После приема внутрь быстро всасывается из желудочно-кишечного тракта. Время достижения максимальной концентрации (ТСmax) в плазме крови 1 ч. Всасывание происходит главным образом в проксимальных отделах желудочно-кишечного тракта. При прохождении через стенку кишечника не подвергается метаболизму.
Распределение
При пероральном введении радиоактивно меченного винпоцетина крысам наибольшая концентрация обнаруживалась в печени и желудочно-кишечном тракте. Максимальная концентрация в тканях отмечалась через 2-4 часа после введения. Радиоактивность в головном мозге не превышала значений, обнаруженных в крови.
У человека связь с белками плазмы составляет 66%, биодоступность при приёме внутрь – 7%. Объем распределения 246,7-88,5 л, что свидетельствует о высоком связывании с тканями. Общий клиренс (66,7 л/ч) превышает скорость печеночного кровотока (50 л/ч), что свидетельствует о внепечёночном метаболизме.
Метаболизм
Основным метаболитом является аповинкаминат (АВА), составляющий
25-30% от исходного соединения. Площадь под кривой «концентрация – время» АВА после приема внутрь вдвое превышает таковую при внутривенном введении винпоцетина. Таким образом, винпоцетин подвержен выраженному эффекту «первичного прохождения» через печень. К прочим метаболитам относятся: гидроксивинпоцетин, гидрокси-АВА, АВА-диоксиглицинат и их конъюгаты (сульфаты и9или) глюкурониды). При нарушении функции печени или почек коррекция дозы не требуется поскольку винпоцетин не кумулирует.
Выведение
Выведение неизменного винпоцетина низкое (несколько процентов). При много кратном введении в дозах 5 мг и 10 мг кинетика носит линейный характер, равновесная плазменная концентрация составляет 1,2±0,27 и 2,1±0,33 нг/мл, соответственно. Период полувыведения у человека
4,8±1,29 ч. Выводится почками и через кишечник в соотношении 60:40. У крыс и собак высокая радиоактивность при введении радиоактивно меченного винпоцетина обнаруживается в желчи, однако отмечена значительная энтерогепатическая рециркуляция.
Особые группы пациентов
Поскольку винпоцетин предназначен в первую очередь для лечения пожилых, необходимо учитывать снижение абсорбции и распределения, а также выведения у этой возрастной группы, особенно при длительном применении. Однако по результатам клинических исследований установлено, что кинетика винпоцетина у пожилых существенно не отличается от молодых, кумуляции не происходит. При нарушениях функции печени и почек кумуляции не отмечается, что позволяет проводить длительную терапию. Винпоцетин проникает через плаценту и выделяется в грудное молоко.
Фармакологические свойства
Механизм действия винпоцетина складывается из нескольких элементов: он улучшает мозговой кровоток и обмен веществ, оказывает благоприятное воздействие на реологические свойства крови.
Нейропротекторное действие реализуется за счет снижения неблагоприятного цитотоксического влияния возбуждающих аминокислот. Блокирует Na+- и Са2+-каналы и NMDA- и АМРА-рецепторы. Селективно ингибирует Са2+-кальмодулинзависимую-ГМФ-фосфодиэстеразу. Повышает обмен серотонина и норадреналина в головном мозге, стимулирует норадренергическую нейромедиаторную систему и оказывает антиоксидантное действие.
Улучшает микроциркуляцию в головном мозге за счет ингибирования агрегации тромбоцитов, снижения патологически повышенной вязкости крови, увеличения деформируемости эритроцитов и ингибирования обратного захвата аденозина; способствует переходу кислорода в клетки за счет снижения сродства к нему эритроцитов. Избирательно увеличивает мозговой кровоток за счет снижения церебрального сосудистого сопротивления без существенного влияния на системные показатели кровообращения (артериальное давление (АД), сердечный выброс, частоту сердечных сокращений, общее периферическое сосудистое сопротивление); не вызывает эффект «обкрадывания».
Хронические сосудистые заболевания сетчатки и сосудистой оболочки глаза.
Отология:
Снижение слуха перцептивного типа;
Болезнь Меньера;
Шум в ушах.
Во избежание осложнений применять строго по назначению врача.
Противопоказания
Гиперчувствительность к винпоцетину или к любому из компонентов препарата.
