Таблетки круглые, двояковыпуклые, покрытые пленочной оболочкой розового цвета . На поперечном разрезе почти белого цвета. Допускается незначительная шероховатость.
Фармакологические свойства
Селективный агонист имидазолиновых рецепторов, принимающих участие в тонической и рефлекторной регуляции симпатической нервной системы (локализованы в вентролатеральном отделе продолговатого мозга).
Уменьшает прессорное действие симпатической системы на периферические сосуды, снижает периферическое сосудистое сопротивление, снижает систолическое и диастолическое АД как при однократном приеме, так и при длительном применении, в то время как сердечный выброс и ЧСС существенно не изменяются. При длительном применении уменьшает гипертрофию миокарда левого желудочка, нивелирует признаки миокардиального фиброза, микроартериопатии, нормализует капиллярное кровоснабжение миокарда. На фоне лечения снижается активность норэпинефрина и эпинефрина, ренина, ангиотензина II в покое и при нагрузке, предсердного натрийуретического пептида (при нагрузке) и альдостерона плазмы крови.
Обладает более низким сродством к α2-адренорецепторам, что объясняет меньшую вероятность развития седативного эффекта и сухости во рту.
Уменьшает резистентность тканей к инсулину. Не влияет на обмен глюкозы и липидов.
Фармакокинетика
Всасывание
Абсорбция после приема внутрь - 90%. Прием пищи не влияет на величину абсорбции. Биодоступность - 88%. Cmax в плазме достигается через 30-180 мин после приема внутрь и составляет 1-3 нг/мл.
Распределение
Связывание с белками плазмы крови - 7.2%. Vd - 1.4-3 л/кг. Проникает через ГЭБ. При длительном применении не кумулирует.
Метаболизм
Основной метаболит - дигидрированный моксонидин. Фармакодинамическая активность дегидрированного моксонидина - около 10% по сравнению с моксонидином.
Выведение
T1/2 моксонидина и метаболитов составляет 2.5 и 5 ч, соответственно. В течение 24 ч более 90% моксонидина выводится почками (78% - в неизмененном виде, 13% - в виде дигидрированного моксонидина, 8% - в виде других метаболитов). Менее 1% дозы выводится через кишечник. Моксонидин в незначительной степени выводится при проведении гемодиализа.
Фармакокинетика у особых групп пациентов
У пациентов с артериальной гипертензией не отмечается изменений фармакокинетики моксонидина.
Отмечены клинически незначимые изменения фармакокинетических показателей моксонидина у пациентов пожилого возраста, вероятно обусловленные снижением интенсивности его метаболизма и/или несколько более высокой биодоступностью.
Выведение моксонидина в значительной степени коррелирует с КК. У пациентов с почечной недостаточностью средней степени (КК в интервале 30-60 мл/мин) Css в плазме крови и конечный T1/2 приблизительно в 2 и 1.5 раза выше, чем у пациентов с нормальной функцией почек (КК более 90 мл/мин). У пациентов с почечной недостаточностью тяжелой степени (КК менее 30 мл/мин) Css в плазме крови и конечный Т1/2 в 3 раза выше, чем у пациентов с нормальной функцией почек. У пациентов с терминальной стадией почечной недостаточности (КК менее 10 мл/мин), находящихся на гемодиализе, Css в плазме крови и конечный T1/2, соответственно, в 6 и 4 раза выше, чем у пациентов с нормальной функцией почек. У пациентов с нарушениями функции почек дозу следует подбирать индивидуально.
Показания к применению
артериальная гипертензия.
Противопоказания
выраженные нарушения ритма сердца;
СССУ;
синоатриальная и AV-блокада II и III степени;
выраженная брадикардия (ЧСС менее 50 уд./мин);
острая и хроническая сердечная недостаточность III и IV функционального класса по классификации NYHA;
ангионевротический отек в анамнезе;
печеночная недостаточность тяжелой степени (более 9 баллов по шкале Чайлд-Пью);
хроническая почечная недостаточность (КК менее 30 мл/мин, концентрация креатинина более 160 мкмоль/л);
гемодиализ;
одновременное применение трициклических антидепрессантов;
период лактации;
возраст до 18 лет (эффективность и безопасность не установлены);
возраст старше 75 лет;
повышенная чувствительность к компонентам препарата.
