Tofacitinib
Generic Details
Generic Name
Tofacitinib
Other Names
- Xeljanz
Drug Class
- Janus kinase (JAK) inhibitor
Chemical Formula
C16H20N6O
Molecular Weight
312.376 g/mol
Mechanism of Action
- Inhibits Janus kinase enzymes, specifically JAK1 and JAK3, which are involved in the signaling pathways of many cytokines
Indications
- Rheumatoid arthritis
- Psoriatic arthritis
- Ulcerative colitis
Common Dosage Forms
- Tablet
- Extended-release tablet
Typical Dosage
- 5 mg twice daily for rheumatoid arthritis
- 5 mg twice daily for psoriatic arthritis
- 10 mg twice daily for ulcerative colitis
Pediatric Dosage
- Safety and efficacy not established in children under 18
Geriatric Dosage
- Dosage adjustment may be needed in elderly patients
Side Effects
- Increased risk of infection
- Headache
- Diarrhea
- Hypertension
- Elevated liver enzymes
Contraindications
- Hypersensitivity to tofacitinib
- Severe liver impairment
- Severe renal impairment
Pregnancy Category
- Category C - Risk cannot be ruled out
Lactation Safety
- Not recommended during breastfeeding
Drug Interactions
- Biologic DMARDs
- Immunosuppressants
- Anticoagulants
Overdose Symptoms
- Nausea
- Vomiting
- Dizziness
- Increased liver enzymes
Antidote for Overdose
- No specific antidote, symptomatic treatment
Storage Conditions
- Store at room temperature (20-25°C)
- Protect from light and moisture
Pharmacokinetics
- Absorption: Rapid and almost complete
- Distribution: Extensively distributed in the body
- Metabolism: Mainly hepatic
- Excretion: Primarily fecal
Precautions
- Monitor for signs of infection
- Monitor liver function tests regularly
Warnings
- Increased risk of serious infections
- Risk of malignancy
- Thrombosis risk in ulcerative colitis patients
Others
- Avoid live vaccinations during treatment