Описание
Элигард (Eligard) — гормональный препарат, который назначают при лечении гормонозависимой опухоли предстательной железы. Активным веществом является Лейпрорелин — это непептидный искусственный аналог натурального гонадотропин-рилизинг-фактора.
Элигард — инъекционная суспензия, стимулирующая выработку определенных гормонов в организме, что в результате снижает количество тестостерона у мужчин. В отличие от естественного гормона, препарат действует эффективнее. Воздействие препарата на организм обратимо после прекращения терапии. Препарат противопоказан к использованию женщинам и детям.
Состав
- Один шприц А — растворитель, состоящий из
- сополимера поли-D,L-лактид-ко-гликолид
- N-метил-2-пирролидона
- Один шприц Б — основное вещество, содержит 7,5; 22,5 или 45 мг лейпрорелина ацетата.
Показания к применению
- Лечение гормонозависимого рака предстательной железы
- Эндометриоза и с целью регрессии внутриматочных патологических изменений и для уменьшения болевого синдрома).
Фармакодинамика
Лейпрорелин является синтетическим непептидным аналогом естественного гонадотропин-рилизинг-гормона (ГнРГ), превосходящий по активности естественный гормон. В начале использования лейпрорелина идет повышение секреции гонадотропных гормонов гипофиза. При длительном использовании Лейпрорелин ингибирует секрецию гипофизарного гонадотропина и подавляет тестикулярный стероидогенез у мужчин. При систематическом применении лейпрорелина возникает десенситизация рецепторов и уменьшение секреции гонадотропинов и половых гормонов. Это обратимый эффект, и после прекращения терапии физиологическая секреция гормонов восстанавливается. У мужчин, в течение 3-5 недель после начала лечения, уровень тестостерона снижается до кастрационного уровня (≤ 50 нг/дл). Средний уровень тестостерона через 6 месяцев лечения составляет 6,1 (± 0,4) нг/дл для дозировки 7,5 мг; 10,1 (± 0,7) нг/дл для дозировки 22,5 мг и 10,4 (± 0,53) нг/дл для дозировки 45 мг.
Пациенты, принимавшие участие в базовом клиническом исследовании препарата Элигард
- при приеме в дозе 7,5 мг, достигли кастрационного уровня тестостерона на 6-й неделе; 94% достигли этого уровня к 28 дню и 98% к 35 дню. Уровни тестостерона достигали значения ниже 20 нг/дл. Уровень ПСА снизился на 94% в течение шести месяцев.
- при приеме лейпрорелина в дозе 22,5 мг в клиническом исследовании, достигли кастрационного уровня на 5-й неделе; 99% достигли этого уровня к 28 дню.Уровень тестостерона — ниже 20 нг/дл. Уровень ПСА снизился на 98% в течение шести месяцев.
- при приеме лейпрорелина в дозе 45 мг в базовом исследовании, достигли кастрационного уровня на 4-й неделе. У большинства пациентов уровни тестостерона были ниже 20 нг/дл. Уровень ПСА снизился на 97% в течение шести месяцев.
Долгосрочные наблюдения показали, что постоянная терапия удерживает концентрацию тестостерона ниже кастрационного уровня на протяжении до 7 лет и далее на неопределенный срок.
Фармакокинетика
После первой инъекции через 4-8 часов средний уровень концентрации лейпрорелина, определяемой в сыворотке крови, при применении лейпрорелина в дозе 7,5 мг, 22,5 мг и 45 мг повышается до 25,3 нг/дл, 127 нг/дл и 82 нг/дл соответственно.
После первоначального повышения (фаза плато составляет 2 -28 дней для дозировки 7,5 мг; 3 -84 дней для дозировки 22,5 мг, 3 -168 дней для 45 мг) уровень лейпрорелина в сыворотке был относительно стабильным (0,28-1,67 нг/мл для дозировки 7,5 мг и 0,2-2 нг/мл для дозировок 22,5 и 45 мг). Данные о накоплении вещества при повторных инъекциях отсутствуют.
В равновесном состоянии средний объем распределения лейпрорелина, после однократного введения, у здоровых добровольцев составлял 27 литров. Связывание с белками плазмы крови человека в лабораторных условиях колебалось в пределах от 43% до 49%.
При введении 1 мг лейпрорелина ацетата внутривенно здоровым добровольцам мужчинам выяснилось, что при применении двухкамерной модели средний клиренс составил 8,34 л/ч с конечным периодом полувыведения приблизительно 3 часа.
Исследования по выведению препарата Элигард не проводились.
Исследования по лекарственному метаболизму препарата Элигард не проводились.
Фармацевтические характеристики
Один шприц Б — основное вещество, содержит 7,5; 22,5 или 45 мг лейпрорелина ацетата
- Дозировка 7,5 мг: От светло-желтой до светло-желтого с коричневатым оттенком прозрачная, вязкая жидкость, без видимых посторонних частиц. Допускается наличие пузырьков воздуха.
- Дозировки 22,5 мг и 45 мг: От бесцветной до светло-желтой, прозрачная, вязкая жидкость, без видимых посторонних частиц. Допускается наличие пузырьков воздуха.
Упаковка, срок годности, условия хранения
Шприцы упакованы в ячейковую упаковке из полиэфира, покрытого ламинированной алюминиевой фольгой. По одному шприцу А (в комплекте с поршнем и влагопоглотителем) и по одному шприцу Б (в комплекте с иглой инъекционной и влагопоглотителем) в ячейках упакованных в пачку картонную вместе с инструкцией по применению.
Хранить в оригинальной упаковке при температуре 2–8 °C.
Срок годности 2 года.
Наша компания работает как на территории Казахстана, так и осуществляет доставку в страны ближнего зарубежья. Обращайтесь к нам за консультациями по контактным телефонам.
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