Дабигатран – это антикоагулянт, который обладает прямым действием.
Имеет торговое название Прадакса. Международное непатентованное название — дабигатрана этексилат.
Это средство чаще всего применяется в общей хирургии для лечения тромбозных состояний различного генеза, а также в целях профилактики тромбозных и тромбоэмболических патологий и прединсультных состояний.
Фармакологическое действие
Дабигатран (Dabigatran) входит в группу средств, которые обладают ингибирующим действием по отношению к тромбину. Основной компонент средства – дабигатрана этексилат. Этот компонент относят к пролекарствам с низкомолекулярным типом. Он не имеет фармакологической активности.
Во время применения этого средства происходит быстрое всасывание основного вещества и при помощи гидролиза, который катализируется эстеразами, происходит его превращение в дабигатран.
Средство относится к препаратам, ингибирующим тромбин, который имеет активное, конкурентное и обратимое воздействие. Его главное влияние происходит в составе плазмы крови.
Во время каскадного процесса коагулятивного действия происходит превращение тромбином (сериновой протеазой) фибриногена в фибрин.
В результате снижения активного состояния тромбина возникает предотвращение появления тромбов. А сам Дабигатран обладает ингибирующим воздействием на свободный тромбин, на тромбин фибриносвязывающего типа, а также влияет на агрегацию тромбоцитов, которая вызвана тромбином.
Фармакокинетические свойства
Препарат обладает следующими фармакокинетическими свойствами:
- Всасывание. При применении лекарства внутрь в плазме крови происходит моментальное повышение уровня концентрации с достижением Cmax от 30 минут до 120 минут. После того как дабигатран достигает максимального уровня концентрации происходит его биэкспоненциальное снижение. В итоге конечный полупериод концентрации активного вещества у молодых людей составляет от 14 до 17 часов, у пожилых людей от 12 до 14 часов. Показатель абсолютной биодоступности дабигатрана этексилат составляет 6,5 %.
- Выведение. Основной уровень выведения препарата происходит через почки, почти 85 %. Через почки средство выводится в неизменном виде. Вместе с калом выводится около 6 % от введённой дозировки препарата. В последующие 168 часов после введения лекарственного средства происходит выведение общей радиоактивности в пределах 88-94 % от общей введенной дозы препарата.
Форма выпуска и составляющие компоненты
Препарат Дабигатран выпускается в виде капсул, продолговатой формы, непрозрачного цвета. Корпус капсулы выполнен в кремовой расцветке и имеет пометку дозировки «R 75» или «R 110».
Сверху имеется крышка, которая обладает светло-синей расцветкой, на ней указана символика фирмы-производителя Берингер Ингельхайм. Внутри капсул имеются пеллеты желтого цвета.
- Основной компонент — дабигатрана этексилат. В одной капсуле с пометкой «R75» его уровень содержания составляет 86,48 мг. В капсуле с пометкой «R110» его содержание достигает 126,83 мг.
- Дополнительные составляющие – акация камедь, винная кислота (крупнозернистого типа в виде кристаллов или порошка), небольшой уровень гипромеллозы, диметикона, а также тальк, гипролоза.
- Компоненты, входящие в состав оболочки — каррагинан (E407), калия хлорид, титана диоксид (E171), индигокармин (E132), краситель солнечный закат желтый (E110), гипромеллоза, вода в очищенном виде.
Сфера применения
Дабигатран назначается при следующих состояниях:
- во время профилактического лечения тромбоэмболического заболевания венозного характера у больных после ортопедических оперативных вмешательств;
- с целью профилактики инсульта и тромбоэмболического заболевания системного течения;
- для лечения тромбоза глубоколежащих вен, а также при тромбоэмболическом заболевании легочной артерии, — применяется для профилактической терапии с целью снижения смертности при этих патологиях;
- для профилактического лечения при тромбозном заболевании глубоколежащих вен с рецидивирующим течением.
