Leflunomide(leh flew’ no mide)
Arava
PREGNANCY CATEGORY X
Drug Classes
Antiarthritic
Pyrimidine synthesis inhibitor
Therapeutic Actions
Reversibly inhibits the enzyme dihydroorotate dehydrogenase, which is active in the autoimmune process that leads to rheumatoid arthritis; blocking this enzyme relieves the signs and symptoms of inflammation and blocks the structural damage caused by the inflammatory response to the autoimmune process.
Indications
Treatment of active rheumatoid arthritis; to relieve symptoms and slow progression
Improvement in physical functioning in adults with active rheumatoid arthritis
Contraindications and Cautions
Contraindicated with allergy to leflunomide, lactation, pregnancy, childbearing age when not using a reliable method of contraception, significant hepatic impairment, hepatitis B or C, severe immune deficiency.
Use cautiously with renal or hepatic disorders.
Available Forms
Tablets—10, 20, 100 mg
Dosages
Adults
Loading dose, 100 mg PO daily for 3 days; maintenance dose, 20 mg PO daily. If not well tolerated or if ALT elevates to more than two times upper level of normal, may reduce to 10 mg PO daily. If elevation of ALT is between two and three times upper limit of normal, monitor closely if continued therapy is desired; if it is three times or greater than upper limit of normal, use of cholestyramine may decrease absorption; consider discontinuation.
Pediatric patients
Safety and efficacy not established.
Patients with hepatic impairment
Do not use with serious hepatic impairment. Decrease dosage and monitor patient closely with mild to moderate hepatic impairment.