С осторожностью
С осторожностью следует назначать препарат при болезни Паркинсона (тяжелая форма); эпилепсии; глаукоме; депрессии; перемежающейся хромоте; болезни Рейно; AV-блокаде I степени; хронической почечной недостаточности (КК более 30 мл/мин, но менее 60 мл/мин); тяжелых цереброваскулярных нарушениях; тяжелых заболеваниях коронарных сосудов; тяжелой ИБС или нестабильной стенокардии (опыт применения недостаточный); хронической сердечной недостаточности I и II функционального класса по классификации NYHA; после перенесенного инфаркта миокарда; при нарушениях функции печени; беременности.
Применение при беременности и в период грудного вскармливания
Клинических данных о негативном влиянии на течение беременности нет. Однако препарат Моксонидин Канон следует назначать беременным только в том случае, когда предполагаемая польза для матери превосходит потенциальный риск для плода.
Моксонидин выделяется с грудным молоком. Если применение препарата Моксонидин Канон необходимо в период лактации, грудное вскармливание следует прекратить.
Способ применения и дозы
Препарат принимают внутрь, 1 раз/сут, предпочтительно в утренние часы, независимо от приема пищи. Таблетки следует запивать достаточным количеством жидкости.
В большинстве случаев начальная доза препарата Моксонидин Канон составляет 0.2 мг/сут. При недостаточности терапевтического эффекта дозу можно увеличить после 3 недель терапии до 0.4 мг/сут (в 2 приема (утром и вечером) или однократно).
Максимальная суточная доза, которую следует разделить на 2 приема (утром и вечером), составляет 0.6 мг. Максимальная разовая доза составляет 0.4 мг.
У пациентов пожилого возраста с нормальной функцией почек рекомендации по режиму дозирования такие же, как и для взрослых пациентов.
У пациентов с почечной недостаточностью (КК 30-60 мл/мин) и пациентов, находящихся на гемодиализе, разовая доза не должна превышать 0.2 мг, максимальная суточная доза - 0.4 мг.
Побочное действие
Классификация ВОЗ частоты развития побочных эффектов: очень часто ≥1/10 назначений (>10%); часто от ≥1/100 до <1/10 назначений (>1% и <10%); нечасто от ≥1/1000 до <1/100 назначений (>0.1% и <1%); редко от ≥1/10 000 до <1/1000 назначений (>0.01% и <0.1%); очень редко <1/10 000 назначений (<0.01%).
Психические нарушения: часто - снижение концентрации внимания; нечасто - депрессия, тревога, нервозность.
Со стороны ЦНС: часто - повышенная утомляемость, сонливость, головная боль, головокружение; нечасто - парестезии, бессонница, обморок.
Со стороны органа зрения: нечасто - сухость глаз, вызывающая зуд или ощущение жжения в глазах.
Со стороны органа слуха: нечасто - звон в ушах.
Со стороны сердечно-сосудистой системы: часто - симптомы вазодилатации; нечасто - снижение АД, ортостатическая гипотензия, синдром Рейно, нарушения периферической циркуляции.
Со стороны пищеварительной системы: часто - сухость слизистой оболочки полости рта, запор, диспепсические расстройства; нечасто - тошнота, анорексия; очень редко - гепатит, холестаз.
Со стороны мочевыделительной системы: нечасто - задержка мочи или недержание.
Со стороны половых органов и молочной железы: нечасто - импотенция, снижение либидо, гинекомастия.
Со стороны кожи и подкожных тканей: нечасто - кожная сыпь, зуд, отеки различной локализации; очень редко - ангионевротический отек.
Со стороны костно-мышечной системы: часто - боль в спине; нечасто - боль в шее.
Прочие: часто - астения; нечасто - слабость в ногах, обморок, боль в области околоушных желез.
Передозировка
Симптомы: головная боль, седативный эффект, сонливость, чрезмерное снижение АД, головокружение, общая слабость, брадикардия, повышенная утомляемость, сухость во рту, рвота и боль в желудке. Потенциально возможны также парадоксальное повышение АД, тахикардия, гипергликемия.
