Симптоматическое лечение заболеваний опорно-двигательного аппарата (ревматоидный артрит псориатический артрит анкилозирующий спондилоартрит; подагрический артрит ревматическое поражение мягких тканей остеоартроз периферических суставов и позвоночника в том числе с радикулярным синдромом тендовагинит бурсит).
основа для суппозиториев: твердый жир, тип А - достаточное количество до получения суппозитория массой 1,25 г или 2,0 г.
Фармакологические свойства
Нестероидный противовоспалительный препарат производное фенилуксусной кислоты; оказывает противовоспалительное анальгезирующее и жаропонижающее действие. Неизбирательно угнетая циклооксигеназу 1 и циклооксигеназу 2 нарушает метаболизм арахидоновой кислоты уменьшает количество простагландинов в очаге воспаления.
Наиболее эффективен при болях воспалительного характера. Как все нестероидные противовоспалительные препараты препарат оказывает антиагрегатную активность.
Фармакокинетика:
Максимальная концентрация в плазме крови создается через 30-40 мин и находится в линейной зависимости от используемой дозы. Изменения фармакокинетики диклофенака на фоне многократного введения не отмечается не кумулирует. Связь с белками плазмы - не более 99 % (большая часть связывается с альбуминами).
Проникает в синовиальную жидкость. Максимальная концентрация в синовиальной жидкости наблюдается на 2-4 ч позже чем в плазме. Период полувыведения из синовиальной жидкости 3-6 ч (концентрация активного вещества в синовиальной жидкости через 4-6 ч после введения препарата выше чем в плазме и остается выше еще в течение 12ч). Взаимосвязь концентрации препарата в синовиальной жидкости с клинической эффективностью препарата не выяснена.
Метаболизм происходит в результате многократного или однократного гидроксилирования и конъюгирования с глюкуроновой кислотой. В метаболизме препарата принимает участие ферментная система Р450 CYP2C9. Фармакологическая активность метаболитов ниже чем диклофенака.
Системный клиренс составляет 350 мл/мин объем распределения - 550 мл/кг. Период полувыведения из плазмы - 2 ч. 65 % введенной дозы выводится в виде метаболитов почками; менее 1 % выводится в неизменненном виде остальная часть дозы выводится в виде метаболитов с желчью.
У больных с выраженной почечной недостаточностью (клиренс креатинина менее 10 мл/мин) увеличивается выведение метаболитов с желчью при этом увеличения их концентрации в крови не наблюдается.
У больных с хроническим гепатитом или компенсированным циррозом печени фармакокинетические параметры диклофенака не изменяются. Диклофенак проникает в грудное молоко.
Показания к применению
Симптоматическое лечение заболеваний опорно-двигательного аппарата (ревматоидный артрит псориатический артрит анкилозирующий спондилоартрит; подагрический артрит ревматическое поражение мягких тканей остеоартроз периферических суставов и позвоночника в том числе с радикулярным синдромом тендовагинит бурсит).
Препарат предназначен для симптоматической терапии уменьшения боли и воспаления на момент использования на прогрессирование заболевания не влияет.
- Период после проведения аортокоронарного шунтирования.
- III триместр беременности период грудного вскармливания.
- Некомпенсированная сердечная недостаточность.
- Гиперчувствительность к активному веществу или вспомогательным компонентам.
- Анамнестические данные о приступе бронхообструкции ринита крапивницы после приема ацетилсалициловой кислоты или иного НПВП (полный или неполный синдром непереносимости ацетилсалициловой кислоты - риносинусит крапивница полипы слизистой оболочки носа астма).
- Эрозивно-язвенные изменения слизистой желудка или 12-перстной кишки активное желудочно-кишечное кровотечение.
- Цереброваскулярное кровотечение или иные кровотечения и нарушения гемостаза.
- Выраженная печеночная недостаточность или активное заболевание печени.
