- Инфильтрационная (в том числе внутрикостная) анестезия;
- вагосимпатическая шейная, паранефральная, циркулярная и паравертебральная блокады.
Противопоказания
- Гиперчувствительность (в том числе к парааминобензойной кислоте и другим местным анестетикам);
- детский возраст до 12 лет:
- выраженные фиброзные изменения в тканях (для анестезии методом ползучего инфильтрата).
Инструкция
Регистрационный номер
ЛП-003091
Торговое название препарата
Новокаин
Лекарственная форма
раствор для инъекций
Состав
1 мл препарата содержит:
0,25% раствор
активное вещество: прокаина гидрохлорид - 2,5 мг;
вспомогательные вещества: 0,1М раствор хлористоводородной кислоты - до pH 3,8-4,5; вода для инъекций - до 1 мл,
0,5% раствор
активное вещество: прокаина гидрохлорид - 5 мг;
вспомогательные вещества: 0,1 М раствор хлористоводородной кислоты - до pH 3,8-4,5; вода для инъекций - до 1 мл.
Описание
Прозрачная бесцветная или слегка окрашенная жидкость.
Фармакотерапевтическая группа
Местноанестезирующее средство
Фармакологические свойства
Фармакодинамика:
Местноанестезирующее средство с умеренной анестезирующей активностью и большой широтой терапевтического действия. Являясь слабым основанием, блокирует натриевые каналы, препятствует генерации импульсов в окончаниях чувствительных нервов и проведению импульсов по нервным волокнам. Изменяет потенциал действия в мембранах нервных клеток без выраженного влияния на потенциал покоя. Подавляет проведение не только болевых, но и импульсов другой модальности.
При всасывании и непосредственном сосудистом введении в ток крови снижает возбудимость периферических холинергических систем, уменьшает образование и высвобождение ацетилхолина из преганглионарных окончаний (обладает некоторым ганглиоблокирующим действием), устраняет спазм гладкой мускулатуры, уменьшает возбудимость миокарда и моторных зон коры головного мозга. Устраняет нисходящие тормозные влияния ретикулярной формации ствола мозга. Угнетает полисинаптические рефлексы. В больших дозах может вызывать судороги. Обладает короткой анестезирующей активностью (продолжительность инфильтрационной анестезии составляет 0,5-1 ч).
Фармакокинетика:
Подвергается полной системной абсорбции. Степень абсорбции зависит от места и пути введения (особенно от васкуляризации и скорости кровотока в области введения) и итоговой дозы (количества и концентрации). Быстро гидролизуется эстеразами плазмы и печени с образованием двух основных фармакологически активных метаболитов: диэтиламиноэтанола (обладает умеренным сосудорасширяющим действием) и парааминобензойной кислоты (является конкурентным антагонистом сульфаниламидных химиотерапевтических лекарственных препаратов и может ослабить их противомикробное действие).
Период полувыведения препарата - 30-50 с, в неонатальном периоде - 54-114 с. Выводится преимущественно почками в виде метаболитов, в неизмененном виде выводится не более 2%.
Показания к применению
- Инфильтрационная (в том числе внутрикостная) анестезия;
- вагосимпатическая шейная, паранефральная, циркулярная и паравертебральная блокады.
Противопоказания
- Гиперчувствительность (в том числе к парааминобензойной кислоте и другим местным анестетикам);
- детский возраст до 12 лет:
- выраженные фиброзные изменения в тканях (для анестезии методом ползучего инфильтрата).
- состояния, сопровождающиеся снижением печеночного кровотока (например, при хронической сердечной недостаточности, заболеваниях печени);
- прогрессирование сердечно-сосудистой недостаточности (обычно вследствие развития блокад сердца и шока);
- воспалительные заболевания или инфицирование места инъекции;
- дефицит псевдохолинэстеразы;
- почечная недостаточность;
- детский возраст (от 12 до 18 лег);
- пожилые пациенты (старше 65 лет);
- ослабленные больные.
Применение при беременности и в период грудного вскармливания
При беременности и в период грудного вскармливания безопасность и эффективность препарата не установлена.
Применение препарата при беременности и в период грудного вскармливания возможно только по назначению врача, если предполагаемая польза для матери превышает потенциальный риск для плода или ребенка.
Способ применения и дозы
Для инфильтрационной анестезии применяют 0,25% и 0,5% растворы; для анестезии по методу Вишневского (тугая ползучая инфильтрация) - 0,125% и 0,25% растворы. Для уменьшения всасывания и удлинения действия при местной анестезии дополнительно вводят 0,1% раствор эпинефрина - по 1 капле на 2-5-10 мл раствора прокаты.
При паранефральной блокаде (по Л. В. Вишневскому) в околопочечную клетчатку вводят 50-80 мл 0,5% раствора или 100-150 мл 0,25%, а при вагосимпатической блокаде - 30-100 мл 0,25% раствора.
Для циркуляторной или паравертебральной блокад внутрикожно вводят 0,25% или 0,5% раствор.
Высшие дозы для инфильтрационной анестезии для взрослых: первая разовая доза в начале операции - не более 500 мл 0,25% раствора и 150 мл 0,5% раствора. Максимальная доза для применения у детей старше 12 лет - 15 мг/кг.
Порядок работы с полимерной ампулой:
1. Взять ампулу и встряхнуть ее, удерживая за горлышко.
2. Сдавить ампулу рукой, при этом не должно происходить выделение препарата, и вращающими движениями повернуть и отделить клапан.
3. Через образовавшееся отверстие немедленно соединить шприц с ампулой.
4. Перевернуть ампулу и медленно набрать в шприц ее содержимое.
5. Надеть иглу на шприц.
Побочное действие
Со стороны центральной и периферической системы: головная боль, головокружение, сонливость, слабость, тризм, тремор, нистагм, стойкая анестезия, двигательное беспокойство, потеря сознания, судороги, зрительные и слуховые нарушения.
Со стороны сердечно-сосудистой системы: повышение или снижение артериального давления, коллапс, периферическая вазодилатация, брадикардия, аритмия, боль в грудной клетке, изменения распространения возбуждения в сердце, которые проявляются на ЭКГ в виде плоского зубца Т или укорочения сегмента ST.
Со стороны дыхательной системы: спазмы дыхательных путей или затруднение дыхания.
Со стороны мочевыделительной системы: непроизвольное мочеиспускание.
Со стороны пищеварительной системы: тошнота, рвота.
Со стороны крови: метгемоглобинемия.
Аллергические реакции: аллергические реакции, вплоть до анафилактического шока.
Прочие: возвращение боли, стойкая анестезия, гипотермия, дрожь, отек губ, лица, рта, языка и горла.
Передозировка
При использовании в высоких дозах возможно избыточное всасывание.
Симптомы: бледность кожных покровов и слизистых оболочек, головокружение, тошнота, рвота, "холодный" пот, учащение дыхания, тахикардия, снижение артериального давления вплоть до коллапса, апноэ, метгемоглобинемия. Действие на центральную нервную систему проявляется чувством страха, галлюцинациями, судорогами, двигательным возбуждением.
Взаимодействие с другими лекарственными средствами
Усиливает угнетающее действие на центральную нервную систему средств для общей анестезии, снотворных и седативных препаратов, наркотических анальгетиков и транквилизаторов.
При обработке места инъекции местного анестетика дезинфицирующими растворами, содержащими тяжелые металлы, повышается риск развития местной реакции в виде болезненности и отека.
Одновременное применение с ингибиторами моноаминоксидазы (фуразолидон, прокарбазин, селегилин) повышает риск развития гипотонии.
Усиливают и удлиняют действие миорелаксантов.
При применении прокаина совместно с наркотическими анальгетиками отмечается аддитивный эффект, что используется при проведении спинальной и эпидуральной анестезии, при этом усиливается угнетение дыхания.
Прокаин снижает антимиастеническое действие лекарственных средств, особенно при применении его в высоких дозах, что требует дополнительной коррекции лечения миастении.
Метаболит прокаина (пара-аминобензойная кислота) является антагонистом сульфаниламидов.
При применении местноанестезирующих средств для эпидуральной анестезии с гуанадрелом, с гуанетидином, мекамиламином, триметафана камзилатом повышается риск развития резкого снижения артериального давления и брадикардии.
