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Левакт (Ливакт) — Levact (Бендамустин)

Левакт

Левакт (Ливакт) — Levact (Бендамустин)

Левакт является противоопухолевым алкилирующим агентом с новой активностью. Основное действующее вещество — Бендамустина гидрохлорид, чье противоопухолевое действие было выявлено в многочисленных исследованиях in vitro, проведенных на различных линиях опухолевых клеток человека (мелкоклеточный и немелкоклеточный рак легкого, рак молочной железы, рак яичников и различные виды лейкемии), и in vivo на различных экспериментальных моделях опухолей (меланома, саркома, рак молочной железы, лейкоз, лимфома и мелкоклеточный рак легкого).

Категория:

Описание

Левакт является противоопухолевым алкилирующим агентом с новой активностью. Основное действующее вещество — Бендамустина гидрохлорид, чье противоопухолевое действие было выявлено в многочисленных исследованиях in vitro, проведенных на различных линиях опухолевых клеток человека (мелкоклеточный и немелкоклеточный рак легкого, рак молочной железы, рак яичников и различные виды лейкемии), и in vivo на различных экспериментальных моделях опухолей (меланома, саркома, рак молочной железы, лейкоз, лимфома и мелкоклеточный рак легкого).

Гидрохлорид бендамустина проявил небольшую перекрестную устойчивость или отсутствие перекрестной устойчивости на моделях опухолевых клеток человека, которые имеют различные механизмы лекарственной резистентности. Кроме того, клинические исследования показали, что нет полной перекрестной резистентности бендамустина к алкилирующим агентам, ритуксимабу или антрациклинам. Тем не менее, количество оцениваемых пациентов невелико.

Показания к применению Левакт

  • Хронический лимфоцитарный лейкоз
  • Индолентные неходжкинские лимфомы в монотерапии и в комбинированной терапии в качестве терапии 1ой линии.
  • Множественная миелома в комбинации с преднизолоном.

Состав Левакт

1 флакон содержит:

  • активное вещество: бендамустина гидрохлорид 100 мг
  • вспомогательные вещества: маннитол

Фармакодинамика

Бендамустина гидрохлорид является противоопухолевым лекарственным средством с бифункциональной алкилирующей активностью.

Механизм действия препарата Левакт включает следующие эффекты: цитотоксическое действие, подавление механизмов, действующих в сверочной точке митоза, нарушение митоза, активацию апоптоза.

Бендамустина гидрохлорид имеет одинаковость как с алкилирующими агентами, так и с пуриновыми аналогами. Бендамустина гидрохлорид включает три структурных элемента: 2-хлорэтиламиновую группу, цепь масляной кислоты, центральное бензимидазольное кольцо. Алкилирующие свойства бендамустина взаимосвязаны с присутствием 2-хлорэтиламиновой группы. Основной процесс, с помощью которого хлорэтиламины приводят к повреждению ДНК — это процесс алкилирования — механизм присоединения алкильных групп к нуклеофильным участкам ДНК. Взаимодействие между участком высокореактивного хлорэтиламина и ДНК создает повреждение ДНК и, как следствие, включению ряда сигнальных путей, вовлеченных в репарацию ДНК. Однако процессы репарации ДНК не могут преодолеть фармакологического нарушения, вызванного препаратом Левакт. На основании того, что клетки не могут восстановиться после повреждений, в них инициируются процессы программной гибели путем апоптоза.

Другой механизм, с помощью которого бендамустина гидрохлорид вызывает повреждение ДНК, состоит в организации перекрестных сшивок ДНК внутри одной или между двумя цепями ДНК. Оба механизма, и образование перекрестных сшивок, и алкилирование приводят к разрывам ДНК, которые также активируют процессы ее восстановления. В дополнение к прямому влиянию на ДНК бендамустина гидрохлорид оказывает не прямое влияние на процессы клеточного деления. Ввиду того, что в клетке имело место повреждение ДНК, вслед за этим осуществляется процесс подавления репликации и транскрипции ее ДНК.

