ЛИДОКАИН Ампулы, 5 шт, 2 мл, 20 мг / мл

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В основе его механизма действия лежит уменьшение проницаемости мембраны нейрона для ионов натрия. В результате этого снижается скорость деполяризации и повышается порог возбуждения, приводя к обратимому местному онемению. Лидокаин применяют в целях достижения проводниковой анестезии в различных участках тела и контроля аритмий. Обладает быстрым началом действия (около одной минуты после внутривенного введения и пятнадцати минут после внутримышечного), быстро распространяется в окружающие ткани. Действие продолжается 10-20 минут и около 60-90 минут после внутривенного и внутримышечного введения соответственно."}},{"type":"header","data":{"text":"Фармакокинетика:","level":3}},{"type":"paragraph","data":{"text":"\u003ci\u003eАбсорбция\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Лидокаин быстро абсорбируется из желудочно-кишечного тракта, однако вследствие эф­фекта \"первичного прохождения\" через печень лишь небольшое его количество достигает системного кровотока. Системная абсорбция лидокаина определяется местом введения, дозой и его фармаколо­гическим профилем. Максимальная концентрация в крови достигается после межреберной блокады, далее (в порядке снижения концентрации), после введения в поясничное эпидуральнос пространство, плечевое сплетение и подкожные ткани. Основным фактором, определяющим скорость абсорбции и концентрацию в крови, является общая введенная доза, независимо от участка введения. Имеется линейная зависимость между количеством введенного лидокаина и результирующей максимальной концентрацией анестетика в кро­ви."}},{"type":"paragraph","data":{"text":"\u003ci\u003eРаспределение\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Лидокаин связывается с белками плазмы, включая α\u003csub\u003e1\u003c/sub\u003e-кислый гликопротеин (АКГ) и аль­бумин. Степень связывания вариабельна, составляя приблизительно 66%. Плазменная концентрация АКГ у новорожденных низкая, поэтому у них отмечается относительно вы­сокое содержание свободной биологически активной фракции лидокаина. Лидокаин проникает через гематоэнцефалический и плацентарный барьеры, вероятно, по­средством пассивной диффузии. \u003ci\u003eМетаболизм\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Лидокаин метаболизируется в печени, около 90% введенной дозы подвергается N- дезалкилированию с образованием моноэтилглицинксилидида (MEGX) и глицинксилидида (GX), оба вносят вклад в терапевтические и токсические эффекты лидокаина. Фар­макологические и токсические эффекты MEGX и GX сопоставимы с таковыми лидокаина, но выражены слабее. GX обладает более длинным, чем лидокаин, периодом полувыведе­ния (около 10 часов) и может кумулировать при многократном введении. Метаболиты, образующиеся в результате последующего метаболизма, выводятся с мочой, содержание неизменного лидокаина в моче не превышает 10%."}},{"type":"paragraph","data":{"text":"\u003ci\u003eВыведение\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Терминальный период полувыведения лидокаина после внутривенного болюсного введе­ния здоровым взрослым добровольцам составляет 1-2 часа. Терминальный период полувыведения GX составляет около 10 часов, MEGX - 2 часа."}},{"type":"paragraph","data":{"text":"\u003ci\u003eОсобые группы пациентов\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Вследствие быстрого метаболизма на фармакокинетику лидокаина могут оказывать влия­ние состояния, нарушающие функцию печени. У пациентов с печеночной дисфункцией период полувыведения лидокаина может повышаться в 2 и более раз. Нарушение функции почек не влияет на фармакокинетику лидокаина, но может приво­дить к кумуляции его метаболитов."}},{"type":"paragraph","data":{"text":"У новорожденных отмечается низкая концентрация АКГ, поэтому связь с белками плазмы может снижаться. Вследствие потенциально высокой концентрации свободной фракции применение лидокаина у новорожденных не рекомендуется."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"paragraph","data":{"text":"Местная и регионарная анестезия, проводниковая анестезия при больших и малых вмешательствах."}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"paragraph","data":{"text":"- Гиперчувствительность к компонентам препарата и к анестетикам амидного типа;"}},{"type":"paragraph","data":{"text":"- атриовентрикулярная (AV) блокада 3 степени;"}},{"type":"paragraph","data":{"text":"- гиповолемия."