Generic
Tofacitinib
27 brands available in the market
At a glance
Tofacitinib is a Janus kinase inhibitor used to treat moderate to severe rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis. It helps decrease pain, tenderness, and swelling in the joints by reducing inflammation.
Description
Tofacitinib is a partial and reversible Janus kinase (JAK) inhibitor. It blocks the JAK-STAT signaling pathway, reducing the production and modulating proinflammatory cytokines central to rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis.
Indications
- Rheumatoid arthritis
- Psoriatic arthritis
- Ulcerative colitis
Therapeutic class
Immunosuppressant
Pharmacological class
Janus Kinase Inhibitor
Pharmacology
Tofacitinib blocks the JAK-STAT pathway, preventing phosphorylation and activation of STATs. This reduces inflammatory response and immune cell function, providing therapeutic benefit in autoimmune diseases.
Mechanism of action
Blocks Janus kinase enzyme, preventing STAT phosphorylation and activation, thereby reducing inflammation.
Dosage
Adult Dose (Oral):
- Rheumatoid arthritis: 5 mg twice daily
- Psoriatic arthritis: 5 mg twice daily
- Ulcerative colitis: 10 mg twice daily for at least 8 weeks, then 5 or 10 mg twice daily
- Moderate/severe renal or moderate hepatic impairment: 5 mg once daily
Administration
- May be taken with or without food
- Take at the same time each day
- Swallow whole; do not chew, crush or break
Missed dose
If you miss a dose, take it as soon as possible; if almost time for next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Diarrhea
- Headache
- High blood pressure
- Nasal congestion
- Runny nose
- Sore throat
- Upper respiratory tract infection
Precautions & warnings
- Avoid use during active serious infection
- May increase risk of serious infections
- Regular blood tests required
- Avoid live vaccines
- Monitor liver, kidney, blood counts, cholesterol
Contraindications
- Hypersensitivity to active substance or excipients
Drug interactions
- Potent CYP3A4 inhibitors (ketoconazole): increased exposure
- Moderate CYP3A4 & potent CYP2C19 inhibitors (fluconazole): increased exposure
- Potent CYP inducers (rifampin): decreased exposure
- Tacrolimus, cyclosporine: increased AUC, decreased Cmax
- Methotrexate: decreased AUC & Cmax
Food interactions
Consuming alcohol with Tofacitinib does not cause any harmful side effects.
Use in pregnancy
Use in Pregnancy: May be unsafe; animal studies show harmful effects; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably unsafe; may pass into breast milk and harm the baby; consult your doctor.
Pediatric use
Safety and efficacy not established in children under 18 years
Geriatric use
Higher incidence of serious infections in patients 65 years and older; caution advised
Renal / hepatic impairment
Renal Impairment: Moderate to severe: 5 mg once daily
Hepatic Impairment: Moderate: 5 mg once daily; Severe: not recommended
Overdose effects
Symptoms: Bone marrow suppression, infections.
Treatment: Supportive; no specific antidote.
Storage conditions
Store below 30°C; protect from light and moisture; keep out of reach of children.