Leflunomidum
Description
A drug that modifies the course of the rheumatic process
(the effect usually appears after 4-6 weeks
of treatment). Inhibits dihydroorotate dehydrogenase,
proliferation, and inflammation.
Indications
Active rheumatoid arthritis; active psoriatic
arthritis.
Contraindications
Increased sensitivity to the active substance or to any excipient;
severe immunodeficiency; significantly
impaired bone marrow function; severe infectious
diseases; moderate to severe hepatic impairment; severe
hypoproteinemia; pregnancy; breastfeeding; in fertile
women not using reliable contraception.
Dosage
For adults. Oral administration. Rheumatoid arthritis:
first 3 days – 100 mg once
daily, then – 10-20 mg once daily. Psoriatic
arthritis: first 3 days – 100 mg once
daily, then – 20 mg once daily.
For elderly patients. No dose adjustment is necessary.
For hepatic impairment. No dose adjustment is necessary.
Adverse reactions
Most common: increased blood pressure; diarrhea,
nausea, vomiting, anorexia, oral
mucosal changes (e.g., aphthous stomatitis, mouth
ulcers), abdominal pain, increased blood creatinine concentration;
elevated liver function tests;
weight loss; headache, dizziness, asthenia, paresthesia; tenosynovitis; increased hair loss, eczema, skin dryness;
vague allergic reactions, rash, itching;
leukopenia.
Others: hepatitis, jaundice, cholestasis, liver necrosis,
hepatic failure (life-threatening due to liver damage, especially during the first 6 months of treatment);
hypokalemia; taste disturbance, anxiety;
tendon rupture; Stevens-Johnson syndrome,
toxic epidermal necrolysis, erythema multiforme;
urticaria, anaphylactic or anaphylactoid reactions;
anemia, mild thrombocytopenia, eosinophilia,
pancytopenia, agranulocytosis.
Pregnancy
Teratogenic effects have been observed in animals. Not to be used.
Breastfeeding
Enters animal milk. No data on use
during breastfeeding. Do not breastfeed.
Warnings
Use with caution in case of impaired bone marrow function
(anemia, leukopenia, or thrombocytopenia;
if these disorders are severe or not related to rheumatoid
arthritis – do not administer), recent use of other drugs
toxic to the liver or bone marrow that modify the course of the rheumatic
process (do not administer together),
as well as in patients with tuberculosis. Monitor CBC. Before prescribing this
medication, every 2 weeks for the first 6 months of treatment
and then every 8 weeks, monitor all blood cell counts,
including a leukogram. Before prescribing the drug to a woman,
ensure she is not pregnant. Women must use
contraception while taking leflunomide and then
for at least 2 years, for men – while taking it and then for at least 3
months. Before prescribing this drug, every month for the first
6 months of treatment and then every 2 months,
monitor liver function, and if it is impaired, discontinue
the drug or reduce its dose (if reducing the dose
does not normalize liver function, discontinue it and perform
its elimination procedure). Drug elimination procedure
(to accelerate drug elimination in case of severe adverse reactions,
before switching leflunomide to another drug modifying the course of the rheumatic
process or if a woman decides
to become pregnant): after discontinuing leflunomide, administer 8 g
of cholestyramine three times a day or 50 g of activated
charcoal four times a day (for 11 days). After
this procedure, the concentration of the active metabolite
in plasma should be less than 20 mg/l (measured
twice with a 14-day interval).
Source | Drug Guide | Lithuanian University of Health Sciences | Institute of Physiology and Pharmacology | Doctor of Medical Sciences Rimas Jankūnas, Doctor of Medical Sciences Arvydas Milašius | Clinic of Internal Diseases | Doctor of Medical Sciences Palmira Leišytė