Allopurinol (allopurinol) tablets 0.1 №50

active substance: allopurinol ;

1 tablet contains allopurinol (in terms of 100% dry matter) – 100 mg;

excipients: lactose monohydrate, microcrystalline cellulose, corn starch, hypromelose, magnesium stearate.

Remedies for gout. Drugs that inhibit the formation of uric acid. Allopurinol. ATX code M04A A01.

Allopurinol is an anti-gout drug that inhibits the synthesis of uric acid and its salts in the body. The drug has a specific ability to inhibit the xanthine oxidase enzyme involved in the conversion of hypoxanthine to xanthine and xanthine to uric acid. As a result, the content of urates in the blood serum decreases, which prevents their deposition in the tissues and kidneys.

Allopurinol in the body turns into oxypurinol (alloxanthin), which also prevents the formation of uric acid, but is inferior in activity to allopurinol.

After oral administration, allopurinol is absorbed rapidly and completely. It is practically not absorbed in the stomach, absorption occurs in the duodenum and in the upper part of the small intestine. As a result of metabolism, the main pharmacologically active metabolite oxypurinol is formed. The maximum levels of oxypurinol are reached after 3-4 hours, the rate of formation depends on the degree and speed of the individual first pass metabolism. Allopurinol and oxypurinol practically do not bind to blood proteins. The half-life of allopurinol from blood plasma is about 40 minutes, oxypurinol – 17-21 hours. 80% of allopurinol and oxypurinol are excreted by the kidneys, 20% – through the intestines. In renal insufficiency, the half-life of oxypurinol increases.

For adults:

• hyperuricemia (with a serum uric acid level of 500 µmol / l (8.5 mg / 100 ml) and above, which is not controlled by diet);
• diseases caused by an increase in the level of uric acid in the blood, especially with gout, urate nephropathy and urate urolithiasis;
• secondary hyperuricemia of various etiologies, incl. with psoriasis;
• primary and secondary hyperuricemia in various hemoblastoses (acute leukemia, chronic myeloid leukemia, lymphosarcoma);
• cytotoxic therapy of neoplastic and myeloproliferative diseases.

For children :

• urate nephropathy as a result of treatment for leukemia;
• secondary hyperuricemia of various etiologies;
• congenital enzymatic deficiency, in particular Lesch-Nien syndrome (partial or complete deficiency of hypoxanthine-guanine phosphoribosyltransferase) and congenital deficiency of adenine phosphoribosyltransferase.

• Hypersensitivity to allopurinol or to other components of the drug;
• severe violations of the liver or kidneys (creatinine clearance less than 2 ml / min);
• acute attack of gout.

Take Allopurinol tablets after meals, without chewing, with plenty of water.

For adults and children over 10 years old, the daily dose should be determined individually, depending on the level of uric acid in the blood serum. Usually the daily dose is 100-300 mg/day. To reduce the risk of adverse reactions, treatment should begin with allopurinol 100 mg once daily.

If necessary, gradually increase the initial dose of Allopurinol tablets by 100 mg every 1-3 weeks until the maximum effect is obtained. The maintenance dose is usually 200-600 mg/day. In some cases, the dose of the drug can be increased to 600-800 mg / day.

If the daily dose exceeds 300 mg, it should be divided into 2-4 equal doses.

When increasing the dose, it is necessary to monitor the level of oxypurinol in the blood serum, which should not exceed 15 μg / ml (100 μmol).

The maximum single dose is 300 mg, the maximum daily dose  is  800 mg.

For children from 3 to 6 years of age, prescribe a daily dose of 5 mg / kg of body weight, from 6 to 10 years – 10 mg / kg of body weight. The multiplicity of reception is 3 times a day, the maximum daily dose is 400 mg.

kidney failure

Treatment should begin with a daily dose of 100 mg and increase only if the drug is not effective enough. When choosing a dose, one should be guided by the creatinine clearance indicator: