Rapamune

Commodity name: Rapamune

English name:Rapamune

Common name:Tsirolimus tablets

English common name: Sirolimu

Main ingredients:

The main ingredient of this product is sirolimus

Characteristics:< /b>

This product is a triangular white or off-white sugar-coated tablet

Indications:

It is suitable for patients who have received kidney transplants to prevent organ rejection. Recommended for use in combination with cyclosporine and corticosteroids.

Mechanism of action:

Sirolimus 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, sirolimus binds to the immunophilin, FK-binding protein-12 (FKBP-12), to generate the FKBP-12 immunosuppressive complex. This complex binds to the mammalian sirolimus BA molecule (mTOR, a key regulatory kinase) and inhibits its activity, thereby inhibiting the progression from the G1 phase to the S phase in the cell cycle.

Usage and dosage:

It is recommended to use it in combination with cyclosporine and corticosteroids. Take orally, once daily. It should be started as soon as possible after transplantation. For new transplant recipients, the loading dose that should be taken for the first time 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. Daily administration of rapamin is recommended in combination with cyclosporine and corticosteroids. The overall safety profile of patients taking Rapamune 2 mg daily was better than that of patients taking Rapamune 5 mg daily

Adverse Reactions:

The frequency of adverse reactions listed below includes adverse reactions reported in patients taking Rapamune, cyclosporine, and corticosteroids concomitantly. Overall, adverse events associated with taking rapamycin uf0d2 are dose/concentration dependent.

According to the classification of CIOMS adverse reaction incidence, the list of adverse reactions is as follows:

Very common: ≥10%

Common: ≥1% and <10%

Rare: ≥0.1% and <1%

Rare: ≥0.01% and <0.1%

Very rare: <0.01%

Hepatotoxicity

Hepatotoxicity has been reported, including fatal hepatic necrosis due to elevated trough sirolimus concentrations (i.e., above therapeutic levels).

Poor healing

There have been reports of poor healing after transplantation, including fascial dehiscence, incisional hernia, and rupture of anastomosis sites (such as wounds, blood vessels, airways, ureters, biliary tracts, etc.).

Other clinical experiences

Spermia has also been reported in patients receiving rapamycin, and most patients will improve after stopping rapamycin.

Clostridium difficile enterocolitis has been reported in patients receiving sirolimus.

Contraindications:

Rapamin is contraindicated in patients who are allergic to sirolimus, derivatives of sirolimus, or to any component of this product.

Pregnant and lactating women:

Pregnancy

Rapamin has not been studied in pregnant women. In animal studies, sirolimus has been associated with embryonic/fetal toxicity, manifested by stillbirth and reduced fetal weight (concomitant with delayed skeletal ossification).

During pregnancy, rapamin should be used only if the potential benefits outweigh the potential risks to the embryo/fetus.

Instructions for effective contraception: See [Precautions] - General Precautions, Contraceptive Pregnancy Category C: In rats at dosage groups of 0.1 mg/kg and above (approximately 0.2-0.5 times the clinical dose corrected by body surface area), sirolimus is toxic to embryos and fetuses, manifesting as stillbirth and fetal weight loss (accompanied by delayed bone ossification). But no abnormalities appeared. When rapamycin is used in combination with cyclosporine, the embryo/fetal mortality rate in mice is higher than when rapamycin is used alone. Rapamin administered to female rabbits at a toxic dose of 0.05 mg/kg (approximately 0.3-0.8 times the clinical dose corrected by body surface area) has no effect on the development of fetal rabbits. Adequate and well-controlled clinical trials have not been conducted in pregnant women. Effective contraception should be used before starting treatment with rapamin, during treatment, and for 12 weeks after stopping treatment. During pregnancy, rapamycin should be used only if the potential benefits outweigh the potential risks to the embryo/fetus.

Drugs during lactation

Sirolimus is secreted in trace amounts in the milk of lactating rats. It is unknown whether sirolimus is excreted in human milk. The pharmacokinetics and safety of sirolimus in infants are also unclear. Considering that many drugs are excreted in human milk and the potential adverse effects of sirolimus in nursing infants, the decision to discontinue breastfeeding or discontinue the drug should be based on the importance of the drug to the mother.

Pediatric use:

The safety and efficacy of rapamycin in children under 13 years of age have not been established. If used in pediatric patients under 13 years of age, monitoring of whole blood trough concentrations of sirolimus is recommended.

The safety and effectiveness of rapamycin have been studied in children 13 years of age and older who are at low to moderate immunological risk. The use of rapamycin in this population of children 13 years of age and older has been supported by adequate, well-controlled clinical trials of rapamycin oral solution in adults. Pharmacokinetic data in pediatric transplant patients were specifically analyzed in these trials.

Geriatric use:

In the clinical trials of rapamycin, a sufficient number of patients aged 65 and above were not included to determine whether the safety and efficacy of the drug in this population were different from those in younger patients. Sirolimus whole blood trough concentration data suggest that for elderly renal transplant patients, there is no need to adjust the dose based on age. Differences in response between younger and older patients were not identified. In general, dosage selection for elderly patients should be cautious, considering the higher frequency of weakened liver and cardiac function or other comorbidities or concomitant use of other drugs in the elderly, and treatment is usually started at the low end of the dosage range.

Storage:

Shield, seal, and store below 25°C.