Описание
Препарат Келикс (Сaelyx) оказывает цитотоксическое противоопухолевое действие – останавливает рост опухоли, ингибирует развитие злокачественных клеток, препятствует появлению метастаз. Действующее вещество препарата Доксорубицин — это цитотоксический антрациклиновый антибиотик, выделяемый из Streptomyces peucetius var. caesius. Точный механизм противоопухолевого действия доксорубицина неизвестен. Вероятно, что цитотоксическое свойство связано с его способностью угнетать синтез ДНК, РНК и белков путем внедрения доксорубицина между основаниями соседних пар двойной спирали ДНК, что блокирует разворачивание спирали для дальнейшей репликации.
Состав
1 мл препарата содержит
действующее вещество — доксорубицина гидрохлорид 2.00 мг (эквивалентно 1.87 мг доксорубицину),
вспомогательные вещества: N-(карбонил-метоксиполиэтиленгликоль 2000)-1,2-дистеароил-sn-глицеро-3-фосфоэтаноламина натриевая соль (MPEG-DSPE), фосфатидилхолин полностью гидрогенизированный соевый (HSPC), аммония сульфат, холестерин, гистидин, сахароза, натрия гидроксид или кислота хлороводородная, вода для инъекций.
Показания к применению
- распространенный рак яичников (при неэффективности химиотерапии препаратами платины),
- монотерапия метастатического РМЖ (при наличии повышенного риска кардиологических осложнений),
- прогрессирующая множественная миелома (в комбинации с бортезомибом) у больных, получивших один или более курс химиотерапии (возможно перенесли трансплантацию костного мозга),
- для системной терапии первой линии или второй линии у больных со СПИД-ассоциированной саркомой Капоши (развивающейся на фоне комбинированной системной терапии, содержащей, по крайней мере, два из следующих веществ – винка алкалоид, блеомицин и стандартный доксорубицин (или другой антрациклин), или лиц, которые не переносят такую терапию).
Фармакодинамика
Препарат Келикс — это пегилированная липосомальная форму доксорубицина, способная длительно циркулировать в крови и обеспечивать более высокое содержание доксорубицина в опухолевых тканях, чем в нормальных тканях. Липосомы содержат поверхностно- связанные гидрофильные полимеры метоксиполиэтиленгликоля (MПЭГ). Эти линейные группы MПЭГ образуют выступающую над поверхностью липосом защитную оболочку, уменьшающую вероятность взаимодействия между компонентами плазмы и липидной двухслойной мембраной. Данная особенность защищает липосомы от распознавания фагоцитарной системой и способствует удлинению времени циркуляции Келикса. Пегилированные липосомы имеют также внутреннюю водную буферную систему и липидную матрицу с низкой проницаемостью, что в сочетании позволяет удерживать доксорубицин внутри липосомы во время циркуляции ее в кровотоке. Довольно маленький размер пегилированных липосом (средний диаметр приблизительно составляет 100 нм) способствует им проникать через дефекты кровеносных сосудов опухоли. По данным результатов экспериментальных исследований показано о проникновении пегилированных липосом из кровеносных сосудов и их кумуляции в опухоли.
В рандомизированном исследовании III фазы Келикс сравнивался с доксорубицином у 509 пациенток с метастатическим раком молочной железы. Это исследование подтвердило, что Келикс по эффективности не уступает доксорубицину. При анализе выживаемости без прогрессирования отношение рисков составило 1.00 (95% доверительный интервал при отношении рисков 0.82-1.22). Значение отношения рисков, рассчитанное с поправкой на прогностические факторы, соответствовало его значению в популяции пациентов с назначенным лечением.
При лечении препаратом Келикс риск развития кардиотоксичности, который зависит от кумулятивной дозы антрациклина, был значительно ниже, чем при применении доксорубицина (отношение рисков 3.16, p<0.001). При кумулятивных дозах препарата Келикс более 450 мг/м2 клинические признаки кардиотоксичности отсутствовали.
В рандомизированном, открытом, многоцентровом исследовании III фазы оценивали безопасность и эффективность комбинированной терапии препаратом Келикс с бортезомибом и монотерапии бортезомибом у 646 больных множественной миеломой, получивших по крайней мере одну линию терапии, у которых не было замечено прогрессирования во время терапии на основе антрациклина. Комбинированная терапия препаратом Келикс с бортезомибом привела к значительному увеличению времени до прогрессирования (первичная конечная точка) по сравнению с монотерапией бортезомибом. Снижение риска составило 35% (95% ДИ 21-47%, p<0.0001; всего было зарегистрировано 407 исходов). Медиана времени до прогрессирования составила 6.9 месяцев при монотерапии бортезомибом и 8.9 месяцев при применении препарата Келикс с бортезомибом. По данным промежуточного анализа, предусмотренного протоколом (когда было зарегистрировано 249 случаев прогрессирования) исследование было досрочно прекращено, исходя из более высокой эффективности комбинированной терапии. При промежуточном анализе выявлено снижение риска прогрессирования на 45% (95% ДИ 29-57%, p<0.0001). Медиана времени до прогрессирования у лиц, получавших монотерапию бортезомибом составила 6.5 и 9.3 месяцев при комбинированной терапии с препаратом Келикс и бортезомибом.
