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Синагис — Synagis (паливизумаб)

Синагис

Синагис — Synagis (паливизумаб)

Результаты исследований свидетельствуют о положительном эффекте профилактического применения препарата Синагис, с действующим веществом — паливизумаб — у детей, подверженных более высокому риску развития осложнений РСВ-инфекции по сравнению с плацебо. Получавшие паливизумаб дети реже госпитализировались, имели меньшую длительность пребывания в стационаре либо реже нуждались в переводе в палату интенсивной терапии, и принимали кислородную терапию меньшее количество дней, по сравнению с детьми, получавшими плацебо.

Категория:

Описание

Результаты исследований свидетельствуют о положительном эффекте профилактического применения препарата Синагис, с действующим веществом — паливизумаб — у детей, подверженных более высокому риску развития осложнений РСВ-инфекции по сравнению с плацебо. Получавшие паливизумаб дети реже госпитализировались, имели меньшую длительность пребывания в стационаре либо реже нуждались в переводе в палату интенсивной терапии, и принимали кислородную терапию меньшее количество дней, по сравнению с детьми, получавшими плацебо.

Одной из основных причин острых респираторных инфекций у детей является респираторно-синцитиальная вирусная (РСВ) инфекция. РСВ-инфекция может быть причиной заболеваемости, что приводит к госпитализации или смертности у детей.

У большинства инфицированных детей наблюдается мало последствий. Однако, дети, имеющие в анамнезе серьезные проблемы со здоровьем, склонны к более высокому риску осложнений от РСВ-инфекции.

По результатам исследований было показано, что нежелательные (побочные) эффекты, у получавших паливизумаб, детей проявлялись так же часто, как и у детей, принимавших плацебо. Во многих странах профилактика паливизумабом может быть недоступна для стандартного применения из-за высокой стоимости препарата.

Состав Синагис

  • действующее вещество:

1 флакон с маркировкой Синагис 50 мг содержит паливизумаб 50 мг в 0,5 мл;

1 флакон с маркировкой Синагис 100 мг содержит паливизумаб 100 мг в 1 мл;

  • вспомогательные вещества: гистидин, глицин, маннит.
  • 1 ампула с растворителем содержит 1 мл воды для инъекций.

Показания к применению Синагис

У детей, высоким риском развития РСВ-заболевания, для профилактики тяжелого заболевания нижних дыхательных путей, вызванного респираторно-синцитиальным вирусом (РСВ), к которым относятся:

  • недоношенные дети, рожденные на 35 неделе беременности или раньше, к началу сезона РСВ инфекции возраст которых находился до 6 месяцев;
  • детей до 2-х лет, которым в течение последних 6 месяцев была необходима терапия бронхолегочной дисплазии;
  • дети до 2-х лет с гемодинамически значимыми врожденными пороками сердца (ВПС).

Фармакологическое действие

Паливизумаб — это гуманизированные моноклональные антитела иммуноглобулина G1к, взаимодействующие с эпитопом А антигена белка слияния (белок F) респираторного синцитиального вируса. Выраженное нейтрализующее и ингибирующее действие на белки слияния штаммов РСВ подтипов А и В оказывает паливизумаб. Молекула паливизумаба состоит из человеческих (95 процентов) и мышиных (5 процентов) аминокислотных последовательностей. При концентрации в плазме крови хлопковых крыс около 30 мкг/мл паливизумаб снижает репликацию РСВ на 99 процентов.

Резистентность

Все мутации респираторного синцитиального вируса (РСВ), приводившие к устойчивости к паливизумабу, характеризовались аминокислотными заменами в участке белка F. Возникновения резистентности РСВ к связыванию паливизумабом в случае неполиморфных или полиморфных аминокислотных замен в белке F не было отмечено, кроме антигенного участка А. Из 126 клинических изолятов РСВ у 8, полученных от пациентов, не ответивших на профилактику иммунитета, определили как минимум одну из аминокислотных замен, ассоциированных с устойчивостью к паливизумабу (N262D, K272E/Q или S275F/L). Общая частота мутаций, ассоциированных с резистентностью к паливизумабу, составила 6.3 процентов. В антигенном участке А между аминокислотными заменами и тяжестью РСВ-инфекции у детей, которым применяли паливизумаб в качестве профилактически и у которых развилась РСВ-инфекция нижних дыхательных путей анализ клинических данных не выявил взаимосвязи. У пациентов, ранее не получавших иммунопрофилактику паливизумабом, полученный анализ 254 клинических изолятов РСВ, выявил 2 случая мутаций, взаимосвязанных с устойчивостью к паливизумабу (с аминокислотными заменами S275F и N262D соответственно). В общем, частота мутаций, ассоциированных с резистентностью к паливизумабу, составила 0.79 процентов.

Фармакокинетика.