}}]},{"id":10,"name":"С осторожностью","slug":"cautions","body":[{"type":"paragraph","data":{"text":"Введение лидокаина следует осуществлять с осторожностью пациентам с миастенией gravis, эпилепсией, хронической сердечной недостаточностью, брадикардией и угнетением дыхания, коагулопатией, полной или неполной блокадой внутрисердечного проведения, судорожными расстройствами, синдромом Мелькерссона-Розенталя, порфирией, а также в третий триместр беременности (см. раздел \"Особые указания\")."}}]},{"id":11,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","body":[{"type":"paragraph","data":{"text":"\u003ci\u003eФертильность\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Данные о влиянии лидокаина на фертильность человека отсутствуют."}},{"type":"paragraph","data":{"text":"\u003ci\u003eБеременность\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Лидокаин разрешается применять во время беременности и грудного вскармливания. Необходимо строго придерживаться назначенного режима дозирования. При осложнениях или кровотечении в анамнезе проведение эпидуральной анестезии лидокаином в акушер­стве противопоказано."}},{"type":"paragraph","data":{"text":"Лидокаин применяли у большого числа беременных женщин и женщин детородного воз­раста. Какие-либо репродуктивные нарушения не зарегистрированы, т.е. повышения ча­стоты пороков развития не отмечалось."}},{"type":"paragraph","data":{"text":"Вследствие потенциального достижения высокой концентрации местных анестетиков у плода после парацервикальной блокады у него могут развиться нежелательные реакции, такие как фетальная брадикардия. В связи с этим лидокаин в концентрации, превышаю­щей 1%, в акушерстве не применяют. В исследованиях на животных вредное воздействие на плод не обнаружено."}},{"type":"paragraph","data":{"text":"\u003ci\u003eГрудное вскармливание\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Лидокаин в небольшом количестве проникает в грудное молоко, его пероральная биодо­ступность очень низкая. Таким образом, ожидаемое количество, поступающее с грудным молоком, очень небольшое, следовательно, потенциальный вред для ребенка очень низ­кий. Решение о возможности применения лидокаина в период грудного скармливания принимает врач."}}]},{"id":12,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Режим дозирования устанавливают индивидуально, в зависимости от вида анестезии и места введения, размера анестезируемого участка, возраста пациента. Средство следует вводить в наименьшей концентрации и наименьшей дозе, дающей требуемый эффект."}},{"type":"paragraph","data":{"text":"Максимальная доза для взрослых не должна превышать 300 мг."}},{"type":"paragraph","data":{"text":"У взрослых, детей и подростков в возрасте 12-18 лет однократная доза лидокаина (за исключением спинальной анестезии) не должна превышать 4.5 мг/кг, при максимальной - 300 мг."}},{"type":"paragraph","data":{"text":"Детям, пожилым и ослабленным пациентам лидокаин вводят в меньших дозах, соответствующих их возрасту и физическому состоянию."}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Нежелательные реакции описаны в соответствии с системно-органными классами MedDRA. Частота определена следующим образом:"}},{"type":"paragraph","data":{"text":"Подобно другим местным анестетикам, нежелательные реакции на лидокаин редки и, как правило, обусловлены повышенной плазменной концентрацией вследствие случайного внутрисосудистого введения, превышения дозы или быстрой абсорбции из участков с обильным кровоснабжением, либо вследствие гиперчувствительности, идиосинкразии или сниженной переносимости пациента. Реакции системной токсичности, главным образом, проявляются со стороны центральной нервной и (или) сердечно-сосудистой системы (см. также раздел \"Передозировка\")."}},{"type":"paragraph","data":{"text":"\u003ci\u003eНарушения со стороны иммунной системы\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Реакции гиперчувствительности (аллергические или анафилактоидные реакции, анафи­лактический шок) - см. также нарушения со стороны кожи и подкожных тканей. Кожная аллергическая проба на лидокаин считается ненадежной."