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Завеска — Zavesca (Миглустат)

Завеска

Завеска — Zavesca (Миглустат)

Препарат Завеска применяется при лечении болезни Гоше 1 типа, квалифицированной легкой и средней степенью развития. Использование препарата рекомендуется взрослым пациентам, не реагирующие на заместительную ферментную терапию. Препарат Завеска используется, также, для лечения детей и взрослых с болезнью Ниманна-Пика типа С, охарактеризованной тяжелыми неврологическими симптомами. Особенности заболеваний Гоше и Ниманна-Пика состоят в том, приводят к аккумуляции в клетках непереработанных продуктов метаболизма. Это ведет к серьезным нарушениям работы внутренних органов, и происходит вследствие недостаточной активности ферментов. Основное действующее вещество препарат Завеска — Миглустат. Миглустат — ингибитор фермента глюкозилцерамидсинтазы — основного фермента синтеза большинства гликолипидов. Миглустат применяется при болезни Гоше I типа и при болезни Ниманна-Пика типа С в качестве субстрат-редуцирующей терапии, вследствии способности снижать синтез гликозилцерамида.

Категория:

Описание

Препарат Завеска применяется при лечении болезни Гоше 1 типа, квалифицированной легкой и средней степенью развития. Использование препарата рекомендуется взрослым пациентам, не реагирующие на заместительную ферментную терапию. Препарат Завеска используется, также, для лечения детей и взрослых с болезнью Ниманна-Пика типа С, охарактеризованной тяжелыми неврологическими симптомами. Особенности заболеваний Гоше и Ниманна-Пика состоят в том, приводят к аккумуляции в клетках непереработанных продуктов метаболизма. Это ведет к серьезным нарушениям работы внутренних органов, и происходит вследствие недостаточной активности ферментов. Основное действующее вещество препарат Завеска — Миглустат. Миглустат — ингибитор фермента глюкозилцерамидсинтазы — основного фермента синтеза большинства гликолипидов. Миглустат применяется при болезни Гоше I типа и при болезни Ниманна-Пика типа С в качестве субстрат-редуцирующей терапии, вследствии способности снижать синтез гликозилцерамида.

Состав Завеска

  • действующее вещество: миглустат 100 мг
  • дополнительные вещества: карбоксиметилкрахмал натрия, повидон К30, магния стеарат, титана диоксид, желатин;
  • cостав чернил: чернила черные Опакод S-1-27794 (шеллак, этанол денатурированный (спирт метилированный), бутанол, изопропанол, краситель железа оксид черный, пропиленгликоль, вода) или TekPrint™ SW-9008 (этанол, шеллак, бутанол, изопропанол, вода, пропиленгликоль, аммиак водный, калия гидроксид, краситель железа оксид черный), или 10A1 (глазурь фармацевтическая (шеллака раствор в этаноле), аммиак водный, пропиленгликоль, краситель железа оксид черный), или 10A2 (шеллак, аммиак водный, пропиленгликоль, краситель железа оксид черный, калия гидроксид).

Показания к применению

  • для перорального лечения взрослых пациентов с болезнью Гоше 1 типа (легкой и средней степени тяжести), не реагирующие на заместительную ферментную терапию;
  • для лечения прогрессирующих сложных неврологических симптомов у детей и взрослых с болезнью Ниманна-Пика тип С.

Фрмакодинамика Завеска

Препарат Завеска используется для лечения наследственных ферментопатий. In vitro в исследованиях миглустат в концентрации IC50 на 20-37 мкмоль оказывает подавляющее воздействие на синтазу глюкозилцерамида. В экспериментальных исследованиях in vitro, кроме того, также установлено его подавляющее влияние на нелизосомальную глюкозилцерамидазу.

