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Алимта — Alimta (Пеметрексед) 500 мг от Lilly, США-Франция

Алимта (Alimta) Пеметрексед 500 мг Lilly США-Франция

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Алимта (Пеметрексед). Активное вещество пеметрексед является антагонистом фолиевой кислоты, которое действует на многие мишени ее метаболизма, поэтому его действие увеличивается именно в опухолевых клетках.

Категория:

Описание

Состав препарата Алимта (Пеметрексед)

Один флакон Алимта (Пеметрексед) содержит:
  • активное вещество: пеметрекседа динагрия гептагидрат, эквивалентный 500 мг пеметрекседа;
  • вспомогательные вещества: маннитол — 500,0 мг.
  • хлористоводородной кислоты раствор 10 %
  • и/или натрия гидроксида раствор 10 % (добавляют в процессе производства для установления pH).

Описание Алимта (Пеметрексед)

Лиофилизат от светло-желтого или светло-желтого с зеленоватым оттенком до белого цвета.

Фармакологическое действие

Активное вещество пеметрексед является антагонистом фолиевой кислоты, которое действует на многие мишени ее метаболизма и ингибирующим in vitro дигидрофолатредуктазу (DHFR), тимидилатсинтазу (TS),  глицинамидрибонуклеотидформилтрансферазу (GARFT), являющиеся ключевыми фолат-зависимыми ферментами при биосинтезе пуриновых и тимидиновых нуклеотидов. Пеметрексед доставляется в клетки при помощи переносчика восстановленных фолатов, а также белковых фолат-связывающих транспортных систем. Проникая в клетку, пеметрексед быстро и эффективно превращается в полиглутаматные формы при помощи фолилполиглутаматсинтетазы.
Полиглутаматные формы остаются в клетках и являются более сильными ингибиторами TS и GARFT. Полиглутаминирование — процесс, зависимый от концентрации и времени, который встречается в опухолевях и в меньшей степени в обычных тканях. У полиглутаминированных метаболитов больше период полувыведения, поэтому его действие увеличивается именно в опухолевых клетках.
При комбинированном применении цисплатина и пеметрекседа в исследованиях in vitro наблюдался синергизм.

Фармакокинетика

Распределение постоянного объема пеметрекседа равно 9 л/кв.м. При этом около 81 % пеметрекседа связывается с белками плазмы, и связывание не нарушается при выраженной почечной недостаточности.
Пеметрексед в небольших количествах подвергается метаболизму в печени.
Около 70 — 90 % препарата выделяется почками в неизмененном виде за первые 24 часа после введения. Общий плазменный клиренс пеметрекседа — 92 мл/мин, а период полувыведения из плазмы пациента составляет около 3,5 часа при нормальной функции почек.

Показания к применению:

  • Злокачественная мезотелиома плевры;

  • Метастатический неплоскоклеточный немелкоклеточный или местнораспространенный рак легкого.

Противопоказания

  • Выраженная почечная недостаточность (если клиренс креатинина (КК) <45 мл/мин);
  • Гиперчувствительность к препарату или вспомогательным веществам, входящим в его состав;
  • Миелосупрессия (если абсолютное количество нейтрофилов <1 500/мкл и тромбоцитов <100 000/мкл);
  • Детский возраст (отсутствуют данные по эффективности и безопасности);
  • Беременность и период лактации;
  • Одновременное использование с вакциной профилактики желтой лихорадки;
  • После консультации с врачом при тяжелых заболеваниях сердечно-сосудистой системы, в том числе при инфарктах или нарушении мозгового кровообращения;
  • С осторожностью при нарушении функции печени.

Способ применения и дозы Алимта (Пеметрексед)

Внутривенно капельно в течение 10 мин.

При злокачественной мезотелиоме плевры (совместно с цисплатином): рекомендованная доза пеметрекседа — в 1-й день каждого 21-дневного цикла 500 мг/кв.м; цисплатин — в 1-й день каждого 21-дневного цикла через 30 минут после введения пеметрекседа 75 мг/кв.м в виде 2-х часовой внутривенной  инфузии на фоне гидратации.

При немелкоклеточном раке легкого (монотерапия): рекомендованная доза — в 1-й день каждого 21-дневного цикла 500 мг/кв.м . Коррекция дозы перед последующими курсами должна основываться на самом низком пороге гематологических показателей и на самом высоком уровне негематологической токсичности в период предыдущего цикла лечения. Лечение может быть отложено для восстановления от токсичности. В ходе восстановления пациенту необходимо продолжать лечение по схеме.

Флакон необходимо аккуратно взбалтывать до полного растворения лиофилизата и получения прозрачного раствора. Возможно изменение цвета раствора от желтоватого или зеленовато-желтого до бесцветного цвета. Полученный раствор пеметрекседа после разводят до 100 мл 0.9% раствором хлорида натрия.

Побочные действия

  • Монотерапия пеметрекседом с добавлением фолиевой кислоты и цианокобаламина: очень часто — более 10%, часто — более 1% и менее 10%, редко — менее 1%.
  • Со стороны пищеварительной системы: очень часто — рвота, тошнота, анорексия, диарея, стоматит/фарингит, повышение активности АЛТ и ACT; часто — боль в животе, запор,  редко — колит.
  • Со стороны органов кроветворения: очень часто — нейтропения, лейкопения, анемия; часто тромбоцитопения.
  • Со стороны периферической нервной системы: часто — моторная или сенсорная нейропатия.
  • Со стороны кожных покровов: очень часто — шелушение/сыпь; часто -алопеция,  кожный зуд; редко — мультиформная эритема.
  • Со стороны ССС: редко — суправентрикулярная тахикардия.
  • Со стороны мочевыделительной системы: часто — повышение содержания креатинина.
  • Прочие: часто — лихорадка, фебрильная нейтропения, аллергические реакции, присоединение вторичных инфекций без нейтропении; очень часто — повышенная утомляемость;.

Условия хранения

Препарат хранить при температуре от 15 до 25 °С.
Приготовленный раствор необходимо хранить не более 24 часов при температуре от 2 до 8 °С .

 

 

 

 

 

Наша компания работает как на территории Казахстана, так и осуществляет доставку в страны ближнего зарубежья. Обращайтесь к нам за консультациями по контактным телефонам.

Заказать и купить Алимта (Пеметрексед) в Алматы

Заказать и купить Алимта (Пеметрексед) в Казахстане

Позвоните и узнайте цену Алимта (Пеметрексед)

Работаем и отправляем Алимта (Пеметрексед) по странами СНГ: Россия, Украина, Кыргызстан (Бишкек), Белоруссия, Узбекистан (Ташкент),
а также можем отправить Алимта (Пеметрексед) по регионам Казахстана: Нур-Султан (Астана), Шымкент, Талдыкорган, Актау и другие.

Детали

Производитель

Эли Лилли

Страна производитель

США

Действующее вещество

Пеметрексед

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