Arava is the international name for the drug Leflunomide, which refers to basic antirheumatic drugs. It has antiproliferative, anti-inflammatory, and immunosuppressive effects. The tablets are yellow, dosage 10 and 20 mg. The mechanism of action is associated with the influence of the main metabolite, called A771736, on the proliferation of lymphocytes. The division of lymphocytes is the key point in the pathogenesis of the development of rheumatoid arthritis.
Drug bioavailability up to 92%. Absorption occurs in the gastrointestinal tract. The drug rapidly converts to its metabolite, which is active. It is due to the fact that metabolism occurs in the intestinal wall itself, and the drug is also characterized by a "first-pass effect" through the liver.
The maximum concentration after the first intake of a loading dose of 100 mg once a day varies from 60 minutes to 24 hours. A dose of 20 mg requires a period of 2 months. Binding occurs with plasma proteins called albumin. Microsomal and intestinal enzymes metabolize it. It is excreted through the kidneys and slightly with feces. The withdrawal period is long, about 14 days. Excretion in persons on hemodialysis is faster due to the displacement of the metabolite from the connection with blood plasma proteins. In the elderly, there is no noticeable difference in drug metabolism and excretion. There is no study of pharmacokinetics in persons under 18 years of age and with hepatic insufficiency.
Leflunomide is applicable to adults with rheumatoid arthritis in the active phase to inhibit joint damage and symptoms of diseases and the active form of psoriatic arthritis.
Take Arava only as directed by a doctor and under the supervision of a doctor who has experience in the treatment of rheumatoid and psoriatic arthritis.
Taking Arava should be started with a loading dose of 100 mg 1 time per day for 3 days. The maintenance dose is 20 mg once a day; if the drug is poorly tolerated, reduce it to 10 mg. The loading dose is recommendatory; however, at the beginning of therapy immediately with a lower dose, the effect was the same, but it took a long time. However, the side effects were less pronounced.
There is information about both chronic overdose and acute. Chronic overdose with prolonged intake at a dose exceeding the daily dose by 5 times caused abdominal pain, upset stool - diarrhea, decreased red blood cells and leukocytes in the blood, an increase in liver enzymes. Acute was observed in adults and children with the same symptoms.
Treatment: taking cholestyramine or activated carbon for faster excretion from the body. Cholestyramine 8 gr 3 times a day reduced the content of leflunomide in plasma by 65%, activated charcoal, when taken 50 gr every 6 hours, reduced by 49%.
• Immunodeficiency (AIDS) • Anemia, leukemia, thrombocytopenia not associated with rheumatoid and psoriatic arthritis • Sodium deficiency in particular neurotic syndrome • Hypersensitivity to the treatment • Men who are about to start conceiving a child at the time of taking the medication • Children under 18 years of age • Childbearing age for women who do not use reliable contraception • Severe renal and hepatic impairment
The use of the drug during pregnancy and breastfeeding is prohibited. In experiments carried out on rats and rabbits, the teratogenic effect of the A771726 metabolite on the fetus has been revealed.
For women planning pregnancy, it is necessary to know the optimal concentration of the metabolite of 0.02 mg/l, and this is considered the minimum for a teratogenic effect on the fetus. A waiting time of 2 years is required to achieve this concentration after systematic use of the treatment. There are also procedures for "washing" with cholestyramine and activated carbon. Use of drugs within 11 days. For cholestyramine 8 gr 3 times a day, activated carbon 50 gr, crushed into powder, 4 times a day.
Regardless of the chosen tactics of waiting or washing, after reaching a drug concentration of 0.02 mg/l, you must wait two months and then make two-time control of the concentration with an interval of 2 weeks.
The most common side effects include increased blood pressure, loose stools, nausea, vomiting, stomatitis, abdominal pain, headache, dizziness, weight loss, increased liver enzymes, rash, itching, hair loss, decreased blood cells (white blood cells, erythrocytes, platelets).
A high risk of developing lymphoproliferative diseases has been noted with the combined use of several immunosuppressants.
When using any immunosuppressants together or other drugs that have a toxic effect on the liver and hematopoietic system, side effects are observed. The use of side drugs is allowed only after the procedure described above - "washing".
With the combined use of leflunomide and methotrexate at a dosage of 10 to 25 mg/week in rheumatoid arthritis, there were no particularly pronounced side effects except for an increase in liver transaminases in 17% patients. Liver enzymes decreased overtime on their own with continued use or with discontinuation of leflunomide.
It is not recommended to take cholestyramine and activated carbon due to a decrease in the active metabolite of the treatment.
There is an increase in PV in the coagulogram when taking "Arava" together with warfarin.
Vaccination with live vaccines is not recommended. It is necessary to stop taking the drug and remember about its long-term withdrawal if it is planned.
Taking the drug is allowed only after examination and prescription by a doctor. The doctor should notify about all side effects and warn about their intensification with the combined use of any other hepato- and hepatotoxic drugs. The half-life of the active metabolite reaches a month, and this should be taken into account in the development of adverse, allergic, or other immunological reactions to the treatment.
• If such situations develop, the "washing" procedure described above in the pregnancy section should be applied.
• If there is a 3-fold increase in alanine aminotransferase (ALT) with a three-fold setting, it is necessary to reduce the dosage to 10 mg, and this will allow not to abandon therapy. If the increase in aspartate aminotransferase (AST) is more than 3 times, it is necessary to stop taking the drug and consider another possible treatment. In this case, it is recommended to use the procedure for the rapid elimination of the metabolite "laundering."It is forbidden to drink alcohol at the time of taking the drug.
A complete blood count (CBC) with an expanded leukocytic formula is required before starting therapy since the existing anemia, leukopenia, and thrombocytopenia can only worsen. In the future, the CBC is recommended to be done at least once a month during the first six months of treatment. Later, repeat the procedure at least once every 2 months.
