Pharm

Leflunomide

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Leflunomide, Arava

  1. First line DMARD instead or Methotrexate
  2. Combination with Methotrexate
  • Mechanism
  1. Pyrimidine inhibitor
  2. T-Cell Activation and proliferation inhibitor
  3. Similar to Methotrexate in effects
  4. Onset of action in 1-2 months
  • Efficacy
  1. Comparable to Methotrexate
  2. Used with Methotrexate for maximal effect
  • Adverse effects
  1. Nausea (may limit use)
  2. Alopecia
  3. Liver injury occurs in 1 in 200 patients
    1. Increased Liver transaminases (e.g. AST, SGOT)
  4. Lung injury (observe for new onset cough)
  • Monitoring
  1. Labs:
    1. Aspartate Transaminase (SGOT, AST)
    2. Complete Blood Count with Platelet Count
  2. History
    1. Ask about new onset cough
  3. Timing
    1. Check monthly for 6 months
    2. Check every 6-8 weeks
  • Dose
  1. Loading dose: 100 mg PO qd for 3 days
  2. Maintenance: 10 mg PO qd (or 20 mg PO qod)
  3. Inadequate relief at lower dose: 20 mg PO qd
  • References
  1. Sharp (2000) Arthritis Rheum 43:495-505 [PubMed]