tofacitinib

Tofacitinib inhibits the activity of JAK1 and JAK3, blocks the signal transduction of various inflammatory cytokines, and exerts an anti-inflammatory effect

1. Drug name

1. Common name: Tofacitinib.

2. Trade names: XELJANZ® (tablets), XELJANZ®XR (sustained-release tablets), XELJANZ®OralSolution (oral solution).

2. Indications

1. Rheumatoid arthritis: used for moderately to severely active adult patients with insufficient response to or intolerance to methotrexate.

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

3. Ulcerative colitis: used for moderately to severely active adult patients with insufficient response to or intolerance to TNF blockers.

4. Polyarticular juvenile idiopathic arthritis: used for active patients 2 years old and above.

3. Specifications and properties

Tablet: 5mg.

IV. Main ingredient

Active ingredient: tofacitinib.

5. Usage and Dosage

1. Rheumatoid/psoriatic arthritis: 5mg 2 times a day.

2. Ulcerative colitis:

Maintenance period: 5 mg twice a day (or 11 mg sustained-release tablet once a day).

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

VI. Dose adjustment

1. Renal insufficiency: For moderate to severe patients, adjust the dosage to 5mg once a day.

2. Hepatic insufficiency: For moderate cases, the dosage is adjusted to 5 mg once a day, and for severe cases, it is prohibited.

3. Concomitant medication: Reduce the dose by 50% when using strong CYP3A4 inhibitors.

4. Blood abnormalities: discontinue medication when lymphocytes <500/mm³ or ANC <500/mm³.

7. Medication Precautions

1. It can be taken before or after meals.

2. Sustained-release tablets must be swallowed whole and should not be broken/chewed.

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

4. Vomiting: If you vomit after taking the medicine, there is no need to take a supplement.

8. Medication for special groups

1. Pregnant women: There is no sufficient data, use with caution.

2. Lactation period: Breastfeeding is not recommended.

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

4. The elderly: infection and cardiovascular risks need to be monitored.

9. Adverse reactions

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

2. Severe: infection (including tuberculosis, fungus), thrombosis, malignant tumor, gastrointestinal perforation.

10. Contraindications

1. There are no absolute contraindications, but it is prohibited in the following situations:

(1) Severe active infection.

(2) Severe liver dysfunction.

(3), Lymphocytes <500/mm³ or ANC <1000/mm³.

11. Drug interactions

1. Strong CYP3A4 inhibitors (such as ketoconazole): the dose needs to be reduced.

2. Immunosuppressants: It is prohibited to use biological agents or cyclosporine in combination.

3. Live vaccines: avoid use during vaccination.

12. Storage method

Tablets: Store at 20-25°C.