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Фампира — Fampyra (Фампридин)

Фампира - Fampyra (Фампридин)

Фампира — Fampyra (Фампридин)

Препарат Фампира, уже получивший одобрение в ряде европейских стран и США, был разработан специально для людей с ограниченными способностями передвижения. По данным исследований, проведённых при участии пациентов с различными типами рассеянного склероза, при различных способах его лечения, показали заметное стойкое улучшение и значительное увеличение (на 25 процентов) скорости ходьбы.

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Описание

Препарат Фампира, уже получивший одобрение в ряде европейских стран и США, был разработан специально для людей с ограниченными способностями передвижения. По данным исследований, проведённых при участии пациентов с различными типами рассеянного склероза, при различных способах его лечения, показали заметное стойкое улучшение и значительное увеличение (на 25 процентов) скорости ходьбы.

Основным действующим веществом препарата является Фампридин, который рекомендован для проведения комбинированной и монотерапии. Фампридин, принадлежит к группе лекарств, который обозначается как блокирующий канал калия. Фампридин предотвращает выход калия из поврежденных рассеянным склерозом нервных клеток. Приём препарата способствует улучшению проводимости по нервным путям. Пациенты, принимающие фампридин, получили возможность вести более активный образ жизни.

Показания к применению препарата Фампира

  • Препарат используется для улучшения ходьбы у взрослых пациентов с диагнозом Рассеянный склероз (РС ), которые не могут передвигаться.

Состав препарата Фампира

  • Препарат содержит активное вещество — Фампридин.

Фармакодинамика препарата Фампира

Препарат – это препарат, существенно улучшающий скорость ходьбы у пациентов с рассеянным склерозом (РС). Механизм действия препарата состоит в том, что молекулы препарата блокируют калиевые каналы, расположенные на поверхности нервных клеток, благодаря которым мышцы приводятся в действие. Таким образом искусственно увеличивается потенциал действия пораженного нерва и улучшается нервно-мышечная проводимость, а следовательно, и двигательные функции человека.

Эффективность препарата доказана в ходе клинических исследований с участием большого количества пациентов с рассеянным склерозом (как рецидивирующего, так и прогрессирующего). У 35 процентов — 43 процентов пациентов, получавших таблетки , значительно возросла скорость ходьбы, а также укрепились мышцы ног. Стоит отметить, что эти пациенты также сообщали о значительном улучшении субъективных показателей, в частности, о увеличении качества их жизни в целом.

Препарат – это первый и пока единственный препарат для улучшения двигательной функции у пациентов с рассеянным склерозом (РС). Препарат Фампира имеет довольно высокий профиль безопасности, большинство наблюдаемых побочных эффектов имеют легкую степень выраженности.

Следует отметить, что препарат не оказывает влияния на течение болезни и не является заменой назначенной схеме лечения.

Фармакокинетика препарата Фампира

Абсорбция

После перорального приёма препарат Фампира быстро и полностью абсорбируется из желудочно-кишечного тракта. Приём пищи снижает AUC0–∞ фампридина приблизительно на 2–7 процента, но повышает максимальную концентрацию (Cmax) на 15–23 процента.

Распределение

Фампридин является жирорастворимым лекарственным веществом и легко проникает через гематоэнцефалический барьер (ГЭБ). Фампридин не является субстратом для Р-гликопротеина. Степень связывания фампридина с белками плазмы у человека составляет 3–7 процентов. Объём распределения (Vd/F) = 332,167 ± 59,696 литров.

Метаболизм

Метаболизируется фампридина путём окисления до З-гидроксиди-4-аминопиридина, далее конъюгируется до З-гидрокси-4-аминопиридина сульфата. В исследованиях in vitro активность метаболитов фампридина в отношении калиевых каналов не обнаружена. 3-гидроксилирование фампридина до З-гидрокси-4-аминопиридина микросомами печени человека, по-видимому, катализируется цитохромом P450 2Е1 (CYP2E1) без признаков значимого ингибирования CYP2E1. Имеются сведения о прямом ингибировании CYP2E1 фампридином в концентрации 30 μМ (примерно на 12 процентов), что примерно в 100 раз превышает среднюю концентрацию фампридина в плазме крови при использовании дозировки 10 мг. Обработка культивируемых гепатоцитов человека фампридином практически не влияла на индукцию ферментов CYP2E1, CYP1A2, CYP2B6, CYP2C9, CYP2C19 или CYP3A4/5.