Фармакокинетика
Фармакокинетика препарата Келикс значительно отличается от фармакокинетики стандартных препаратов доксорубицина гидрохлорида. В низких дозах (10-20 мг/м2) Келикс обнаруживает линейную фармакокинетику, в более высоких дозах (10-60 мг/м2) – нелинейную. Стандартный доксорубицина гидрохлорид имеет быстрый клиренс (24-73 л/г/м2) и значительное распределение в тканях (объем распределения: 700-1100 л/м2). В отличие от него Келикс находится преимущественно в объеме кровяной жидкости и клиренс доксорубицина из крови зависит от липосомального носителя. Вещество становится биодоступным после транссудации липосом и их попадания в ткани.
Для препарата Келикс, представленного преимущественно пегилированным липосомальным доксорубицина гидрохлоридом (содержащего от 90% до 95% измеренного доксорубицина), при применении эквивалентных дозировок величина площади под кривой (AUC) и концентрация в плазме значительно выше показателей, полученных для стандартных (непегилированных нелипосомальных) композиций доксорубицина.
Фармакокинетический профиль доксорубицина показывает на то, что его клиренс из плазмы ориентируется на его липосомный носитель. Доксорубицин становится доступным только после выхода липосом из кровяного русла и проникновения их в ткани.
В низких дозах (10-20 мг/м2) препарат демонстрирует линейную фармакокинетику, в более высоких дозах (20-60 мг/м2) — нелинейную.
Показатели фармакокинетики при введении в дозировке от 10 до 60 мг/м2: клиренс доксорубицина — в среднем 0.03 л/ч/м2 (0.008-0.152 л/ч/м2), объем распределения – 1.93 л/м2 (0.96-3.85 л/м2), период полувыведения – 73.9 ч (24-231 ч).
Фармакокинетика в особых клинических случаях
Фармакокинетические показатели при гипербилирубинемии и нарушении функции печени отличаются незначительно от фармакокинетических параметров нормальной концентрации общего билирубина.
На фармакокинетические параметры почечная недостаточность (КК 30-156 мл/мин) не оказывает влияния. Данных по фармакокинетике препарата у пациентов с клиренсом креатинина менее 30 мл/мин нет.
На фармакокинетические показатели препарата Келикс возраст пациентов (21-75 лет) не оказывает существенного влияния.
Популяционная фармакокинетика
Популяционный анализ фармакокинетики препарата Келикс проводили у 120 пациентов, принимавших участие в 10 клинических исследованиях. Фармакокинетика препарата Келикс в диапазоне доз 10-60 мг/м2 описывалась двухкамерной нелинейной моделью нулевого порядка. Клиренс препарата Келикс составил в среднем 0.030 л/ч/м2 (0.008-0.152 л/ч/м2); объем распределения – 1.93 л/м2 (0.96-3.85 л/м2); период полувыведения – 73.9 ч (24-231 ч).
Фармацевтические характеристики
Концентрат для приготовления раствора для инфузий 2 мг/мл. Описание полупрозрачная суспензия красного цвета.
Упаковка, срок годности, условия хранения
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Shut Grip Push-Ups are an ideal different if you’re really restricted on gear.
As such, the shut grip barbell curl is a valuable exercise for lifters who already
have a solid basis of mass and want to bring up their weak points.
Yet, the movement is also useful for beginners as a end result of it
has you press your elbows towards your torso as you raise the load, which minimizes cheating and keeps tension on the target muscle tissue.
The proven reality that you’re lifting an Olympic bar signifies that
the shut grip barbell curl is an effective mass-building movement.
This is as a result of barbells allow you to overload the goal muscles with more resistance than any other training
software. Primarily all you’re doing right here is using momentum to cheat
the load up. This will increase the chance of harm
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tissues.
However, what the barbell bench press does is construct strength that transfers over to things we do outside of the gym.
Getting stronger is always better, and this train builds power by the bucket load.
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After 30 hours of research and testing 40 multi-grip
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Extend your arms straight up and grip the barbell about shoulder width apart.
A good rule of thumb is to maintain your grip width around
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The wide-grip barbell curl variation is among the many hottest and extremely favored variations.