Вследствие наследственных нарушений метаболизма, при болезни Гоше 1 типа, не возникает естественной деградации глюкозилцерамида, что приводит к аккумуляции его в лизосомах и сопровождается патологическими изменениями во многих органах. Препарат Завеска оказывает подавляющее действие на глюкозилцерамидсинтазу, которая является ферментом, ответственного за первый этап синтеза большинства гликолипидов. В основе субстратснижающей терапии болезни Гоше лежит ингибирующее действие глюкозилцерамидсинтазы.

Болезнь Ниманна-Пика тип C или сфингомиелиновый липидоз — это очень редкое заболевание, которое проявляющееся нейродегенеративными изменениями и развивается вследствии нарушения внутриклеточного транспорта липидов. Заболевание характеризуется неизменно прогрессирующим течением, высокой летальностью. Неврологические изменения при болезни Ниманна-Пика тип С, считается, что развиваются вторично в результате накопления гликосфинголипидов в глиальных клетках и нейронах.

Фармакокинетика Завеска

Фармакокинетические параметры миглустата изучали у ограниченного числа больных болезнью Гоше 1 типа, у больных болезнью Фабри, у ВИЧ-инфицированных больных, у взрослых и детей, страдающих болезнью Ниманна-Пика тип С и болезнью Гоше 3 типа, у здоровых добровольцев.

Всасывание

Фармакокинетические параметры препарата Завеска находятся в прямо пропорциональной зависимости от дозировки и не зависят от времени. после приема препарата внутрь у здоровых добровольцев препарат Завеска быстро всасывается, Cmax в плазме крови определяется примерно через 2 ч. Абсолютная биодоступность миглустата не установлена. Скорость абсорбции миглустата уменьшается, при совместном приеме препарата с пищей (Cmax снижается на 36%, а время достижения Cmax увел-ичивается на 2 часа). При приеме препарата Завеска с пищей степень абсорбции препарата достоверно не снижается (AUC уменьшается на 14процентов).

Распределение

Объем распределения миглустата составляет 83 литров. Миглустат не связывается с белками плазмы крови.

Метаболизм и выведение Завеска

Миглустат выводится преимущественно (70-80процентов от введенной дозы) почками в неизмененном виде. Образуется множество метаболитов в ходе биотрансформации миглустата, которые выводятся через кишечник и почки.

Клиренс миглустата составляет 230±39 мл/минуту, период полураспада — 6-7 часов.

После приема внутрь 100 мг меченного 14С-миглустата у здоровых добровольцев обнаружено, что 83процента радиоактивного вещества выводится почками и 12процентов — через кишечник.

Основной метаболит, обнаруживающийся в моче, миглустата глюкуронид, он составляет 5 процентов принятой дозы миглустата. Период полураспада радиоактивного вещества составляет 150 часов. Предполагается наличие одного или нескольких метаболитов с очень продолжительным периодом полураспада. Не установлен еще метаболит, который имел бы такую продолжительность действия, однако, возможно, происходит его накопление и тогда его концентрация превышает Css миглустата.

Фармакокинетические показатели миглустата у взрослых больных с болезнью Ниманна-Пика тип С и с болезнью Гоше 1 типа от соответствующих показателей у здоровых добровольцев не отличаются.

Фармакокинетические показатели изучали у детей у детей с болезнью Ниманна-Пика тип С в возрасте 5-16 лет, с болезнью Гоше 3 типа в возрасте 3-15 лет. Применение миглустата у детей в дозировке 200 мг, с коррекцией в зависимости от площади поверхности тела, сопровождалось почти двукратным увеличением максимальной концентрации и экпозиции AUC по сравнению с соответствующими значениями максимальной концентрации и экспозиции AUC после применения миглустата в дозировке 100 мг при болезни Гоше 1 типа и также характеризовалось линейной зависимостью. В равновесном состоянии концентрация миглустата в цереброспинальной жидкости 6 больных болезнью Гоше 3 типа составляла 31.4-67.2 процента концентрации в плазме крови.

