Таблетки почти белого цвета, круглой формы, двояковыпуклые, с риской с одной стороны.
Фармакологические свойства
Максимальные концентрации в плазме крови достигаются через 1,7-3,2 часа после приема пиридостигмина бромида. После приема 60 мг пиридостигмина бромида плазменный уровень составляет 40-60 нг/мл. В исследованиях у пациентов с миастенией гравис максимальные уровни в крови достигаются через 3 часа, а проявления клинического и нейрофизиологического эффектов наблюдались через 30 мин и достигали максимума через 120-150 мин. Четкой связи между дозой и концентрацией в плазме крови/величине уровня в плазме крови или изменениями миастенических симптомов нет. Однако при уровнях более 100 нг/мл эффективность препарата не растет.
Объем распределения пиридостигмина бромида составляет примерно 0,5- 1,7 л/кг массы тела.
Пиридостигмина бромид метаболизируется в печени. Основным метаболитом является 3-гидрокси-N-метилпиридин. Выводится главным образом почками, после введения период полувыведения из плазмы составляет около 1,5 часа. После перорального применения период полувыведения увеличивается до 3-3,5 часов. Биодоступность пиридостигмина бромида после перорального приема колебалась от 8% до 20%. У больных миастенией биодоступность может снижаться ниже 4%.
Фармакодинамика
Пиридостигмина бромид ингибирует холинэстеразу. Относится к холиномиметикам не прямого действия. Ингибирование фермента способствует накоплению ацетилхолина на рецепторах в холинергических синапсах, приводит к более выраженному и долговременному эффекту ацетилхолина. Препарат преимущественно действует на периферическую нервную систему. Он не влияет на функции центральной нервной системы, поскольку из-за низкой растворимости в липидах не проникает через гематоэнцефалический барьер.
Показания к применению
Миастения гравис (gravis).
Противопоказания
Повышенная чувствительность к пиридостигмина бромиду и другим компонентам препарата;
спастические состояния органов желудочно-кишечного тракта;
миотония;
шок в послеоперационном периоде.
Применение при беременности и в период грудного вскармливания
Противопоказан детям до 18 лет, при беременности и лактации.
Способ применения и дозы
Миастения гравис.
Для симптоматического лечения миастении гравис у взрослых рекомендуется применять по 1-3 таблетки препарата Пиридостигмина бромид 3-4 раза в сутки (180-720 мг в сутки).
Больные миастенией гравис требуют тщательного индивидуального подбора дозы в зависимости от течения заболевания и ответа больного на лечение. Приведенные выше дозы являются лишь рекомендациями, однако не следует превышать максимальную суточную дозу 720 мг.
Лечение пациентов с заболеваниями почек.
Пациентам с заболеваниями почек препарат следует назначать в низких дозах, потому что пиридостигмина бромид в неизмененном виде выводится из организма в основном почками (75%). При уровне креатинина 2 мг/дл следует применять половинную поддерживающую дозу или соответственно увеличить вдвое интервал между приемом доз. Поэтому необходимую дозу следует подбирать индивидуально для каждого больного, в зависимости от реакции на терапию препаратом. Рекомендовано тщательное медицинское обследование.
Внутрь, запивая водой.
Дозу и продолжительность лечения определяет врач в зависимости от течения заболевания и реакции пациента на лечение.
Побочное действие
Со стороны органа зрения: частота неизвестна: миоз, слезотечение, нарушение аккомодации.
Со стороны сердца: частота не известна: аритмия (в том числе брадикардия, тахикардия, АВ-блокада), а также гипотония.
Со стороны дыхательной системы, органов грудной клетки и средостения: частота не известна: усиление секреции бронхиальных желез в сочетании с бронхоспазмом.
Со стороны желудочно-кишечного тракта: частота не известна: тошнота, рвота, диарея, спазматические боли в животе, желудочно-кишечная гиперкинезия, повышенное слюноотделение.
Со стороны кожи и подкожных тканей: частота не известна: кожная сыпь (обычно исчезает вскоре после прекращения лечения), интенсивное потоотделение.
Со стороны скелетно-мышечной и соединительной ткани: частота не известна: повышенная мышечная слабость, тремор и миофибрилляция или мышечная гипотония.
Со стороны почек и мочевыводящих путей: частота не известна: позывы к мочеиспусканию.
Указанные нежелательные реакции могут быть признаками передозировки или холинергического криза. Поэтому следует обязательно выяснить причину симптомов и, при необходимости, применить 1-2 мг атропина сульфат путем подкожного, внутримышечного или медленного введения для устранения холиномиметических эффектов.