Фармакокинетика

Распределение

По прошествии однократной 30-минутной внутривенной системы бендамустина гидрохлорида в дозе 120 мг/м2 поверхности тела бета-фаза элиминации (T1/2β) составляет мин. Центральный объём распределения при болюсной 30-минутной внутривенной системы составляет 19,3 литров, при дальнейшем систематическом вливании и достижении равновесной концентрации объем распределения составляет от 15,8 до 20,5 литров. В системном кровотоке Левакт активно связывается с белками плазмы, преимущественно, с альбумином.

Способность бендамустина гидрохлорида к взаимодействию с белками плазмы крови не нарушается у пациентов в возрасте старше 70 лет, при поздних стадиях опухолей и при низких концентрациях альбумина в плазме крови.

Метаболизм

Бендамустина гидрохлорид метаболизируется преимущественно в печени. Основным путем элиминации бендамустина гидрохлорида из организма составляет его гидролиз с формированием моногидрокси- и дигидроксибендамустина. В формировании окисленного метаболита и N-десметилбендамустина в печени задействован изофермент СУР 1А2 цитохрома Р450. In vitro бендамустин не ингибирует СYР1lA4, СYР 2D6, СYР 2C9/10, СYР ЗА4 и СYР 2El.

Элиминация и экскреция

После 30-минутной внутривенной инфузии среднее значение общего клиренса лекарственного средства 12 субъектам составило 639,4 мл/мин в дозировке 120 мл/м2 поверхности тела. На протяжении 24 часов около 2094 введенной дозы лекарственного средства экскретировалось почками.

Количества элиминируемого с почками неизмененного бендамустина гидрохлорида и его метаболитов располагается в порядке снижения следующим образом: мононадроксибендамустин > бендамустин > дигидроксибендамустин > окисленный метаболит > 14деметилбендамустин. С желчью выводятся преимущественно полярные метаболиты.

Фармакокинетика у различных групп пациентов

Пациенты с нарушенной функцией печени

Фармакокинетика, при 30-70% опухолевом поражении печени и незначительно сниженной функцией печени (сывороточный билирубин <1,2 мг/дл), не имела значимых отличий от такой же у больных с нормальной функцией печени и почек в отношении tmax, Сmах, AUC, выведения и объема распределения.

Пациенты с нарушением функции почек

Фармакокинетика у больных с клиренсом креатинина > 10 мл/мин, в том числе находящиеся на диализе, существенно не отличались от таковых у больных с нормальной функцией почек в отношении Сmах, tmax, AUC, T1/2β, объема распределения и выведения.

Пожилые пациенты

В исследование фармакокинетики бендамустина включались пациенты до 84 лет. У лиц старшего возраста фармакокинетические параметры значимо не отличались. Точных  данных по рекомендации корректировки дозировки у пожилых пациентов нет.

Печеночная недостаточность

На основании фармакокинетических данных, коррекция дозы у пациентов с легкими нарушениями печени (билирубин сыворотки <1, 2 мг / дл). 30% не требуется. Снижение дозы рекомендуется для пациентов с умеренной печеночной недостаточностью (сывороточный билирубин 1, 2 — 3, 0 мг / дл).
Для пациентов с тяжелой печеночной недостаточностью (сывороточный билирубин> 3, 0 мг / дл) нет данных. Потому как, данные по фармакокинетике бендамустина гидрохлорида у больных с нарушением функции печени ограничены, при легкой степени печеночной недостаточности препарат Левакт следует использовать с осторожностью. Нельзя использовать бендамустин гидрохлорид при умеренной и тяжелой печеночной недостаточности.

Почечная недостаточность

Коррекция дозы, на основании фармакокинетических данных у пациентов с клиренсом креатинина> 10 мл / мин не требуется. Опыт работы с пациентами с тяжелой почечной недостаточностью ограничен. У больных с клиренсом креатинина более 10 мл/мин, в т. ч. находящихся на гемодиализе, фармакокинетические параметры существенно не отличаются от таких у больных с нормальной функцией почек, соответственно необходимости в коррекции дозы препарата нет.

Педиатрия

Не установлена эффективность и безопасность бендамустина гидрохлорида у детей еще. Для предоставления рекомендации по дозировке доступных в настоящее время данных недостаточно.

Фармацевтические характеристики

Бендамустина гидрохлорид представляет собой белый или почти белый, лиофилизированный брикет, микрокристаллический порошок или брикет с порошком, с амфотерными свойствами. Растворим в воде.

