Tacrolimus
Function and Efficacy
At the molecular level, the action of tacrolimus is apparently through binding to a cellular protein (FKBP12) that accumulates in cells and produces its effects. The FKBP12-tacrolimus complex specifically binds to and inhibits calcinurin, which inhibits the calcium-dependent signal transduction pathway in T cells, thereby preventing the transcription of discrete lymphokine genes. This drug is a highly immunosuppressive drug, and its activity has been demonstrated in vitro and in vivo. This drug inhibits the production of cytotoxic lymphocytes that are the main cause of transplant rejection. This drug inhibits the activation of T cells and the proliferation of T-helper cell-dependent B cells, and also inhibits the production of lymphokines such as interleukin-2, interleukin-3 and gamma-interferon and the expression of interleukin-2 receptors. At the molecular level, the effect of this drug seems to be produced by binding to a cellular protein (FKBP), which also causes the compound to accumulate in the intercellular space. In vivo studies have found that this drug has shown efficacy in liver and kidney transplants.
Ingredients
The main ingredient of this product is tacrolimus. In addition to the active ingredient, this medicine contains hydroxypropyl and methylcellulose, sodium salt of croscarmellose, lactose, magnesium stearate and dioxy peptide (E171). The infusion solution contains polyethylene hydrogenated castor oil and anhydrous ethanol.
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| TacrolimusIngredients |
It binds to FKBP12 and accumulates in cells, inhibiting calcinurin and calcium-dependent signal transduction pathways in T cells, preventing lymphokine gene transcription; inhibiting T cell activation, T helper cell-dependent B cell proliferation, inhibiting the production of multiple lymphokines and interleukin-2 receptor expression; it is effective in liver and kidney transplantation in vivo. More |
104987-11-3 | 33 |
Indication
Prevention of graft rejection after liver or kidney transplantation; treatment of graft rejection after liver or kidney transplantation that cannot be controlled by other immunosuppressive drugs
Adverse Reactions
It is often difficult to identify adverse reactions associated with immunosuppressive drugs because most users have serious medical conditions and are taking many other medications at the same time. There is evidence that many of the following adverse drug reactions are reversible and can be improved by dose reduction. The frequency of adverse reactions is significantly lower with oral administration compared to intravenous administration. The following adverse drug reactions are organized according to body system and their frequency of occurrence. Cardiovascular system - Frequent: hypertension. Occasional: angina, palpitations, effusions (e.g., pericardial effusion, pleural effusion). Rare: hypotension including shock, ECG abnormalities, arrhythmias, atrial/ventricular fibrillation and cardiac arrest, thrombophlebitis, bleeding (e.g., gastrointestinal, brain), heart failure, cardiomegaly, bradycardia,
Precautions
Pregnancy. Known allergy to tacrolimus or other macrocyclic drugs. Known allergy to other components of the capsule. Known allergy to polyethylene hydrogenated castor oil (HCO-60) or similar structural compounds.
Storage
When stored in a dark place and below 25°C, it can be stored for 24 months. After being prepared in a glass or polyethylene bottle with normal saline or 5% glucose injection, it should be used within 24 hours.
Packaging Specification
API
Manufacturer
Fujian Kerui Pharmaceutical Co., Ltd.
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Founded in:
1999-09-07 -
Address:
No. 1069-15, Niuzhai Village, Haikou Town, Fuqing City, Fuzhou City, Fujian Province -
Tax NO.:
913501816110101446 -
Registered Funds:
25 million yuan -
Website:
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Email: