Летрозол таблетки Таблетки, пачка, 30 шт, 2,5 мг, для приема внутрь, для тела, для взрослых

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Супрессия синтеза эстрогенов поддерживается на протяжении всего периода лечения."}},{"type":"paragraph","data":{"text":"При применении летрозола в диапазоне доз от 0.1 до 5 мг нарушения синтеза стероидных гормонов в надпочечниках не наблюдается, тест с АКТГ не выявляет нарушений синтеза альдостерона или кортизола. Дополнительного назначения глюкокортикоидов и минералокортикоидов не требуется."}},{"type":"paragraph","data":{"text":"Блокада биосинтеза эстрогенов не приводит к накоплению андрогенов, являющихся предшественниками эстрогенов. На фоне приема летрозола изменений концентраций лютеинизирующего и фолликулостимулирующего гормонов в плазме крови, изменений функции щитовидной железы, изменений липидного профиля, повышения частоты инфарктов миокарда и инсультов отмечено не было."}},{"type":"paragraph","data":{"text":"На фоне лечения летрозолом слабо повышается частота остеопороза (6.9% по сравнению с 5.5% на плацебо). Однако частота переломов костей у пациенток, получающих летрозол, не отличается от таковой у здоровых людей того же возраста."}},{"type":"paragraph","data":{"text":"Адьювантная терапия летрозолом ранних стадий рака молочной железы снижает риск рецидивов, увеличивает выживаемость без признаков заболевания в течение 5 лет, снижает риск развития вторичных опухолей."}},{"type":"paragraph","data":{"text":"Продленная адьювантная терапия летрозолом снижает риск рецидивов на 42%. Достоверное преимущество по выживаемости без признаков заболевания в группе летрозола отмечалось вне зависимости от вовлеченности лимфатических узлов. Лечение летрозолом снижает смертность пациенток с вовлечением лимфатических узлов на 40%."}}]},{"id":7,"name":"Фармакологические свойства","slug":"","body":[{"type":"paragraph","data":{"text":"Всасывание"}},{"type":"paragraph","data":{"text":"Летрозол быстро и полностью всасывается из ЖКТ, средняя биодоступность составляет 99.9%. Прием пищи незначительно снижает скорость абсорбции. Среднее значение времени достижения Cmax летрозола в крови составляет 1 ч при приеме летрозола натощак и 2 ч - при приеме с пищей; среднее значение Cmax составляет 129±20.3 нмоль/л при приеме натощак и 98.7±18.6 нмоль/л - при приеме с пищей, однако степень всасывания летрозола (при оценке по AUC) не изменяется. Небольшие изменения в скорости всасывания расцениваются как не имеющие клинического значения, поэтому летрозол можно принимать независимо от приема пищи."}},{"type":"paragraph","data":{"text":"Распределение"}},{"type":"paragraph","data":{"text":"Связь летрозола с белками плазмы крови составляет приблизительно 60% (преимущественно с альбумином - 55%). Концентрация летрозола в эритроцитах составляет около 80% от таковой в плазме крови. Кажущийся Vd в равновесном состоянии составляет около 1.87±0.47 л/кг. Css достигается в течение 2-6 недель ежедневного приема суточной дозы 2.5 мг. Фармакокинетика нелинейна. Кумуляции при длительном применении не отмечено."}},{"type":"paragraph","data":{"text":"Метаболизм"}},{"type":"paragraph","data":{"text":"Летрозол в значительной степени подвергается метаболизму под действием изоферментов CYP3A4 и CYP2A6 цитохрома Р450 с образованием фармакологически неактивного карбинолового соединения."}},{"type":"paragraph","data":{"text":"Выведение"}},{"type":"paragraph","data":{"text":"Выводится преимущественно почками в виде метаболитов, в меньшей степени - через кишечник. Конечный T1/2 составляет 48 ч."}},{"type":"paragraph","data":{"text":"Фармакокинетика в особых клинических случаях"}},{"type":"paragraph","data":{"text":"Фармакокинетические параметры летрозола не зависят от возраста пациента."}},{"type":"paragraph","data":{"text":"При почечной недостаточности фармакокинетические параметры не изменяются. При умеренно выраженном нарушении функции печени (класс В по шкале Чайлд-Пью) средние величины AUC хотя и выше на 37%, но остаются в пределах того диапазона значений, которые отмечаются у лиц без нарушений функции печени. У больных с циррозом печени и тяжелыми нарушениями ее функции (класс С по шкале Чайлд-Пью) AUC увеличивается на 95% и T1/2 на 187%. Однако, учитывая хорошую переносимость высоких доз препарата (5-10 мг/сут) в этих случаях необходимости изменять дозу летрозола нет."