}},{"type":"paragraph","data":{"text":"\u003ci\u003eНарушения со стороны нервной системы и психические расстройства\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"К неврологическим признакам системной токсичности относятся головокружение, нервозность, тремор, парестезия вокруг рта, онемение языка, сонливость, судороги, кома. Реакции со стороны нервной системы могут проявляться се возбуждением или угнетени­ем. Признаки стимуляции ЦНС могут быть непродолжительными или не возникать вовсе, вследствие чего первыми проявлениями токсичности могут служить спутанность сознания и сонливость, сменяющиеся комой и дыхательной недостаточностью. К неврологическим осложнениям спинальной анестезии относятся преходящие невроло­гические симптомы, такие как боль в пояснице, ягодицах и ногах. Эти симптомы развива­ются, как правило, в течение 24 часов после анестезии и разрешаются в течение несколь­ких дней. После спинальной анестезии лидокаином и сходными средствами описаны от­дельные случаи арахноидита и синдрома конского хвоста со стойкой парестезией, дис­функцией кишечника и мочевыводящих путей или параличом нижних конечностей. Большинство случаев обусловлено гипербарической концентрацией лидокаина или дли­тельной спинальной инфузией."}},{"type":"paragraph","data":{"text":"\u003ci\u003eНарушения со стороны органа зрения\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Признаками лидокаиновой токсичности могут быть затуманенное зрение, диплопия и преходящий амавроз."}},{"type":"paragraph","data":{"text":"Двусторонний амавроз также может быть следствием случайного введения в ложе зри­тельного нерва в ходе офтальмологических процедур. После ретро- и перибульбарной анестезии сообщалось о воспалении глаза и диплопии (см. раздел \"Особые указания\")."}},{"type":"paragraph","data":{"text":"\u003ci\u003eНарушения со стороны органа слуха и лабиринта\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Шум в ушах, гиперакузия."}},{"type":"paragraph","data":{"text":"\u003ci\u003eНарушения со стороны сердечно-сосудистой системы\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Сердечно-сосудистые реакции проявляются артериальной гипотензией, брадикардией, угнетением миокарда (отрицательный инотропный эффект), аритмиями, возможны оста­новка сердца или недостаточность кровообращения."}},{"type":"paragraph","data":{"text":"\u003ci\u003eНарушения со стороны дыхательной системы, органов грудной клетки и средостения \u003c/i\u003eОдышка, бронхоспазм, угнетение дыхания, остановка дыхания."}},{"type":"paragraph","data":{"text":"\u003ci\u003eНарушения со стороны желудочно-кишечного тракта\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Тошнота, рвота."}},{"type":"paragraph","data":{"text":"\u003ci\u003eНарушения со стороны кожи и подкожных тканей\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Сыпь, крапивница, ангионевротический отек, отек лица."}}]},{"id":14,"name":"Передозировка","slug":"overdose","body":[{"type":"paragraph","data":{"text":"\u003ci\u003eСимптомы\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Токсичность со стороны центральной нервной системы проявляется симптомами, нарас­тающими по тяжести. Сначала может развиться парестезия вокруг рта, онемение языка, головокружение, гиперакузия и шум в ушах. Нарушение зрения и мышечный тремор или мышечные подергивания свидетельствуют о более серьезной токсичности и предшеству­ют генерализованным судорогам. Эти признаки не следует путать с невротическим пове­дением. Затем могут наступить потеря сознания и большие судорожные припадки про­должительностью от нескольких секунд до нескольких минут. Судороги приводят к быст­рому нарастанию гипоксии и гиперкапнии, обусловленных повышенной мышечной ак­тивностью и нарушением дыхания. В тяжелых случаях может развиться апноэ. Ацидоз усиливает токсические эффекты местных анестетиков."}},{"type":"paragraph","data":{"text":"В тяжелых случаях возникают нарушения со стороны сердечно-сосудистой системы. При высокой системной концентрации могут развиться артериальная гипотензия, брадикардия, аритмия и остановка сердца, которые могут оказаться летальными."}},{"type":"paragraph","data":{"text":"Разрешение передозировки происходит вследствие перераспределения местного анестети­ка из центральной нервной системы и его метаболизма, оно может протекать достаточно быстро (если не была введена очень большая доза препарата)."