Беременность, период лактации.
Дети до 18 лет (в связи с недостаточностью данных).
Способ применения и дозы
Внутрь, после еды. Курс лечения и доза определяется лечащим врачом. Обычно суточная доза составляет 15-30 мг (по 5-10 мг 3 раза в день). Начальная суточная доза составляет 15 мг. Максимальная суточная доза 30 мг. Коррекции дозы для пожилых, при нарушениях функции печени или почек не требуется.
Побочное действие
Для определения частоты возникновения побочных эффектов препарата применяют следующую классификацию: очень часто (≥ 1/10), часто (≥ 1/100 и < 1/10), нечасто (≥ 1/1000 и < 1/100), редко (≥ 1/10 000 и < 1/1000), очень редко (≥ 1/10 000).
Со стороны сердца: редко – ишемия/инфаркт миокарда, брадикардия, стенокардия, тахикардия, экстрасистолия, ощущение сердцебиения; очень редко – аритмия, фибрилляция предсердий.
Со стороны сосудов: нечасто – снижение АД; редко – повышение АД, ощущение приливов, тромбофлебит; очень редко – неустойчивость АД.
Со стороны центральной нервной системы: нечасто – головная боль; редко – дисгевзия, ступор, гемипарез, сонливость, амнезия; очень редко – тремор, спазмы.
Со стороны органа зрения: редко – отек диска зрительного нерва; очень редко – гиперемия конъюнктивы.
Со стороны органа слуха и равновесия: нечасто – вертиго; редко – гиперакузия, гипоакузия, шум в ушах.
Со стороны системы пищеварения: нечасто – дискомфорт в животе, сухость во рту, тошнота; редко – диспепсия, рвота, запор, диарея, боли в эпигастрии; очень редко – стоматит, дисфагия.
Психические нарушения: редко - нарушения сна (бессонница, повышенная сонливость), беспокойство; очень редко – эйфория, депрессия.
Со стороны крови и лимфатической системы: редко – лейкопения, тромбоцитопения; очень редко – анемия, агглютинация эритроцитов.
Иммунологические нарушения: очень редко – гиперчувствительность.
Нарушения метаболизма и питания: нечасто – гиперхолестеринемия; редко –снижение аппетита, анорексия, сахарный диабет.
Со стороны кожи и подкожной клетчатки: редко – гиперемия кожных покровов, гипергидроз, кожный зуд, крапивница, кожная сыпь; очень редко – дерматит.
Общие расстройства и расстройства в месте введения: редко – астения, недомогание, чувство жжения; очень редко – дискомфорт в грудной клетке, гипотермия.
Лабораторные нарушения: нечасто – снижение АД; редко – повышение АД гипертриглицеридемия, изменение ЭКГ (депрессия ST, удлинение интервала QT), эозинопения, нарушение функциональных печеночных проб; очень редко – лейкопения, лейкоцитопения, эритропения, уменьшение тромбинового времени, повышение массы тела.
Передозировка
Случаи передозировки не зарегистрированы. По данным литературы применение 60 мг винпоцетина в сутки безопасно. Однократный пероральный прием винпоцетина в дозе 360 мг не вызывает клинически значимых сердечно-сосудистых и прочих реакций. Лечение симптоматическое.
Взаимодействие с другими лекарственными средствами
Взаимодействия не наблюдается при одновременном применении с бета- адреноблокаторами (пиндолол), клопамидом, глибенкламидом, дигоксином, аценокумаролом и гидрохлоротиазидом.
Метилдопа может усиливать гипонензивное действие винпоцетина, поэтому при их одновременном применении требуется систематический контроль АД.
Несмотря на отсутствие данных, подтверждающих возможность взаимодействия, рекомендуется проявлять осторожность при одновременном назначении с препаратами центрального, противоаритмического и антикоагулянтного действия.
Особые указания
При наличии синдрома пролонгированного интервала QT или одновременном приёме препаратов, вызывающих удлинение интервала QT, требуется периодический контроль ЭКГ. При тяжелых нарушениях ритма сердца, повышении внутричерепного давления, приеме антиаритмических препаратов, синдроме удлиненного QT или одновременном применении препаратов, вызывающих удлинение интервала QT препарат применять с осторожностью. Влияние на способности к концентрации внимания: в период лечения необходимо соблюдать осторожность при вождении автотранспорта и занятии другими потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций.
