Leflunomide

Aka: Leflunomide, Arava

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II. Indications: Rheumatoid Arthritis

  1. First line DMARD instead or Methotrexate
  2. Combination with Methotrexate

III. 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

IV. Efficacy

  1. Comparable to Methotrexate
  2. Used with Methotrexate for maximal effect

V. 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)

VI. 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

VII. 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

VIII. References

  1. Sharp (2000) Arthritis Rheum 43:495-505 [PubMed]

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Cost: Medications

leflunomide (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
LEFLUNOMIDE 10 MG TABLET Generic $3.88 each
LEFLUNOMIDE 20 MG TABLET Generic $3.29 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

Ontology: 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_NCI-GLOSS) An anticancer drug that works by inhibiting a cancer cell growth factor.
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 Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C045463
SnomedCT 109143003, 386981009
LNC LP34970-1, MTHU017708
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
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Arava (C0718644)

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

Related Topics in Pharmacology

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