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Эстрацит — Estracyt (Эстрамустина фосфат)

Эстрацит — Estracyt (Эстрамустина фосфат)

Медицинский препарат Эстрацит (Estracyt) назначают при терапии карциномы предстательной железы. Эстрацит — это конъюгат эстрадиола и азотистого иприта, представляющий собой противоопухолевый препарат с двойным механизмом действия. Действующим веществом Эстрацита является эстрамустина фосфат, вещество принадлежащее к группе цитостатиков, Действие эстрамустина заключается в угнетении выработки половых гормонов и повреждении раковых клеток предстательной железы.

Описание

Медицинский препарат Эстрацит (Estracyt) назначают при терапии карциномы предстательной железы. Эстрацит — это конъюгат эстрадиола и азотистого иприта, представляющий собой противоопухолевый препарат с двойным механизмом действия. Действующим веществом Эстрацита является эстрамустина фосфат, вещество принадлежащее к группе цитостатиков, Действие эстрамустина заключается в угнетении выработки половых гормонов и повреждении раковых клеток предстательной железы.

В большинстве случаев, рак предстательной железы протекает бессимптомно. Больше половины пациентов обращаются тогда, когда болезнь уже перешла на серьёзные стадии, когда первым признаком является боль в костях или суставах, когда уже имеют место различные метастазы.

Однако за последнее время смертность от рака предстательной железы значительно уменьшилась – благодаря эффективным программам лечения, где одну из существенных значений в положительной динамике отдано Эстрациту, который назначают в очень сложных ситуациях.

Состав

Одна капсула содержит:

  • 156,7 мг моногидрата натриевой соли эстрамустина фосфата, что эквивалентно 140 мг эстрамустина,
  • дополнительные вещества:натрия лаурилсульфат; тальк; стеарат магния; диоксид кремния коллоидный безводный;
  • оболочка капсул: диоксид титана, желатин, чернила черные.

Один флакон порошка лиофилизированного для приготовления раствора для инъекций содержит:

  • действующее вещество: эстрамустина фосфат 300 мг,
  • вспомогательные вещества: меглумин; маннит

Показания препарата

  • поздние стадии карциномы предстательной железы, особенно при рефрактерности к гормональной терапии;
  • первичная терапия карциномы предстательной железы при наличии низкой эффективности гормональной терапии.

Фармакодинамика

Установлено, что в результате биотрансформации эстрамустина фосфата, получающиеся вещества эстрон и эстрадиол характеризуются антигонадотропной активностью и приводят к снижению уровня тестостерона. Эти метаболиты обладают антимитотическим действием, подавляя образование микротрубочек в метафазу и разрушая их в интерфазу митоза. В терапевтических дозах миелодепрессия проявляется слабо или практически отсутствует. Не оказывает иммунодепрессивного действия. Воздействет на переднюю долю гипофиза. Уменьшает продукцию гонадотропных гормонов, снижает концентрацию тестостерона в крови.

Фармакокинетика

Распределение и метаболизм

После в/в инфузии неизмененный эстрамустина фосфат обнаруживается в плазме, однако он быстро преобразуется с образованием эстрамустина, а затем — эстромустина, являющегося основным метаболитом в плазме. Связывание эстрамустина и эстромустина с белками плазмы высокое. Эстрамустин и эстромустин подвергаются дальнейшему преобразованию с образованием — эстрадиола и эстрона.

После введения препарата эстрамустин и эстромустин в основном обнаруживаются в опухолевой ткани предстательной железы человека. В опухолевой ткани концентрации эстрамустина и эстромустина выше, чем в плазме. Вероятно, потому что эстрамустин и эстромустин поглощаются тканью предстательной железы за счет их связывания со специфичным белком в опухолевой ткани предстательной железы.

Выведение

Эстрамустин и эстромустин выделяются с желчью и калом. Не обнаруживаются в моче.

Фармацевтическая характеристика

  • Эстрацит выпускается в виде белых твердых желатиновых капсул по 140 мг, содержащих белый порошок. Капсулы размера 1, с черными надписями на крышке «ESTRACYT» и «К Ph 750» — на корпусе.
  • Лиофилизированный порошок для приготовления раствора во флаконах по 300 мг. Растворитель (вода для инъекций) в ампулах по 8 мл. В коробке по 10 флаконов и по 10 ампул вместе с инструкцией.

Упаковка, срок годности, условия хранения

  • По 40 или 100 капсул с осушителем во флаконах из темного стекла.
  • Один флакон с инструкцией по применению в пачке картонной.

Хранить в недоступном для детей месте, при температуре не выше 25°C.

Срок годности — 3 года.

 

 

 

 

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

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Работаем и отправляем Эстрацит (Эстрамустина фосфат) по странам СНГ: Россия, Украина, Кыргызстан (Бишкек), Белоруссия, Узбекистан (Ташкент),
а также мы можем отправить Эстрацит (Эстрамустина фосфат) по регионам Казахстана: Нур-Султан (Астана), Шымкент, Талдыкорган, Актау и другие.

 

Отзывы

  1. Rochell

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