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Мозобаил — Mozobil (Плериксафор)

Мозобаил (Плериксафор)

Мозобаил — Mozobil (Плериксафор)

Препарат Мозобаил главным образом применяют с целью увеличения количества стволовых клеток, необходимых для начала процедуры аутотрансплантации, в тех случаях, когда в организме больного устанавливается их недостаток. Попадая в кровоток, препарат Мозабайл способствует увеличению количества стволовых клеток, благодаря чему их забор пройдёт без осложнений. По отзывам специалистов Мозобаил показывает высокую эффективность: благодаря ему 90 процентов пациентов смогли начать процедуру аутотрансплантации.

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Описание

Препарат Мозобаил — это современный иммуностимулирующий препарат, стимулятор лейкопоэза, представляет собой производное бициклама, а также является селективным обратимым антагонистом CXCR4 хемокинового рецептора, ингибируя его за счет взаимодействия с когнатным лигандом, фактором стромальных клеток-1α (SDF-1α), также установленным как CXCL12. Основным действующим веществом является Плериксафор.

Препарат Мозобаил главным образом применяют с целью увеличения количества стволовых клеток, необходимых для начала процедуры аутотрансплантации, в тех случаях, когда в организме больного устанавливается их недостаток. Попадая в кровоток, препарат Мозабайл способствует увеличению количества стволовых клеток, благодаря чему их забор пройдёт без осложнений. По отзывам специалистов Мозобаил показывает высокую эффективность: благодаря ему 90 процентов пациентов смогли начать процедуру аутотрансплантации.

Считается, что индуцированный препаратом Мозобаил лейкоцитоз и увеличение количества циркулирующих гемопоэтических прогениторных клеток является следствием нарушения связи между CXCR4 и его когнатным лигандом. Это приводит к появлению в системном кровотоке как зрелых, так и полипотентных клеток. CD34+ клетки, мобилизованные с помощью плериксафора, являются функциональными и способными к приживлению, с долгосрочным потенциалом восстановления популяции.

Состав Мозобаил

1 флакон содержит

  • активное вещество: плериксафор — 24 мг.
  • вспомогательные вещества: натрия хлорид, 0,1 М раствор натрия гидроксида либо 0,1 М раствора кислоты хлористоводородной (до рН 6,0–7,5); вода для инъекций.

Показания к применению Мозобаил

  • для усиления мобилизации в периферический кровоток гемопоэтических стволовых клеток . С целью сбора их и последующей аутотрансплантации в сочетании с Г-КСФ больным с лимфомой и множественной миеломой.

Фармакодинамика

Препарат Мозобаил представляет собой производное бициклама, а также является селективным обратимым антагонистом CXCR4 хемокинового рецептора, ингибируя его за счет связывания с когнатным лигандом, фактором стромальных клеток-1α (SDF-1α), также известным как CXCL12. Считается, что индуцированный препаратом Мозобаил лейкоцитоз и увеличение количества циркулирующих гемопоэтических прогениторных клеток является следствием нарушения связи между CXCR4 и его когнатным лигандом. Это приводит к появлению в системном кровотоке как зрелых, так и полипотентных клеток. CD34+ клетки, мобилизованные с помощью плериксафора, являются функциональными и способными к приживлению, с долгосрочным потенциалом восстановления популяции.

Фармакодинамика с участием пациентов с лимфомой и множественной миеломой соответственно) в двух плацебо-контролируемых клинических исследованиях оценивалось увеличение содержания CD34+ клеток (клеток/мкл) за 24 часа, перед первым аферезом в течение дня. Первая дозировка плериксафора (0.24 мг/кг) или плацебо в оцениваемый 24-часовой период вводилась за 10-11 часов до афереза.

У здоровых добровольцев в исследованиях фармакодинамики с применением только плериксафора пик мобилизации CD34+ клеток наблюдался в течение 6-9 часов после введения препарата.как у здоровых добровольцев, так и у пациентов при исследовании фармакодинамики с применением схемы мобилизации, включающей Г-КСФ и плериксафор в тех же дозировках, наблюдался более длительный подъем CD34+ клеток в периферической крови в течение с 4 часов до 18 часов после введения препарата. Пик был отмечен между 10 часами и 14 часами.

