Leflunomide
ARAVA
What it isDihydroorotate dehydrogenase inhibitor blocking pyrimidine synthesis; rheumatoid arthritis.
Why this oneEfficacy comparable to methotrexate, so it is the main alternative when methotrexate is not tolerated.
What limits itHepatotoxicity and teratogenicity, with a half-life of weeks — cholestyramine washout is needed before conception. Monitor counts and liver function.
FDA-approved for
- rheumatoid arthritis (1998)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Rheumatoid arthritis | Adults | 100 mg QD ×3 days loading (low-risk), then 20 mg QD | 20 mg QD | 20 mg QD |
Renal Undefined
Hepatic Contraindicated in severe hepatic impairment; avoid with pre-existing liver disease or ALT >2×ULN
Instructions
- May reduce to 10 mg QD if 20 mg not tolerated
- Screen for active/latent TB, pregnancy, blood pressure, and labs before starting
- Monitor ALT
- After stopping, use accelerated drug elimination procedure to lower teriflunomide
Contraindications
- Pregnancy
- Severe hepatic impairment
- Current teriflunomide treatment
Cautions
- Hepatotoxicity
- Embryo-fetal toxicity
- Severe infections/sepsis; pancytopenia, agranulocytosis, thrombocytopenia
- SJS/TEN and DRESS
- Skin ulcers
- Peripheral neuropathy
- Interstitial lung disease (may be fatal)
- Increased blood pressure
Adverse reactions
- Diarrhea
- Respiratory infection
- Nausea
- Headache
- Rash
- Abnormal liver enzymes
- Dyspepsia
Pregnancy Contraindicated — potential fetal harm; teratogenic/embryolethal in animals
Lactation Advise not to breastfeed during treatment
⚠ BOXED WARNINGS
- Hepatotoxicity
- Embryo-fetal toxicity
Cost, est. cash$100–$5,000/month
Generic entry2005
Classes and tags
Clinical profile
Legacy pregnancy categoryX
Defining liabilitySerious infection, cytopenias, hepatic injury and malignancy risk require laboratory and clinical monitoring.
Mechanism of action: Leflunomide ballicule
