Pharm

Upadacitinib

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Upadacitinib, Rinvoq

  • See Also
  1. Janus Kinase Inhibitor
  • Indications
  1. Rheumatoid Arthritis
    1. Refractory to non-biologic DMARD
  • Contraindications
  1. Severe hepatic Impairment (Child-Pugh Class C)
  2. Concurrent Immunosuppressants
    1. Biologic DMARDs
    2. Cyclosporine, azathoprine and other potent Immunosuppressants
    3. Probenacid (OAT3 transport inhibitor)
  • Mechanism
  1. See Janus Kinase Inhibitor
  • Dosing
  • Adults
  1. Rheumatoid Arthritis: 15 mg orally daily
  • Adverse Effects
  1. See Janus Kinase Inhibitor
  2. Serious infections (e.g. Sepsis)
  3. Opportunistic infections (e.g. invasive fungal)
  4. Infection Reactivation (e.g. Tb reactivation, Shingles reactivation)
    1. Screen for Latent Tuberculosis before starting
  5. Malignancy including Lymphoma
  6. Major cardiovascular events
  7. Venous Thromboembolism
  8. Hepatotoxicity
  9. Myelosuppression
    1. Lymphopenia
      1. Avoid starting if Absolute Lymphocyte Count <500
    2. Anemia
      1. Avoid starting if Hemoglobin <8 mg/dl
    3. Neutropenia
      1. Avoid starting if Absolute Neutrophil Count (ANC) <1000
  • Safety
  1. Avoid in pregnancy (Unknown safety)
    1. Use reliable Contraception during and for at least 4 weeks after stopping Upadacitinib
  2. Avoid in Lactation
    1. Wait at least 4 days after last dose to begin Breast Feeding
  3. Monitoring (obtain baseline and recheck periodically)
    1. Complete Blood Count
    2. Liver Function Tests
    3. Lipid panel (after 3 months of use)
  • Drug Interactions
  1. See Contraindications above
  2. Strong CYP3A4 Inducers
    1. Lower Upadacitinib levels
  3. Strong CYP3A4 Inhibitors
    1. Raise Upadacitinib levels
  • Resources
  1. Upadacitinib (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2966aec7-2ef0-923c-d8ff-fe1a957bf095