Лаципил - гипотензивное. Оказывает селективное действие на к... Инструкция
Показания к применению
Лечение артериальной гипертензии в качестве монотерапии или в комбинации с другими антигипертензивными средствами, например с бета-адреноблокаторами, диуретиками или ингибиторами АПФ.
Противопоказания
Повышенная чувствительность к любому из компонентов препарата.
Оказывает селективное действие на кальциевые каналы гладких мышц сосудов.
Фармакодинамика
Главный эффект Лаципила состоит в расширении периферических артериол, уменьшении ОПСС и снижении АД. В терапевтических дозах нормализует трансмембранный ток Са2+, не влияет на тонус вен, синоатриальный и AV узлы, не обладает отрицательным инотропным действием.
При назначении лацидипина в дозе 4 мг наблюдается минимальное удлинение интервала QT.
Фармакокинетика
После приема внутрь лацидипин быстро, но в незначительной степени всасывается из ЖКТ и подвергается интенсивному метаболизму при «первом прохождении» через печень. Его абсолютная биодоступность составляет приблизительно 10%.
Cmax в плазме крови достигается через 30–150 мин. Лацидипин обладает очень высокой (более 95%) способностью связываться с альбумином и альфа1-гликопротеином. Лацидипин метаболизируется главным образом в печени с образованием четырех основных метаболитов, обладающих незначительной фармакологической активностью. Нет данных, подтверждающих способность лацидипина индуцировать или ингибировать активность печеночных ферментов. Приблизительно 70% от принятой дозы лацидипина выводится в виде метаболитов с фекалиями, а оставшаяся часть дозы — в виде метаболитов с мочой.
При достижении равновесной концентрации T1/2 лацидипина варьирует от 13 до 19 ч.
Показания к применению
Лечение артериальной гипертензии в качестве монотерапии или в комбинации с другими антигипертензивными средствами, например с бета-адреноблокаторами, диуретиками или ингибиторами АПФ.
Противопоказания
Повышенная чувствительность к любому из компонентов препарата.
С осторожностью
С осторожностью: следует применять у пациентов с нарушением функции синоатриального и АV узлов, с врожденным и приобретенным (документально подтвержденным) удлинением интервалаQT, с низким сердечным выбросом (например при тяжелом аортальном стенозе), с нестабильной стенокардией, с недавно перенесенным инфарктом миокарда, с нарушением функции печени, а также при одновременном назначении с препаратами, удлиняющими интервал QT.
Способ применения и дозы
Внутрь. При лечении артериальной гипертензии необходимо ориентироваться на тяжесть заболевания и индивидуальную реакцию пациента.
Начальная доза — 2 мг 1 раз в сутки, в одно и то же время, предпочтительно утром, независимо от приема пищи.
При необходимости возможно увеличение дозы до 4 мг/сут и даже до 6 мг/сут по истечении времени, необходимого для достижения терапевтического эффекта. Обычно в клинической практике этот период составляет 3–4 нед, если только состояние пациента не требует более быстрого увеличения дозы.
У пациентов с нарушением функции печени или почек, пожилого возраста коррекции дозы Лаципила не требуется.
Лаципил не рекомендуется применять у пациентов младше 18 лет, поскольку опыт применения препарата в педиатрии отсутствует.
Побочное действие
Обычно Лаципил хорошо переносится. У некоторых пациентов могут возникать легкие побочные эффекты, связанные с расширением периферических сосудов. Наиболее типичными являются: головная боль, приливы, периферические отеки, головокружение и сердцебиение. Они обычно носят преходящий характер и, как правило, исчезают при продолжении приема Лаципила в прежней дозе.
Редко — астения, кожные высыпания (включая эритему и зуд), функциональные расстройства желудка, тошнота, полиурия и гиперплазия десен.
Как и другие препараты дигидропиридинового ряда, у небольшого числа пациентов лаципил вызывает обострение стенокардии обычно в начале лечения. К данному побочному эффекту более всего склонны пациенты с клинически выраженной ИБС.
Лаципил не вызывает значимых изменений показателей крови и биохимических параметров. В очень редких случаях наблюдается обратимое повышение уровня ЩФ в плазме крови.
Передозировка
Симптомы: выраженная артериальная гипотензия и тахикардия. Теоретически лацидипин способен вызывать брадикардию и замедление AV проводимости.
Лечение: симптоматическая терапия. Специфического антидота не существует.
Взаимодействие с другими лекарственными средствами
Сочетанное применение лацидипина и других антигипертензивных препаратов, например, диуретиков, бета-адреноблокаторов или ингибиторов АПФ, может оказывать аддитивный гипотензивный эффект.
