Arava (leflunomide), - a medicine from the group of immunosuppressants used in the treatment of rheumatoid arthritis and psoriasis.
Structure and Composition Arava
Arava - coated tablets, 10, 20 and 100 mg.
1 consists of a tablet Arava leflunomide (10, 20, and 100 mg of active substance) and excipients (lactose monohydrate, corn starch, povidone, colloidal silicon dioxide, magnesium stearate, crospovidone).
Coated tablet Arava contains hypromellose, macrogol, titanium dioxide and talc.
The pharmacological action of the drug Arava
The drug belongs to the basic anti-rheumatic drugs and has antiproliferative (prevents excessive formation of various cells), immunomodulating, immunosuppressive (suppresses the immune system) and anti-inflammatory action. Since lymphocyte proliferation is one of the basic stages in the development of rheumatoid arthritis, the drug Arava is one of the main treatment for this disease.
Arava slows the progression of joint damage (the active form of rheumatoid arthritis), and reduces the severity of symptoms.
Arava tablets may be taken with food. The maximum concentration of drug is determined by 1-24 hours after a single dose. Arava is excreted in the feces and urine. The half-life of the drug is very long (up to 2 weeks). In patients on hemodialysis, the elimination of the drug faster (due to the displacement of its association with proteins).
Studies on the pharmacokinetics of the drug Arava patients with signs of hepatic insufficiency and in patients younger than 18 years of age have not been conducted.
- Basic therapy of active forms of rheumatoid arthritis (to reduce the symptoms and delay the development of joint damage);
- Psoriatic arthritis (active form).
Hypersensitivity to any of the components, severe liver problems, severe renal dysfunction, anemia, leukopenia and thrombocytopenia pronounced degree (which have resulted from other causes), immunodeficiency (eg HIV), severe generalized infection, pregnancy and lactation.
The drug is also Arava is contraindicated in patients with severe hypoproteinaemia (reduced serum protein).
Men receiving Arabia should be aware of its negative impact on spermatogenesis. They should also be aware of the need for a reliable means of contraception (a toxic effect on embryogenesis because of the possible effect of the drug on the sperm of the father).
According to the instructions Arava is contraindicated in persons under 18 years of age due to insufficient clinical research.
Use of the drug during pregnancy and lactation
Before starting treatment with Arava in women of childbearing age should exclude pregnancy (especially if the woman does not use a reliable means of contraception). Patients should be informed about the toxic effects of the drug on the developing fetus.
According to the instructions Arabia, women are breast-feeding is contraindicated its use as animal studies have shown that the drug and its metabolites pass into breast milk.
Dosage and administration of the drug Arava
According to the drug treatment should be under the supervision of a doctor who has experience of its use in patients with rheumatoid arthritis.
According to the instructions Arava therapy begins with a single application of a loading dose (100 mg) for 3 days. Then, a maintenance dose - rheumatoid arthritis 10-20 mg once a day, psoriatic arthritis 20 mg per day. The therapeutic effect is noted Arava 4-6 weeks and increases in the next 4-6 months.
Arava tablets are taken by mouth, they should drink plenty of fluids. Ingestion of reviews Arava has no effect on absorption of the drug.
Cardio vascular system may occur: increased blood pressure, vasculitis.
From the gastrointestinal tract: nausea, vomiting, diarrhea, anorexia, oral diseases (stomatitis, mouth ulceration), abdominal pain. In rare cases, there may be jaundice, cholestasis and hepatitis. Very rarely (less than 0, 01%) noted the development of liver failure, acute hepatic necrosis, pancreatitis.
Laboratory may experience increased transaminases (ALT, AST), rarely can increase the level of gamma-glutamyl and alkaline phosphatase.
The nervous system can be observed headache, dizziness, paresthesia, taste disturbance, anxiety. In rare cases, peripheral neuropathy.
From the musculoskeletal system may occur occurrence tendovaginitis (inflammation of the tendon).
According to the instructions Arava can cause allergic reactions (usually a rash, pruritus, urticaria). Very rarely, anaphylactic reactions.
Besides the above receiving the drug Arava can cause hair loss, eczema, dry skin.
Judging by the reviews of Arabia in very rare cases may develop serious infections (less than 0, 01%), including sepsis.
Side effects from the hematopoietic system can be as follows: anemia, leukopenia, thrombocytopenia. Very rarely Arava is agranulocytosis (less than 0, 01%).
The men from the reproductive system may decrease the total number of sperm and reduce their mobility.
Overdose of the drug Arava
There have been reports of chronic overdose in patients who received a dose of the drug in 5 times the recommended daily allowance.
In the opinion of most of the Arava overdose does not cause any adverse effects. In some cases, can appear abdominal pain, diarrhea, anemia, leukopenia.
For the treatment of overdosing Arabia appointed chelators, to speed up the elimination of the drug from the body.
Interaction Arava with other drugs
In the case of administration of the drug after the recent use of hepatotoxic agents (including alcohol) may be a strengthening of side effects.
The drug Arava may be used in conjunction with methotrexate, but their combination can cause hepatotoxic effects.
Chelators (activated carbon) contribute to more rapid clearance of the drug from the body.
NSAIDs (non-steroidal anti-inflammatory drugs) and corticosteroids may be used in conjunction with Arava, as no interaction between them is not recorded.
It is not recommended to use the drug with phenytoin, warfarin and tolbutamide.
The drug Arava may be imposed only after careful expert medical examination.