Form of production, composition and packing
White or almost white film-coated, round, biconvex tablets.
leflunomide 10 mg
Lactose monohydrate 80.0 mg, low-substituted hyprolose 5.0 mg, tartaric acid 3.0 mg, sodium lauryl sulfate 0.5 mg, magnesium stearate 1.5 mg.
Contents of the film coating: polyvinyl alcohol – 1.3656 mg, titanium dioxide – 0.9600 mg, talc – 0.6000 mg, lecithin – 0.0600 mg, xanthan gum – 0.0144 mg. hat is Ehlafra? Ehlafra affects the immune system and reduces swelling and inflammation in the body. Ehlafra is used to treat the symptoms of rheumatoid arthritis. Ehlafra also helps reduce joint damage and improves physical functioning. Ehlafra may also be used for other purposes not listed in this medication guide. Ehlafra indications
30 pcs. – Polyethylene vials (1) – cardboard boxes.
Filmed film-coated white or almost white, round, biconvex, with a one-sided ridge.
leflunomide 20 mg
PRING] lactose monohydrate – 160.0 mg, low-substituted hyprolose – 10.0 mg, tartaric acid – 6.0 mg, sodium lauryl sulfate – 1.0 mg, magnesium stearate – 3.0 mg.
Contents of the coating: polyvinyl alcohol – 2.7312 mg, titanium dioxide – 1.9200 mg, talc – 1.2000 mg, lecithin – 0.1200 mg, xanthan gum – 0.0288 mg.
30 pcs. – PE vials (1) – cardboard boxes.
Elafra is a basic antirheumatic drug that modifies the course of the disease, with antiproliferative action. Active metabolite of leflunomide – A771726 – inhibits dihydrorotate dehydrogenase enzyme and has antiproliferative activity. In vitro A771726 inhibits mitogen-induced proliferation and DNA synthesis of T-lymphocytes. The antiproliferative activity of A771726 appears to be manifested at the level of pyrimidine biosynthesis, since the addition of uridine to the cell culture eliminates the inhibitory effect of the metabolite A771726. Using radioisotope ligands, it was shown that A771726 selectively binds to the enzyme dihydrorotate dehydrogenase, which explains its ability to inhibit this enzyme and lymphocyte proliferation at the G1 stage. At the same time A771726 inhibits the expression of receptors to interleukin-2 and Ki-67 and PCNA cell-cycle-related antigens.
The therapeutic effect of leflunomide has been shown in several experimental models of autoimmune diseases, including rheumatoid arthritis.
Absorption and distribution
Absorption of the drug is 82-95% and is not dependent on food intake. The period to reach a stable plasma concentration of the drug is approximately 2 months of daily dosing, provided that a loading dose is not used at the beginning of treatment. Because of the long T1/2 of A771726, a loading dose of 100 mg for 3 days was used. This allowed rapid equilibrium plasma concentrations of A771726 to be achieved.
The pharmacokinetic parameters of A771726 have a linear relationship when administered at doses ranging from 5 mg to 25 mg. In these studies, the clinical effect is closely related to the plasma concentration of A771726 and the daily dose of leflunomide. When administered at a dose of 20 mg/day, the average plasma concentrations of A771726 at equilibrium were 35 µg/ml. Plasma concentrations of the drug increased by a factor of 33-35 when administered multiple times compared to single administration.
In plasma A771726 is rapidly bound to albumin. The unbound fraction of A771726 is 0.62%. A771726 binding is more variable and is slightly reduced in patients with rheumatoid arthritis or chronic renal impairment.
Metabolism and excretion
Leflunomide is rapidly metabolized in the intestinal wall and liver to one major (A771726) metabolite and several minor metabolites, including 4-trifluoromethylalanine. The biotransformation of leflunomide to A771726 and the subsequent metabolism of A771726 itself is controlled by several enzymes and occurs in microsomal and other cellular fractions.
Trace amounts of leflunomide are detected in plasma, urine, and feces. The excretion of A771726 is slow and characterized by a clearance of 31 ml/h. T1/2 is about 2 weeks.
Tablets are taken orally, swallowed whole and washed down with enough liquid. Food intake has no effect on absorption of leflunomide.
Treatment with leflunomide should be started under the supervision of a doctor experienced in the treatment of rheumatoid arthritis. Treatment with leflunomide begins with a shock dose of 100 mg for 3 days.
The maintenance dose in rheumatoid arthritis is 10-20 mg once daily.
The therapeutic effect usually appears after 4-6 weeks and may increase further up to 4-6 months.
There are no recommendations regarding the dosage of the drug in patients with mild renal insufficiency.
No dose adjustment is required in patients over 65 years of age.
- hepatic insufficiency;
- Severe immunodeficiencies (including AIDS);
- severe bone marrow dysfunction or anemia, leukopenia, neutropenia, thrombocytopenia due to other causes (except rheumatoid arthritis);
- severe infections;
- moderate or severe renal failure;
- severe hypoproteinemia (including in nephrotic syndrome);
- pregnancy (pregnancy should be excluded before starting treatment with leflunomide);
- Children and adolescents under 18 years of age;
- Hypersensitivity to the components of the drug.
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