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"Ранние стадии рака молочной железы, клетки которого имеют рецепторы к гормонам, у женщин в постменопаузе, в качестве адъювантной терапии;"}},{"type":"paragraph","data":{"text":"ранние стадии рака молочной железы у женщин в постменопаузе после завершения стандартной адъювантной терапии тамоксифеном в качестве продленной адъювантной терапии;"}},{"type":"paragraph","data":{"text":"распространенные гормонозависимые формы рака молочной железы у женщин в постменопаузе (терапия первой линии);"}},{"type":"paragraph","data":{"text":"распространенные формы рака молочной железы у женщин в постменопаузе (естественной или вызванной искусственно), получавших предшествующую терапию антиэстрогенами."}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"paragraph","data":{"text":"Эндокринный статус, характерный для репродуктивного периода;"}},{"type":"paragraph","data":{"text":"беременность;"}},{"type":"paragraph","data":{"text":"период лактации (грудного вскармливания);"}},{"type":"paragraph","data":{"text":"детский возраст (эффективность и безопасность для детей не установлена);"}},{"type":"paragraph","data":{"text":"повышенная чувствительность к летрозолу или любому другому компоненту препарата."}},{"type":"paragraph","data":{"text":"С осторожностью и после тщательного взвешивания соотношения между потенциальным риском и ожидаемым эффектом лечения следует назначать препарат пациенткам с КК менее 10 мл/мин, т.к. нет данных о применении летрозола в этих случаях."}}]},{"id":11,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","body":[{"type":"paragraph","data":{"text":"Противопоказано назначение препарата при беременности и в период лактации."}},{"type":"paragraph","data":{"text":"Во время терапии летрозолом, учитывая потенциальную возможность наступления беременности, женщинам в перименопаузном и раннем постменопаузном периоде следует использовать надежные способы контрацепции до установления стабильного постменопаузного гормонального уровня."}},{"type":"paragraph","data":{"text":"Противопоказание: детский возраст (эффективность и безопасность для детей не установлена)."}}]},{"id":12,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Препарат принимают внутрь, независимо от приема пищи. Рекомендуемая доза препарата Летрозол составляет 2.5 мг 1 раз/сут, ежедневно, длительно (в течение 5 лет или до рецидива). В качестве продленной адъювантной терапии лечение должно продолжаться в течение 4 лет (не дольше 5 лет). При появлении признаков прогрессирования заболевания прием препарата Летрозол следует прекратить. У пациенток с заболеванием на последней стадии или метастазирующей опухоли, лечение Летрозолом следует продолжать до тех пор, пока выражено прогрессирование опухоли. У пациенток пожилого возраста коррекции дозы препарата Летрозол не требуется. При нарушениях функции печени или почек (КК >10 мл/мин) коррекция дозы препарата не требуется. Тем не менее, при тяжелых нарушениях функции печени (класс С по шкале Чайлд- Пью) пациентам требуется постоянный медицинское наблюдение."}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Как правило, побочные реакции были слабо или умеренно выражены и, в основном, связаны с подавлением синтеза эстрогенов."}},{"type":"paragraph","data":{"text":"Частота возникновения побочных реакций оценивается следующим образом: возникающие очень часто (>10%), часто (1-10%), иногда (0.1-1%), редко (0.01- 0.1%), очень редко ("}},{"type":"paragraph","data":{"text":"Со стороны пищеварительной системы: часто - тошнота, рвота, диспепсия, запор, диарея; иногда - боли в животе, стоматит, сухость во рту, повышение активности печеночных ферментов."}},{"type":"paragraph","data":{"text":"Со стороны нервной системы: часто - головная боль, головокружение, депрессия; иногда - тревога, нервозность, раздражительность, сонливость, бессонница, ухудшение памяти, дизестезия, парестезия, гипестезия, нарушения вкусового восприятия, эпизоды нарушения мозгового кровообращения."}},{"type":"paragraph","data":{"text":"Со стороны органов кроветворения: иногда - лейкопения."}},{"type":"paragraph","data":{"text":"Со стороны сердечно-сосудистой системы: иногда - ощущение сердцебиения, тахикардия, тромбофлебит поверхностных и глубоких вен, повышение АД, ИБС (стенокардия, инфаркт миокарда, сердечная недостаточность), тромбоэмболия; редко - эмболия легочной артерии, тромбоз артерий, инсульт."}},{"type":"paragraph","data":{"text":"Со стороны дыхательной системы: иногда - одышка, кашель."