Нестероидный противовоспалительный препарат (НПВП) из класса... Инструкция
Показания к применению
Ревматоидный артрит, остеоартроз, артриты различной этиологии, артралгии, миалгии, послеоперационные и посттравматические боли, бурсит, тенденит, альгодисменорея, зубная и головная боль.
Противопоказания
повышенная чувствительность к компонентам препарата,
полное или неполное сочетание бронхиальной астмы, рецидивирующего полипоза носа или околоносовых пазух и непереносимости ацетилсалициловой кислоты и других НПВП (в том числе в анамнезе),
эрозивно-язвенные поражения слизистой оболочки желудка и двенадцатиперстной кишки,
Нестероидный противовоспалительный препарат (НПВП) из класса сульфонанилидов. Является селективным конкурентным ингибитором циклооксигеназы-2 (ЦОГ-2) – фермента, участвующего в синтезе простагландинов – медиаторов отека, воспаления и боли. Оказывает противовоспалительное, анальгезирующее и жаропонижающее действие.
Обратимо ингибирует образование простагландина Е2, как в очаге воспаления, так и в восходящих путях ноцицептивной системы, включая пути проведения болевых импульсов спинного мозга.
Снижает концентрацию короткоживущего простагландина Н2, из которого под действием простагландин-изомеразы образуется простагландин Е2. Уменьшение концентрации простагландина Е2 ведет к снижению степени активации простаноидных рецепторов ЕР типа, что выражается в анальгетическом и противовоспалительном эффектах.
В незначительной степени действует на ЦОГ-1, практически не препятствуя образованию простагландина Е2 из арахидоновой кислоты в физиологических условиях, благодаря чему снижается количество побочных эффектов препарата.
Препарат также подавляет агрегацию тромбоцитов путем ингибирования синтеза эндопероксидов и тромбоксана А2, ингибирует синтез фактора агрегации тромбоцитов, тормозит активацию плазминогена путем увеличения концентрации ингибитора-1. Подавляет высвобождение гистамина, а также уменьшает степень бронхоспазма, вызванного воздействием гистамина и ацетальдегида. Ингибирует высвобождение фактора некроза опухолей а, обуславливающего образование цитокининов.
Показано, что нимесулид способен подавлять синтез интерлейкина-6 и урокиназы, тем самым препятствуя разрушению хрящевой ткани. Ингибирует синтез металлопротеаз (эластазы, коллагеназы), предотвращая разрушение протеогликанов и коллагена хрящевой ткани.
Обладает антиоксидантными свойствами, тормозит образование токсических продуктов распада кислорода за счет уменьшения активности миелопероксидазы. Взаимодействует с глюкокортикоидными рецепторами, активируя их путем фосфориляции, что также усиливает противовоспалительное действие препарата.
Фармакокинетика
Абсорбция при приеме внутрь – высокая. Прием пищи снижает скорость абсорбции, не оказывая влияния на ее степень. Время достижения максимальной концентрации активного вещества в плазме крови – 1,5-2,5 ч. Связь с белками плазмы составляет 95%, с эритроцитами – 2%, с липопротеинами – 1%, с кислыми альфа1-гликопротеидами – 1%.
Доза препарата не влияет на степень его связывания с белками крови.
Максимальная концентрация нимесулида в плазме крови достигает 3,5-6,5 мг/л. Объем распределения – 0,19-0,35 л/кг. Проникает в ткани женских половых органов, где после однократного приема его концентрация составляет около 40% от концентрации в плазме. Хорошо проникает в кислую среду очага воспаления (40%), синовиальную жидкость (43%).
Легко проникает через гисто-гематические барьеры.
Метаболизируется в печени тканевыми монооксигеназами. Основной метаболит – 4-гидроксинимесулид (25%) обладает сходной фармакологической активностью.
Период полувыведения нимесулида составляет 1,56-4,95 часа, 4-гидроксинимесулида – 2,89-4,78 часа. 4-гидроксинимесулид выводится почками (65%) и с желчью (35%).