Особые указания
Анестезия должна проводиться опытными специалистами в соответствующим образом оборудованном помещении при доступности готовых к немедленному использованию оборудования и препаратов, необходимых для проведения кардиомониторинга и реанимационных мероприятий. Для предотвращения случайного внутрисосудистого введения, рекомендуется проводить аспирационную пробу (в два этапа).
Пациентам требуется контроль за функциями сердечно-сосудистой, дыхательной и центральной нервной систем. Применение ингибиторов моноаминоксидазы по меньшей мере за 10 дней до введения местного анестетика противопоказано. Перед применением обязательное проведение проб на индивидуальную чувствительность к препарату. Необходимо учитывать, что при проведении местной анестезии при применении одной и той же общей дозы, токсичность прокаина тем выше, чем более концентрированный раствор применяется.
Препарат следует хранить во вторичной упаковке.
Влияние на способность управлять автомобилем и движущимися механизмами
В период лечения необходимо воздерживаться от вождения автотранспорта и занятий потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций.
Форма выпуска
Раствор для инъекций, 0,25% и 0,5%.
Условия хранения
Хранить при температуре не выше 25 °С.
Хранить в недоступном для детей месте.
Срок годности
2 года.
Не применять после окончания срока годности
Условия отпуска
По рецепту
Производитель
Общество с ограниченной ответственностью "Гротекс" (ООО "Гротекс"), 195279, г. Санкт-Петербург, Индустриальный проспект, д. 71, корп. 2, лит. А, Россия
Организация, принимающая претензии потребителей
ООО "Гротекс"
Для описания товара использована информация от партнера 36.6
Мобильное приложение «Все аптеки»
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мг;"}},{"type":"paragraph","data":{"text":"\u003ci\u003eвспомогательные вещества\u003c/i\u003e: 0,1 М раствор хлористоводородной кислоты - до pH 3,8-4,5; вода для инъекций - до 1 мл."}}]},{"id":5,"name":"Описание","slug":"common_description","body":[{"type":"paragraph","data":{"text":"Прозрачная бесцветная или слегка окрашенная жидкость."}}]},{"id":6,"name":"Фармакотерапевтическая группа","slug":"","body":[{"type":"paragraph","data":{"text":"Местноанестезирующее средство"}}]},{"id":7,"name":"Фармакологические свойства","slug":"pharmacologic_effects","body":[{"type":"header","data":{"text":"Фармакодинамика:","level":3}},{"type":"paragraph","data":{"text":"Местноанестезирующее средство с умеренной анестезирующей активностью и большой широтой терапевтического действия. Являясь слабым основанием, блокирует натриевые каналы, препятствует генерации импульсов в окончаниях чувствительных нервов и проведению импульсов по нервным волокнам. Изменяет потенциал действия в мембранах нервных клеток без выраженного влияния на потенциал покоя. Подавляет проведение не только болевых, но и импульсов другой модальности."}},{"type":"paragraph","data":{"text":"При всасывании и непосредственном сосудистом введении в ток крови снижает возбудимость периферических холинергических систем, уменьшает образование и высвобождение ацетилхолина из преганглионарных окончаний (обладает некоторым ганглиоблокирующим действием), устраняет спазм гладкой мускулатуры, уменьшает возбудимость миокарда и моторных зон коры головного мозга. Устраняет нисходящие тормозные влияния ретикулярной формации ствола мозга. Угнетает полисинаптические рефлексы. В больших дозах может вызывать судороги. Обладает короткой анестезирующей активностью (продолжительность инфильтрационной анестезии составляет 0,5-1 ч)."}},{"type":"header","data":{"text":"Фармакокинетика:","level":3}},{"type":"paragraph","data":{"text":"Подвергается полной системной абсорбции. Степень абсорбции зависит от места и пути введения (особенно от васкуляризации и скорости кровотока в области введения) и итоговой дозы (количества и концентрации). Быстро гидролизуется эстеразами плазмы и печени с образованием двух основных фармакологически активных метаболитов: диэтиламиноэтанола (обладает умеренным сосудорасширяющим действием) и парааминобензойной кислоты (является конкурентным антагонистом сульфаниламидных химиотерапевтических лекарственных препаратов и может ослабить их противомикробное действие)."