Allopurinol tablets 100mg, No. 50

• Treatment and prevention of gout and hyperuricemia of various origins (including in combination with nephrolithiasis, renal failure, urate nephropathy).

• Recurrent mixed calcium oxalate kidney stones in the presence of hyperuricosuria. Increased formation of urates due to enzyme disorders.

• Prevention of acute nephropathy with cytostatic and radiation therapy of tumors and leukemias, as well as with complete medical fasting.

Set individually, under the control of the concentration of urate and uric acid in the blood and urine. Adults when taken orally - 100-900 mg / day, depending on the severity of the disease. The frequency of admission is 2-4 times / day after meals. Children under 15 years old - 10-20 mg / kg / day or 100-400 mg / day.

Maximum doses: for impaired renal function (including those caused by urate nephropathy) - 100 mg / day. An increase in the dose is possible in cases where, against the background of the therapy, an increased concentration of urates in the blood and urine remains

Allopurinol

Excipients: microcrystalline cellulose - 54 mg, corn starch - 25 mg, sodium carboxymethyl starch - 10 mg, povidone K-25 - 8 mg, colloidal silicon dioxide - 1 mg, magnesium stearate - 2 mg.

• Severe liver and / or kidney dysfunction,

• pregnancy,

• lactation,

• hypersensitivity to allopurinol.

pharmachologic effect

A drug that disrupts the synthesis of uric acid. It is a structural analogue of hypoxanthine. Inhibits the enzyme xanthine oxidase, which is involved in the conversion of hypoxanthine to xanthine and xanthine to uric acid. This is due to a decrease in the concentration of uric acid and its salts in body fluids and urine, which helps to dissolve the existing urate deposits and prevents their formation in tissues and kidneys. When allopurinol is taken, the urinary excretion of hypoxanthine and xanthine increases.

Pharmacokinetics

After oral administration, it is almost completely (90%) absorbed from the gastrointestinal tract. It is metabolized to form alloxanthin, which retains the ability to inhibit xanthine oxidase for a long time. Cmax of allopurinol in blood plasma is reached on average after 1.5 hours, alloxanthin - after 4.5 hours after a single dose. T1 / 2 of allopurinol is 1-2 hours, alloxanthin - about 15 hours. About 20% of the dose taken is excreted through the intestines, the rest - by the kidneys.

Side effect

From the side of the cardiovascular system: in isolated cases - arterial hypertension, bradycardia.

From the digestive system: possible dyspeptic symptoms (including nausea, vomiting), diarrhea, transient increase in the activity of transaminases in the blood serum; rarely - hepatitis; in isolated cases - stomatitis, liver dysfunction (transient increase in the activity of transaminases and alkaline phosphatase), steatorrhea.

From the side of the central nervous system and peripheral nervous system: in isolated cases - weakness, fatigue, headache, dizziness, ataxia, drowsiness, depression, coma, paresis, paresthesia, convulsions, neuropathy, visual impairment, cataracts, changes in the papilla of the optic nerve, taste disturbances sensations.

From the hematopoietic system: in some cases - thrombocytopenia, agranulocytosis and aplastic anemia, leukopenia (most likely in patients with impaired renal function). From the urinary system: rarely - interstitial nephritis; in isolated cases - edema, uremia, hematuria.

From the endocrine system: in isolated cases - infertility, impotence, gynecomastia, diabetes mellitus.

From the side of metabolism: in isolated cases - hyperlipidemia.

Allergic reactions: skin rash, flushing, itching; in some cases - angioimmunoblastic lymphadenopathy, arthralgia, fever, eosinophilia, fever, Stevens-Johnson syndrome, Lyell's syndrome. Dermatological reactions: in isolated cases - furunculosis, alopecia, hair discoloration.

Application during pregnancy and lactation

Contraindicated for use during pregnancy and lactation (breastfeeding).

