Комбинированное лекарственное средство. Сочетание трех компонентов препарата приводит к взаимному усилению их фармакологического действия.
Парацетамол и пропифеназон обладают обезболивающим и жаропонижающим действием. Парацетамол - ненаркотический анальгетик. Блокирует ЦОГ только в ЦНС, воздействуя на центры боли и терморегуляции (в воспаленных тканях клеточные пероксидазы нейтрализуют влияние парацетамола на ЦОГ), что объясняет практически полное отсутствие противовоспалительного эффекта. Отсутствие влияния на синтез простагландинов (ПГ) в периферических тканях обусловливает отсутствие у него отрицательного влияния на водно-солевой обмен (задержка натрия и воды) и слизистую ЖКТ.
Пропифеназон является производным пиразолона. Механизм действия осуществляется путем ингибирования ЦОГ, участвующей в образовании простагландинов из арахидоновой кислоты.
Кофеин повышает рефлекторную возбудимость спинного мозга, возбуждает дыхательный и сосудодвигательный центры, расширяет кровеносные сосуды скелетных мышц, головного мозга, сердца, почек, снижает агрегацию тромбоцитов; уменьшает сонливость, чувство усталости. В данной комбинации кофеин в малой дозе практически не оказывает стимулирующего действия на ЦНС, однако способствует регуляции тонуса сосудов мозга, уменьшает сонливость, усиливает болеутоляющее действие других компонентов препарата.
Фармакокинетика
Парацетамол
Абсорбция - высокая, связь с белками плазмы - 15%, TCmax - 20-30 мин. Проникает через ГЭБ. Менее 1% от принятой кормящей матерью дозы проникает в грудное молоко. Терапевтическая эффективная концентрация парацетамола в плазме достигается при его назначении в дозе 10-15 мг/кг.
Метаболизируется в печени: 80% вступает в реакцию конъюгации с глюкуроновой и серной кислотами с образованием неактивных метаболитов: 17% подвергается гидроксилированию с образованием неактивных метаболитов, которые коныогируют с глутатионом и образуют неактивные метаболиты. При недостатке глутадиона эти метаболиты могут блокировать ферментные системы гепатоцитов и вызывать их некроз. T1/2 - 2-3 ч. У пожилых пациентов снижается клиренс парацетамола и увеличивается период полувыведения. Выводится почками в неизмененном виде 3%.
Пропифеназон
Cmax пропифеназона в плазме достигается через 30 мин. Метаболизируется в печени. T1/2 составляет 1-1,5 ч. Сочетание с парацетамолом увеличивает время его выведения на 40%, что играет значительную роль, т.к позволяет сократить число приемов препарата в течение суток. Выводится почками.
Кофеин
Время достижения Cmax - 1 ч; T1/2 - 3.5 ч; 65- 80% кофеина выводится почками главным образом в виде 1-метилксатина, 1-метилмочевой кислоты и ацетилированных производных урацила, небольшое количество превращается в теофиллин и теобромин.
Показания к применению
Купирование болевого синдрома слабой и средней интенсивности различного генеза: головная боль; мигрень; зубная боль; артралгии; миалгии; альгодисменорея.
В качестве жаропонижающего средства при лихорадочных состояниях на фоне инфекционно-воспалительных заболеваний (ОРВИ, в том числе грипп и т.п.).
Противопоказания
Повышенная чувствительность к компонентам препарата; тяжелая почечная и/или печеночная недостаточность; дефицит фермента глюкозо-6-фосфатдегидрогеназы; угнетение костномозгового кроветворения (лейкопения, анемия, в т.ч. гемолитическая); острая гематопорфирия; полное или неполное сочетание бронхиальной астмы, рецидивирующего полипоза носа и околоносовых пазух и непереносимости НПВС (в том числе в анамнезе); состояния, сопровождающиеся угнетением дыхания; внутричерепная гипертензия; острый инфаркт миокарда; ИБС; аритмии; артериальная гипертензия; язвенная болезнь желудка и двенадцатиперстной кишки; глаукома; бессонница; беременность; период лактации; детский возраст до 12 лет.