}},{"type":"paragraph","data":{"text":"Период полувыведения препарата - 30-50 с, в неонатальном периоде - 54-114 с. Выводится преимущественно почками в виде метаболитов, в неизмененном виде выводится не более 2%."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"- Инфильтрационная (в том числе внутрикостная) анестезия;"}},{"type":"paragraph","data":{"text":"- вагосимпатическая шейная, паранефральная, циркулярная и паравертебральная блокады."}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"paragraph","data":{"text":"- Гиперчувствительность (в том числе к парааминобензойной кислоте и другим местным анестетикам);"}},{"type":"paragraph","data":{"text":"- детский возраст до 12 лет:"}},{"type":"paragraph","data":{"text":"- выраженные фиброзные изменения в тканях (для анестезии методом ползучего инфильтрата)."}}]},{"id":10,"name":"С осторожностью","slug":"cautions","body":[{"type":"paragraph","data":{"text":"- Экстренные операции, сопровождающиеся острой кровопотерей;"}},{"type":"paragraph","data":{"text":"- состояния, сопровождающиеся снижением печеночного кровотока (например, при хронической сердечной недостаточности, заболеваниях печени);"}},{"type":"paragraph","data":{"text":"- прогрессирование сердечно-сосудистой недостаточности (обычно вследствие развития блокад сердца и шока);"}},{"type":"paragraph","data":{"text":"- воспалительные заболевания или инфицирование места инъекции;"}},{"type":"paragraph","data":{"text":"- дефицит псевдохолинэстеразы;"}},{"type":"paragraph","data":{"text":"- почечная недостаточность;"}},{"type":"paragraph","data":{"text":"- детский возраст (от 12 до 18 лег);"}},{"type":"paragraph","data":{"text":"- пожилые пациенты (старше 65 лет);"}},{"type":"paragraph","data":{"text":"- ослабленные больные."}}]},{"id":11,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","body":[{"type":"paragraph","data":{"text":"При беременности и в период грудного вскармливания безопасность и эффективность препарата не установлена."}},{"type":"paragraph","data":{"text":"Применение препарата при беременности и в период грудного вскармливания возможно только по назначению врача, если предполагаемая польза для матери превышает потенциальный риск для плода или ребенка."}}]},{"id":12,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"\u003ci\u003eДля инфильтрационной анестезии\u003c/i\u003e применяют 0,25% и 0,5% растворы; \u003ci\u003eдля анестезии по методу Вишневского\u003c/i\u003e (тугая ползучая инфильтрация) - 0,125% и 0,25% растворы. Для уменьшения всасывания и удлинения действия при местной анестезии дополнительно вводят 0,1% раствор эпинефрина - по 1 капле на 2-5-10 мл раствора прокаты."}},{"type":"paragraph","data":{"text":"\u003ci\u003eПри паранефральной блокаде \u003c/i\u003e(по Л. В. Вишневскому) в околопочечную клетчатку вводят 50-80 мл 0,5% раствора или 100-150 мл 0,25%, а при вагосимпатической блокаде - 30-100 мл 0,25% раствора."}},{"type":"paragraph","data":{"text":"\u003ci\u003eДля циркуляторной или паравертебральной блокад\u003c/i\u003e внутрикожно вводят 0,25% или 0,5% раствор."}},{"type":"paragraph","data":{"text":"\u003ci\u003eВысшие дозы для инфильтрационной анестезии для взрослых\u003c/i\u003e: первая разовая доза в начале операции - не более 500 мл 0,25% раствора и 150 мл 0,5% раствора. Максимальная доза для применения у детей старше 12 лет - 15 мг/кг."}},{"type":"paragraph","data":{"text":"\u003ci\u003eПорядок работы с полимерной ампулой:\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"1. Взять ампулу и встряхнуть ее, удерживая за горлышко."}},{"type":"paragraph","data":{"text":"2. Сдавить ампулу рукой, при этом не должно происходить выделение препарата, и вращающими движениями повернуть и отделить клапан."}},{"type":"paragraph","data":{"text":"3. Через образовавшееся отверстие немедленно соединить шприц с ампулой."}},{"type":"paragraph","data":{"text":"4. Перевернуть ампулу и медленно набрать в шприц ее содержимое."}},{"type":"paragraph","data":{"text":"5. Надеть иглу на шприц."