Кветиапин - антипсихотическое средство (нейролептик). Проявляет более высокое сродство к рецепторам серотонина (5-HT2), чем к рецепторам дофамина D1 и D2 в головном мозге. Обладает тропизмом к гистаминовым и альфа1-адренорецепторам, менее активен по отношению к альфа2-адренорецепторам. Не обнаружено избирательного сродства к
м-холино- и бензодиазепиновым рецепторам. Уменьшает активность мезолимбических А10-дофаминергических нейронов, в сравнении с А9-нигростриатными нейронами, вовлеченными в двигательные функции. Не вызывает длительного повышения концентрации пролактина. Длительность связи с 5-HT2-серотониновыми и D2-дофами-новыми рецепторами составляет менее 12 ч.
Показания к применению
Острые и хронические психозы (в т.ч. при шизофрении); маниакальные эпизоды в структуре биполярного расстройства.
Противопоказания
Повышенная чувствительность к любому из компонентов препарата.
Способ применения и дозы
Внутрь, 2 раза в сутки, независимо от приема пищи.
Лечение острых и хронических психозов, включая шизофрению.
Суточная доза для первых 4 дней терапии — 50 мг (1 день), 100 мг (2 день), 200 мг (3 день), 300 мг (4 день). Начиная с 4 дня, доза должна титроваться до эффективной, в пределах от 300 до 450 мг/сут, при необходимости — до 750 мг/сут.
Лечение маниакальных эпизодов в структуре биполярного расстройства.
Кветиапин применяется в качестве монотерапии или в качестве адьювантной терапии для стабилизации настроения.
Суточная доза для первых 4-х дней терапии — 100 мг (1 день), 200 мг (2 день), 300 мг (3 день), 400 мг (4 день). В дальнейшем к 6-му дню терапии суточная доза препарата может быть увеличена до 800 мг. Увеличение суточной дозы не должно превышать 200 мг в день.
В зависимости от клинического эффекта и индивидуальной переносимости, доза может варьировать в пределах от 200 до 800 мг/сут. Обычно эффективная доза составляет от 400 до 800 мг/сут.
Для лечения шизофрении максимальная рекомендованная суточная доза кветиапина составляет 750 мг, для лечения маниакальных эпизодов в структуре биполярного расстройства максимальная рекомендованная суточная доза кветиапина составляет 800 мг/сут.
При почечной и/или печеночной недостаточности и у пожилых пациентов начальная доза — 25 мг/сут, с последующим ежедневным увеличением на 25–50 мг до достижения эффективной дозы.
Побочное действие
Со стороны нервной системы: сонливость, головокружение, головная боль, тревожность, астения, враждебность, возбуждение, бессонница, акатизия, тремор, судороги, депрессия, парестезии, злокачественный нейролептический синдром (гипертермия, мышечная ригидность, измененный ментальный статус, лабильность вегетативной нервной системы, повышение активности креатинфосфокиназы).
Со стороны сердечно-сосудистой системы: ортостатическая гипотензия (сопровождающаяся головокружением), тахикардия, обморок, удлинение интервала QT (взаимосвязи применения кветиапина с постоянным увеличением QTc не выявлено).
Со стороны пищеварительной системы: сухость слизистой оболочки полости рта, тошнота, рвота, боль в животе, диарея или запор, повышение активности «печеночных» трансаминаз.
Прочие: боль в пояснице, боль в грудной клетке, субфебрилитет, увеличение массы тела (преимущественно в первые недели лечения), миалгия, сухость кожи, ослабление зрения.
Взаимодействие с другими лекарственными средствами
При одновременном назначении препаратов, обладающих сильным ингибирующим действием наCYP3A4 (таких как противогрибковые средства группы азолов и макролидные антибиотики), концентрация кветиапина в плазме может повышаться.
В таких случаях следует применять более низкие дозы кветиапина. Особенное внимание должно быть уделено пожилым и ослабленным пациентам. Необходимо индивидуально оценивать соотношение риска и пользы для каждого пациента.
Индукторы микросомальных систем печени (фенитоин и др.), тиоридазин повышают клиренс кветиапина, ингибиторы микросомальных систем печени — снижают; в то же время одновременное назначение кветиапина и антидепрессантов — имипрамина (ингибитор CYP2D6) или флуоксетина (ингибитор CYP3A4 и CYP2D6) не оказывает существенного влияния на его фармакокинетику.
Фармакокинетика кветиапина существенно не изменяется при одновременном назначении с антипсихотическими препаратами рисперидоном или галоперидолом.
Не вызывает индукцию ферментных систем печени, вовлеченных в метаболизм антипирина.
Фармакокинетика препаратов лития не изменяется при одновременном назначении кветиапина.
Не отмечено клинически значимых изменений фармакокинетики вальпроевой кислоты и кветиапина при совместном назначении дивальпроекса натрия (натрия вальпроат и вальпроевая кислота в молярном соотношении 1:1) и Кветиапина.
Лекарственные средства, угнетающие центральную нервную систему, и этанол повышают риск развития побочных эффектов.
Форма выпуска
Таблетки
Условия хранения
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Проявляет более высокое сродство к рецепторам серотонина (5-HT2), чем к рецепторам дофамина D1 и D2 в головном мозге. Обладает тропизмом к гистаминовым и альфа1-адренорецепторам, менее активен по отношению к альфа2-адренорецепторам. Не обнаружено избирательного сродства к "}},{"type":"paragraph","data":{"text":"м-холино- и бензодиазепиновым рецепторам. Уменьшает активность мезолимбических А10-дофаминергических нейронов, в сравнении с А9-нигростриатными нейронами, вовлеченными в двигательные функции. Не вызывает длительного повышения концентрации пролактина. 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