With your arms gripping the barbell in a supinated group wider than shoulder-width, it is
done. The extensive grip for a wide grip barbell curl ought to
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of the exercise, and alternative ways to do it.
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The entrance squat is a common squat variation used in Olympic weightlifting
training, contemplating the function entrance squat power plays within the clear
and jerk. Nonetheless, this motion has nice carryover with all other strength
and conventional sports athletes.
We’ve gone over all the reasons why you must do it, however now we’re at crucial half.
Make positive you employ correct kind so you’re getting as a lot
out of this train as possible. Examine out our strength standards for Barbell Curl, Pendlay Row, Pull Ups,
and more. Focus on maintaining your elbows tucked in, it’s easy to by accident let them rotate outwards.
Don’t just drop the barbell – actively information it back down slowly.
The effectiveness of the Conjugate Method can be attributed to the system’s capability to address…
The close-grip bench is perhaps the most typical assistance exercise for the bench press – an assistance train being outlined as a
variation of the basic exercise. In this case, it is a full
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within the competitive version of the movement, just like a stiff-legged deadlift or a low-box squat.
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presses on an incline bench. To get probably the most out of this motion, you must experiment with with a
beginning place at angles from 15 to 45-degrees. To
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inhale, and grab the bar with a double overhand grip.
Contract the traps to elevate the shoulders, squeeze onerous on the high, and slowly lower the bar again to the beginning place.
By following these directions, you can perform the barbell shrug train with correct form and maximize your features.
If nothing else, switching to an underhand grip will let you
do extra reps or raise slightly extra weight than traditional.
You could make reverse grip rows safer by doing them with a slightly arched and by no means rounded lower back.
You must additionally brace your core and stop your sets before your kind begins to interrupt down. This is
good news for anybody who does bodyweight or resistance band training,
the place excessive reps are the norm.
The barbell shrug is a extremely effective train for constructing a stronger and more resilient
upper back, while also decreasing the risk of injury.
Despite its association with the universal gesture of confusion, this compound carry can ship spectacular gains in muscle
mass and power for the traps. Keep Away From swinging the burden up using your body when performing the Barbell
Seated Close-grip Concentration Curl. This is a common mistake that may lead to ineffective results and potential injuries.
It’s essential to maintain proper type throughout the train to ensure maximum benefits and minimize
the danger of injury. Today’s star of the present may have your palms lined up immediately according to your shoulders in a shoulder width
grip. This will allow you to hold your arms nearer to
your body as you lower the load.
At Westside, we’ve an amazing quantity of experience
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Regardless of whether or not you have a bicep harm or not,
close-grip pulldowns are massively effective. As are chin-ups – one other Cavaliere recommendation – because of the compound nature of the movement utilizing a number
of muscle teams and sharing the load on different joints apart from the elbow.
I was making an attempt to forestall my son from falling on the ice after
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Cavaliere recommends the close-grip pulldown over the
rest as it really works everything of the bicep muscle.
That mentioned, there are circumstances where it’s necessary so that you
just can sprinkle isolation actions into your arms programming.
The barbell seated close-grip concentration curl targets particular
muscle tissue in your arms, including the biceps and brachialis.
By focusing on these muscle tissue, this train helps to build energy
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close grip bench press is the master at constructing your lockout in your bench press.
The Place the wide-grip bench press shortens your range
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backside of the exercise. The barbell upright row is an efficient way to
build stronger shoulders, traps, and higher again muscle tissue.
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Typically speaking, it’s the variation the place you’ll have the power
to lift essentially the most weight. A well-balanced triceps workout should embody a mixture of compound and isolation exercises.
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heavy, whereas isolation exercises like cable pushdowns and dumbbell overhead extensions concentrate on specific tricep heads.
Unlike the the close grip bench press, the usual grip goes to encourage more pec and delt
activation due to the change in biomechanics.
This is why you’re more more likely to see the standard grip barbell
bench press as a staple in muscle constructing routines.
Similar to the close-grip bench press, chest dips are an effective compound exercise that strengthens your
pectorals, deltoids, and triceps. However, as a substitute of performing the motion whereas mendacity on a bench, you leverage your physique weight
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and raise yourself.
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regular bench press energy may also get a pleasant increase.
With this barbell tricep exercise, you’ll carry out nine to 12 sets of triceps training per workout at intermediate to superior ranges.
The triceps, officially known as the triceps brachii, is the muscle on the
again of your upper arms.
Make certain to always use weight clips everytime you use a
barbell, to prevent the plates from sliding off.
You can also use the EZ bar, which is more snug
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Moreover, adding pauses at different points in the carry
can also add an extra challenge and exploit any weaknesses off the chest
or on the sticking level of the lift. An instance could
be basketball players who pass the ball off
the chest to other gamers but additionally include netball,
boxing, rugby, and American soccer athletes.
