Tofacitinib exerts anti-inflammatory effects by inhibiting the activity of JAK1 and JAK3, blocking the signal transduction of various inflammatory cytokines

1、 Drug name

1. Common name: Tofacitinib.

2. Product Name: XELJANZ ® (tablets) XELJANZ ® XR (sustained-release tablets) XELJANZ ® Oral Solution.

2、 Indications

1. Rheumatoid arthritis: Used for moderate to severe active adult patients with insufficient or intolerant response to methotrexate.

2. Psoriatic arthritis: Used for adult patients with insufficient or intolerant response to methotrexate or other DMARDs.

3. Ulcerative colitis: Used for moderate to severe active adult patients with insufficient response or intolerance to TNF blockers.

4. Multi joint juvenile idiopathic arthritis: used for active patients aged 2 years and above.

3、 Specifications and characteristics

Tablets: 5mg.

4、 Main components

Active ingredient: Tofacitinib.

5、 Usage and dosage

1. Rheumatoid/psoriatic arthritis: 5mg twice a day.

2. Ulcerative colitis:

Maintenance period: 5mg twice daily (or 11mg sustained-release tablets once daily).

Pediatric patients: Adjust the dosage according to body weight (3.2mg-5mg twice daily).

6、 Dose adjustment

1. Renal insufficiency: For moderate to severe cases, adjust to 5mg once daily.

2. Liver dysfunction: moderate cases are adjusted to 5mg once daily, and severe cases are contraindicated.

3. Combination therapy: Reduce dosage by 50% when using strong CYP3A4 inhibitors.

4. Blood abnormalities: Discontinue medication when lymphocytes are less than 500/mm ³ or ANC is less than 500/mm ³.

7、 Medication precautions

1. It can be taken before and after meals.

2. The sustained-release tablets should be swallowed whole and should not be broken or chewed.

3. Missed medication: Take it as soon as possible, skip if it is close to the next medication time.

4. Vomiting: If vomiting occurs after taking medication, there is no need to take additional medication.

8、 Medication for special populations

1. Pregnant women: Without sufficient data, use with caution.

2. Breastfeeding period: It is not recommended to breastfeed.

3. Children: Only applicable for PCJIA indications (≥ 2 years old).

4. Older adults: need to be monitored for infection and cardiovascular risk.

9、 Adverse reactions

1. Common: Upper respiratory tract infection, nasopharyngitis, diarrhea, headache.

2. Serious: infection (including tuberculosis, fungi), thrombosis, malignant tumor, gastrointestinal perforation.

10、 Contraindications

1. There are no absolute taboos, but the following situations are prohibited:

(1) Severe active infection.

(2) Severe liver dysfunction.

(3) Lymphocytes<500/mm ³ or ANC<1000/mm ³.

11、 Drug interactions

1. Strong CYP3A4 inhibitors (such as ketoconazole): need to be reduced.

2. Immunosuppressants: Combination use of biological agents or cyclosporine is prohibited.

3. Live vaccine: Avoid use during vaccination.

12、 Storage method

Tablets: Store at 20-25 ℃.

tofacitinibinformation