leflunomide | Elafra tablets are covered.pl.ob. 20 mg 30 pcs.

Release form

Tablets, film-coated

Packing

30 pcs.

Pharmacological action

Elafra is a basic antirheumatic drug that modifies the course of the disease, with antiproliferative effect. The active metabolite of leflunomide - A771726 - inhibits the enzyme dihydroorotate dehydrogenase and has antiproliferative activity. A771726 in vitro inhibits mitogen-induced proliferation and DNA synthesis of T-lymphocytes. The antiproliferative activity of A771726 appears, apparently, at the level of pyrimidine biosynthesis, since the addition of uridine to the cell culture eliminates the inhibitory effect of metabolite A771726.

Using radioisotope ligands, A771726 was shown to selectively bind to the enzyme dehydroorotate dehydrogenase, which explains its ability to inhibit this enzyme and lymphocyte proliferation in stage G1. At the same time, A771726 inhibits the expression of interleukin-2 receptors and Ki-67 and PCNA core antigens associated with the cell cycle. The therapeutic effects of leflunomide have been shown in several experimental models of autoimmune diseases, including rheumatoid arthritis.

Indications

Active form of rheumatoid arthritis.

Contraindications

Hypersensitivity, impaired liver function, severe immunodeficiency, significant disorders of bone marrow hematopoiesis or anemia, leukopenia or thrombocytopenia, severe uncontrolled infections, renal failure, hypoproteinemia, 18 years of age, pregnancy.

Special instructions

The drug can be prescribed to patients only after a thorough medical examination. It is recommended to refrain from drinking alcohol. A complete clinical blood test should be performed before treatment, as well as every 2 weeks during the first 6 months of treatment and every 8 weeks after completion of treatment. In the case of the development of hematological reactions, including pancytopenia, it is necessary to stop taking the drug and any other concomitant drug that suppresses bone marrow hematopoiesis, and begin the washing procedure. Switching to taking another basic drug without a washing procedure can increase the possibility of an additional risk even after a long time after the transition. In the case of ulcerative stomatitis, stop taking leflunomide. In case of skin and / or mucous reactions, it is necessary to stop treatment with the drug and start the washing procedure. Patients with tuberculin reactivity should be monitored because of the risk of reactivation of tuberculosis. Before starting treatment with leflunomide and periodically after it began, the level of blood pressure should be monitored. It is not recommended to take cholestyramine or activated carbon during treatment. The drug should not be prescribed to pregnant women or women of childbearing age who do not use reliable contraception in the treatment of leflunomide and for some time after this treatment. Washing procedure: after stopping treatment with leflunomide: Cholestyramine 8 g is administered 3 times a day for 11 days. Alternatively, 50 g of powdered activated carbon is administered 4 times a day for 11 days. Regardless of the rinsing procedure chosen, it is necessary to carry out a test with two separate tests with an interval of at least at 14 days and wait 1.5 months from the moment when the concentration of the drug in the plasma for the first time is fixed below 0.02 mg / l, until fertilization. Women of childbearing age should remember that 2 years must pass after the treatment with leflunomide is discontinued before they can become pregnant. Cholestyramine and activated carbon can affect the absorption of estrogen and progesterone in such a way that oral contraceptives do not give a 100% guarantee. Alternative contraceptive methods are recommended.

Composition

1 tab. contains leflunomide 20 mg

Dosage and administration of

Leflunamide treatment begins with a single dose of 100 mg for 3 days. As a maintenance dose, it is recommended to take from 10 mg to 20 mg of leflunomide once a day. The therapeutic effect usually manifests itself after 4-6 weeks and can increase up to 4-6 months. No dosage adjustment is required for patients over 65 years of age. The tablets must be swallowed whole with a sufficient amount of liquid.

Side effects

The most common side effects (1-10%): leukopenia allergic reactions loss of appetite, weight loss (usually slight) fatigue (weakness), headache, dizziness, paresthesia moderate increase in blood pressure, diarrhea, nausea, vomiting, erosive and ulcerative lesions of the oral mucosa, abdominal pain, increased liver function, increased hair loss, eczema, dry skin, rash, itching, tendovaginitis, an increase in certain enzymes in the blood (creatine phosphokinase).

Atypical side effects (0.1-1%): decrease in the number of red blood cells, thrombocytopenia, decrease in potassium levels in the blood, anxiety, taste disturbance, urticaria, increase in blood fats (cholesterol and triglycerides), decrease in blood phosphates.

Rare side effects (0.01-0.1%): eosinophilia, leukopenia, pancytopenia, a sharp increase in blood pressure impaired liver function in the form of hepatitis, cholestasis, jaundice sepsis (possibly fatal).

Very rare side effects (0.001% or less): agranulocytosis, severe allergic reactions, Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, vasculitis, peripheral neuropathy, pancreatitis.

Drug Interactions

There is no information on the combined use of leflunomide with antimalarial drugs used in rheumatology, administered intramuscularly or orally with gold preparations, D-penicillamine, azathioprine and other immunosuppressive drugs (with the exception of methotrexate). The risk associated with the appointment of complex therapy is not known, especially with prolonged treatment. The increase in side effects may be in the case of recent or concomitant use of hepatotoxic or hematotoxic drugs.

Overdose

In case of overdose or toxicity, it is recommended to take cholestyramine or activated charcoal.

Storage conditions

The product should be stored out of reach of children, in a dry, dark place at a temperature not exceeding 25 РC.

Dosage form

tablet

K.O. Rompharm Company S.R.L., Romania