Leflunomide
Anti-rheumatic, Systemic · Antimetabolite; DMARD (Disease modifying antirheumatic drugs)
Indications
Active rheumatoid arthritis.
Dosage
Adults: Loading Dose: 100 mg once daily for 3 days. Maintenance: 20 mg once daily. Max: 20 mg/day. If dose not tolerated or ALT elevations >2 but 3X ULN: Reduce dose to 10 mg/day. If elevations persist or ALT >3X ULN, discontinue. Children: Not recommended.
Adverse Effects
Increased BP, GI upset, oral mucosal disorders, abdominal pain, colitis, altered liver function, leucopenia, tenosynovitis, headache, dizziness, asthaenia, paraesthesia, weight loss, allergy, hair loss, dry skin. Rarely, severe hepatotoxicity sometimes fatal, Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, peripheral neuropathy, severe infection incl progressive multifocal leukoencephalopathy, pustular psoriasis or worsening of psoriasis.
Risk Factor (Pregnancy/Lactation)
Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Severe immunodeficiency, bone marrow dysfunction, blood dyscrasias, serious infections, hepatic impairment, moderate to severe renal insufficiency, severe hypoproteinaemia, ulcerative stomatitis. Contraception must be used by men and women during and for 2 years after use or until plasma levels fall below 0.02 mg/l. Precautions: Use under specialist supervision. Risk of hepatotoxicity; monitor ALT before treatment and every 2 weeks for 6 months, then every 8 weeks; withdraw and washout if elevated and continue to monitor liver enzymes until normal. Take complete differential blood counts before treatment and every 2 weeks for first 6 months, then every 8 weeks. A washout procedure must be performed if toxicity develops, or when switching to another DMARD or for a desired pregnancy.…
Interactions
Other DMARDs, alcohol, hepatotoxic, or haematotoxic drugs, methotrexate, drugs metabolised by CYP2C9 (not NSAIDs), live vaccines, cholestyramine, activated charcoal.
Advice to Patient
Take with or without meals. Report immediately if there is nausea, vomiting, stomach pain, unusual tiredness, dark urine, jaundice, swelling. Contact prescriber if there is acute headache, anxiety, depression, ulcers, difficulty in sleeping, skin rash, redness, acne, difficult or painful urination, chest pain, palpitations, fast heartbeat, constant GI upset, muscle cramps or tremors, weakness, back pain, change in gait, difficulty in breathing, cough, cold symptoms, wheezing, yellowing of skin or eyes, unusual bruising or bleeding, blood in vomitus/stool/urine. Take sufficient amount of fluids (2-3 litres per day) to maintain hydration, unless restricted by the prescriber. Avoid receiving live vaccines during therapy. Protect medication from light, store in a dark place. If you have diabetes, check blood glucose level regularly.
Pharmacokinetics
Metabolism: Hepatic; undergoes enterohepatic recirculation. Half-life elimination: Teriflunomide: Mean: 18 to 19 days. Time to peak: Teriflunomide: 6 to 12 hours. Excretion: Feces (37.5%); urine (22.6%).
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
Always consult a pharmacist or doctor.