Лечение: специфического антидота нет. Показано промывание желудка (сразу после приема), прием активированного угля и слабительных средств, проведение симптоматической терапии. В случае чрезмерного снижения АД рекомендуется восстановление ОЦК за счет введения жидкости, назначение допамина. Брадикардия может быть купирована введением атропина. Антагонисты α-адренорецепторов могут уменьшить или устранить преходящую артериальную гипертензию при передозировке препаратом Моксонидин Канон.
Взаимодействие с другими лекарственными средствами
Моксонидин Канон можно назначать с тиазидными диуретиками и блокаторами медленных кальциевых каналов. Совместное применение препарата Моксонидин Канон с этими и другими антигипертензивными средствами приводит к аддитивному эффекту и усилению гипотензивного эффекта.
При назначении препарата Моксонидин Канон с гидрохлоротиазидом, глибенкламидом (глибуридом) или дигоксином фармакокинетическое взаимодействие отсутствует.
Трициклические антидепрессанты могут снизить эффективность антигипертензивных средств центрального действия, поэтому, их одновременное применение не рекомендуется.
Препарат Моксонидин Канон умеренно усиливает сниженную когнитивную способность у пациентов, принимающих лоразепам.
Назначение препарата Моксонидин Канон совместно с производными бензодиазепина может сопровождаться усилением седативного эффекта последних.
Препарат Моксонидин Канон усиливает угнетающее действие на ЦНС анксиолитиков, барбитуратов и этанола.
Бета-адреноблокаторы при совместном применении с моксонидином усиливают брадикардию, выраженность отрицательного ино- и дромотропного действия.
При назначении препарата Моксонидин Канон совместно с моклобемидом фармакодинамическое взаимодействие отсутствует.
Особые указания
При необходимости отмены одновременно принимаемых бета-адреноблокаторов и препарата Моксонидин Канон, сначала отменяют бета-адреноблокаторы и только через несколько дней - препарат Моксонидин Канон.
Не рекомендуется назначать трициклические антидепрессанты одновременно с препаратом Моксонидин Канон.
Во время лечения необходим регулярный контроль АД, ЧСС и ЭКГ.
Препарат Моксонидин Канон можно назначать с тиазидными диуретиками, ингибиторами АПФ и блокаторами медленных кальциевых каналов.
Прекращать прием препарата Моксонидин Канон следует постепенно.
Влияние на способность к управлению транспортными средствами и механизмами
Принимая во внимание возможное возникновение сонливости и головокружения, в период лечения препаратом Моксонидин Канон пациентам следует соблюдать осторожность при занятии потенциально опасными видами деятельности, требующими повышенной концентрации внимания, таких как вождение автотранспорта или управление механизмами.
Условия хранения
Препарат следует хранить в недоступном для детей, сухом, защищенном от света месте при температуре не выше 25°С.