}},{"type":"paragraph","data":{"text":"\u003ci\u003eЛечение\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"При возникновении признаков передозировки введение анестетика следует немедленно прекратить."}},{"type":"paragraph","data":{"text":"Судороги, угнетение ЦНС и кардиотоксичность требуют медицинского вмешательства. Главные цели терапии заключаются в поддержании оксигенации, прекращении судорог,"}},{"type":"paragraph","data":{"text":"поддержании кровообращения и купировании ацидоза (в случае его развития). В соответ­ствующих случаях необходимо обеспечить проходимость дыхательных путей и назначить кислород, а также наладить вспомогательную вентиляцию легких (масочную или с помо­щью мешка Амбу). Поддержание кровообращения осуществляется посредством вливания плазмы или инфузионных растворов. При необходимости длительного поддержания кро­вообращения следует рассмотреть возможность введения вазопрессоров, однако они по­вышают риск возбуждения ЦНС. Контроль судорог можно достичь посредством внутри­венного введения диазепама (0,1 мг/кг) или тиопентана натрия (1-3 мг/кг), при этом следу­ет учитывать, что противосудорожные средства могу т также угнетать дыхание и кровооб­ращение. Продолжительные судороги могут препятствовать вентиляции легких и оксигенации пациента, в связи с чем следует рассмотреть возможность ранней эндотрахеальной интубации. При остановке сердца приступают к стандартной сердечно-легочной реанимации."}},{"type":"paragraph","data":{"text":"Эффективность диализа при лечении острой передозировки лидокаином очень низкая."}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"Токсичность лидокаина увеличивается при его одновременном применении с циметидином и пропранололом вследствие повышения концентрации лидокаина, это требует снижения дозы лидокаина. Оба препарата снижают печеночный кровоток. Кроме того, циметидин ингибирует микросомальную активность. Ранитидин незначительно снижает клиренс лидокаина, что приводит к повышению его концентрации. Повышение сывороточной концентрации лидокаина также могут вызывать противовирусные средства (например, ампренавир, атазанавир, дарунавир, лопинавир)."}},{"type":"paragraph","data":{"text":"Гипокалиемия, вызываемая диуретиками, может снижать действие лидокаина при их одновременном применении (см. раздел \"Особые указания\")."}},{"type":"paragraph","data":{"text":"Лидокаин следует с осторожностью применять у пациентов, получающих другие местные анестетики или средства, структурно сходные с местными анестетиками амидного типа (например, антиаритмиками, такими как мексилетин, токаинид), поскольку системные токсические эффекты носят аддитивный характер. Отдельные исследования лекарственного взаимодействия между лидокаином и антиаритмиками III класса (например, амиодароном) не проводились, однако рекомендуется соблюдать осторожность. У пациентов, одновременно получающих антипсихотические средства, удлиняющие или способные удлинять интервал QT (например, пимозид, сертиндол, оланзаиин, кветиапин, зотепин), прениламин, эпинефрин (при случайном внутривенном введении) или антагонисты 5-НТЗ-серотониновых рецепторов (например, трописетрон, доласетрон), может повышаться риск желудочковых аритмий."}},{"type":"paragraph","data":{"text":"Одновременное применение хинупристина/далфопристина может увеличивать концентрацию лидокаина и повышать, таким образом, риск желудочковых аритмий; их одновременного применения следует избегать."}},{"type":"paragraph","data":{"text":"У пациентов, одновременно получающих миорелаксанты (например, суксаметоний), может повышаться риск усиленной и пролонгированной нервно-мышечной блокады. После применения бупивакаииа у пациентов, получавших верапамил и тимолол, сообщалось о развитии сердечно-сосудистой недостаточности; лидокаин близок по структуре к бупивакаину."}},{"type":"paragraph","data":{"text":"Допамин и 5-гидрокситриптамии снижают порог судорожной готовности к лидокаину. Опиоиды, вероятно, обладают просудорожным действием, что подтверждается данными, что лидокаин снижает судорожный порог к фентанилу у человека."}},{"type":"paragraph","data":{"text":"Комбинация опиоидов и противорвотных средств, иногда применяемая в целях седации у детей, может снизить судорожный порог к лидокаину и повысить его угнетающее действие на ЦНС."