Тамоксифен является нестероидным антиэстрогенным средством,... Инструкция
Показания к применению
Эстрогенозависимый рак молочных желез у женщин (особенно в менопаузе) и грудных желез у мужчин. Препарат может быть применен для лечения рака яичников, рака эндометрия, рака почки, меланомы, сарком мягких тканей при наличии в опухоли эстрогенных рецепторов, а также для лечения рака предстательной железы при резистентности к другим лекарственным средствам....
Тамоксифен является нестероидным антиэстрогенным средством, обладающим также слабыми эстрогенными свойствами. Его действие основано на способности блокировать рецепторы эстрогенов. Тамоксифен, а также некоторые его метаболиты конкурируют с эстрадиолом за места связывания с цитоплазматическими рецепторами эстрогена в тканях молочной железы, матки, влагалища, передней доли гипофиза и опухолях с высоким содержанием рецепторов эстрогена. В противоположность рецепторному комплексу эстрогена рецепторный комплекс тамоксифена не стимулирует синтез ДНК в ядре, а угнетает деление клетки, что приводит к регрессии опухолевых клеток и их гибели.
Показания к применению
Эстрогенозависимый рак молочных желез у женщин (особенно в менопаузе) и грудных желез у мужчин. Препарат может быть применен для лечения рака яичников, рака эндометрия, рака почки, меланомы, сарком мягких тканей при наличии в опухоли эстрогенных рецепторов, а также для лечения рака предстательной железы при резистентности к другим лекарственным средствам.
Противопоказания
Тромбофлебит, беременность, повышенная чувствительность к тамоксифену.
Применение при беременности и в период грудного вскармливания
Противопоказано
Способ применения и дозы
Режим дозирования обычно устанавливается индивидуально в зависимости от показаний. Суточная доза составляет 20-40 мг. В качестве стандартной дозы рекомендуется прием 20 мг тамоксифена внутрь ежедневно длительно. При появлении признаков прогрессирования заболевания прием препарата отменяют. Таблетки следует принимать не разжевывая, запивая небольшим количеством жидкости, в 1 прием утром, или, разделив необходимую дозу на 2 приема утром и вечером.
Побочное действие
Со стороны пищеварительной системы: тошнота, рвота, повышение активности печеночных трансаминаз, в отдельных случаях - жировая инфильтрация печени, холестаз, гепатит. Со стороны ЦНС: редко - депрессия, головокружение, головная боль, ретробульбарный неврит. Со стороны органа зрения: редко - ретинопатия, кератопатия, катаракта. Со стороны системы кроветворения: редко - тромбоцитопения, лейкопения. Со стороны эндокринной системы: у женщин - гиперплазия эндометрия, вагинальные кровотечения, приливы, увеличение массы тела, у мужчин - импотенция, снижение либидо. Со стороны сердечно-сосудистой системы: отеки, тромбоэмболия, флебит. Дерматологические реакции: алопеция, сыпь, зуд. Прочие: боли в костях и очагах поражения, повышение температуры тела.
Особые указания
С осторожностью применяют при лейкопении, тромбоцитопении, гиперкальциемии, у пациентов с катарактой, гиперлипидемией. В процессе лечения следует регулярно контролировать картину периферической крови (особенно количество тромбоцитов), уровень кальция и глюкозы в крови, при длительном применении показано наблюдение окулиста (каждые 3 мес). Не следует сочетать с препаратами, содержащими гормоны, особенно эстрогены. При одновременном применении с препаратами, оказывающими влияние на свертывающую систему крови, необходима коррекция дозы тамоксифена. В экспериментальных исследованиях установлено канцерогенное действие тамоксифена.
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