С осторожностью
С осторожностью: доброкачественные гипербилирубинемии (в т.ч. синдром Жильбера, Дубина-Джонсона, Ротора), пожилой возраст, алкоголизм, эпилепсия и склонность к судорожным припадкам.
Применение при беременности и в период грудного вскармливания
Противопоказан при беременности и в период лактации (грудного вскармливания).
Побочное действие
Со стороны нервной системы: головокружение, бессонница.
Со стороны ЖКТ: тошнота, рвота, тяжесть и неприятные ощущения в области желудка;
Со стороны системы кроветворения: тромбоцнтопения, агранулоцитоз, гемолитическая анемия.
Аллергические реакции: кожная сыпь, зуд, крапивница, отек Квинке, мультиформная эксудативная эритема (в т.ч. синдром Стивенса-Джонсона), токсический эпндермальный некролиз (синдром Лайела).
Взаимодействие с другими лекарственными средствами
Эффективность данной комбинации может снизиться при одновременном применении с колестирамином, холинолитиками, антидепрессантами, щелочными веществами.
При одновременном применении с барбитуратами, противосудорожными препаратами, этанолом значительно повышается гепатотоксичное действие.
Метоклопрамид ускоряет всасывание парацетамола.
Под воздействием парацетамола период полувыведения хлорафеникола увеличивается в 5 раз.
Одновременное применение парацетамола в высоких дозах повышает эффект антикоагулянтов.
Миелотоксичные средства усиливают проявления гематотоксичности парацетамола.
Кофеин ускоряет всасывание эрготамина; снижает всасывание препаратов кальция; снижает эффект наркотических и снотворных средств, увеличивает выведение препаратов лития; ускоряет всасывание и усиливает действие сердечных гликозидов, повышает их токсичность.
Одновременное применение кофеина с бета-адреноблокаторами может приводить к взаимному подавлению терапевтических эффектов, с бета-адреномиметиками к дополнительной стимуляции ЦНС и другим токсическим эффектам.
Кофеин может снижать клиренс теофиллина, и возможно других ксантинов, увеличивая возможность аддитивных фармакодинамических и других токсических эффектов.
Ингибиторы МАО, фуразолидон, прокарбазин, селегилин и большие дозы кофеина могут вызывать развитие опасных аритмий сердца или выраженное повышение артериального давления.
Никотин увеличивает скорость выведения кофеина.
Кофеин является антагонистом аденозина.
Пропифеназон может усиливать действие пероральных гиполипидемических средств, сульфаниламидных препаратов., антикоагулянтов, ульцерогенный эффект глюкокортикостероидов, снижает эффективность калийсберегающих диуретиков.
Особые указания
При длительном применении (более 5 дней) необходим контроль картины периферической крови и функционального состояния печени.
Во время лечения следует отказаться от употребления алкогольсодержаших напитков (повышение риска желудочно-кишечного кровотечения).
Чрезмерное употребление кофеинсодержащих продуктов (кофе, чай) на фоне лечения может вызвать симптомы передозировки.
Прием препарата может затруднить установление диагноза при остром абдоминальном болевом синдроме.
Влияние на способность к управлению транспортными средствами и механизмами
В период приема следует соблюдать осторожность при управлении транспортными средствами и занятии другими видами деятельности, требующей повышенной концентрации внимания и быстроты психомоторных реакций.
