Generic Name and Formulations:
Leflunomide 10mg, 20mg, 100mg; tabs.
Indications for ARAVA:
Active rheumatoid arthritis.
Arava-associated hepatotoxicity and myelosuppression (low-risk): give loading dose of 100mg once daily for 3 days; then 20mg daily thereafter; (high-risk): give 20mg once daily without loading dose. Max 20mg/day. If not well tolerated, consider reducing to 10mg daily; monitor closely. Perform accelerated drug elimination procedure with cholestyramine and/or activated charcoal after stopping therapy.
Severe hepatic impairment. Concomitant teriflunomide. Pregnancy.
Pre-existing hepatic disease or ALT>2xULN: not recommended. Monitor liver function (esp. ALT) and blood (WBCs, platelets, hemoglobin, HCT) at baseline, then monthly for 1st six months; then every 6–8 weeks. If ALT elevations >3xULN, interrupt and evaluate; if likely leflunomide-induced, perform accelerated drug elimination procedure and monitor LFTs weekly until normalized; if unlikely, may consider resuming therapy. Obtain (–) pregnancy test before starting therapy. Females of reproductive potential should use effective contraception during treatment and during an accelerated drug elimination procedure after stopping treatment (see full labeling). Test and treat, if positive for active or latent TB infection prior to starting therapy. Renal impairment. Monitor BP. Severe immunodeficiency, bone marrow dysplasia, severe uncontrolled infections, nursing mothers: not recommended.
DMARD (pyrimidine synthesis inhibitor).
See Contraindications. Concomitant methotrexate, other immunosuppressants: monitor for hepatic or hematologic toxicity monthly. Caution with rifampin, and with other hepatotoxic drugs. May potentiate CYP2C8 (eg, paclitaxel, pioglitazone, repaglinide) or OAT3 (eg, cefaclor, cimetidine, ciprofloxacin) substrates, oral contraceptives; monitor and adjust dose as needed. May antagonize CYP1A2 (eg, alosetron, duloxetine, theophylline) substrates; monitor and adjust dose as needed. Consider reducing dose of OATP or BCRP substrates, esp. statins (limit rosuvastatin dose to 10mg/day). Concomitant live vaccines: not recommended; consider leflunomide long half-life before vaccination after stopping therapy. Monitor warfarin.
Diarrhea, elevated liver enzymes, alopecia, rash, respiratory infection, hypertension, headache, GI upset; rare: hepatotoxicity (may be fatal), interstitial lung disease, immunosuppression (possible sepsis), bone marrow suppression, Stevens-Johnson syndrome, toxic epidermal necrolysis, DRESS, peripheral neuropathy: stop therapy and perform drug elimination procedure.
Tabs 10mg, 20mg—30; 100mg—blister pack (1 x 3)
Clinical Pain Advisor Articles
- Radiofrequency Denervation Efficacious in Treating Thoracic Zygapophyseal Joint Pain
- Prescribed Opioids Difficulties Scale Effective for Assessing Concerns of Patients With Chronic Pain
- Predictors of Opioid Overdose in High-Risk Users
- Optimal Strategies for Opioid Weaning After Ambulatory Surgery
- Emergency Physicians Offer Recommendations for Identifying and Managing Opioid Use Disorder
- Consensus Guidelines for the Use of Intravenous Ketamine for Chronic Pain
- Pain Societies Issue Guidelines on Use of Ketamine for the Management of Acute Pain
- Labor Epidural Analgesia Linked to Reduced Likelihood of Successful Breastfeeding
- Novel Oral Treatment Safe, Effective for Migraine Headache Relief
- DFN-02 Nasal Spray Safe, Effective for Acute Treatment of Episodic Migraine
- Higher PainDETECT Scores, Neuropathic Pain Preoperatively May Increase Risk for Chronic Pain Post-TKR
- Terms Used for Addiction May Be Associated With Explicit, Implicit Bias
- Erenumab Reduces Monthly Migraine Days in Patients With Treatment-Resistant Migraine
- Government and Industry Lead the Way in Funding USPSTF Systematic Reviews
- Communication-Based Intervention Increases Goals-of-Care Discussions Between Physicians, Patients With Serious Illness