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Неуластим — Neulastim (Пэгфилграстим)

Неуластим (Пэгфилграстим)

Неуластим — Neulastim (Пэгфилграстим)

Препарат Неуластим относится к гемопоэтическим факторам роста. Препарат производится из культур клеток Escherichia coli с помощью технологии рекомбинантных ДНК с последующей конъюгацией с полиэтиленгликолем (ПЭГ). Действующее вещество неуластима — Пэгфилграстим — это ковалентный конъюгат филграстима. Филграстим — рекомбинантный человеческий гранулоцитарный колониестимулирующий фактор (Г-КСФ), с одной молекулой полиэтиленгликоля (ПЭГ). Пэгфилграстим, аналогично филграстиму, корректирует формирование и высвобождение нейтрофилов из костного мозга, заметно повышает количество нейтрофилов с нормальной или повышенной функциональной активностью (хемотаксис и фагоцитоз) в периферической крови в течение 24 часов и вызывает небольшое повышение количества лимфоцитов и/или моноцитов. Г-КСФ может стимулировать эндотелиальные клетки in vitro, как и другие гемопоэтические факторы роста.

Категория:

Описание

Препарат Неуластим относится к гемопоэтическим факторам роста. Препарат производится из культур клеток Escherichia coli с помощью технологии рекомбинантных ДНК с последующей конъюгацией с полиэтиленгликолем (ПЭГ). Действующее вещество неуластима — Пэгфилграстим — это ковалентный конъюгат филграстима. Филграстим — рекомбинантный человеческий гранулоцитарный колониестимулирующий фактор (Г-КСФ), с одной молекулой полиэтиленгликоля (ПЭГ). Пэгфилграстим, аналогично филграстиму, корректирует формирование и высвобождение нейтрофилов из костного мозга, заметно повышает количество нейтрофилов с нормальной или повышенной функциональной активностью (хемотаксис и фагоцитоз) в периферической крови в течение 24 часов и вызывает небольшое повышение количества лимфоцитов и/или моноцитов. Г-КСФ может стимулировать эндотелиальные клетки in vitro, как и другие гемопоэтические факторы роста.

Лейкоцитоз (Транзиторное увеличение лейкоцитов) является ожидаемым последствием терапии пэгфилграстимом, т.к. соответствует его фармакодинамическим свойствам. Каких-то определенных побочных явлений, непосредственно связанных с таким лейкоцитозом, не показано.

Показания препарата Неуластим

При цитотоксической химиотерапии по поводу злокачественных заболеваний для снижения:

  • продолжительности нейтропении;
  • частоты возникновения фебрильной нейтропении;
  • частоты развития инфекций, проявляющихся фебрильной нейтропенией.

Состав

Каждый предварительно заполненный шприц (0,6 мл) содержит:

  • Активное вещество: пэгфилграстим — 6 мг (концентрация 10 мг/мл рассчитана только для белка, если включен фрагмент ПЭГ, концентрация составляет 20 мг/мл.);
  • Вспомогательные вещества: натрия ацетат — q.s. до pH 4,0, сорбитол, полисорбат-20, вода для инъекций;

Фармакодинамика

Пэгфилграстим является пролонгированной формой филграстима вследствие снижения почечного клиренса. Было показано, что пэгфилграстим и филграстим имеют сходный механизм действия, создавая значительное повышение количества нейтрофилов в периферической крови в течение 24 часов и незначительное повышение лимфоцитов и/или моноцитов. Нейтрофилы, образовавшиеся в ответ на воздействие пэгфилграстима, аналогично как при воздействии филграстима, показывают нормальную или увеличенную функциональную активность. Данный факт подтверждается с помощью теста хемотаксиса фагоцитарной функции. Как и другие гемопоэтические факторы роста, Г-КСФ in vitro может стимулировать эндотелиальные клетки человека.Г-КСФ может содействовать росту миелоидных клеток, в том числе злокачественных клеток, аналогичные эффекты могут наблюдаться in vitro для некоторых немиелономных клеток.