У больных с почечной недостаточностью (клиренс креатинина 1,8-4,8 л/ч или 30-80 мл/мин), а также у детей и лиц пожилого возраста фармакокинетический профиль нимесулида существенно не меняется.
Показания к применению
Ревматоидный артрит, остеоартроз, артриты различной этиологии, артралгии, миалгии, послеоперационные и посттравматические боли, бурсит, тенденит, альгодисменорея, зубная и головная боль.
Противопоказания
повышенная чувствительность к компонентам препарата,
полное или неполное сочетание бронхиальной астмы, рецидивирующего полипоза носа или околоносовых пазух и непереносимости ацетилсалициловой кислоты и других НПВП (в том числе в анамнезе),
эрозивно-язвенные поражения слизистой оболочки желудка и двенадцатиперстной кишки,
активное желудочно-кишечное кровотечение,
цереброваскулярное или иное кровотечение,
воспалительные заболевания кишечника (болезнь Крона, язвенный колит) в фазе обострения,
гемофилия и другие нарушения свертываемости крови,
печеночная недостаточность или любое активное заболевание печени,
гепатотоксические реакции при использовании нимесулида в анамнезе,
алкоголизм,
наркомания,
выраженная хроническая почечная недостаточность (клиренс креатинина менее 30 мл/мин),
прогрессирующие заболевания почек,
подтвержденная гиперкалиемия,
период после проведения аортокоронарного шунтирования,
одновременный прием других гепатотоксических лекарственных средств,
беременность,
период лактации,
детский возраст до 12 лет.
С осторожностью
ишемическая болезнь сердца, цереброваскулярные заболевания, хроническая сердечная недостаточность, дислипидемия/гиперлипидемия, сахарный диабет, заболевания периферических артерий, курение, почечная недостаточность (клиренс креатинина 30-60 мл/мин), анамнестические данные о развитии язвенного поражения желудочно-кишечного тракта, наличие инфекции Helicobacter pylori, пожилой возраст, длительное использование нестероидных противовоспалительных препаратов, алкоголизм, тяжелые соматические заболевания, одновременный прием антикоагулянтов (в т.ч. варфарин), антиагрегантов (в т.ч. ацетилсалициловая кислота, клопидогрел), пероральных глюкокортикостероидов, селективных ингибиторов обратного захвата серотонина (в т.ч. циталопрам, флуоксетин, пароксетин, сертралин).
Способ применения и дозы
Внутрь, после еды, по 50-100 мг 2 раза в сутки.
У пациентов с хронической печеночной недостаточностью суточная доза – 100 мг.
Следует использовать минимальную эффективную дозу минимально возможным коротким курсом.
Детям старше 12 лет назначают из расчета разовой дозы 1,5 мг/кг массы тела ребенка, максимальная суточная доза препарата – 5 мг/кг в сутки (не более 200 мг/сутки).
Побочное действие
Частота классифицируется по рубрикам, в зависимости от встречаемости случая: очень часто (>10), часто (< 10-< 100), нечасто (< 100-< 1000), редко (< 1000-< 10000), очень редко (< 10000).
Желудочно-кишечный тракт: часто – диарея, тошнота, рвота; нечасто – запор, метеоризм, гастрит; очень редко – боли в животе, стоматит, дегтеобразный стул, желудочно-кишечное кровотечение, язва и/или перфорация желудка или двенадцатиперстной кишки.
Центральная нервная система: нечасто – головокружение; редко – ощущение страха, нервозность, кошмарные сновидения; очень редко – головная боль, сонливость, энцефалопатия (синдром Рейе).
Органы дыхания: нечасто – одышка; очень редко – бронхиальная астма, бронхоспазм.
Органы чувств: редко – нечеткость зрения, очень редко – головокружение.