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На поперечном разрезе почти белого цвета. Допускается незначительная шероховатость."}}]},{"id":7,"name":"Фармакологические свойства","slug":"pharmacologic_effects","body":[{"type":"paragraph","data":{"text":"Селективный агонист имидазолиновых рецепторов, принимающих участие в тонической и рефлекторной регуляции симпатической нервной системы (локализованы в вентролатеральном отделе продолговатого мозга)."}},{"type":"paragraph","data":{"text":"Уменьшает прессорное действие симпатической системы на периферические сосуды, снижает периферическое сосудистое сопротивление, снижает систолическое и диастолическое АД как при однократном приеме, так и при длительном применении, в то время как сердечный выброс и ЧСС существенно не изменяются. При длительном применении уменьшает гипертрофию миокарда левого желудочка, нивелирует признаки миокардиального фиброза, микроартериопатии, нормализует капиллярное кровоснабжение миокарда. На фоне лечения снижается активность норэпинефрина и эпинефрина, ренина, ангиотензина II в покое и при нагрузке, предсердного натрийуретического пептида (при нагрузке) и альдостерона плазмы крови."}},{"type":"paragraph","data":{"text":"Обладает более низким сродством к α\u003csub\u003e2\u003c/sub\u003e-адренорецепторам, что объясняет меньшую вероятность развития седативного эффекта и сухости во рту."}},{"type":"paragraph","data":{"text":"Уменьшает резистентность тканей к инсулину. Не влияет на обмен глюкозы и липидов."}},{"type":"header","data":{"text":"Фармакокинетика","level":4}},{"type":"paragraph","data":{"text":"\u003ci\u003eВсасывание\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Абсорбция после приема внутрь - 90%. Прием пищи не влияет на величину абсорбции. Биодоступность - 88%. C\u003csub\u003emax\u003c/sub\u003e в плазме достигается через 30-180 мин после приема внутрь и составляет 1-3 нг/мл."}},{"type":"paragraph","data":{"text":"\u003ci\u003eРаспределение\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Связывание с белками плазмы крови - 7.2%. V\u003csub\u003ed\u003c/sub\u003e - 1.4-3 л/кг. Проникает через ГЭБ. При длительном применении не кумулирует."}},{"type":"paragraph","data":{"text":"\u003ci\u003eМетаболизм\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Основной метаболит - дигидрированный моксонидин. Фармакодинамическая активность дегидрированного моксонидина - около 10% по сравнению с моксонидином."}},{"type":"paragraph","data":{"text":"\u003ci\u003eВыведение\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"T\u003csub\u003e1/2\u003c/sub\u003e моксонидина и метаболитов составляет 2.5 и 5 ч, соответственно. В течение 24 ч более 90% моксонидина выводится почками (78% - в неизмененном виде, 13% - в виде дигидрированного моксонидина, 8% - в виде других метаболитов). Менее 1% дозы выводится через кишечник. Моксонидин в незначительной степени выводится при проведении гемодиализа."}},{"type":"paragraph","data":{"text":"\u003ci\u003eФармакокинетика у особых групп пациентов\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"У пациентов с артериальной гипертензией не отмечается изменений фармакокинетики моксонидина."}},{"type":"paragraph","data":{"text":"Отмечены клинически незначимые изменения фармакокинетических показателей моксонидина у пациентов пожилого возраста, вероятно обусловленные снижением интенсивности его метаболизма и/или несколько более высокой биодоступностью."}},{"type":"paragraph","data":{"text":"Выведение моксонидина в значительной степени коррелирует с КК. У пациентов с почечной недостаточностью средней степени (КК в интервале 30-60 мл/мин) C\u003csub\u003ess\u003c/sub\u003e в плазме крови и конечный T\u003csub\u003e1/2 \u003c/sub\u003eприблизительно в 2 и 1.5 раза выше, чем у пациентов с нормальной функцией почек (КК более 90 мл/мин). У пациентов с почечной недостаточностью тяжелой степени (КК менее 30 мл/мин) C\u003csub\u003ess\u003c/sub\u003e в плазме крови и конечный Т\u003csub\u003e1/2\u003c/sub\u003e в 3 раза выше, чем у пациентов с нормальной функцией почек. У пациентов с терминальной стадией почечной недостаточности (КК менее 10 мл/мин), находящихся на гемодиализе, C\u003csub\u003ess\u003c/sub\u003e в плазме крови и конечный T\u003csub\u003e1/2\u003c/sub\u003e, соответственно, в 6 и 4 раза выше, чем у пациентов с нормальной функцией почек. У пациентов с нарушениями функции почек дозу следует подбирать индивидуально."