Sirolimus tablets, as immunosuppressants, are contraindicated to individuals with specific disease states, physiological stages, and drug allergies. They should be avoided in combination with specific foods/drugs and strictly follow dosage limits and monitoring requirements to ensure medication safety.

1. Taboo population

(1) Allergic constitution

It is contraindicated for individuals allergic to sirolimus or its excipients (such as lactose), as it may cause severe hypersensitivity reactions.

(2) Pregnant women

Animal experiments have shown embryonic toxicity, and pregnant women may use it to cause fetal malformations. Therefore, strict contraception is required until 12 weeks after discontinuation of the medication.

(3) Severe liver and kidney dysfunction

Patients with Child Pugh C grade or CrCl<30mL/min are contraindicated as decreased metabolic clearance may exacerbate toxicity.

(4) Active infection

Uncontrolled bacterial/viral/fungal infections are contraindicated, as immunosuppressive effects may exacerbate the infection.

2. Forbidden foods

(1) Grapefruit and its products

Containing strong CYP3A4 inhibitors can increase the blood concentration of sirolimus by 3-5 times, increasing the risk of adverse reactions.

(2) High-fat diet

Taking it after meals can reduce absorption by 28%, and it should be administered on an empty stomach or on a fixed low-fat diet.

3. Restrictive conditions

(1) Upper limit of dosage

The maintenance dose for adults is usually ≤ 2mg/day, and the blood drug concentration should be maintained at 4-12ng/mL. Excessive doses may cause pulmonary toxicity.

(2) Combination therapy

Do not use in combination with potent CYP3A4/P-gp inhibitors (such as ketoconazole) or inducers (such as rifampicin), with an interval of ≥ 2 weeks.

(3) Monitoring requirements

At the beginning of medication, blood routine, blood lipids, and liver and kidney function should be tested weekly. After stabilization, monthly follow-up should be conducted, and proteinuria should be evaluated immediately.

(4) Vaccination

During the medication period, live vaccines (such as measles vaccine) are prohibited, and the response to inactivated vaccines may be weakened. It is recommended to receive them in advance.