}},{"type":"paragraph","data":{"text":"Дерматологические реакции: часто - алопеция, повышенная потливость, кожная сыпь (включая эритематозную, макулопапулезную, везикулярную сыпь, псориазоподобные высыпания); иногда - кожный зуд, сухость кожи, крапивница; очень редко - ангионевротический отек, анафилактические реакции."}},{"type":"paragraph","data":{"text":"Со стороны костно-мышечной системы: очень часто - артралгия; часто - миалгия, боли в костях, остеопороз, переломы костей, иногда - артрит."}},{"type":"paragraph","data":{"text":"Со стороны органов чувств: иногда - катаракта, раздражение глаз, \"затуманивание\" зрения, нарушение вкусовых ощущений."}},{"type":"paragraph","data":{"text":"Со стороны мочевыводящей системы: иногда - учащенное мочеиспускание, инфекции мочевыводящих путей."}},{"type":"paragraph","data":{"text":"Со стороны половой системы: иногда - вагинальные кровотечения, выделения из влагалища, сухость влагалища, боль в молочных железах."}},{"type":"paragraph","data":{"text":"Прочие: очень часто - приступообразные ощущения жара (\"приливы\"); часто - повышенная утомляемость, астения, недомогание, периферические отеки, увеличение массы тела, гиперхолестеринемия, анорексия, повышение аппетита; иногда - снижение массы тела, жажда, гипертермия (пирексия), сухость слизистых оболочек, генерализованные отеки, боли в опухолевых очагах."}}]},{"id":14,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"Имеются отдельные сообщения о случаях передозировки летрозола."}},{"type":"paragraph","data":{"text":"Какие-либо специфические методы лечения передозировки не известны. Показана симптоматическая и поддерживающая терапия. Летрозол выводится из плазмы посредством гемодиализа."}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"При одновременном назначении летрозола с циметидином и варфарином клинически значимого взаимодействия не наблюдается."}},{"type":"paragraph","data":{"text":"Согласно результатам исследований in vitro летрозол подавляет активность изоферментов цитохрома Р450 CYP2A6 и CYP2C19 (последнего - умеренно). При решении вопроса о значении этих данных для клиники необходимо учитывать, что изофермент CYP2A6 не играет существенной роли в метаболизме лекарственных препаратов. В экспериментах in vitro было показано, что летрозол в концентрациях, в 100 раз превышающих равновесные значения в плазме, не обладает способностью существенно подавлять метаболизм диазепама (субстрата для CYP2C19). Таким образом, клинически значимое взаимодействие с изоферментом CYP2C19 маловероятно. Тем не менее, следует соблюдать осторожность при совместном применении летрозола и препаратов, метаболизирующихся преимущественно при участии вышеназванных изоферментов и имеющих узкий терапевтический индекс."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"Пациентки с тяжелыми нарушениями функции печени должны находиться под постоянным наблюдением."}},{"type":"paragraph","data":{"text":"Клинического опыта по применению летрозола в комбинации с другими противоопухолевыми средствами в настоящее время не имеется."}},{"type":"paragraph","data":{"text":"Влияние на способность к вождению автотранспорта и управлению механизмами"}},{"type":"paragraph","data":{"text":"Некоторые побочные эффекты препарата, такие как общая слабость и головокружение, могут влиять на способность выполнения потенциально опасных видов деятельности, требующих концентрации внимания и быстрых реакций. В этой связи следует соблюдать осторожность при управлении транспортными средствами и механизмами."}}]},{"id":18,"name":"Форма выпуска","slug":"","body":[{"type":"paragraph","data":{"text":"Таблетки, покрытые пленочной оболочкой желтого цвета, круглые, двояковыпуклые, на поперечном разрезе - ядро белого или белого с желтоватым оттенком цвета."}}]},{"id":19,"name":"Условия хранения","slug":"storage","body":[{"type":"paragraph","data":{"text":"Препарат следует хранить в недоступном для детей, сухом, защищенном от света месте при температуре не выше 25°C."}}]},{"id":20,"name":"Срок годности","slug":"expiry_date","body":[{"type":"paragraph","data":{"text":"2 года."}}]},{"id":21,"name":"Условия отпуска","slug":"release_condition","body":[{"type":"paragraph","data":{"text":"По рецепту."}}]},{"id":22,"name":"Производитель","slug":"","body":[{"type":"paragraph","data":{"text":"Велфарм"}}]}],"source":null},"description_toggle":false,"short_description":"Противоопухолевый препарат. 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