レフルノミド

使用用途

• Rheumatoid arthritis
• Immunosuppressive as part of a protocol (with cyclosporine) following organ transplant
• Adjunctive immunosuppressive for immune-mediated hemolytic anemia
• Treatment of systemic and cutaneous reactive histiocytosis
• Treatment of Evans' Syndrome in a diabetic dog

投与方法

考えられる副作用

• Decreased appetite
• Lethargy
• Vomiting
• Diarrhea
• Lymphopenia
• Anemia
• Alopecia
• Rash
• Hepatotoxicity
• Severe dermatologic reactions (Toxic Epidermal Necrolysis, Stevens-Johnson syndrome - reported in humans)
• Gastrointestinal upset (vomiting, diarrhea, anorexia)
• Bone marrow suppression (leukopenia, anemia, thrombocytopenia)
• Unexplained bleeding

注意事項と禁忌

• Pregnancy (Category X teratogen)
• Hypersensitivity to leflunomide
• Pre-existing immunodeficiency
• Significant renal impairment
• Pregnancy and lactation
• Pre-existing severe bone marrow suppression
• Severe hepatic impairment
• Active severe infections
• **Teratogenicity Warning**: Leflunomide is an FDA Category X teratogen. It must not be used in pregnant animals, and pregnant women should not handle this medication. **Prolonged Half-Life**: The active metabolite (A77 1726) can persist in the body for up to 2 years after discontinuation. If severe toxicity occurs, a washout procedure using cholestyramine or activated charcoal is required. Use with extreme caution in patients with hepatic disease, renal impairment, or pre-existing immunodeficiency.

薬物相互作用

• Charcoal, Activated: Can increase elimination and decrease A77 1726 drug concentrations; used for rapid washout.
• Cholestyramine: Can increase elimination and decrease A77 1726 drug concentrations; used for rapid washout.
• Hepatotoxic Agents: Increased risk for hepatotoxicity when used concurrently.
• Methotrexate: Increased risk of adverse effects and elevated ALT.
• Phenytoin: Leflunomide can increase phenytoin levels.
• Rifampin: Can increase A77 1726 peak levels.
• Vaccines, Live Virus: Should be used with extreme caution, if at all, due to immunosuppression.
• Warfarin: Leflunomide may increase INR.
• Other immunosuppressants (e.g., cyclosporine, azathioprine): Increased risk of severe immunosuppression and bone marrow toxicity
• Live vaccines: Risk of disseminated infection due to immunosuppression

よくある質問