Влияние варфарина, гепарина и новых пероральных прямых антикоагулянтов (дабигатрана этексилата, ривароксабана, апиксабана) на уровень факторов свертывания: V, VII, VIII, IX, XII, WF

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Гепарин применяют в качестве стандартной начальной терапии у пациентов с острой венозной тромбоэмболией. Обычная клиническая практика в этой ситуации состоит в немедленном начале терапии гепарином и назначении варфарина натрия в течение 24 ч; как правило, введение гепарина прекращается через 5 дней. Пациентам с CF-LVAD (вспомогательными устройствами левого желудочка непрерывного тока) также назначают внутривенную терапию нефракционированным гепарином. Гепарин преимущественно оказывает антикоагулянтное действие, катализируя антитромбин, что приводит к ингибированию факторов II (тромбина), X и в меньшей степени IX, XI и XII.

В течение последних 50 лет варфарин является наиболее широко используемым антикоагулянтным препаратом из группы антагонистов витамина K для лечения пациентов с риском развития артериального и венозного тромбоза. Из-за неблагоприятной фармакокинетики он имеет малое терапевтическое окно, требует частого мониторинга и восприимчив к взаимодействию с лекарственными препаратами и пищевыми продуктами. Кроме того, эффект варфарина не ограничивается влиянием на гемостаз, он также воздействует на все витамин-K-зависимые белки. Варфарин оказывает антикоагулянтное действие, уменьшая функциональные уровни витамин-K-зависимых факторов II, VII, IX и X. В то же время синтез двух физиологических антикоагулянтов — белков C и S — блокируется. Варфарин конкурирует с витамином K, таким образом нейтрализуя действие этого витамина.

Новые пероральные прямые антикоагулянты: прямой ингибитор тромбина — дабигатран и ингибиторы фактора Xa — ривароксабан и апиксабан — были разработаны как альтернатива варфарину. Они также демонстрируют негемостатические сосудистые эффекты через протеазоактивированные рецепторы (PARs).

Об авторах

Дарья Евгеньевна Гуляихина

ФГБОУ ВО «Северо-Западный государственный медицинский университет им. И.И. Мечникова» Минздрава России

Автор, ответственный за переписку.
Email: gde81@mail.ru
ORCID iD: 0000-0002-5208-669X

Ассистент кафедры трансфузиологии 

Россия, 191015, Санкт-Петербург, ул. Кирочная, 41

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3. Рис. 2. Терапевтические подходы, включающие введение витамина К: СЗП — свежезамороженная плазма, АЧТВ — активированное частичное тромбопластиновое время

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