Yixinke
Yixinke Uses, Dosage, Side Effects, Food Interaction and all others data.
A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to immunophilins. Yixinke is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.
Yixinke, a macrocyclic lactone produced by Streptomyces hygroscopicus, is an immunosuppressive agent indicated for the prophylaxis of organ rejection in patients receiving renal transplants. It is recommended that sirolimus be used in a regimen with cyclosporine and corticosteroids.
Trade Name | Yixinke |
Availability | Prescription only |
Generic | Sirolimus |
Sirolimus Other Names | Rapamycin, Sirolimús, Sirolimus, Sirolimusum |
Related Drugs | Sabril, Rapamune, tacrolimus, azathioprine, cyclosporine, mycophenolate mofetil, CellCept, Imuran |
Type | |
Formula | C51H79NO13 |
Weight | Average: 914.187 Monoisotopic: 913.555141608 |
Protein binding | 92% |
Groups | Approved, Investigational |
Therapeutic Class | |
Manufacturer | |
Available Country | China |
Last Updated: | September 19, 2023 at 7:00 am |
![Yixinke Yixinke](https://www.medicinesfaq.com/media/png/yixinke.png)
Uses
Yixinke is an immunosuppressant used to prevent organ transplant rejections and to treat lymphangioleiomyomatosis.
For the prophylaxis of organ rejection in patients receiving renal transplants.
Yixinke is also used to associated treatment for these conditions: Chordomas, Graft Versus Host Disease (GVHD), Heart Transplant Rejection, Liver Transplant Rejection, Lung Transplant Rejection, Lymphangioleiomyomatosis, Renal Angiomyolipomas, Moderate renal transplant rejection
How Yixinke works
Yixinke inhibits T lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (Interleukin IL-2, IL-4, and IL-15) stimulation by a mechanism that is distinct from that of other immunosuppressants. Yixinke also inhibits antibody production. In cells, sirolimus binds to the immunophilin, FK Binding Protein-12 (FKBP-12), to generate an immunosuppressive complex. The sirolimus:FKBP-12 complex has no effect on calcineurin activity. This complex binds to and inhibits the activation of the mammalian Target Of Rapamycin (mTOR), a key regulatory kinase. This inhibition suppresses cytokine-driven T-cell proliferation, inhibiting the progression from the G1 to the S phase of the cell cycle.
Food Interaction
- Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of sirolimus and increases its serum concentration.
- Exercise caution with St. John's Wort. This herb induces CYP3A4 and P-gp; thus it may reduce sirolimus serum concentrations.
- Take with or without food. Take consistently with regard to food.
[Moderate] ADJUST DOSING INTERVAL: Consumption of food can decrease the rate and extent of gastrointestinal absorption of sirolimus.
Also, the consumption of grapefruit juice may result in increased sirolimus trough concentrations.
MANAGEMENT: Experts recommend that this drug be taken either at least one hour prior to eating or consistently with or without food to avoid variations in sirolimus blood levels.
The manufacturer recommends against using grapefruit juice for dilution of sirolimus doses.
Patients should be monitored for clinical and laboratory evidence of altered immunosuppressant effects.
Yixinke Cholesterol interaction
[Moderate] The use of sirolimus may increase serum cholesterol and triglycerides.
Care should be taken when prescribing this agent to hyperlipidemic patients.
It is recommended to assess the risk It is recommended to monitor patients regularly for elevated lipids.
Yixinke Drug Interaction
Moderate: mycophenolate mofetil, loratadine, losartan, insulin glargine, mycophenolic acidUnknown: aspirin, aspirin, sulfamethoxazole / trimethoprim, carvedilol, apixaban, tamsulosin, furosemide, metoprolol, tacrolimus, pantoprazole, valganciclovir, cyanocobalamin, ergocalciferol, cholecalciferol, cetirizine
Yixinke Disease Interaction
Major: infections, PMLModerate: angioedema, hyperlipidemia, liver disease, liver transplantation, lung dysfunction, lung transplant, renal dysfunction
Half Life
57-63 hours
Innovators Monograph
You find simplified version here Yixinke