Description
Leflunomide Pharmacodynamics
A drug with antiproliferative, immunomodulatory (immunosuppressive) and anti-inflammatory effects. The active metabolite of leflunomide A771726 inhibits the enzyme dehydrorotate dehydrogenase and has an antiproliferative effect. In vitro A771726 inhibits mitogen-induced proliferation and DNA synthesis of T-lymphocytes.
The therapeutic effect of leflunomide has been shown in several experimental models of autoimmune diseases, including rheumatoid arthritis.
Indications
Basal therapy of rheumatoid arthritis in order to reduce the symptoms of the disease and delay the development of structural joint damage.
Contraindications
Liver function abnormalities, severe immunodeficiency states (including AIDS); expressed disorders of medullary hematopoiesis or anemia, leukopenia, thrombocytopenia due to other causes (except rheumatoid arthritis), severe infections, moderate or severe renal failure (due to little experience in clinical observation), severe hypoproteinemia (including nephrotic syndrome). including in nephrotic syndrome), pregnancy, lactation, children and adolescents under 18 years of age, hypersensitivity to leflunomide.
Dosage and administration regimen
- The initial dose is 100 mg daily for 3 days. Maintenance dose – 10-20 mg once a day.
- Therapeutic effect appears 4-6 weeks after the start of treatment and may increase within 4-6 months.