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Луцентис — Lucentis (ранибизумаб)

Луцентис (ранибизумаб)

Луцентис — Lucentis (ранибизумаб)

Для лечения пациентов с макулодистрофией в настоящее время стал препарат Луцентис, который был утвержден FDA в июне 2006 года, как уникальное средство для лечения возрастной макулярной дегенерации. Основное действующее вещество препарата Луцентис — ранибизумаб.

Препарат Луцентис был специально разработан для использования в офтальмологии, что обеспечивает его высокую безопасность и эффективность. Препарат Луцентис – раствор для интравитреального введения, революционное средство, позволяющее сохранить и улучшить зрение пациентов с серьезными заболеваниями глаз, еще недавно считавшихся обреченными на полную его утерю.

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Описание

Для лечения пациентов с макулодистрофией в настоящее время стал препарат Луцентис, который был утвержден FDA в июне 2006 года, как уникальное средство для лечения возрастной макулярной дегенерации. Основное действующее вещество препарата Луцентис — ранибизумаб.

Препарат Луцентис был специально разработан для использования в офтальмологии, что обеспечивает его высокую безопасность и эффективность. Препарат Луцентис – раствор для интравитреального введения, революционное средство, позволяющее сохранить и улучшить зрение пациентов с серьезными заболеваниями глаз, еще недавно считавшихся обреченными на полную его утерю.

Препарат Луцентис нормализует толщину сетчатки, уменьшает избыточную стимуляцию роста аномальных сосудов при возрастной макулярной дегенерации, действует на связь только с активными изоформами фактора роста новых сосудов, обеспечивая патогенетический подход к лечению. Препарат Луцентисполностью и быстро проникает во все слои сетчатки, таким образом предотвращает увеличение размера поражения, снижает макулярный отек, новые кровоизлияния и прогрессию роста патологических сосудов.

Состав Луцентис

  • активное вещество: ранибизумаб
  • дополнительные вещества: α,α-трегалозы дигидрат; L-гистидина гидрохлорида моногидрат; L-гистидин; полисорбат 20; вода для инъекций.

Показания препарата Луцентис

  • при терапии неоваскулярной (влажной) формы возрастной макулярной дегенерации у взрослых;
  • при терапии снижения остроты зрения, связанного с диабетическим отеком макулы. В качестве монотерапии или в сочетании с ЛК у больных, у которых ранее проводилась ЛК;
  • при терапии снижения остроты зрения, вызванного отеком макулы вследствие окклюзии вен сетчатки;
  • при терапии снижения остроты зрения, вызванного хориоидальной неоваскуляризацией, обусловленной патологической миопией.

Фармакодинамика

Препарат Луцентис — это средство для лечения экссудативно-геморрагической формы возрастной макулярной дегенерации. В основе препарата заявлено вещество ранибизумаб, который является субстанцией из фрагментов антител, способных не допускать пролиферацию клеток и тормозить появление новых сосудов. Вещество Ранибизумаб экспрессируется рекомбинантным штаммом Escherichia coli и является человеческим моноклональным фрагментом антител к эндотелиальному фактору роста А (VEGF-A).

Ранибизумаб — это фрагмент рекомбинантного гуманизированного моноклонального антитела против человеческого сосудистого эндотелиального фактора роста А (VEGF-A). Он соединяет с высокой аффинностью изоформы VEGF-A (например, VEGF121, VEGF165, VEGF110) и, таким образом, не допускает прикрепление VEGF-A к его рецепторам VEGFR-2 и VEGFR-1. Присоединения VEGF-A к его рецепторам ведет к пролиферации эндотелиальных клеток и неоваскуляризации, а также ведет проницаемости сосудов, что, способствет прогрессированию неоваскулярной формы возрастной макулярной дегенерации (ВМД) или патологической миопии, а также макулярного отека, приводящего к нарушению зрения окклюзии вен сетчатки или при диабете.

Ранибизумаб избирательно взаимодействует с изоформами эндотелиального фактора роста сосудов, VEGF-A (VEGF110, VEGF165, VEGF121), а также ингибирует взаимодействие VEGF-A с его рецепторами на поверхности клеток эндотелия (VEGR1 и VEGR2), что ведет к подавлению пролиферации сосудов и снижению неоваскуляризации. ранибизумаб, ингибируя пролиферацию новообразованных сосудов хориоидеи в сетчатку, останавливает прогрессирование экссудативно-геморрагической формы возрастной макулярной дегенерации и макулярного отека у пациентов с сахарным диабетом.

