Описание
2017 году Европейская Комиссия (ЕК) разрешила применение препарата Дарзалекс у взрослых с множественной миеломой, в комбинации с леналидомидом, бортезомибом и/или дексаметазоном.
Результаты исследований показали, что препарат Дарзалекс, с основным действующим веществом — даратумумаб, в составе комбинированной терапии приводит к глубокому и длительному ответу у пациентов, в независимости от наличия у них цитогенетических изменений. Полученные данные подтверждают способность препарата Дарзалекс приводить к устойчивому клиническому улучшению в сочетании с часто применяющимися схемами лечения и улучшения неблагоприятных исходов, связанных с цитогенетическими изменениями, являющимися фактором высокого риска.
Препарат Дарзалекс является первым в своем классе биологическим препаратом, который действует на поверхностный белок CD38, который в значительной степени экспрессирован на всех миеломных клетках, независимо от стадии заболевания.
Препарат Дарзалекс индуцирует быстрое разрушение опухолевых клеток в результате апоптоза (запрограммированной гибели клеток), а также за счет некоторых иммунных механизмов действия, к которым относятся:
- комплементзависимая цитотоксичность (КЗЦ),
- антителозависимая клеточная цитотоксичность (АЗКЦ),
- антителозависимый клеточный фагоцитоз (АЗКФ).
Дарзалекс оказывает также иммуномодулирующее действие, способствующее разрушению опухолевых клеток за счет снижения количества иммуносупрессорных клеток, таких как регуляторные T- и B-лимфоциты, а также миелоидных клеткок-супрессоров.
В настоящее время планируются или проводятся дополнительные исследования с целью оценки вероятности использования препарата Дарзалекс для лечения других злокачественных и предраковых заболеваний, при которых экспрессируется белок CD38.
Состав Дарзалекс
1 флакон препарата содержит
- активное вещество — даратумумаб 100 мг или 400 мг,
- вспомогательные вещества: кислота уксусная ледяная, натрия хлорид, натрия ацетата тригидрат, маннитол, полисорбат 20, вода для инъекций.
Показания к применению Дарзалекс
- в качестве монотерапии у больных с рецидивирующей или рефрактерной множественной миеломой.
Фармакодинамика
Даратумумаб — это человеческое моноклональное антитело иммуноглобулин IgG1κ, которое взаимодействует с белком CD38, экспрессирующейся на поверхности клеток при различных гематологических злокачественных патологиях, включая клетки множественной миеломы, а также другие типы клеток и тканей. Белок CD38 обладает множеством функций, включая опосредованную рецепторами адгезию, ферментативную и сигнальную активность.
In vivo была продемонстрирована способность препарата Дарзалекс к мощному подавлению роста экспрессирующих CD38 белок опухолевых клеток. По данным in vitro исследований даратумумаб может вызывать опосредованную иммунной системой гибель опухолевых клеток за счет множества эффекторных функций. .По данным этих исследований предполагают, что даратумумаб способен индуцировать лизис опухолевых клеток посредством:
- комплементзависимой цитотоксичности,
- антителозависимой клеточной цитотоксичности,
- антителозависимого клеточного фагоцитоза при злокачественных новообразованиях.
Иммуногенность
У больных, в клинических исследованиях получавших препарат Дарзалекс, неоднократно проводился анализ образования антител к даратумумабу в течении всего времени лечения и в течение периода до 8 недель после её окончания. после начала терапии препаратом Дарзалекс ни у одного из пациентов не было выявлено антител к даратумумабу.
Данные по иммуногенности в довольно большой степени зависят от специфичности и чувствительности используемых методов анализа. Также, ряд факторов может повлиять на наблюдаемую частоту положительных результатов анализа, включая:
- условия хранения взятых образцов,
- время взятия образцов,
- влияние других препаратов,
- сопутствующая терапия,
- изучаемое заболевание.
Таким образом, сравнение частоты появления антител к даратумумабу может послужить основанием для неверных выводов.
Фармакокинетика
После внутривенного введения фармакокинетику даратумумаба изучали у пациентов с рецидивирующей и рефрактерной множественной миеломой при применении в дозировках от 0,1 до 24 мг/кг. Для описания характеристик фармакокинетики препарата, а также для оценки влияния ковариат на распределение даратумумаба у пациентов с множественной миеломой, была разработана модель популяционной фармакокинетики даратумумаба. Популяционный анализ фармакокинетики включал 223 пациента в двух клинических исследованиях, 150 пациентов получали препарат в дозировке 16 мг/кг.