Кожные и слизистые покровы: нечасто – зуд, сыпь, усиление потоотделения; редко: эритема, дерматит; очень редко: крапивница, ангионевротический отек, отечность лица, многоформная экссудативная эритема, в т.ч. синдром Стивенса-Джонсона, токсический эпидермальный некролиз (синдром Лайелла).
Печень и желчевыводящая система: часто – повышение «печеночных» трансаминаз; очень редко – гепатит, молниеносный гепатит, желтуха, холестаз.
Почки и мочевыводящая система: нечасто – отеки; редко – дизурия, гематурия, задержка мочи, гиперкалиемия; очень редко – почечная недостаточность, олигурия, интерстициальный нефрит.
Органы кроветворения: редко – анемия, эозинофилия; очень редко – тромбоцитопения, панцитопения, пурпура, удлинение времени кровотечения.
Аллергические реакции: редко – реакции гиперчувствительности; очень редко – анафилактоидные реакции.
Общие реакции: редко – общая слабость; очень редко – гипотермия.
В случае появления других, не упомянутых выше, побочных действий или ухудшения Вашего самочувствия обратитесь, пожалуйста, незамедлительно к своему врачу.
Передозировка
Симптомы: апатия, сонливость, тошнота, рвота. Они, как правило, обратимы при оказании поддерживающего ухода за больными. Может возникнуть желудочно-кишечное кровотечение, артериальная гипертензия, острая почечная недостаточность, угнетение дыхания.
Лечение: требуется симптоматическое лечение пациента и поддерживающий уход за ним. Специфического антидота нет. В случае если передозировка произошла в течение последних 4 часов необходимо вызвать рвоту, обеспечить прием активированного угля (60-100 г на взрослого человека), осмотические слабительные. Форсированный диурез, гемодиализ неэффективны из-за высокой связи препарата с белками.
Взаимодействие с другими лекарственными средствами
Действие медикаментов, уменьшающих свертываемость крови, усиливается при их одновременном применении с нимесулидом.
Нимесулид может снижать действие фуросемида. Уменьшает терапевтический эффект антигипертензивных препаратов. Нимесулид может увеличивать возможность наступления побочных действий при одновременном приеме метотрексата.
Уровень лития в плазме повышается при одновременном приеме препаратов лития и нимесулида. Из-за высокой степени связывания нимесулида с белками плазмы пациенты, которых одновременно лечат гидантоином и сульфаниламидами, должны находиться под наблюдением врача, проходя обследование через короткие промежутки времени.
Нимесулид может усиливать действие циклоспорина на почки.
Использование с глюкокортикостероидами, ингибиторами обратного захвата серотонина увеличивает риск развития ЖКТ-кровотечений.
Особые указания
При назначении препарата пожилым пациентам коррекции режима дозирования не требуется.
При длительном применении необходим систематический контроль функции печени и почек. Необходимо проведение контроля лабораторных показателей активности печеночных трансаминаз не реже 1 раза в неделю.
Условия хранения
При температуре не выше 25°С.
Хранить в недоступном для детей месте.
Срок годности
3 года.
Не использовать по истечении срока годности, указанного на упаковке.