}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны центральной и периферической системы\u003c/i\u003e: головная боль, головокружение, сонливость, слабость, тризм, тремор, нистагм, стойкая анестезия, двигательное беспокойство, потеря сознания, судороги, зрительные и слуховые нарушения."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны сердечно-сосудистой системы\u003c/i\u003e: повышение или снижение артериального давления, коллапс, периферическая вазодилатация, брадикардия, аритмия, боль в грудной клетке, изменения распространения возбуждения в сердце, которые проявляются на ЭКГ в виде плоского зубца Т или укорочения сегмента ST."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны дыхательной системы\u003c/i\u003e: спазмы дыхательных путей или затруднение дыхания."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны мочевыделительной системы\u003c/i\u003e: непроизвольное мочеиспускание."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны пищеварительной системы\u003c/i\u003e: тошнота, рвота."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны крови\u003c/i\u003e: метгемоглобинемия."}},{"type":"paragraph","data":{"text":"\u003ci\u003eАллергические реакции\u003c/i\u003e: аллергические реакции, вплоть до анафилактического шока."}},{"type":"paragraph","data":{"text":"\u003ci\u003eПрочие:\u003c/i\u003e возвращение боли, стойкая анестезия, гипотермия, дрожь, отек губ, лица, рта, языка и горла."}}]},{"id":14,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"При использовании в высоких дозах возможно избыточное всасывание."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСимптомы:\u003c/i\u003e бледность кожных покровов и слизистых оболочек, головокружение, тошнота, рвота, \"холодный\" пот, учащение дыхания, тахикардия, снижение артериального давления вплоть до коллапса, апноэ, метгемоглобинемия. Действие на центральную нервную систему проявляется чувством страха, галлюцинациями, судорогами, двигательным возбуждением."}},{"type":"paragraph","data":{"text":"\u003ci\u003eЛечение: \u003c/i\u003eподдержание адекватной легочной вентиляции, дезинтоксикационная симптоматическая терапия."}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"Усиливает угнетающее действие на центральную нервную систему средств для общей анестезии, снотворных и седативных препаратов, наркотических анальгетиков и транквилизаторов."}},{"type":"paragraph","data":{"text":"Антикоагулянты (ардепарин натрия, далтепарин натрия, данапароид натрия, эноксапарин натрия, гепарин, варфарин) повышают риск развития кровотечений."}},{"type":"paragraph","data":{"text":"При обработке места инъекции местного анестетика дезинфицирующими растворами, содержащими тяжелые металлы, повышается риск развития местной реакции в виде болезненности и отека."}},{"type":"paragraph","data":{"text":"Одновременное применение с ингибиторами моноаминоксидазы (фуразолидон, прокарбазин, селегилин) повышает риск развития гипотонии."}},{"type":"paragraph","data":{"text":"Усиливают и удлиняют действие миорелаксантов."}},{"type":"paragraph","data":{"text":"При применении прокаина совместно с наркотическими анальгетиками отмечается аддитивный эффект, что используется при проведении спинальной и эпидуральной анестезии, при этом усиливается угнетение дыхания."}},{"type":"paragraph","data":{"text":"Вазоконстрикторы (эпинефрин, метоксамин, фенилэфрин) удлиняют местно-анестезирующее действие."}},{"type":"paragraph","data":{"text":"Прокаин снижает антимиастеническое действие лекарственных средств, особенно при применении его в высоких дозах, что требует дополнительной коррекции лечения миастении."}},{"type":"paragraph","data":{"text":"Ингибиторы холинэстеразы (антимиастенические лекарственные средства, циклофосфамид, демекария бромид, экотиопата йодид, тиотепа) снижают метаболизм прокаина."}},{"type":"paragraph","data":{"text":"Метаболит прокаина (пара-аминобензойная кислота) является антагонистом сульфаниламидов."}},{"type":"paragraph","data":{"text":"При применении местноанестезирующих средств для эпидуральной анестезии с гуанадрелом, с гуанетидином, мекамиламином, триметафана камзилатом повышается риск развития резкого снижения артериального давления и брадикардии."