В группах, получавших 1-24 мг/кг, максимальная концентрация в плазме (Сmax) после первой дозировки повышалась приблизительно пропорционально дозировке, объем распределения соответствовал первоначальному распределению в плазме. наблюдалось снижение клиренса по мере увеличения дозировки, кроме того, увеличения площади под кривой «концентрация- время» (AUC) происходило с опережением прямой пропорциональности дозе. Это вероятно свидетельствует о возможном насыщении CD38 при более высоких дозировках, после чего влияние опосредованного мишенью клиренса сводится к минимуму, и клиренс препарата Дарзалекс приближается к линейному клиренсу, характерному для эндогенного иммунноглобулина G1. Также наблюдалось снижение клиренса, после многократного введения, что вероятно может быть связано с уменьшением опухолевой нагрузки.
С увеличением дозы и при многократном введении препарата терминальный период полувыведения повышается. После первой инфузии в дозе 16 мг/кг среднее значение (стандартное отклонение) расчетного терминального периода полувыведения даратумумаба было равно 9 дней. Среднее значение (стандартное отклонение) периода полувыведения для неспецифичной линейной элиминации на основании популяционного анализа фармакокинетики было равно примерно 18 дней. Данный терминальный период полувыведения можно ожидать при многократном введении даратумумаба и в случае полного насыщения опосредованного мишенью клиренса.
Примерно через 5 месяцев на фоне перехода к инфузиям каждые 4 недели (к 21-ой инфузии) на основании популяционного анализа фармакокинетики достигается равновесное состояние даратумумаба, среднее (стандартное отклонение) соотношение значений максимальной концентрации Сmax в равновесном состоянии и максимальной концентрации Сmах после первой дозировки было равно 1,6. Среднее значение (стандартное отклонение) центрального объема распределения было равно 56,98 мл/кг.
Масса тела на основании популяционного анализа фармакокинетики была идентифицирована как статистически значимая ковариата клиренса препарата Дарзалекс. Таким образом, подбор дозировки по массе тела является подходящей стратегией для расчета дозировки у пациентов с множественной миеломой.
Особые группы пациентов
Возраст и пол
На фармакокинетику даратумумаба на основании популяционного анализа фармакокинетики возраст (диапазон: 31-84 года) не обладает клинически значимым эффектом. Концентрация даратумумаба была схожей у более молодых (возраст <65 лет) и пожилых (возраст ≥65 лет) пациентов.
Пол не влиял на концентрацию препарата Дарзалекса.
Пациенты с нарушением функции почек
Не проводилось исследования препарата Дарзалекс у пациентов с нарушением функции почек. На основании имеющихся данных по функциональному состоянию почек у пациентов, получавших препарат Дарзалекс, был выполнен популяционных анализ фармакокинетики включая:
- 71 пациента с нормальной функцией почек (клиренс креатинина ≥90 мл/мин),
- 78 пациентов с нарушением функции почек легкой степени (клиренс креатинина <90 и ≥60 мл/мин),
- 68 — с нарушением функции почек средней степени (клиренс креатинина <60 и ≥30 мл/мин),
- 6 — с нарушением функции почек тяжелой степени (клиренс креатинина <30 мл/мин).
Не было выявлено между пациентами с нарушением функции почек и с нормальной функцией клинически значимых различий концентрации даратумумаба.
Пациенты с нарушением функции печени
Не проводилось исследования препарата Дарзалекс у пациентов с нарушением функции печени. С целью оценки влияния нарушения функции печени, был проведен популяционный анализ фармакокинетики определенного в соответствии с критериями дисфункции печени, на клиренс даратумумаба с использованием имеющихся данных по функциональному состоянию печени у 223 пациентов. Клинически значимых различий концентрации даратумумаба между пациентами с нарушением функции печени легкой степени (концентрация общего билирубина 1-1,5 верхней границы нормы или активность аспартатаминотрансферазы выше верхней границы нормы) и с нормальной функцией печени (концентрация общего билирубина и активность аспартатаминотрансферазы ≤ верхней границы нормы) не было выявлено. Использование препарата Дарзалекс не изучалось у пациентов с нарушением функции печени средней степени (концентрация общего билирубина >1,5-3 верхней границы нормы и любая активность аспартатаминотрансферазы) или с нарушением функции печени тяжелой степени (концентрация общего билирубина >3 верхних границ нормы и любая активность аспартатаминотрансферазы).
