雷帕鸣的功效与作用

The role and efficacy of rapamin (sirolimus tablets, sirolimus): It is suitable for patients receiving kidney transplants to prevent organ rejection. It is recommended to be used in combination with cyclosporine and corticosteroids.

Sirolimus is a triene macrolide antibiotic extracted from Streptomyces culture fluid and is a T cell inhibitor. This product has a different mechanism of action from other immunosuppressants. This product inhibits the activation and proliferation of T lymphocytes stimulated by antigens and cytokines (interleukin IL-2, IL-4 and IL-15), and also inhibits the production of antibodies. This complex binds to the mammalian sirolimus target molecule (a regulatory kinase) and inhibits its activity, blocking the proliferation of cytokine-driven T cells, that is, inhibiting the progression from the G1 phase to the S phase in the cell cycle. This product is rapidly absorbed after oral administration, with an average peak time of 1 hour in healthy volunteers. In kidney transplant recipients, the average peak time after multiple oral doses is approximately 2 hours, and the bioavailability is approximately 14%. In renal transplant recipients, the mean blood/plasma concentration ratio of this product was 36, indicating widespread distribution of this product into the formed components of the blood. This product is cytochrome P4503A4.

Rapamin is taken orally, once a day. It should be started as soon as possible after transplantation. For new transplant recipients, the loading dose of Rapamune should be taken for the first time, which is three times the maintenance dose. The recommended loading dose for kidney transplant patients is 6 mg and the maintenance dose is 2 mg/day. Although the loading dose of 15 mg and the maintenance dose of 5 mg/day used in clinical trials are safe and effective, the therapeutic benefits of doses above 2 mg are unclear for kidney transplant patients. The overall safety profile of patients taking 2 mg of rapamide daily was better than that of patients taking 5 mg rapamide daily. Rapamin (sirolimus) is used in combination with cyclosporine and corticosteroids.