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Тасигна — Tasigna (Нилотиниб) 150мг, 200 мг

Тасигна (нилотиниб) 150мг , 200 мг , Новартис , Швейцария

Тасигна — Tasigna (Нилотиниб) 150мг, 200 мг

Компания Medical&Pharma предлагает современное лекарство Тасигна (Нилотиниб) — это противоопухолевое средство, содержит активное вещество Нилотиниб. Препарат эффективно ингибирует тирозинкиназную активность у взрослых с хроническим миелолейкозом (ХМЛ) , а также у первично положительных лейкозных клеток по филадельфийской хромосоме (Ph-положительных). Тирозинкиназы — это белки, стимулирующие рост раковых клеток. Белки производятся клетками ХМЛ, они имеют аномальную филадельфийскую хромосому. Нилотиниб блокирует белок тирозинкиназы, препятствуя тем самым росту и распространению раковых клеток, и индуцируя у них апоптоз.

Категория:

Описание

Компания Medical&Pharma предлагает современное лекарство Тасигна (Нилотиниб) — это противоопухолевое средство, содержит активное вещество Нилотиниб. Препарат эффективно ингибирует тирозинкиназную активность у взрослых с хроническим миелолейкозом (ХМЛ) , а также у первично положительных лейкозных клеток по филадельфийской хромосоме (Ph-положительных). Тирозинкиназы — это белки, стимулирующие рост раковых клеток. Белки производятся клетками ХМЛ, они имеют аномальную филадельфийскую хромосому. Нилотиниб блокирует белок тирозинкиназы, препятствуя тем самым росту и распространению раковых клеток, и индуцируя у них апоптоз.

Состав

Одна капсула 150 мг содержит

  • 165,45 мг нилотиниба гидрохлорида моногидрата, что эквивалентно 150 мг нилотиниба безводного основания;
  • дополнительные вещества: моногидрат лактозы, полоксамер 188, кросповидон, стеарат магния, диоксид кремния коллоидный безводный;
  • оболочка капсулы: желатин, титана диоксид, железа оксид красный, железа оксид желтый,
  • чернила: шеллак, пропиленгликоль, калия гидроксид, краситель железа оксид черный, вода.

Одна капсула 200 мг содержит

  • 220,6 мг нилотиниба гидрохлорида моногидрата, что эквивалентно 200 мг нилотиниба безводного основания;
  • дополнительные вещества: моногидрат лактозы, полоксамер 188, кросповидон, стеарат магния, кремния диоксид коллоидный безводный;
  • оболочка капсулы: желатин, титана диоксид, железа оксид красный, железа оксид желтый,
  • чернила: шеллак, пропиленгликоль, краситель железа оксид красный, калия гидроксид, вода.

Показания

  • Лечение взрослых пациентов с впервые диагностированным хроническим миелолейкозом, положительным по филадельфийской хромосоме (Ph+ ХМЛ) в хронической фазе.
  • Лечение Ph+ ХМЛ в хронической фазе и в фазе акселерации взрослых пациентов с резистентностью или непереносимостью терапии с иматинибом.

Фармакологическое действие

Нилотиниб — эффективно ингибирующее тирозинкиназную активность Bcr-Abl онкопротеина клеток, а также первично положительных лейкозных клеток по филадельфийской хромосоме (Ph-положительных).

Вещество обладает большим сходством к участкам связывания с АТФ и, именно поэтому, оказывает ингибирующее действие на BCR-ABL онкопротеин дикого типа, и при этом показывает активность в отношении 32 из 33 основных -резистентных к иматинибу мутантных форм BCR-ABL-тирозинкиназы. Нилотиниб избирательно подавляет пролиферацию клеточных линий и Ph- положительных лейкозных клеток у пациентов с хроническим миелолейкозом (ХМЛ), а также индуцирует у них апоптоз. Вещество не оказывает или оказывает незначительное влияние на другие известные протеинкиназы.

