Круглые двояковыпуклые таблетки белого или почти белого цвета со скошенными краями с риской на одной стороне таблетки и гравировкой «289» с обеих сторон от риски.
Фармакотерапевтическая группа
Препарат гистамина.
Фармакологические свойства
Фармакодинамика
Механизм действия бетагистина известен только частично. Существует несколько возможных гипотез, подтвержденных доклиническими и клиническими данными:
Влияние на гистаминергическую систему
Частичный агонист Н1-гистаминовых и антагонист НЗ-гистаминовых рецепторов вестибулярных ядер Ц, обладает незначительной активностью в отношении Н2-рецепторов. Бетагистин увеличивает обмен гистамина и его высвобождение путем блокирования пресинаптических НЗ-рецепторов и снижения количества НЗ-рецепторов.
Усиление кровотока кохлеарной области, а также всего головного мозга
Согласно доклиническим исследованиям бетагистин улучшает кровообращение в сосудистой полоске внутреннего уха за счет расслабления прекапиллярных сфинктеров сосудов внутреннего уха. Также показано, что бетагистин усиливает кровоток головного мозга у человека.
Облегчение процесса центральной вестибулярной компенсации
Бетагистин ускоряет восстановление вестибулярной функции у животных после односторонней вестибулярной нейрэктомии, ускоряя и облегчая центральную вестибулярную компенсацию за счет антагонизма с НЗ-гистаминовыми рецепторами.
Время восстановления после вестибулярной нейрэктомии у человека при лечении бетагистином также уменьшается.
Возбуждение нейронов в вестибулярных ядрах
Дозозависимо снижает генерацию потенциалов действия в нейронах латеральных и медиальных вестибулярных ядер.
Фармакодинамические свойства, выявленные на животных, обеспечивают положительный терапевтический эффект бетагистина в вестибулярной системе.
Эффективность бетагистина была продемонстрирована у пациентов с вестибулярным головокружением и синдромом Меньера, что проявлялось уменьшением выраженности и частоты головокружений.
Фармакокинетика
Всасывание
При пероральном приеме бетагистин быстро и практически полностью всасывается в желудочно-кишечном тракте. После всасывания препарат быстро и почти полностью метаболизируется с образованием метаболита 2-пиридилуксусной кислоты. Концентрация бетагистина в плазме крови очень низкая. Таким образом, фармакокинетические анализы основаны на измерении концентрации метаболита 2-пиридилуксусной кислоты в плазме и моче.
При приеме препарата с пищей максимальная концентрация (Стах) препарата в крови ниже, чем при приеме натощак. Однако суммарная абсорбция бетагистина одинакова в обоих случаях, что указывает на то, что прием пищи лишь замедляет всасывание бетагистина.
Распределение
Связывание бетагистина с белками плазмы крови составляет менее 5 %.
Биотрансформация
После всасывания бетагистин быстро и почти полностью метаболизируется с образованием метаболита 2-пиридилуксусной кислоты (который не обладает фармакологической активностью). Максимальная концентрация 2-пиридилуксусной кислоты в плазме крови (или моче) достигается через час после приема. Период полувыведения приблизительно 3,5 часа.
Выведение
2-пиридилуксусная кислота быстро выводится с мочой. При приеме препарата в дозе 8-48 мг около 85 % начальной дозы обнаруживается в моче. Выведение бетагистина почками или через кишечник незначительно.
Линейность
Скорость выведения остается постоянной при пероральном приеме 8-48 мг препарата, указывая на линейность фармакокинетики бетагистина, и позволяет предположить, что задействованный метаболический путь остается ненасыщенным.
Показания к применению
Синдром Меньера, характеризующийся следующими основными симптомами:
- повышенная чувствительность к любому из компонентов препарата.
Бетасерк не рекомендуется для применения у детей в возрасте до 18 лет в связи с недостаточностью данных по эффективности и безопасности.
С осторожностью
Пациенты с бронхиальной астмой, язвенной болезнью желудка и/или двенадцатиперстной кишки требуют тщательного наблюдения в период лечения.