Если любые из указанных в инструкции побочных эффектов усугубляются, или Вы заметили любые другие побочные эффекты, не указанные в инструкции, сообщите об этом врачу.
Взаимодействие с другими лекарственными средствами
Сочетание с другими ингибиторами холинэстеразы или холиномиметиками может усиливать действие пиридостигмина бромида.
Препарат способен усиливать холиномиметические эффекты морфия и его производных.
Усиливает действие деполяризующих миорелаксантов (например, сукцинилхолина).
Атропин ослабляет побочные действия пиридостигмина бромида на слюнные железы, глаза, сердце, мышцы бронхов и кишечник. При этом никотинергические эффекты на скелетные мышцы остаются без изменений.
Метилцеллюлоза полностью тормозит всасывание пиридостигмина бромида, а активированный уголь почти полностью его адсорбирует.
Аминогликозиды (например, стрептомицин, неомицин, канамицин, гентамицин), полипептидные антибиотики (полимиксин, колистин), некоторые другие антибиотики, например, окситетрациклин, клиндамицин и линкомицин, многочисленные антиаритмические средства (хинидин, прокаинамид, пропранолол), пеницилламин, литий, транквилизаторы бензодиазепинового типа и фенотиазины (например, хлорпромазин) могут ослаблять эффект пиридостигмина бромида и за счет этого вызвать миастенические симптомы.
Высокие дозы кортикостероидов также могут ослаблять эффект пиридостигмина бромида.
В том случае, если Вы принимаете другие лекарства, перед приемом препарата обязательно проконсультируйтесь с врачом.
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После приема 60 мг пиридостигмина бромида плазменный уровень составляет 40-60 нг/мл. В исследованиях у пациентов с миастенией гравис максимальные уровни в крови достигаются через 3 часа, а проявления клинического и нейрофизиологического эффектов наблюдались через 30 мин и достигали максимума через 120-150 мин. Четкой связи между дозой и концентрацией в плазме крови/величине уровня в плазме крови или изменениями миастенических симптомов нет. Однако при уровнях более 100 нг/мл эффективность препарата не растет."}},{"type":"paragraph","data":{"text":"Объем распределения пиридостигмина бромида составляет примерно 0,5- 1,7 л/кг массы тела."}},{"type":"paragraph","data":{"text":"Пиридостигмина бромид метаболизируется в печени. Основным метаболитом является 3-гидрокси-N-метилпиридин. Выводится главным образом почками, после введения период полувыведения из плазмы составляет около 1,5 часа. После перорального применения период полувыведения увеличивается до 3-3,5 часов. Биодоступность пиридостигмина бромида после перорального приема колебалась от 8% до 20%. У больных миастенией биодоступность может снижаться ниже 4%."}},{"type":"header","data":{"text":"Фармакодинамика","level":3}},{"type":"paragraph","data":{"text":"Пиридостигмина бромид ингибирует холинэстеразу. Относится к холиномиметикам не прямого действия. Ингибирование фермента способствует накоплению ацетилхолина на рецепторах в холинергических синапсах, приводит к более выраженному и долговременному эффекту ацетилхолина. Препарат преимущественно действует на периферическую нервную систему. Он не влияет на функции центральной нервной системы, поскольку из-за низкой растворимости в липидах не проникает через гематоэнцефалический барьер."}}]},{"id":7,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"Миастения гравис (gravis)."}}]},{"id":8,"name":"Противопоказания","slug":"contraindications","body":[{"type":"list","data":{"style":"ordered","items":["Повышенная чувствительность к пиридостигмина бромиду и другим компонентам препарата;","предшествующее введение деполяризующих миорелаксантов (суксаметоний, декаметония бромид);","ирит;","хронический обструктивный бронхит, бронхиальная астма;","обтурационная (механическая) кишечная непроходимость;","обструкция желчевыводящих и мочевыводящих путей;","спастические состояния органов желудочно-кишечного тракта;","миотония;","шок в послеоперационном периоде."]}}]},{"id":10,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","body":[{"type":"paragraph","data":{"text":"Противопоказан детям до 18 лет, при беременности и лактации."}}]},{"id":11,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Миастения гравис."}},{"type":"paragraph","data":{"text":"Для симптоматического лечения миастении гравис у взрослых рекомендуется применять по 1-3 таблетки препарата Пиридостигмина бромид 3-4 раза в сутки (180-720 мг в сутки)."}},{"type":"paragraph","data":{"text":"Больные миастенией гравис требуют тщательного индивидуального подбора дозы в зависимости от течения заболевания и ответа больного на лечение. Приведенные выше дозы являются лишь рекомендациями, однако не следует превышать максимальную суточную дозу 720 мг."