Verify out my different article on alternatives to the bench press that
will help activate the higher pecs. Using an EZ bar—a shorter bar with a piece that zig-zags—provides
areas to grip that can relieve discomfort in your wrists.
Its distinctive shape permits you to position your grip more ergonomically.
You can learn extra about this in our article Does
the Bench Press Work Your Triceps? This is the place most
people find yourself having a hard time with the train. Ideally,
your palms must be shoulder-width or just inside shoulder-width aside, permitting
for optimal muscle engagement without overloading the joints.
Body Weight actions such as inchworm with push up, wall slides, band
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To maximize your close grip bench press performance and restoration, deciding on the right dietary supplements
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It doesn’t goal the heads of our triceps equally; it’s just pretty a
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Maybe most of all, it’s one of the best possible assistance lifts
for powerlifters who are trying to increase their bench
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version of the barbell bench press, however it’s certainly a extra specialised variation. It’s
an even bigger compound lift that’s a bit extra intuitive to be taught,
and it will do a better job of stimulating your complete
chest as nicely as your shoulders, upper chest, and triceps.
To get the most out of this exercise, it’s essential to do the correct exercise method.
Proper form and beginning place will ensure that your train is successfully carried
out and can scale back your risk of damage.
A shut grip bench press is sometimes called any bench press where the hands are placed closer together than what you’d sometimes use
to bench press. Skull crushers are one other train that can enhance
triceps energy; nonetheless, the close-grip bench press might be
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routines and one I consider should be in virtually any program attempting to develop upper physique dimension and strength.
In a Commonplace Bench Press, your hands are spaced wider
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(pectoralis major) and less in your triceps. Equally, athletes and lifters with elbow pain would possibly discover the narrower grip
much less aggravating, highlighting the importance of aligning bench variations
with private health considerations and health objectives.
Focusing on the triceps through the Close Grip Bench Press, by consciously
contracting and lengthening them, enhances
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Snatch Grip Shrugs is a little-used variation apart from presumably Olympic
weightlifters. Barbell Shrugs are top-of-the-line workout routines for
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These kinds of sport athletes would profit as a outcome of
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stored near the body or they need robust elbow extension. This is also an important consideration for other sport athletes the place shoulder health and recovery is necessary and who don’t wish
to add any difficult horizontal urgent work for the shoulders.
Flex your triceps as you drive the barbell again up until your arms are totally prolonged.
Lay on a flat bench and unrack your barbell with a shoulder width grip.
You can put your palms within the in style diamond formation should you like, but really
the key is keeping your elbows tight to the body all through the
movement.
To execute it, the beginning place of your dumbbells ought to
be nearer than shoulder width. This exercise is carried
out with decrease reps to achieve more strength or with higher reps for extra muscle progress.
You would be hard pressed to discover a lifter with a bench press that is
price a shit that has small triceps.
In Distinction To the usual bench press, the
narrower grip places a heightened emphasis on the triceps whereas nonetheless recruiting
the chest and shoulders. This makes it a great movement for athletes
trying to improve lockout energy, bodybuilders aiming for defined arms, and health fanatics looking for well-rounded pressing
power. Professional athletes will often perform compound exercises such
as the shut grip bench press as it pertains to their
sporting requirements. For instance in rugby or wrestling,
you will want to usually push heavy opponents away from you.
This requires your whole physique to have the ability to supply
and exhibit pressure, which is precisely what you
training when performing the shut grip bench press. The close-grip dumbbell bench
press is a well-liked variation of the dumbbell bench press.
The shut grip bench press is an effective barbell exercise that may add some further fatigue and depth for those trying to grow the muscle
area. What we’re seeing right here is that as you deliver your
grip in narrower, the second arm between your palms and your sternum shrinks, decreasing the demands
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This makes it a poorer variation for gaining overall pec measurement and
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down in your torso, which will increase the second arms
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To do the close-grip bench press, set up for an everyday bench press—feet planted firmly,
a strong arch, shoulder blades down and back—but grip the barbell with a narrow
grip. After doing a little warm-up sets with a lighter weight,
your body will intuitively discover proper leverage.
You may at all times perform close grip preacher curls with an unloaded barbell, so your muscular tissues turn into
used to the movement and develop a foundation of energy.
Carry Out 3 rounds of half B, resting for 2-3 minutes between rounds.
Use a weight that lets you carry out not extra than 10 chest supported rows.
Whether Or Not you’re centered on bodybuilding, powerlifting, or common health, a structured triceps workout will allow
you to build stronger, more outlined arms and enhance general pushing power.
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