Описание
Селлсепт 500 мг примсеняется при профилактики отторжения после трансплантиции почки, сердца или печени. Возможно назначение Селлсепта в комбинации со следующими препаратами: иммуноглобулином антитимоцитарным,циклоспорином, кортикостероидами и ОКТ3 (ортоклон мышиных моноклональных антител). Основное действующее вещество Селлсепта — Микофенолата мофетил (ММФ). ММФ оказывает сильно выраженное цитостатическое влияние на лимфоциты, благодаря чему минимизируется риск отторжения органов – почки, сердца, печени. Препарат Селлсепт не обладает большим количеством побочных действий, как у конкурентов.
Состав препарата Селлсепт 500 мг
1 таблетка, покрытая оболочкой, содержит:
- активное вещество: микофенолата мофетил 500 мг,
- дополнительные вещества: целлюлоза микрокристаллическая, повидон К90, кроскармеллоза натрия, стеарат магния.
- оболочка: опадрай лавандовый (Opadry Lavender) Y-5-10272-A (гипромеллоза, титана диоксид, гипролоза, краситель индигокармин, макрогол 400, краситель оксид железа красный).
Показания препарата Селлсепт 500 мг
Взрослым и детям старше 12 лет:
- лечение и профилактика терапии отторжения трансплантата после аллогенной пересадки почки, сердца, печени;
- в виде комбинированной терапии с циклоспорином и кортикостероидами.
Фармакодинамика
Микофенолата мофетил (ММФ) — иммунодепрессант, ингибитор инозинмонофосфатдегидрогеназы, который представляет собой 2-морфолиноэтиловый эфир микофеноловой кислоты (МФК). ММФ — мощный избирательный ингибитор инозинмонофосфатдегидрогеназы (ИМФДГ), который подавляет синтез de novo гуанозиновых нуклеотидов. Микофенолата мофетил оказывает явное цитостатическое влияние на лимфоциты, чем на другие клетки. Потому что пролиферация Т- и В-лимфоцитов сильно подчиняется синтезу пуринов de novo, в то время как клетки других типов могут использовать на иные пути метаболизма.
Фармакокинетика
Фармакокинетика изучались на пациентах, перенесших трансплантацию почки, печени или сердца. У пациентов после пересадки в целом фармакокинетика микофенолата сходна. У пациентов, перенесших пересадку печени, в раннем посттрансплантационном периоде и получающих ММФ в дозе 1.5 грамма, концентрации МФК сходная как и у больных после пересадки почки, получающих ММФ в дозе 1 грамм.
Всасывание
При пероральном приеме идет быстрое и полное всасывание, а также полный метаболизм ММФ с появлением активного метаболита – МФК. Биодоступность ММФ при пероральном приеме, составляет 94%. После перорального приема лекарства, концентрация ММФ в плазме не определяется.
Прием еды не влияет на степень всасывания ММФ при его назначении по 1.5 г два раза в сутки.
Распределение
Как правило, примерно через 6-12 часов после приема препарата наблюдается вторичное увеличение концентрации МФК в плазме крови, что показывает о печеночно-кишечной рециркуляции лекарства. При одновременном назначении колестирамина AUC МФК снижается примерно на 40%, что свидетельствует о прерывании печеночно-кишечной рециркуляции.
В клинически значимых концентрациях МФК на 97% связывается с альбумином плазмы.
Метаболизм
В основном МФК метаболизируется с образованием фармакологически неактивного фенольного глюкуронида МФК (МФКГ), под действием глюкуронилтрансферазы. Показано, что in vivo МФКГ в ходе печеночно-кишечной рециркуляции преобразуется в свободную МФК.
Выведение
После перорального приема радиоактивно меченного ММФ 93% полученной дозы выводится с мочой, а 6% — с калом. Большая часть (около 87%) введенной дозы выводится с мочой в виде МФКГ. Незначительные количества препарата (<1% дозы) выводятся с мочой в виде МФК.
Путем гемодиализа клинически определяемые концентрации МФК и МФКГ не элиминируются. Секвестранты желчных кислот наподобие колестирамина понижают AUC МФК, останавливая печеночно-кишечную рециркуляцию.
Биоэквивалентность
В исследованиях показано, что две таблетки ММФ по 500 мг эквивалентны четырем капсулам по 250 мг.
Фармацевтические характеристики
Вещество в таблетках — мелкий гранулированный порошок, от белого до почти белого цвета. Таблетки, покрытые пленочной оболочкой бледно-лилового цвета, с гравировкой «CellCept 500» на одной стороне и «Roche» — на другой.
