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Тизабри — Tysabri (Натализумаб)

Тизабри

Тизабри — Tysabri (Натализумаб)

Препарат Тизабри, с основным действующим веществом — Натализумаб, оказывает селективное влияние на иммунную систему. Препарат Тизабри — это моноклональное антитело — селективный ингибитор молекул адгезии, снижающий воспалительную активность в пораженных тканях и дальнейшее привлечение иммунных клеток к очагу воспаления, что уменьшает или замедляет повышение объема поражения головного мозга.

На данный момент в реальной клинической практике имеется более чем десятилетний опыт эксплуатации препарата Тизабри. В выборочном, двойном слепом, плацебо-контролируемом эксперименте было обнаружено, что терапия Тизабри позволяет снизить частоту обострений на 68 процентов, а риск прогрессирования инвалидизации на 42 процента. Использование препарата позволяет достигнуть долговременного управления над заболеванием и в некоторых случаях восстановить утраченные функции. На фоне терапии препаратом Тизабри существует риск развития ПМЛ, частота которой составляет 4,08 на 1000 случаев.

Категория:

Описание

Препарат Тизабри, с основным действующим веществом — Натализумаб, оказывает селективное влияние на иммунную систему. Препарат Тизабри — это моноклональное антитело — селективный ингибитор молекул адгезии, снижающий воспалительную активность в пораженных тканях и дальнейшее привлечение иммунных клеток к очагу воспаления, что уменьшает или замедляет повышение объема поражения головного мозга.

На данный момент в реальной клинической практике имеется более чем десятилетний опыт эксплуатации препарата Тизабри. В выборочном, двойном слепом, плацебо-контролируемом эксперименте было обнаружено, что терапия Тизабри позволяет снизить частоту обострений на 68 процентов, а риск прогрессирования инвалидизации на 42 процента. Использование препарата позволяет достигнуть долговременного управления над заболеванием и в некоторых случаях восстановить утраченные функции. На фоне терапии препаратом Тизабри существует риск развития ПМЛ, частота которой составляет 4,08 на 1000 случаев.

Показания препарата Тизабри

Препарат Тизабри воздействует на хронические, вялотекущие, острые формы рассеянного склероза. Используется для монотерапии высокоактивных форм заболеваний, с осложнениями в форме ремитирующего рассеянного склероза. Для монотерапии ремиттирующей формы рассеянного склероза следующим группам больных:

  • пациентам с активным течением заболевания, не поддающемуся лечению полным и адекватным курсом (как минимум в течение одного года) интерферона бета, имеющим не менее одного рецидива в течение года терапии и не менее 9 Т2-гиперинтенсивных очагов на МРТ головного мозга или не менее одного очага, видимого при использовании МРТ с контрастным веществом. Под людьми «без ответа» на проводимое лечение подразумеваются пациенты с неизменной или повышенной частотой обострений в сравнении с предыдущим годом, либо с протекающими тяжелыми обострениями даже при терапии длительностью менее года;
  •  пациентам с резко прогрессирующим тяжелым ремиттирующим заболеванием. К данной категории относятся пациенты, перенесшие две или более количество обострений в течение года и/или имеющим один и/или более очагов поражения головного мозга на МРТ с контрастным веществом. Также к этой категории относятся пациенты, со значительным увеличением объема поражения головного мозга в режиме Т2 по сравнению с результатами предыдущей МРТ;
  • препарат также хорошо применяется для облегчения прогрессирующего заболевания, при применении бета-интерферона и его производных.

Состав Тизабри

1 мл концентрата содержит:

Активное вещество: Натализумаб 20,00 мг/мл;

Вспомогательные компоненты: Натрия дигидрофосфата моногидрат, натрия гидрофосфата гептагидрат, натрия хлорид, полисорбат, вода для инъекций.

Фармакодинамика Тизабри

Препарат Тизабри содержит натализумаб — селективный ингибитор молекул адгезии. Тизабри взаимодействует с α4-субъединицей человеческого интегрина, на поверхности всех лейкоцитов в большом количестве экспрессирующегося (за исключением нейтрофилов). Натализумаб специфически связывается с α4β1-интегрином, блокируя при этом взаимосвязь с идентичным рецептором, адгезивной молекулой клеток сосудов (VCAM-1) и лигандом остеопонтина, доменом фибронектина. Также, натализумаб ингибирует взаимодействие α4β7-интегрина с адрессином-1 (MadCAM-1) — молекулой адгезии слизистой оболочки. Воздействия на эти молекулярные влияния тормозит миграцию мононуклеарных лейкоцитов через эндотелий в очаги воспаления органов. Механизм дальнейшего действия препарата может быть связан ингибированием воспалительных процессов путем торможения взаимодействия α4-экспрессирующих лейкоцитов с их лигандами. Следовательно натализумаб может ингибировать в пораженных тканях воспалительную активность и тем самым подавлять дальнейший иммунный ответ к очагу воспаления.

