Rheumatology Book

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LeflunomideAka: Arava

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  1. Indications: Rheumatoid Arthritis
    1. First line DMARD instead or Methotrexate
    2. Combination with Methotrexate
  2. 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
  3. Efficacy
    1. Comparable to Methotrexate
    2. Used with Methotrexate for maximal effect
  4. 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)
  5. 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
  6. 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
  7. References
    1. Sharp (2000) Arthritis Rheum 43:495

leflunomide (C0063041)

Definition (NCI)An anticancer drug that works by inhibiting a cancer cell growth factor. Also called SU101.
Definition (PDQ)A derivative of isoxazole used for its immunosuppressive and anti-inflammatory properties. As a prodrug, leflunomide is converted to an active metabolite, A77 1726, which blocks dihydroorotate dehydrogenase, a key enzyme of de novo pyrimidine synthesis, thereby preventing the expansion of activated T lymphocytes. This agent also inhibits various protein tyrosine kinases, such as protein kinase C (PKC), thereby inhibiting cell proliferation. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42253&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42253&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1128" NCI Thesaurus)
Definition (NCI)A derivative of isoxazole used for its immunosuppressive and anti-inflammatory properties. As a prodrug, leflunomide is converted to an active metabolite, A77 1726, which blocks dihydroorotate dehydrogenase, a key enzyme of de novo pyrimidine synthesis, thereby preventing the expansion of activated T lymphocytes. This agent also inhibits various protein tyrosine kinases, such as protein kinase C (PKC), thereby inhibiting cell proliferation. (NCI04)
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC045463
Englishleflunomide, LEFLUNOMIDE PREPARATION
Spanishleflunomida
Parent ConceptsPyrimidine analog (C0280039), Dihydroorotate Dehydrogenase Inhibitor (C1511961), Angiogenesis Activator Inhibitor (C1515993), Isoxazoles (C0022266), Other antirheumatics (C0973578), Antirheumatic Agents (C0003191), Drug allergen (C1320237), Immunomodulators (C1527392)
SourcesLNC, MSH, MTHSPL, NCI, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Arava (C0718644)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC045463
EnglishArava, Aventis Behring Brand of Leflunomide, Aventis Brand of Leflunomide, Aventis Pharma Brand of Leflunomide, Hoechst Brand of Leflunomide
SourcesMSH, MTH, NCI, PDQ, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)



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