Лечение: специфического антидота для оланзапина не существует. Не рекомендуется провоцирование рвоты. Могут быть показаны стандартные процедуры при передозировке (промывание желудка, назначение активированного угля). Совместное назначение активированного угля приводит к снижению биодоступности оланзапина при приеме внутрь до 50-60%. Показано симптоматическое лечение в соответствии с клиническим состоянием и контроль над функциями жизненно важных органов, включая лечение артериальной гипотонии, нарушения кровообращения и поддержание дыхательной функции. Не следует применять эпинефрин, дофамин и другие симпатомиметики, которые являются агонистами бета-адренорецепторов, так как стимуляция этих рецепторов может усугублять артериальную гипотензию.
Особые указания
Клиническое улучшение может занимать несколько дней и требует наблюдения за пациентом. Злокачественный нейролептический синдром (ЗНС) (потенциально летальный симптомокомплекс) может развиваться при лечении любыми нейролептиками, включая препарат Оланзапин Канон, однако к настоящему времени нет данных, подтверждающих достоверную связь приема оланзапина с развитием данного состояния. Клинические проявления злокачественного нейролептического синдрома включают значительное повышение температуры тела, ригидность мускулатуры, изменение психического статуса и вегетативные нарушения (нестабильный пульс или артериальное давление, тахикардия, сердечные аритмии, повышенное потоотделение). Дополнительные признаки могут включать увеличение уровня креатинфосфокиназы, миоглобинурию (рабдомиолиз) и острую почечную недостаточность. Клинические проявления злокачественного нейролептического синдрома или значительное повышение температуры тела без других симптомов злокачественного нейролептического синдрома требуют отмены всех нейролептиков, включая препарат Оланзапин Канон. Лечение оланзапином реже сопровождается развитием дискинезии, требующей медикаментозной коррекции, чем при применении галоперидола. Однако следует учитывать риск поздней дискинезии при длительной терапии нейролептиками. При развитии признаков поздней дискинезии рекомендуется снижение дозы или отмена препарата Оланзапин Канон. Следует учитывать, что при переводе на препарат Оланзапин Канон симптомы поздней дискинезии могут развиваться вследствие одномоментной отмены предшествующей терапии. Симптомы поздней дискинезии могут нарастать или манифестировать после отмены препарата. Эффективность при применении при болезни Паркинсона не превышает плацебо (в целях купирования ятрогенных психозов). Не рекомендуется применение препарата Оланзапин Канон при лечении психозов, индуцированных приемом агонистов дофаминовых рецепторов при болезни Паркинсона, у таких пациентов отмечается усиление симптомов паркинсонизма и галлюцинации. Цереброваскулярные нежелательные явления (например, инсульт, транзиторная ишемическая атака), включая летальные исходы, отмечаются у пожилых пациентов с психозом на фоне деменции. В плацебо-контролированных исследованиях отмечались более высокая частота цереброваскулярных нежелательных явлений у пациентов в группе оланзапина, по сравнению с группой плацебо. Данные пациенты имели предшествующие факторы риска (цереброваскулярные нарушения (в анамнезе), транзиторная ишемическая атака, артериальная гипертензия, курение), а также сопутствующие заболевания и/или прием лекарственных препаратов, по времени связанные с цереброваскулярными нарушениями. Эффективность оланзапина у пожилых пациентов с психозом на фоне деменции не установлена. Основными факторами риска повышенной смертности для данной группы пациентов при лечении оланзапином являются возраст ≥ 80 лет, седация, сочетанное применение с бензодиазепинами или наличие патологии легких (например, пневмония с аспирацией или без нее). Не существует достаточных данных, чтобы установить различия в частоте возникновения цереброваскулярных нарушений и/или смертности (по сравнению с плацебо), и в факторах риска у этой группы пациентов при приеме оланзапина внутрь и при внутримышечных инъекциях. Препарат Оланзапин Канон не рекомендован для терапии пациентов с психозом на фоне деменции.
