Содержание
Латинское название [ править ]
Фармакологическая группа [ править ]
Фениндион — непрямой антикоагулянт
Характеристика вещества [ править ]
Фармакология [ править ]
За счет конкурентного антагонизма с витамином K фениндион блокирует K-витаминредуктазу, нарушает образование в печени его активной формы, необходимой для синтеза протромбина и других факторов свертывания (VII, IX, X).
Фениндион быстро и полно всасывается, проходит гистогематические барьеры и накапливается в тканях. Метаболизируется в печени. Выделяется почками (в т.ч. и продукты биотрансформации).
Гипокоагулянтный эффект (понижение концентрации факторов свертывания в крови) фениндиона наступает через 8–10 ч и достигает максимума через 24–30 ч после приема. Для контроля за антикоагуляционной активностью фениндиона используют показатель протромбинового времени; надежная профилактика венозного тромбоза достигается при увеличении ПВ в 2 раза, артериального — в 3–4 раза (норма 11–14 с).
Применение [ править ]
Профилактика и лечение тромбозов и тромбоэмболических осложнений.
Фениндион: Противопоказания [ править ]
Гиперчувствительность к фениндиону, геморрагический синдром, исходный уровень протромбина менее 70%, беременность (I триместр).
Применение при беременности и кормлении грудью [ править ]
Фениндион противопоказан в I триместре беременности.
Фениндион: Побочные действия [ править ]
Лихорадка, тошнота, понос, поражения печени, парестезии, угнетение кроветворения; окрашивание ладоней в оранжевый цвет и мочи — в розовый, дерматиты, аллергические реакции.
Взаимодействие [ править ]
Анаболические стероиды, ненаркотические анальгетики, левомицетин, аминогликозиды, тетрациклины, др. антикоагулянты, тромболитические и антиагрегационные средства, азатиоприн, аллопуринол, амиодарон, наркотические анальгетики, андрогены, трициклические антидепрессанты, окисляющие мочу средства, глюкокортикоиды, диазоксид, дизопирамид, изониазид, налидиксовая кислота, метронидазол, парацетамол, резерпин, растворы кристаллоидов, бутадион, сульфаниламиды, токоферол, дисульфирам, хинидин, циклофосфан, циметидин, гормоны щитовидной железы — усиливают эффект фениндиона.
Барбитураты, дифенин, спиронолактон, ощелачивающие мочу средства, пропранолол, антациды, феназон, витамины К и С, галоперидол, диуретики, карбамазепин, пероральные контрацептивы, мепробамат, рифампицин — ослабляют эффект фениндиона.
Фениндион: Способ применения и дозы [ править ]
Взрослые, внутрь: средняя терапевтическая доза фениндиона — 0,06–0,09 г в сутки в 3 приема, максимальная разовая доза фениндиона для взрослых — 0,05 г, максимальная суточная — 0,2 г.
Меры предосторожности [ править ]
Кроме исследования ПВ, необходим строгий врачебный контроль и регулярное расширенное коагулологическое исследование крови (коагулограмма, тромбоэластограмма, количество тромбоцитов).
Лечение фениндионом может сопровождаться окрашиванием ладоней в оранжевый и мочи — в розовый цвет.
Условия хранения [ править ]
Торговые наименования [ править ]
Фенилин: таблетки 30 мг. «Здоровье — фармацевтическая компания (Украина)»
Инструкция по применению
Антикоагулянт непрямого действия. Вызывает гипопротромбинемию, связанную с нарушением процесса образования протромбина в печени, вызывает также уменьшение образования VII, IX, X факторов свертывания крови, снижение толерантности плазмы к гепарину, содержания липидов в крови и повышение проницаемости сосудов. Действие наступает через 8-10 ч и достигает максимума через 24-30 ч после приема фениндиона.
Клинические данные по фармакокинетике фениндиона ограничены. Кумуляция выражена меньше, чем у неодикумарина.
Противопоказания ФЕНИНДИОН
Гемофилия, гипокоагуляция, I триместр беременности, повышенная чувствительность к фениндиону.
C осторожностью следует применять препарат у пациентов пожилого возраста, при печеночной и/или почечной недостаточности, тромбоэмболии легочной артерии (в т.ч. в онкологии), эрозивно-язвенных поражениях ЖКТ, при перикардите, в послеродовом периоде.
Лечение следует проводить под тщательным врачебным контролем с обязательным систематическим исследованием содержания в крови протромбина и других факторов свертывания. Систематически проводят общие анализы мочи для раннего выявления гематурии.
У некоторых больных наблюдается окрашивание ладоней в оранжевый цвет и мочи — в розовый, что связано с метаболизмом фениндиона.
Противопоказан при беременности. Избегать применения в первые дни после родов.
Фениндион не следует применять в период лактации (грудного вскармливания).
Фениндион следует отменить за 2 дня до начала и не применять во время менструации.
Со стороны пищеварительной системы: тошнота, диарея, нарушение функции печени, токсический гепатит.
Со стороны системы кроветворения: угнетение костномозгового кроветворения.