Дети

В клинических исследованиях не изучались эффективность и безопасность применения у детей и подростков в возрасте до 18 лет препарата Мозобаил.

Медицинское европейское агентство отказалось от обязательного предоставления компанией результатов исследований по использованию препарата Мозобаил у детей и подростков в возрасте до 18 лет при миелосупрессии (вследствие химиотерапии), нуждающейся в аутотрансплантации гемопоэтических стволовых клеток.

Фармакокинетика

У пациентов с лимфомой и множественной миеломой изучали фармакокинетику плериксафора с применением клинической дозы (0.24 мг/кг) после предварительного лечения Г-КСФ (10 мкг/кг 1 раз/сутки в течение от 2 — 4 дней, курс продлевали до 7 дней при необходимости).

Всасывание

После подкожного введения препарат плериксафор быстро всасывается, максимальная концентрация (Cmax) достигается приблизительно через 30-60 минут — максимальное время (Тmax). Послеподкожного введения плериксафора в дозе 0.24 мг/кг, которому предшествовало предварительное лечение Г-КСФ в течение 4 дней подряд, максимальная концентрация (Сmах) и кривой плериксафора в плазме крови и среднее фуцнкциональное значение (AUC) составили 887±217 нг/мл и 4337±922 нг×ч/мл соответственно.

Распределение Мозобаил

Плериксафор умеренно связывается с белками плазмы человека (до 58процентов). Кажущийся объем распределения плериксафора составляет 0.3 л/кг, что свидетельствует о том, что препарат Мозобаил склонен к распространению во внесосудистом пространстве, но не ограничен им.

Метаболизм

Плериксафор не подвергался метаболизму печеночными микросомами человека и эмбриональными гепатоцитами человека в экспериментах in vitro. Препарат не угнетает основные метаболизирующие изоферменты цитохрома Р450 ( 2А6, 1А2, 2В6, 2С8, 2С9, 2С19, 2D6, 2Е1 и 3А4/5), это также было показано. В экспериментах in vitro с человеческими гепатоцитами плериксафор не индуцировал изоферменты CYP1A2, CYP2B6 и CYP3A4. Согласно полученным данным предполагают, что потенциал лекарственного взаимодействия, опосредованного системой Р450, для плериксафора низок.

Выведение Мозобаил

Основной путь элиминации плериксафора — выведение почками. После введения плериксафора в дозе 0.24 мг/кг здоровым добровольцам с нормальной функцией почек, примерно 70процента препарата выводилось в неизмененном виде с мочой в течение первых 24 часов после введения. Период полурасада (Т1/2) составляет 3-5 часов. In vitro исследования с использованием клеточных моделей MDCKII и MDCKII-MDR1 показали, что препарат Мозобаил субстратом или ингибитором Р-гликопротеина не является.

Фармакокинетика у особых групп пациентов

У больных с разной степенью почечной недостаточности клиренс препарата Мозобаил после однократной дозы (0.24 мг/кг) снижался; наблюдалась положительная корреляция с КК. Средние показатели AUC0-24 для препарата Мозобаил , вводимого пациентам с легкой почечной недостаточностью (КК 51-80 мл/мин), умеренной (КК 31-50 мл/мин) и тяжелой (КК ≤30 мл/мин) степени, составили 5410, 6780 и 6990 нг×ч/мл соответственно, что превышает значения экспозиции плериксафора, наблюдаемые при нормальной функции почек (5070 нг×ч/мл). Почечная недостаточность не оказывала влияния на максимальную концентрацию (Сmax).

В зависимости от пола и возраста популяционный анализ не выявил различий фармакокинетики плериксафора.

Данные по фармакокинетике у детей ограничены.

Применение у детей

В связи с отсутствием опыта применения, использование препарата Мозобаил противопоказано в возрасте до 18 лет.

Применение у пожилых пациентов

Не требуется коррекция дозы у пожилых пациентов с нормальной функцией почек. При клиренсе креатинина (КК) ≤50 мл/мин рекомендуется коррекция дозы препарата.

Фармацевтические характеристики

Прозрачный раствор для подкожного введения, бесцветный или светло-желтый.