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"list","data":{"style":"ordered","items":["артериальная гипертензия."]}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"list","data":{"style":"ordered","items":["выраженные нарушения ритма сердца;","СССУ;","синоатриальная и AV-блокада II и III степени;","выраженная брадикардия (ЧСС менее 50 уд./мин);","острая и хроническая сердечная недостаточность III и IV функционального класса по классификации NYHA;","ангионевротический отек в анамнезе;","печеночная недостаточность тяжелой степени (более 9 баллов по шкале Чайлд-Пью);","хроническая почечная недостаточность (КК менее 30 мл/мин, концентрация креатинина более 160 мкмоль/л);","гемодиализ;","одновременное применение трициклических антидепрессантов;","период лактации;","возраст до 18 лет (эффективность и безопасность не установлены);","возраст старше 75 лет;","повышенная чувствительность к компонентам препарата."]}}]},{"id":10,"name":"С осторожностью","slug":"cautions","body":[{"type":"paragraph","data":{"text":"\u003ci\u003eС осторожностью\u003c/i\u003e следует назначать препарат при болезни Паркинсона (тяжелая форма); эпилепсии; глаукоме; депрессии; перемежающейся хромоте; болезни Рейно; AV-блокаде I степени; хронической почечной недостаточности (КК более 30 мл/мин, но менее 60 мл/мин); тяжелых цереброваскулярных нарушениях; тяжелых заболеваниях коронарных сосудов; тяжелой ИБС или нестабильной стенокардии (опыт применения недостаточный); хронической сердечной недостаточности I и II функционального класса по классификации NYHA; после перенесенного инфаркта миокарда; при нарушениях функции печени; беременности."}}]},{"id":11,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","body":[{"type":"paragraph","data":{"text":"Клинических данных о негативном влиянии на течение беременности нет. Однако препарат Моксонидин Канон следует назначать беременным только в том случае, когда предполагаемая польза для матери превосходит потенциальный риск для плода."}},{"type":"paragraph","data":{"text":"Моксонидин выделяется с грудным молоком. Если применение препарата Моксонидин Канон необходимо в период лактации, грудное вскармливание следует прекратить."}}]},{"id":12,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Препарат принимают внутрь, 1 раз/сут, предпочтительно в утренние часы, независимо от приема пищи. Таблетки следует запивать достаточным количеством жидкости."}},{"type":"paragraph","data":{"text":"В большинстве случаев начальная доза препарата Моксонидин Канон составляет 0.2 мг/сут. При недостаточности терапевтического эффекта дозу можно увеличить после 3 недель терапии до 0.4 мг/сут (в 2 приема (утром и вечером) или однократно)."}},{"type":"paragraph","data":{"text":"Максимальная суточная доза, которую следует разделить на 2 приема (утром и вечером), составляет 0.6 мг. Максимальная разовая доза составляет 0.4 мг."}},{"type":"paragraph","data":{"text":"У \u003cb\u003eпациентов пожилого возраста\u003c/b\u003e с нормальной функцией почек рекомендации по режиму дозирования такие же, как и для взрослых пациентов."}},{"type":"paragraph","data":{"text":"У \u003cb\u003eпациентов с почечной недостаточностью (КК 30-60 мл/мин)\u003c/b\u003e и \u003cb\u003eпациентов, находящихся на гемодиализе\u003c/b\u003e, разовая доза не должна превышать 0.2 мг, максимальная суточная доза - 0.4 мг."}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Классификация ВОЗ частоты развития побочных эффектов: очень часто ≥1/10 назначений (>10%); часто от ≥1/100 до <1/10 назначений (>1% и <10%); нечасто от ≥1/1000 до <1/100 назначений (>0.1% и <1%); редко от ≥1/10 000 до <1/1000 назначений (>0.01% и <0.1%); очень редко <1/10 000 назначений (<0.01%)."}},{"type":"paragraph","data":{"text":"\u003ci\u003eПсихические нарушения: \u003c/i\u003eчасто - снижение концентрации внимания; нечасто - депрессия, тревога, нервозность."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны ЦНС:\u003c/i\u003e часто - повышенная утомляемость, сонливость, головная боль, головокружение; нечасто - парестезии, бессонница, обморок."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны органа зрения:\u003c/i\u003e нечасто - сухость глаз, вызывающая зуд или ощущение жжения в глазах."