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Principle effects based on the inhibition of xanthine oxidase, preventing transition hypoxanthine to xanthine, which is formed from
uric acid
. The drug lowers a concentration of uric acid salts, most uric acid in liquid media in humans. The drug prevents the formation of
urate deposits
in the renal system, in the tissue and promotes their dissolution. Allopurinol by reducing the transformation of hypoxanthine to xanthine leads to increased their use in the process of synthesizing nucleotides
nucleic acid
. With the accumulation of xanthine in plasma does not change the normal exchange of nucleic acid, the precipitation process is not violated, and xanthines do not precipitate in the plasma due to the high solubility. When xanthine excretion in the urine does not increase the risk
nefrourolitiaza
. Allopurinol is available in tablet dosage form.
Indications:
Allopurinol applies at diseases of, accompanied by hyperuricemia : Nephrolithiasis, gout. The drug is prescribed for psoriasis, radiation and cytostatic therapy of tumors, with hyperuricemia at gemablastozah (lymphosarcoma, chronic myelogenous leukemia, acute leukemia), and solid therapy glucocorticosteroids , With extensive traumatic injuries (syndrome Lesch-Nihena), in violation of purine metabolism in children. The medicament appoint at urikozurii when of recurrent of mixed oxalate-calcium kidney stones, when Uric acid nephropathy with disturbances in the renal system (kidney failure).
Contraindications:
Allopurinol is not indicated in patients with chronic renal failure in stage azotemia, intolerance to the active component, pregnancy, acute attack of gout, hemochromatosis , Breastfeeding, asymptomatic hyperuricemia. In patients with hypertension, renal disease, with diabetes Allopurinol is prescribed with caution.
Side effect:
Senses: amblyopia Perversion of taste perception, cataracts, disorders of vision, loss of taste, conjunctivitis . Nervous system: drowsiness, depression, paresis, neuritis, headache, paresthesia, peripheral neuropathy. The digestive tract: diarrhea, dyspepsia , Epigastric pain, nausea, vomiting, increased liver enzymes, cholestatic jaundice , Hyperbilirubinemia, rare granulomatous hepatitis, hepatomegaly , Gepatonekroz. Cardiovascular system: vasculitis, bradycardia, increase in blood pressure, pericarditis. Musculoskeletal system: myalgia, myopathy, arthralgia. Urogenital: peripheral edema, gynecomastia, infertility, hematuria, increased levels of urea, proteinuria, acute renal failure, reduced potency, interstitial nephritis . Bodies of blood: anemia, agranulocytosis, leukopenia, eosinophilia, thrombocytopenia , Aplastic anemia. Because of possible allergic reactions: erythema multiforme exudative, hives . itching , Rash, bronchospasm, exfoliative dermatitis , Eczematous dermatitis, purpura, toxic epidermal necrolysis, bullous dermatitis. Also available nosebleeds, dehydration, alopecia, abrasions, pyrexia, lymphadenopathy, necrotic angina , Hyperlipidemia.
Overdose:
Manifested oliguria, dizziness, vomiting, diarrhea, nausea. It is recommended to conduct peritoneal dialysis, hemodialysis is effective forced diuresis .
Mode of application:
Allopurinol is taken after food inside. When Just noticeable symptoms of gout is recommended daily to receive 200-300 grams of the drug. In severe form, in the presence of tophi appoint 400-600 mg daily. The daily amount of the drug can be divided into 2 doses. The dose of 300 mg taken fractionally. The minimum effective dose is considered to be 100-200 mg / day. To reduce the risk of acute gout therapy is recommended to start with small doses of 100 mg per day, with a consequent increase in the dose of 100 mg every week. During the chemotherapy of malignant diseases of the blood to prevent urate nephropathy within three days appoint 600-800 mg per day, be sure to drink plenty of liquids. Elderly people prescribed the minimum dose of the drug allopurinol.
Special instructions:
Allopurinol is not recommended for appointment at asymptomatic urikozurii . Appropriate therapy can lead to dissolution of large uric acid stones in the renal pelvis system with access to the ureter and the formation of renal colic. The drug is prescribed only to children in congenital diseases of purine metabolism in malignant tumors. It is unacceptable to begin treatment until complete relief of acute attack of gout. In the first month of therapy prescribed drugs of the NSAID, Colchicine . With the development of an acute attack of gout is added to the treatment regimen anti-inflammatory medicines. In violation of the liver, renal system reduce the dosage allopurinol. The drug can be combined with vidarabine under medical supervision, with caution.
Drug Interactions:
Uricosuric medications increase the renal clearance of the active metabolite oksipurinola, unlike thiazide diuretics Which increase the toxicity and slow renal clearance . Allopurinol increases the impact of hypoglycemic, oral agents. The drug inhibits metabolism, increases concentration, and accordingly, the toxicity of methotrexate, mercaptopurine, azathioprine, xanthine, adenine arabinoside. At reception acetylsalicylic acid and increases the efficiency of the drug colchicine. Allopurinol prolongs the half-life of coumarin anticoagulants, which leads to increased gipoprotrombinemicheskogo effect. The frequency of of development of of dermal rashes increases when appointing of amoxicillin, of ampicillin. The risk of developing bone marrow aplasia increases when receiving doxorubicin, cyclophosphamide, procarbazine, bleomycin. The accumulation of iron in the liver is observed when co-administered allopurinol and iron preparations. In renal insufficiency, a combination with ACE inhibitors leads to increased risk of toxicity. Nephrotoxicity observed in the appointment of cyclosporine. Antigiperurikemicheskoe effects reduced while taking ethacrynic acid, furosemide, thiazide diuretics, pyrazinamide, tiofosfamida, uricosuric drugs .