Для описания товара использована информация от партнера 36.6
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Уменьшение концентрации простагландина Е2 ведет к снижению степени активации простаноидных рецепторов ЕР типа, что выражается в анальгетическом и противовоспалительном эффектах."}},{"type":"paragraph","data":{"text":"В незначительной степени действует на ЦОГ-1, практически не препятствуя образованию простагландина Е2 из арахидоновой кислоты в физиологических условиях, благодаря чему снижается количество побочных эффектов препарата."}},{"type":"paragraph","data":{"text":"Препарат также подавляет агрегацию тромбоцитов путем ингибирования синтеза эндопероксидов и тромбоксана А2, ингибирует синтез фактора агрегации тромбоцитов, тормозит активацию плазминогена путем увеличения концентрации ингибитора-1. Подавляет высвобождение гистамина, а также уменьшает степень бронхоспазма, вызванного воздействием гистамина и ацетальдегида. Ингибирует высвобождение фактора некроза опухолей а, обуславливающего образование цитокининов."}},{"type":"paragraph","data":{"text":"Показано, что нимесулид способен подавлять синтез интерлейкина-6 и урокиназы, тем самым препятствуя разрушению хрящевой ткани. Ингибирует синтез металлопротеаз (эластазы, коллагеназы), предотвращая разрушение протеогликанов и коллагена хрящевой ткани."}},{"type":"paragraph","data":{"text":"Обладает антиоксидантными свойствами, тормозит образование токсических продуктов распада кислорода за счет уменьшения активности миелопероксидазы. Взаимодействует с глюкокортикоидными рецепторами, активируя их путем фосфориляции, что также усиливает противовоспалительное действие препарата."}},{"type":"paragraph","data":{"text":"Фармакокинетика"}},{"type":"paragraph","data":{"text":"Абсорбция при приеме внутрь – высокая. Прием пищи снижает скорость абсорбции, не оказывая влияния на ее степень. Время достижения максимальной концентрации активного вещества в плазме крови – 1,5-2,5 ч. Связь с белками плазмы составляет 95%, с эритроцитами – 2%, с липопротеинами – 1%, с кислыми альфа1-гликопротеидами – 1%."}},{"type":"paragraph","data":{"text":"Доза препарата не влияет на степень его связывания с белками крови."}},{"type":"paragraph","data":{"text":"Максимальная концентрация нимесулида в плазме крови достигает 3,5-6,5 мг/л. Объем распределения – 0,19-0,35 л/кг. Проникает в ткани женских половых органов, где после однократного приема его концентрация составляет около 40% от концентрации в плазме. Хорошо проникает в кислую среду очага воспаления (40%), синовиальную жидкость (43%)."}},{"type":"paragraph","data":{"text":"Легко проникает через гисто-гематические барьеры."}},{"type":"paragraph","data":{"text":"Метаболизируется в печени тканевыми монооксигеназами. Основной метаболит – 4-гидроксинимесулид (25%) обладает сходной фармакологической активностью."}},{"type":"paragraph","data":{"text":"Период полувыведения нимесулида составляет 1,56-4,95 часа, 4-гидроксинимесулида – 2,89-4,78 часа. 4-гидроксинимесулид выводится почками (65%) и с желчью (35%)."}},{"type":"paragraph","data":{"text":"У больных с почечной недостаточностью (клиренс креатинина 1,8-4,8 л/ч или 30-80 мл/мин), а также у детей и лиц пожилого возраста фармакокинетический профиль нимесулида существенно не меняется."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"Ревматоидный артрит, остеоартроз, артриты различной этиологии, артралгии, миалгии, послеоперационные и посттравматические боли, бурсит, тенденит, альгодисменорея, зубная и головная боль."