- Выраженная почечная недостаточность (клиренс креатинина менее 30 мл/мин) прогрессирующие заболевания почек в т.ч. подтвержденная гиперкалиемия.
- Детский возраст (до 18 лет для суппозиториев по 100 мг до 15 лет для суппозиториев по 50 мг).
- Ректальные кровотечения геморрой травма или воспаление прямой кишки.
С осторожностью:
Анемия бронхиальная астма цереброваскулярные заболевания ишемическая болезнь сердца застойная сердечная недостаточность артериальная гипертензия заболевания периферических артерий отечный синдром печеночная или почечная недостаточность дислипидемия/ гиперлипидемия сахарный диабет курение воспалительные заболевания кишечника состояние после обширных хирургических вмешательств индуцируемая порфирия пожилой возраст дивертикулит системные заболевания соединительной ткани клиренс креатинина от 30 до 60 мл/мин беременность (I-II триместр).
Анамнестические данные о развитии язвенного заболевания желудочно-кишечного тракта наличие инфекции Helicobacter pylori длительное использование НПВП частое употребление алкоголя тяжелые соматические заболевания.
Ректально взрослым начальная доза 100-150 мг/сут разделенная на 2-3 приема; в нетяжелых случаях и при длительной терапии - 50-100 мг/сут; в дополнение к пероральному приему суммарная суточная доза (ректально и перорально) не должна превышать 150 мг.
При альгодисменорее (при появлении первых симптомов) начальная доза 50-100 мг/сут которую при необходимости повышают в течение нескольких менструальных циклов до 150 мг. Приступ мигрени - 100 мг при первых признаках приступа.
При необходимости -повторно 100 мг. При необходимости продолжения лечения в последующие дни суточная доза не должна превышать 150 мг за несколько введений. У подростков старше 15 лет используются только суппозитории по 50 мг разовая доза - не более 1 суппозитория.
Побочное действие
Часто - 1-10 %; иногда - 01-1 %; редко - 001-01 %; очень редко - менее 0001 % включая отдельные случаи.
Со стороны пищеварительной системы: часто - эпигастральная боль тошнота рвота диарея диспепсия метеоризм анорексия повышение активности аминотрансфераз; редко - гастрит проктит кровотечение из ЖКТ (рвота с кровью мелена диарея с примесью крови) язвы ЖКТ (с или без кровотечения или перфорации) гепатит желтуха нарушение функции печени; очень редко - стоматит глоссит повреждения пищевода диафрагмоподобные стриктуры кишечника неспецифический геморрагический колит обострение язвенного колита или болезни Крона запор панкреатит молниеносный гепатит обострение геморроя.
Со стороны нервной системы: часто - головная боль головокружение; редко - сонливость; очень редко - нарушение чувствительности в т.ч. парестезии расстройства памяти тремор судороги тревога цереброваскулярные нарушения асептический менингит дезориентация депрессия бессонница ночные "кошмары" раздражительность психические нарушения.
Со стороны органов чувств: часто - вертиго; очень редко - нарушение зрения (затуманивание зрения диплопия) нарушение слуха шум в ушах нарушение вкусовых ощущений.
Со стороны мочевыделительной системы: очень редко - острая почечная недостаточность гематурия протеинурия интерстициальный нефрит нефротический синдром папиллярный некроз.
Со стороны органов кроветворения: очень редко - тромбоцитопения лейкопения гемолитическая и апластическая анемия агранулоцитоз.
Аллергические реакции: анафилактические/ анафилактоидные реакции включая выраженное снижение артериального давления и шок; очень редко - ангионевротический отек (в т.ч. лица).
Со стороны сердечно-сосудистой системы: очень редко - сердцебиение боль в груди повышение артериального давления васкулит сердечная недостаточность инфаркт миокарда.
Со стороны дыхательной системы: редко - бронхиальная астма (включая одышку); очень редко - пневмонит.