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низкозамещенная гипролоза, гидрофосфат кальция, кроскармеллоза натрия, маннитол, стеарат магния."}}]},{"id":2,"name":"Фармакологические свойства","slug":"pharmacologic_effects","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Оланзапин является антипсихотическим средством (нейролептиком) с широким фармакологическим спектром влияния на ряд рецепторных систем. Установлено сродство оланзапина к серотониновым, дофаминовым, мускариновым, адренергическим альфа1 и гистаминовым H1-рецепторам. В экспериментах на животных было выявлено наличие антагонизма оланзапина по отношению к 5НТ, дофаминовым и холинергическим рецепторам. В условиях in vitro и in vivo оланзапин обладает более выраженным сродством и активностью в отношении серотониновых рецепторов, в сравнении с дофаминовыми D2 рецепторами. Оланзапин снижает условный защитный рефлекс (тест, характеризующий антипсихотическую активность) в дозах более низких, чем дозы, вызывающие каталепсию (расстройство, отражающее побочное влияние на моторную функцию). В отличие от других нейролептиков, оланзапин усиливает противотревожный эффект при проведении \"анксиолитического\" теста. Оланзапин обеспечивает статистически достоверную редукцию как продуктивных (бред, галлюцинации и др.), так и негативных расстройств."}}]},{"id":3,"name":"Показания к применению","slug":"indications","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Шизофрения у взрослых, биполярное аффективное расстройство у взрослых, терапевтически резистентная депрессия."}}]},{"id":4,"name":"Противопоказания","slug":"contraindications","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Повышенная чувствительность к любому из компонентов препарата, при риске развития глаукомы, закрытоугольная глаукома, возраст до 18 лет (эффективность и безопасность не доказаны), период грудного вскармливания."}}]},{"id":5,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Противопоказано."}}]},{"id":6,"name":"Способ применения и дозы","slug":"dosage","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Внутрь, независимо от приема пищи. Рекомендуемая терапевтическая доза препарата Оланзапин Канон составляет от 5 мг до 20 мг в сутки. Суточную дозу необходимо подбирать индивидуально в зависимости от клинического состояния пациента."}}]},{"id":7,"name":"Побочное действие","slug":"side_effects","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Нарушения со стороны крови и лимфатической системы: часто - эозинофилия, нечасто - лейкопения, нейтропения, редко: тромбоцитопения. Нарушения со стороны иммунной системы: очень редко - аллергические реакции (анафилактический шок, ангионевротический отек, кожный зуд, крапивница). Нарушения со стороны обмена веществ: очень редко - развитие или декомпенсация сахарного диабета, в некоторых случаях сопровождающейся кетоацидозом и диабетической комой, в том числе с летальным исходом, после отмены терапии, спустя 9-12 месяцев лечения, возможно снижение концентрации глюкозы в крови. Нарушения со стороны обмена веществ и питания: очень часто - увеличение массы тела, часто - повышение концентрации холестерина, триглицеридов, глюкозурия, повышение аппетита. Изменение концентрации глюкозы от нормальных значений натощак (\u003c5,56 ммоль/л) до повышенных (≥7 ммоль/л) наблюдается часто. Изменение концентрации глюкозы от пограничных значений (≥5,56 ммоль/л - \u003c7 ммоль/л) до повышенных (≥7 ммоль/л) наблюдается очень часто, очень редко: гипертриглицеридемия, гиперхолистеринемия, частота не известна - вздутие живота. Нарушения со стороны нервной системы: очень часто - сонливость, часто - головокружение, акатизия, паркинсонизм, дискинезия, нечасто: судороги (чаще на фоне судорожного синдрома в анамнезе), очень редко - злокачественный нейролептический синдром, дистония (включая окулогирный криз), поздняя дискинезия, синдром \"отмены\" (потливость, бессонница, тремор, тревога, тошнота или рвота). Нарушения со стороны сердца: нечасто - брадикардия, удлинение интервала QT, очень редко - желудочковая тахикардия/ фибрилляция желудочков, внезапная смерть. Нарушения со стороны сосудов: часто - ортостатическая гипотензия, очень редко - тромбоэмболия легочной артерии, тромбоз глубоких вен. Нарушения со стороны желудочно-кишечного тракта: часто - транзиторные антихолинергические эффекты, в том числе сухость во рту, запор, редко: панкреатит, Нарушения со стороны печени и желчевыводящих путей: часто - преходящее повышение активности \"печеночных\" трансфераз (аланинаминотрансферазы (АЛТ), аспартатаминотрансферазы (ACT)), особенно в ранний период исследования, редко: гепатит (включая печеночно-клеточный, гепатоцеллюлярный или смешанный). Нарушения со стороны колеи и подкожных тканей: часто - кожная сыпь, нечасто - реакции фотосенсибилизации, очень редко - алопеция. Нарушения со стороны скелетно-мышечной и соединительной ткани: редко - рабдомиолиз, частота не известна: артралгия. Нарушения со стороны почек и мочевыводящих путей: нечасто - недержание мочи, редко: задержка начала мочеиспускания, частота неизвестна: повышение мочевой кислоты. Нарушения со стороны половых органов и молочной железы: редко - приапизм. Общие расстройства и нарушения в месте введения: часто - астения, усталость, отеки, редко - гипотермия, частота не известна - лихорадка. Лабораторные и инструментальные данные: очень часто - увеличение концентрации пролактина в плазме, по клинические проявления (например, гинекомастия, галакторея и увеличение молочных желез) редко. У большинства пациентов уровень пролактина спонтанно нормализовался без отмены препарата, часто - увеличение активности креатинфосфокиназы (КФК), общего билирубина, очень редко - увеличение активности щелочной фосфатазы."