Упаковка, срок годности, условия хранения

По 1.2 мл содержится во флаконах из  бесцветного стекла I типа. Каждый флакон вместе с инструкцией по применению помещен в пачки картонные.

Препарат Мозобаил следует хранить в недоступном для детей месте при температуре от 15°С до 30°С.
Срок годности — 3 года. Не применять по истечении срока годности.

 

 

 

 

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

 

 

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    workout. I hereby comply with assume and settle for any and all risks of damage or
    dying related to stated health activities. They comprise the best cable pec
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    to build full, proportional pecs without wearing you to a frazzle.
    They’re a protected, efficient, and even beginner-friendly alternative to your favorite
    barbell and dumbbell exercises—but will contribute to larger hypertrophy
    and pace up muscle failure. The more time your muscles spend underneath rigidity,
    the sooner they reach muscle fatigue and finally muscle failure,
    which in flip leads to larger growth throughout your post-workout restoration.
    Since the chest exercise routine is the star of this show, I Am going to focus on it first, so you can see what you’re getting into.
    And we won’t consider a greater means than following this ultimate chest workout routine.
    Now, we know that you just’re giving all of your muscle tissue equal love and a focus
    in your workout break up, as nobody needs a jacked higher body paired with chicken legs.
    Below are seven of the most effective variations of the
    hammer press exercise for creating balanced chest muscle tissue.
    Additionally, discover that you’re doing reps of every train, but just for three sets—this is actually helping
    you grasp the movement and construct some endurance with out overdoing it.
    Then, incorporate Cable Bench Fly and Cable
    Pallof Press workout routines to further have interaction and challenge your chest and core muscles.

    Incorporate the cable chest fly into your chest exercise routine to expertise its unique benefits.

    By targeting specific muscle teams and providing fixed rigidity, this exercise might help you build a stronger and more
    defined chest. With the proper equipment and proper type, you
    possibly can elevate your chest workouts and achieve your health
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    It is amongst the best cable exercises for chest that also engages the shoulders and triceps,
    selling balanced higher body growth and practical strength.

    As A Substitute of utilizing dumbbells for
    this train, switching to cables will maximize
    the time beneath tension for sooner fatigue and
    potentially larger hypertrophy. Swap up the angle of your Bench Press to
    emphasize the middle and upper chest space, as nicely as emphasize anterior deltoid (shoulder) energy.
    Cable chest workout routines should be included in each Chest Day workout—if not the star of the present, at least an necessary finisher.
    Jeff Cavaliere is a Physical Therapist, Power Coach and creator of the ATHLEAN-X
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    Thanks to their versatility, you presumably can add them to any
    training program. The glutes are our body’s largest and strongest muscle group,
    and the cable glute kickback helps isolate the
    butt. You should regularly train them to ensure optimum strength
    and muscle gains.Focus on driving your heel towards the ceiling while squeezing your glutes at
    the high of the motion.
    With constant tension on the chest all through the whole vary of movement, this exercise effectively promotes muscle development.
    That mentioned, certain workout routines deliver the pec minor right into a more
    important role, which can help to further strengthen it.
    Firstly, give attention to squeezing your chest muscular tissues at the peak of the motion to maximise muscle activation, whereas also maintaining your shoulders back and down to maintain good posture throughout.
    Secondly, choosing an acceptable cable height is crucial to ensure a
    snug and smooth vary of motion, while minimizing pressure on the
    shoulder joints. Cable crossovers are a protected chest train, however newbies ought to
    be cautious earlier than including cable machines to their routine.

    The cable bench press is a extremely efficient train that targets the chest muscular tissues, triceps, and anterior deltoids.

    Thirdly, constructing muscle mass via chest workouts can also contribute to a better resting metabolic rate,
    resulting in more efficient calorie burning even at relaxation. A decrease chest workout is
    a set of workout routines that focus on the lower portion of the pectoralis major and pectoralis minor muscular tissues.
    Targeting the decrease chest is critical to develop a more defined and proportional chest.

    The flooring press emphasizes the upper chest and triceps greater than a daily bench press, thanks to the
    shorter range of movement. The finest decrease chest exercise
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    head of the sternal area. This is a bit more complicated,
    as it makes use ofsuper units, large sets and workout routines not
    on our list above, as we attempt toincorporate some additional muscle groups into our chest workout.