Со стороны кожных покровов: часто - кожная сыпь; редко - крапивница; очень редко - буллезные высыпания экзема в т.ч. мультиформная и синдром Стивенса-Джонсона синдром Лайелла эксфолиативный дерматит зуд выпадение волос фотосенсибилизация пурпура в т.ч. аллергическая.
Местные реакции при ректальном применении: раздражение слизистой оболочки прямой кишки слизистые выделения с примесью крови боли при дефекации ректальное кровотечение.
Передозировка
Симптомы: головокружение головная боль гипервентиляция легких помутнение сознания у детей - миоклонические судороги тошнота рвота боль в животе кровотечения из ЖКТ нарушение функции печени и почек.
Взаимодействие с другими лекарственными средствами
Повышает концентрацию в плазме дигоксина метотрексата препаратов лития и циклоспорина.
Снижает эффект диуретиков на фоне калийсберегающих диуретиков усиливается риск гиперкалиемии; на фоне антикоагулянтов тромболитических средств (альтеплаза стрептокиназа урокиназа) - риск кровотечений (чаще из желудочно-кишечного тракта). Уменьшает эффекты гипотензивных и снотворных средств.
Увеличивает вероятность возникновения побочных эффектов других нестероидных противовоспалительных препаратов и глюкокортикостероидных средств (кровотечения в желудочно-кишечном тракте) токсичность метотрексата и нефротоксичность циклоспорина. Ацетилсалициловая кислота снижает концентрацию диклофенака в крови. Одновременное использование с парацетамолом повышает риск развития нефротоксических эффектов диклофенака. Уменьшает эффект гипогликемических средств.
Цефамандол цефоперазон цефотетан вальпроевая кислота и пликамицин увеличивают частоту развития гипопротромбинемии.
Циклоспорин и препараты золота повышают влияние диклофенака на синтез простагландинов в почках что повышает нефротоксичность.
Одновременное назначение с этанолом колхицином кортикотропином ингибиторами обратного захвата серотонина и препаратами зверобоя продырявленного повышает риск развития кровотечений в желудочно-кишечном тракте.
Диклофенак усиливает действие препаратов вызывающих фотосенсибилизацию. Препараты блокирующие канальцевую секрецию повышают концентрацию в плазме диклофенака тем самым повышая его токсичность.
Антибактериальные лекарственные средства из группы хинолона - риск развития судорог. Влияние на результаты лабораторных анализов: диклофенак может влиять на показатели сывороточных трансаминаз (если это влияние носит продолжительный характер или если имеют место осложнения лечение необходимо прекратить) а также может вызвать повышение концентрации калия.
Особые указания
Из-за важной роли простагландинов в поддержании почечного кровотока следует проявлять особую осторожность при назначении пациентам с сердечной или почечной недостаточностью а также при терапии пожилых пациентов принимающих диуретики и больных у которых по какой-либо причине наблюдается снижение объема циркулирующей крови (например после крупного хирургического вмешательства).
Если в таких случаях назначают диклофенак рекомендуют в качестве меры предосторожности контролировать функцию почек.
У пациентов с печеночной недостаточностью (хронический гепатит компенсирующий цирроз печени) кинетика и метаболизм не отличаются от аналогичных процессов у пациентов с нормальной функцией печени. При проведении длительной терапии необходимо контролировать функцию печени картину периферической крови анализ кала на скрытую кровь.
В период лечения возможно снижение скорости психических и двигательных реакций поэтому необходимо воздержаться от вождения автотранспорта и занятий другими потенциально опасными видами деятельности требующими повышенной концентрации внимания и быстроты психомоторных реакций.