Со стороны мочевыделительной системы: нарушения функции почек.
Со стороны сердечно-сосудистой системы: миокардит.
Со стороны свертывающей системы крови: при длительном применении — микро- и макрогематурия, кровотечения из полости рта и носоглотки, из ЖКТ, кровоизлияния в мышцы.
Со стороны ЦНС: головная боль.
Аллергические реакции: кожная сыпь, дерматит, эозинофилия, повышение температуры.
При одновременном применении с АКТГ усиливается антикоагулянтное действие.
При одновременном применении с дипиридамолом описаны случаи повышения кровоточивости, по-видимому, вследствие уменьшения адгезивности и агрегации тромбоцитов под влиянием дипиридамола.
При одновременном применении с клофибратом усиливается антикоагулянтное действие. Полагают, что фибраты могут повышать сродство пероральных антикоагулянтов к соответствующим рецепторам или, возможно, нарушать метаболизм антикоагулянтов.
При одновременном применении с лиотиронином усиливается антикоагулянтное действие фениндиона. Полагают, что тиреоидные гормоны могут повышать сродство пероральных антикоагулянтов к соответствующим рецепторам.
При одновременном применении с миконазолом усиливается антикоагулянтное действие фениндиона. Повышается риск развития кровотечений.
При одновременном применении с циметидином усиливается антикоагулянтное действие фениндиона вследствие замедления его метаболизма в печени под влиянием циметидина, который является ингибитором микросомальных ферментов печени.
При одновременном применении с этилэстренолом усиливается антикоагулянтное действие, возникает риск развития кровотечений.
Способ применения и дозировка ФЕНИНДИОН
Внутрь в 1-й день суточная доза составляет 120-180 мг в 3-4 приема, во 2-й день — 90-150 мг, затем по 30-60 мг/сут в зависимости от содержания в крови протромбина. Отмену фениндиона следует проводить постепенно.
Информация предоставлена справочником лекарственных средств «Видаль».
Последняя актуализация описания 28.09.2011
Торговые названия
Фенилин.
Групповая принадлежность
Описание действующего вещества (МНН)
Фениндион
Лекарственная форма
таблетки
Фармакологическое действие
Антикоагулянт непрямого действия; обладает K-антивитаминной активностью, тормозит образование протромбина, вызывает гипопротромбинемию, уменьшает образование VII, IX, X факторов свертывания крови, снижает толерантность плазмы к гепарину. Действие наступает через 8-10 ч и достигает максимума через 24-30 ч.
Показания
Профилактика тромбоэмболии (в т.ч. при инфаркте миокарда, после хирургических вмешательств); тромбоз коронарных сосудов, тромбофлебит и тромбоз глубоких вен нижних конечностей; профилактика тромбоза после операции по поводу протезирования клапанов сердца (постоянный прием).
Противопоказания
Гиперчувствительность, гемофилия, гипокоагуляция, беременность (I триместр).C осторожностью. Пожилой возраст, печеночная и/или почечная недостаточность, тромбоэмболия легочной артерии (в т.ч. в онкологии), эрозивно-язвенные поражения ЖКТ, перикардит, послеродовой период.
Побочные действия
Головная боль, тошнота, диарея, токсический гепатит, лихорадка, угнетение костномозгового кроветворения, окрашивание ладоней в оранжевый цвет, мочи — в розовый, аллергические реакции (лихорадка, дерматит). При длительном применении — микро- и макрогематурия, кровотечения из полости рта и носоглотки, из ЖКТ, кровоизлияние в мышцы.
Способ применения и дозы
Внутрь, в первый день — в суточной дозе 0.12-0.18 г в 3-4 приема, во второй день — 0.09-0.15 г/сут, затем — по 0.03-0.06 г в день в 1-2 приема, под контролем протромбинового времени. Высшая разовая доза для взрослых — 0.05 г, суточная — 0.2 г. Прекращение лечения следует проводить постепенно.
Особые указания
Необходим систематический контроль протромбинового соотношения (нормальные показатели — 2.0-4.0), анализов мочи для раннего выявления гематурии. Не следует назначать во время менструации (прекращают за 2 дня до начала) и в первые дни после родов.
Взаимодействие
Усиливают эффект тромболитические, антиагрегантные ЛС, др. антикоагулянты, анаболики, азатиоприн, аллопуринол, амиодарон, наркотические анальгетики, андрогены, антибиотики, трициклические антидепрессанты, окисляющие мочу ЛС, ГКС, диазоксид, дизопирамид, изониазид, налидиксовая кислота, клофибрат, метронидазол, парацетамол, резерпин, альфа-токоферол, бутадион, сульфаниламиды, дисульфирам, хинидин, циклофосфан, гормоны щитовидной железы, циметидин и др. ингибиторы микросомального окисления. Пропранолол, ощелачивающие мочу ЛС, антациды, колестирамин, витамин К, феназон, галоперидол, диуретики, карбамазепин, барбитураты, пероральные контрацептивы, рифампицин и др. индукторы микросомального окисления ослабляют действие фениндиона.
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