Препарат опасен: противопоказания и «побочки»
У Дабигатрана большое количество противопоказаний и возможных побочных эффектов. Так, данный препарат не рекомендуется применять в следующих ситуациях:
- при наличии почечной недостаточности с тяжелым течением;
- различные поражения внутренних органов из-за сильного кровотечения, а также инсульт с геморрагическим характером;
- наличие кровотечения активного вида, а также диатез с геморрагическим течением, проблемы процесса гомеостаза спонтанного или фармакологически индуцированного типа;
- если имеется большой риск возникновения сильных кровотечений, которые связаны с язвенными заболеваниями желудка и кишечника, из-за злокачественных опухолевых процессов и образований, недавнего повреждения головного мозга или спинного;
- если пациенту недавно проводилось оперативное вмешательство на головном или спинном мозге, или же офтальмологические операции;
- у пациента в анамнезе присутствует недавнее внутричерепное кровоизлияние;
- если имеется или подозревается варикозное заболевание пищевода, наличие врожденных артериовенозных нарушений, сосудистых аневризм или больших внутрипозвоночных или внутримозговых сосудистых патологий;
- при нарушениях функционирования печени и почек;
- возраст до 18 лет;
- возрастная категория людей 75 лет и более;
- если имеется протезированный клапан сердца;
- повышенная чувствительность к активному составляющему средства.
Кроме этого следует с осторожностью применять медикамент при следующих показаниях:
- при массе тела пациента менее 50 килограмм;
- одновременный прием ингибиторов с Р-гликопротеином;
- при наличии врожденных или приобретенных заболеваний связанных с нарушением свертываемости крови;
- при эндокардите бактериального типа;
- при эзофагите, гастрите или гастроэзофагеальном рефлюксном заболевании.
Побочные явления
Среди побочных действий наблюдаются следующие состояния:
- состояние анемии и тромбоцитопении;
- иногда могут возникать гематомы, сильные кровотечения из ран, появления кровотечений из носа, повышенное выделение крови из желудка и кишечника, кровоточивость из прямой кишки, кровотечения с геморроидальным характером, возникновение кожного геморрагического синдрома, гематурия, гемартроз;
- нарушения функционирования печени;
- появление гипербилирубинемии;
- иногда может снизиться гемоглобин и гематокрит.
Исследований о том можно ли применять Дабигатран в период беременности, нет. Но все же многие специалисты не советуют принимать данный препарат беременным женщинам, потому что его составляющие компоненты могут оказать токсическое воздействие на плод.
Кормление грудью в период лечения с помощью препарата стоит прекратить. Составляющие компоненты могут попасть в состав молока.
Как применять препарат: дозировки и схема назначений
Капсулы препарата принимаются внутрь. В сутки нужно принимать 1 или 2 раза. Принимать можно перед едой или после приема пищи, капсулы запиваются небольшим количеством воды.
Как изъять капсулы из блистера:
- капсулы следует вынуть из блистера, фольга отслаивается;
- ни в коем случае не выдавливайте капсулы из фольги;
- фольгу следует удалить так, чтобы потом можно было с легкостью вынуть капсулу.
Дозировки в зависимости от целей терапии и сопутствующих рисков:
- При профилактическом лечении тромбозного заболевания у больных после ортопедических оперативных вмешательств рекомендуется принимать по 220 мг препарата 1 раз в 24 часа. В сутки принимается 2 капсулы по 110 мг.
- При профилактическом лечении инсульта и тромбоэмболии с системным течением препарат принимается в дозировке 300 мг в сутки. Каждые 12 часов нужно принимать по 2 капсулы с дозировкой 75 мг. Терапия продолжается пожизненно.
- При тромбозном заболевании глубоких вен и легочной артерии в сутки следует принимать 300 мг препарата. Каждые 12 часов следует принимать по 2 капсулы объемом по 75 мг. Длительность терапии составляет полгода.
- При тромбозном заболевании глубоких вен рецидивирующего характера следует в сутки принимать по 300 мг препарата. Каждые 12 часов принимается по 2 капсулы с объемом каждой 75 мг. Терапия длится пожизненно.
Рекомендуем к изучению — отзывы специалистов
Из отзывов врачей, которые применяют в практической деятельности Дабигатран.
Дабигатран или Прадакса – это антикоагулянт, который оказывает эффективное воздействие при лечении тромбозных и тромбоэмболических заболеваний. Я считаю, что данное средство обладает хорошим действием и всегда приносит положительный результат.
Часто назначаю своим пациентам при серьезных формах тромбоза глубоких вен и тромбоэмболии. Многие из них отмечают, что почти с первых дней применения у них намного улучшилось самочувствие. Однако данный препарат обладает большим количеством противопоказаний и побочных явлений, которые могут нанести серьезный вред здоровью.
