Specific contraindications for the use of Simorox tablets
1. Sirolimus is only for use by physicians experienced in immunosuppressive therapy and the management of kidney transplant patients. Patients receiving this drug should be treated in an institution equipped with appropriate laboratory and auxiliary medical facilities and personnel. Physicians responsible for maintenance therapy should have complete information necessary for patient follow-up.
2. It is recommended to use sirolimus in combination with cyclosporine and corticosteroids.
3. Sirolimus is taken orally, once a day, with or without food.
4. The bioavailability of crushed, chewed, or cut tablets has not been established and such use is not recommended. Oral solutions should be prescribed and instructed to use in patients who cannot take tablets.
5. Sirolimus should be started as soon as possible after transplantation. It is recommended that sirolimus should be taken 4 hours after cyclosporine oral solution (modified) and/or cyclosporine capsules (modified) [cyclosporine microemulsion (modified)] (see [Drug Interactions]). ]).
6. Frequent adjustment of the sirolimus dose based on unstable sirolimus plasma concentrations may lead to overdose or underdose because of the longer half-life of sirolimus. Once the maintenance dose of sirolimus is adjusted, patients should continue to take the new maintenance dose for at least 7-14 days before further dose adjustments are made under blood level monitoring.
In most patients, dose adjustments can be calculated based on a simple ratio: new sirolimus dose = current dose × (target plasma concentration/current plasma concentration).
When the trough concentration of sirolimus needs to be greatly increased, a loading dose can be considered on the basis of the new maintenance dose: sirolimus loading dose = 3 × (new maintenance dose - current maintenance dose).
The maximum administered dose of sirolimus should not exceed 40 mg/day. If the estimated daily dose of sirolimus exceeds 40 mg due to an additional loading dose, the loading dose may be administered over two days. Sirolimus trough levels should be monitored for at least 3-4 days after taking a loading dose.
7. The 2 mg sirolimus oral solution has been proven to be clinically equivalent to 2 mg sirolimus tablets, and therefore, can be interchanged in equal amounts. However, the clinical equivalence of larger doses of sirolimus oral solution to larger doses of tablets is unknown (see Pharmacokinetics).
8. To minimize differences in the absorption of sirolimus, this drug should be taken consistently with or without food. Grapefruit juice slows CYP3A4-mediated metabolism of sirolimus and potentially enhances P-glycoprotein (P-gp)-mediated reverse translocation of sirolimus from intestinal epithelial cells to the lumen and is therefore not available In the delivery of sirolimus.
9. Combination of sirolimus and cyclosporine in patients with low to moderate immune risk: For new kidney transplant recipients, the combination of sirolimus with cyclosporine and corticosteroids is recommended. The loading dose of sirolimus 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. To maintain sirolimus plasma levels within the target range, sirolimus plasma levels should be monitored. Although a loading dose of 15 mg and a maintenance dose of 5 mg/day have been used in clinical trials to be safe and effective, the efficacy of doses above 2 mg in renal transplant patients is unclear. The overall safety profile of patients taking sirolimus oral solution 2 mg daily was better than that of patients taking sirolimus oral solution 5 mg daily.
10. Dosage adjustment
(1) Low body weight patients:
The starting dose for patients aged 13 years and above but weighing less than 40kg should be adjusted to 1 mg/m2/day based on body surface area. The loading dose should be adjusted to 3 mg/m2.
(2) Patients with hepatic impairment:
It is suggested that the maintenance dose of sirolimus in patients with hepatic impairment can be reduced by about 1/3 to 1/2. The loading dose of sirolimus does not require adjustment: (see Pharmacokinetics). In patients with hepatic impairment, monitoring of trough sirolimus concentrations is recommended.
(3) Patients with impaired renal function:
No need to adjust the loading dose of sirolimus. No dose adjustment is required for renal impairment.
(4) Pediatric use:
The safety and efficacy of sirolimus in children under 13 years of age have not been established. The safety and efficacy of sirolimus have been studied in children 13 years of age and older with low to moderate immune risk. The use of sirolimus in this population of children 13 years of age and older is supported by adequate, well-controlled clinical trials of adult sirolimus oral solution. In particular, pharmacokinetic data in pediatric kidney transplant patients were analyzed in these trials (see Pharmacokinetics).
(5) Medication in elderly patients:
No dose adjustment is required.
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