雷帕鸣口服液和片剂的区别

For use only by physicians experienced with immunosuppressive therapy and managing renal transplant patients. Patients receiving this drug should be treated in an institution with appropriate laboratory and ancillary medical facilities and personnel. Physicians responsible for maintenance therapy should have complete information necessary for patient follow-up. Rapamin tablets are recommended for use in combination with cyclosporine and corticosteroids. Rapamin is taken orally once a day, regularly with or without food. Because the bioavailability of crushed, chewed, or cut tablets has not been established, such use is not recommended. Patients who cannot take tablets should be prescribed the oral solution and instructed on its use. Rapamin should be started as soon as possible after transplantation.

It is recommended that rapamycin should be taken 4 hours after taking cyclosporine oral solution (modified) and/or cyclosporine capsules (modified) [cyclosporine microemulsion (modified)]. Frequent adjustments of rapamin dosage based on unstable sirolimus plasma concentrations may result in overdose or underdosing because of the long half-life of sirolimus.

Once the maintenance dose of rapamin is adjusted, the patient should remain on the new maintenance dose for at least 7-14 days before further dose adjustments are made with monitoring of plasma concentrations. In most patients, dose adjustments can be calculated based on a simple ratio: new Rapamin® dose = current dose × (target plasma concentration/current plasma concentration). When the trough concentration of sirolimus needs to be significantly increased, a loading dose may be considered based on the new maintenance dose: Rapamamine loading dose = 3 × (new maintenance dose – current maintenance dose).

The maximum dose of rapamycin should not exceed 40 mg/day. If the daily dose of rapamin is estimated to exceed 40 mg due to an additional loading dose, the loading dose may be given on more than two days. After a loading dose, sirolimus trough concentrations should be monitored for at least 3-4 days. Rapamin oral solution 2 mg has been shown to be clinically equivalent to Rapamin tablets 2 mg and, therefore, are interchangeable in equivalent amounts.

However, the clinical equivalence of higher doses of rapamycin oral solution to higher dose tablets is unknown. To minimize differences in the absorption of rapamycin, the drug should be taken consistently with or without food. Grapefruit juice can slow down the metabolism of rapamin mediated by CYP3A4 and potentially enhance the reverse transport of rapamin from the small intestinal epithelial cells to the intestinal lumen mediated by P-glycoprotein (P-gp), so it should not be used to deliver rapamin. Rapamune in combination with cyclosporine in patients with low to moderate immune risk: For new kidney transplant recipients, Rapamune in combination with cyclosporine and corticosteroids is recommended. A loading dose of rapamin should be taken for the first time, which is 3 times the maintenance dose. The recommended loading dose for renal transplant patients is 6 mg and the maintenance dose is 2 mg/day. To maintain sirolimus plasma concentrations within the target range, sirolimus plasma concentrations should be monitored. Although the loading dose of 15 mg and the maintenance dose of 5 mg/day used in clinical trials are safe and effective, the efficacy benefit of doses above 2 mg in renal transplant patients is unclear. The overall safety profile of patients taking 2 mg of rapamycin oral solution daily was better than that of patients taking 5 mg daily oral solution.