Фармакокинетика в особых клинических случаях

Возраст, пол, расовая принадлежность и индекс массы тела клинически значимого влияния на фармакокинетические параметры на препарат Завеска не оказывают. Коррекции дозы препарата, соответственно, в зависимости от вышеуказанных параметров не требуется.

Не изучались фармакокинетические параметры миглустата у пациентов старше 70 лет.

В связи с тем, что миглустат не метаболизируется печенью, не изучались фармакокинетические параметры миглустата у пациентов с печеночной недостаточностью.

Ограниченные данные, полученные у больных с нарушением функции почек и с болезнью Фабри демонстрируют снижение клиренса миглустата по мере ухудшения состояния функции почек. При почечной недостаточности легкой и средней степени тяжести клиренс миглустата снижался, соответственно, на 40процентов и 60 процентов. Данные при почечной недостаточности тяжелой степени ограничены 2 пациентами (КК 18-29 мл/мин). Но эти данные нельзя экстраполировать относительно более низких значений. Эти данные позволяют предположить снижение клиренса на 70процентов и ниже у пациентов почечной недостаточностью тяжелой степени.

Применение при беременности и кормлении грудью

Контролируемых исследований препарата Завеска у беременных не проводилось. По данным экспериментальных исследований, есть свидетельства о наличии репродуктивной токсичности, включая осложненные роды. Потенциальный риск у человека неизвестен. Препарат Завеска проникает через плацентарный барьер, поэтому применять миглустат при беременности не следует. Необходимо использовать надежные методы контрацепции женщинам детородного возраста во время лечения препаратом. Попадание миглустата в грудное молоко у человека не установлено. Не следует препарат Завеска назначать в период лактации (грудного вскармливания).

Применение при нарушениях функции печени

При назначении препарата Завеска пациентам с печеночной недостаточностью, в связи с недостаточным клиническим опытом, следует соблюдать осторожность.

Применение при нарушениях функции почек

При назначении препарата Завеска пациентам с почечной недостаточностью, в связи с недостаточным клиническим опытом, следует соблюдать осторожность. По мере нарастания почечной недостаточности клиренс миглустата пропорционально снижается. Лечение пациентов с почечной недостаточностью тяжелой степени (КК <30 мл/мин/1.73 м2) препаратом Завеска не рекомендуется.

Применение у детей

Имеются противопоказание к применению у следующей категории детей, ввиду недостаточности клинического опыта:

возраст пациентов с болезнью Гоше до 18 лет и старше 70 лет;

возраст пациентов с болезнью Ниманна-Пика младше 4 лет.

Применение у пожилых пациентов

Из-за недостаточности клинического опыта имеется противопоказание к применению у пациентов с болезнью Гоше в возрасте до 18 лет и старше 70 лет

Фармацевтические характеристики Завеска

Выпускается в желатиновых  капсулах:

  • непрозрачные твердые №4 цилиндрической формы, состоящие из корпуса и крышечки белого цвета, с маркировкой черного цвета «100» (на корпусе) и «OGT 918» (на крышечке).

Содержимое капсул — порошок белого или почти белого цвета.

Упаковка, срок годности, условия хранения Завеска

Капсулы, 100 мг. В контурной ячейковой упаковке (блистер) (ламинированная пленка (ПВХ/Aclar®)/фольга алюминиевая), 21 шт. 4 блистера в картонной пачке с контролем первого вскрытия.

Препарат Завеска следует хранить в недоступном для детей месте при температуре не выше 30°С.

Срок годности препарата Завеска — 5 лет.

 

 

 

 

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

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    hamstrings. The bent-over row is an outstanding free-weight
    exercise that works quite a few muscle tissue, most notably the center and decrease again muscular tissues.
    It requires very minimal equipment and could be very conducive to
    progressive overload. In the video under, Mind Pump’s head trainer demonstrates how to do T-bar rows
    the proper method. This ought to have interaction the muscles
    of the back while simultaneously bending the elbows parallel to the ribs, the bands forming a straight line from anchor point to the chest or shoulders.