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мг"}},{"type":"paragraph","data":{"text":"парацетамол\t250 мг"}},{"type":"paragraph","data":{"text":"пропифеназон\t210 мг"}},{"type":"paragraph","data":{"text":"\u003ci\u003eВспомогательные вещества\u003c/i\u003e: целлюлоза микрокристаллическая, крахмал картофельный, кросповидон (коллидон CL или полипласдон XL), гипромеллоза (гидроксипропилметилцеллюлоза), натрия кроскармеллоза (примеллоза), натрия додецилсульфат, коповидон (коллидон VA64 или пласдон S-630), магния стеарат. "}}]},{"id":6,"name":"Фармакотерапевтическая группа","slug":"","body":[{"type":"paragraph","data":{"text":"Анальгетик-антипиретик"}}]},{"id":7,"name":"Фармакологические свойства","slug":"pharmacologic_effects","body":[{"type":"paragraph","data":{"text":"Комбинированное лекарственное средство. Сочетание трех компонентов препарата приводит к взаимному усилению их фармакологического действия."}},{"type":"paragraph","data":{"text":"\u003ci\u003eПарацетамол и пропифеназон\u003c/i\u003e обладают обезболивающим и жаропонижающим действием. Парацетамол - ненаркотический анальгетик. Блокирует ЦОГ только в ЦНС, воздействуя на центры боли и терморегуляции (в воспаленных тканях клеточные пероксидазы нейтрализуют влияние парацетамола на ЦОГ), что объясняет практически полное отсутствие противовоспалительного эффекта. Отсутствие влияния на синтез простагландинов (ПГ) в периферических тканях обусловливает отсутствие у него отрицательного влияния на водно-солевой обмен (задержка натрия и воды) и слизистую ЖКТ."}},{"type":"paragraph","data":{"text":"\u003ci\u003eПропифеназон\u003c/i\u003e является производным пиразолона. Механизм действия осуществляется путем ингибирования ЦОГ, участвующей в образовании простагландинов из арахидоновой кислоты."}},{"type":"paragraph","data":{"text":"\u003ci\u003eКофеин\u003c/i\u003e повышает рефлекторную возбудимость спинного мозга, возбуждает дыхательный и сосудодвигательный центры, расширяет кровеносные сосуды скелетных мышц, головного мозга, сердца, почек, снижает агрегацию тромбоцитов; уменьшает сонливость, чувство усталости. В данной комбинации кофеин в малой дозе практически не оказывает стимулирующего действия на ЦНС, однако способствует регуляции тонуса сосудов мозга, уменьшает сонливость, усиливает болеутоляющее действие других компонентов препарата."}},{"type":"header","data":{"text":"Фармакокинетика","level":4}},{"type":"paragraph","data":{"text":"\u003ci\u003eПарацетамол\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Абсорбция - высокая, связь с белками плазмы - 15%, TC\u003csub\u003emax\u003c/sub\u003e - 20-30 мин. Проникает через ГЭБ. Менее 1% от принятой кормящей матерью дозы проникает в грудное молоко. Терапевтическая эффективная концентрация парацетамола в плазме достигается при его назначении в дозе 10-15 мг/кг."}},{"type":"paragraph","data":{"text":"Метаболизируется в печени: 80% вступает в реакцию конъюгации с глюкуроновой и серной кислотами с образованием неактивных метаболитов: 17% подвергается гидроксилированию с образованием неактивных метаболитов, которые коныогируют с глутатионом и образуют неактивные метаболиты. При недостатке глутадиона эти метаболиты могут блокировать ферментные системы гепатоцитов и вызывать их некроз. T\u003csub\u003e1/2\u003c/sub\u003e - 2-3 ч. У пожилых пациентов снижается клиренс парацетамола и увеличивается период полувыведения. Выводится почками в неизмененном виде 3%."}},{"type":"paragraph","data":{"text":"\u003ci\u003eПропифеназон\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"C\u003csub\u003emax\u003c/sub\u003e пропифеназона в плазме достигается через 30 мин. Метаболизируется в печени. T\u003csub\u003e1/2 \u003c/sub\u003eсоставляет 1-1,5 ч. Сочетание с парацетамолом увеличивает время его выведения на 40%, что играет значительную роль, т.