Блокатор гистаминовых H1-рецепторов длительного действия. Обладает противоаллергическим, противозудным, противоэкссудативным действием. Предупреждает развитие и облегчает течение аллергических реакций.
Подавляет высвобождение гистамина и лейкотриена С4 из тучных клеток. Уменьшает проницаемость капилляров, предупреждает развитие отека тканей, снимает спазмы гладкой мускулатуры.
Не влияет на ЦНС (т.к. не проникает через ГЭБ) и не вызывает привыкания.
Противоаллергический эффект развивается через 30 мин, достигает максимума через 8-12 ч и длится 24 ч.
Фармакокинетика
Всасывание и распределение
Быстро и полностью всасывается их ЖКТ. Время достижения Cmax в плазме крови после приема препарата - 1.3-2.5 ч; прием пищи замедляет время достижения Cmax на 1 ч.
Связывание с белками плазмы - 97%. Css лоратадина и метаболита в плазме достигаются на 5 сут введения. Не проникает через ГЭБ.
Метаболизм и выведение
Метаболизируется в печени с образованием активного метаболита дезкарбоэтоксилоратадина при участии изоферментов CYP3A4 и в меньшей степени CYP2D6.
Выводится почками и с желчью. Т1/2 лоратадина - 3-20 ч (в среднем 8.4 ч), активного метаболита - 8.8-92 ч (в среднем 28 ч).
Фармакокинетика у особых групп пациентов
Cmax препарата в плазме крови у пожилых людей возрастает на 50%. Т1/2 лоратадина и активного метаболита у пожилых пациентов соответственно - 6.7-37 ч (в среднем 18.2 ч) и 11-38 ч (17.5 ч).
При алкогольном поражении печени Cmax и Т1/2 увеличиваются пропорционально тяжести заболевания.
У пациентов с хронической почечной недостаточностью и при проведении гемодиализа фармакокинетика практически не меняется.
Показания к применению
сезонный и круглогодичный ринит (в т.ч. поллиноз);
непереносимость лактозы, дефицит лактазы, синдром мальабсорбции глюкозы-галактозы (для таблеток);
повышенная чувствительность к любому из компонентов препарата.
С осторожностью
Следует назначать препарат при печеночной недостаточности, беременности.
Применение при беременности и в период грудного вскармливания
Применение препарата при беременности возможно только в тех случаях, когда предполагаемая польза для матери превышает потенциальный риск для плода.
На время лечения следует прекратить грудное вскармливание (выделяется с грудным молоком).
Способ применения и дозы
Препарат принимают внутрь.
Взрослым и Детям с массой тела более 30 кг назначают по 10 мг (1 таб. или 2 мерные ложки сиропа) 1 раз/сут.
Детям в возрасте от 2 до 12 лет с массой тела менее 30 кг назначают по 5 мг (1 мерная ложка сиропа) 1 раз/сут.
При почечной недостаточности начальная доза составляет 10 мг через день.
При печеночной недостаточности начальная доза препарата составляет 5 мг/сут или 10 мг через день.
Побочное действие
Нежелательные явления встречались приблизительно с той же частотой, что и при применении плацебо.
У взрослых: головная боль, повышенная утомляемость, сухость во рту, сонливость, тошнота, гастрит, аллергические реакции (сыпь), анафилаксия, алопеция, нарушение функции печени, тахикардия.
У детей: головная боль, повышенная нервная возбудимость, седативный эффект.
Передозировка
Симптомы: сонливость, тахикардия, головная боль.
Лечение: промывание желудка, прием активированного угля. Не выводится с помощью гемодиализа.
Взаимодействие с другими лекарственными средствами
Ингибиторы CYP3A4 (в т.ч. эритромицин, кетоконазол) ингибиторы CYP3A4 и CYP2D6 (циметидин и другие) при совместном применении с лоратадином увеличивают концентрацию лоратадина в плазме крови, не вызывая клинических проявлений и не оказывая влияния на данные ЭКГ.
Влияние на способность управлять автомобилем и движущимися механизмами
В период лечения необходимо соблюдать осторожность при вождении автотранспорта и занятии другими потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций.
Форма выпуска
Таблетки.
Условия хранения
Препарат в форме таблеток следует хранить в сухом, недоступном для детей месте при температуре не выше 25°С; срок годности – 5 лет.
Условия отпуска
Препарат разрешен к применению в качестве средства безрецептурного отпуска.
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Время достижения C\u003csub\u003emax\u003c/sub\u003e в плазме крови после приема препарата - 1.3-2.5 ч; прием пищи замедляет время достижения C\u003csub\u003emax\u003c/sub\u003e на 1 ч."}},{"type":"paragraph","data":{"text":"Связывание с белками плазмы - 97%. C\u003csub\u003ess\u003c/sub\u003e лоратадина и метаболита в плазме достигаются на 5 сут введения. Не проникает через ГЭБ."}},{"type":"paragraph","data":{"text":"\u003ci\u003eМетаболизм и выведение\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Метаболизируется в печени с образованием активного метаболита дезкарбоэтоксилоратадина при участии изоферментов CYP3A4 и в меньшей степени CYP2D6."}},{"type":"paragraph","data":{"text":"Выводится почками и с желчью. 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