Применение при беременности и в период грудного вскармливания
Беременность
Имеющихся данных о применении бетагистина беременными женщинами недостаточно.
Исследования на животных не выявили прямой или непрямой репродуктивной токсичности. Бетагистин не должен использоваться во время беременности за исключением случаев очевидной необходимости.
Грудное вскармливание
Неизвестно выделяется ли бетагистин с грудным молоком у человека. Бетагистин выделяется с грудным молоком у крыс. Исследования на животных были ограничены применением препарата в очень высоких дозах. Вопрос о назначении лекарственного препарата матери должен приниматься только после сопоставления пользы грудного вскармливания с потенциальным риском для грудного ребенка.
Фертильность
В исследованиях на животных (крысах) влияния на фертильность не выявлено.
Способ применения и дозы
Всегда принимайте Бетасерк точно так, как прописал Ваш лечащий врач. Если у Вас есть какие-либо вопросы, проконсультируйтесь с Вашим лечащим врачом.
Внутрь, во время еды.
Доза препарата для взрослых составляет 48 мг бетагистина в день.
Бетасерк 24 мг следует принимать по 1 таблетке 2 раза в день. Таблетку можно разделить на две равные части
Дозу следует подбирать индивидуально в зависимости от реакции на лечение. Улучшение иногда наблюдается только через несколько недель лечения. Наилучшие результаты иногда достигаются после нескольких месяцев лечения. Имеются данные о том, что назначение лечения в начале заболевания предотвращает его прогрессирование и/или потерю слуха на более поздних стадиях.
Пожилой возраст
Пациенты с почечной/печеночной недостаточностью
Специальные клинические исследования в этой группе пациентов не проводились, однако пострегистрационный опыт дает основания предполагать, что коррекция дозы у данной группы пациентов не требуется.
Побочное действие
Если Вы заметили какие-либо побочные эффекты, не упомянутые в данной инструкции, или какой-либо побочный эффект принял серьезный характер, уведомите, пожалуйста, Вашего лечащего врача.
Нарушения со стороны желудочно-кишечного тракта: Часто (от ≥1/100 до <1/10): тошнота и диспепсия.
Нарушения со стороны нервной системы: Часто (от ≥1/100 до <1/10): головная боль.
Кроме этих эффектов, выявленных при проведении клинических исследований, в процессе пострегистрационного применения и в научной литературе сообщалось о нижеследующих нежелательных эффектах. Имеющихся данных недостаточно, чтобы оценить их частоту.
Нарушения со стороны иммунной системы: реакция гиперчувствительности, в том числе анафилактическая реакция.
Нарушения со стороны желудочно-кишечного тракта: умеренные расстройства, такие как рвота, желудочно-кишечные боли, вздутие живота. Эти эффекты обычно исчезают после приема препарата одновременно с пищей или после снижения дозы.
Нарушения со стороны кожи и подкожных тканей: реакции гиперчувствительности, в особенности ангионевротический отек, крапивница, зуд и сыпь.
Передозировка
Известно несколько случаев передозировки препарата. У некоторых пациентов наблюдались легкие и умеренные симптомы (тошнота, сонливость, боль в животе) после приема препарата в дозах до 640 мг. Более серьезные осложнения (судороги, сердечно-легочные осложнения) наблюдались при преднамеренном приеме повышенных доз бетагистина, особенно в сочетании с передозировкой других лекарственных средств.
Рекомендуется симптоматическое лечение.
Взаимодействие с другими лекарственными средствами
Если в настоящее время или в недавнем прошлом Вы принимали другие лекарственные средства, в том числе без назначения врача, сообщите об этом, пожалуйста, своему лечащему врачу.
Исследования in vivo, направленные на изучение взаимодействия с другими лекарственными препаратами, не проводились. Основываясь на данных in vitro, можно предположить отсутствие ингибирования активности изоферментов цитохрома Р450 in vivo.
