Rapamune的用法以及用量

Rapamin () inhibits the activation and proliferation of T lymphocytes stimulated by antigens and cytokines (interleukins IL-2, IL-4 and IL-15). It also inhibits the production of antibodies. In cells, rapamune binds to the immunophilin, FK-binding protein-12 (FKBP-12), to generate the FKBP-12 immunosuppressive complex. This complex binds to the mammalian rapamune BA molecule (mTOR, a key regulatory kinase) and inhibits its activity, thereby inhibiting the progression from G1 phase to S phase in the cell cycle.

Usage and dosage of Rapamune: It is recommended to use Rapamune in combination with cyclosporine and corticosteroids. Rapamune is for oral administration, once a day. Rapamune should be started as soon as possible after transplantation. For new transplant recipients, a 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 Rapamune daily was better than that of patients taking 5 mg of Rapamune daily. To minimize differences in the absorption of Rapamune, Rapamune should be taken consistently with or without food. Dose adjustment: For patients over 13 years of age but weighing less than 40 kg, the starting dose should be adjusted to 1 mg/m2/day based on body surface area, and the loading dose should be 3 mg/m2. It is recommended that the maintenance dose of this drug be reduced by approximately 1/3 in patients with liver function impairment, but the loading dose does not need to be adjusted. The pharmacokinetics of rapamycin have not been studied in patients with severe hepatic impairment. No dosage adjustment is required in patients with renal impairment.