Клиническая эффективность

При однократном введении пэгфилграстима после каждого цикла миелосупрессивной цитостатической терапии укорачивает продолжительность нейтропении и снижает частоту возникновения фебрильной нейтропении эквивалентно ежедневному введению филграстима (в среднем, 11 ежедневных введений). Кроме того показано, что использование пэгфилграстима после химиотерапии значительно снижает частоту в/в инфузий противомикробных лекарств и госпитализации в связи с фебрильной нейтропенией.

Фармакокинетика

Всасывание

После однократного подкожного введения дозы пэгфилграстима, максимальная концентрация в сыворотке крови наблюдается в период от 16 до 120 часов.

Распределение

Концентрация пэгфилграстима, после миелосупрессивной химиотерапии, в сыворотке крови поддерживается в течение периода нейтропении.

Распределение пэгфилграстима ограничено плазмой.

Выведение

Выведение пэгфилграстима нелинейное, дозозависимое, насыщаемое. Клиренс, в основном, осуществляется нейтрофилами (>99%) и снижается с увеличением дозы пэгфилграстима. Концентрация пэгфилграстима, в соответствии с саморегулирующимся механизмом клиренса, в сыворотке быстро снижается с началом восстановления числа нейтрофилов.

Фармакокинетика у особых групп пациентов

С учетом клиренса с участием нейтрофилов, считается, что фармакокинетика пэгфилграстима при почечной или печеночной недостаточности не изменяется. В открытом исследовании однократной дозы (n = 31) различные стадии нарушения функции почек, в том числе терминальная стадия почечной недостаточности, не оказывали влияния на фармакокинетику пэгфилграстима.

Пожилые пациенты

Имеющиеся ограниченные данные о фармакокинетика пэгфилграстима у пожилых пациентов (> 65 лет) свидетельствтуют, что она сходна с фармакокинетикой у взрослых.

Доклинические данные по безопасности

По данным доклинических исследований о токсичности многократной дозы, выявили ожидаемые фармакологические эффекты, включая увеличение количества лейкоцитов, экстрамедуллярный гематопоэз, миелоидную гиперплазию в костном мозге и увеличение селезенки.

У потомства беременных крыс, получавших пэгфилграстим подкожно, не было отмечено каких-либо побочных эффектов, в то время как у кроликов пэгфилграстим оказал токсическое действие на эмбрион/плод (потеря эмбрионов) при кумулятивных дозах, которые примерно в 4 раза превышали рекомендуемую дозу для человека. Токсическое действие не наблюдалось у беременных кроликов, которые были подвергнуты воздействию дозы, рекомендованной для человека. В исследованиях на крысах было показано, что пэгфилграстим может проникать через плаценту. Исследования на крысах показали, что влиянию пэгфилграстима, который вводился подкожно, репродуктивные характеристики, фертильность, дни между спариванием и коитусом и внутриутробная выживаемость не подвергались. Актуальность этих данных для человека неизвестна.

Фармацевтические характеристики

Прозрачная бесцветная жидкость.

Упаковка, срок годности, условия хранения

Раствор для подкожного введения — шприц-тюбик 0,6 мл пэгфилграстим — 6 мг вспомогательные вещества в шприц-тюбике 0,6 мл, в комплекте с иглой для инъекций; в картонной пачке 1 комплект.

Хранить в защищенном от света месте, при температуре 2–8 °C, в оригинальной упаковке (не замораживать). Хранить в недоступном для детей месте.

Срок годности раствора для подкожного введения 10 мг/мл — 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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Неуластим (Пэгфилграстим)

Работаем и отправляем Неуластим (Пэгфилграстим) по странам СНГ: Россия, Украина, Кыргызстан (Бишкек), Белоруссия, Узбекистан (Ташкент),
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