Данные in vitro показали ингибирование метаболизма бетагистина под действием препаратов, которые ингибируют моноаминоксидазу (МАО), включая МАО подтипа В (например, селегилин). Следует соблюдать осторожность при одновременном назначении бетагистина и ингибиторов МАО (включая МАО-В).
Бетагистин является аналогом гистамина, взаимодействие бетагистина с блокаторами H1-гистаминовых рецепторов теоретически может влиять на эффективность одного из этих лекарственных средств.
Особые указания
Риска на таблетке предназначена для разламывания таблетки с целью облегчения ее проглатывания и не предназначена для деления её на две равные дозы.
Влияние на способность управлять автомобилем и движущимися механизмами
Бетагистин не влияет или незначительно влияет на способность управлять транспортными средствами и работать с механизмами, в клинических исследованиях нежелательные реакции, которые могли бы повлиять на такую способность, не выявлены.
Форма выпуска
Таблетки, 24 мг.
По 10 таблеток в ПВХ/ПВДХ/Ал блистер, по 5 блистеров вместе с инструкцией по применению в пачку картонную.
По 15 таблеток в ПВХ/ПВДХ/Ал блистер, по 2 блистера вместе с инструкцией по применению в пачку картонную.
По 20 таблеток в ПВХ/ПВДХ/Ал блистер, по 1, 2, 3 или 5 блистеров вместе с инструкцией по применению в пачку картонную.
По 25 таблеток в ПВХ/ПВДХ/Ал блистер, по 1, 2 или 4 блистера вместе с инструкцией по применению в пачку картонную.
Условия хранения
Хранить при температуре не выше 25 °C.
Хранить в недоступном для детей месте!
Срок годности
3 года. Не применять по истечении срока годности, указанного на упаковке.
Условия отпуска
Отпускают по рецепту.
Производитель
Майлан Лэбораториз САС,
Рут де Бельвилль, Лье-ди Майар,
01400, Шатийон-сюр-Шаларон, Франция
или
АО "ВЕРОФАРМ",
308013, Россия, г. Белгород, ул. Рабочая, д. 14
Организация, принимающая претензии потребителей
ООО «Эбботт Лэбораториз»
125171, г. Москва, Ленинградское шоссе, дом 16А, стр. 1
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гравировкой «289» с обеих сторон от риски."}}]},{"id":6,"name":"Фармакотерапевтическая группа","slug":"","body":[{"type":"paragraph","data":{"text":"Препарат гистамина."}}]},{"id":7,"name":"Фармакологические свойства","slug":"pharmacologic_effects","body":[{"type":"paragraph","data":{"text":"Фармакодинамика"}},{"type":"paragraph","data":{"text":"Механизм действия бетагистина известен только частично. Существует несколько возможных гипотез, подтвержденных доклиническими и клиническими данными:"}},{"type":"list","data":{"style":"ordered","items":["Влияние на гистаминергическую систему"]}},{"type":"paragraph","data":{"text":"Частичный агонист Н1-гистаминовых и антагонист НЗ-гистаминовых рецепторов вестибулярных ядер Ц, обладает незначительной активностью в отношении Н2-рецепторов. Бетагистин увеличивает обмен гистамина и его высвобождение путем блокирования пресинаптических НЗ-рецепторов и снижения количества НЗ-рецепторов."}},{"type":"list","data":{"style":"ordered","items":["Усиление кровотока кохлеарной области, а также всего головного мозга"]}},{"type":"paragraph","data":{"text":"Согласно доклиническим исследованиям бетагистин улучшает кровообращение в сосудистой полоске внутреннего уха за счет расслабления прекапиллярных сфинктеров сосудов внутреннего уха. Также показано, что бетагистин усиливает кровоток головного мозга у человека."}},{"type":"list","data":{"style":"ordered","items":["Облегчение процесса центральной вестибулярной компенсации"]}},{"type":"paragraph","data":{"text":"Бетагистин ускоряет восстановление вестибулярной функции у животных после односторонней вестибулярной нейрэктомии, ускоряя и облегчая центральную вестибулярную компенсацию за счет антагонизма с НЗ-гистаминовыми рецепторами."