    This is doubtless considered one of the few rear deltoid workout routines that involve shoulder joint extension. Trying like a cross between a barbell
    hack squat, bent-over row, and triceps kickback, this unusual movement is
    slightly awkward however highly effective for building posterior
    deltoid strength and mass. The clue is in the name; you’re performing
    a really similar motion to that on a rowing machine. What’s great right
    here is that the additional weight is actually working your back muscles, specifically the lats.
    Compared to seated cable rows you’ll have interaction core
    muscle tissue like your abs and obliques more when doing the renegade
    row. One factor to hold in mind is that bent-over rows are more difficult for your lower back muscular tissues.

    If you may have entry to a T-Bar Row machine,
    T-Bar Rows might actually be the closest different to the Barbell Row out of
    any of the Barbell Row options listed above. You’ll end up
    in the same physique place but most machines (but not all) may also provide chest support.
    Inverted Rows are probably the greatest, and most overlooked,
    horizontal rows you are able to do within the weight room. They place zero stress on the
    low again and can be modified to be good for each beginners and challenging for superior lifters.
    A common mistake is rotating your shoulder again on the lift, but
    doing that can trigger shoulder pain and stop you from getting essentially the
    most out of the exercise. For those who liked the bent-over row from the bottom of their hear and do not wish
    to exchange it — an incline barbell row may be the closest various.

    This exercise locations you in a hip-hinged position akin to a deadlift,
    effectively cultivating power, control, and endurance all through your legs.
    It is usually carried out for average to excessive reps, no much less than 8–12 reps per set, as part of an upper-body or shoulder-focused exercise.
    The cable rear delt row will turn into more of
    a standard wide-grip cable row. The meadows row is a single arm landmine row that may
    simply replace the t-bar row by allowing you to create a
    larger stretch on the backside of the motion. If you want to target your lats extra, you’ll be able to set the incline to a
    lower angle while tucking your elbows during the row. If you
    want to goal your higher back extra, you possibly can set a higher incline whereas flaring your elbows
    out during the row.
    As you presumably can see, your grip, angle you bend over
    at, and where you row the bar in relation to your torso will heavily affect the muscle tissue that you
    just primarily work. Simply understand that this is nonetheless
    a compound exercise and it will subsequently work
    everything of your upper posterior chain to some extent.
    The barbell row is amongst the best back building workouts
    that you could possibly add to your routine. It offers a great route by means of progressive overload and for that purpose, it is often thought of a compound
    exercise (alongside the fact that it engages multiple muscle groups).
    Read on to learn about options to the seated cable
    row that may have your again getting wider, thicker, and extra defined in no time.

    In this article, we lay out 9 alternatives to the Hammer Power high-row machine.
    To be sincere, none of them are as effective as doing the train on an precise
    Hammer Energy machine.
    You also can transfer them by way of numerous
    angles with out being restricted to a machine’s motion path.
    Hammer Power machines allow you to work with weight
    plates via varied angles that you can’t do with free weights.
    They also present a secure seating position that removes any momentum from the motion. This is a minor muscle group that aids in the external rotation of the humerus.

    One draw back is that resistance bands usually are not the kind of health
    club equipment you must use for the relaxation of your life.
    At least each few years you will need to exchange the last set with new resistance bands to construct muscle.
    They can be utilized for a wide selection of exercises, including choices that can function an alternative to each the cardio and resistance training rowing
    machine. The face pull helps goal your trapezius muscles, upper
    lats, and rhomboids. This can be an excellent exercise that can help you achieve and preserve an upright posture.
    Incorporating a variety of alternative workouts 
    with the normal T-Bar Row not only provides variety to your workout routine but also ensures a complete development of your again muscles.
    When performing any rowing movement it’s necessary to maintain a impartial head and backbone to stop harm.