Rheumatoid arthritis is a chronic, systemic, immune-inflammatory disease that affects a person's connective tissue and its osteoarticular system. Most often, the lesion occurs at the level of small joints, such as the interphalangeal and metacarpal. The destruction of the joint occurs, its shape changes and its functions are limited.
According to statistics, about 1% of people in the world are susceptible to this disease.
The problem with this disease is that there are still no exact reasons for its appearance and development. It is only known that women get sick 3 times more often, the disease begins at the age of 30-40, and further only progresses, leading to a decrease in the standard of living of a person and his/her ability to work.
Current known reasons are: • Hereditary predisposition; • Infectious agents; • Unfavorable conditions: stress, hypothermia, frequent bacterial infections, intoxication, Etc.
A varied course characterizes the disease. RA can begin with the involvement of one or more joints. Primarily, according to the manifestation of the course of this disease, it should be noted - stiffness in the joints in the morning. Waking up in the morning and during the first hour, a person cannot perform the usual actions: pick up, shift, take. He/She feels a restriction of his/her regular activity in the affected joints.
Joint pain is not constant, and it can appear and disappear. There is no periodicity. When you touch the joints, the pain may increase, and the temperature above them may be higher than in other areas of the skin. There may be swelling of the joints, the inability to squeeze the hand, and pain at the base of the toes when walking with damage to the joints of the feet. A decrease in pain syndrome can be observed with the use of non-steroidal anti-inflammatory treatments.
Over time, rheumatoid nodules may appear. Rheumatoid nodules are dense, subcutaneous, rounded formations that appear in the area of the joints.
Common symptoms include fatigue, weight loss, loss of appetite, general ill health, subfebrile body temperature, lymphadenopathy.
The disease is systemic in nature, but damage to other organs is extremely rare. And in the case of systemic damage, there is a deposition of abnormal protein in the heart, kidneys, lungs, and nervous system.
It is necessary to highlight a particularly severe form of the disease - juvenile rheumatoid arthritis. A disease that begins in childhood and adolescence and is more aggressive.
• Quitting bad habits: smoking, alcohol, drugs; • Increased dietary fiber, vitamin C-rich fruits and vegetables; • Additional use of biologically active supplements with omega 3; • Drink enough clean water; • Reduce fast carbohydrates and sugar.
Rheumatoid arthritis is one of the most severe joint diseases. And in addition to the damage to the joints, heart diseases can develop, including heart attack, aortic stenosis, mitral valve insufficiency, lung diseases: alveolitis, fistula, pleurisy, chronic renal failure, polyserositis, visceral amyloidosis. Each of which is unfavorable and carries enormous damage to health, up to and including the development of a lethal outcome. That is why there is a need for a doctor and patient compliance with treatment and clear guidelines in the fight against RA.
The advantage of traditional methods, according to sources, are natural ingredients and supposedly lack of side effects. One cannot but agree with the first, which cannot be said about the second. After all, side reactions and allergies can be to various herbs. Treatment of RA with traditional methods includes decoctions, medicinal tinctures, compresses, baths, homemade creams, and herbal ointments.
For homemade ointments, petroleum jelly, paraffin, vegetable oils, and herbs are used.
The most popular types for relieving pain, swelling, and relieving inflammation
• Callisia fragrans is crushed, squeezed, and mixed with any baby cream. Use in the morning and the evening, lubricating the affected joint, relieving swelling and pain. • Mustard powder 100 gr + sea salt 200 gr. Mix with a bit of paraffin. Mix 1/3 of the mixture. Apply once a day in the evening on the joint, wrap with foil and a warm wrap. • Olive oil 500 ml, turpentine, rubbing alcohol. Mix, add 1/3 camphor oil. Apply in the evening with a film and a warm wrap. It has anti-inflammatory and analgesic effects. • 2 tbsp. of St. John's wort, 2 tbsp. of hop cones, 2 tbsp. of sweet clover flowers. Grind into powder, mix, add 5 drops of eucalyptus oil and 50 ml of petroleum jelly. Apply 2 times a day to the affected joint. Above the film, warm wrap. It relieves swelling, pain, and inflammation.
All methods existing in traditional medicine relieve pain and swelling but do not inhibit the destruction process itself. Therefore, in the modern world, treatment protocols have been developed with the basic treatment of this disease, to which Arava belongs. In addition to the drug leflunomide, it is also worth highlighting methotrexate, sulfasalazine, hormonal drugs - prednisolone, methylprednisolone. In order to relieve inflammation, there is a group of non-steroidal anti-inflammatory drugs (NSAID) - diclofenac, meloxicam, lornoxicam, nimesulide and others. All of them are actively used now and inhibit the process of joint destruction, making life easier for people suffering from RA.
Feature a genetic predisposition and other factors described above. The exact reasons, in addition to predisposing factors, have not yet been identified. Most often, there are provoking factors in stress, infections, hormonal changes, emotional instability.
RA shortens life expectancy by 3-12 years. The disease is characterized by high disability, about 70% of the working-age population, which affects the social, economic, and medical aspects. The main causes of death are the renal failure or heart complications. In a 2005 study by the Mayo Clinic, it is found that rheumatoid arthritis increases the risk of heart disease 2 times higher than hypercholesterolemia, alcoholism, and even diabetes mellitus.
Treatment of the disease is based on alleviating the condition - slowing down the destruction process, reducing pain, relieving inflammation, and restoring damaged joints through joint prosthetics and surgical intervention. Early warning of the disease can significantly reduce the damage done to the joints. There are no overt measures for primary prevention of disease, but a healthy lifestyle prevents most diseases, and RA is no exception.