}},{"type":"paragraph","data":{"text":"Применение эпинефрина вместе с лидокаином может снизить системную абсорбцию, но при случайном внутривенном введении резко возрастает риск желудочковой тахикардии и фибрилляции желудочков."}},{"type":"paragraph","data":{"text":"Одновременное применение прочих антиаритмиков, β-адреноблокаторов и блокаторов \"медленных\" кальциевых каналов может дополнительно снижать AV-проведение, проведение по желудочкам и сократимость."}},{"type":"paragraph","data":{"text":"Одновременное применение сосудосуживающих средств увеличивает длительность действия лидокаина."}},{"type":"paragraph","data":{"text":"Одновременное применение лидокаина и алкалоидов спорыньи (например, эрготамина) может вызвать тяжелую артериальную гипотензию."}},{"type":"paragraph","data":{"text":"Необходимо соблюдать осторожность при применении седативных средств, поскольку они могут повлиять на действие местных анестетиков на ЦНС."}},{"type":"paragraph","data":{"text":"Следует соблюдать осторожность при длительном применении противоэпилептических средств (фенитоин), барбитуратов и других ингибиторов микросомальных ферментов печени, поскольку это может привести к снижению эффективности и, как следствие, повышенной потребности в лидокаине."}},{"type":"paragraph","data":{"text":"С другой стороны, внутривенное введение фенитоина может усилить угнетающее действие лидокаина на сердце."}},{"type":"paragraph","data":{"text":"Анальгезирующий эффект местных анестетиков может усиливаться опиоидами и клонидипом."}},{"type":"paragraph","data":{"text":"Этиловый спирт, особенно при длительном злоупотреблении, может снижать действие местных анестетиков."}},{"type":"paragraph","data":{"text":"Лидокаин несовместим с амфотерицином В, метогекситоном и нитроглицерином. Смешивать лидокаин с другими лекарственными препаратами не рекомендуется."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"Регионарная и местная анестезия должна проводиться опытными специалистами в соответствующем образом оборудованном помещении при доступности готового к немедленному использованию оборудования и препаратов, необходимых для проведения мониторинга сердечной деятельности и реанимационных мероприятий. Персонал, выполняющий анестезию, должен быть квалифицированным и обучен технике выполнения анестезии, должен быть знаком с диагностикой и лечением системных токсических реакций, нежелательных явлений и реакций и других осложнений."}},{"type":"paragraph","data":{"text":"Его следует с осторожностью применять у пациентов с миастенией gravis, эпилепсией, хронической сердечной недостаточностью, брадикардией и угнетением дыхания, а также в комбинации с препаратами, взаимодействующими с лидокаином и приводящими к повышению его биодоступности, потенцированию эффектов (например, фенитоином) или удлинению выведения (например, при печеночной или терминальной почечной недостаточности, при которой могут кумулировать метаболиты лидокаина). За пациентами, получающими антиаритмические препараты III класса (например, амиодарон) необходимо установить тщательное наблюдение и ЭКГ-мониторинг, поскольку влияние на сердце может потенцироваться."}},{"type":"paragraph","data":{"text":"Поступали пострегистрационные сообщения о хондролизе у пациентов, которым осуществляли длительную внутрисуставную инфузию местных анестетиков после операции. В большинстве случаев хондролиз отмечался в плечевом суставе. Вследствие множества вносящих вклад факторов и противоречивости научной литературы относительно механизма реализации эффекта, причинно-следственная связь не выявлена. Длительная внутрисуставная инфузия не является разрешенным показанием к применению лидокаина. Внутримышечное введение лидокаина может повышать активность креатинфосфокиназы, что может затруднить диагностику острого инфаркта миокарда."}},{"type":"paragraph","data":{"text":"Показано, что лидокаин может вызывать порфирию у животных, его применения у лиц с порфирией следует избегать."}},{"type":"paragraph","data":{"text":"При введении в воспаленные или инфицированные ткани эффект лидокаина может снижаться."}},{"type":"paragraph","data":{"text":"Перед началом внутривенного введения лидокаина необходимо устранить гипокалиемию, гипоксию и нарушение кислотно-основного состояния."}},{"type":"paragraph","data":{"text":"Некоторые процедуры местной анестезии могут приводить к серьезным нежелательным реакциям, независимо от применяемого местного анестетика."