Описание
Селлсепт 500 мг примсеняется при профилактики отторжения после трансплантиции почки, сердца или печени. Возможно назначение Селлсепта в комбинации со следующими препаратами: иммуноглобулином антитимоцитарным,циклоспорином, кортикостероидами и ОКТ3 (ортоклон мышиных моноклональных антител). Основное действующее вещество Селлсепта — Микофенолата мофетил (ММФ). ММФ оказывает сильно выраженное цитостатическое влияние на лимфоциты, благодаря чему минимизируется риск отторжения органов – почки, сердца, печени. Препарат Селлсепт не обладает большим количеством побочных действий, как у конкурентов.
Состав препарата Селлсепт 500 мг
1 таблетка, покрытая оболочкой, содержит:
- активное вещество: микофенолата мофетил 500 мг,
- дополнительные вещества: целлюлоза микрокристаллическая, повидон К90, кроскармеллоза натрия, стеарат магния.
- оболочка: опадрай лавандовый (Opadry Lavender) Y-5-10272-A (гипромеллоза, титана диоксид, гипролоза, краситель индигокармин, макрогол 400, краситель оксид железа красный).
Показания препарата Селлсепт 500 мг
Взрослым и детям старше 12 лет:
- лечение и профилактика терапии отторжения трансплантата после аллогенной пересадки почки, сердца, печени;
- в виде комбинированной терапии с циклоспорином и кортикостероидами.
Фармакодинамика
Микофенолата мофетил (ММФ) — иммунодепрессант, ингибитор инозинмонофосфатдегидрогеназы, который представляет собой 2-морфолиноэтиловый эфир микофеноловой кислоты (МФК). ММФ — мощный избирательный ингибитор инозинмонофосфатдегидрогеназы (ИМФДГ), который подавляет синтез de novo гуанозиновых нуклеотидов. Микофенолата мофетил оказывает явное цитостатическое влияние на лимфоциты, чем на другие клетки. Потому что пролиферация Т- и В-лимфоцитов сильно подчиняется синтезу пуринов de novo, в то время как клетки других типов могут использовать на иные пути метаболизма.
Фармакокинетика
Фармакокинетика изучались на пациентах, перенесших трансплантацию почки, печени или сердца. У пациентов после пересадки в целом фармакокинетика микофенолата сходна. У пациентов, перенесших пересадку печени, в раннем посттрансплантационном периоде и получающих ММФ в дозе 1.5 грамма, концентрации МФК сходная как и у больных после пересадки почки, получающих ММФ в дозе 1 грамм.
Всасывание
При пероральном приеме идет быстрое и полное всасывание, а также полный метаболизм ММФ с появлением активного метаболита – МФК. Биодоступность ММФ при пероральном приеме, составляет 94%. После перорального приема лекарства, концентрация ММФ в плазме не определяется.
Прием еды не влияет на степень всасывания ММФ при его назначении по 1.5 г два раза в сутки.
Распределение
Как правило, примерно через 6-12 часов после приема препарата наблюдается вторичное увеличение концентрации МФК в плазме крови, что показывает о печеночно-кишечной рециркуляции лекарства. При одновременном назначении колестирамина AUC МФК снижается примерно на 40%, что свидетельствует о прерывании печеночно-кишечной рециркуляции.
В клинически значимых концентрациях МФК на 97% связывается с альбумином плазмы.
Метаболизм
В основном МФК метаболизируется с образованием фармакологически неактивного фенольного глюкуронида МФК (МФКГ), под действием глюкуронилтрансферазы. Показано, что in vivo МФКГ в ходе печеночно-кишечной рециркуляции преобразуется в свободную МФК.
Выведение
После перорального приема радиоактивно меченного ММФ 93% полученной дозы выводится с мочой, а 6% — с калом. Большая часть (около 87%) введенной дозы выводится с мочой в виде МФКГ. Незначительные количества препарата (<1% дозы) выводятся с мочой в виде МФК.
Путем гемодиализа клинически определяемые концентрации МФК и МФКГ не элиминируются. Секвестранты желчных кислот наподобие колестирамина понижают AUC МФК, останавливая печеночно-кишечную рециркуляцию.
Биоэквивалентность
В исследованиях показано, что две таблетки ММФ по 500 мг эквивалентны четырем капсулам по 250 мг.
Фармацевтические характеристики
Вещество в таблетках — мелкий гранулированный порошок, от белого до почти белого цвета. Таблетки, покрытые пленочной оболочкой бледно-лилового цвета, с гравировкой «CellCept 500» на одной стороне и «Roche» — на другой.
Упаковка, срок годности, условия хранения
По 10 таблеток в контурной ячейковой упаковке из пвх пленки и фольги алюминиевой. По 5, 10, 15 контурных ячейковых упаковок вместе с инструкцией упакованы в картоннную пачку.
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Срок хранения 3 года. Не применять по истечении срока годности!
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