Специалист флеболог
Я часто назначаю своим пациентам Дабигатран. На мой взгляд, это одно из эффективных средств лечения тромбозных и тромбоэмболических заболеваний.
Он намного облегчает течение острых форм патологий, снижает воспаление, боли. Но все-таки этот препарат имеет много противопоказаний и побочных явлений, поэтому его принимать стоит с особой осторожностью и только по показаниям врача.
Заведующий палатой интенсивной терапии
Из практики применения
Слово берут пациенты.
После полного обследования у флеболога мне поставили диагноз тромбоз глубоких вен с рецидивирующим течением. Мне врач назначил прием препарата Дабигатран.
В сутки я принимаю по 300 мг этого средства. Курс лечения пожизненный. После того, как начала принимать это лекарство мое состояние намного улучшилось, пропали боли и дискомфорт.
Галина, 57 лет
У меня уже давно тромбоз и тромбоэмболия. После консультации и обследования, врач назначил принимать Дабигатран. В сутки я принимаю по 2 капсулы во 110 мг. Курс лечения 6 месяцев. В течение этого периода я заметил положительные результаты. Мое состояние стало намного лучше, прошло воспаление, пропали сильные боли. Я стал себя чувствовать намного легче.
Константин, 62 года
Цена кусается
Цена упаковки Дабигатрана с 60 капсулами 110 мг составляет около 2800-3000 рублей, за упаковку с 10 капсулами 75 мг 100-1200 рублей и с 30 капсулами 150 мг 1400-1700 рублей.
Аналоги Дабигатрана, на которые можно заменить препарат при необходимости или при отсутствии его в атеках:
Лекарство назначается под контролем лечащего врача, который устанавливает необходимую дозировку. Применяется у людей, которые подверглись ортопедическому оперативному вмешательству, помогая предотвратить развитие венозной тромбоэмболии. Также, прадакса применяется для профилактики инсультов и при атриальной фибрилляции для предотвращения сердечно-сосудистых кризов.
Препарат обладает значительным перечнем противопоказаний:
- почечная недостаточность;
- кровотечения различного генеза;
- диатез геморрагического характера;
- одномоментное применение совместно с кетоконазолом;
- возраст менее 18-и лет;
- печеночная недостаточность;
- нарушения в работе внутренних органов, сопровождаемые кровотечениями;
- коагулопатии.
Обратите внимание! Во время вынашивания ребенка лекарство допускается применять только в ситуациях, которые непосредственно угрожают жизни матери. В целях предосторожности, необходимо остановить вскармливание грудью на время лечения.
Дженерики Прадаксы, выпускаемые в России
Производство препарата «Прадакса» осуществляется на территории Австрии и Германии. Основным недостатком лекарства является его высокая стоимость. Упаковка с десятью капсулами стоит порядка 600-700 рублей, а 180 капсул – около 8-9 тысяч.
Отечественные производители предлагают ряд аналогов медикамента, которые можно приобрести по более доступным ценам.
- Варфарин. Это медикамент, предотвращающий излишнюю свертываемость крови. Представляет собою лекарство старого поколения, наиболее дешевый аналог прадаксы, представленный на отечественном рынке. Стоимость в среднем составляет до 200 рублей. Применяется при тромбоэмболии вен и артерий, в том числе, магистральных; рекомендован для профилактики инфаркта миокарда. Инструкция включает в себя детальное описание противопоказаний и возможных побочных эффектов.
- Фраксипарин Форте. Препарат является одним из ближайших заменителей прадаксы. Выпускается в форме раствора для инъекций. Демонстрирует эффективное действие при лечении тромбоэмболии сосудов или тромбозов. Противопоказан при возрасте менее 18-и лет, не рекомендуется применять больным с кровотечениями, недостаточностью – почечной или печеночной, людям, страдающим повышенным кровеносным давлением. Средняя стоимость достигает 650 рублей.
Заменители Прадаксы на украинском рынке
В случаях, когда представляется невозможным применение прадаксы, более бюджетные дженерики могут стать единственным и хорошим выходом из ситуации.
- Атерокард. В качестве активного вещества выступает клопидогрел. Препарат входит в группу антикоагулянтов, средняя стоимость находится в диапазоне от 100 до 350 рублей. Выпуск лекарства производится в форме таблеток. Применяется для предотвращения развития атеротромбоза.