}}]},{"id":8,"name":"Передозировка","slug":"overdose","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Частые симптомы: тахикардия, возбуждение/агрессивность, расстройство артикуляции, различные экстрапирамидные расстройства и нарушения сознания разной степени тяжести (от седативного эффекта до комы). Лечение: специфического антидота для оланзапина не существует. Не рекомендуется провоцирование рвоты. Могут быть показаны стандартные процедуры при передозировке (промывание желудка, назначение активированного угля). Совместное назначение активированного угля приводит к снижению биодоступности оланзапина при приеме внутрь до 50-60%. Показано симптоматическое лечение в соответствии с клиническим состоянием и контроль над функциями жизненно важных органов, включая лечение артериальной гипотонии, нарушения кровообращения и поддержание дыхательной функции. Не следует применять эпинефрин, дофамин и другие симпатомиметики, которые являются агонистами бета-адренорецепторов, так как стимуляция этих рецепторов может усугублять артериальную гипотензию."}}]},{"id":9,"name":"Особые указания","slug":"cautions","displayInMenu":true,"body":[{"type":"paragraph","data":{"text":"Клиническое улучшение может занимать несколько дней и требует наблюдения за пациентом. Злокачественный нейролептический синдром (ЗНС) (потенциально летальный симптомокомплекс) может развиваться при лечении любыми нейролептиками, включая препарат Оланзапин Канон, однако к настоящему времени нет данных, подтверждающих достоверную связь приема оланзапина с развитием данного состояния. Клинические проявления злокачественного нейролептического синдрома включают значительное повышение температуры тела, ригидность мускулатуры, изменение психического статуса и вегетативные нарушения (нестабильный пульс или артериальное давление, тахикардия, сердечные аритмии, повышенное потоотделение). Дополнительные признаки могут включать увеличение уровня креатинфосфокиназы, миоглобинурию (рабдомиолиз) и острую почечную недостаточность. Клинические проявления злокачественного нейролептического синдрома или значительное повышение температуры тела без других симптомов злокачественного нейролептического синдрома требуют отмены всех нейролептиков, включая препарат Оланзапин Канон. Лечение оланзапином реже сопровождается развитием дискинезии, требующей медикаментозной коррекции, чем при применении галоперидола. Однако следует учитывать риск поздней дискинезии при длительной терапии нейролептиками. При развитии признаков поздней дискинезии рекомендуется снижение дозы или отмена препарата Оланзапин Канон. Следует учитывать, что при переводе на препарат Оланзапин Канон симптомы поздней дискинезии могут развиваться вследствие одномоментной отмены предшествующей терапии. Симптомы поздней дискинезии могут нарастать или манифестировать после отмены препарата. Эффективность при применении при болезни Паркинсона не превышает плацебо (в целях купирования ятрогенных психозов). Не рекомендуется применение препарата Оланзапин Канон при лечении психозов, индуцированных приемом агонистов дофаминовых рецепторов при болезни Паркинсона, у таких пациентов отмечается усиление симптомов паркинсонизма и галлюцинации. Цереброваскулярные нежелательные явления (например, инсульт, транзиторная ишемическая атака), включая летальные исходы, отмечаются у пожилых пациентов с психозом на фоне деменции. В плацебо-контролированных исследованиях отмечались более высокая частота цереброваскулярных нежелательных явлений у пациентов в группе оланзапина, по сравнению с группой плацебо. Данные пациенты имели предшествующие факторы риска (цереброваскулярные нарушения (в анамнезе), транзиторная ишемическая атака, артериальная гипертензия, курение), а также сопутствующие заболевания и/или прием лекарственных препаратов, по времени связанные с цереброваскулярными нарушениями. Эффективность оланзапина у пожилых пациентов с психозом на фоне деменции не установлена. Основными факторами риска повышенной смертности для данной группы пациентов при лечении оланзапином являются возраст ≥ 80 лет, седация, сочетанное применение с бензодиазепинами или наличие патологии легких (например, пневмония с аспирацией или без нее). Не существует достаточных данных, чтобы установить различия в частоте возникновения цереброваскулярных нарушений и/или смертности (по сравнению с плацебо), и в факторах риска у этой группы пациентов при приеме оланзапина внутрь и при внутримышечных инъекциях. Препарат Оланзапин Канон не рекомендован для терапии пациентов с психозом на фоне деменции."}}]}],"source":{"title":"36.6","url":"https://366.ru"}},"description_toggle":false,"short_description":"Оланзапин является антипсихотическим средством (нейролептиком) с широким фармакологическим спектром влияния на ряд рецепторных систем. Установлено сродство оланзапина к серотониновым, дофаминовым, мускариновым, адренергическим альфа1 и гистаминовым H1-рецепторам. В экспериментах на животных было выявлено наличие антагонизма оланзапина по отношению к 5НТ, дофаминовым и холинергическим рецепторам. В условиях in vitro и in vivo оланзапин обладает более выраженным сродством и активностью в отношении серотониновых рецепторов, в сравнении с дофаминовыми D2 рецепторами. Оланзапин снижает условный защитный рефлекс (тест, характеризующий антипсихотическую активность) в дозах более низких, чем дозы, вызывающие каталепсию (расстройство, отражающее побочное влияние на моторную функцию). В отличие от других нейролептиков, оланзапин усиливает противотревожный эффект при проведении \"анксиолитического\" теста. 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