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
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.