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Arava user manual

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Composition

The composition of 1 tablet of Arava includes the active substance leflunomide in the amount of 10, 20 or 100 mg, as well as auxiliary substances and components of the film shell.

Form of issue

The drug is issued in tablet form for 10, 20 or 100 mg of the active substance.

pharmachologic effect

An antirheumatic drug. Arava has a pronounced immunosuppressive activity, it also has an anti-inflammatory and antiproliferative effect.

Pharmacodynamics and pharmacokinetics

The active substance is leflunomide. The mechanism of action of leflunomide is associated with inhibition of the dehydroorotate dehydrogenase enzyme. In studies it was proved that the active metabolite leflunomide, which is formed in the process of metabolism in the human body, selectively interacts with this enzyme, which is accompanied by inhibition of proliferation of T-lymphocytes. This mechanism of action provides an immunosuppressive effect. T-lymphocytes trigger the chain of reactions underlying the pathogenesis of rheumatoid arthritis, and therefore, the suppression of the cellular immune link positively affects the course of the disease in its acute stage.
This effect of leflunomide is not the only one. In addition to inhibition of T-cell proliferation, Arava lowers receptivity of tissue receptors to interleukin-2. The latter is a trigger factor for triggering an inflammatory response in organs and tissues, so that a decrease in sensitivity to the mediator has an anti-inflammatory effect.
Accept Arava orally, regardless of food intake (the latter does not affect bioavailability).
In the intestine, up to 90% of the active substance leflunomide is absorbed. Leflunomide in the liver is rapidly metabolized to form an active form, which influences the cellular link of the immune response.
Half-life is up to two weeks. The effect of taking leflunomide occurs four to six weeks after the start of the medication, the drug has the property of being cumulated in organs and tissues, and therefore the effect persists for a long period of time - up to six months.

Indications for use

Arava (leflunomide) is used to treat patients with rheumatoid arthritis in the active stage. There are also data on the possibility of using the drug in psoriatic arthritis (also in active form).

Contraindications

Arava is contraindicated in the presence of hypersensitivity to the active substance.
Do not prescribe leflunomide in case of liver failure, with severe immunodeficiency (including AIDS).
Contraindication to the appointment of Arava will also be significant disorders of hematopoiesis, severe anemia, thrombocytopenia or leukopenia. Do not prescribe Arava for severe infectious diseases.
Renal insufficiency, both mild and severe, is a relative contraindication to the administration of leflunomide (due to insufficient experience of use).
Reducing the protein content in the blood can be a contraindication for the administration of leflunomide.
Arava is not intended for use in pregnancy. You can not prescribe leflunomide during lactation.

Side effects

Cardiovascular system: when taking leflunomide, it is possible to increase blood pressure, in extremely rare cases, inflammation of the blood vessels (vasculitis) can be attached.
The digestive tract can respond to taking the drug with diarrhea, vomiting or nausea, and reducing appetite. Often there is a violation of the liver, which can be fixed by increasing the activity of specific enzymes of transaminases.
It is also possible to increase the level of bilirubin in the blood plasma. Much less often with leflunomide, hepatitis develops, which can be accompanied by hepatic insufficiency. In the worst case, acute necrosis can occur in the liver.
Suffers from the reception of Arava and the musculoskeletal system, in particular, the ligamentous apparatus (the most common complication is tendon inflammation, tendovaginitis).
Since leflunomide affects all actively proliferating tissues, it can cause hair loss and changes in the skin condition (dry skin, eczematous manifestations), it may develop polymorphic exudative erythema and Lyell's syndrome. Also, an allergic reaction to the drug may manifest as anaphylactic shock.
The hematopoietic system may respond to leflunomide leukopenia, a decrease in the level of erythrocytes, and minor thrombocytopenia. In more severe cases, agranulocytosis may develop. Leflunomide in combination with other immunosuppressants increases the likelihood of developing infections, malignant neoplasms, diseases of the hematopoietic system.

Arava, instructions for use (Method and dosage)

Arava is available in tablets that contain 10 mg, 20 mg or 100 mg leflunomide.
Admission of the drug is possible only with the direct participation of a doctor who has experience in the use of such drugs in the treatment of rheumatoid arthritis. According to the instructions for the use of Arava, as a rule, therapy starts with a shock starting dose of 100 mg per day, which is prescribed for three days. After this, they switch to a maintenance dosage of 10 or 20 mg per day. Take once, regardless of food intake, drink medicinal product with plenty of water.

Overdose

When taking leflunomide, an overdose is possible. The treatment consists in taking the same drugs that are used for washing - activated charcoal and colestyramine.
Kolestiramin is taken orally 8 g 3 times during the day. Activated carbon - orally or through a probe of 50 g for one day every six hours.

Interaction

Since leflunomide has a toxic effect on the liver, it is possible to intensify this effect when using other hepatotoxic (including alcohol-containing beverages) and immunosuppressive agents. The same increase in toxic effect can occur if the administration of these drugs begins without the above described procedure of "laundering".
With rheumatoid arthritis, there have been no reported cases of interaction between leflunomide and cytostatic drug methotrexate, which is also included in the treatment regimen of this disease.
Leflunomide should be used with preparations such as phenytoin, tolbutamide, warfarin, as leflunomide inhibits the activity of the enzyme responsible for the metabolism of these drugs.
Leflunomide does not reduce the effectiveness of oral contraceptives.

Storage conditions

In a place inaccessible to children at a temperature of no more than 25 degrees Celsius.

Shelf life

Not more than three years.

special instructions

Since leflunomide has the property of accumulating in organs and tissues, and, among other things, it has a long half-life, after stopping the use of Arava, it is necessary to carry out the procedure of "laundering". To this end, the patient is prescribed colestramine in a dosage of 8 g three times a day for 11 days, or alternatively, an activated charcoal can be used. It must be taken as follows: 50 g of powdered powder four times a day for the same eleven days.
Since it is possible to develop serious complications from the liver, the leflunomide should be accompanied by a constant control of the level of hepatic enzymes and other indicators of the liver parenchyma.
Men who receive leflunomide should be aware of its possible toxic effects on spermatozoa, and accordingly, it becomes necessary to use proven contraceptives.
Children under the age of 18 are not prescribed Arava.
Women of fertile age before the start of the leflunomide therapy course must be examined by a gynecologist for pregnancy and warned of possible consequences. If a woman expresses a desire to have a child at the end of the course of taking leflunomide, she should undergo the procedure of washing, after which the level of the drug in the blood plasma will be determined. After it falls to the level of 0.02 milligrams per liter, you need to wait another month and a half, and only then you can think about conception. Ideally, after the end of the course of treatment with leflunomide from conception, it is necessary to abstain for another two years.

Reviews about Arava

The agent, mainly, helps with rheumatoid arthritis, stopping the progression of the disease. The destruction of the joints is terminated, however, weak pains in them, as well as swelling in the heat, are possible.
According to reviews on Arava on the forums, side effects from this remedy are frequent. Hair starts to fall out, there is diarrhea, however, usually these symptoms pass with the passage of time.