}},{"type":"paragraph","data":{"text":"Лечение пациентов с заболеваниями почек."}},{"type":"paragraph","data":{"text":"Пациентам с заболеваниями почек препарат следует назначать в низких дозах, потому что пиридостигмина бромид в неизмененном виде выводится из организма в основном почками (75%). При уровне креатинина 2 мг/дл следует применять половинную поддерживающую дозу или соответственно увеличить вдвое интервал между приемом доз. Поэтому необходимую дозу следует подбирать индивидуально для каждого больного, в зависимости от реакции на терапию препаратом. Рекомендовано тщательное медицинское обследование."}},{"type":"paragraph","data":{"text":"Внутрь, запивая водой."}},{"type":"paragraph","data":{"text":"Дозу и продолжительность лечения определяет врач в зависимости от течения заболевания и реакции пациента на лечение."}}]},{"id":12,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Со стороны органа зрения: частота неизвестна: миоз, слезотечение, нарушение аккомодации."}},{"type":"paragraph","data":{"text":"Со стороны сердца: частота не известна: аритмия (в том числе брадикардия, тахикардия, АВ-блокада), а также гипотония."}},{"type":"paragraph","data":{"text":"Со стороны дыхательной системы, органов грудной клетки и средостения: частота не известна: усиление секреции бронхиальных желез в сочетании с бронхоспазмом."}},{"type":"paragraph","data":{"text":"Со стороны желудочно-кишечного тракта: частота не известна: тошнота, рвота, диарея, спазматические боли в животе, желудочно-кишечная гиперкинезия, повышенное слюноотделение."}},{"type":"paragraph","data":{"text":"Со стороны кожи и подкожных тканей: частота не известна: кожная сыпь (обычно исчезает вскоре после прекращения лечения), интенсивное потоотделение."}},{"type":"paragraph","data":{"text":"Со стороны скелетно-мышечной и соединительной ткани: частота не известна: повышенная мышечная слабость, тремор и миофибрилляция или мышечная гипотония."}},{"type":"paragraph","data":{"text":"Со стороны почек и мочевыводящих путей: частота не известна: позывы к мочеиспусканию."}},{"type":"paragraph","data":{"text":"Указанные нежелательные реакции могут быть признаками передозировки или холинергического криза. Поэтому следует обязательно выяснить причину симптомов и, при необходимости, применить 1-2 мг атропина сульфат путем подкожного, внутримышечного или медленного введения для устранения холиномиметических эффектов."}},{"type":"paragraph","data":{"text":"Если любые из указанных в инструкции побочных эффектов усугубляются, или Вы заметили любые другие побочные эффекты, не указанные в инструкции, сообщите об этом врачу."}}]},{"id":14,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"Сочетание с другими ингибиторами холинэстеразы или холиномиметиками может усиливать действие пиридостигмина бромида."}},{"type":"paragraph","data":{"text":"Препарат способен усиливать холиномиметические эффекты морфия и его производных."}},{"type":"paragraph","data":{"text":"Усиливает действие деполяризующих миорелаксантов (например, сукцинилхолина)."}},{"type":"paragraph","data":{"text":"Атропин ослабляет побочные действия пиридостигмина бромида на слюнные железы, глаза, сердце, мышцы бронхов и кишечник. При этом никотинергические эффекты на скелетные мышцы остаются без изменений."}},{"type":"paragraph","data":{"text":"Метилцеллюлоза полностью тормозит всасывание пиридостигмина бромида, а активированный уголь почти полностью его адсорбирует."}},{"type":"paragraph","data":{"text":"Аминогликозиды (например, стрептомицин, неомицин, канамицин, гентамицин), полипептидные антибиотики (полимиксин, колистин), некоторые другие антибиотики, например, окситетрациклин, клиндамицин и линкомицин, многочисленные антиаритмические средства (хинидин, прокаинамид, пропранолол), пеницилламин, литий, транквилизаторы бензодиазепинового типа и фенотиазины (например, хлорпромазин) могут ослаблять эффект пиридостигмина бромида и за счет этого вызвать миастенические симптомы."}},{"type":"paragraph","data":{"text":"Высокие дозы кортикостероидов также могут ослаблять эффект пиридостигмина бромида."}},{"type":"paragraph","data":{"text":"В том случае, если Вы принимаете другие лекарства, перед приемом препарата обязательно проконсультируйтесь с врачом."}}]}],"source":{"title":"ЗдравСити","url":"https://zdravcity.ru"}},"description_toggle":false,"short_description":"Максимальные концентрации в плазме крови достигаются через 1,7-3,2 часа после приема пиридостигмина бромида. 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