Leflunomide

Indications

Leflunomide is used for: Rheumatoid arthritis, Psoriatic arthritis

Adult Dose

Oral Rheumatoid arthritis; Psoriatic arthritis Adult: Loading dose: 100 mg once daily for 3 days. Maintenance: 10-20 mg once daily. Hepatic impairment: Contraindicated.

Child Dose

Safety and efficacy not established

Renal Dose

Renal impairment: Mild: No dosage adjustment needed. Moderate to Severe: Contraindicated.

Administration

May be taken with or without food.

Contra Indications

Significant hepatic impairment, compromised immune function including bone marrow dysplasia or severe uncontrolled infection; concurrent vaccination with live vaccines. Pregnancy, lactation.

Precautions

Renal and hepatic impairment; Women with childbearing potential. Caution should be taken for those female with child bearing potential who are not using reliable contraception and for the subject of renal insufficiency. Leflunomide should be stopped before becoming pregnant. Liver function should be monitored before starting treatment. Monitor blood counts and BP regularly. Avoid alcohol. Lactation: not known if excreted in breast milk

Pregnancy-Lactation

Pregnancy Category: X Lactation: not known if excreted in breast milk

Interactions

Cholestyramine and activated charcoal may decrease plasma concentration of active metabolite. Concurrent use of methotrexate and other hepatotoxic drugs may increase the risk of hepatotoxicity. Rifampicin increases serum levels of the active metabolite. Potentially Fatal: May enhance the adverse effects of live vaccines.

Adverse Effects

Side effects of Leflunomide : >10% Diarrhea (17%), Respiratory infections (15%) 1-10% (selected) Alopecia (10%), Hypertension (10%), Rash (10%), Nausea (9%), Bronchitis (7%), Headache (7%), Abdominal pain (5%), Abnormal LFT's (5%), Accidental injury (5%), Back pain (5%), Dyspepsia (5%), UTI (5%), Dizziness (4%), Infection (4%), Joint disorder (4%), Pruritus (4%), Weight loss (4%), Anorexia (3%), Cough (3%), Gastroenteritis (3%), Pharyngitis (3%), Stomatitis (3%), Tenosynovitis (3%), Vomiting (3%), Weakness (3%), Allergic reaction (2%), Chest pain (2%), Dry skin (2%), Eczema (2%), Pain (2%), Paresthesia (2%), Pneumonia (2%), Rhinitis (2%), Sinusitis (2%), Synovitis (2%) Potentially Fatal: Hepatotoxicity.

Mechanism of Action

Leflunomide is an immunomodulating agent and DMARD. It inhibits pyrimidine synthesis by inhibiting dihydroorotate dehydrogenase enzyme activity resulting in antiproliferative and anti-inflammatory effects.