При использовании препарата Луцентис наблюдалось выраженное стабильное уменьшение толщины центральной зоны сетчатки, измеренной с помощью оптической когерентной томографии. Препарат Луцентис нормализует толщину сетчатки, снижает избыточную стимуляцию ангиогенеза при возрастной макулярной дегенерации, действует на связь только с активными изоформами фактора роста новообразованных сосудов, обеспечивая патогенетический подход к лечению. Препарат Луцентис быстро и полностью проникает во все слои сетчатки, таким образом уменьшает макулярный отек и предотвращает увеличение размера поражения, прогрессию хориоидальной неоваскуляризации и новые кровоизлияния.

Лечение препаратом Луцентис – это внутриглазные инъекции, проводимые не чаще одного раза в месяц. Лечение проводят до достижения максимального уровня остроты зрения, который определяется с помощью мониторинга на трех ежемесячных последовательных визитах к лечащему врачу. Профиль безопасности препарата Луцентис у пациентов с диабетическим макулярным отеком был сходен с таковым при лечении влажной формы возрастной макулярной дегенерации.

Препарат Луцентис эффективно улучшает зрение у больных при экссудативной возрастной макулярной дегенерации с классическим компонентом хориоидальной неоваскуляризации (ХНВ) или без него. Уже после трех последовательных ежемесячных инъекций Рост остроты зрения и уменьшение толщины сетчатки может достигать максимума — фаза стабилизации (у некоторых пациентов может проявиться уже в течение первой недели, после первой инъекции препарата Луцентис), и поддерживается на фоне лечения на протяжении 24 месяцев.

Инъекции препарата Луцентиса могут быть назначены как средство монотерапии так и в комплексе с другими методами терапии. Эффективность инъекций подтверждают многочисленные исследования, доказывающие остановку потери зрения на фоне лечения препаратом Луцентис и даже значимое повышение остроты зрения.

Фармакокинетика

Абсорбция

При ежемесячном интравитреального использовании препарата Луцентис у больных с неоваскулярной возрастной макулярной дегенерацией (ВМД), как правило, концентрация ранибизумаба в сыворотке крови низкая, с максимальным уровнемконцентрации (Cmax) ниже необходимой концентрации для подавления биологической активности сосудистого эндотелиального фактора роста (VEGF) на 50процентов 11 27 нг/мл, как определено в исследовании клеточной пролиферации in vitrо. Максимальная концентрация Cmax пропорциональна дозировке 0,05–1,0 мг/глаз.

После ежемесячного интравитреальном введения ранибизумаба в дозировке 0,5 мг на каждый глаз, максимальная концентрация ранибизумаба в сыворотке наблюдается ориентировочно через день после применения препарата и составляет 0,79–2,90 нг/мл. Минимальная концентрация Cmin может составлять 0,07–0,49 нг/мл. Сывороточные концентрации у больных с диабетическим макулярным отеком и окклюзией вены сетчатки были аналогичны концентрациям у больных с неоваскулярной (экссудативной формы) возрастной макулярной дегенерации.

Распределение/Выведение

При введении препарата в дозировке 0,5 мг, среднее значение периода полувыведения ранибизумаба из стекловидного тела составляет приблизительно 9 дней. Приблизительно в 90 000 раз ниже экспозиция ранибизумаба в сыворотке крови, чем в стекловидном теле.

Фармакокинетика в особых группах пациентов.

Пациенты с нарушением функции почек.

Фармакокинетические исследования препарата Луцентис у больных с нарушением функции почек не проводились. При изучении фармакокинетики в популяции пациентов с неоваскулярной формой возрастной макулярной дегенерации 68 процентов 136 из 200 пациентов с возрастной макулярной дегенерации, включенных в фармакокинетический анализ, имелись нарушения функции почек (46,5процентов — легкой степени [50-80 мл / мин], 20процентов — умеренной степени [30-50 мл / мин] и 1,5процента — тяжелой степени [менее 30 мл / мин]). Уровень системного клиренса был несколько ниже, но клинически незначительным.

У 48,2процентов 253 из 525 пациентов с окклюзией вен сетчатки (ОВС) имелись нарушения функции почек (36,4процентов — легкой степени, 9,5процентов — умеренной степени и 2,3процента — тяжелой степени). На фоне лечения препаратом Луцентис у больных с нарушением функции почек отмечалось минимальное снижение клиренса ранибизумаба, клинического значения не имеющее.

Пациенты с нарушением функции печени.

Фармакокинетические исследования препарата Луцентис у больных с нарушением функции печени не проводились. У больных с нарушением функции печени специальные фармакокинетические исследования по использованию ранибизумаба не проводились.

Фармацевтические характеристики

Прозрачный или слегка опалесцирующий раствор. Может быть бесцветным или очень слабо окрашенным.

Упаковка, срок годности, условия хранения Луцентис

Раствор для внутриглазного введения, в дозировке 10 мг/мл. В каждом флаконе по 0,23 мл. Флакон — из бесцветного стекла, закупоренный резиновой пробкой, обкатанный алюминиевым колпачком с отщелкивающейся крышкой. По одному флакону в комплекте с иглой, снабженной фильтром, для извлечения содержимого из флакона, шприцем, иглой для инъекций. Весь комплект вместе с инструкцией по применению упакован в пачку из картона.