}},{"type":"paragraph","data":{"text":"Время восстановления после вестибулярной нейрэктомии у человека при лечении бетагистином также уменьшается."}},{"type":"list","data":{"style":"ordered","items":["Возбуждение нейронов в вестибулярных ядрах"]}},{"type":"paragraph","data":{"text":"Дозозависимо снижает генерацию потенциалов действия в нейронах латеральных и медиальных вестибулярных ядер."}},{"type":"paragraph","data":{"text":"Фармакодинамические свойства, выявленные на животных, обеспечивают положительный терапевтический эффект бетагистина в вестибулярной системе."}},{"type":"paragraph","data":{"text":"Эффективность бетагистина была продемонстрирована у пациентов с вестибулярным головокружением и синдромом Меньера, что проявлялось уменьшением выраженности и частоты головокружений."}},{"type":"paragraph","data":{"text":"Фармакокинетика"}},{"type":"paragraph","data":{"text":"Всасывание"}},{"type":"paragraph","data":{"text":"При пероральном приеме бетагистин быстро и практически полностью всасывается в желудочно-кишечном тракте. После всасывания препарат быстро и почти полностью метаболизируется с образованием метаболита 2-пиридилуксусной кислоты. Концентрация бетагистина в плазме крови очень низкая. Таким образом, фармакокинетические анализы основаны на измерении концентрации метаболита 2-пиридилуксусной кислоты в плазме и моче."}},{"type":"paragraph","data":{"text":"При приеме препарата с пищей максимальная концентрация (Стах) препарата в крови ниже, чем при приеме натощак. Однако суммарная абсорбция бетагистина одинакова в обоих случаях, что указывает на то, что прием пищи лишь замедляет всасывание бетагистина."}},{"type":"paragraph","data":{"text":"Распределение"}},{"type":"paragraph","data":{"text":"Связывание бетагистина с белками плазмы крови составляет менее 5 %."}},{"type":"paragraph","data":{"text":"Биотрансформация"}},{"type":"paragraph","data":{"text":"После всасывания бетагистин быстро и почти полностью метаболизируется с образованием метаболита 2-пиридилуксусной кислоты (который не обладает фармакологической активностью). Максимальная концентрация 2-пиридилуксусной кислоты в плазме крови (или моче) достигается через час после приема. Период полувыведения приблизительно 3,5 часа."}},{"type":"paragraph","data":{"text":"Выведение"}},{"type":"paragraph","data":{"text":"2-пиридилуксусная кислота быстро выводится с мочой. При приеме препарата в дозе 8-48 мг около 85 % начальной дозы обнаруживается в моче. Выведение бетагистина почками или через кишечник незначительно."}},{"type":"paragraph","data":{"text":"Линейность"}},{"type":"paragraph","data":{"text":"Скорость выведения остается постоянной при пероральном приеме 8-48 мг препарата, указывая на линейность фармакокинетики бетагистина, и позволяет предположить, что задействованный метаболический путь остается ненасыщенным."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"Синдром Меньера, характеризующийся следующими основными симптомами:"}},{"type":"paragraph","data":{"text":"- головокружение (сопровождающееся тошнотой/рвотой)"}},{"type":"paragraph","data":{"text":"- снижение слуха (тугоухость)"}},{"type":"paragraph","data":{"text":"- шум в ушах"}},{"type":"paragraph","data":{"text":"Симптоматическое лечение вестибулярного головокружения (вертиго)."}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"paragraph","data":{"text":"- феохромоцитома;"}},{"type":"paragraph","data":{"text":"- повышенная чувствительность к любому из компонентов препарата."}},{"type":"paragraph","data":{"text":"Бетасерк не рекомендуется для применения у детей в возрасте до 18 лет в связи с недостаточностью данных по эффективности и безопасности."}}]},{"id":10,"name":"С осторожностью","slug":"cautions","body":[{"type":"paragraph","data":{"text":"Пациенты с бронхиальной астмой, язвенной болезнью желудка и/или двенадцатиперстной кишки требуют тщательного наблюдения в период лечения."