Фармацевтические характеристики
Концентрат для приготовления раствора для инфузий в виде прозрачной или опалесцирующей, бесцветной жидкости или жидкости с коричневатым или коричневато-желтоватым или желтоватым оттенком, в котором могут содержаться единичные частицы белка.
Упаковка, срок годности, условия хранения Дарзалекс
- 5 мл укупорены во флаконы из стекла I типа, с прорезиненной крышечкой и вместе с инструкцией упакованы в картонные пачки.
- 20 мл укупорены во флаконы из стекла I типа, с прорезиненной крышечкой и вместе с инструкцией упакованы в картонные пачки.
Препарат следует хранить в недоступном для детей, защищенном от света месте, при температуре от 2° до 8°С. Не замораживать. Не встряхивать.
Срок годности — 24 месяца. Не применять по истечении срока годности.
После приготовления раствор можно хранить при температуре от 2° до 8°С в защищенном от света месте не более 24 ч.
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 Дарзалекс (даратумумаб) в Алматы
Заказать и купить Дарзалекс (даратумумаб) в Казахстане
Позвоните и узнайте цену Дарзалекс (даратумумаб)
Работаем и отправляем Дарзалекс (даратумумаб) по странам СНГ: Россия, Украина, Кыргызстан (Бишкек), Белоруссия, Узбекистан (Ташкент),
а также можем отправить Дарзалекс (даратумумаб) по регионам Казахстана: Нур-Султан (Астана), Шымкент, Талдыкорган, Актау и другие.
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So we’ve collected our record of the highest 8 shoulder workout routines that you should try to include in your exercise.
One of probably the most aesthetically appealing muscle
groups is your shoulders. Nonetheless, constructing spectacular boulder shoulders could be challenging.
Training shoulders with dumbbells can improve your physique, improve
shoulder power, improve posture, and help with
bilateral muscular imbalances. I program the dumbbell face pull
into my athletes’ routine during a power section. This
train directly correlates to higher back power, so working on the
rounded shoulder physique can be beneficial.
Suppose about driving the elbows up and back, and pulling the middle of the rope in the course of your forehead.
You will need a barbell for this one and, ideally, a landmine anchor (or an alternative
way to securely anchor one facet of the barbell to the floor).
If you’re uncertain what a barbell landmine is or the place to find one, they’re
often connected to the underside of the squat/power rack within the fitness center (check out What Is A Barbell Landmine?).
As the name implies, this train takes the chest flye and inverts the muscular tissues affected.
They’re also great to introduce on back/shoulder workout classes.
To make real positive aspects on your shoulders, you should give them
a centered exercise.
The anterior or entrance deltoid is primarily responsible for shoulder
flexion and horizontal adduction. That is elevating your arm in entrance of you (e.g., entrance
raise) and performing a chest fly motion [1,2]. The barbell
overhead carry places your body underneath lots of tension whereas constructing shoulder strength and
mass. What’s higher is that the exercise doesn’t only improve your bodily power, but
additionally your mental toughness. Push-ups are one of the efficient,
effective and finest shoulder workouts for males – they’ll goal your chest muscles in the process, too.
The cable face pull targets your trapezius muscle tissue and different areas of
the upper back, including all round strength and
stability to your upper physique.
Additionally, being seated additionally offers a greater,
extra steady base to push from which may place a higher demand on the delts.
Pull-ups are a challenging compound exercise that
targets the shoulders, arms, and back, making them a great addition to
any higher physique exercise. The reverse fly targets the rear
deltoids, enhancing total shoulder steadiness and stability.
If the weight you select is merely too heavy, you threat strain or
damage. If it finally ends up being too gentle, you won’t be getting the exercise you need.
Compared to different joints in our body, such because the elbow or knee,
the shoulder joint can be fairly cellular. This important ball-and-socket
joint permits our shoulders to maneuver in several instructions, like up,
again, and sideways, so it’s simple to exercise. For the larger muscular
tissues of the neck to work as they should, the smaller muscles
have to do their job too. Doing this with weight in opposition to gravity helps
strengthen the smaller posterior neck muscular tissues.
