What Is Leflunomide?
Leflunomide is a prescription pyrimidine synthesis inhibitor indicated for adults with active rheumatoid arthritis. Current tablets are available in 10 mg and 20 mg strengths.
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How Does Leflunomide Work?
Leflunomide is converted to the active metabolite teriflunomide. Teriflunomide inhibits dihydroorotate dehydrogenase, an enzyme involved in de novo pyrimidine synthesis, which reduces proliferation of activated lymphocytes and inflammatory activity.
Who Is Treated With Leflunomide?
Leflunomide is used in adults with active rheumatoid arthritis. Pregnancy and severe liver impairment are contraindications. Patients are screened for tuberculosis, liver abnormalities, blood-cell abnormalities, pregnancy, and elevated blood pressure before treatment.
How Is Leflunomide Dosed?
The recommended dose is 20 mg once daily. Patients at low risk for liver toxicity and bone marrow suppression can receive a loading regimen of 100 mg once daily for three days before 20 mg daily. Patients at higher risk start 20 mg once daily without a loading dose. A reduction to 10 mg once daily can be considered when 20 mg is not tolerated.
What Serious Risks Are Linked to Leflunomide?
Leflunomide carries boxed warnings for embryo-fetal toxicity and hepatotoxicity. Other serious concerns include bone marrow suppression, severe infections, Stevens-Johnson syndrome, toxic epidermal necrolysis, DRESS, peripheral neuropathy, interstitial lung disease, and increased blood pressure. An accelerated drug elimination procedure is used after selected severe reactions or pregnancy.
Frequently Asked Questions About Leflunomide
What condition does leflunomide treat?
Leflunomide treats active rheumatoid arthritis in adults.
What is the usual leflunomide dose?
The recommended maintenance dose is 20 mg once daily.
Does leflunomide use a loading dose?
Selected patients at low risk for liver toxicity and bone marrow suppression can receive 100 mg once daily for three days before the 20 mg daily regimen.
Does leflunomide have boxed warnings?
Yes. The boxed warnings concern embryo-fetal toxicity and hepatotoxicity.
References
DailyMed - LEFLUNOMIDE tablet. https://www.dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=40dd071a-d07f-452f-bf1a-2a23b9d22ca4. Date Accessed October 8, 2026.
Leflunomide. LiverTox. https://www.ncbi.nlm.nih.gov/books/NBK548725/. Date Accessed October 8, 2026.
Leflunomide. MedlinePlus. https://www.medlineplus.gov/druginfo/meds/a600032.html. Date Accessed October 8, 2026.
Leflunomide. PubChem. https://pubchem.ncbi.nlm.nih.gov/compound/Leflunomide. Date Accessed October 8, 2026.
Leflunomide. StatPearls. https://www.ncbi.nlm.nih.gov/books/NBK557799/. Date Accessed October 8, 2026.