}}]},{"id":11,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","body":[{"type":"paragraph","data":{"text":"Беременность"}},{"type":"paragraph","data":{"text":"\n\nИмеющихся данных о применении бетагистина беременными женщинами недостаточно."}},{"type":"paragraph","data":{"text":"Исследования на животных не выявили прямой или непрямой репродуктивной токсичности. Бетагистин не должен использоваться во время беременности за исключением случаев очевидной необходимости.\n\n"}},{"type":"paragraph","data":{"text":"Грудное вскармливание"}},{"type":"paragraph","data":{"text":"Неизвестно выделяется ли бетагистин с грудным молоком у человека. Бетагистин выделяется с грудным молоком у крыс. Исследования на животных были ограничены применением препарата в очень высоких дозах. Вопрос о назначении лекарственного препарата матери должен приниматься только после сопоставления пользы грудного вскармливания с потенциальным риском для грудного ребенка."}},{"type":"paragraph","data":{"text":"Фертильность"}},{"type":"paragraph","data":{"text":"В исследованиях на животных (крысах) влияния на фертильность не выявлено."}}]},{"id":12,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Всегда принимайте Бетасерк точно так, как прописал Ваш лечащий врач. Если у Вас есть какие-либо вопросы, проконсультируйтесь с Вашим лечащим врачом."}},{"type":"paragraph","data":{"text":"Внутрь, во время еды."}},{"type":"paragraph","data":{"text":"Доза препарата для взрослых составляет 48 мг бетагистина в день."}},{"type":"paragraph","data":{"text":"Бетасерк 24 мг следует принимать по 1 таблетке 2 раза в день. Таблетку можно разделить на две равные части"}},{"type":"paragraph","data":{"text":"Дозу следует подбирать индивидуально в зависимости от реакции на лечение. Улучшение иногда наблюдается только через несколько недель лечения. Наилучшие результаты иногда достигаются после нескольких месяцев лечения. Имеются данные о том, что назначение лечения в начале заболевания предотвращает его прогрессирование и/или потерю слуха на более поздних стадиях."}},{"type":"paragraph","data":{"text":"Пожилой возраст"}},{"type":"paragraph","data":{"text":"Пациенты с почечной/печеночной недостаточностью"}},{"type":"paragraph","data":{"text":"Специальные клинические исследования в этой группе пациентов не проводились, однако пострегистрационный опыт дает основания предполагать, что коррекция дозы у данной группы пациентов не требуется."}}]},{"id":0,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Если Вы заметили какие-либо побочные эффекты, не упомянутые в данной инструкции, или какой-либо побочный эффект принял серьезный характер, уведомите, пожалуйста, Вашего лечащего врача."}},{"type":"paragraph","data":{"text":"Нарушения со стороны желудочно-кишечного тракта: Часто (от ≥1/100 до <1/10): тошнота и диспепсия."}},{"type":"paragraph","data":{"text":"Нарушения со стороны нервной системы: Часто (от ≥1/100 до <1/10): головная боль."}},{"type":"paragraph","data":{"text":"Кроме этих эффектов, выявленных при проведении клинических исследований, в процессе пострегистрационного применения и в научной литературе сообщалось о нижеследующих нежелательных эффектах. Имеющихся данных недостаточно, чтобы оценить их частоту."}},{"type":"paragraph","data":{"text":"Нарушения со стороны иммунной системы: реакция гиперчувствительности, в том числе анафилактическая реакция."}},{"type":"paragraph","data":{"text":"Нарушения со стороны желудочно-кишечного тракта: умеренные расстройства, такие как рвота, желудочно-кишечные боли, вздутие живота. Эти эффекты обычно исчезают после приема препарата одновременно с пищей или после снижения дозы."