к позволяет сократить число приемов препарата в течение суток. Выводится почками."}},{"type":"paragraph","data":{"text":"\u003ci\u003eКофеин\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Время достижения C\u003csub\u003emax\u003c/sub\u003e - 1 ч; T\u003csub\u003e1/2 \u003c/sub\u003e- 3.5 ч; 65- 80% кофеина выводится почками главным образом в виде 1-метилксатина, 1-метилмочевой кислоты и ацетилированных производных урацила, небольшое количество превращается в теофиллин и теобромин."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"Купирование болевого синдрома слабой и средней интенсивности различного генеза: головная боль; мигрень; зубная боль; артралгии; миалгии; альгодисменорея."}},{"type":"paragraph","data":{"text":"В качестве жаропонижающего средства при лихорадочных состояниях на фоне инфекционно-воспалительных заболеваний (ОРВИ, в том числе грипп и т.п.)."}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"paragraph","data":{"text":"Повышенная чувствительность к компонентам препарата; тяжелая почечная и/или печеночная недостаточность; дефицит фермента глюкозо-6-фосфатдегидрогеназы; угнетение костномозгового кроветворения (лейкопения, анемия, в т.ч. гемолитическая); острая гематопорфирия; полное или неполное сочетание бронхиальной астмы, рецидивирующего полипоза носа и околоносовых пазух и непереносимости НПВС (в том числе в анамнезе); состояния, сопровождающиеся угнетением дыхания; внутричерепная гипертензия; острый инфаркт миокарда; ИБС; аритмии; артериальная гипертензия; язвенная болезнь желудка и двенадцатиперстной кишки; глаукома; бессонница; беременность; период лактации; детский возраст до 12 лет."}}]},{"id":10,"name":"С осторожностью","slug":"cautions","body":[{"type":"paragraph","data":{"text":"\u003ci\u003eС осторожностью:\u003c/i\u003e доброкачественные гипербилирубинемии (в т.ч. синдром Жильбера, Дубина-Джонсона, Ротора), пожилой возраст, алкоголизм, эпилепсия и склонность к судорожным припадкам. "}}]},{"id":11,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","body":[{"type":"paragraph","data":{"text":"\u003ci\u003eПротивопоказан\u003c/i\u003e при беременности и в период лактации (грудного вскармливания). "}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны нервной системы:\u003c/i\u003e головокружение, бессонница."}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны ЖКТ:\u003c/i\u003e тошнота, рвота, тяжесть и неприятные ощущения в области желудка;"}},{"type":"paragraph","data":{"text":"\u003ci\u003eСо стороны системы кроветворения:\u003c/i\u003e тромбоцнтопения, агранулоцитоз, гемолитическая анемия."}},{"type":"paragraph","data":{"text":"\u003ci\u003eАллергические реакции:\u003c/i\u003e кожная сыпь, зуд, крапивница, отек Квинке, мультиформная эксудативная эритема (в т.ч. синдром Стивенса-Джонсона), токсический эпндермальный некролиз (синдром Лайела)."}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"Эффективность данной комбинации может снизиться при одновременном применении с колестирамином, холинолитиками, антидепрессантами, щелочными веществами."}},{"type":"paragraph","data":{"text":"При одновременном применении с барбитуратами, противосудорожными препаратами, этанолом значительно повышается гепатотоксичное действие."}},{"type":"paragraph","data":{"text":"\u003ci\u003eМетоклопрамид\u003c/i\u003e ускоряет всасывание парацетамола."}},{"type":"paragraph","data":{"text":"Под воздействием парацетамола период полувыведения \u003ci\u003eхлорафеникола\u003c/i\u003e увеличивается в 5 раз."}},{"type":"paragraph","data":{"text":"Одновременное применение парацетамола в высоких дозах повышает эффект антикоагулянтов."}},{"type":"paragraph","data":{"text":"\u003ci\u003eМиелотоксичные средства усиливают\u003c/i\u003e проявления гематотоксичности парацетамола."