}},{"type":"paragraph","data":{"text":"Проводниковая анестезия спинномозговых нервов может приводить к угнетению сердечно-сосудистой системы, особенно на фоне гиповолемии, поэтому при проведении эиидуральной анестезии пациентам с сердечно-сосудистыми нарушениями следует соблюдать осторожность."}},{"type":"paragraph","data":{"text":"Эпидуральная анестезия может приводить к артериальной гипотензии и брадикардии. Риск можно снизить предварительным введением кристаллоидных или коллоидных растворов. Необходимо немедленно купировать артериальную гииотензию. В некоторых случаях парацервикальная блокада при беременности может приводить к брадикардии или тахикардии у плода, в связи с чем требуется тщательный мониторинг частоты сердцебиения у плода (см. раздел \"Применение во время беременности и в период грудного вскармливания\")."}},{"type":"paragraph","data":{"text":"Введение в область головы и шеи может привести к непреднамеренному попаданию в артерию с развитием церебральной симптоматики даже в низких дозах. Ретробульбарное введение в редких случаях может приводить к попаданию в субарахноидальное пространство черепа, приводя к серьезным/тяжелым реакциям, включая сердечно-сосудистую недостаточность, апноэ, судороги и временную слепоту. Ретро- и перибульбарное введение местных анестетиков несет низкий риск стойкой глазодвигательной дисфункции. К основным причинам относят травму и (или) местное токсическое действие на мышцы и (или) нервы."}},{"type":"paragraph","data":{"text":"Тяжесть подобных реакций зависит от степени травмы, концентрации местного анестетика и продолжительности его экспозиции в тканях. В связи с этим любой местный анестетик необходимо применять в наименьшей эффективной концентрации и дозе. Раствор для инъекций лидокаина не рекомендуется применять у новорожденных. Оптимальная сывороточная концентрация лидокаина, позволяющая избежать такой токсичности как судороги и аритмии, у новорожденных не установлена. Следует избегать внутрисосудистого введения, если таковое напрямую не показано."}},{"type":"paragraph","data":{"text":"\u003ci\u003eПрименение с осторожностью:\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"- у пациентов с коагулопатией. Терапия антикоагулянтами (например, гепарином), НПВП или плазмозаменителями повышает склонность к кровотечениям. Случайное повреждение сосудов может привести к тяжелым кровотечениям. При необходимости следует проверить время кровотечения, активированное частичное тромбопластиновое время (АЧТВ) и содержание тромбоцитов;"}},{"type":"paragraph","data":{"text":"- пациенты с полной или неполной блокадой внутрисердечного проведения, поскольку местные анестетики могут угнетать AV-проведепие;"}},{"type":"paragraph","data":{"text":"- необходимо тщательно наблюдать за пациентами с судорожными расстройствами на предмет симптоматики со стороны ЦНС. Низкие дозы лидокаина также могут повышать судорожную готовность. У пациентов с синдромом Мелькерссона-Розенталя аллергические и токсические реакции со стороны нервной системы в ответ па введение местных анестетиков могут развиваться чаще;"}},{"type":"paragraph","data":{"text":"- третий триместр беременности."}},{"type":"paragraph","data":{"text":"Лидокаин, раствор для инъекций, 20 мг/мл, не разрешен для интратекального введения (субарахноидальной анестезии)."}}]},{"id":17,"name":"Влияние на способность управлять автомобилем и движущимися механизмами","slug":"","body":[{"type":"paragraph","data":{"text":"После введения местных анестетиков может отмечаться преходящее снижение чувствительности и (или) моторный блок. До разрешения этих эффектов пациентам не рекомендуется управлять транспортными средствами и работать с механизмами."}}]},{"id":18,"name":"Форма выпуска","slug":"","body":[{"type":"paragraph","data":{"text":"Раствор для инъекций 20 мг/мл."}}]},{"id":19,"name":"Условия хранения","slug":"storage","body":[{"type":"paragraph","data":{"text":"Хранить в защищенном от света месте при температуре не выше 25 °С. 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 использовать но истечении срока годности, указанного на упаковке."