Leflunomide

Brand Obolensky OP

In stock 757 Items

Available since: 2019-09-19

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Clinical Pharmacology

Leflunomide is a basic antirheumatic drug with antiproliferative, immunosuppressive and anti-inflammatory properties. The active metabolite of leflunomide A771726 inhibits dehydroorotatdehydrogenase and exhibits antiproliferative activity. A771726 in vitro inhibits mitogen-induced proliferation and DNA synthesis of T-lymphocytes.
The antiproliferative activity of A771726 appears, apparently, at the stage of pyrimidine synthesis, since the addition of uridine to the cell culture eliminates the inhibitory effect of metabolite A771726. Using radioisotope ligands, it was shown that A771726 binds selectively to dehydroorotat dehydrogenase, which explains its ability to inhibit this enzyme and the proliferation of lymphocytes at the G1 stage. Lymphocyte proliferation is one of the key stages in the development of rheumatoid arthritis.
At the same time, A771726 inhibits the expression of receptors for interleukin2 (CD25) and Ki-67 and PCNA core antigens associated with the cell cycle.
The therapeutic effect usually appears after 4-6 weeks and may increase further over 4-6 months.

Indications

- As a basic remedy for the treatment of adult patients with the active form of rheumatoid arthritis in order to reduce the symptoms of the disease and delay the development of structural damage to the joints;
-Active form of psoriatic arthritis.

Leflunomide is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Ralef	Obolensky OP	Russia	pills
Elafra	K.O.Romparm Company S.R.L	Romania	pills
Leflunomide	Canonpharma	Russia	pills
Arava	Sanofi-aventis	France	pills

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Dosage and Administration

Leflunamide treatment begins with a single dose of a 100 mg dose for 3 days. As a maintenance dose, it is recommended to take from 10 mg to 20 mg of leflunomide 1 time per day. The therapeutic effect usually occurs after 4-6 weeks and can increase to 4-6 months. No dose adjustment is required for patients over 65 years of age. pills need to be swallowed whole, drinking plenty of liquids.

Adverse reactions

The most frequent side effects (1-10%): leukopenia; allergic reactions; loss of appetite, weight loss (usually minor); 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 tests; increased hair loss, eczema, dry skin, rash, itching; tendovaginitis, an increase in some enzymes in the blood (creatine phosphokinase).

Atypical side effects (0.1-1%):decrease in the number of red blood cells, thrombocytopenia; decrease in the level of potassium in the blood; anxiety; violation of taste sensations; hives; increased levels of fat in the blood (cholesterol and triglycerides), reduced phosphate levels in the blood.

Rare side effects (0.01-0.1%): eosinophilia, leukopenia, pancytopenia; a sharp increase in blood pressure; abnormal 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.

Contraindications

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

Drug interactions

There is no information regarding the joint use of leflunomide with antimalarial drugs used in rheumatology, intramuscularly or orally administered gold preparations, D-penicillamine, azathioprine and other immunosuppressive drugs (except for methotrexate). Unknown risk associated with the appointment of complex therapy, especially with long-term treatment. Strengthening side effects may be in the case of recent or concomitant use of hepatotoxic or hematotoxic drugs.

Special instructions

The drug can be prescribed to patients only after a thorough medical examination. It is recommended to refrain from taking alcohol. A complete blood count should be carried out before the start of treatment, as well as every 2 weeks during the first 6 months of treatment and every 8 weeks after completion of treatment. In the event of hematological reactions, including pancytopenia, it is necessary to stop taking the drug and any other concomitant drug that suppresses bone marrow hematopoiesis, and start the "laundering" procedure. Switching to a different basic drug without a “laundering” procedure may increase the possibility of additional risk even after a long time after the transition. In case of development of ulcerative stomatitis, discontinue taking leflunomide. In the event of skin and / or mucous reactions, it is necessary to stop treatment with the drug and begin the "laundering" procedure. Patients with tuberculin reactivity should be monitored due to the risk of reactivation of tuberculosis. Before starting treatment with leflunomide and periodically after starting it, blood pressure should be monitored. It is not recommended to take cholestyramine or Activated charcoal during treatment.The drug should not be prescribed to pregnant women or women of childbearing age who do not use reliable contraception during treatment with leflunomide and for some time after this treatment. The procedure of "laundering": after discontinuation of treatment with leflunomide: cholestyramine 8 g is administered 3 times a day for 11 days. Alternatively, 50 g of activated charcoal, powdered, is injected 4 times a day for 11 days. Regardless of the chosen washing procedure, it is necessary to check two separate tests at intervals of at least 14 days and wait 1.5 months from the time when the plasma concentration of the drug will first be fixed below 0.02 mg / l until fertilization. . Women of childbearing age must remember that it must be 2 years after cessation of treatment with leflunomide before they can become pregnant. Cholestyramine and Activated charcoal can affect the absorption of estrogen and progesterone in such a way that oral contraceptives do not provide a 100% guarantee. It is recommended to use alternative methods of contraception.