При переходе активированных Т-лимфоцитов через гематоэнцефалический барьер (ГЭБ) происходит повреждение тканей головного мозга при рассеянном склерозе. Взаимодействие между молекулами адгезии на поверхности активированных лейкоцитов и эндотелием кровеносных сосудов включает в себя миграция лейкоцитов через ГЭБ. Важным компонентом патогенеза формирования очагов воспаления в головном мозге является взаимодействие между α4β1 и его мишенями, поэтому активность воспаления снижает нарушение этих взаимодействий. VCAM-1 не экспрессируется при нормальных условиях в паренхиме головного мозга. Однако в присутствии противоспалительных цитокинов возможно выработка VCAM-1 в клетках эндотелия и в глиальных клетках, находящихся вблизи очага воспаления, регулируется по механизму положительной обратной связи. В условиях воспаления ЦНС при PC взаимодействие α4β1 с VCAM-1, CS-1 и остеопонтином опосредует прочную адгезию и миграцию лейкоцитов в головном мозге. Следовательно, в тканях ЦНС усиливается воспалительная активность. при PC в паренхиме головного мозга воспалительную активность снижает блокада молекулярных взаимодействий α4β1 с его мишенями и подавляет дальнейшее привлечение иммунных клеток, тем самым замедляя увеличение или снижая образование объема поражения.

Фармакокинетика

После повторного внутривенного введения в дозировке 300 мг больным с рассеянным склерозом средняя максимальная сывороточная концентрация натализумаба была 110 ± 52 мкг/мл. В период введения средняя стационарная концентрация натализумаба варьировала от 23 до 29 мкг/мл. Прогнозируемое время достижения равновесной концентрации составляло приблизительно 36 недель.
Для фармакокинетического анализа выборка включала более 1100 больных с рассеянным склерозом, получавших натализумаб в дозировке от 3 до 6 мг/кг. Из них в качестве монотерапии 581 человек получали фиксированную дозировку 300 мг. Среднее ± SD (стандартное отклонение) время клиренса при стационарном состоянии составляло 13,1±5,0 мл/ч со средним ± SD временем полувыведения 16±4 дня. влияние выборочных переменных было исследовано при анализе на фармакокинетику, включая массу возраст, пол, тела, функцию почек и печени, а также наличие антител к натализумабу.На распределение препарата было показано, что влияют только антитела к натализумабу и масса тела. Выявлено, что на клиренс натализумаба влияет масса тела, при этом это влияние меньше пропорционального; например 43 процента изменения массы тела приводит к изменению клиренса на 31-34 процента. Изменения клиренса не имеют клинического значения. Примерно втрое повышают клиренс к натализумабу циркулирующие антитела к нему, что соответствует наблюдаемому у больных с циркулирующими антителами снижению концентрации натализумаба.

Для снижения концентрации натализумаба в крови проводились исследования с участием 12 пациентов с PC эффективности и фармакодинамики плазмафореза. После трех процедур плазмафереза результаты выведения препарата (с более чем 5-8 дневным интервалом) составляли примерно 70-80 процентов. Это сопоставимо с 40 процентами выявленных в предыдущем исследовании после отмены препарата за аналогичный период времени. На восстановление миграции лимфоцитов влияние плазмафереза и, в конечном счете, на клиническое использование неизвестно.

Повторное введение

Эффективность и безопасность препарата при повторном введении не определяли.

Применение при беременности и кормлении грудью

Данных о введении натализумаба беременным женщинам недостаточно. Исследования на животных показали репродуктивную токсичность. Возможный риск для людей неизвестен. Не рекомендуется применять натализумаб во время беременности без особой необходимости. Терапию следует прекратить, если пациентка забеременеет во время приема Тизабри.

Тизабри выделяется с грудным молоком. Пациентки, получающие Тизабри, должны прекратить кормление грудью.

Применение при нарушениях функции печени

Не проводилось исследований по оценке результатов препарата Тизабри при нарушении функции печени.

Результаты изучения фармакокинетики и способа элиминации позволяют допустить, что препарат Тизабри можно назначать пациентам с нарушением функции печени без изменения дозы.

Применение при нарушениях функции почек

Не проводилось исследований по оценке результатов препарата Тизабри при нарушении функции почек.

Результаты изучения фармакокинетики и способа элиминации позволяют допустить, что препарат Тизабри можно назначать пациентам с нарушением функций почек без изменения дозы.

Применение у детей

Тизабри противопоказан детям и подросткам.

Применение у пожилых пациентов

Не рекомендуется использование препарата Тизабри у пациентов от 65 лет и старше, ввиду отсутствия данных о безопасности для этой категории пациентов.

Фармацевтические характеристики

Концентрат для приготовления раствора для инфузий. Бесцветный прозрачный или слегка опалесцирующий раствор

Упаковка, срок годности, условия хранения

Концентрат для приготовления раствора для инфузий 20 мг/мл. Тизабри поставляется в форме раствора. Продается во флаконах из медицинского стекла (первый тип). Пробка дополняется алюминиевой прокладкой-колпачком. Материал — бромбутил. Сверху устанавливается особая крышка, контролирующая процедуру первого вскрытия. По 15 мл в одном флаконе. Стеклянные флаконы вместе с инструкцией помещают в картонные упаковки. Внутри коробка разделена на несколько отсеков. Предусмотрена бумажная перфорация и защитные наклейки, для контроля первого вскрытия.