}}]},{"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":"Республиканское унитарное производственное предприятие \"Белмедпрепараты\" (РУП \"Белмедпрепараты\"), 220007, Республика Беларусь, г. Минск, ул. Фабрициуса, д. 30, Республика Беларусь"}}]},{"id":23,"name":"Организация, принимающая претензии потребителей","body":[{"type":"paragraph","data":{"text":"РУП \"Белмедпрепараты\""}}]}],"source":null},"description_toggle":false,"short_description":"Лидокаин является короткодействующим местным анестетиком амидного типа. В основе его механизма действия лежит уменьшение проницаемости мембраны нейрона для ионов натрия. В результате этого снижается скорость деполяризации и повышается порог возбуждения, приводя к обратимому местному онемению. Лидокаин применяют в целях достижения проводниковой анестезии в различных участках тела и контроля аритмий. Обладает быстрым началом действия (около одной минуты после внутривенного введения и пятнадцати минут после внутримышечного), быстро распространяется в окружающие ткани. Действие продолжается 10-20 минут и около 60-90 минут после внутривенного и внутримышечного введения соответственно.АбсорбцияЛидокаин быстро абсорбируется из желудочно-кишечного тракта, однако вследствие эф­фекта \"первичного прохождения\" через печень лишь небольшое его количество достигает системного кровотока. Системная абсорбция лидокаина определяется местом введения, дозой и его фармаколо­гическим профилем. Максимальная концентрация в крови достигается после межреберной блокады, далее (в порядке снижения концентрации), после введения в поясничное эпидуральнос пространство, плечевое сплетение и подкожные ткани. Основным фактором, определяющим скорость абсорбции и концентрацию в крови, является общая введенная доза, независимо от участка введения. Имеется линейная зависимость между количеством введенного лидокаина и результирующей максимальной концентрацией анестетика в кро­ви.РаспределениеЛидокаин связывается с белками плазмы, включая α1-кислый гликопротеин (АКГ) и аль­бумин. Степень связывания вариабельна, составляя приблизительно 66%. Плазменная концентрация АКГ у новорожденных низкая, поэтому у них отмечается относительно вы­сокое содержание свободной биологически активной фракции лидокаина. Лидокаин проникает через гематоэнцефалический и плацентарный барьеры, вероятно, по­средством пассивной диффузии.МетаболизмЛидокаин метаболизируется в печени, около 90% введенной дозы подвергается N- дезалкилированию с образованием моноэтилглицинксилидида (MEGX) и глицинксилидида (GX), оба вносят вклад в терапевтические и токсические эффекты лидокаина. Фар­макологические и токсические эффекты MEGX и GX сопоставимы с таковыми лидокаина, но выражены слабее. GX обладает более длинным, чем лидокаин, периодом полувыведе­ния (около 10 часов) и может кумулировать при многократном введении. Метаболиты, образующиеся в результате последующего метаболизма, выводятся с мочой, содержание неизменного лидокаина в моче не превышает 10%.ВыведениеТерминальный период полувыведения лидокаина после внутривенного болюсного введе­ния здоровым взрослым добровольцам составляет 1-2 часа. Терминальный период полувыведения GX составляет около 10 часов, MEGX - 2 часа.Особые группы пациентовВследствие быстрого метаболизма на фармакокинетику лидокаина могут оказывать влия­ние состояния, нарушающие функцию печени. У пациентов с печеночной дисфункцией период полувыведения лидокаина может повышаться в 2 и более раз. Нарушение функции почек не влияет на фармакокинетику лидокаина, но может приво­дить к кумуляции его метаболитов. У новорожденных отмечается низкая концентрация АКГ, поэтому связь с белками плазмы может снижаться. Вследствие потенциально высокой концентрации свободной фракции применение лидокаина у новорожденных не рекомендуется.","substance":[{"id":542,"title":"Лидокаин","title_latin":"Lidocainum","slug":"lidokain_542"}],"branding":null,"valid_for_quick_buy":false,"is_available_to_delivery":false,"comments":null,"image_alt":"ЛИДОКАИН - фото упаковки","image_share":{"isTouch":{"default":"https://vseapteki.ru/cropping/thumbnails/101/204337/share_default/"},"isFromTablet":{"default":"https://vseapteki.ru/cropping/thumbnails/101/204337/share_default/"}},"diseases":[],"other_packages":[],"other_product_forms":[{"id":96396,"title":"Лидокаин","subtitle":{"full":"Спрей, аэрозоль, 50 мл, 38 г, для местного применения","short":"Спрей, 50 мл, 38 г","package":"50 мл, 38 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