Форма выпуска
Таблетки.
Условия хранения
В защищенном от света месте, при температуре не выше 25 °С. Хранить в недоступном для детей месте.
Срок годности
3 года. Не использовать препарат по истечении срока годности.
Условия отпуска
По рецепту.
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"}},{"type":"paragraph","data":{"text":"\u003ci\u003eВсасывание\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"После приема внутрь быстро всасывается из желудочно-кишечного тракта. Время достижения максимальной концентрации (ТСmax) в плазме крови 1 ч. Всасывание происходит главным образом в проксимальных отделах желудочно-кишечного тракта. При прохождении через стенку кишечника не подвергается метаболизму."}},{"type":"paragraph","data":{"text":"\u003ci\u003eРаспределение\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"При пероральном введении радиоактивно меченного винпоцетина крысам наибольшая концентрация обнаруживалась в печени и желудочно-кишечном тракте. Максимальная концентрация в тканях отмечалась через 2-4 часа после введения. Радиоактивность в головном мозге не превышала значений, обнаруженных в крови."}},{"type":"paragraph","data":{"text":"У человека связь с белками плазмы составляет 66%, биодоступность при приёме внутрь – 7%. Объем распределения 246,7-88,5 л, что свидетельствует о высоком связывании с тканями. Общий клиренс (66,7 л/ч) превышает скорость печеночного кровотока (50 л/ч), что свидетельствует о внепечёночном метаболизме."}},{"type":"paragraph","data":{"text":"\u003ci\u003eМетаболизм\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Основным метаболитом является аповинкаминат (АВА), составляющий"}},{"type":"paragraph","data":{"text":"25-30% от исходного соединения. Площадь под кривой «концентрация – время» АВА после приема внутрь вдвое превышает таковую при внутривенном введении винпоцетина. Таким образом, винпоцетин подвержен выраженному эффекту «первичного прохождения» через печень. К прочим метаболитам относятся: гидроксивинпоцетин, гидрокси-АВА, АВА-диоксиглицинат и их конъюгаты (сульфаты и9или) глюкурониды). При нарушении функции печени или почек коррекция дозы не требуется поскольку винпоцетин не кумулирует."}},{"type":"paragraph","data":{"text":"\u003ci\u003eВыведение\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Выведение неизменного винпоцетина низкое (несколько процентов). При много кратном введении в дозах 5 мг и 10 мг кинетика носит линейный характер, равновесная плазменная концентрация составляет 1,2±0,27 и 2,1±0,33 нг/мл, соответственно. Период полувыведения у человека"}},{"type":"paragraph","data":{"text":"4,8±1,29 ч. Выводится почками и через кишечник в соотношении 60:40. У крыс и собак высокая радиоактивность при введении радиоактивно меченного винпоцетина обнаруживается в желчи, однако отмечена значительная энтерогепатическая рециркуляция."}},{"type":"paragraph","data":{"text":"\u003ci\u003eОсобые группы пациентов\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Поскольку винпоцетин предназначен в первую очередь для лечения пожилых, необходимо учитывать снижение абсорбции и распределения, а также выведения у этой возрастной группы, особенно при длительном применении. Однако по результатам клинических исследований установлено, что кинетика винпоцетина у пожилых существенно не отличается от молодых, кумуляции не происходит. При нарушениях функции печени и почек кумуляции не отмечается, что позволяет проводить длительную терапию. Винпоцетин проникает через плаценту и выделяется в грудное молоко."}}]},{"id":7,"name":"Фармакологические свойства","slug":"pharmacologic_effects","body":[{"type":"paragraph","data":{"text":"Механизм действия винпоцетина складывается из нескольких элементов: он улучшает мозговой кровоток и обмен веществ, оказывает благоприятное воздействие на реологические свойства крови. \n\nНейропротекторное действие реализуется за счет снижения неблагоприятного цитотоксического влияния возбуждающих аминокислот. Блокирует Na+- и Са2+-каналы и NMDA- и АМРА-рецепторы. Селективно ингибирует Са2+-кальмодулинзависимую-ГМФ-фосфодиэстеразу. Повышает обмен серотонина и норадреналина в головном мозге, стимулирует норадренергическую нейромедиаторную систему и оказывает антиоксидантное