Выведение

Фампридин обладает линейной фармакокинетикой. Период полувыведения составляет около 6 часов. Cmax и, в меньшей степени AUC, увеличивается пропорционально принятой дозе. Основным методом элиминации фампридина является почечная экскреция, причём приблизительно 90 % дозы выделяется в неизменённом виде в течение 24 часов. Почечный клиренс значительно выше, чем скорость клубочковой фильтрации, благодаря активному участию транспортёра органического катиона 2 (OCT 2). С фекалиями выводится менее 1 процента от вводимой дозы.

Особые группы пациентов

Данных о клинически значимом накоплении фампридина при приёме в рекомендуемой дозировке у пациентов с нормальной функцией почек нет. У больных с почечной недостаточностью происходит аккумуляция фампридина пропорционально степени тяжести почечной недостаточности.

Особенности применения

Таблетки Фампира следует глотать целиком, не разжевывая и не разделяя на части, это связано с тем, что действующее вещество фампридин будет выделяться слишком быстро. Соответственно, увеличиться риск нарушения фармакокинетики и развития побочных реакций (в частности, возникновения судорог).

Если доза пропущена, следующую принимают в надлежащее время. Промежуток между приемами таблеток должен составлять не менее 12 часов. Одновременный прием двух и более таблеток противопоказан.

Начало лечением Фампира и оценка эффективности лечения:

Первые приемы должны быть ограничены 2 неделями. Так после двух недель лечения препаратом Фампира необходимо увидеть помогает ли он пациенту или нет.

После двухнедельного лечения лекарством , проведите тест ходьбы и оцените насколько хорошо пациент стал ходить . Посмотрите сколько шагов за какое время он проходит.

Если никакое улучшение не наблюдается, следует прекратить принимать препарат .

Возможные нежелательные реакции

В ходе клинических исследований, где принимало участие 1000 человек, принимающих препарат на протяжении 12 недель, оценивали риск побочных эффектов. Изучали 819 пациентов, находящихся на лечении в течение полугода, 628 больных, состояние которых отслеживали год, и 526 пациентов, наблюдавшихся на протяжении двух лет и более. Подавляющее большинство нежелательных реакций были связаны с повышением частоты инфекций мочевыделительного тракта и неврологическими расстройствами.

Беременность и грудное вскармливание

Применение при беременности

Категория действия на плод по FDA — N. Имееется ограниченное количество данных об использовании препарата Фампира у беременных женщин. Исследования на животных показали репродуктивную токсичность. Рекомендуется избегать применения фампридина при беременности.

Применение в период грудного вскармливания

Неизвестно, выделяется ли фампридин с молоком человека или животного. Применение препарата Фампира не рекомендуется во время кормления грудью.

Фертильность

В исследованиях на животных никакого влияния не было обнаружено на фертильность.

Фармакокинетика у отдельных групп больных

Применение при нарушениях функции печени

Для пациентов с печёночной недостаточностью коррекция дозы не требуется.

Применение при нарушениях функции почек

Препарат Фампира противопоказан пациентам с лёгкой, умеренной и тяжёлой почечной недостаточностью (клиренс креатинина <80 мл/мин).

Применение в детском возрасте

Эффективность и безопасность фампридина у детей в возрасте от 0 до 18 лет не установлены.

Применение у пожилых пациентов

У пожилых пациентов перед началом лечения следует проверить функцию почек, а также проводить оценку функции почек в процессе лечения.

Фармацевтические характеристики

Препарат Фампира — таблетки с пролонгированным освобождением.

Упаковка, срок годности, условия хранения

Таблетки Фампира по 10 мг; по 10 таблеток упакованы в лекартсвенные баночки и вместе с инструкцией по применению упакованы к картонную упаковку.

Препарат Фампира следует хранить при температуре выше 25 Градусов. Таблетки хранить в сухом, темном месте.

Срок годности препарата Фампира — 2 года.

 

 

 

 

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