Упаковка, срок годности, условия хранения

Левакт 2,5 мг/мл, порошок для концентрата, раствор для инфузий. Лиофилизат для приготовления концентрата для приготовления раствора 100 мг.

Левакт упакован во флаконы из темного стекла, закупоренных резиновой пробкой с отщелкивающейся крышкой темно-синего цвета. Флакон помещен в пластиковый контейнер, который вместе с инструкцией упакован в картонную пачку . Упаковка по 20 флаконов по 10 мл или коробка из 5 флаконов по 40 мл.

Хранить в защищенном от света месте при температуре не выше 25° С. После приготовления раствор следует использовать немедленно. Транспортирование лекарственного средства возможно при температуре не выше 30°С. Хранить в недоступном для детей месте.

Срок годности 2 года. Не использовать по истечении срока годности.

 

 

 

 

Наша компания работает как на территории Казахстана, так и осуществляет доставку в страны ближнего зарубежья. Обращайтесь к нам за консультациями по контактным телефонам.

Заказать и купить Левакт (Бендамустин) в Алматы

Заказать и купить Левакт (Бендамустин) в Казахстане

Позвоните и узнайте цену Левакт (Бендамустин)

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

 

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    Best Steroid Cycles for Lean Mass and Legal Alternatives

    Steroids have long been a cornerstone of bodybuilding, offering
    athletes the ability to build muscle, shed fat, and enhance performance.
    However, with the rise of awareness about health
    risks and legal concerns, many are turning to legal alternatives and natural supplements to achieve
    similar results. In this article, we explore the best steroid cycles for lean mass, along with
    legal alternatives that can help you achieve your bodybuilding goals without
    compromising your health.

    Trenbolone and Legal Alternative

    Trenbolone is one of the most popular steroids among
    bodybuilders, known for its ability to promote lean muscle growth
    and fat loss. While it’s highly effective, it also carries a high risk
    of side effects, including liver damage and
    hormonal imbalance. For those who want to avoid the health risks associated with Trenbolone,
    legal alternatives like Winsol or MST (Methylstanoval) can provide similar benefits with fewer risks.

    Testosterone and Legal Alternative

    Testosterone is another cornerstone of steroid use, primarily for its ability
    to enhance muscle growth and recovery. While injectable testosterone is
    highly effective, it can also lead to side effects like
    hair loss, acne, and testicular atrophy. A legal
    alternative to testosterone is D-Bal, a natural supplement that mimics the anabolic effects of testosterone without the harmful side
    effects.

    Best Steroid Cycle for Lean Muscle Gain

    If your goal is lean muscle gain, the best steroid cycle for this
    purpose is typically Trenbolone combined with Testosterone
    Enanthate. This stack promotes both muscle growth and fat loss, providing a shredded, athletic physique.

    For those who prefer legal alternatives, you can combine Winsol or
    MST with a high-quality protein powder and intense
    training regimen to achieve similar results.

    Other Steroids for Lean Muscle Gain

    Besides Trenbolone and Testosterone, other steroids
    like Anadrol and Dianabol are often used in lean mass cycles.
    However, these steroids can be harsher on the liver and overall health,
    making them less ideal for long-term use.

    Legal alternatives to Anadrol include Androstanediol and Tevion, which provide similar muscle-building benefits without the health risks.

    Anadrol and Legal Alternative

    Anadrol, also known as Oxandrolone, is a potent steroid that’s highly effective for
    lean mass gain. However, its use can lead
    to side effects like liver damage and acne. For those who want to avoid Anadrol, Androstanediol is a solid legal alternative that mimics the anabolic effects
    of Anadrol while being gentler on the body.

    Dianabol and Legal Alternative

    Dianabol is another powerful steroid used for lean mass gain. While
    it’s effective, it can cause significant liver damage and other side effects.
    A legal alternative to Dianabol is Tevion, which offers
    similar muscle-building benefits without the health risks
    associated with Dianabol.

    More Effective Steroids:

    When it comes to lean mass gain, the most effective steroids are those that enhance protein synthesis while minimizing fat retention. Steroids like
    Trenbolone, Anadrol, and Dianabol are often considered the best for this purpose.
    However, if you’re looking for legal alternatives, products like Winsol, MST, and D-Bal
    can provide comparable results with improved
    safety profiles.

