Leflunomide


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Rheumatoid arthritis; Psoriatic arthritis Loading dose: 100 mg once daily for 3 days. Maintenance: 10-20 mg once daily.
Dosage Details
Oral
Rheumatoid arthritis, Psoriatic arthritis
Adult: Loading dose: 100 mg once daily for 3 days. Maintenance: 10-20 mg once daily.
Renal Impairment
Mild: No dosage adjustment needed. Moderate to Severe: Contraindicated.
Hepatic Impairment
Contraindicated.
Administration
May be taken with or without food.
Contraindications
Hepatic impairment, moderate and severe renal impairment, compromised immune function including bone marrow dysplasia or severe uncontrolled infection, severe hypoproteinaemia; concurrent vaccination w/ live vaccines. Pregnancy and lactation.
Special Precautions
Mild renal impairment. Patient w/ history of TB due to the possibility of reactivation of the infection.
Adverse Reactions
HTN, diarrhoea, upper respiratory tract infections, thrombocytopenia, leukopenia, pancytopenia, agranulocytosis, headache, alopecia, dry skin, eczema, erythema multiforme, hypokalaemia, weight loss, asthenia, anxiety, paraesthesia, synovitis, joint disorder, peripheral neuropathy, mild hyperlipidaemia, interstitial lung disease, vasculitis.
Potentially Fatal: Hepatotoxicity, sepsis, Stevens-Johnson syndrome, toxic epidermal necrolysis, pancreatitis.
MonitoringParameters
Monitor BP and liver enzyme values prior to initiation and periodically during therapy.
Overdosage
Symptoms: Abdominal pain, nausea, diarrhoea, elevated liver enzymes, anaemia, leucopenia, pruritus and rash. Management: Administer cholestyramine or charcoal to hasten elimination of the drug. Supportive and symptomatic treatment should also be initiated and observed patient closely.
Drug 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.
Food Interaction
Avoid alcohol due to increased risk of hepatotoxicity. Echinacea may reduce the therapeutic effect of leflunomide.
Action
Description: Leflunomide is an immunomodulating agent and DMARD. It inhibits pyrimidine synthesis by inhibiting dihydroorotate dehydrogenase enzyme activity resulting in antiproliferative and anti-inflammatory effects.
Pharmacokinetics:
Absorption: Bioavailability: Approx 82-95%. Time to peak plasma concentration (active metabolite): 6-12 hr.
Distribution: Volume of distribution: 0.13 L/kg. Plasma protein binding (active metabolite): 99% (mainly albumin).
Metabolism: Rapidly converted to active metabolite A77 1726 in GI mucosa and the liver.
Excretion: Via urine (approx 43% as glucuronides) and faeces (approx 48%). Elimination half-life (active metabolite): Approx 14-18 days.
Storage
Store at 25°C.
Disclaimer: This information is independently developed by MIMS based on Leflunomide from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
  • Arava
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in