Sirolimus tablets are a type of mTOR (mammalian target protein of rapamycin) inhibitor immunosuppressant that specifically blocks mTOR activity, inhibits T lymphocyte activation and proliferation, and exerts immunomodulatory effects.

1、 Drug name

Common name: Sirolimus

Product Name: Rapamune ®

2、 Indications

Prevention of kidney transplant rejection: applicable to patients aged 13 and above who undergo kidney transplantation

Patients with low to moderate immune risk: need to use cyclosporine and corticosteroids in combination, and discontinue cyclosporine 2-4 months after transplantation.

High risk patients: need to use cyclosporine and corticosteroids in combination for the first 12 months after transplantation.

Lymphatic leiomyomatosis (LAM) treatment.

3、 Specifications and characteristics

1mg: Tablets

4、 Main components

Active ingredient: Sirolimus (macrolide mTOR inhibitor)

5、 Usage and dosage

Renal transplant patients:

Take orally once a day, consistent with or different from food intake

Low to moderate risk patients: initial loading dose of 6mg, subsequent maintenance dose of 2mg/day

High risk patients: The maximum loading dose on the first day is 15mg, and the subsequent maintenance dose is 5mg/day

LAM patients: initial dose of 2mg/day, adjusted to 5-15ng/mL based on blood drug concentration

6、 Dose adjustment

Patients with liver dysfunction:

Mild to moderate injury: maintenance dose reduction of approximately ⅓.

Severe injury: The maintenance dose is reduced by about half.

Low weight patients (≥ 13 years old and weight<40kg): Adjust to 1mg/m ²/day based on body surface area.

Therapeutic drug monitoring: All patients are required to monitor the trough concentration of sirolimus.

7、 Medication precautions

Medication time: If used with cyclosporine, it should be taken 4 hours after cyclosporine administration.

8、 Medication for special populations

Pregnant women: Based on animal data, it can cause fetal damage. It is recommended that women of childbearing age adopt efficient contraception during treatment and within 12 weeks after discontinuation of medication.

Breastfeeding period: may cause serious adverse reactions to breastfed infants.

Children: Safety and efficacy have not been established for patients under 13 years old.

Elderly people: The dosage selection should be cautious, usually starting from the lower limit of the dosage range.

9、 Adverse reactions

Common reactions (≥ 30%) in kidney transplant patients: peripheral edema, hypertriglyceridemia, hypertension, hypercholesterolemia, elevated creatinine, abdominal pain, diarrhea, headache, fever, urinary tract infection, anemia, nausea, joint pain, pain, and thrombocytopenia.

Common reactions (≥ 20%) in LAM patients: stomatitis, diarrhea, abdominal pain, nausea, nasopharyngitis, acne, chest pain, peripheral edema, upper respiratory tract infection, dizziness, and muscle pain.

10、 Contraindications

Prohibited for individuals allergic to any ingredient of sirolimus or Rapamune.

11、 Drug interactions

Cyclosporine: It should be taken every 4 hours.

Strong CYP3A4/P-gp inducers or inhibitors should not be used in combination.

Cannabidiol: It is necessary to closely monitor the blood concentration of sirolimus.

Grapefruit juice: Do not consume or dilute oral solutions together.

12、 Storage method

Tablets: Store at room temperature (20-25 ℃).

13、 Important Warning

Prohibited for liver/lung transplant patients: may lead to increased mortality, graft loss, and hepatic artery thrombosis.

Sirolimusinformation