    Best Steroid for Lean Muscle

    The best steroid for lean muscle is often considered to be Trenbolone, due to its ability to promote
    both muscle growth and fat loss. However, if you’re looking for legal alternatives, D-Bal is a top choice,
    as it mimics the anabolic effects of testosterone without the harmful side
    effects.

    Dianabol Steroid Cycles for Lean Mass

    Dianabol cycles are another popular option for lean mass gain. A typical Dianabol cycle involves taking 25-50mg of the steroid per day, often combined with other steroids like Trenbolone or Testosterone.
    For legal alternatives, you can use Winsol or
    MST, which provide similar benefits without the health risks.

    Lean Bulk Cycle

    For those who want to focus on muscle gain rather than fat loss, a
    lean bulk cycle typically involves using steroids like Dianabol or Anadrol,
    along with high-calorie meals and intense training.
    Legal alternatives to this approach include using protein-rich
    supplements like Bulk-Builders and combining them with natural anabolics like
    Tevion.

    Best Cycle for Lean Mass and Strength

    If your goal is to build both lean mass and strength, the
    best steroid cycle would likely include a combination of Trenbolone, Anadrol, and Dianabol.

    For legal alternatives, consider using Winsol, MST, and Bulk-Builders to achieve similar results
    while maintaining your health.

    What About Legal Mass Building Steroids?

    While no legal steroids can fully replicate the effects of anabolic steroids, there are several supplements that can help you build mass.
    These include whey protein, creatine monohydrate, and natural anabolics like Tevion.
    Combining these with a rigorous training regimen and a
    high-calorie diet can yield significant muscle growth over
    time.

    What Sort of Results Can You Expect?

    With the right steroid cycle or legal alternative, you can expect to
    see measurable increases in muscle mass, fat loss, and overall strength.

    Results will vary depending on individual genetics, diet, and training
    intensity. However, with consistent effort and proper supplementation, you
    can achieve a lean, muscular physique that rival’s anabolic steroid users.

    How Should You Train & Eat for Mass?

    To maximize your muscle gain and fat loss, ensure that your training regimen includes compound movements like
    squats, deadlifts, bench presses, and pull-ups.
    Aim for 4-5 training sessions per week, with at least 48 hours
    of rest between sessions. Your diet should be calorie-dense, with a focus
    on whole foods, proteins, carbohydrates, and healthy fats.

    Supplements like Bulk-Builders can further enhance your muscle growth.

    Best Muscle Builder: TestoPrime

    TestoPrime is one of the most effective natural supplements for muscle growth,
    as it helps boost testosterone levels and promote protein synthesis.
    By using TestoPrime alongside a solid training regimen and
    a high-calorie diet, you can achieve impressive muscle gains
    without resorting to steroids.

    Winsol

    Winsol is another top choice for legal steroid alternatives.
    It’s designed to mimic the effects of Winstrol, providing
    lean muscle growth and fat loss with minimal side effects.
    Winsol is particularly popular among athletes who want to maintain their performance without the risks associated with anabolic steroids.

    D-Bal

    D-Bal is a natural supplement that mimics the effects of testosterone, making it an excellent choice for muscle
    growth and recovery. D-Bal helps boost testosterone levels, improve muscle synthesis, and enhance strength,
    all while being gentle on your body’s health.

    Comments and Questions?

    If you have any questions about steroid cycles, legal
    alternatives, or how to achieve lean mass gain, feel
    free to leave a comment below. Our team of experts is here to help you navigate the world of bodybuilding supplements and provide tailored advice to meet your goals.

    Best Cycle Support – Liver, Kidney, Cholesterol Support

    Using steroids can be hard on your liver, kidneys, and cholesterol levels.
    To minimize these risks, ensure that you’re taking a
    liver protectant like Milk Thistle, staying hydrated, and maintaining a
    healthy diet. Regular health screenings are also recommended to monitor your organ function.

    Most Dangerous Anabolic Steroids

    Among the most dangerous anabolic steroids are Methandione, Trenbolone, and Dianabol.
    These steroids have been linked to severe health risks, including liver damage, kidney failure, and hormonal imbalances.
    It’s crucial to avoid these substances unless you’re under the supervision of a medical
    professional.

