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Sirolimus (also known as "rapamycin") is a secondary metabolite secreted by soil Streptomyces that was first discovered by scientists in 1975 from the soil of Easter Island in Chile. It is suitable for patients receiving kidney transplants to prevent organ rejection. It is clinically recommended to use sirolimus tablets in combination with cyclosporine and corticosteroids.

Rapamin can be taken orally once a day. Rapamin should be started as soon as possible after transplantation. For new transplant recipients, the loading dose of rapamin should be taken for the first time, that is, 3 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 Rapamune 2 mg daily is better than that of patients taking Rapamune 5 mg daily.

To minimize differences in the absorption of Rapamune, the drug should be taken regularly with or without food. Grapefruit juice slows the metabolism of rapamune, which is regulated by CYP3A4, and should not be used to administer or dilute rapamune.

Sirolimus is poorly absorbed in the gastrointestinal tract, and its oral bioavailability is about 15%. The drug is rapidly absorbed in the body in 1.42 ± 1.20 hours. Sirolimus is widely distributed in various tissues. In patients with stable kidney transplantation, sirolimus has a large apparent distribution volume with obvious individual differences, ranging from 5.6L/kg to 16.7L/kg. The average distribution volume after the first month of life is 12±4.6L/kg. The distribution ratio of whole blood to plasma is large and varies among individuals. Among stable kidney transplant recipients, the average plasma-to-blood ratio is 36 ± 17.9%. Sirolimus, which is sold in India, is very popular among patients. For details, please consult the medical companion travel service.