Упаковка, срок годности, условия хранения
По 10 таблеток в контурной ячейковой упаковке из пвх пленки и фольги алюминиевой. По 5, 10, 15 контурных ячейковых упаковок вместе с инструкцией упакованы в картоннную пачку.
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Срок хранения 3 года. Не применять по истечении срока годности!
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The Science Behind PCT: How It Helps Restore Hormone Balance After A Cycle
Introduction to Post-Cycle Therapy (PCT)
Post-Cycle Therapy (PCT) is a recovery phase
designed for individuals who have completed a cycle of anabolic steroid usage.
The primary goal of PCT is to restore natural hormone production and overall bodily
health after the steroid cycle.
Key Benefits of PCT
Testosterone Restoration: PCT helps in the recovery of endogenous testosterone levels,
which are crucial for muscle growth, fat loss, and overall health.
Estrogen Balance: Properly managing estrogen levels
is essential to avoid hormone imbalances and potential side effects.
PCT aids in this balance by resetting the body’s hormonal equilibrium.
Cortisol Levels: Excess cortisol can lead to muscle breakdown and other
health issues. PCT helps in normalizing cortisol levels, promoting recovery and muscle retention.
How Post-Cycle Therapy Works
PCT involves a carefully designed regimen of medications and supplements that
target the hormonal imbalances caused by
steroid use. The therapy works by:
Suppressing Estrogen: By reducing estrogen levels, PCT
helps to minimize the risk of side effects like gynecomastia and mood swings.
Supporting Liver Health: A healthy liver is essential for hormone regulation. PCT includes interventions that support
liver functionality and overall health.
Restoring Testosterone Production: Through strategic use of medications, PCT
facilitates the body’s natural ability to resume
producing testosterone post-cycle.
Conclusion
Post-Cycle Therapy is a critical step for athletes and cyclists who have completed a steroid cycle.
It not only helps in restoring hormonal balance but also ensures overall
physical health and well-being, allowing individuals to return to their performance goals safely
and effectively.
The Science Behind PCT: How It Helps Restore Hormone Balance After A
Cycle
21 December 2023
Post-Cycle Therapy (PCT) has become a popular topic in the fitness and bodybuilding communities, particularly among individuals
who undergo anabolic steroid cycles. While PCT is often associated with
recovery after steroid use, it’s important to understand how it works and why
it’s considered beneficial for hormone balance.
What is Post-Cycle Therapy (PCT)?
PCT refers to a period of time during which individuals take specific supplements or medications
to help their bodies recover after a cycle of anabolic steroid use.
The goal of PCT is to restore the body’s natural hormone production, particularly testosterone, and to minimize the negative effects of steroid use.
How Does PCT Work?
PCT works through two main mechanisms: blocking estrogen production and stimulating testosterone production. During a cycle,
the use of anabolic steroids can suppress the body’s own hormone production and increase estrogen levels, which can lead
to negative side effects such as testicular atrophy and mood swings.
PCT aims to counteract these effects.
Block Estrogen Production
Estrogen is a hormone that plays a role in female physiology but also has steroid-like effects in males.
During PCT, anti-estrogen supplements are often used to reduce estrogen levels.
Lowering estrogen can help prevent issues like gynecomastia (breast development in males) and improve testosterone levels.
Stimulate Testosterone Production
Testosterone is the primary anabolic hormone, and its suppression during steroid use can lead to muscle loss, fatigue,
and other negative effects. PCT involves the use of supplements like testosterone boosters
or hormones that stimulate the body’s own testosterone production. This helps restore muscle mass, strength,
and overall vitality.
What Happens During PCT?
During PCT, individuals experience a variety of physiological changes aimed at restoring hormone balance.
These include:
Improved Recovery: Testosterone plays a crucial role in recovery,
and restoring its levels can enhance muscle repair and growth.
Enhanced Muscle Growth: Testosterone is essential for building muscle mass,
and PCT helps maintain or even increase muscle size.
Increased Energy Levels: Low testosterone often leads to fatigue,
and restoring it can provide more energy for daily activities and workouts.
Hormonal Balance: PCT helps regulate hormones like estrogen and cortisol, reducing negative side effects of steroid use.
The Bottom Line
PCT is not a miracle cure, but it is a valuable tool for individuals who have undergone
steroid cycles. It can help restore hormone balance and mitigate some of the negative effects
of anabolic steroid use. However, it’s important to approach PCT with caution and under professional guidance.
The supplements used in PCT can have side effects,
and their effectiveness varies depending on individual circumstances.
Nicolas Desjardins
Writer and Fitness Expert
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