действие. \n\nУлучшает микроциркуляцию в головном мозге за счет ингибирования агрегации тромбоцитов, снижения патологически повышенной вязкости крови, увеличения деформируемости эритроцитов и ингибирования обратного захвата аденозина; способствует переходу кислорода в клетки за счет снижения сродства к нему эритроцитов. Избирательно увеличивает мозговой кровоток за счет снижения церебрального сосудистого сопротивления без существенного влияния на системные показатели кровообращения (артериальное давление (АД), сердечный выброс, частоту сердечных сокращений, общее периферическое сосудистое сопротивление); не вызывает эффект «обкрадывания»."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"\u003ci\u003eНеврология\u003c/i\u003e:"}},{"type":"list","data":{"style":"ordered","items":["Симптоматическая терапия последствий ишемического инсульта;","Сосудистой вертебробазилярной недостаточности;","Сосудистой деменции;","Атеросклероза сосудов головного мозга;","Посттравматической;","Гипертонической энцефалопатии."]}},{"type":"paragraph","data":{"text":"\u003ci\u003eОфтальмология\u003c/i\u003e:"}},{"type":"list","data":{"style":"ordered","items":["Хронические сосудистые заболевания сетчатки и сосудистой оболочки глаза."]}},{"type":"paragraph","data":{"text":"\u003ci\u003eОтология\u003c/i\u003e:"}},{"type":"list","data":{"style":"ordered","items":["Снижение слуха перцептивного типа;","Болезнь Меньера;","Шум в ушах."]}},{"type":"paragraph","data":{"text":"Во избежание осложнений применять строго по назначению врача."}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"list","data":{"style":"ordered","items":["Гиперчувствительность к винпоцетину или к любому из компонентов препарата.","Беременность, период лактации.","Дети до 18 лет (в связи с недостаточностью данных)."]}}]},{"id":12,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Внутрь, после еды. Курс лечения и доза определяется лечащим врачом. Обычно суточная доза составляет 15-30 мг (по 5-10 мг 3 раза в день). Начальная суточная доза составляет 15 мг. Максимальная суточная доза 30 мг. Коррекции дозы для пожилых, при нарушениях функции печени или почек не требуется."}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Для определения частоты возникновения побочных эффектов препарата применяют следующую классификацию: очень часто (≥ 1/10), часто (≥ 1/100 и < 1/10), нечасто (≥ 1/1000 и < 1/100), редко (≥ 1/10 000 и < 1/1000), очень редко (≥ 1/10 000)."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны сердца:\u003c/i\u003e редко – ишемия/инфаркт миокарда, брадикардия, стенокардия, тахикардия, экстрасистолия, ощущение сердцебиения; очень редко – аритмия, фибрилляция предсердий."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны сосудов: \u003c/i\u003eнечасто – снижение АД; редко – повышение АД, ощущение приливов, тромбофлебит; очень редко – неустойчивость АД."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны центральной нервной системы: \u003c/i\u003eнечасто – головная боль; редко – дисгевзия, ступор, гемипарез, сонливость, амнезия; очень редко – тремор, спазмы."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны органа зрения:\u003c/i\u003e редко – отек диска зрительного нерва; очень редко – гиперемия конъюнктивы."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны органа слуха и равновесия:\u003c/i\u003e нечасто – вертиго; редко – гиперакузия, гипоакузия, шум в ушах."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны системы пищеварения:\u003c/i\u003e нечасто – дискомфорт в животе, сухость во рту, тошнота; редко – диспепсия, рвота, запор, диарея, боли в эпигастрии; очень редко – стоматит, дисфагия."}},{"type":"paragraph","data":{"text":"\u003ci\u003eПсихические нарушения:\u003c/i\u003e редко - нарушения сна (бессонница, повышенная сонливость), беспокойство; очень редко – эйфория, депрессия."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны крови и лимфатической системы:\u003c/i\u003e редко – лейкопения, тромбоцитопения; очень редко – анемия, агглютинация эритроцитов."}},{"type":"paragraph","data":{"text":"\u003ci\u003eИммунологические нарушения:\u003c/i\u003e очень редко – гиперчувствительность."