Фармакокинетика

Абсорбция

Максимальной концентрации в плазме крови нилотиниб достигает в среднем за 3 часа. Абсорбция нилотиниба после перорального применения — около 30%. Абсолютная биодоступность нилотиниба не определена. Относительная биодоступность капсул нилотиниба составляет примерно 50%.

При одновременном приеме препарата с пищей у здоровых добровольцев максимальная концентрация (Сmах) и площадь под кривой «концентрация-время» (AUC) нилотиниба повышались на 112% и 82%, соответственно, по сравнению с применением нилотиниба натощак. Применение препарата через 30 мин или 2 ч после приема пищи повышало биодоступность нилотиниба на 29% и 15%, соответственно. У пациентов, перенесших тотальную или частичную гастрэктомию, всасывание нилотиниба (относительная биодоступность) снижается приблизительно на 48% и 22%, соответственно.

Распределение

Соотношение концентраций нилотиниба в крови и плазме составляет 0,71. Связь с белками плазмы in vitro составляет около 98%.

В равновесном состоянии системная экспозиция нилотиниба была дозозависимой.

Плазменная экспозиция нилотиниба в период между приемом первой дозы и достижением равновесной концентрации повышается примерно в 2 раза при применении лекарства один раз в сутки и в 3,8 раз при приеме препарата два раза в сутки. Равновесная концентрация достигалась к 8-му дню.

Метаболизм

Основными способами метаболизма нилотиниба у здоровых добровольцев являются гидроксилирование и окисление. В плазме крови нилотиниб циркулирует в основном в неизменной форме. Все метаболиты нилотиниба обладают незначительной фармакологической активностью.

Выведение

После однократного применения нилотиниба у здоровых добровольцев более 90% дозы выводится в течение 7 дней в основном с калом. 69% препарата выводится в неизмененном виде. При многократном применении суточной дозы период полувыведения составлял приблизительно 17 часов.

При применении лекарства у больных с нарушениями функции печени значительного изменения фармакокинетических параметров не отмечалось. При однократном приеме лекарства отмечалось снижение AUC нилотиниба на 35%, 35% и 19% у пациентов с нарушением функции печени легкой, средней и тяжелой степени (по сравнению с больными без нарушений функции печени). Сmaх нилотиниба в равновесном состоянии увеличивалась на 29%, 18% и 22%, соответственно.

Особые группы пациентов

Нарушение функции печени.

Не наблюдалось значительных изменений фармакокинетических параметров нилотиниба у больных с нарушениями функции печени. Коррекция режима дозирования препарата Тасигна у данной категории больных не требуется, однако требуется применять Тасигна с осторожностью.

Нарушение функции почек.

Данных по использованию лекарства у больных с нарушением функции почек нет (концентрация креатинина в плазме в 1,5 раза >ВГН). Ввиду того, что почки не играют важной роли в выведении нилотиниба и его метаболитов, то у данной категории пациентов не ожидается снижение общего клиренса при применении препарата Тасигна.

Пациенты ≥65 лет.

Не выявлено существенных различий в безопасности и эффективности использования Тасигна у данной категории больных в сравнении с пациентами от 18 до 65 лет.

Дети (до 18 лет).

Не изучена эффективность и безопасность препарата у детей и подростков до 18 лет.

Фармацевтические характеристики

Капсулы с порошоком белого или желтоватого цвета:

  • в дозировке по 150 мг. Красные матовые непрозрачные твердые желатиновые капсулы № 1; с черными, расположенными по оси надписями «NVR» и «BCR».
  • в дозировке по 200 мг. Светло-желтые матовые твердые желатиновые капсулы №0; с красными, расположенными по оси надписями «NVR» и «ТК1».

Упаковка, срок годности, условия хранения

Препарат выпускают в виде капсул упакованных:

  • по 4 капсулы в блистере, по 7 блистеров в картонной коробке
  • по 14 капсул в блистере, по 2 блистера в картонной коробке.

Срок годности 3 года.

Хранить в оригинальной упаковке. Хранить в недоступном для детей месте, при температуре не выше 30°C.

 

 

 

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

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