Application for violations of liver function

Contraindication: severe liver dysfunction. Allopurinol should be used with caution in case of liver dysfunction (dose reduction is necessary).

Application for impaired renal function

Contraindication: severe renal dysfunction. Allopurinol should be used with caution in case of impaired renal function (dose reduction is necessary).

Application in children

In children, it is used only for malignant neoplasms (especially leukemias), as well as for some enzymatic disorders (Lesch-Nychen syndrome). The dosage regimen is set individually, under the control of the concentration of urates and uric acid in the blood and urine: for children under 15 years of age - 10-20 mg / kg / day or 100-400 mg / day.

special instructions

Allopurinol should be used with caution in case of impaired liver and / or kidney function (in both cases, a dose reduction is necessary), hypothyroidism. In the initial period of the course of therapy with allopurinol, a systematic assessment of liver function indicators is necessary. During the period of treatment with allopurinol, the daily amount of fluid consumed should be at least 2 liters (under the control of diuresis). At the beginning of the course of treatment for gout, an exacerbation of the disease may occur. For prevention, you can use NSAIDs or colchicine (0.5 mg 3 times / day). It should be borne in mind that with adequate therapy with allopurinol, large urate stones may dissolve in the renal pelvis and then enter the ureter. Asymptomatic hyperuricemia is not an indication for the use of allopurinol.In children, it is used only for malignant neoplasms (especially leukemia), as well as for some enzymatic disorders (Lesch-Nychen syndrome). For the correction of hyperuricemia in patients with neoplastic diseases, it is recommended to use allopurinol before starting treatment with cytostatics. In such cases, the minimum effective dose should be used. In addition, in order to reduce the risk of xanthine deposition in the urinary tract, measures must be taken to maintain optimal urine output and urinary alkalinization. With the simultaneous use of allopurinol and cytostatics, more frequent monitoring of the picture of peripheral blood is necessary. During the period of taking allopurinol, alcohol is not allowed.For the correction of hyperuricemia in patients with tumor diseases, it is recommended to use allopurinol before starting treatment with cytostatics. In such cases, the minimum effective dose should be used. In addition, in order to reduce the risk of xanthine deposition in the urinary tract, measures must be taken to maintain optimal urine output and urinary alkalinization. With the simultaneous use of allopurinol and cytostatics, more frequent monitoring of the picture of peripheral blood is necessary. During the period of taking allopurinol, alcohol is not allowed.For the correction of hyperuricemia in patients with neoplastic diseases, it is recommended to use allopurinol before starting treatment with cytostatics. In such cases, the minimum effective dose should be used. In addition, in order to reduce the risk of xanthine deposition in the urinary tract, measures must be taken to maintain optimal urine output and urinary alkalinization. With the simultaneous use of allopurinol and cytostatics, more frequent monitoring of the picture of peripheral blood is necessary. During the period of taking allopurinol, alcohol is not allowed.With the simultaneous use of allopurinol and cytostatics, more frequent monitoring of the picture of peripheral blood is necessary. During the period of taking allopurinol, alcohol is not allowed.With the simultaneous use of allopurinol and cytostatics, more frequent monitoring of the picture of peripheral blood is necessary. During the period of taking allopurinol, alcohol is not allowed.

Influence on the ability to drive vehicles and use mechanisms

Use with caution in patients whose activities require a high concentration of attention and quick psychomotor reactions.

Drug interactions

With the simultaneous use of allopurinol enhances the effect of coumarin anticoagulants, adenine arabinoside, as well as hypoglycemic drugs (especially with impaired renal function). Uricosuric agents and salicylates in high doses reduce the activity of allopurinol. With the simultaneous use of allopurinol and cytostatics, myelotoxic effect is more often manifested than with separate use. With the simultaneous use of allopurinol and azathioprine or mercaptopurine, accumulation of the latter in the body is observed, because due to the inhibition of xanthine oxidase activity by allopurinol, which is necessary for the biotransformation of drugs, their metabolism and elimination slows down.