| fmyykjm | Дата: Пятница, 13.02.2015, 13:18 | Сообщение # 1 |
| Tacrolimus (also FK-506 or fujimycin, selling names Prograf, Advagraf, Protopic) is an immunosuppressive pharmaceutical that is mainly used after allogeneic medium displace to subdue the vocation of the perseverant's immune set-up and so debase the danger of process rejection. It is also occupied in a topical preparation in the treatment of atopic dermatitis (eczema), strict refractory uveitis after bone marrow transplants, exacerbations of tiniest transform blight, and the fleece condition vitiligo.
It is a 23-membered macrolide lactone discovered in 1984 from the fermentation decoction of a Japanese filth representative that contained the bacteria Streptomyces tsukubaensis. It reduces interleukin-2 (IL-2) forming by T-cells.
Olden days
Tacrolimus was discovered in 1984; it was middle the maiden macrolide immunosuppressants discovered, preceded by the disclosure of rapamycin (sirolimus) on Rapa Nui (Easter Island) in 1975.<> - It is produced by a archetype of loam bacterium,Streptomyces tsukubaensis.<> - The name tacrolimus is derived from 'Tsukuba macrolide immunosuppressant'.<> -
Tacrolimus was to begin approved during the Commons and Drug Superintendence (FDA) in 1994 for end in liver transplantation; this has been extended to comprehend kidney, resolution, miniature bowel, pancreas, lung, trachea, pellicle, cornea, bone marrow, and limb transplants.
Availability
The branded version of the dull is owned next to Astellas Pharma, and is sold below the marketing names Prograf assumption twice everyday,Advagraf, a unceasing unfetter formulation allowing a single time finally constantly dosing, and Protopic (Eczemus in Pakistan before Brookes Pharma), the current formulation.<> - Advagraf is handy in 0.5, 1, 3 and 5 mg capsules, the ointment is concentrations of 0.1% and 0.03%.
A other once-daily formulation of tacrolimus is in Phase 3 clinical trials in the U.S. and Europe. This formulation also has a smoother pharmacokinetic profile that reduces the peak-to-trough range in blood levels compared to twice-daily tacrolimus.<> - Figures from the primary Configuration 3 litigation in steady kidney move patients showed that this once-daily formulation was non-inferior in efficacy and sanctuary compared to twice-daily tacrolimus.<> - A aid Juncture 3 trial in de novo patients is ongoing.<> -
Mechanism of vigour
Tacrolimus is chemically known as a macrolide. In T-cells, activation of the T-cell receptor normally increases intracellular calcium, which acts via calmodulin to get started calcineurin. Calcineurin then dephosphorylates the transcription constituent NF-AT (atomic aspect of activated T-cells), which moves to the core of the T-cell and increases the undertaking of genes coding for IL-2 and common cytokines. Tacrolimus prevents the dephosphorylation of NF-AT.<> - In detail, Tacrolimus reduces peptidyl-prolyl isomerase vocation via binding to the immunophilin FKBP12 (FK506 binding protein) creating a up to date complex. This FKBP12-FK506 complex interacts with and inhibits calcineurin therefore inhibiting both T-lymphocytesignal transduction and IL-2 transcription.<> - Although this occupation is nearly the same to ciclosporin, studies from shown that the occurrence of keen renunciation is reduced by tacrolimus utilization above ciclosporin.<>0 - Although short-term immunosuppression with an eye to submissive and extortion survival is develop to be similar between the two drugs, tacrolimus results in a more favorable lipid portrait, and this may acquire important long-term implications fact the prognostic influence of also brush on implant survival.<>1 -
From http://www.fmyykj.com - suzhou pharmaceutical technology co.,ltd.
| |
| |
| RobertHuch | Дата: Понедельник, 06.04.2015, 20:31 | Сообщение # 2 |
| Вот смех )))Ты видел уже знакомиться по голому )) http://goo.gl/Xx1FAV
| |
| |
10:54