II. Indications
- Rheumatoid Arthritis (moderate to severe, refractory to non-biologic DMARD)
- Psoriatic Arthritis (moderate to severe, refractory to non-biologic DMARD)
- Ulcerative Colitis (moderate to severe, refractory to TNF agents)
III. Contraindications
- Severe hepatic Impairment
- Live Vaccines (including Herpes Zoster Vaccine)
- Concurrent Immunosuppressants
- Biologic DMARDs
- Cyclosporine, azathoprine and other potent Immunosuppressants
- Probenacid (OAT3 transport inhibitor)
IV. Precautions
- Multiple FDA black box warnings
- Serious infections
- Thrombosis (e.g. Venous Thromboembolism)
- Cardiovascular events (e.g. Myocardial Infarction)
- Lung Cancer
- Increased mortality
- References
- (2021) Presc Lett 28(4): 22
V. Mechanism
VI. Medications
- Tofacitinib (Xeljanz): 5 mg tablets
- Tofacitinib Extended Release (Xeljanz XR): 11 mg
- Do not cut, split or chew extended release tablets
VII. Dosing: Adults
-
Rheumatoid Arthritis or Psoriatic Arthritis
- Tofacitinib 5 mg orally twice daily
- Tofacitinib XR 11 mg orally once daily
- May be given with non-biologic DMARD
-
Ulcerative Colitis
- Start induction: 10 mg orally twice daily for 8 weeks (up to 16 weeks)
- Maintenance: 5 mg orally twice daily (up to 10 mg orally twice daily in lower dose ineffective)
- Lower dose indications (decreasing frequency to once daily or decreasing dose to 50%)
- Strong CYP3A4 Inhibitor (e.g. Fluconazole, Carbamazepine, Phenobarbital, Phenytoin, Rifampin, St. Johns Wort)
- Moderate CYP3A4 Inhibitor AND Strong CYP2C19 Inhibitor
- Myelosuppression (lymphopenia, Neutropenia, Anemia)
- Moderate to severe renal Impairment (and dose after Hemodialysis)
- Moderate hepatic Impairment (avoid in severe hepatic Impairment)
VIII. Adverse Effects
- See Janus Kinase Inhibitor
- See precautions above
- Serious infections
- Opportunistic infections
- Major cardiovascular events
- Malignancy including Lymphoma
- Venous Thromboembolism
- Infection Reactivation (e.g. Tb reactivation, Hepatitis BVirus, Shingles reactivation)
- Screen for Latent Tuberculosis, Viral Hepatitis before starting
- Gastrointestinal perforation (esp. if history of Diverticulitis)
- Hepatotoxicity
- Hyperlipidemia
- Myelosuppression
- Lymphopenia
- Avoid starting if Absolute Lymphocyte Count (ALC) <500
- Stop if ALC <500
- Anemia
- Avoid starting if Hemoglobin <9 mg/dl
- Neutropenia
- Avoid starting if Absolute Neutrophil Count (ANC) <1000
- Stop if ANC <500
- Lymphopenia
IX. Safety
- Avoid in pregnancy (Unknown safety)
- Use reliable Contraception during and for at least 4 weeks after stopping Tofacitinib
- Avoid in Lactation
- Wait at least 4 days after last dose to begin Breast Feeding
- Monitoring (obtain baseline and recheck periodically every 3 months)
- Complete Blood Count
- Liver Function Tests
- Lipid panel (after 1-2 months of use)
X. Drug Interactions
- See Contraindications above
- Strong CYP3A4 Inhibitors
- Strong CYP2C19 Inhibitors
XI. Resources
Images: Related links to external sites (from Bing)
Related Studies
| xeljanz (on 1/1/2023 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| XELJANZ 5 MG TABLET | $89.28 each | |
| XELJANZ XR 11 MG TABLET | $178.55 each | |