Arava

« Rheumatoid arthritis » … It sounds not so dramatically, as "heart attack" or "diabetes". Nevertheless, this disease is considered to be one of the most dangerous and guileful. It is practically impossible to distinguish it at early stages, and consequently the doctor more often deals already with the consequences and when the patient addresses to the doctor it appears, that the disease has already been progressing. And it appears much more difficultly to treat it.

A rheumatoid arthritis is one of the most dangerous and difficult for treatment diseases. If to speak about parameters of its prevalence at first sight they do not seem too high - only near 1 % of the population. However among those who addresses to a polyclinic, the quantity of patients with arthritis makes already 12,5 % (for the comparison, sick of an arterial hypertension – all about 10 %). The most unpleasant is perhaps that this disease not only carries lifelong character, but practically inevitably leads to physical inability. Especially, if not to distinguish it in time. If to consider, that a rheumatoid arthritis is a chronic disease, then the consequences appear to be even more catastrophic.

A rheumatoid arthritis (RA) is a complicated incapacitating disease for the treatment of which it is necessary to appoint basic preparations in the earliest terms. From the preparations which are used as basic, the most widely applied for today are methotrexate (the gold standard of treatment of the RA) and sulfasalazone. Unfortunately, the quantity and weight of the by-effects caused by application of these medical products, at times surpass expressiveness of therapeutic effect. In this connection, the special importance is represented at the moment by release of new, more safe preparations for treatment of a rheumatoid arthritis (RA).

The unique new first line preparation for therapy of this pathology, introduced in clinical practice for last 10 years, is the Arava (leflunomide).

During application of Arava in the world (more than five years) at hundreds thousand patients with a RA the huge experience is gained, allowing to make substantiated conclusions about a role of this preparation in treatment of a rheumatoid arthritis. The key moment in estimation of necessity of application of Arava in basic therapy is the parity of advantage and risk of the conducted therapy.

Numerous long-term researches were conducted in this direction by the results of which the commission of FDA (USA) has made the general analysis in the end of 2002. As sources of the information for an estimation of efficiency and safety of a preparation Arava were considered:

• Database of clinical researches;
• Postmarketing researches of the combined therapy;
• Database Aetna (the greatest for today database of by-effects);
• The analysis of researches Protocare/Pharmetrics;
• National databank on therapy of RA;
• The data of the group of studying of cases of occurrence of sharp hepatic insufficiency (USA);
• Analytical database of by-effects.

The results of not only clinical, but also postmarketing researches have unequivocally demonstrated, that the Arava is a highly effective preparation in treatment of RA. One of the most significant advantages of a preparation — the early beginning of clinical action, on the average in 4 weeks after the beginning of application. Besides Arava is in a greater degree, than other basic preparations, improves a functional condition of patients, and it is reflected in recommendations of the commission of FDA, where the new indications for prescription of leflunomide are fixed at RA, namely — improvement of a physical condition of patients (increase of functional activity).

Arava (leflunomide) — a basic antirheumatic preparation possessing antiproliferative, immunosuppressive and anti-inflammatory properties. It is a highly effective preparation in treatment of a rheumatoid arthritis at all stages of diseases, therapeutic effect of which is stably kept during all period of treatment.

Indications

• As a basic preparation for treatment of the active form of a rheumatoid arthritis with the purpose of reduction of symptoms of disease and at delay of development of structural damages of joints;
• The active form of a psoriatic arthritis.

Collateral action

The classification of a prospective frequency of by-effects: typical - 1-10 %, atypical - 0.1-1 %, rare - 0.01-0.1 %, very rare - 0.01 % and less.
From cardiovascular system: typical - the moderate increase of the ABP; rare - the expressed increase of the ABP; very rare - vasculitis (because of presence of the basic disease the causal relationship with reception of leflunomide could not be established).
From digestive system: typical - diarrhea, nausea, vomiting, anorexia, defeats of a mucous membrane of an oral cavity (an aphthous stomatitis, ulceration of lips), pains in a belly cavity, increase of activity of hepatic transminase (especially alanine aminotransferase), less often - gonadotropic hormone, alkaline phosphatase, hyperbilirubinemia; rare - a hepatites, a jaundice, cholestasis; very rare - heavy defeats of the liver (hepatic insufficiency, acute necrosis of the liver which can lead to a lethal outcome), pancreatitis.
From respiratory system: very rare - interstitial pulmonary process (including a interstitial pneumonia) with a possible lethal outcome.
From a metabolism: typical - loss of weight of a body, asthenia; atypical - hypokaliemia.
From CNS and peripheral nervous system: typical - headache, dizziness, asthenias, paresthesia; atypical - infringement of taste, anxiety; very rare - peripheral neuropathy.
From musculoskeletal system: typical - tendovaginitis; atypical - break of sinews.
Dermatological reactions: typical - the strengthened loss of hair, eczema, dryness of skin; very rare – a multiform erythema.
Allergic reactions: typical - easy allergic reactions, a rash (including maculo-papular), an itch; atypical - nettle-rash; very rare - Stevens-Johnson's syndrome, Lyell’s syndrome.
From the system of hematosis: typical - leukopenia (leukocytes more 2000/mcl); atypical - an anemia, a thrombocytopenia (thrombocytes less than 100 000/mcl); rare - eosinophilia, leukopenia (leukocytes less than 2000/mcl), pancytopenia; very rare - agranulocytosis. The risk of development of hematologic infringements increases at recent, accompanying and subsequent application of myelotoxic preparations.
Other: very rare - development of heavy infections (including opportunistic) and a sepsis; the increase in frequency of occurrence of possible infections (a rhinitis, a bronchitis and a pneumonia) is possible.

At application of immune depressive preparations the risk of development of malignant and some lymphoproliferative processes increases.

A light hyperlipidemia may be observed. The level of the uric acid usually decreases. The laboratory data (not confirmed clinically) testify small increase of LDH, creatine phosphokinase. A hypophosphatemia is atypical.

It is impossible to exclude the opportunity of a reversible reduction of concentration of sperm, total spermatozoa and their mobility.

Contra-indications

• Infringements of function of the liver;
• Heavy immunodeficiency conditions (including AIDS);
• The expressed infringements of a marrowy hematosis or anemia, leukopenia, thrombocytopenia as a result of other reasons (except for a rheumatoid arthritis);
• Infections of heavy current;
• Moderated or heavy renal insufficiency (because of insignificant experience of clinical supervision);
• Heavy hypoproteinemia (including at a nephrotic syndrome);
• Pregnancy;
• A lactation (the period of breast feeding);
• Children's and teenage age till 18 years;
• The raised sensitivity to the components of a preparation.

The preparation is counter-indicative to women of genital age who do not use adequate means of contraception.

The men treated by lephlunomiyde, should be warned about possible fetotoxic of a preparation and about the necessity to use adequate means of contraception.

What is the shelf life of the pills?

• The expiry date is mentioned on each blister. It is different for different batches. The shelf life is 2 years from the date of manufacture and would differ from batch to batch depending on when they were manufactured.