sirolimus的注意事项

Sirolimus is a new type of immunosuppressant developed by the American Wyeth Company. The drug was approved by the FDA as early as September 1999 and officially launched in the United States. It was later approved for sale in China in 2002, providing certain help for the treatment of domestic kidney transplant patients.

Despite this, patients still need to pay attention to the following aspects during actual treatment:

1. General precautions

(1) Sirolimus is for oral administration only.

(2) There have not been sufficient clinical studies to confirm the use of sirolimus in patients with high immune risk, so its use in this patient group is not recommended.

2. Monitoring method of sirolimus blood concentration

The recommended 24-hour blood trough concentration range of sirolimus is based on a chromatographic method. In current clinical experience, both chromatographic and immunoassay methods can be used to measure whole blood concentrations of sirolimus. Concentration values ​​measured by these different methods are not interchangeable.

3. Contraception

Effective contraception should be used before initiation of sirolimus treatment, during maintenance of treatment, and for 12 weeks after discontinuation of treatment.

4. Vaccination

Immunosuppressants may affect the effectiveness of vaccination. The effectiveness of the vaccine may be reduced if the vaccine is received during treatment with immunosuppressants, including sirolimus. Live vaccines should be avoided during sirolimus treatment.

5. Laboratory examination

Sirolimus whole blood concentrations should be monitored in patients taking sirolimus under concentration monitoring. Sirolimus plasma concentrations must be monitored closely in the following patients: patients with altered drug metabolism, patients aged ≥13 years and weighing less than 40 kg, patients with hepatic impairment, and patients taking concurrently strong inducers and inhibitors of CYP3A4. In patients with severe hepatic impairment, it is recommended to reduce the maintenance dose by half based on decreased clearance. Due to the prolonged half-life in these patients, therapeutic monitoring of the drug product should be extended after loading doses or dose changes until stable concentrations are achieved.