}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"list","data":{"style":"ordered","items":["повышенная чувствительность к компонентам препарата,","полное или неполное сочетание бронхиальной астмы, рецидивирующего полипоза носа или околоносовых пазух и непереносимости ацетилсалициловой кислоты и других НПВП (в том числе в анамнезе),","эрозивно-язвенные поражения слизистой оболочки желудка и двенадцатиперстной кишки,","активное желудочно-кишечное кровотечение,","цереброваскулярное или иное кровотечение,","воспалительные заболевания кишечника (болезнь Крона, язвенный колит) в фазе обострения,","гемофилия и другие нарушения свертываемости крови,","декомпенсированная хроническая сердечная недостаточность,","печеночная недостаточность или любое активное заболевание печени,","гепатотоксические реакции при использовании нимесулида в анамнезе,","алкоголизм,","наркомания,","выраженная хроническая почечная недостаточность (клиренс креатинина менее 30 мл/мин),","прогрессирующие заболевания почек,","подтвержденная гиперкалиемия,","период после проведения аортокоронарного шунтирования,","одновременный прием других гепатотоксических лекарственных средств,","беременность,","период лактации,","детский возраст до 12 лет."]}}]},{"id":10,"name":"С осторожностью","slug":"cautions","body":[{"type":"paragraph","data":{"text":"ишемическая болезнь сердца, цереброваскулярные заболевания, хроническая сердечная недостаточность, дислипидемия/гиперлипидемия, сахарный диабет, заболевания периферических артерий, курение, почечная недостаточность (клиренс креатинина 30-60 мл/мин), анамнестические данные о развитии язвенного поражения желудочно-кишечного тракта, наличие инфекции Helicobacter pylori, пожилой возраст, длительное использование нестероидных противовоспалительных препаратов, алкоголизм, тяжелые соматические заболевания, одновременный прием антикоагулянтов (в т.ч. варфарин), антиагрегантов (в т.ч. ацетилсалициловая кислота, клопидогрел), пероральных глюкокортикостероидов, селективных ингибиторов обратного захвата серотонина (в т.ч. циталопрам, флуоксетин, пароксетин, сертралин)."}}]},{"id":12,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Внутрь, после еды, по 50-100 мг 2 раза в сутки."}},{"type":"paragraph","data":{"text":"У пациентов с хронической печеночной недостаточностью суточная доза – 100 мг."}},{"type":"paragraph","data":{"text":"Следует использовать минимальную эффективную дозу минимально возможным коротким курсом."}},{"type":"paragraph","data":{"text":"Детям старше 12 лет назначают из расчета разовой дозы 1,5 мг/кг массы тела ребенка, максимальная суточная доза препарата – 5 мг/кг в сутки (не более 200 мг/сутки)."}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Частота классифицируется по рубрикам, в зависимости от встречаемости случая: очень часто (>10), часто (< 10-< 100), нечасто (< 100-< 1000), редко (< 1000-< 10000), очень редко (< 10000)."}},{"type":"paragraph","data":{"text":"Желудочно-кишечный тракт: часто – диарея, тошнота, рвота; нечасто – запор, метеоризм, гастрит; очень редко – боли в животе, стоматит, дегтеобразный стул, желудочно-кишечное кровотечение, язва и/или перфорация желудка или двенадцатиперстной кишки."}},{"type":"paragraph","data":{"text":"Центральная нервная система: нечасто – головокружение; редко – ощущение страха, нервозность, кошмарные сновидения; очень редко – головная боль, сонливость, энцефалопатия (синдром Рейе)."}},{"type":"paragraph","data":{"text":"Органы дыхания: нечасто – одышка; очень редко – бронхиальная астма, бронхоспазм."}},{"type":"paragraph","data":{"text":"Сердечно-сосудистая система: нечасто – артериальная гипертензия; редко – тахикардия, геморрагии, «приливы»."}},{"type":"paragraph","data":{"text":"Органы чувств: редко – нечеткость зрения, очень редко – головокружение."}},{"type":"paragraph","data":{"text":"Кожные и слизистые покровы: нечасто – зуд, сыпь, усиление потоотделения; редко: эритема, дерматит; очень редко: крапивница, ангионевротический отек, отечность лица, многоформная экссудативная эритема, в т.ч. синдром Стивенса-Джонсона, токсический эпидермальный некролиз (синдром Лайелла)."}},{"type":"paragraph","data":{"text":"Печень и желчевыводящая система: часто – повышение «печеночных» трансаминаз; очень редко – гепатит, молниеносный гепатит, желтуха, холестаз."