Leflunomide

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Arava; Belgium: Arava; Cyprus: Arava; Czech Republic: Arava, Leflunomid; Denmark: Arava; Estonia: Arava; Finland: Arava; France: Arava; Germany: Arava; Greece: Arava; Hungary: Arava; Ireland: Arava; Italy: Arava; Latvia: Arava; Lithuania: Arava; Luxembourg: Arava; Malta: Arava; Netherlands: Arava; Poland: Arava; Portugal: Arava; Romania: Arava; Slovakia: Arava; Slovenia: Arava; Spain: Arava; Sweden: Arava; UK: Arava.

North America

Canada: Arava, Leflunomide; USA: Arava, Leflunomide.

Latin America

Argentina: Afiancen, Arava, Filartros, Inmunoartro, Lefluar, Leflunomida SC; Brazil: Arava; Mexico: Arava.

Asia

Japan: Arava.

Drug combinations

Chemistry

Leflunomide: C~12~H~9~F~3~N~2~O~2~. Mw: 270.21. (1) 4-Isoxazolecarboxamide, 5-methyl-N-[4-(trifluoromethyl)phenyl]-; (2) α,α,α-Trifluoro-5-methyl-4-isoxazolecarboxy-p-toluidide. CAS-75706-12-6 (1998).

Pharmacologic Category

Biologic Response Modifiers. Disease-modifying Antirheumatic Drugs. (ATC-Code: L04AA13).

Mechanism of action

Inhibits pyrimidine synthesis, resulting in antiproliferative and anti-inflammatory effects. For cytomegalovirus (CMV), may interfere with virion assembly.

Therapeutic use

Treatment of active rheumatoid arthritis.

Pregnancy and lactiation implications

Associated with teratogenic and embryolethal effects in animal models at low doses. Leflunomide contraindicated in pregnant women or women of childbearing potential who are not using reliable contraception. Pregnancy must be excluded prior to initiating treatment. Contraindicated during lactation.

Unlabeled use

Treatment of CMV disease.

Contraindications

Hypersensitivity to leflunomide or any component of the formulation. Pregnancy.

Warnings and precautions

Women of childbearing potential. Rare cases of dermatologic reactions (including Stevens-Johnson syndrome and toxic epidermal necrolysis) reported. Rare reports of hepatotoxicity, hepatic failure, and death with use. Might increase susceptibility to infection, including opportunistic pathogens. Caution when considering use in history of new/recurrent infections, with conditions which predispose patients to infections, or with chronic, latent, or localized infections. Use associated (rarely) with interstitial lung disease. Use may affect defenses against malignancies. Use with caution in prior history of significant hematologic abnormalities including bone marrow dysplasia; use associated with rare pancytopenia, agranulocytosis, and thrombocytopenia, particularly when given in combination with methotrexate or other immunosuppressive agents. Avoid use in hepatic impairment or evidence of hepatitis B or C. Use with caution in renal impairment (will increase uric acid excretion). Contraindicated during pregnancy. Live vaccines should not be given concurrently.

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