Противоопухолевый препарат, действие которого обусловлено нарушением синтеза ДНК и РНК. Образующийся в результате гидролиза фторурацил ингибирует фермент тимидилатсинтетазу и синтез ДНК, внедряется в структуру РНК вместо урацила, делая ее дефектной, и ингибирует клеточную пролиферацию. В клетках опухоли превращается в 5-фтор-дезоксиуридин-5-монофосфат, который затем фосфорилируется в трифосфат и включается в РНК, и флоксуридина монофосфат, который ингибирует тимидилатсинтетазу. Менее токсичен и лучше переносится пациентами, чем 5-фторурацил.
Показания к применению
Рак толстой и прямой кишки
Рак желудка
Рак молочной железы
Диффузный нейродермит
Кожные лимфомы
Противопоказания
Терминальная стадия заболевания
Острые профузные кровотечения
Тяжелые нарушения функции печени
Тяжелые нарушения функции почек
Лейкопения (менее 3000/мкл)
Тромбоцитопения (менее 100 000/мкл)
Анемия (уровень гемоглобина менее 65 г/л)
Беременность
Лактация (грудное вскармливание)
Повышенная чувствительность к компонентам препарата. С осторожностью следует применять препарат у пациентов с нарушением функции кроветворения, печени и почек, метаболизма глюкозы, при язвенной болезни желудка и двенадцатиперстной кишки, склонностью к кровотечениями, с инфекционными заболеваниями
Применение при беременности и в период грудного вскармливания
Фторафур противопоказан к применению при беременности и в период лактации (грудного вскармливания). Следует иметь ввиду, что препарат угнетает репродуктивную функцию пациента.
Способ применения и дозы
Назначают внутрь. Суточная доза препарата Фторафур составляет 800-1000 мг/м2 (20-30 мг/кг массы тела) в 2-4 приема, но не более 2 г/сут. Курсовая доза при приеме внутрь составляет 30-40 г. Интервал между курсами составляет 4 недели. Дозу препарата Фторафур можно уменьшить у пациентов пожилого возраста и на поздней стадии заболевания.
Побочное действие
Со стороны системы кроветворения: лейкопения, тромбоцитопения, анемия. Со стороны пищеварительной системы: тошнота, рвота, анорексия, боли в животе, диарея; редко - стоматит, эзофагит, язвенные поражения слизистой оболочки ЖКТ, желудочно-кишечные кровотечения, нарушения функции печени, острый гепатит, острый панкреатит. Со стороны ЦНС: головокружение, спутанность сознания, сонливость, атаксия, эйфория, симптомы лейкоэнцефалита. Со стороны сердечно-сосудистой системы: кардиалгия, стенокардия, ишемия миокарда, инфаркт миокарда. Со стороны органов чувств: диплопия, слезотечение, фиброз слезных протоков, потеря обоняния. Дерматологические реакции: алопеция, нарушение регенерации кожи, ногтей. Прочие: фарингит, аллергические реакции (в т.ч. анафилактический шок), нарушение функции почек, дегидратация организма, интерстициальная пневмония.
Передозировка
Симптомы: усиление токсических эффектов со стороны ЖКТ, ЦНС и угнетение гемопоэза. Лечение: контроль функции кроветворения в течение не менее чем 4 недель, при необходимости проводят симптоматическую терапию. Специфический антидот к тегафуру неизвестен.
Особые указания
При необходимости назначения препарата Фторафур пациентам с нарушениями кроветворения, функций печени и почек, метаболизма глюкозы, с язвенной болезнью желудка и двенадцатиперстной кишки, склонностью к геморрагиям, с инфекционными заболеваниями следует учитывать потенциальный риск развития побочных реакций. В период лечения следует регулярно контролировать картину периферической крови, функциональное состояние печени и почек. При длительном применении препарата его побочное действие усиливается. Головокружение, тошнота и рвота уменьшаются при фракционировании суточной дозы. При развитии серьезных побочных эффектов необходимо прекратить применение препарата. Использование в педиатрииБезопасность применения препарата у детей не установлена.
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