3、Mechanism and clinical use:
Tacrolimus is strong-efficacy macrolide immunosuppressant. At the molecular level, its effect is mediated through protein FKBP12 in cytoplasm which is binding with it. FKBP12 makes this drug into cell, and form complex, and the complex competitively and specifically binds with calmodulin and inhibits calmodulin (the latter mediates calcium-dependent inhibitory signal transduction system in T-cells), so as to block a series Gene transcription of lymphokine. In-vitro experiments demonstrate that Tacrolimus is strong-efficacy macrolide immunosuppressant, it can inhibit formation of cytotoxic lymphocytes, and allograft rejection is mainly caused by the latter.
This drug inhibits activation of T-cells, inhibits TH-cell-dependent B-cells-propagation, and inhibits generation of lymphokine such as express of interleukin 2, interleukin 3, β-interferon and interleukin 2 receptor. Tacrolimus can inhibit allograft rejection of skin, heart, kidney and liver, extend live time of allograft, and this is evidenced in bodies of rodent, dogs, primate and human. From its marketing, it is widely used in treatment of rejection of allograft of liver, kidney and bone marrow.
4、Packaging size specification
Inner package: single-layers polyethylene bag and aluminum foil bag.
Outer package: aluminum bottle (pharmaceutical use).
Packaging size: 500 g/bottle
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