The effectiveness of Reverse Pec Deck Flys in concentrating
on the rear deltoids lies within the mechanics of the motion. As you perform the reverse fly motion, your rear deltoids
are activated to control and execute the motion towards resistance.
This exercise ensures a direct and intense exercise, particularly honing in on these essential shoulder muscles.
What makes the Wide-Grip Lat Pulldown significantly
efficient for the rear deltoids?
From an aesthetic perspective, well-developed rear delts
contribute to a fuller, more balanced upper body (Source).
They add depth and definition to the shoulders, creating a extra pronounced V-shape that’s highly sought after in bodybuilding and health.
Coaching the rear delts not solely complements the entrance
and aspect deltoids but in addition enhances the general appearance of the upper
back. In today’s world, the place many people spend hours hunched over computers or smartphones, training the rear delts is
important for counteracting the widespread ahead shoulder posture.
Strengthening the rear deltoids helps stability the muscle improvement
around the shoulder girdle (Source). This balance is key to maintaining an upright posture, lowering the strain in your neck and
backbone, and stopping the onset of postural points like
kyphosis. Bent over reverse flyes are sometimes accomplished using dumbbells,
but they’re actually far better done using a cable machine.
We’re going to dive deep into the ten best workouts that will beef up your
delts, one of the best methods to project an even bigger body, and some pitfalls to keep away from on the
road to success. Simply ensure you are coaching with sufficient quantity so it leads to adequate stimulus for muscle adaption, but not an extreme amount
of the place you aren’t recovering fully. Moreover, employ the
progressive overload techniques we talked about earlier in this submit.
The key is to give attention to progressive overload, which implies progressively rising your rep rely or the difficulty of those exercises as you get
stronger. Cable front raises are a very efficient, popular anterior deltoid exercise.
Like most cable exercises, they hold the goal muscles beneath near-constant pressure,
producing a deep burn and satisfying pump.
Whereas the anterior deltoid is normally essentially the most well-developed deltoid head, the posterior
deltoid is commonly the least developed. Just as you’d
get bored eating the same dinner every day, your muscle tissue get bored of doing the same workouts.
If you don’t problem your muscular tissues with new actions, your progress will slow
down and could even grind to a halt. Position your dumbbells so they’re according to
your hips and lie back on the ground.
She has over ten years of experience within the health, community development, and communications sectors.
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Now, this prime 10 train we’ve covered are to not be
handled as unique and I would not recommend making an attempt to include all 10
workout routines right into a coaching program. As An Alternative, think about training targets, exercise preferences and experience earlier than deciding
on a selection of the aforementioned workout routines. Leonard’s articles have been printed in lots of prime publications around
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You can carry out this train standing or sitting, and we’d advise utilizing lighter weights.
This is a vital transfer for so incremental all upper physique exercises.
Back coaching is usually ignored in favor
of chest, arms, and shoulders. Nonetheless, a strong back performs a vital role in supporting compound actions like deadlifts, squats, and
bench presses.
Therefore, we recommend that you simply decide one or two workouts per deltoid head (front, aspect, and rear) to work your
shoulder muscular tissues totally, as we do in our
shoulder workout routine. Via focusing on the lateral and anterior heads of the deltoid muscle, upright rows promote wonderful
progress in the upper body area. Often, lifters do the alternative, utilizing gentle weights to prepare their shoulders.
For example, individuals not often perform heavy triples (3 sets
of 3 reps) on the overhead press. Pick up your dumbbells and let them hold straight
down by your sides. Make sure that you just keep your shoulders back, not permitting
them to slump forward at any time in the course of the set.
With solely a slight bend on the elbows, increase
the dumbbells out to the perimeters till your arms are parallel with the ground.
Maintain a dumbbell in the other hand so that it hangs straight down beneath your shoulder.
For each rep, raise your arm until it is parallel with
the ground. Slowly decrease the dumbbell again to
the beginning position, then repeat. After finishing all
reps with one arm, do the identical on the alternative facet.
Many lifters depart their shoulder coaching to probability,
hoping that a few sets of presses and lateral raises are
all they should develop robust, steady, muscular delts.
The different half of your training could be cut up between heavier
hundreds, fewer reps, and higher-rep, lower-intensity training.
Underdeveloped or lagging shoulders outcome from poor training approach, lack of progressive overload, and imbalanced quantities of rear, medial, and front delt
training. Inadequate carbohydrate and protein consumption can also trigger weak
shoulders. Don’t underestimate the degree to which different muscle groups take over when your shoulders fatigue.
