Clinical Information
Gen. Code and Des.
40549 leflunomide ORAL TABLET 10 MG
GCN and Des.
67031 leflunomide ORAL TABLET 10 MG
Strength
10MG
Dose Form
TABLET
Product Category
RX Pharmaceuticals
Fine Line Class
850085008510 All Rx Products
DEA Class
NC
OMP Family
AHFS Class
92360000 DISEASE-MODIFYING ANTIRHEUMATIC AGENTS
92200000 IMMUNOMODULATORY AGENTS
Active Ingredients
7642 leflunomide 75706126
Inactive Ingredients
2432 lactose 64044515
2537 povidone 9003398
These highlights do not include all the information needed to use ARAVA safely and effectively. See full prescribing information for ARAVA.
ARAVA (leflunomide), tablets, for oral use
Initial U.S. Approval: 1998
WARNING: EMBRYO-FETAL TOXICITY and HEPATOTOXICITY
See full prescribing information for complete boxed warning.
Embryo-Fetal Toxicity
Teratogenicity and embryo-lethality occurred in animals administered leflunomide. ( 5.1, 8.1)
Exclude pregnancy prior to initiating ARAVA therapy. ( 5.1, 8.3)
Advise use of effective contraception in females of reproductive potential during treatment and during a drug elimination procedure. ( 5.1, 5.3, 8.3)
Stop ARAVA and use an accelerated drug elimination procedure if the patient becomes pregnant. ( 5.1, 5.3, 8.1)
Hepatotoxicity
Severe liver injury and fatal liver failure have been reported. ( 5.2)
Avoid ARAVA use in patients with pre-existing liver disease, or those with serum alanine aminotransferase (ALT) >2 �- ULN. ( 5.2, 8.6)
Use caution when ARAVA is given with other potentially hepatotoxic drugs. ( 5.2)
Monitor ALT levels. Interrupt ARAVA treatment if ALT elevation >3-fold ULN. If likely leflunomide-induced, start accelerated drug elimination procedure and monitor liver tests weekly until normalized. ( 5.2, 5.3)
INDICATIONS AND USAGE
ARAVA is a pyrimidine synthesis inhibitor indicated for the treatment of adults with active rheumatoid arthritis. ( 1)
DOSAGE AND ADMINISTRATION
Loading dosage for patients at low risk for ARAVA-associated hepatotoxicity and ARAVA-associated myelosuppression: 100 mg daily for 3 days. ( 2.1)
Maintenance dosage: 20 mg daily. ( 2.1)
Maximum recommended daily dosage: 20 mg once daily. ( 2.1)
If 20 mg once daily is not tolerated, may decrease dosage to 10 mg once daily. ( 2.1)
Screen patients for active and latent tuberculosis, pregnancy test (females), blood pressure, and laboratory tests before starting ARAVA. ( 2.2)
DOSAGE FORMS AND STRENGTHS
Tablets: 10 mg, 20 mg, 100 mg. ( 3)
CONTRAINDICATIONS
Pregnancy. ( 4, 5.1, 8.1)
Severe hepatic impairment. ( 4, 5.2)
Hypersensitivity to ARAVA or any of its inactive components. ( 4)
Current teriflunomide treatment. ( 4)
WARNINGS AND PRECAUTIONS
After stopping ARAVA, it is recommended that an accelerated drug elimination procedure be used to reduce the plasma concentrations of the active metabolite, teriflunomide. ( 5.3)
Severe infections (including sepsis), pancytopenia, agranulocytosis, and thrombocytopenia: Stop ARAVA and use accelerated elimination procedure. Do not start ARAVA in patients with active infection. Monitor CBCs during treatment with ARAVA. ( 5.4)
Stevens-Johnson syndrome and toxic epidermal necrolysis, Drug reaction with eosinophilia and systemic symptoms (DRESS): Stop ARAVA and use accelerated elimination procedure. ( 5.5)
Peripheral neuropathy: If patient develops symptoms consistent with peripheral neuropathy, evaluate patient and consider discontinuing ARAVA. ( 5.7)
Interstitial lung disease: May be fatal. New onset or worsening symptoms may necessitate discontinuation of ARAVA and initiation of accelerated elimination procedure. ( 5.8)
Increased blood pressure: Monitor and treat. ( 5.10)
ADVERSE REACTIONS
The most commonly reported adverse reactions (≥10%) regardless of relation to ARAVA treatment were diarrhea, respiratory infection, nausea, headache, rash, abnormal liver enzymes, and dyspepsia. ( 6.1)
To report SUSPECTED ADVERSE REACTIONS, contact sanofi-aventis U.S. LLC at 1-800-633-1610 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
DRUG INTERACTIONS
Drugs metabolized by CYP2C8 and OAT3 transporters: Monitor patients because teriflunomide may increase exposure of these drugs. ( 7)
Teriflunomide may increase exposure of ethinylestradiol and levonorgestrel. Choose an appropriate oral contraceptive. ( 7)
Drugs metabolized by CYP1A2: Monitor patients because teriflunomide may decrease exposure of these drugs. ( 7)
Warfarin: Monitor INR as teriflunomide may decrease INR. ( 7)
Drugs metabolized by BCRP and OATP1B1/B3 transporters: Monitor patients because teriflunomide may increase exposure of these drugs. ( 7)
Rosuvastatin: The dose of rosuvastatin should not exceed 10 mg once daily in patients taking ARAVA. ( 7)
USE IN SPECIFIC POPULATIONS
Lactation: Discontinue breastfeeding. ( 8.2)
Safety and effectiveness in pediatric patients <12 years of age have not been established. ( 8.4)
See 17 for PATIENT COUNSELING INFORMATION.
Revised: 12/2021