Паливизумаб в исследованиях на здоровых взрослых волонтерах показал фармакокинетический профиль, подобный антителам иммуногобулина G1 человека относительно периода полувыведения (в среднем 18 дней) и объема распределения (в среднем 57 мл/кг). У недоношенных детей и детей с бронхолегочной дисплазией, в исследованиях по профилактике РСВ-инфекции, средний период полувыведения паливизумаба составлял 20 дней, а ежемесячные внутримышечные дозировки 15 мг/кг создавали среднюю 30-дневную концентрацию действующего вещества в сыворотке крови около 40 мкг/мл после первого введения, 60 мкг/мл после второго введения и приблизительно 70 мкг/мл после третьего и четвертого введения.

Сконцентрация препарата в сыворотке крови после первого и четвертой инъекции, у детей, которым вводили паливизумаб в течение второго сезона, составляла от 60 до 90 мкг/мл, соответственно.
средняя концентрация паливизумаба в сыворотке крови, у детей в возрасте 24 месяца с гемодинамически значимыми врождёнными пороками сердца (ВПС), получавшим паливизумаб и которым требовалось сердечно-легочное шунтирование на открытом сердце, была приблизительно 100 мкг/мл перед шунтированием и уменьшалась до 40 мкг/мл после него.

В течение одного сезона РСВ проспективное открытое исследование (фаза II) для оценки иммуногенных и фармакокинетических свойств и безопасности после инъекций 7 доз паливизумаба свидетельствует о том, что у всех 18 детей, включенных в исследование, был достигнут соответствующий средний уровень паливизумаба.

Микробиология.

Противовирусная активность (исследования in vitro).

Противовирусная активность паливизумаба оценивалась методом микронейтрализации. При данном методе, перед добавлением эпителиальных клеток человека НЕр-2, возрастающие концентрации антител были инкубированы с РСВ. В течение 4-5 суток после инкубации РСВ-антиген измерялся методом иммуносорбентного ферментного анализа. Титр нейтрализации (50% эффективной концентрации [ЕС50]) выражается концентрацией антител, необходимой для снижения частоты выявления РСВ-антигена на 50 %, в сравнении с нелечеными инфицированными клетками. Паливизумаб демонстрирует среднее значение ЕС50 0,65 мкг/мл и 0,28 мкг/мл против клинических РСВ А и РСВ В изолятов соответственно. У пациентов из США были отобрано большинство исследованных клинических изолятов (n = 96), остальные из Японии (n = 1), Австралии (n = 5) и Израиля (n = 2). Среди полиморфизмов, выявленных во всем мире, указанные изоляты кодируют наиболее распространенную РСВ F последовательность.

Беременность

Соответствующих исследований не проводилось. Может ли паливизумаб нанести вред плоду при применении его у беременных не известно.

Взаимодействие с другими лекарственными средствами и другие виды взаимодействий

Не проводились исследования взаимодействия с лекарственными препаратами, и не описаны до настоящего времени такие взаимодействия. у детей с бронхолегочной дисплазией (IMpact-RSV), в клиническом исследовании, количество детей в группе паливизумаба и в группе плацебо, которые получали вакцинацию против гриппа, плановые профилактические прививки, кортикостероиды или бронходилятаторы, была одинаковой, и у них увеличение количества побочных реакций не отмечалось.
Не ожидается влияния паливизумаба на поствакцинальный иммунитет, в том числе после применения живых вирусных вакцин, поскольку моноклональные антитела являются специфичными к РСВ.
Взаимодействие и влияние на результаты лабораторных тестов.

На результаты иммунологических диагностических РСВ-тестов паливизумаб может влиять, например, на некоторые тесты, основанных на определении антигена. Паливизумаб в культуре клеток ингибирует репликацию вируса, может также влиять на результаты тестов с использованием вирусных культур. На результаты тестов с применением полимеразной цепной реакции с обратной транскриптазой паливизумаб не влияет. К ошибочно-негативным результатам диагностики РСВ может привести влияние на результаты лабораторных тестов. Следовательно, результаты диагностических тестов следует толковать с учетом клинических данных.

Фармацевтические характеристики

Порошок лиофилизированный. Однородный лиофилизат белого или почти белого цвета. В виде непрессованной сухой таблетки, без посторонних примесей;

готовый раствор — прозрачный или слегка опалесцирующий раствор;

Упаковка, срок годности, условия хранения

Флакон содержит избыток паливизумаба (73 мг для 50 мг, и 122 мг для 100 мг) с целью обеспечения полноты извлекаемого активного вещества.

Объем готового продукта составляет

  • 0.7 мл ± 0.1 мл (номинальный объем 0.5 мл)
  • 1.2 мл ± 0.1 мл (номинальный объем 1 мл)

Флаконы запакованы в пластиковые контейнеры, которые вместе с инструкцией упакованы в картонные пачки.

Хранить препарат следует в недоступном для детей месте при температуре от 2° до 8°С. Не замораживать.

Срок годности — 4 года. Не применять после истечения срока годности, указанного на упаковке.

 

 

 

 

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

 

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