Leflunomide tabs 20mg #30

Leflunomide user manual

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Composition

The preparation includes the following substances: leflunomide, giprolose, calcium hydrogen phosphate dihydrate, corn starch, croscarmellose sodium, magnesium stearate, microcrystalline cellulose, seleoate, macrogol, titanium dioxide.

Form of issue

Tablets biconvex round in a film wrapper in a blister for 10, 20 and 100 mg in a carton No. 30.

pharmachologic effect

Immunodepressive, antirheumatic, anti-inflammatory, antiproliferative.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

A drug with immunomodulatory, antiproliferative, anti-inflammatory and antiproliferative effect. It inhibits the proliferation and formation of T-lymphocyte DNA. The active metabolite of the drug (A77172), destroys the enzyme dehydroorotate dehydrogenase.

Pharmacokinetics

Absorption of the drug after ingestion is about 90%, while the absorption of leflunomide food intake is not affected.
The drug is rapidly metabolized in the liver and intestinal wall to the main metabolite (A771726) and several secondary ones. Cmax of the main metabolite after a single dose is achieved within a day. In the blood it binds to albumin. The unbound fraction is only 0.62%. The excretion of the main metabolite is slow, the half-life is about 2 weeks.

Indications for use

    as the main therapeutic agent in the therapy of rheumatoid arthritis in active form for relief of the symptoms of the disease and delay of the process of structural damage to the joints;
    psoriatic arthritis in active form.

Contraindications

Immunodeficiency conditions, liver disease, severe anemia or severe disorders of bone marrow hematopoiesis, thrombocytopenia, leukopenia, severe renal failure, severe hypoproteinemia expressed, up to 18 years, lactation, pregnancy, hypersensitivity to the drug.

Side effects

Increased blood pressure, nausea, vomiting, aphthous stomatitis, diarrhea, abdominal pain, anorexia, tenosynovitis, ligament rupture, eczema, hair loss, dry skin, local allergic reactions, rhinitis, pneumonia, hypophosphatemia, hyperlipidemia.

Leflunomide, instructions for use (Method and dosage)

Tablets Leflunomide 20 mg swallow whole, take without binding to the time of eating, squeezed with water.
Treatment begins with taking the drug in a shock dose of 100 mg per day at a time for three days. Further - the maintenance dosage:
    with rheumatoid arthritis 10 mg - 20 mg of the drug once a day;
    with psoriatic arthritis in a dosage of 20 mg once a day.
The effect is manifested after 1-1,5 months and in the future can grow up to 6 months. No dose adjustment is required for patients over 65 years of age.

Interaction

It is not recommended to take Leflunomide with the concomitant or recent use of hematotoxic and hepatotoxic drugs because of the possible increase in adverse reactions.
The main metabolite of leflunomide inhibits the activity of the enzyme CYP2S9, so that, when taken concomitantly with drugs metabolized in connection with this enzyme system (Warfarin, phenytoin, tolbutamide), the development of negative effects is possible.

Storage conditions

At temperatures up to 25 ° C.
Shelf life - 2 years.

Reviews about Leflunomide

Reviews about the drug are favorable. Patients with rheumatoid arthritis note its high efficacy and democratic price compared to the drug Arava.