Towards the tip of a tough set, your legs, core, and lower back may begin to engage to complete the ultimate reps.
Using dumbbells for trap workout routines helps promote balanced muscular growth.
Since each side of the body works independently,
unilateral coaching with dumbbells helps to establish and proper power imbalances between each
side of the body. This balanced strategy contributes to
symmetrical muscle development and functional strength.
In his spare time he enjoys health of every kind, from deadlifts to lengthy
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Use lighter weights for the elevate strategies than the shoulder
press. Carry Out these seven strikes twice a week and watch as your
shoulders double in measurement. Assume press-up place, then push your hips
up to type an inverted ‘V’. Lower your nose to the ground between your arms, then shift your weight forwards and
raise your chest as your hips lower to the ground.
The further below the rings your torso is, the tougher this train goes to be.
Now that your shoulders are warmed up, we’re getting you yoked up
by throwing within the army press as your finishing
transfer. Dr. Israetel credited the machine lateral elevate for its versatility.
Since you possibly can adjust the burden in addition to how excessive or low
you’re taking the vary of movement, he emphasizes that this could
be one of the more joint-friendly shoulder actions.
Positive Aspects apart, broadening out up high
will increase energy in your other lifts, help with stability, and lessen the prospect of injury.
Rotator cuff muscular tissues are also included, each in shoulder workouts with dumbbells and shoulder
barbell exercises. This shoulder workout routine
utilizes heavy loads, high reps, and compound and isolation workout routines
to hit every variable. Take maintain of a barbell with your hands set at shoulder width,
or just slightly wider.
High Quality reps trump every little thing, and don’t worry when you discover you want to start with a light-weight weight.
I’m having you do three sets of 15, however
you should give attention to doing 15 sets of 1, 3 times.
We’re going to do this train for 4 sets in a
descending style. Ideally, you’re going to add some weight to the
bar and never just allow fatigue to deliver your reps down. In a Aspect Lateral Elevate corresponding to a
dumbbell lateral elevate or a cable lateral increase, arm stops right in conjunction with my physique.
As all the time, begin with a lighter weight, and focus on growing your weights or reps carried out from one week to the following to keep getting larger and stronger.
From the position of your head to your movement, you’re going to
need to overhaul your form. In the most common version of facet lateral raises, you have been probably
distributing pressure among all the other muscular tissues that had
been helping you. The push press is considered one of
the greatest shoulder workout routines to show this.
Making your shoulders seem wider requires emphasizing the center delts.
Doing so helps broaden your V-taper while creating the phantasm of a
smaller waist. The key to the exercise, after all, is to
do extra actions that focus on the center delts.
Even if you don’t have an exclusive shoulder day, work your
shoulders first on your higher physique workout or urgent day.
The shoulders are sometimes thrown in with the arms, nearly as an afterthought.
In reality, your deltoids are extremely essential for performance and aesthetics, which
implies they need to be handled as a primary muscle. The shoulder is an advanced muscle
in that it has three completely different heads that
every one have distinctive capabilities (we’ll speak
about this extra within the subsequent section). Therefore, you
should hit the deltoids from all directions to optimize your coaching.
So, when you have tried your share of normal facet lateral raises
and discover that you’re still fitting via most
doorways far too simply, give the following workouts
a strive.
If the push press is extra of an athletic energy exercise, the seated dumbbell press
is extra of a bodybuilding train. The overhead press is
as old because the barbell itself, and is possibly one
of the best shoulder train of all. Jacked Gorilla was based in 2013,
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Shoulder joints could be prone to injury,
so you should consider proscribing training your shoulders intensely
to at least one or two classes per week.
It’s slightly more advanced than some other shoulder exercises, so practice form using decrease weights,
to start with. Lateral raises increase muscle growth within the triceps and
shoulders and work to improve your shoulder mobility.
Whereas bent-over reverse flyes aren’t an train you’ll be performing daily, they’re beneficial for classes the place you wish to target
a spread of shoulder and back muscle tissue. Our next barbell-related shoulder exercise brings in a extensive range of muscle groups to deliver excellent full-body conditioning.
Carry Out dumbbell shrugs on days when you’re in search of a exercise that targets your shoulders, specifically your traps.
If you don’t have access to weights or the gym, the pike pushup lets you actually work
your shoulders using just your physique weight.
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