}},{"type":"paragraph","data":{"text":"\u003ci\u003eНарушения метаболизма и питания:\u003c/i\u003e нечасто – гиперхолестеринемия; редко –снижение аппетита, анорексия, сахарный диабет."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны кожи и подкожной клетчатки:\u003c/i\u003e редко – гиперемия кожных покровов, гипергидроз, кожный зуд, крапивница, кожная сыпь; очень редко – дерматит."}},{"type":"paragraph","data":{"text":"\u003ci\u003eОбщие расстройства и расстройства в месте введения: \u003c/i\u003eредко – астения, недомогание, чувство жжения; очень редко – дискомфорт в грудной клетке, гипотермия."}},{"type":"paragraph","data":{"text":"\u003ci\u003eЛабораторные нарушения:\u003c/i\u003e нечасто – снижение АД; редко – повышение АД гипертриглицеридемия, изменение ЭКГ (депрессия ST, удлинение интервала QT), эозинопения, нарушение функциональных печеночных проб; очень редко – лейкопения, лейкоцитопения, эритропения, уменьшение тромбинового времени, повышение массы тела."}}]},{"id":14,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"Случаи передозировки не зарегистрированы. По данным литературы применение 60 мг винпоцетина в сутки безопасно. Однократный пероральный прием винпоцетина в дозе 360 мг не вызывает клинически значимых сердечно-сосудистых и прочих реакций. Лечение симптоматическое."}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"Взаимодействия не наблюдается при одновременном применении с бета- адреноблокаторами (пиндолол), клопамидом, глибенкламидом, дигоксином, аценокумаролом и гидрохлоротиазидом."}},{"type":"paragraph","data":{"text":"Метилдопа может усиливать гипонензивное действие винпоцетина, поэтому при их одновременном применении требуется систематический контроль АД."}},{"type":"paragraph","data":{"text":"Несмотря на отсутствие данных, подтверждающих возможность взаимодействия, рекомендуется проявлять осторожность при одновременном назначении с препаратами центрального, противоаритмического и антикоагулянтного действия."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"При наличии синдрома пролонгированного интервала QT или одновременном приёме препаратов, вызывающих удлинение интервала QT, требуется периодический контроль ЭКГ. При тяжелых нарушениях ритма сердца, повышении внутричерепного давления, приеме антиаритмических препаратов, синдроме удлиненного QT или одновременном применении препаратов, вызывающих удлинение интервала QT препарат применять с осторожностью. \u003ci\u003eВлияние на способности к концентрации внимания: \u003c/i\u003eв период лечения необходимо соблюдать осторожность при вождении автотранспорта и занятии другими потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций."}}]},{"id":18,"name":"Форма выпуска","slug":"","body":[{"type":"paragraph","data":{"text":"Таблетки."}}]},{"id":19,"name":"Условия хранения","slug":"storage","body":[{"type":"paragraph","data":{"text":"В защищенном от света месте, при температуре не выше 25 °С. Хранить в недоступном для детей месте."}}]},{"id":20,"name":"Срок годности","slug":"expiry_date","body":[{"type":"paragraph","data":{"text":"3 года. Не использовать препарат по истечении срока годности.\n\n"}}]},{"id":21,"name":"Условия отпуска","slug":"release_condition","body":[{"type":"paragraph","data":{"text":"По рецепту."}}]}],"source":null},"description_toggle":false,"short_description":"Механизм действия винпоцетина складывается из нескольких элементов: он улучшает мозговой кровоток и обмен веществ, оказывает благоприятное воздействие на реологические свойства крови. Нейропротекторное действие реализуется за счет снижения неблагоприятного цитотоксического влияния возбуждающих аминокислот. Блокирует Na+- и Са2+-каналы и NMDA- и АМРА-рецепторы. Селективно ингибирует Са2+-кальмодулинзависимую-ГМФ-фосфодиэстеразу. Повышает обмен серотонина и норадреналина в головном мозге, стимулирует норадренергическую нейромедиаторную систему и оказывает антиоксидантное действие. Улучшает микроциркуляцию в головном мозге за счет ингибирования агрегации тромбоцитов, снижения патологически повышенной вязкости крови, увеличения деформируемости эритроцитов и ингибирования обратного захвата аденозина; способствует переходу кислорода в клетки за счет снижения сродства к нему эритроцитов. 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