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Фармакотерапевтическая группа
Противоаллергическое средство - H1-гистаминовых рецепторов блокатор.
Фармакологические свойства
Всасывание. После приема внутрь фексофенадин быстро всасывается из желудочно-кишечного тракта (ЖКТ), время достижения максимальной концентрации (Тmах) в плазме составляет приблизительно 1-3 ч. После приема внутрь дозы 60 мг один раз в день среднее значение максимальной концентрации (Сmах) составляет приблизительно 142 нг/мл, дозы 120 мг один раз в день - приблизительно 289 нг/мл, а после приема внутрь дозы 180 мг один раз в день - приблизительно 494 нг/мл.
Метаболизм, распределение и выведение. Связывание с белками плазмы составляет 60-70%. Метаболизируется примерно 5% принятой дозы. 80% и 11% принятой дозы выводится с желчью и мочой соответственно. Период полувыведения (Т1/2) после многократного приема составляет 11-16 ч. 10% дозы выводится почками в неизмененном виде.
Фармакокинетика фексофенадина при приеме препарата внутрь однократной или многократной дозы от 20 мг до 120 мг носит линейный характер. После приема препарата внутрь в дозе 240 мг 2 раза/сут наблюдается пропорциональное увеличение площади под фармакокинетической кривой (AUC) (8,8%).
Фексофенадин является специфическим антагонистом гистаминовых H1-рецепторов. Фексофенадин в терапевтических дозах не обладает антихолинергической, антиадренергической или антидопаминергической активностью. Даже в высоких дозах фексофенадин не блокирует каналы калия в миокардиоцитах, таким образом, не обладает кардиотоксическим эффектом (пролонгирование QT-интервала, аритмии). Фексофенадин не проходит через гематоэнцефалический барьер и, следовательно, не взаимодействует с H1-рецепторами центральной нервной системы (ЦНС).
Клинические испытания, проведенные на взрослых пациентах с сезонным аллергическим ринитом, показали, что прием препарата в дозе 60, 120, 180 мг вызывал быстрое симптоматическое улучшение в течение 1 ч, эффект сохранялся в течение 24 ч.
Показания к применению
180 мг: хроническая крапивница: покраснение, кожный зуд и другие симптомы крапивницы.
Противопоказания
Повышенная чувствительность к компонентам препарата.
Симптомы: головокружение, сонливость, сухость во рту.
Лечение: проведение стандартных мер по удалению из ЖКТ неабсорбированного препарата. Симптоматическая и поддерживающая терапия. Гемодиализ неэффективен.
Взаимодействие с другими лекарственными средствами
Антациды могут влиять на эффективность фексофенадина. Рекомендуемый интервал времени между приемом фексофенадина и антацидов, содержащих гидроксид алюминия или магния, составляет 2 ч.
При одновременном приеме фексофенадина с эритромицином или кетоконазолом возможно увеличение концентрации фексофенадина в плазме в 2-3 раза (не ассоциируется со значимым удлинением интервала QT).
Не взаимодействует с омепразолом, с лекарственными средствами, метаболизирующимися в печени.
Особые указания
Исследования, проведенные у пожилых пациентов, у пациентов с нарушениями функций почек и печени показали отсутствие необходимости в коррекции дозы препарата.
Влияние на способность к вождению автотранспорта и управлению механизмами
При проведении объективных испытаний было показано, что фексофенадин не оказывает существенного воздействия на функции ЦНС. Тем не менее, для того чтобы выявить чувствительных больных, обладающих нестандартной реакцией на лекарственное средство, рекомендуется проверить индивидуальную реакцию перед тем, как приступить к работе, требующей концентрации внимания.
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