Rheumatology Book

http://www.fpnotebook.com/

Leflunomide

Aka: Leflunomide, Arava
  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 43:495-505

leflunomide (C0063041)

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)
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)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C045463
SnomedCT 109143003, 386981009
English 4-Isoxazolecarboxamide, 5-methyl-N-(4-(trifluoromethyl)phenyl)-, leflunomide, N-(4-trifluoromethyphenyl)-5-methylisoxazole-4-carboxamide, 4-Isoxazolecarboxamide, 5-Methyl-N-(4-(trifluoromethyl)phenyl)-, leflunomide (medication), LEFLUNOMIDE, leflunomide [Chemical/Ingredient], Leflunomide (product), Leflunomide (substance), Leflunomide
Spanish leflunomida (producto), leflunomida (sustancia), leflunomida
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Arava (C0718644)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C045463
English arava, Hoechst Brand of Leflunomide, Aventis Behring Brand of Leflunomide, Aventis Brand of Leflunomide, Aventis Pharma Brand of Leflunomide, Arava
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Navigation Tree