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Leflunomide information from DrugsUpdate  

See Available Brands of Leflunomide in India

P - Contraindicated in pregnancy
L - Contraindicated in lactation

Leflunomide is a medication of the DMARD type, used in active moderate to severe rheumatoid arthritis and psoriatic arthritis. It is a pyrimidine synthesis inhibitor.

Pharmacodynamics

Pharmacokinetics

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 hours

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.

Leflunomide Indications / Leflunomide Uses

Information Not Available

Leflunomide Adverse Reactions / Leflunomide Side Effects

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.

Precautions

Warnings
Contraindicated in pregnancy. Pregnancy must be excluded prior to initiation of therapy. Ensure reliable use of contraception in women with childbearing potential during therapy. Patient must avoid pregnancy prior to completion of the drug elimination procedure after leflunomide treatment.

Special Precautions

Renal and hepatic impairment; women with childbearing potential. Monitor blood counts and BP regularly. Avoid alcohol.

Other 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.

Other Interactions

Information Not Available

Dosage

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.

Food(before/after)

May be taken with or without food.

List of Contraindications

Leflunomide and Pregnancy

Contraindicated in pregnancy

Category X: Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

Leflunomide and Lactation

Contraindicated in lactation

Leflunomide and Children

Not established

Leflunomide and Geriatic

No dosage adjustment is needed in patients older than 65 yr of age.

Leflunomide and Other Contraindications

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

Storage

Information Not Available

Lab interference

Information Not Available

Leflunomide brands in India:

Arava Avara. Cleft Lefno Lefra Lefuma Lefumide Lisifen Rumalef

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