}},{"type":"paragraph","data":{"text":"Почки и мочевыводящая система: нечасто – отеки; редко – дизурия, гематурия, задержка мочи, гиперкалиемия; очень редко – почечная недостаточность, олигурия, интерстициальный нефрит."}},{"type":"paragraph","data":{"text":"Органы кроветворения: редко – анемия, эозинофилия; очень редко – тромбоцитопения, панцитопения, пурпура, удлинение времени кровотечения."}},{"type":"paragraph","data":{"text":"Аллергические реакции: редко – реакции гиперчувствительности; очень редко – анафилактоидные реакции."}},{"type":"paragraph","data":{"text":"Общие реакции: редко – общая слабость; очень редко – гипотермия."}},{"type":"paragraph","data":{"text":"В случае появления других, не упомянутых выше, побочных действий или ухудшения Вашего самочувствия обратитесь, пожалуйста, незамедлительно к своему врачу."}}]},{"id":14,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"\n\nСимптомы: апатия, сонливость, тошнота, рвота. Они, как правило, обратимы при оказании поддерживающего ухода за больными. Может возникнуть желудочно-кишечное кровотечение, артериальная гипертензия, острая почечная недостаточность, угнетение дыхания."}},{"type":"paragraph","data":{"text":"Лечение: требуется симптоматическое лечение пациента и поддерживающий уход за ним. Специфического антидота нет. В случае если передозировка произошла в течение последних 4 часов необходимо вызвать рвоту, обеспечить прием активированного угля (60-100 г на взрослого человека), осмотические слабительные. Форсированный диурез, гемодиализ неэффективны из-за высокой связи препарата с белками.\n\n"}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"Действие медикаментов, уменьшающих свертываемость крови, усиливается при их одновременном применении с нимесулидом."}},{"type":"paragraph","data":{"text":"Нимесулид может снижать действие фуросемида. Уменьшает терапевтический эффект антигипертензивных препаратов. Нимесулид может увеличивать возможность наступления побочных действий при одновременном приеме метотрексата."}},{"type":"paragraph","data":{"text":"Уровень лития в плазме повышается при одновременном приеме препаратов лития и нимесулида. Из-за высокой степени связывания нимесулида с белками плазмы пациенты, которых одновременно лечат гидантоином и сульфаниламидами, должны находиться под наблюдением врача, проходя обследование через короткие промежутки времени."}},{"type":"paragraph","data":{"text":"Нимесулид может усиливать действие циклоспорина на почки."}},{"type":"paragraph","data":{"text":"Использование с глюкокортикостероидами, ингибиторами обратного захвата серотонина увеличивает риск развития ЖКТ-кровотечений."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"\n\nПри назначении препарата пожилым пациентам коррекции режима дозирования не требуется."}},{"type":"paragraph","data":{"text":"При длительном применении необходим систематический контроль функции печени и почек. Необходимо проведение контроля лабораторных показателей активности печеночных трансаминаз не реже 1 раза в неделю.\n\n"}}]},{"id":19,"name":"Условия хранения","slug":"storage","body":[{"type":"paragraph","data":{"text":"\n\nПри температуре не выше 25°С."}},{"type":"paragraph","data":{"text":"Хранить в недоступном для детей месте.\n\n"}}]},{"id":20,"name":"Срок годности","slug":"expiry_date","body":[{"type":"paragraph","data":{"text":"\n\n3 года."}},{"type":"paragraph","data":{"text":"Не использовать по истечении срока годности, указанного на упаковке.\n\n"}}]},{"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":"\u003ca href=\"https://www.eapteka.ru/goods/manufacturer/shreya/\"\u003eШрея Лайф Саенсиз Пвт.Лтд, Индия\u003c/a\u003e"}}]}],"source":null},"description_toggle":false,"short_description":"Нестероидный противовоспалительный препарат (НПВП) из класса сульфонанилидов. Является селективным конкурентным ингибитором циклооксигеназы-2 (ЦОГ-2) – фермента, участвующего в синтезе простагландинов – медиаторов отека, воспаления и боли. Оказывает противовоспалительное, анальгезирующее и жаропонижающее действие. Обратимо ингибирует образование простагландина Е2, как в очаге воспаления, так и в восходящих путях ноцицептивной системы, включая пути проведения болевых импульсов спинного мозга. Снижает концентрацию короткоживущего простагландина Н2, из которого под действием простагландин-изомеразы образуется простагландин Е2. Уменьшение концентрации простагландина Е2 ведет к снижению степени активации простаноидных рецепторов ЕР типа, что выражается в анальгетическом и противовоспалительном эффектах. В незначительной степени действует на ЦОГ-1, практически не препятствуя образованию простагландина Е2 из арахидоновой кислоты в физиологических условиях, благодаря чему снижается количество побочных эффектов препарата. Препарат также подавляет агрегацию тромбоцитов путем ингибирования синтеза эндопероксидов и тромбоксана А2, ингибирует синтез фактора агрегации тромбоцитов, тормозит активацию плазминогена путем увеличения концентрации ингибитора-1. Подавляет высвобождение гистамина, а также уменьшает степень бронхоспазма, вызванного воздействием гистамина и ацетальдегида. Ингибирует высвобождение фактора некроза опухолей а, обуславливающего образование цитокининов. Показано, что нимесулид способен подавлять синтез интерлейкина-6 и урокиназы, тем самым препятствуя разрушению хрящевой ткани. Ингибирует синтез металлопротеаз (эластазы, коллагеназы), предотвращая разрушение протеогликанов и коллагена хрящевой ткани. Обладает антиоксидантными свойствами, тормозит образование токсических продуктов распада кислорода за счет уменьшения активности миелопероксидазы. Взаимодействует с глюкокортикоидными рецепторами, активируя их путем фосфориляции, что также усиливает противовоспалительное действие препарата. Фармакокинетика Абсорбция при приеме внутрь – высокая. Прием пищи снижает скорость абсорбции, не оказывая влияния на ее степень. Время достижения максимальной концентрации активного вещества в плазме крови – 1,5-2,5 ч. Связь с белками плазмы составляет 95%, с эритроцитами – 2%, с липопротеинами – 1%, с кислыми альфа1-гликопротеидами – 1%. Доза препарата не влияет на степень его связывания с белками крови. Максимальная концентрация нимесулида в плазме крови достигает 3,5-6,5 мг/л. Объем распределения – 0,19-0,35 л/кг. Проникает в ткани женских половых органов, где после однократного приема его концентрация составляет около 40% от концентрации в плазме. Хорошо проникает в кислую среду очага воспаления (40%), синовиальную жидкость (43%). Легко проникает через гисто-гематические барьеры. Метаболизируется в печени тканевыми монооксигеназами. Основной метаболит – 4-гидроксинимесулид (25%) обладает сходной фармакологической активностью. Период полувыведения нимесулида составляет 1,56-4,95 часа, 4-гидроксинимесулида – 2,89-4,78 часа. 4-гидроксинимесулид выводится почками (65%) и с желчью (35%). У больных с почечной недостаточностью (клиренс креатинина 1,8-4,8 л/ч или 30-80 мл/мин), а также у детей и лиц пожилого возраста фармакокинетический профиль нимесулида существенно не меняется.","substance":[{"id":129,"title":"Нимесулид","title_latin":"Nimesulidum","slug":"nimesulid_129"}],"branding":null,"valid_for_quick_buy":true,"is_available_to_delivery":false,"comments":null,"image_alt":"Нимесан - фото упаковки","image_share":{"isTouch":{"default":"https://vseapteki.ru/cropping/thumbnails/101/3791/share_default/"},"isFromTablet":{"default":"https://vseapteki.ru/cropping/thumbnails/101/3791/share_default/"}},"diseases":[{"id":"1012","title":"Серопозитивный ревматоидный артрит","slug":"1012-seropozitivnyy_revmatoidnyy_artrit"},{"id":"1016","title":"Полиартроз","slug":"1016-poliartroz"},{"id":"1020","title":"Боль в суставе","slug":"1020-bol_v_sustave"},{"id":"1147","title":"Первичная дисменорея","slug":"1147-pervichnaya_dismenoreya"},{"id":"1148","title":"Вторичная 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