- Фенилин Здоровье. Медикамент, предназначенный для предотвращения тромбозов. Выпускается в таблетированной форме, содержит в себе фениндион. Достаточно бюджетный аналог прадаксы. Стоимость составляет порядка 40-60 рублей.
- Магникор. Это лекарственное средство содержит в себе гидроксид магния, сочетаемый с ацетилсалициловой кислотой. Относится к группе лекарств антитромботического рода. Стоимость обычно не превышает 170 рублей.
Дженерики средства из Белоруссии
Те пациенты, что нуждаются в высококачественной замене прадаксы на более бюджетный медикамент, могут использовать следующие аналоги:
- Гепарин. Максимальная стоимость препарата может достигать 500 рублей. Выпуск лекарства производится в форме раствора, предназначенного для инъекций под кожу или внутривенно. Помимо этого, клопидогрел доступен в форме геля или мазей для наружного применения. Используется препарат с целью предотвращения развития тромбозов или эмболий.
- Клопидогрел. Данный медикамент представляет собою вещество из группы антикоагулянтов, которое весьма успешно применяется для снижения уровня агрегации тромбоцитов. Используется для профилактики атеротромботических нарушений. Применяется пациентами, у которых выявлен ОКС (острый коронарны й синдром). Стоимость препарата не превышает 350 рублей.
Аналоги Прадаксы иностранного производства
Существует ряд заменителей Прадаксы, которые являются импортными, но при этом – более дешевыми и не менее эффективными.
- Варфарин Никомед. Активным веществом в данном медикаменте является варфарин. Показания для применения и противопоказания схожи с аналогичными для варфарина. Производится препарат на территории Дании, Польши, а также в Японии. В среднем, стоимость составляет 150 рублей.
- Синкумар. Это антикоагулянт непрямого действия, основанный на аценокумароле. Выпускается медикамент в таблетированной форме, производство располагается в Германии, а также в Венгрии. Стоимость может достигать 400 рублей.
- Варфарекс. Это один из наиболее хороших импортных дженериков прадаксы, который основан на варфарине. Препарат латвийского производства, стоимость обычно не превышает 220 рублей.
- Ксарелто. Активным веществом в лекарственном средстве является ривароксабан. Антикоагулянт прямого действия, который используется для предотвращения тромбоэмболии вен после проведенных оперативных вмешательств на опорно-двигательном аппарате.
У данного средства имеются противопоказания – существует риск возникновения активных кровотечений. Запрещается применение лекарства во время беременности, в периоды вскармливания малышей грудью, а также в возрасте до 18 лет. Нижняя планка стоимости начинается от полутора тысяч рублей.
Лекарственный препарат Прадакса, а также его дженерики или ближайшие заменители входят в число медикаментов, применяемых в ситуациях, которые могут угрожать здоровью или жизни человека.
Ни в коем случае не рекомендуется самостоятельное назначение и применение антикоагулянтов без консультации с лечащим врачом. Препарат, который подобран неправильно, а также ошибка при выборе дозировке превращают качественный медикамент в сильный яд.
В случае передозировки существует сильная вероятность того, что разовьется спонтанное и активное кровотечение. Риск чрезмерно высок, поэтому не следует ставить под угрозу собственную жизнь, пытаясь сэкономить деньги или время на консультации у профессионала. Для предотвращения необдуманных и неверных решений следует четко осознавать эту простую истину.
Прадакса – это серьёзный лекарственный препарат из группы антикоагулянтов. Эти вещества способны препятствовать образованию тромбов путём угнетения активности тромбина. Действующее вещество этексилат дабигатрана положительно влияет на фактор свёртываемости плазмы крови, а также воздействует на агрегацию тромбоцитов и фибриновые сгустки.
Назначение лекарства, как и установление необходимой дозировки, должно быть согласовано с лечащим врачом и находиться под его постоянным контролем. Неправильное назначение медикамента может обернуться опасным геморрагическим расстройством.
Средство имеет внушительный список противопоказаний, среди которых почечная недостаточность, кровотечения различного происхождения, геморрагический диатез, нарушения гемостаза, внутренние поражения органов, сопровождающиеся кровотечениями, одновременное применение кетоконазола, печёночная недостаточность, возраст до 18 лет.