    You can also get greater muscle activation by exaggerating the
    completely different phases of the raise. By reaching your shoulder forward
    on the bottom you can get a greater stretch, by throwing your elbow further back you
    will get higher lat activation. The banded row is a highly versatile banded exercise making it helpful for any lifter’s training protocol.
    You can do this train with high reps and high units while causing minimal fatigue
    to the nervous system. Band Rows aren’t going to switch a One Arm Dumbbell Row for growing strength, but
    they’ll work great in a pinch if you’re traveling.
    Even when you don’t have something sturdy you probably can connect the resistance band
    to, you probably can always wrap them around your ft if need be.

    The landmine row (or T-bar row) is on our record of prime 3 rows and is an ideal substitute for the cable
    row. Landmine rows afford multiple grip options; thus, you possibly can target the identical muscles because the seated
    row. You’ll need to perform this exercise
    on a cable machine although you’ll be able to elicit
    comparable outcomes when utilizing a chest-supported t-bar row 
    and maintaining your elbows out extensive.

    And, in fact, you’ll want somewhere to do that exercise – like a house pull-up bar, a tree department, or a
    monkey gym bar. But, neglecting this small however
    necessary muscle could have a significant influence on not just
    the looks of your shoulders but additionally how they function. Underdeveloped
    rear deltoids can contribute to shoulder pain, which is something that each lifter needs to avoid.

    By utilizing dumbbells as a substitute of a barbell, both sides of the back is engaged
    independently, serving to to appropriate any imbalances and improve total
    power. Dumbbells goal your muscle tissue from
    different angles than a barbell, but you’ll nonetheless get a great
    again and lat workout. Variations like single-arm dumbbell rows
    allow you to steadiness the strength in your left and proper side.

    Resistance bands are an usually missed piece of equipment in the fitness center,
    however they’ve plenty of potential uses. Resistance bands are nice at mimicking
    weighted workouts with none bulky tools.

    You can take a resistance band with you wherever to
    do your workout at residence or whereas traveling.
    Performing rows with a band may give you an excellent stimulus
    without fatiguing the nervous system so that you
    just can do them extra often and with larger quantity.
    Inverted bodyweight rows are nice for strengthening the again for more complicated workouts like pull-ups.
    You can use this exercise to target the back from different angles by varying your grip width or experimenting with a
    supinated (underhand grip). If you don’t have entry to a T-Bar Row machine with a chest pad, you can also carry out
    this exercise by lying face down on a bench with a dumbbell
    in each hand and pulling them in the course of your torso.

    Relying on the machine, you possibly can both use a double overhead
    (pronated) grip or a impartial grip. The pronated grip will
    goal the upper/middle back extra, whereas the impartial
    grip will engage extra of the lats. You can carry out this motion anytime throughout
    a again or higher physique exercise. T-bar rows are a
    variation of barbell row where a T-bar deal with is affixed
    to 1 end of the barbell, retaining the pronated grip, a
    somewhat greater stage of hip hinge and a unique angle of resistance.
    Finally, bent over rows aren’t the heaviest variation of row one can carry out, and neither characteristic the biggest vary
    of motion. This can limit the extent of the athlete’s training, particularly on the
    larger ranges where specificity and issues like sticking points are vital obstacles.

    Whereas each workout routines work the again, barbell rows target the lats, upper
    again, rear delts and biceps, whereas the deadlift hits the lower again, glutes
    and hamstrings. Partaking in the seated cable row exercise is useful for focusing on your
    again muscle tissue, notably your lats, while minimizing the chance of
    decrease again injury. If you prefer to switch bent over rows with body weight workout
    routines, you can perform inverted rows (also generally recognized as Australian rows) or TRX
    rows. These workouts have you work by pulling your body upward whilst you lean again,
    rather than lifting a weight from the bottom.
    It additionally helps you burn more calories, as you have to burn up extra energy.
    Kroc recommends contracting your shoulders on the prime and
    letting your arm drop at the descent. Seal rows deliver your physique perfectly parallel to the floor,
    making it an excellent exercise to work on the thickness of the
    back. The barbell is stored in an elevated position to help the lifter give consideration to the concentric flexion without worrying in regards to the eccentric phase.
    Anybody experiencing lower again ache should do this exceptional
    variation, because it completely eliminates the stress off the
    lumbar spine. With that mentioned, most lifters begin to
    really feel discomfort as they start to carry heavier weights.

