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Tofacitinib: Uses, Dosage, Side Effects & Brands | MedexInfo

Tofacitinib: Uses, Dosage, Side Effects & Brands | MedexInfo

Tofacitinib

Rx
Generic NameTofacitinib
Therapeutic ClassJanus kinase (JAK) inhibitor
Common Dose5 mg twice daily (immediate-release) or 11 mg once daily (extended-release)
Max / 24h20 mg (ulcerative colitis), 10–11 mg (RA/psoriatic arthritis)
PregnancyAvoid; use contraception
Indications ▼
Moderate to severe rheumatoid arthritis in adults with inadequate response to methotrexate
Active psoriatic arthritis in adults
Moderate to severe ulcerative colitis in adults
Investigational use in ankylosing spondylitis and other autoimmune conditions
Mechanism & Pharmacokinetics ▼
Mechanism: Tofacitinib inhibits Janus kinase (JAK) enzymes, reducing phosphorylation of STAT proteins and downstream cytokine signaling, leading to decreased inflammation in autoimmune diseases.
Pharmacokinetics: Rapid oral absorption; peak plasma levels ~1 hour. Metabolized primarily by CYP3A4. Half-life ~3 hours (immediate-release). Excreted mainly via urine (~70%) and feces (~30%).
Dosage & Administration ▼
IndicationFormDoseFrequency
Rheumatoid arthritisImmediate-release tablet5 mgTwice daily
Rheumatoid arthritisExtended-release tablet11 mgOnce daily
Ulcerative colitisImmediate-release tablet10 mgTwice daily for 8 weeks, then 5 mg twice daily
Psoriatic arthritisImmediate-release tablet5 mgTwice daily
Note: Dose adjustment may be required in renal or hepatic impairment. Avoid abrupt discontinuation. Monitor blood counts and liver function.
Side Effects ▼
Upper respiratory tract infections
Headache, dizziness
Diarrhea, nausea
Increased risk of herpes zoster
Elevated liver enzymes, lipid changes
Rare: thromboembolism, malignancy, cytopenias
Contraindications ▼
Active serious infection (sepsis, tuberculosis)
Hypersensitivity to tofacitinib
Severe hepatic impairment (Child-Pugh C)
Pregnancy or breastfeeding unless benefit outweighs risk
Drug Interaction ▼
Strong CYP3A4 inhibitors (e.g., ketoconazole) increase exposure
Strong CYP3A4 inducers (e.g., rifampicin) reduce efficacy
Live vaccines: avoid during treatment
Other immunosuppressants: additive immunosuppression
Pregnancy & Lactation ▼
Not recommended during pregnancy; use effective contraception
Breastfeeding not recommended due to immunosuppressive effect
Clinical / Research Summary ▼
Clinical Role: Oral JAK inhibitor for autoimmune conditions unresponsive to conventional therapy.
Advantage: Rapid onset of action, convenient oral dosing, effective in multiple inflammatory pathways.
Monitoring: CBC, liver function, renal function, lipid profile; screen for infections before and during therapy.
Patient Counseling Points ▼
Take exactly as prescribed; do not skip or double doses
Report signs of infection (fever, cough, sore throat)
Avoid live vaccines during therapy
Use contraception during and 4 weeks after therapy
Regular follow-up with labs and physician required
Storage & Handling ▼
Store below 25°C, in original container
Protect from moisture and light
Keep out of reach of children
Medical Disclaimer: For educational purposes only. Not a substitute for professional medical advice.

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