Хранить препарат Луцентис нужно в защищенном от света месте, при температуре 2–8 °C. Не замораживать. Хранить в недоступном для детей месте.

Срок годности препарата Луцентис 3 года. Не применять 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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Заказать и купить Луцентис (ранибизумаб) в Казахстане

Позвоните и узнайте цену Луцентис  (ранибизумаб)

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

 

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    ### Introduction to Anabolic-Androgenic Steroids (AAS)
    AAS are synthetic hormones that mimic the effects of testosterone, one of the primary hormones responsible for
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    #### Stacking Steroids
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    Medium-length cycles are popular among experienced users who want to balance muscle growth with recovery.

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    #### Long Cycles (3-9 months)
    Long-term use is often reserved for advanced users or those looking to build significant muscle mass or achieve a specific aesthetic goal.

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    #### Testosterone (and Its Esters)
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    Anavar is a mild steroid often used in cutting phases or for maintaining muscle mass during a break from growth hormones.

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    #### Trenbolone Acetate
    Trenbolone is a potent steroid with strong anabolic and anti-catabolic effects.
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    #### Winstrol (Stanozolol)
    Winstrol is a powerful steroid with minimal estrogenic activity, making it a popular choice for cutting cycles.

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    #### Clenbuterol (Clen)
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    Proviron is used primarily for hormone optimization, helping to maintain testoster-one levels during steroid use.

    #### Masteron (Drostanolone)
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    #### Halotestin (Fluoxymesterone)
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    #### Equipoise (Boldenone)
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    #### Oral Turinabol (Tbol)
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    #### T3 Cytomel
    T3 Cytomel is a thyroid hormone analog that’s sometimes used
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    ### Beginner Steroid Cycles
    For those new to AAS, starting with a simple, well-structured cycle is key.
    Below are some recommendations for beginner cycles:

    #### Should I use steroids?
    Before deciding to use steroids, consider the following questions:
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    — Have you been training for less than five years?

    — Do you have poor training and diet discipline?

    — Are you carrying excess body fat?
    — Do you struggle with emotional or psychological issues?

    If you answered yes to any of these, it might be best
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    #### Option #2: The 1-vial Testosterone Cycle for Beginners
    For those looking for simplicity, a single vial of Testosterone Enanthate (100-200mg per week) is often recommended as
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    For more significant muscle gain, you can combine Testosterone with Dianabol.
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    — Dianabol: 25-50mg/day
    This combination provides a strong anabolic effect while minimizing side effects like estrogen buildup.

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    Deca-Durabolin is often paired with Dianabol for its anti-inflammatory properties and synergy with Testosterone.
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    — Dianabol: 50mg/day

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    Doses vary widely depending on the steroid and user goals, but sticking to recommended ranges is crucial
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    #### Bulking Stacks
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    — Deca Durabolin + Dbol + Testosterone
    — Sustanon + Tren + Anadrol (Mass Stack)

    #### Cutting Stacks
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    — Primobolan + Anavar + Deca + Test
    — Test Prop + Tren + Winstrol
    — Tren + Test Prop + Halotestin + Anavar

    ### Cycle Diet, Supplements and Training
    While on a steroid cycle, maintaining a calorie surplus
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    — Acne
    — Hair loss
    — Gynecomastia (gyno)
    — Testicular atrophy
    — Mood swings
    — Liver damage
    — High blood pressure

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    **What are anabolic-androgenic steroids (AAS)?**
    AAS are synthetic hormones that mimic the effects of testosterone, promoting muscle growth
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    **What is a half-life?**
    The half-life refers to how long it takes for a drug to be eliminated from the body.
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    **Is it safe to inject steroids? Does it hurt?**
    Steroid injection itself is generally safe when done properly.
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    **At what age should I start using steroids?**
    The general recommendation is to wait until you’re at least 21 years old and have a solid understanding of steroid biology and
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    **What should my diet and training be like when I’m on a steroid cycle?**

    A calorie surplus with high-protein meals, adequate hydration, and rest are
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    **What is an ester?**
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    Yes, especially if you’re using steroids like Dianabol or Anavar, which
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    **What is gyno?**
    Gyno refers to gynecosmodystrophy, a condition where breast tissue develops in males
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    Yes, steroid use can lead to acne and male pattern baldness in some users.

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    High doses of steroids can suppress libido, but this
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    **How fast do anabolic steroids work?**
    Steroids work relatively quickly, with noticeable changes
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    **What happens when you stop taking steroids?**
    Stopping steroids suddenly can cause hormonal imbalances and side effects like gyno or testicular atrophy.

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