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны органа слуха:\u003c/i\u003e нечасто - звон в ушах."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны сердечно-сосудистой системы:\u003c/i\u003e часто - симптомы вазодилатации; нечасто - снижение АД, ортостатическая гипотензия, синдром Рейно, нарушения периферической циркуляции."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны пищеварительной системы:\u003c/i\u003e часто - сухость слизистой оболочки полости рта, запор, диспепсические расстройства; нечасто - тошнота, анорексия; очень редко - гепатит, холестаз."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны мочевыделительной системы:\u003c/i\u003e нечасто - задержка мочи или недержание."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны половых органов и молочной железы:\u003c/i\u003e нечасто - импотенция, снижение либидо, гинекомастия."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны кожи и подкожных тканей: \u003c/i\u003eнечасто - кожная сыпь, зуд, отеки различной локализации; очень редко - ангионевротический отек."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны костно-мышечной системы: \u003c/i\u003eчасто - боль в спине; нечасто - боль в шее."}},{"type":"paragraph","data":{"text":"\u003ci\u003eПрочие:\u003c/i\u003e часто - астения; нечасто - слабость в ногах, обморок, боль в области околоушных желез."}}]},{"id":14,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"\u003ci\u003eСимптомы:\u003c/i\u003e головная боль, седативный эффект, сонливость, чрезмерное снижение АД, головокружение, общая слабость, брадикардия, повышенная утомляемость, сухость во рту, рвота и боль в желудке. Потенциально возможны также парадоксальное повышение АД, тахикардия, гипергликемия."}},{"type":"paragraph","data":{"text":"\u003ci\u003eЛечение:\u003c/i\u003e специфического антидота нет. Показано промывание желудка (сразу после приема), прием активированного угля и слабительных средств, проведение симптоматической терапии. В случае чрезмерного снижения АД рекомендуется восстановление ОЦК за счет введения жидкости, назначение допамина. Брадикардия может быть купирована введением атропина. Антагонисты α-адренорецепторов могут уменьшить или устранить преходящую артериальную гипертензию при передозировке препаратом Моксонидин Канон."}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"Моксонидин Канон можно назначать с тиазидными диуретиками и блокаторами медленных кальциевых каналов. Совместное применение препарата Моксонидин Канон с этими и другими антигипертензивными средствами приводит к аддитивному эффекту и усилению гипотензивного эффекта."}},{"type":"paragraph","data":{"text":"При назначении препарата Моксонидин Канон с гидрохлоротиазидом, глибенкламидом (глибуридом) или дигоксином фармакокинетическое взаимодействие отсутствует."}},{"type":"paragraph","data":{"text":"Трициклические антидепрессанты могут снизить эффективность антигипертензивных средств центрального действия, поэтому, их одновременное применение не рекомендуется."}},{"type":"paragraph","data":{"text":"Препарат Моксонидин Канон умеренно усиливает сниженную когнитивную способность у пациентов, принимающих лоразепам."}},{"type":"paragraph","data":{"text":"Назначение препарата Моксонидин Канон совместно с производными бензодиазепина может сопровождаться усилением седативного эффекта последних."}},{"type":"paragraph","data":{"text":"Препарат Моксонидин Канон усиливает угнетающее действие на ЦНС анксиолитиков, барбитуратов и этанола."}},{"type":"paragraph","data":{"text":"Бета-адреноблокаторы при совместном применении с моксонидином усиливают брадикардию, выраженность отрицательного ино- и дромотропного действия."}},{"type":"paragraph","data":{"text":"При назначении препарата Моксонидин Канон совместно с моклобемидом фармакодинамическое взаимодействие отсутствует."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"При необходимости отмены одновременно принимаемых бета-адреноблокаторов и препарата Моксонидин Канон, сначала отменяют бета-адреноблокаторы и только через несколько дней - препарат Моксонидин Канон."}},{"type":"paragraph","data":{"text":"Не рекомендуется назначать трициклические антидепрессанты одновременно с препаратом Моксонидин Канон."}},{"type":"paragraph","data":{"text":"Во время лечения необходим регулярный контроль АД, ЧСС и ЭКГ."