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"Анестезия должна проводиться опытными специалистами в соответствующим образом оборудованном помещении при доступности готовых к немедленному использованию оборудования и препаратов, необходимых для проведения кардиомониторинга и реанимационных мероприятий. Для предотвращения случайного внутрисосудистого введения, рекомендуется проводить аспирационную пробу (в два этапа)."}},{"type":"paragraph","data":{"text":"Пациентам требуется контроль за функциями сердечно-сосудистой, дыхательной и центральной нервной систем. Применение ингибиторов моноаминоксидазы по меньшей мере за 10 дней до введения местного анестетика противопоказано. Перед применением обязательное проведение проб на индивидуальную чувствительность к препарату. Необходимо учитывать, что при проведении местной анестезии при применении одной и той же общей дозы, токсичность прокаина тем выше, чем более концентрированный раствор применяется."}},{"type":"paragraph","data":{"text":"Препарат следует хранить во вторичной упаковке."}}]},{"id":17,"name":"Влияние на способность управлять автомобилем и движущимися механизмами","slug":"","body":[{"type":"paragraph","data":{"text":"В период лечения необходимо воздерживаться от вождения автотранспорта и занятий потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций."}}]},{"id":18,"name":"Форма выпуска","slug":"","body":[{"type":"paragraph","data":{"text":"Раствор для инъекций, 0,25% и 0,5%."}}]},{"id":19,"name":"Условия хранения","slug":"storage","body":[{"type":"paragraph","data":{"text":"Хранить при температуре не выше 25 °С."}},{"type":"paragraph","data":{"text":"Хранить в недоступном для детей месте."}}]},{"id":20,"name":"Срок годности","slug":"expiry_date","body":[{"type":"paragraph","data":{"text":"2 года."}},{"type":"paragraph","data":{"text":"Не применять после окончания срока годности"}}]},{"id":21,"name":"Условия отпуска","slug":"release_condition","body":[{"type":"paragraph","data":{"text":"По рецепту"}}]},{"id":22,"name":"Производитель","slug":"","body":[{"type":"paragraph","data":{"text":"Общество с ограниченной ответственностью \"Гротекс\" (ООО \"Гротекс\"), 195279, г. Санкт-Петербург, Индустриальный проспект, д. 71, корп. 2, лит. А, Россия"}}]},{"id":23,"name":"Организация, принимающая претензии потребителей","body":[{"type":"paragraph","data":{"text":"ООО \"Гротекс\""}}]}],"source":null},"description_toggle":false,"short_description":"Местноанестезирующее средство с умеренной анестезирующей активностью и большой широтой терапевтического действия. Являясь слабым основанием, блокирует натриевые каналы, препятствует генерации импульсов в окончаниях чувствительных нервов и проведению импульсов по нервным волокнам. Изменяет потенциал действия в мембранах нервных клеток без выраженного влияния на потенциал покоя. Подавляет проведение не только болевых, но и импульсов другой модальности. При всасывании и непосредственном сосудистом введении в ток крови снижает возбудимость периферических холинергических систем, уменьшает образование и высвобождение ацетилхолина из преганглионарных окончаний (обладает некоторым ганглиоблокирующим действием), устраняет спазм гладкой мускулатуры, уменьшает возбудимость миокарда и моторных зон коры головного мозга. Устраняет нисходящие тормозные влияния ретикулярной формации ствола мозга. Угнетает полисинаптические рефлексы. В больших дозах может вызывать судороги. Обладает короткой анестезирующей активностью (продолжительность инфильтрационной анестезии составляет 0,5-1 ч). Подвергается полной системной абсорбции. Степень абсорбции зависит от места и пути введения (особенно от васкуляризации и скорости кровотока в области введения) и итоговой дозы (количества и концентрации). Быстро гидролизуется эстеразами плазмы и печени с образованием двух основных фармакологически активных метаболитов: диэтиламиноэтанола (обладает умеренным сосудорасширяющим действием) и парааминобензойной кислоты (является конкурентным антагонистом сульфаниламидных химиотерапевтических лекарственных препаратов и может ослабить их противомикробное действие). Период полувыведения препарата - 30-50 с, в неонатальном периоде - 54-114 с. 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