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Неизбирательно угнетая циклооксигеназу 1 и циклооксигеназу 2 нарушает метаболизм арахидоновой кислоты уменьшает количество простагландинов в очаге воспаления. "}},{"type":"paragraph","data":{"text":"Наиболее эффективен при болях воспалительного характера. Как все нестероидные противовоспалительные препараты препарат оказывает антиагрегатную активность. "}},{"type":"paragraph","data":{"text":"Фармакокинетика:"}},{"type":"paragraph","data":{"text":"Максимальная концентрация в плазме крови создается через 30-40 мин и находится в линейной зависимости от используемой дозы. Изменения фармакокинетики диклофенака на фоне многократного введения не отмечается не кумулирует. Связь с белками плазмы - не более 99 % (большая часть связывается с альбуминами). "}},{"type":"paragraph","data":{"text":"Проникает в синовиальную жидкость. Максимальная концентрация в синовиальной жидкости наблюдается на 2-4 ч позже чем в плазме. Период полувыведения из синовиальной жидкости 3-6 ч (концентрация активного вещества в синовиальной жидкости через 4-6 ч после введения препарата выше чем в плазме и остается выше еще в течение 12ч). Взаимосвязь концентрации препарата в синовиальной жидкости с клинической эффективностью препарата не выяснена."}},{"type":"paragraph","data":{"text":"Метаболизм происходит в результате многократного или однократного гидроксилирования и конъюгирования с глюкуроновой кислотой. В метаболизме препарата принимает участие ферментная система Р450 CYP2C9. Фармакологическая активность метаболитов ниже чем диклофенака."}},{"type":"paragraph","data":{"text":"Системный клиренс составляет 350 мл/мин объем распределения - 550 мл/кг. Период полувыведения из плазмы - 2 ч. 65 % введенной дозы выводится в виде метаболитов почками; менее 1 % выводится в неизменненном виде остальная часть дозы выводится в виде метаболитов с желчью."}},{"type":"paragraph","data":{"text":"У больных с выраженной почечной недостаточностью (клиренс креатинина менее 10 мл/мин) увеличивается выведение метаболитов с желчью при этом увеличения их концентрации в крови не наблюдается."}},{"type":"paragraph","data":{"text":"У больных с хроническим гепатитом или компенсированным циррозом печени фармакокинетические параметры диклофенака не изменяются. Диклофенак проникает в грудное молоко."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"\n\nСимптоматическое лечение заболеваний опорно-двигательного аппарата (ревматоидный артрит псориатический артрит анкилозирующий спондилоартрит; подагрический артрит ревматическое поражение мягких тканей остеоартроз периферических суставов и позвоночника в том числе с радикулярным синдромом тендовагинит бурсит). "}},{"type":"paragraph","data":{"text":"Препарат предназначен для симптоматической терапии уменьшения боли и воспаления на момент использования на прогрессирование заболевания не влияет. "}},{"type":"paragraph","data":{"text":"Болевой синдром слабой или умеренной выраженности: невралгия миалгия люмбоишиалгия посттравматический болевой синдром сопровождающийся воспалением послеоперационная боль головная боль мигрень альгодисменорея аднексит зубная боль.\n\n"}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"paragraph","data":{"text":"- Период после проведения аортокоронарного шунтирования."}},{"type":"paragraph","data":{"text":"- III триместр беременности период грудного вскармливания."}},{"type":"paragraph","data":{"text":"- Некомпенсированная сердечная недостаточность."}},{"type":"paragraph","data":{"text":"- Гиперчувствительность к активному веществу или вспомогательным компонентам."}},{"type":"paragraph","data":{"text":"- Анамнестические данные о приступе бронхообструкции ринита крапивницы после приема ацетилсалициловой кислоты или иного НПВП (полный или неполный синдром непереносимости ацетилсалициловой кислоты - риносинусит крапивница полипы слизистой оболочки носа астма)."}},{"type":"paragraph","data":{"text":"- Эрозивно-язвенные изменения слизистой желудка или 12-перстной кишки активное желудочно-кишечное кровотечение."}},{"type":"paragraph","data":{"text":"- Обострение воспалительных заболеваний кишечника (неспецифический язвенный колит болезнь Крона)."}},{"type":"paragraph","data":{"text":"- Цереброваскулярное кровотечение или иные кровотечения и нарушения гемостаза."}},{"type":"paragraph","data":{"text":"- Выраженная печеночная недостаточность или активное заболевание печени."}},{"type":"paragraph","data":{"text":"- Выраженная почечная недостаточность (клиренс креатинина менее 30 мл/мин) прогрессирующие заболевания почек в т.ч. подтвержденная гиперкалиемия."}},{"type":"paragraph","data":{"text":"- Детский возраст (до 18 лет для суппозиториев по 100 мг до 15 лет для суппозиториев по 50 мг)."}},{"type":"paragraph","data":{"text":"- Ректальные кровотечения геморрой травма или воспаление прямой кишки."}},{"type":"paragraph","data":{"text":"С осторожностью:"}},{"type":"paragraph","data":{"text":"Анемия бронхиальная астма цереброваскулярные заболевания ишемическая болезнь сердца застойная сердечная недостаточность артериальная гипертензия заболевания периферических артерий отечный синдром печеночная или почечная недостаточность дислипидемия/ гиперлипидемия сахарный диабет курение воспалительные заболевания кишечника состояние после обширных хирургических вмешательств индуцируемая порфирия пожилой возраст дивертикулит системные заболевания соединительной ткани клиренс креатинина от 30 до 60 мл/мин беременность (I-II триместр)."}},{"type":"paragraph","data":{"text":"Анамнестические данные о развитии язвенного заболевания желудочно-кишечного тракта наличие инфекции Helicobacter pylori длительное использование НПВП частое употребление алкоголя тяжелые соматические заболевания."}},{"type":"paragraph","data":{"text":"Одновременная терапия антикоагулянтами (например варфарин) антиагрегантами (например ацетилсалициловая кислота клопидогрель) пероральными глюкокортикостероидами (например преднизолон) селективными ингибиторами обратного захвата серотонина (например циталопрам флуоксетин пароксетин сертралин)."}}]},{"id":12,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Ректально взрослым начальная доза 100-150 мг/сут разделенная на 2-3 приема; в нетяжелых случаях и при длительной терапии - 50-100 мг/сут; в дополнение к пероральному приему суммарная суточная доза (ректально и перорально) не должна превышать 150 мг."}},{"type":"paragraph","data":{"text":"При альгодисменорее (при появлении первых симптомов) начальная доза 50-100 мг/сут которую при необходимости повышают в течение нескольких менструальных циклов до 150 мг. Приступ мигрени - 100 мг при первых признаках приступа."}},{"type":"paragraph","data":{"text":"При необходимости -повторно 100 мг. При необходимости продолжения лечения в последующие дни суточная доза не должна превышать 150 мг за несколько введений. У подростков старше 15 лет используются только суппозитории по 50 мг разовая доза - не более 1 суппозитория."}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Часто - 1-10 %; иногда - 01-1 %; редко - 001-01 %; очень редко - менее 0001 % включая отдельные случаи."}},{"type":"paragraph","data":{"text":"Со стороны пищеварительной системы: часто - эпигастральная боль тошнота рвота диарея диспепсия метеоризм анорексия повышение активности аминотрансфераз; редко - гастрит проктит кровотечение из ЖКТ (рвота с кровью мелена диарея с примесью крови) язвы ЖКТ (с или без кровотечения или перфорации) гепатит желтуха нарушение функции печени; очень редко - стоматит глоссит повреждения пищевода диафрагмоподобные стриктуры кишечника неспецифический геморрагический колит обострение язвенного колита или болезни Крона запор панкреатит молниеносный гепатит обострение геморроя."}},{"type":"paragraph","data":{"text":"Со стороны нервной системы: часто - головная боль головокружение; редко - сонливость; очень редко - нарушение чувствительности в т.ч. парестезии расстройства памяти тремор судороги тревога цереброваскулярные нарушения асептический менингит дезориентация депрессия бессонница ночные \"кошмары\" раздражительность психические нарушения."}},{"type":"paragraph","data":{"text":"Со стороны органов чувств: часто - вертиго; очень редко - нарушение зрения (затуманивание зрения диплопия) нарушение слуха шум в ушах нарушение вкусовых ощущений."}},{"type":"paragraph","data":{"text":"Со стороны мочевыделительной системы: очень редко - острая почечная недостаточность гематурия протеинурия интерстициальный нефрит нефротический синдром папиллярный некроз."}},{"type":"paragraph","data":{"text":"Со стороны органов кроветворения: очень редко - тромбоцитопения лейкопения гемолитическая и апластическая анемия агранулоцитоз."}},{"type":"paragraph","data":{"text":"Аллергические реакции: анафилактические/ анафилактоидные реакции включая выраженное снижение артериального давления и шок; очень редко - ангионевротический отек (в т.ч. лица)."}},{"type":"paragraph","data":{"text":"Со стороны сердечно-сосудистой системы: очень редко - сердцебиение боль в груди повышение артериального давления васкулит сердечная недостаточность инфаркт миокарда."}},{"type":"paragraph","data":{"text":"Со стороны дыхательной системы: редко - бронхиальная астма (включая одышку); очень редко - пневмонит."}},{"type":"paragraph","data":{"text":"Со стороны кожных покровов: часто - кожная сыпь; редко - крапивница; очень редко - буллезные высыпания экзема в т.ч. мультиформная и синдром Стивенса-Джонсона синдром Лайелла эксфолиативный дерматит зуд выпадение волос фотосенсибилизация пурпура в т.ч. аллергическая."}},{"type":"paragraph","data":{"text":"Местные реакции при ректальном применении: раздражение слизистой оболочки прямой кишки слизистые выделения с примесью крови боли при дефекации ректальное кровотечение."}}]},{"id":14,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"Симптомы: головокружение головная боль гипервентиляция легких помутнение сознания у детей - миоклонические судороги тошнота рвота боль в животе кровотечения из ЖКТ нарушение функции печени и почек."}},{"type":"paragraph","data":{"text":"Лечение: активированный уголь симптоматическая терапия. Форсированный диурез гемодиализ малоэффективны."}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"Повышает концентрацию в плазме дигоксина метотрексата препаратов лития и циклоспорина."}},{"type":"paragraph","data":{"text":"Снижает эффект диуретиков на фоне калийсберегающих диуретиков усиливается риск гиперкалиемии; на фоне антикоагулянтов тромболитических средств (альтеплаза стрептокиназа урокиназа) - риск кровотечений (чаще из желудочно-кишечного тракта). Уменьшает эффекты гипотензивных и снотворных средств."}},{"type":"paragraph","data":{"text":"Увеличивает вероятность возникновения побочных эффектов других нестероидных противовоспалительных препаратов и глюкокортикостероидных средств (кровотечения в желудочно-кишечном тракте) токсичность метотрексата и нефротоксичность циклоспорина. Ацетилсалициловая кислота снижает концентрацию диклофенака в крови. Одновременное использование с парацетамолом повышает риск развития нефротоксических эффектов диклофенака. Уменьшает эффект гипогликемических средств."}},{"type":"paragraph","data":{"text":"Цефамандол цефоперазон цефотетан вальпроевая кислота и пликамицин увеличивают частоту развития гипопротромбинемии."}},{"type":"paragraph","data":{"text":"Циклоспорин и препараты золота повышают влияние диклофенака на синтез простагландинов в почках что повышает нефротоксичность."}},{"type":"paragraph","data":{"text":"Одновременное назначение с этанолом колхицином кортикотропином ингибиторами обратного захвата серотонина и препаратами зверобоя продырявленного повышает риск развития кровотечений в желудочно-кишечном тракте."}},{"type":"paragraph","data":{"text":"Диклофенак усиливает действие препаратов вызывающих фотосенсибилизацию. Препараты блокирующие канальцевую секрецию повышают концентрацию в плазме диклофенака тем самым повышая его токсичность."}},{"type":"paragraph","data":{"text":"Антибактериальные лекарственные средства из группы хинолона - риск развития судорог. Влияние на результаты лабораторных анализов: диклофенак может влиять на показатели сывороточных трансаминаз (если это влияние носит продолжительный характер или если имеют место осложнения лечение необходимо прекратить) а также может вызвать повышение концентрации калия."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"Из-за важной роли простагландинов в поддержании почечного кровотока следует проявлять особую осторожность при назначении пациентам с сердечной или почечной недостаточностью а также при терапии пожилых пациентов принимающих диуретики и больных у которых по какой-либо причине наблюдается снижение объема циркулирующей крови (например после крупного хирургического вмешательства)."}},{"type":"paragraph","data":{"text":"Если в таких случаях назначают диклофенак рекомендуют в качестве меры предосторожности контролировать функцию почек."}},{"type":"paragraph","data":{"text":"У пациентов с печеночной недостаточностью (хронический гепатит компенсирующий цирроз печени) кинетика и метаболизм не отличаются от аналогичных процессов у пациентов с нормальной функцией печени. При проведении длительной терапии необходимо контролировать функцию печени картину периферической крови анализ кала на скрытую кровь."}},{"type":"paragraph","data":{"text":"В период лечения возможно снижение скорости психических и двигательных реакций поэтому необходимо воздержаться от вождения автотранспорта и занятий другими потенциально опасными видами деятельности требующими повышенной концентрации внимания и быстроты психомоторных реакций."}}]}],"source":null},"description_toggle":false,"short_description":"Нестероидный противовоспалительный препарат производное фенилуксусной кислоты; оказывает противовоспалительное анальгезирующее и жаропонижающее действие. Неизбирательно угнетая циклооксигеназу 1 и циклооксигеназу 2 нарушает метаболизм арахидоновой кислоты уменьшает количество простагландинов в очаге воспаления. Наиболее эффективен при болях воспалительного характера. Как все нестероидные противовоспалительные препараты препарат оказывает антиагрегатную активность. Фармакокинетика: Максимальная концентрация в плазме крови создается через 30-40 мин и находится в линейной зависимости от используемой дозы. Изменения фармакокинетики диклофенака на фоне многократного введения не отмечается не кумулирует. Связь с белками плазмы - не более 99 % (большая часть связывается с альбуминами). Проникает в синовиальную жидкость. Максимальная концентрация в синовиальной жидкости наблюдается на 2-4 ч позже чем в плазме. Период полувыведения из синовиальной жидкости 3-6 ч (концентрация активного вещества в синовиальной жидкости через 4-6 ч после введения препарата выше чем в плазме и остается выше еще в течение 12ч). Взаимосвязь концентрации препарата в синовиальной жидкости с клинической эффективностью препарата не выяснена. Метаболизм происходит в результате многократного или однократного гидроксилирования и конъюгирования с глюкуроновой кислотой. В метаболизме препарата принимает участие ферментная система Р450 CYP2C9. Фармакологическая активность метаболитов ниже чем диклофенака. Системный клиренс составляет 350 мл/мин объем распределения - 550 мл/кг. Период полувыведения из плазмы - 2 ч. 65 % введенной дозы выводится в виде метаболитов почками; менее 1 % выводится в неизменненном виде остальная часть дозы выводится в виде метаболитов с желчью. У больных с выраженной почечной недостаточностью (клиренс креатинина менее 10 мл/мин) увеличивается выведение метаболитов с желчью при этом увеличения их концентрации в крови не наблюдается. У больных с хроническим гепатитом или компенсированным циррозом печени фармакокинетические параметры диклофенака не изменяются. 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