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Актуальная тема!
AdvastalsДата: Среда, 12.02.2014, 09:10 | Сообщение # 466
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MazurenkoДата: Среда, 12.02.2014, 09:32 | Сообщение # 467
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RussellHawДата: Среда, 12.02.2014, 23:52 | Сообщение # 468
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TravisMepДата: Четверг, 13.02.2014, 01:28 | Сообщение # 469
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WilliamBipДата: Четверг, 13.02.2014, 02:31 | Сообщение # 470
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CarlosKnДата: Четверг, 13.02.2014, 02:45 | Сообщение # 471
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DerickKaДата: Четверг, 13.02.2014, 22:47 | Сообщение # 472
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ArrandackДата: Пятница, 14.02.2014, 00:04 | Сообщение # 473
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BassynicaДата: Пятница, 14.02.2014, 02:33 | Сообщение # 474
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Uv1IIbcrh8Дата: Пятница, 14.02.2014, 14:06 | Сообщение # 475
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Vu4FLjblp3Дата: Пятница, 14.02.2014, 15:41 | Сообщение # 476
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famuyiyaozДата: Пятница, 14.02.2014, 15:53 | Сообщение # 477
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It is a 23-membered macrolide lactone discovered in 1984 from the fermentation broth of a Japanese befoul sampling that contained the bacteria Streptomyces tsukubaensis. It reduces interleukin-2 (IL-2) forming past T-cells.
Olden days
Tacrolimus was discovered in 1984; it was among the maiden macrolide immunosuppressants discovered, preceded by the disclosure of rapamycin (sirolimus) on Rapa Nui (Easter Islet) in 1975.<> - It is produced on a class of soil bacterium,Streptomyces tsukubaensis.<> - The name tacrolimus is derived from 'Tsukuba macrolide immunosuppressant'.<> -
Tacrolimus was beforehand approved by the Comestibles and Narcotize Superintendence (FDA) in 1994 someone is concerned make use of in liver transplantation; this has been extended to include kidney, affection, small bowel, pancreas, lung, trachea, overlay, cornea, bone marrow, and limb transplants.
Availability
The branded version of the dull is owned close to Astellas Pharma, and is sold under the trade names Prograf given twice everyday,Advagraf, a continual launch formulation allowing in the good old days daily dosing, and Protopic (Eczemus in Pakistan before Brookes Pharma), the current formulation.<> - Advagraf is at one's fingertips 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 Stage 3 clinical trials in the U.S. and Europe. This formulation also has a smoother pharmacokinetic profile that reduces the peak-to-trough assortment in blood levels compared to twice-daily tacrolimus.<> - Statistics from the primary Phase 3 woe in stable kidney transfer patients showed that this once-daily formulation was non-inferior in efficacy and safety compared to twice-daily tacrolimus.<> - A second Phase 3 hearing in de novo patients is ongoing.<> -
Mechanism of action
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 turn on calcineurin. Calcineurin then dephosphorylates the transcription go-between NF-AT (nuclear factor of activated T-cells), which moves to the core of the T-cell and increases the activity of genes coding in behalf of IL-2 and tied up cytokines. Tacrolimus prevents the dephosphorylation of NF-AT.<> - In group specifically, Tacrolimus reduces peptidyl-prolyl isomerase vocation during binding to the immunophilin FKBP12 (FK506 binding protein) creating a uncharted complex. This FKBP12-FK506 complex interacts with and inhibits calcineurin wise inhibiting both T-lymphocytesignal transduction and IL-2 transcription.<> - Although this activity is nearly the same to ciclosporin, studies secure shown that the incidence of shrewd renunciation is reduced about tacrolimus utilization from ciclosporin.<>0 - Although short-term immunosuppression anent patient and shoot survival is found to be be like between the two drugs, tacrolimus results in a more favorable lipid portrait, and this may eat substantial long-term implications given the prognostic play of rejection on graft survival.<>1 -
 
RoberteaДата: Пятница, 14.02.2014, 18:03 | Сообщение # 478
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BassynicaДата: Суббота, 15.02.2014, 03:06 | Сообщение # 479
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evendancyДата: Суббота, 15.02.2014, 20:10 | Сообщение # 480
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