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Иресса — Iressa (Гефитиниб) 250 мг

Таблетки Иресса

Иресса — Iressa (Гефитиниб) 250 мг

Иресса (Iressa) — противораковый препарат, для лечения распространенного немелкоклеточного рака легкого (НМРЛ) с действующим веществом — Гефитиниб. Он подавляет работу тирозинкиназы — фермента, способствующего росту раковых клеток.

Препарат Иресса — селективный ингибитор рецепторов эпидермального фактора роста, способный тормозить рост опухоли, ангиогенез и метастазирование, а также ускоряет появление апоптоза у опухолевых клеток. Также препарат увеличивает противоoпухолевую активность химиотерапевтическогo лечения, гормональной и лучевой терапии.

Категория:

Описание

Иресса (Iressa) — противораковый препарат, для лечения распространенного немелкоклеточного рака легкого (НМРЛ) с действующим веществом — Гефитиниб. Он подавляет работу тирозинкиназы — фермента, способствующего росту раковых клеток.

Препарат Иресса — селективный ингибитор рецепторов эпидермального фактора роста, способный тормозить рост опухоли, ангиогенез и метастазирование, а также ускоряет появление апоптоза у опухолевых клеток. Также препарат увеличивает противоoпухолевую активность химиотерапевтическогo лечения, гормональной и лучевой терапии.

Показания препарата Иресса

  • метастатический немелкоклеточный рак легкого с мутациями тирозинкиназного домена рецептора эпидермального фактора роста в первой линии терапии;
  • метастатический немелкоклеточный рак легкого, устойчивый к химиотерапии на основе производных платины.

Состав

Таблетки, покрытые оболочкой

  • активное вещество — гефитиниб 250 мг
  • вспомогательные вещества: моногидрат лактозы; МКЦ; кроскармеллоза натрия; магния стеарат; повидон; лаурилсульфат натрия;
  • состав оболочки: гипромеллоза; макрогол 300; оксид железа желтый; титана диоксид; оксид железа красный.

Фармакодинамика

Согласно исследованиям, показано, что таблетки Иресса, статистически достоверно увеличивают период до прогрессирования заболевания у больных с метастатическим или местнораспространенным немелкоклеточным раком легкого. Также показано, что гефитиниб, пo сравнению с доцетакселом, создает более положительный профиль переносимости, улучшенное качество жизни и повышенную общую выживаемость у ранее леченых лиц с распространенным немелкоклеточным раком легкого.

Лица, не курившие никогда и имеющие вариант опухоли аденокарцинома, женский пол или являющиеся представителями азиатской расы, гораздо вероятнее будут иметь положительный результат от терапии гефитинибом. Эти клинические характеристики также ассоциируются с высокой частотой мутаций рецептора эпидермального фактора роста опухоли.

Фармакокинетика

Всасывание

После приема внутрь всасывание происходит относительно медленно. Cmax в плазме крови достигается в течение 3–7 ч. Абсолютная биодоступность составляет в среднем 59%. Прием пищи не влияет на биодоступность препарата. При показателе желудочного рН выше 5, биодоступность гефитиниба снижалась на 47%.

Распределение

Регулярное применение препарата 1 раз/сут приводит к увеличению концентрации в 2-8 раз по сравнению с однократным приемом. Css достигается после приема 7-10 доз.

Объем распределения гефитиниба при достижении Css составляет 1400 л, что свидетельствует об экстенсивном распределении препарата в тканях.

Связывание с белками плазмы (с сывороточным альбумином и α1-гликопротеином) составляет приблизительно 90%.

Метаболизм

Гефитиниб подвергается окислительному метаболизму посредством изофермента CYP3A4.

Метаболизм гефитиниба происходит тремя путями: метаболизм N-пропилморфолиновой группы, деметилирование метоксильной группы на хиназолиновую часть и окислительное дефосфорилирование галогенизированной фенильной группы.

Основной метаболит, определяемый в плазме крови человека – О-десметилгефитиниб. Метаболит обладает в 14 раз меньшей активностью по сравнению с гефитинибом в отношении клеточного роста, стимулированного эпидермальным фактором роста, что делает маловероятным его существенное влияние на клиническую активность гефитиниба.

Выведение

Общий плазменный клиренс гефитиниба — приблизительно 500 мл/мин. период полувыведения в среднем составляет 41 час. Препарат выводится в основном с калом. С мочой выводится менее 4% от введенной дозы.

Фармакокинетика в особых клинических случаях

Связи между нижним уровнем Css препарата и возрастом, массой тела, полом, этнической принадлежностью или Cl креатинина не выявлено.

На фоне ежедневного приема препарата Иресса в дозе 250 мг время достижения Css, общий плазменный клиренс и Css были схожи для групп пациентов с нормальной функцией печени и с умеренной печеночной недостаточностью. Данные по 4 пациентам с тяжелой печеночной недостаточностью вследствие метастазов в печень позволяют предположить, что Css у этих пациентов схожа с таковой у пациентов с нормальной функцией печени.

Не исследованы принципы действия Иресса у больных с нарушениями функции печени вследствие цирроза или гепатита.

Фармацевтические характеристики

Круглая, двояковыпуклая таблетка коричневого цвета. Таблетка с пленочной оболочкой, на одной стороне есть надпись «IRESSA» и «250», другая сторона не маркирована. На изломе таблетки ядро белого цвета.

Упаковка, срок годности, условия хранения

Таблетки по 250 мг. По 10 таблеток в блистер из ПВХ/алюминия. По 3 блистера в пакете из алюминиевой фольги. Пакет вместе с инструкцией помещен в картонную пачку с контролем первого вскрытия.

Хранить При температуре не выше 300С в оригинальной упаковке. Хранить в местах, недоступных для детей. Срок годности 4 года. Не применять по истечении срока годности, указанного на упаковке.

При температуре не выше 30 °C (в оригинальной упаковке). Хранить в недоступном для детей месте.

Срок годности препарата Иресса 4 года.

 

 

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 Иресса (Гефитиниб) в Алматы

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Позвоните и узнайте цену Иресса (Гефитиниб)

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

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