    Cable bench presses provide a special resistance angle than traditional barbell
    or dumbbell bench presses. They help to strengthen the chest muscles, particularly the sternal portion of
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    Avoid locking out your elbows on the top of the motion and control both the concentric (lifting) and eccentric (lowering) phases.
    Common errors embody using momentum to swing weight up instead of participating the chest
    muscles properly. Focus on a slow and controlled movement to reap all the advantages of this killer exercise without risking harm.

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    Actually, there are only 2 heads of the biceps that, when nicely developed, give it that full and extensive look.

    And with the best workouts, you can truly select which
    one to emphasise. Perform the underhand-grip inverted row
    in the midst of your exercise.
    When doing a bicep exercise with a cable machine,
    you’ll be able to add loads of single-arm exercises to
    correct potential imbalances. The cable reverse curl
    helps to stability arm improvement by focusing on the less typically
    focused muscles of the forearms and 
    brachialis. The cable hammer curl is amongst the finest workout routines that you are
    able to do to construct your arm muscular tissues.
    The High cable curl exercise is a superb possibility for targeting the biceps and building the
    width and thickness of the bicep muscle. With the next dumbbell
    exercises, you can hammer your back and biceps successfully and construct power, muscle, and definition. If you like feeling the
    pump and the mind-muscle connection, this machine-based biceps workout is made for you.
    Designed with high reps and minimal relaxation,
    you’ll feel the blood rushing into your biceps,
    creating that full, tight sensation.
    Nicely, the preacher curls led to more development in any respect
    3 measurement websites of the biceps, particularly within the backside a part of the biceps.
    This is because the muscle cells swell with blood and lactic acid when you contract
    them repeatedly by performing curls and other such workout routines.
    So ensure to carry out some sort of reverse curl and/or
    hammer curl in your exercise if you would like to maximize your muscle definition as a whole.
    For example, building the brachialis can actually enhance your bicep peak because the brachialis is a deep muscle that lies beneath the biceps.
    Therefore, when you add measurement to this deep muscle, it naturally
    pushes your biceps out and makes them look extra prominent.

    Twist the towel a few times until it varieties a long, noodle-like
    shape. Sitting within the chair with your toes on the ground, place the middle of the towel under one foot.
    You don’t need any complicated gear to do that transfer — simply an everyday bath
    towel and a chair. Overlook common push-ups — your biceps will really
    take off with dive-bombers. Modify the pose by putting your forearm on the
    ground as a substitute of your hand.
    In other words, your bigger compound workouts will stay comparable whereas
    you will use the smaller workout routines to add the
    assorted angles and stimuli. For strength positive
    aspects, start with 5 units of 5 reps for a few arm days and then add weight or reps.
    Constructing strong arms and back muscular tissues
    with a bar and body weight.
    Despite its effectiveness, the lying dumbbell curl can really
    feel awkward at first. Nevertheless, once you modify to the motion, it could turn out to be considered one of your go-to bicep exercises
    with dumbbells. I place it within the A-tier for
    its unique ability to target the biceps from a special angle.

    Keep In Mind to choose on a weight that lets you keep proper kind throughout the exercises.
    Firstly, they fail to provide the muscle much
    of a stretch and need to be used with different, extra full,
    workouts. Cable variations are typically better, offering rigidity over a greater vary of movement.
    As lengthy as you’re conscious of its pitfalls, it can be
    used effectively in a program. Cranium crushers can grate on the elbows, even with dumbbells so be wary of any ache and build energy and volume slowly.

    Also, since your arms are braced towards the Scott curl pad, you can’t swing the
    weights up with your different body components. As a end result, your biceps should handle just about the entire tension by themselves, which puts them in a major position for growing larger and stronger.
    Performing sitting down bicep curls might not seem like anything special in relation to
    building defined biceps. Nonetheless, whenever you do your curls seated
    rather than standing, you can actually carry heavier weights and thus
    overload your biceps with more resistance.
    For our pull movement compound exercise we’re going to
    be focusing on the Barbell Row. I’d such as you to keep the rep vary for these bent-over barbell rows
    on the higher facet, round 10 – 15 reps to keep away from
    heaving the weight with dangerous kind to keep away from danger
    of injury.
    Okay, all you need to do is carry out some high rep
    curls (ideally using fixed tension and brief relaxation periods) to get
    an excellent pump. If you wish to enhance the looks of your upper arms by bettering their size and
    symmetry, then make sure to include one arm Scott curls in your bicep definition exercise.