    Seek new and attention-grabbing methods to perform all
    of your staple actions so that you never get caught ready
    on the health club, never develop bored, and always keep growing.
    Now that you realize a couple of variations for
    your rear delts row, hit the health club
    and verify out every one to get the complete impact. Working your delts can be done by numerous workouts; we will point out a extremely popular different
    exercise – that you can do alongside or instead of the regular rear delt row.
    Whether or not you employ one or two arms you’ll be able to goal the totally
    different muscle tissue of the back.
    Keep studying to search out out why each was included, how to
    perform them, and some tips to get probably the most out of the
    exercise. The bent over dumbbell row is a barbell row
    variation that, though being a bilateral transfer, forces each side of the physique
    to hold its personal load. This overcomes a common downside when rowing with a barbell of the
    strongest side taking the majority of the load. Utilizing dumbbells on workouts like
    this helps in attaining balanced energy and muscular improvement.

    It allows for higher physique stability than the bent-over row and doesn’t require as much gear.
    You’ll be performing a row with one dumbbell at a time – it’s an alternating row.
    A good tip is to place your empty hand on your front-facing leg for stability.
    If you need to improve the difficulty of the movement, stretch it out to your facet.

    Novices ought to embark on their journey with lighter weights
    and incrementally add extra as they grow stronger. This technique helps prevent accidents while guaranteeing that correct form
    is maintained all through. This alternative targets the higher again muscular tissues and might help construct overall higher body strength for different
    pulling and even pushing workouts like the bench press. Not to mention that the resistance band is flexible and easy to make use of, making it a
    fantastic choice for lifters of all fitness levels.

    To perform T-bar rows successfully, begin with a
    weight that challenges you however permits for correct form.

    A seated cable row prompts the lats greater
    than other actions like the upright row. However,
    as a outcome of it’s a machine, you might end up unable to do that train or just plain uninterested
    in it. That’s ok as a result of there are lots of lat pulldown alternative
    workouts you have to use to train the same muscle tissue.
    A good primer for pull-ups – a lot of exercises name for pull-ups and chin-ups, which
    are two of one of the best body weight lat workouts you can do.
    But, as these workouts contain lifting your whole body utilizing simply your arms, they are often exhausting to study
    and master. Lat pulldowns work the same muscle
    tissue, so they’re a useful steppingstone toward
    doing pull-ups and chin-ups. Whereas extensive grip bent over rows are a wonderful exercise, they
    can be onerous on your lower again.
    Not only does that increase your threat for damage, but it’s additionally not advantageous
    for hypertrophy. Having your chest supported by the bench permits you to target the again with out involving the core and erectors and makes it so
    much tougher to cheat the movement. If you struggle with feeling your again working
    during a row, strive an incline dumbbell row to see should you can create a greater
    mind-muscle connection. The single-arm dumbbell row could be performed by standing
    along with your arm supported against a bench or dumbbell rack.
    The farther you pull the dumbbell again in the path
    of your hip, the more you’ll hit your lat.
    Maintaining a neutral backbone in a bent-over position whereas supporting a heavy barbell takes lots of strength.
    Having mastered the approach, it’s necessary to consider how your grip can isolate specific again muscles and cater to your consolation. Using an overhand
    grip slightly past shoulder width is good for partaking the latissimus dorsi and center trapezius.
    Whichever various you determine to perform, know that proper form is crucial for muscle growth and
    growth, as nicely as injury prevention. Resistance bands can produce comparable power gains to that of traditional
    energy coaching and might help improve efficiency within the gym and performance in everyday life.
    The barbell can build strength and muscle, but if one
    facet is weaker than the other, it could possibly
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