}},{"type":"paragraph","data":{"text":"Нарушения со стороны кожи и подкожных тканей: реакции гиперчувствительности, в особенности ангионевротический отек, крапивница, зуд и сыпь."}}]},{"id":13,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"\n\nИзвестно несколько случаев передозировки препарата. У некоторых пациентов наблюдались легкие и умеренные симптомы (тошнота, сонливость, боль в животе) после приема препарата в дозах до 640 мг. Более серьезные осложнения (судороги, сердечно-легочные осложнения) наблюдались при преднамеренном приеме повышенных доз бетагистина, особенно в сочетании с передозировкой других лекарственных средств."}},{"type":"paragraph","data":{"text":"Рекомендуется симптоматическое лечение.\n\n"}}]},{"id":14,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"Если в настоящее время или в недавнем прошлом Вы принимали другие лекарственные средства, в том числе без назначения врача, сообщите об этом, пожалуйста, своему лечащему врачу."}},{"type":"paragraph","data":{"text":"Исследования in vivo, направленные на изучение взаимодействия с другими лекарственными препаратами, не проводились. Основываясь на данных in vitro, можно предположить отсутствие ингибирования активности изоферментов цитохрома Р450 in vivo."}},{"type":"paragraph","data":{"text":"Данные in vitro показали ингибирование метаболизма бетагистина под действием препаратов, которые ингибируют моноаминоксидазу (МАО), включая МАО подтипа В (например, селегилин). Следует соблюдать осторожность при одновременном назначении бетагистина и ингибиторов МАО (включая МАО-В)."}},{"type":"paragraph","data":{"text":"Бетагистин является аналогом гистамина, взаимодействие бетагистина с блокаторами H1-гистаминовых рецепторов теоретически может влиять на эффективность одного из этих лекарственных средств."}}]},{"id":15,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"Риска на таблетке предназначена для разламывания таблетки с целью облегчения ее проглатывания и не предназначена для деления её на две равные дозы."}}]},{"id":16,"name":"Влияние на способность управлять автомобилем и движущимися механизмами","slug":"","body":[{"type":"paragraph","data":{"text":"Бетагистин не влияет или незначительно влияет на способность управлять транспортными средствами и работать с механизмами, в клинических исследованиях нежелательные реакции, которые могли бы повлиять на такую способность, не выявлены."}}]},{"id":17,"name":"Форма выпуска","slug":"","body":[{"type":"paragraph","data":{"text":"\n\nТаблетки, 24 мг."}},{"type":"paragraph","data":{"text":"По 10 таблеток в ПВХ/ПВДХ/Ал блистер, по 5 блистеров вместе с инструкцией по применению в пачку картонную."}},{"type":"paragraph","data":{"text":"По 15 таблеток в ПВХ/ПВДХ/Ал блистер, по 2 блистера вместе с инструкцией по применению в пачку картонную."}},{"type":"paragraph","data":{"text":"По 20 таблеток в ПВХ/ПВДХ/Ал блистер, по 1, 2, 3 или 5 блистеров вместе с инструкцией по применению в пачку картонную."}},{"type":"paragraph","data":{"text":"По 25 таблеток в ПВХ/ПВДХ/Ал блистер, по 1, 2 или 4 блистера вместе с инструкцией по применению в пачку картонную.\n\n"}}]},{"id":18,"name":"Условия хранения","slug":"storage","body":[{"type":"paragraph","data":{"text":"\n\nХранить при температуре не выше 25 °C."}},{"type":"paragraph","data":{"text":"Хранить в недоступном для детей месте!\n\n"}}]},{"id":19,"name":"Срок годности","slug":"expiry_date","body":[{"type":"paragraph","data":{"text":"3 года. Не применять по истечении срока годности, указанного на упаковке."}}]},{"id":20,"name":"Условия отпуска","slug":"release_condition","body":[{"type":"paragraph","data":{"text":"Отпускают по рецепту."