}},{"type":"paragraph","data":{"text":"Кофеин ускоряет всасывание \u003ci\u003eэрготамина\u003c/i\u003e; снижает всасывание \u003ci\u003eпрепаратов кальция\u003c/i\u003e; снижает эффект\u003ci\u003e наркотических и снотворных средств\u003c/i\u003e, увеличивает выведение \u003ci\u003eпрепаратов лития\u003c/i\u003e; ускоряет всасывание и усиливает действие \u003ci\u003eсердечных гликозидов\u003c/i\u003e, повышает их токсичность."}},{"type":"paragraph","data":{"text":"Одновременное применение кофеина с \u003ci\u003eбета-адреноблокаторами\u003c/i\u003e может приводить к взаимному подавлению терапевтических эффектов, с \u003ci\u003eбета-адреномиметиками\u003c/i\u003e к дополнительной стимуляции ЦНС и другим токсическим эффектам."}},{"type":"paragraph","data":{"text":"Кофеин может снижать клиренс \u003ci\u003eтеофиллина\u003c/i\u003e, и возможно других \u003ci\u003eксантинов\u003c/i\u003e, увеличивая возможность аддитивных фармакодинамических и других токсических эффектов."}},{"type":"paragraph","data":{"text":"\u003ci\u003eИнгибиторы МАО, фуразолидон, прокарбазин, селегилин и большие дозы кофеина\u003c/i\u003e могут вызывать развитие опасных аритмий сердца или выраженное повышение артериального давления."}},{"type":"paragraph","data":{"text":"\u003ci\u003eНикотин\u003c/i\u003e увеличивает скорость выведения кофеина."}},{"type":"paragraph","data":{"text":"Кофеин является антагонистом \u003ci\u003eаденозина\u003c/i\u003e."}},{"type":"paragraph","data":{"text":"Пропифеназон может усиливать действие\u003ci\u003e пероральных гиполипидемических средств, сульфаниламидных препаратов., антикоагулянтов, ульцерогенный эффект глюкокортикостероидов\u003c/i\u003e, снижает эффективность \u003ci\u003eкалийсберегающих диуретиков\u003c/i\u003e."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"При длительном применении (более 5 дней) необходим контроль картины периферической крови и функционального состояния печени."}},{"type":"paragraph","data":{"text":"Во время лечения следует отказаться от употребления алкогольсодержаших напитков (повышение риска желудочно-кишечного кровотечения)."}},{"type":"paragraph","data":{"text":"Чрезмерное употребление кофеинсодержащих продуктов (кофе, чай) на фоне лечения может вызвать симптомы передозировки."}},{"type":"paragraph","data":{"text":"Прием препарата может затруднить установление диагноза при остром абдоминальном болевом синдроме."}},{"type":"paragraph","data":{"text":"\u003ci\u003eВлияние на способность к управлению транспортными средствами и механизмами\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"В период приема следует соблюдать осторожность при управлении транспортными средствами и занятии другими видами деятельности, требующей повышенной концентрации внимания и быстроты психомоторных реакций."}}]}],"source":null},"description_toggle":false,"short_description":"Комбинированное лекарственное средство. 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Механизм действия осуществляется путем ингибирования ЦОГ, участвующей в образовании простагландинов из арахидоновой кислоты.Кофеинповышает рефлекторную возбудимость спинного мозга, возбуждает дыхательный и сосудодвигательный центры, расширяет кровеносные сосуды скелетных мышц, головного мозга, сердца, почек, снижает агрегацию тромбоцитов; уменьшает сонливость, чувство усталости. В данной комбинации кофеин в малой дозе практически не оказывает стимулирующего действия на ЦНС, однако способствует регуляции тонуса сосудов мозга, уменьшает сонливость, усиливает болеутоляющее действие других компонентов препарата.ПарацетамолАбсорбция - высокая, связь с белками плазмы - 15%, TCmax- 20-30 мин. Проникает через ГЭБ. Менее 1% от принятой кормящей матерью дозы проникает в грудное молоко. Терапевтическая эффективная концентрация парацетамола в плазме достигается при его назначении в дозе 10-15 мг/кг. 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