    Arimistane Review

    Arimistane is an aromatase inhibitor that’s often used in steroid cycles to prevent estrogen-related side effects.
    It helps reduce water retention and enhances muscle definition, making it a valuable tool for
    bodybuilders. Arimistane is particularly useful when using
    steroids like Trenbolone or Anadrol.

    Best Prohormone Companies

    When looking for prohormones and legal steroid alternatives, it’s
    important to choose reputable brands that have
    a strong track record of quality and safety. Some top companies include APS
    Nutritionals, Bodybuilding Warehouse, and ProDot. These companies offer high-quality products that can help you
    achieve your bodybuilding goals without the risks associated with illegal steroids.

    PCT for Testosterone Cycle: Your Guide to Reclaiming Natural Levels

    After completing a testosterone cycle, it’s crucial to undergo a Post-Cycle Therapy (PCT) to restore your natural testosterone
    levels. This typically involves taking supplements like
    Clenbutrol, Milk Thistle, and Testosterone Booster for several
    weeks after finishing your cycle. Following a proper PCT ensures that your body
    recovers and returns to its natural state,
    minimizing the risk of side effects.

    Turkesterone vs Ecdysterone

    Turkesterone and Ecdysterone are two of the most popular prohormones available today.
    Turkesterone is known for its ability to enhance nitrogen retention and muscle
    growth, while Ecdysterone has been shown to boost
    testosterone levels and promote fat loss. Both compounds
    can be effective in a steroid cycle, but they work differently, so it’s essential to research them carefully before choosing one.

    Contributors

    Ernst Peibst Writer

    Learn More On This Subject..

    If you’re interested in learning more about steroid cycles,
    legal alternatives, and natural supplements for bodybuilding, we recommend
    checking out our guide to the best PCT supplements and how they can help you
    maintain your gains after a cycle. Additionally, if you have any specific questions about steroids like Testosterone Propionate, Halotestin, or Enclomiphene, feel free to leave them in the comments section below.

    Best PCT Supplements for Bodybuilding

    Post-Cycle Therapy (PCT) is essential for anyone who has completed a steroid cycle,
    as it helps restore your body’s natural hormone production. The best PCT supplements include Clenbutrol, Milk Thistle,
    and Testosterone Booster. These supplements work together
    to support liver health, enhance testosterone levels, and minimize the
    risk of side effects.

    What Is Testosterone Propionate? – Cycle, Dosage And Side
    Effects

    Testosterone Propionate is one of the most commonly used anabolic steroids, known for its ability to
    promote muscle growth and fat loss. It’s often preferred by bodybuilders
    due to its short ester cycle, which allows for frequent injections and rapid results.
    However, it also carries a high risk of side effects, including acne,
    hair loss, and testicular atrophy.

    Halotestin: Results, Dosage And Side Effects!

    Halotestin is another potent anabolic steroid that’s often used
    for cutting and building muscle. It’s known for
    its ability to enhance fat loss while maintaining
    muscle mass. Halotestin can be taken orally, making it a popular choice among
    bodybuilders who want the convenience of not injecting multiple times per week.

    Enclomiphene: Review, PCT, Side Effects, Cycle

    Enclomiphene is an oral steroid that’s often used in cutting
    cycles. It works by inhibiting estrogen receptors, which helps reduce fat retention and improve muscle definition. While it’s
    effective, Enclomiphene can also lead to side effects like hair loss and acne,
    so proper PCT is essential after the cycle.

    Best Steroids for Women

    While many women are hesitant to use steroids due to concerns
    about masculine side effects, there are still some that choose to do so under medical supervision. The best steroids
    for women include Testosterone Enanthate, Dianabol, and Trenbolone.

    However, these should be used with caution and only after consulting
    with a healthcare professional.

    Trenabol Review: Cycle, Dosage And Side Effects!

    Trenabol is another popular anabolic steroid that’s often used in cutting cycles.
    It’s known for its ability to enhance fat loss while maintaining muscle
    mass. Trenabol should be taken with caution, as it can cause
    significant side effects like liver damage and hormonal imbalances.

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