    This additional resistance will assist to build more bicep muscle mass, which, in addition to
    having a sufficiently low physique fats level, is the sine qua non to building well-defined biceps.
    Most people’s biceps can get extra outlined in the event
    that they lift weights constantly and reduce
    their body fat. But depending on which area of your
    biceps is much less developed (inner vs outer head), you can even build well-defined biceps by improving that lagging area with particular workouts.

    Bigger biceps are sometimes seen as the final word sign of strength
    and aesthetics. But whereas many gym-goers rely on traditional curls to construct their arms, not all biceps workouts are equally efficient.
    To get into the chin up starting position we now have to
    have a supinated forearm. We additionally get flexion of the shoulder to assist
    us get peak contraction of the biceps muscle fibers because we’ve our arm out in entrance of our body to seize the bar.

    «Keep your core tight all through, and avoid initiating the upward movement of the barbell by using your decrease again and hips to generate momentum,» she says.
    When we use a pronated position, we shift the
    load to the elbow flexor, which is the brachialis.
    This portion of the series might be carried out with a pronated grip / overhand grip.

    Constructing bicep energy effectively by lifting heavier than normal as a outcome of the burden distribution on a barbell is easier to carry than with dumbbells.
    The burn comes quicker and feels more effective, resulting in hypertrophy («gains») as a outcome of you’re doing double the
    reps as you raise one arm at a time. Maintaining pressure within the
    biceps through the curl makes your muscular tissues work
    successfully through time beneath pressure.
    If you should drop weight, that’s completely acceptable because
    your upper arms might be more engaged than in different curl exercises.
    The semi-supinated grip additionally will increase brachialis and brachioradialis
    engagement, which are smaller but no much less important arm muscle tissue.

    When it involves arm coaching, one muscle in particular all the time appears to hog the spotlight.

    The biceps brachii is the large two-headed muscle that makes up a lot
    of your upper arm, however it doesn’t work alone. Traditionally, it was
    well-liked to train every main muscle group once a week—e.g., chest day on Monday, legs on Tuesday, back and biceps on Wednesday, and so forth.
    This was regarded as the best break up for muscle growth because it gave every
    muscle group a full seven days to recuperate earlier than working it once more.

    In this text, we’ve suggested sticking to a rep range of
    8-12 reps for 3-4 sets. If your objective is
    construct measurement, that is the optimum rep vary for hypertrophy, so choose an appropriate weight that allows you to stay inside this
    rep range whereas still feeling challenged.

    This exercise combines the experts’ picks into one
    killer coaching session. We suggest doing this exercise on its own and not paired with one other bigger physique part beforehand, so you’re fresh
    and at your strongest. Really Feel free to make use of one
    or two of the «Intensify It» methods outlined within the article.
    Grasp an overhead bar with an underhand grip, arms spaced just
    a few inches apart.
    You must continually switch up your coaching routine to keep away from hitting an overhead ceiling.
    Many lifters make the error of heading proper into
    their workout as soon as they step into the gym. Neglecting to heat
    up your goal muscle tissue will increase your
    odds of damage. Biceps are particularly vulnerable to tears
    should you do too much too soon.
    It’s simply that you just’re most likely
    doing it mistaken – curls will solely get you so far. In fact,
    there are loads of bicep workouts out there, more
    than sufficient to make your whole coaching classes unique, and we’ll present you the most effective ones.
    The standard shoulder-width grip tends to hit each the lengthy
    and quick head of the two-headed biceps muscle well, but you probably can adjust your grip to emphasise certainly one of
    them more.
    Reverse curls drive your brachialis and forearm muscles to do extra of the work.
    In addition, they are a good way to boost your grip strength.

