Фазлодекс Раствор, шприц, 2 шт, 5 мл, для внутримышечного введения, для бюста

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При использовании препарата Фазлодекс в дозе 500 мг равновесное состояние достигается в течение 1-го месяца терапии (AUC — 546 нг·день/мл, C\u003csub\u003emax\u003c/sub\u003e — 25,1 нг/мл, C\u003csub\u003emin\u003c/sub\u003e — 16,3 нг/мл). При равновесном состоянии содержание фулвестранта в плазме колеблется в относительно узких границах — максимальные и минимальные показатели отличаются примерно в 3 раза."}},{"type":"paragraph","data":{"text":"После в/м инъекции экспозиция примерно пропорциональна введенной дозе (в интервале доз от 50 до 500 мг)."}},{"type":"paragraph","data":{"text":"Фулвестрант характеризуется экстенсивным и быстрым распределением. Большой кажущийся V\u003csub\u003ed\u003c/sub\u003e (от 3 до 5 л/кг) при равновесной концентрации предполагает преимущественно экстраваскулярное распределение. Связь с белками плазмы — 99%. Главные компоненты связывания включают фракции ЛПОНП, ЛПНП и ЛПВП. Роль связывающего половые гормоны глобулина не установлена."}},{"type":"paragraph","data":{"text":"Метаболизм фулвестранта включает комбинации множества потенциальных путей биотрансформации, аналогичных механизмам метаболизма эндогенных стероидов (включают метаболиты 17-кетон, сульфон, 3-сульфат, 3- и 17-глюкуронид). Идентифицированные метаболиты менее активны или равны по активности фулвестранту. CYP 3A4 является единственным изоферментом из семейства P450, который участвует в окислении фулвестранта. Однако представляется, что in vivo преобладает биотрансформация без участия Р450. Фулвестрант в основном выводится с фекалиями, с мочой — менее 1% вещества. Клиренс фулвестранта составляет (11±1,7) мл/мин/кг, что предполагает высокий уровень печеночной экстракции. 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Однако применение препарата Фазлодекс у этой группы пациентов требует осторожности. Безопасность и эффективность препарата у пациентов с тяжелыми нарушениями функции печени не установлены."}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Наблюдавшиеся нежелательные реакции представлены ниже."}},{"type":"paragraph","data":{"text":"Определение частоты побочных реакций: очень часто (>10%); часто (>1-≤10%); редко (>0,1-≤1%)."}},{"type":"paragraph","data":{"text":"Со стороны системы пищеварения: часто — тошнота, рвота, диарея, анорексия."}},{"type":"paragraph","data":{"text":"Со стороны сердечно-сосудистой системы: очень часто — ощущение жара («приливы»); часто — тромбоэмболия."}},{"type":"paragraph","data":{"text":"Со стороны кожи и кожных придатков: часто — сыпь."}},{"type":"paragraph","data":{"text":"Местные реакции: часто — транзиторные боли, воспалительные реакции."}},{"type":"paragraph","data":{"text":"Со стороны мочеполовой системы: часто — инфекции мочевыводящих путей; редко — вагинальные кровотечения, вагинальный кандидоз."}},{"type":"paragraph","data":{"text":"Прочие: часто — головные боли, астения, боль в спине; редко — галакторея, реакции повышенной чувствительности (отеки, крапивница)."}}]},{"id":14,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"Случаи передозировки у человека неизвестны. В исследованиях на животных при введении высоких доз фулвестранта наблюдались только эффекты, непосредственно или опосредованно связанные с антиэстрогенной активностью."}},{"type":"paragraph","data":{"text":"Лечение: симптоматическая терапия."}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"По результатам исследования клинического взаимодействия с мидазоламом, фулвестрант не подавляет активность CYP3A4. Данные in vitro свидетельствуют, что фулвестрант не влияет на активность CYP1A2, 2C9, 2C19 и 2D6. Возможное подавление активности CYP2A6, 2C8 и 2E1 не оценивалось."}},{"type":"paragraph","data":{"text":"В исследовании клинического взаимодействия с рифампицином (индуктор CYP3A4) и кетоконазолом (ингибитор CYP3A4) не обнаружено клинически значимых изменений клиренса фулвестранта. Поэтому при назначении фулвестранта в комбинации с индукторами или ингибиторами CYP3A4 коррекции дозы не требуется."