Описание
Овастат — противоопухолевое средство с действующим веществом — Треосульфан. Он относится к двухфункциональным алкилирующим соединениям и является водорастворимым структурным аналогом бусульфана. В физиологических условиях in vitro (рН 7,4; t = 37 °C) превращается неферментативным путем в алкилирующие два метаболита: моно- и диэпоксид (диэпоксидбутан) с периодом полураспада 2,2 часа, которые отвечают за цитотоксическое воздействие против ряда сóлидных опухолей, Т и В лимфоцитов, гемопоэтических стволовых клеток и гемопоэтических опухолей. Эпоксиды ответственны за противоопухолевый эффект через вторичные биологические механизмы и обладают способностью к алкилированию нуклеофильного центра ДНК.
Сформировавшись in vivo моноэпоксид уже компетентен алкилировать нуклеофильный центр ДНК. Еще до того, как сформируется второе эпоксидное кольцо, путем химического процесса это соединение прикрепляется к нуклеофильному центру ДНК.
В неактивной фазе он преобразуется в алкилирующие 2 метаболита – моно и диэпоксибутан. Они способны оказывать подавляющее влияние на гемопоэтические стволовые клетки раковых опухолей. Препарат Овастат назначается для лечения гемопоэтических опухолей, а также T и B лимфоцитов и против ряда сóлидных опухолей.
Треосульфан — это новый, экспериментальный противоопухолевый цитостатический химиотерапевтический препарат из группы алкилирующих средств. В данное время он дополнительно исследуется в качестве средства лечения различных видов злокачественных образований, в частности меланомы радужки глаза, как в в монотерапии, так и в сочетании с гемцитабином. Треосульфан используется в основном как заменитель бусульфана у сильно ослабленных больных, поскольку его токсичность (в частности гематотоксичность) и другие побочные эффекты, существенно меньше, чем у бусульфана.
Показания препарата
- при лечении всех форм рака яичников в паллиативном режиме или в дополнение к хирургическому вмешательству, как в режиме монотерапии, так и в комбинации с другими противоопухолевыми препаратами;
- может быть использован при любых новообразованиях, устойчивых к общепринятой химиотерапии.
Состав
треосульфан 1 г
вспомогательные вещества: нет
Фармакодинамика
Треосульфан является предшественником бифункционального алкилирующего цитотоксического агента диэпоксибутана. При физиологических условиях (рН=7,4; t = 37 °C) фармакологически неактивный треосульфан с периодом полураспада 2,2 часа превращается (неферментативным путем) в алкилирующие два активных метаболита — моно- и диэпоксибутан. Метаболиты обладают способностью алкилировать нуклеофильные центры ДНK. Активные метаболиты треосульфана специфически проявляют угнетающее воздействие на лимфоциты Т и В, гемопоэтические стволовые клетки, а также оказывают цитотоксическое действие на ряд гемопоэтических и сóлидных опухолей.
Эпоксиды характеризуются способностью к алкилированию нуклеофильного центра ДНК и ответственны за противоопухолевый эффект через вторичные биологические процессы. Имеет большое значение то, что in vivo моноэпоксид, сформировавшись, способен алкилировать нуклеофильный центр ДНК. Еще до того, как сформируется второе эпоксидное кольцо, путем химического процесса это соединение прикрепляется к нуклеофильному центру ДНК.
Фармакокинетика
При внутривенном введении для треосульфана характерно быстрое распределение с последующей экскрецией в соответствии с кинетикой первого порядка и периодом полураспада, который составляет около 88 минут. Приблизительно 22 процента введенной дозы выделяется в неизмененном виде с мочой в течение 24 часов, около 90 процентов от этого количества — в течение первых 6 часов после введения.
Применение при беременности и детям
Внимание! Данных о применении треосульфана у беременных и при грудном вскармливании нет. Исходя из того, что треосульфан потенциально способен повреждать плод и то, есть вероятность его проникновение в грудное молоко. Препарат не должен назначаться при грудном вскармливании и во время беременности. Пациентам детородного возраста в период лечения и после окончания терапии треосульфаном в течении трех месяцев следует применять контрацепцию. В случае наступлении беременности в период лечения треосульфаном в обязательном порядке должна быть проведена генетическая экспертиза.
Фармацевтические характеристики
Белый кристаллический порошок для приготовления раствора для инфузий.
Упаковка, срок годности, условия хранения
Порошок для приготовления раствора для инфузий — 1 флакон. Упакован бесцветные стеклянные флаконы вместимостью 100 мл, закупоренных пробкой из резины, с алюминиевой обкаткой и пластиковой защитной крышкой. В каждом флаконе по 1 грамму; в пачке картонной 5 флаконов.
Препарат выпускается в виде капсул и порошка концентрацией 250 и 500 мг соответственно.
Капсулы 250 мг — 100 штук/действующее вещество без растворителя 5000 mg, в упаковке 1 штука.
Хранить в недоступном для детей, защищенном от света месте при температуре не выше 25 °С.
Срок годности препарата — 5 лет. Не использовать по истечении срока годности, указанного на упаковке.
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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