    Incorporating bicep workout routines into your higher physique exercises
    is the best approach to construct confidence and swagger in your
    arms. Biceps brachii – the full name for the muscle on the front
    of your higher arm is biceps brachii, which means two-headed arm muscle.
    Recognized as the biceps for short, this muscle is
    responsible for flexion of the elbow, flexion of the shoulder, and supination of the forearm.
    The biceps have two heads (the long head and the quick head) which check with the place
    they connect onto the shoulder joint. In this 30-minute dumbbell exercise to build your biceps, we’ll hammer through these seven moves in a circuit.

    Look at pictures of him posing and you’ll notice that
    he would typically twist his upper body in such a way that he’d
    end up facing the digital camera or the judges whatever the pose.
    This gave him the looks of having a smaller waist, and
    was an important technique for him in competitors.
    I’m Murshid Akram, a personal coach, fitness blogger, and founder of thefitnessphantom.com.
    I primarily design workout plans and share science-based and practical information that may allow you to become
    stronger, practical, and more healthy.
    «Intensity» refers to how close to failure you perform an exercise.
    It is essential to train by way of a full range
    to make certain you practice the physique of the muscle fully.
    Dumbbells allow you to concentrate on one arm at a time, making sure they get the same
    work done and helping to minimize any asymmetries. This can be especially useful if you’re struggling
    to get a great mind-muscle connection.
    It is vital to balance coaching and recovery to reduce injury threat and burnout.
    This will range significantly from person to
    person and depend in your exercise split! In basic,
    we propose choosing 2 to four bicep workout routines
    to pair along with your again exercises or different upper body actions.

    Even only one exercise will provide advantages, but more volume has been found to immediately correlate with elevated muscle hypertrophy [8].
    It places the arm in an externally rotated place, challenges the biceps differently, and
    engages the shoulders more than other bicep curl variations to
    stabilize the motion. The high position of this exercise primarily targets
    the short head of the bicep, which is recruited to stabilize the shoulder joint.
    Another cause we love these is that they’re carried out in a standing position, which implies they activate your biceps, core, and glutes as stabilizers.

    Once More, this varies significantly from person to person, however typically, it takes 6-8 weeks to note a change in appearance and
    12 weeks to see vital changes, though this may be longer.
    It’s really going to rely on your current training (including frequency), diet,
    and genetics. This is a hard query to reply, however it’s going
    to depend on your coaching experience and strength ranges to your private training objectives, whether
    they be aesthetic or athletic. But the short-head, on the opposite hand, is emphasized by inner rotation. I
    attached electrodes to my pores and skin; hooked myself
    up to an electromyography or EMG machine and measured the level of muscle
    activation in each motion. If you want to work one
    head of your bicep greater than the opposite, it all comes right
    down to positioning.
    Start by warming up your muscle tissue with a minimum of 5 minutes of cardio.
    Jumping jacks, a fast jog, or a spin on the elliptical will work to get your blood pumping
    and cut back your danger of injury. Start together with your palms wrapped intently around the chin-up bar, thumbs dealing with
    you.
    This is ideally carried out in a squat rack with a barbell,
    but you have a few options should you don’t have one.
    If you could have two very steady chairs and a powerful pole or bar you could set on the tops of the chairs again rest, but watch out as you have to make sure it is secure and
    the bar can support your weight. Related to the mendacity double leg hammer curl above besides your using your legs as resistance and
    not your torso. Now as you’re at the prime of
    the sit-up, your core power comes into play to carry this place.

    You need to actively resist along with your legs right here to supply the
    required resistance. As a complete, the first perform of the biceps is elbow flexion (aka curls).
    The biceps supinate the forearm as well (rotate the forearm laterally), and this movement
    is extra highly effective when the elbow is flexed.
    Not Like common curls, hammer curls completely ‘hammer’ the brachialis and brachioradialis in addition to the
    biceps. So you might get ahead of the pack now (even as a beginner) by
    prioritizing muscular tissues that most people overlook.
    For bicep body weight workout routines which may
    be tough, like chin ups, you’ll have to simply do
    your finest with rep and time beneath tension. However the great thing
    is, you’ll be able to easily progressive overload by
    doing more reps after which eventually adding an external load like a weighted vest.

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