}}]},{"id":21,"name":"Производитель","slug":"","body":[{"type":"paragraph","data":{"text":"\n\nМайлан Лэбораториз САС,"}},{"type":"paragraph","data":{"text":"Рут де Бельвилль, Лье-ди Майар,"}},{"type":"paragraph","data":{"text":"01400, Шатийон-сюр-Шаларон, Франция"}},{"type":"paragraph","data":{"text":"или"}},{"type":"paragraph","data":{"text":"АО \"ВЕРОФАРМ\","}},{"type":"paragraph","data":{"text":"308013, Россия, г. Белгород, ул. Рабочая, д. 14\n\n"}}]},{"id":22,"name":"Организация, принимающая претензии потребителей","body":[{"type":"paragraph","data":{"text":"\n\nООО «Эбботт Лэбораториз»"}},{"type":"paragraph","data":{"text":"125171, г. Москва, Ленинградское шоссе, дом 16А, стр. 1\n\n"}}]}],"source":null},"description_toggle":false,"short_description":"Фармакодинамика Механизм действия бетагистина известен только частично. Существует несколько возможных гипотез, подтвержденных доклиническими и клиническими данными: - Влияние на гистаминергическую систему Частичный агонист Н1-гистаминовых и антагонист НЗ-гистаминовых рецепторов вестибулярных ядер Ц, обладает незначительной активностью в отношении Н2-рецепторов. Бетагистин увеличивает обмен гистамина и его высвобождение путем блокирования пресинаптических НЗ-рецепторов и снижения количества НЗ-рецепторов. - Усиление кровотока кохлеарной области, а также всего головного мозга Согласно доклиническим исследованиям бетагистин улучшает кровообращение в сосудистой полоске внутреннего уха за счет расслабления прекапиллярных сфинктеров сосудов внутреннего уха. Также показано, что бетагистин усиливает кровоток головного мозга у человека. - Облегчение процесса центральной вестибулярной компенсации Бетагистин ускоряет восстановление вестибулярной функции у животных после односторонней вестибулярной нейрэктомии, ускоряя и облегчая центральную вестибулярную компенсацию за счет антагонизма с НЗ-гистаминовыми рецепторами. Время восстановления после вестибулярной нейрэктомии у человека при лечении бетагистином также уменьшается. - Возбуждение нейронов в вестибулярных ядрах Дозозависимо снижает генерацию потенциалов действия в нейронах латеральных и медиальных вестибулярных ядер. Фармакодинамические свойства, выявленные на животных, обеспечивают положительный терапевтический эффект бетагистина в вестибулярной системе. Эффективность бетагистина была продемонстрирована у пациентов с вестибулярным головокружением и синдромом Меньера, что проявлялось уменьшением выраженности и частоты головокружений. Фармакокинетика Всасывание При пероральном приеме бетагистин быстро и практически полностью всасывается в желудочно-кишечном тракте. После всасывания препарат быстро и почти полностью метаболизируется с образованием метаболита 2-пиридилуксусной кислоты. Концентрация бетагистина в плазме крови очень низкая. Таким образом, фармакокинетические анализы основаны на измерении концентрации метаболита 2-пиридилуксусной кислоты в плазме и моче. При приеме препарата с пищей максимальная концентрация (Стах) препарата в крови ниже, чем при приеме натощак. Однако суммарная абсорбция бетагистина одинакова в обоих случаях, что указывает на то, что прием пищи лишь замедляет всасывание бетагистина. Распределение Связывание бетагистина с белками плазмы крови составляет менее 5 %. Биотрансформация После всасывания бетагистин быстро и почти полностью метаболизируется с образованием метаболита 2-пиридилуксусной кислоты (который не обладает фармакологической активностью). Максимальная концентрация 2-пиридилуксусной кислоты в плазме крови (или моче) достигается через час после приема. Период полувыведения приблизительно 3,5 часа. Выведение 2-пиридилуксусная кислота быстро выводится с мочой. При приеме препарата в дозе 8-48 мг около 85 % начальной дозы обнаруживается в моче. Выведение бетагистина почками или через кишечник незначительно. 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