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"Лечение препаратом Фазлодексдолжно проводиться только под наблюдением врача, имеющего опыт применения противоопухолевых препаратов."}},{"type":"paragraph","data":{"text":"Рекомендуется соблюдать осторожность при применении препарата Фазлодекс пациентам с легким или умеренным нарушением функции печени и с тяжелым нарушением функции почек (Cl креатинина"}},{"type":"paragraph","data":{"text":"Учитывая способ применения, рекомендуется соблюдать осторожность при использовании препарата Фазлодекс у пациентов со склонностью к кровотечениям, тромбоцитопенией или у пациентов, принимающих антикоагулянты."}},{"type":"paragraph","data":{"text":"Тромбоэмболии у женщин с распространенным раком молочной железы наблюдаются часто. Это необходимо принимать во внимание при назначении препарата Фазлодекс у пациентов с риском тромбоэмболии."}},{"type":"paragraph","data":{"text":"Эффекты длительного применения фулвестранта на костную ткань не установлены. Учитывая механизм действия фулвестранта, нельзя исключить потенциальный риск остеопороза."}},{"type":"paragraph","data":{"text":"Фазлодексне должен смешиваться с другими ЛС."}},{"type":"paragraph","data":{"text":"Влияние на способность управлять автомобилем или выполнять работы, требующие повышенной скорости физических и психических реакций. Это влияние незначительно. Пациентам с симптомами астении необходимо соблюдать осторожность при управлении автомобилем или другими механизмами."}}]},{"id":18,"name":"Форма выпуска","slug":"","body":[{"type":"paragraph","data":{"text":"\u003ca href=\"https://www.eapteka.ru/goods/drugs/oncology/?drug_form=rastvor_dlya_inektsiy\"\u003eраствор для инъекций\u003c/a\u003e"}}]},{"id":19,"name":"Условия хранения","slug":"storage","body":[{"type":"paragraph","data":{"text":"В защищенном от света месте, при температуре 2–8 °C"}}]},{"id":20,"name":"Срок годности","slug":"expiry_date","body":[{"type":"paragraph","data":{"text":"4 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":"\u003ca href=\"https://www.eapteka.ru/goods/manufacturer/astrazeneka/\"\u003eАстраЗенека, Великобритания\u003c/a\u003e"}}]}],"source":null},"description_toggle":false,"short_description":"Фулвестрант является конкурентным антагонистом рецепторов эстрогенов. По уровню аффинности к рецепторам сопоставим с эстрадиолом. Фулвестрант блокирует трофическое действие эстрогенов, не проявляя собственной эстрогеноподобной активности. Механизм действия связан с подавлением активности и деградацией эстроген-рецепторов. Также фулвестрант достоверно снижает экспрессию рецепторов прогестерона. Фулвестрант не оказывает стимулирующего эффекта на эндометрий у женщин в постменопаузе. Эффекты длительной терапии фулвестрантом на эндотелий в постменопаузе не установлены. Также нет данных по морфологии эндометрия. Данных о влиянии длительного применения фулвестранта на костную ткань нет.ФармакокинетикаПосле внутримышечной инъекции фулвестрант медленно всасывается, достигая Cmaxв плазме примерно через 7 дней. При использовании препарата Фазлодекс в дозе 500 мг равновесное состояние достигается в течение 1-го месяца терапии (AUC — 546 нг·день/мл, Cmax— 25,1 нг/мл, Cmin— 16,3 нг/мл). При равновесном состоянии содержание фулвестранта в плазме колеблется в относительно узких границах — максимальные и минимальные показатели отличаются примерно в 3 раза. После в/м инъекции экспозиция примерно пропорциональна введенной дозе (в интервале доз от 50 до 500 мг). Фулвестрант характеризуется экстенсивным и быстрым распределением. Большой кажущийся Vd(от 3 до 5 л/кг) при равновесной концентрации предполагает преимущественно экстраваскулярное распределение. Связь с белками плазмы — 99%. Главные компоненты связывания включают фракции ЛПОНП, ЛПНП и ЛПВП. Роль связывающего половые гормоны глобулина не установлена. Метаболизм фулвестранта включает комбинации множества потенциальных путей биотрансформации, аналогичных механизмам метаболизма эндогенных стероидов (включают метаболиты 17-кетон, сульфон, 3-сульфат, 3- и 17-глюкуронид). Идентифицированные метаболиты менее активны или равны по активности фулвестранту. 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