таблетки белого или белого с кремоватым оттенком цвета,
плоскоцилиндрические с риской
Фармакотерапевтическая группа
анальгезирующее ненаркотическое средство
Фармакологические свойства
Фармакодинамика:
Парацетамол обладает обезболивающим и жаропонижающим действием.
Препарат блокирует циклооксигеназу в центральной нервной системе воздействуя на центры боли и терморегуляции. В воспаленных тканях клеточные пероксидазы нейтрализуют влияние парацетамола на циклооксигеназу что объясняет отсутствие значимого противовоспалительного эффекта. Препарат не оказывает отрицательного влияния на водно-солевой обмен и слизистую оболочку желудочно-кишечного тракта.
Фармакокинетика:
Абсорбция - высокая максимальная концентрация (Сmах) составляет 5-20 мкг/мл время достижения максимальной концентрации (Tmax) - 0.5-2 ч; связь с белками плазмы - 15%. Терапевтически эффективная концентрация парацетамола в плазме достигается при его назначении в дозе 10-15 мг/кг.
Проникает через гематоэнцефалический барьер. 1-2% от принятой кормящей матерью дозы препарата проникает в грудное молоко.
Метаболизируется в печени: 80% вступает в реакции конъюгации с глюкуроновой кислотой и сульфатами с образованием неактивных метаболитов 17% подвергается гидроксилированию с образованием 8 активных метаболитов которые конъюгируют с глутатионом и образуют неактивные метаболиты. При недостатке глутатиона эти метаболиты могут блокировать ферментные системы гепатоцитов и вызывать их некроз. Период полувыведения (Т1/2) - 1-4 часа. Преимущественно выводится почками в виде метаболитов - глюкуронидов и сульфатов 3% - в неизмененном виде.
У пациентов пожилого возраста отмечается снижение клиренса препарата и увеличение Т1/2.
Показания к применению
Болевой синдром слабой и умеренной интенсивности различного генеза (в т.ч. головная боль, мигрень, зубная боль, невралгия, миалгия, альгодисменорея; боль при травмах, ожогах). Лихорадка при инфекционно-воспалительных заболеваниях.
Противопоказания
- индивидуальная повышенная чувствительность к компонентам препарата;
- детский возраст до 6 лет (для данной лекарственной формы).
С осторожностью
Почечная и печеночная недостаточность вирусный гепатит алкогольное поражение печени алкоголизм доброкачественные гипербилирубинемии (синдромы Жильбера Дубина-Джонсона и Ротора) дефицит глкжозо-6-фосфатдегидрогеназы пожилой возраст беременность период лактации.
Применение при беременности и в период грудного вскармливания
Парацетамол проникает через плацентарный барьер. До настоящего времени не отмечено отрицательного воздействия парацетамола на плод у человека. Парацетамол выделяется с грудным молоком: содержание в молоке составляет 0.04-0.23% дозы, принятой матерью. При необходимости применения парацетамола при беременности и в период лактации (грудного вскармливания) следует тщательно взвесить ожидаемую пользу терапии для матери и потенциальный риск для плода или ребенка. В экспериментальных исследованиях не установлено эмбриотоксическое, тератогенное и мутагенное действие парацетамола.
Способ применения и дозы
Внутрь или ректально у взрослых и подростков с массой тела более 60 кг применяют в разовой дозе 500 мг, кратность приема - до 4 раз/сут. Максимальная продолжительность лечения - 5-7 дней. Максимальные дозы: разовая - 1 г, суточная - 4 г. Разовые дозы для приема внутрь для детей в возрасте 6-12 лет - 250-500 мг, 1-5 лет - 120-250 мг, от 3 месяцев до 1 года - 60-120 мг, до 3 месяцев - 10 мг/кг. Разовые дозы при ректальном применении у детей в возрасте 6-12 лет - 250-500 мг, 1-5 лет - 125-250 мг. Кратность применения - 4 раза/сут с интервалом не менее 4 ч. Максимальная продолжительность лечения - 3 дня. Максимальная доза: 4 разовые дозы в сутки.
Побочное действие
Со стороны пищеварительной системы: редко - диспептические явления, при длительном применении в высоких дозах - гепатотоксическое действие. Со стороны системы кроветворения: редко - тромбоцитопения, лейкопения, панцитопения, нейтропения, агранулоцитоз. Аллергические реакции: редко - кожная сыпь, зуд, крапивница.
Передозировка
Симптомы: бледность кожных покровов, анорексия, тошнота, рвота, гепатонекроз (выраженность некроза прямо зависит от степени передозировки). Лечение: промывание желудка, активированный уголь.
Взаимодействие с другими лекарственными средствами
Индукторы микросомального окисления в печени (фенитоин этанол барбитураты флумецинол рифампицин фенилбутазон трициклические антидепрессанты) увеличивают продукцию гидроксилированных активных метаболитов что обусловливает возможность развития тяжелой интоксикации при небольших передозировках.
Длительное использование барбитуратов снижает эффективность парацетамола. Одновременное применение с этанолом повышает риск возникновения острого панкреатита.
Ингибиторы микросомального окисления (в т.ч. циметидин) снижают риск гепатотоксического действия.
При приеме вместе с нестероидными противовоспалительными препаратами в том числе салицилатами нефротоксическое действие парацетамола возрастает.
Дифлунисал повышает плазменную концентрацию парацетамола на 50% что повышает риск развития гепатотоксичноcти.
Парацетамол усиливает действие антикоагулянтов непрямого действия и снижает эффективность урикозурических препаратов.
Особые указания
Следует избегать одновременного применения парацетамола с другими парацетамолсодержащими препаратами поскольку это может вызвать передозировку парацетамола.
При применении препарата более 5 дней следует контролировать показатели периферической крови и функциональное состояние печени.
Парацетамол искажает результаты лабораторных исследований содержания глюкозы и мочевой кислоты в плазме крови.
Форма выпуска
Таблетки 500 мг.
Условия хранения
Хранить при температуре не выше 25 °С.
Хранить в недоступном для детей месте.
Срок годности
4 года. Не использовать по истечении срока годности указанного на упаковке.
Условия отпуска
Без рецепта
Производитель
Фармстандарт-Лексредства ОАО, 305022, Курск, 2-ая Агрегатная, 1А/18, Россия
Организация, принимающая претензии потребителей
Фармстандарт-Лексредства ОАО
Для описания товара использована информация от партнера 36.6
Мобильное приложение «Все аптеки»
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Терапевтически эффективная концентрация парацетамола в плазме достигается при его назначении в дозе 10-15 мг/кг."}},{"type":"paragraph","data":{"text":"Проникает через гематоэнцефалический барьер. 1-2% от принятой кормящей матерью дозы препарата проникает в грудное молоко."}},{"type":"paragraph","data":{"text":"Метаболизируется в печени: 80% вступает в реакции конъюгации с глюкуроновой кислотой и сульфатами с образованием неактивных метаболитов 17% подвергается гидроксилированию с образованием 8 активных метаболитов которые конъюгируют с глутатионом и образуют неактивные метаболиты. При недостатке глутатиона эти метаболиты могут блокировать ферментные системы гепатоцитов и вызывать их некроз. Период полувыведения (Т1/2) - 1-4 часа. 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