}},{"type":"paragraph","data":{"text":"Препарат Моксонидин Канон можно назначать с тиазидными диуретиками, ингибиторами АПФ и блокаторами медленных кальциевых каналов."}},{"type":"paragraph","data":{"text":"Прекращать прием препарата Моксонидин Канон следует постепенно."}},{"type":"paragraph","data":{"text":"\u003ci\u003eВлияние на способность к управлению транспортными средствами и механизмами\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Принимая во внимание возможное возникновение сонливости и головокружения, в период лечения препаратом Моксонидин Канон пациентам следует соблюдать осторожность при занятии потенциально опасными видами деятельности, требующими повышенной концентрации внимания, таких как вождение автотранспорта или управление механизмами."}}]},{"id":19,"name":"Условия хранения","slug":"storage","body":[{"type":"paragraph","data":{"text":"Препарат следует хранить в недоступном для детей, сухом, защищенном от света месте при температуре не выше 25°С."}}]},{"id":20,"name":"Срок годности","slug":"expiry_date","body":[{"type":"paragraph","data":{"text":" 2 года."}}]},{"id":21,"name":"Условия отпуска","slug":"release_condition","body":[{"type":"paragraph","data":{"text":"Препарат отпускается по рецепту."}}]}],"source":{"title":"('Эркафарм/Столетов',)","url":"https://stoletov.ru/"}},"description_toggle":false,"short_description":"Селективный агонист имидазолиновых рецепторов, принимающих участие в тонической и рефлекторной регуляции симпатической нервной системы (локализованы в вентролатеральном отделе продолговатого мозга). Уменьшает прессорное действие симпатической системы на периферические сосуды, снижает периферическое сосудистое сопротивление, снижает систолическое и диастолическое АД как при однократном приеме, так и при длительном применении, в то время как сердечный выброс и ЧСС существенно не изменяются. При длительном применении уменьшает гипертрофию миокарда левого желудочка, нивелирует признаки миокардиального фиброза, микроартериопатии, нормализует капиллярное кровоснабжение миокарда. На фоне лечения снижается активность норэпинефрина и эпинефрина, ренина, ангиотензина II в покое и при нагрузке, предсердного натрийуретического пептида (при нагрузке) и альдостерона плазмы крови. Обладает более низким сродством к α2-адренорецепторам, что объясняет меньшую вероятность развития седативного эффекта и сухости во рту. Уменьшает резистентность тканей к инсулину. Не влияет на обмен глюкозы и липидов.ВсасываниеАбсорбция после приема внутрь - 90%. Прием пищи не влияет на величину абсорбции. Биодоступность - 88%. Cmaxв плазме достигается через 30-180 мин после приема внутрь и составляет 1-3 нг/мл.РаспределениеСвязывание с белками плазмы крови - 7.2%. Vd- 1.4-3 л/кг. Проникает через ГЭБ. При длительном применении не кумулирует.МетаболизмОсновной метаболит - дигидрированный моксонидин. Фармакодинамическая активность дегидрированного моксонидина - около 10% по сравнению с моксонидином.ВыведениеT1/2моксонидина и метаболитов составляет 2.5 и 5 ч, соответственно. В течение 24 ч более 90% моксонидина выводится почками (78% - в неизмененном виде, 13% - в виде дигидрированного моксонидина, 8% - в виде других метаболитов). Менее 1% дозы выводится через кишечник. Моксонидин в незначительной степени выводится при проведении гемодиализа.Фармакокинетика у особых групп пациентовУ пациентов с артериальной гипертензией не отмечается изменений фармакокинетики моксонидина. Отмечены клинически незначимые изменения фармакокинетических показателей моксонидина у пациентов пожилого возраста, вероятно обусловленные снижением интенсивности его метаболизма и/или несколько более высокой биодоступностью. Выведение моксонидина в значительной степени коррелирует с КК. У пациентов с почечной недостаточностью средней степени (КК в интервале 30-60 мл/мин) Cssв плазме крови и конечный T1/2приблизительно в 2 и 1.5 раза выше, чем у пациентов с нормальной функцией почек (КК более 90 мл/мин). У пациентов с почечной недостаточностью тяжелой степени (КК менее 30 мл/мин) Cssв плазме крови и конечный Т1/2в 3 раза выше, чем у пациентов с нормальной функцией почек. У пациентов с терминальной стадией почечной недостаточности (КК менее 10 мл/мин), находящихся на гемодиализе, Cssв плазме крови и конечный T1/2, соответственно, в 6 и 4 раза выше, чем у пациентов с нормальной функцией почек. 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