Leflunomide

Indications
 Oral
Rheumatoid arthritis, Psoriatic arthritis
Adult: 100 mg daily for 3 days as a loading dose. Maintenance: 10-20 mg daily.
Renal impairment: Dosage may need to be reduced.
Hepatic impairment: Dosage may need to be reduced.
Contraindications
 Significant hepatic impairment, compromised immune function including bone marrow dysplasia or severe uncontrolled infection; concurrent vaccination with live vaccines. Pregnancy, lactation.
Warnings / Precautions
 Renal and hepatic impairment; women with childbearing potential. Monitor blood counts and BP regularly. Avoid alcohol.
Adverse Reactions
 Thrombocytopenia, anaphylaxis, eosinophilia, leukopenia, pancytopenia. Headache, dizziness, weakness, bronchitis, urinary tract infection, alopecia, rash, dry skin, eczema, pruritus, hypokalaemia, weight loss, arthralgia, joint disorder, leg cramps, rhinitis, sinusitis, hypertension, diarrhoea, nausea, abdominal pain, synovitis, tenosynovitis, paraesthesia, pharyngitis, anorexia, vomiting, oral thrush, stomatitis.
Potentially Fatal: Hepatotoxicity.
Drug Interactions
 Cholestyramine and activated charcoal decrease active metabolite. Concurrent use of methotrexate and other hepatotoxic drugs increase the risk of hepatotoxicity. Rifampicin increases blood levels of the active metabolite.
See Below for More leflunomide Drug Interactions
Mechanism of Actions
 Leflunomide is an immodulating agent and DMARD. It inhibits pyrimidine synthesis by inhibiting dihydroorotate dehydrogenase enzyme activity. It also has antinflammatory properties.
Absorption: Peak plasma concentrations of active metabolite within 6-12 hr.
Distribution: Active metabolite is 99% protein bound and has a low volume of distribution (0.13 L/kg).
Metabolism: Rapidly converted to active metabolite A77 1726 in GI mucosa and the liver.
Excretion: Urine (as glucuronides), faeces. Elimination half life of active metabolite approximately 14-18 days.
Administration
 May be taken with or without food.
ATC Classification
 L04AA13 - leflunomide ; Belongs to the class of selective immunosuppressive agents. Used to induce immunosuppression.
Available As
  • Leflunomide 10 mg
  • Leflunomide 20 mg

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