Однако специфических взаимодействий лацидипина с другими широко применяемыми антигипертензивными препаратами, например с бета-адреноблокаторами и диуретиками, а также с дигоксином, толбутамидом и варфарином не отмечается.
Гипотензивное действие Лаципила ослабляют НПВС (блокирование синтеза ПГ почками и задержка Na+) и эстрогены (задержка Na+).
Концентрация лацидипина в плазме крови может повышаться при одновременном приеме циметидина.
Как и другие препараты дигидропиридинового ряда, Лаципил нельзя запивать грейпфрутовым соком, поскольку это может снизить его биодоступность.
У пациентов после трансплантации почки, принимавших циклоспорин, Лаципил устраняет вызванное циклоспорином снижение почечного кровотока и скорости клубочковой фильтрации.
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Лацидипин метаболизируется главным образом в печени с образованием четырех основных метаболитов, обладающих незначительной фармакологической активностью. Нет данных, подтверждающих способность лацидипина индуцировать или ингибировать активность печеночных ферментов. Приблизительно 70% от принятой дозы лацидипина выводится в виде метаболитов с фекалиями, а оставшаяся часть дозы — в виде метаболитов с мочой."}},{"type":"paragraph","data":{"text":"При достижении равновесной концентрации T\u003csub\u003e1/2\u003c/sub\u003e лацидипина варьирует от 13 до 19 ч."}}]},{"id":10,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"Лечение артериальной гипертензии в качестве монотерапии или в комбинации с другими антигипертензивными средствами, например с бета-адреноблокаторами, диуретиками или ингибиторами АПФ."}}]},{"id":11,"name":"Противопоказания","slug":"contraindications","body":[{"type":"paragraph","data":{"text":"Повышенная чувствительность к любому из компонентов препарата."}}]},{"id":12,"name":"С осторожностью","slug":"cautions","body":[{"type":"paragraph","data":{"text":"С осторожностью: следует применять у пациентов с нарушением функции синоатриального и АV узлов, с врожденным и приобретенным (документально подтвержденным) удлинением интервалаQT, с низким сердечным выбросом (например при тяжелом аортальном стенозе), с нестабильной стенокардией, с недавно перенесенным инфарктом миокарда, с нарушением функции печени, а также при одновременном назначении с препаратами, удлиняющими интервал QT."}}]},{"id":14,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Внутрь. При лечении артериальной гипертензии необходимо ориентироваться на тяжесть заболевания и индивидуальную реакцию пациента."}},{"type":"paragraph","data":{"text":"Начальная доза — 2 мг 1 раз в сутки, в одно и то же время, предпочтительно утром, независимо от приема пищи."}},{"type":"paragraph","data":{"text":"При необходимости возможно увеличение дозы до 4 мг/сут и даже до 6 мг/сут по истечении времени, необходимого для достижения терапевтического эффекта. Обычно в клинической практике этот период составляет 3–4 нед, если только состояние пациента не требует более быстрого увеличения дозы."}},{"type":"paragraph","data":{"text":"У пациентов с нарушением функции печени или почек, пожилого возраста коррекции дозы Лаципила не требуется."}},{"type":"paragraph","data":{"text":"Лаципил не рекомендуется применять у пациентов младше 18 лет, поскольку опыт применения препарата в педиатрии отсутствует."}}]},{"id":15,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Обычно Лаципил хорошо переносится. У некоторых пациентов могут возникать легкие побочные эффекты, связанные с расширением периферических сосудов. Наиболее типичными являются: головная боль, приливы, периферические отеки, головокружение и сердцебиение. Они обычно носят преходящий характер и, как правило, исчезают при продолжении приема Лаципила в прежней дозе."}},{"type":"paragraph","data":{"text":"Редко — астения, кожные высыпания (включая эритему и зуд), функциональные расстройства желудка, тошнота, полиурия и гиперплазия десен."}},{"type":"paragraph","data":{"text":"Как и другие препараты дигидропиридинового ряда, у небольшого числа пациентов лаципил вызывает обострение стенокардии обычно в начале лечения. К данному побочному эффекту более всего склонны пациенты с клинически выраженной ИБС."}},{"type":"paragraph","data":{"text":"Лаципил не вызывает значимых изменений показателей крови и биохимических параметров. В очень редких случаях наблюдается обратимое повышение уровня ЩФ в плазме крови."}}]},{"id":16,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"Симптомы: выраженная артериальная гипотензия и тахикардия. 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