Аналоги российского производства
Прадакса производится в Германии и Австрии. Форма выпуска – капсулы. Цены высокие, что является главным недостатком медикамента. Упаковка с 10 таблетками обойдётся в 670 рублей, пачка с 180 штуками – 8670 рублей.
Дешёвые аналоги препарата прадакса от отечественного производителя включает таблица ниже:
Наименование препарата | Средняя цена в рублях | Характеристика |
Варфарин | 90–190 | Препарат, препятствующий излишней свёртываемости, антикоагулянт старого поколения. Самый дешёвый близкий заменитель прадаксы российского производства. |
В аптеках также встречается это средство белорусского происхождения.
Область применения охватывает такие заболевания, как тромбоз и эмболия сосудов, эмболия лёгочной артерии, венозный тромбоз, профилактика инфаркта миокарда, при тромбоэмболических нарушениях у пациентов с фибрилляцией предсердий, после ортопедических вмешательств.
В инструкции подробно указаны противопоказания и побочные эффекты.
Средство продаётся в виде раствора для инъекционного введения. Антикоагулянт прямого влияния, которым эффективно лечат тромбозы и тромбоэмболии.
Недорогой близкий заменитель прадаксы.
Препарат не назначают детям до 18 лет, беременным, больным с нарушениями кровообращения или кровотечением, при печёночной, почечной недостаточности, тромбоцитопении, артериальной гипертензии, лицам с массой тела менее 40 кг.
Украинские заменители
При невозможности использовать препарат прадакса, аналоги более дешёвые становятся отличным выходом из положения. Лекарства украинского производства подскажут чем заменить дорогое средство.
- Фенилин Здоровье. Антитромботическое средство, таблетки с фениндионом. Антикоагулянт из категории «подешевле». Средняя цена 40–55 рублей.
- Атерокард. Активное вещество – клопидогрел. Антикоагулянт. Средняя цена 95–370 рублей.
- Магникор. Антитромботическое лекарство с ацетилсалициловой кислотой и гидроксидом магния в составе лекарства. Средняя цена 60–120 рублей.
Белорусские дженерики
Белорусские дженерики лекарства прадакса помогут пациентам, которым требуется качественная замена на дешёвый медикамент.
Наименование препарата | Средняя цена в рублях | Характеристика |
Гепарин | 330–490 | Выпускается в виде раствора для внутривенного или подкожного введения, а также в виде мази и геля. |
Применение включает лечение и профилактику тромбоэмболий и тромбозов.
Применяется при профилактике атеротромбических случаев, а также у пациентов с острым коронарным синдромом.
Прочие иностранные аналоги
Современные импортные синонимы прадаксы представлены в нижеприведённом списке:
- Варфарекс. Лучший недорогой зарубежный заменитель прадаксы на основе варфарина. Страна производитель – Латвия. Средняя цена 115–215 рублей.
- Варфарин Никомед. Действующее вещество в лекарстве – варфарин. Имеет аналогичные отечественному варфарину показания и противопоказания. Препарат производят в Польше, Японии, Дании. Средняя цена 110–180 рублей.
- Варфарин Орион. Состав лекарства включает варфарин. Страна производитель – Финляндия. Средняя цена 150–390 рублей.
- Синкумар. Непрямой антикоагулянт на основе аценокумарола. Форма выпуска – таблетки. Препарат производится в Венгрии и Германии. Средняя цена 365–390 рублей.
- Ксарелто. Действующее вещество – ривароксабан. Прямой антикоагулянт, применяющийся в качестве профилактики возникновения венозной тромбоэмболии после ортопедических хирургических вмешательств.
Средство имеет противопоказания, основные из них связаны с наличием или риском развития активного кровотечения.
Препарат категорически запрещён при беременности, в период грудного вскармливания и в детском и подростковом возрасте. Страна производитель – Германия, Италия. Средняя цена 1500–10800 рублей.
Прадакса, его аналоги и близкие заменители относятся к категории лекарственных средств, которые приходится применять в очень рискованных для здоровья ситуациях.
Риск возникновения спонтанного кровотечения при передозировке слишком высок, чтобы рисковать своей жизнью сэкономив время или деньги на поход к врачу. Чёткое осознание этой истины удержит пациентов от необдуманных решений.
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