Хранить концентрат и готовый к применению раствор при температуре 2-8°С, в защищенном от света месте. Не замораживать. Хранить в недоступном для детей месте.

Срок годности: концентрат — 4 года, готовый к применению раствор — 8 часов. Не использовать по истечении срока годности.

 

 

 

 

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Работаем и отправляем Тизабри (Натализумаб) по странам СНГ: Россия, Украина, Кыргызстан (Бишкек), Белоруссия, Узбекистан (Ташкент),
а также можем отправить Тизабри (Натализумаб) по регионам Казахстана: Нур-Султан (Астана), Шымкент, Талдыкорган, Актау и другие.

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    The bench press is certainly one of the most popular exercises at the health club for building chest,
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    From there, the necessary thing step will once again be to observe what your weight does over the
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    In this instance, this particular person would
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    Any type of cardio that raises your coronary heart rate could be accomplished to increase your endurance.
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    calories being burnt. A good rule of thumb to ask yourself is, «Would I be comfy in public with no shirt?» If the answer isn’t any,
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    Just stick to the above carbs and eat them round your exercise instances (before and after) and
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    All in all, you will not see us condemning white rice or fruits as
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    The TDEE calculator will take all issues under consideration, corresponding to your gender, age, height, weight and exercise level.
    Of course, it’s not going to be actual, but typically it is fairly correct, so it’s the way most individuals determine on their maintenance level.

    Something much less and you won’t see much in the
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    This program puts a huge emphasis on progressive overload.
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    On the contrary, very excessive doses of vitamins C and E can impair your coaching results.10 Long-term overdosing on some micronutrients
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    Let’s take a better take a glance at the best dietary dietary supplements to support
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    You can optimize your bulking food plan for muscle progress and
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    A sensible bulk will not harm you, but gaining weight too quickly or eating massive amounts of unhealthy foods
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    If you’ve sure medical situations, like heart disease, diabetes, and hypertension, it’s a good
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    Because you eat virtually no carbs on keto, your muscles
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    They are principally a very calorie-dense meals in powdered type.
    Creatine is a natural substance present in your muscles.

    Your BMR is an estimate of the entire energy burned a day, while in a state of relaxation. I spent four years of faculty figuring out 5 days a week for
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    They should not be used to exchange a food regimen, however to help it.
    Whereas it would be ideal to devour many dietary supplements a day,
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    The drawback is not the carbohydrates, but the amount of them that people eat at a
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    600 or so could be used for normal features, whereas the opposite 2900 energy
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    In only one month you’ll look greater and really feel better with this all-out energy assault.
    It takes effort, dedication and a solid plan that covers all bases.

    You need to commit to the journey and live the life totally.
    For this reason I stick with the confirmed complement, creatine monohydrate.

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    If you’re new to exercise or haven’t skilled in properly over 3 months we’d suggest you opt
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    If you conquered Week 1, get ready to elevate your recreation.
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    Let’s delve into the primary points of this week’s routine designed to propel your features to the subsequent degree.
    «Remember, we weren’t coaching to truly box three-minute rounds, however to drop physique fats and add most muscle bulk in a relatively quick area of time,»
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    Slowly work up in weight, performing multiple mild warmup units.
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    So, you should try to add slightly weight or maximize the reps in the recommended vary on a weekly basis.
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    The main purpose we’re utilizing an underhand grip is to construct
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    If you’re a beginner, it’ll eat you alive – you’d most likely be higher trying certainly one of our much less intense programs to
    begin with. He holds a journalism diploma from the
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    He is a four-decade veteran of the medical system
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    Aim for a nutrient stability of 40% protein, 20-25% fats, and 35-40% carbohydrates.

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    This always issues, but it issues even more while slicing as a end result of you’re in a
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    Cardio is further exercise… and additional train requires extra recovery.

    When slicing in the manner outlined above, you’ll certainly lose weight quick.
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    The typical old-school approach to slicing is basically
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    Progressive overload refers again to the process of continually difficult your body.
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    Anavar (oxandrolone) is a popular anabolic steroid used by many individuals for different
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    There are a couple of primary the purpose why Anvarol is better and safer than Anavar.

    A few of our sufferers have skilled insomnia or issue sleeping on anabolic
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    These unwanted effects don’t apply to everybody,
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    References:

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    Next, educate your self on the significance of food regimen and vitamin when combined with an Anavar cycle.

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    This may cause symptoms of low testosterone when your cycle ends, including lack of muscle and fats gain. It’s strongly beneficial that Anavar not be used for longer than eight weeks because of its potential to cause stress to the liver as an oral steroid.

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    We have found incidents of zits vulgaris to be more prevalent on trenbolone as a result of excessive stimulation of
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    On the opposite, legal Anavar options are substances created
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    Testosterone suppression will happen; nonetheless, post-cycle recovery is more probably to be quick, with this
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    Mild opposed fluctuations in HDL and LDL levels of cholesterol
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    References:

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