Allopurinol is a remedy for gout, belongs to the pharmacological group of xanthine oxidase inhibitors. The drug violates the synthesis of uric acid. The main action of Allopurinol is urostatic, it inhibits the action of the enzyme xanthine oxidase, which stimulates the oxidation of hypoxanthine to xanthine, and its subsequent conversion to uric acid. These substances are much more soluble. Thus, the drug reduces the level of uric acid in the body and helps to dissolve urates, thereby preventing their deposition in the tissues and kidneys.
Allopurinol is well absorbed by the digestive tract, reaches maximum plasma concentration in 3-5 hours. The substance practically does not bind to plasma proteins, it leaves mostly with the kidneys, approximately 20% is excreted by the intestines in 48-72 hours.
Release form and composition
Allopurinol is available in the form of tablets of 100 and 300 mg, packaged in blisters of 10 pieces, or in vials of 50 pieces. One tablet contains 100 or 300 mg of allopurinol, as well as excipients: sucrose, potato starch, magnesium stearate, edible gelatin, lactose monohydrate, colloidal silicon dioxide.
Indications for use Allopurinol
The use of Allopurinol is indicated for diseases accompanied by hyperuricemia, which cannot be controlled only by diet, with a level of uric acid in the range of 500 μmol and above. Such diseases include gout (primary and secondary), urate urolithiasis, urate nephropathy, renal disease with the formation of urates. The use of Allopurinol takes place in the treatment of primary and secondary hyperuricomia in such conditions and diseases as: renal failure, massive therapy of GCS, various types of hematoblast: acute leukemia, chronic myeloid leukemia, lymphosarcoma, as well as cytostatic and radiation treatment of tumors (including children), psoriasis. Allopurinol is used in pathologies associated with enzyme disorders (Lesch-Nihena syndrome), extensive traumatic injuries, impaired purine metabolism in children, and the formation of mixed calcium oxalate stones. For the treatment of children over 15 years old, Allopurinol is used for urate nephropathy, which occurred on the background of leukemia.
The use of Allopurinol is contraindicated in people with intolerance to the active ingredient or auxiliary components of the drug. Other contraindications are severe liver dysfunction, renal failure with creatinine clearance less than 2 ml / min, age up to 15 years. Allopurinol is not prescribed in cases where the level of uric acid in plasma can be regulated by diet.
With caution, the drug is prescribed to patients with impaired hematopoiesis, with hepatic and renal insufficiency. Also in cases of arterial hypertension and heart failure, when the patient is being treated with angiotensin-converting enzyme inhibitors and diuretics. Allopurinol is not prescribed to people suffering from acute attacks of gout, drug treatment can be started only when the patient's condition improves.
Dosing and Administration Allopurinol
The instructions for Allopurinol said that the pill must be taken orally, drinking plenty of water. It is recommended to use the drug after meals. During treatment with Allopurinol, it is necessary to drink as much liquid as possible in order to maintain normal diuresis. The course of treatment and the exact dosage of the drug can be prescribed only by a doctor, based on the patient's condition and the amount of uric acid in the blood.
The minimum daily dose of the drug is 100 mg, the maximum - 800 mg, the average - 200-300 mg. According to the instructions for Allopurinol, therapy is recommended to start with a minimum dose of 100 mg per day, gradually adjusting it. To do this, it is necessary to conduct a weekly analysis of the level of uric acid in the blood. For the treatment of moderate hyperuricemia, 200-400 mg per day is prescribed in a course of 2-4 weeks, then the dosage is reduced to 200-300 mg. In severe hyperuricemia and gout, 600-800 mg of Allopurinol is prescribed in a course of 2-4 weeks, after which the dosage is reduced to 100-300 g per day. Maintenance dosage is 200-600 mg, it can be taken for several months. You can not interrupt treatment for longer than 3 days, since therapy requires a long period of time. For the prevention of hyperuricemia with radiation or chemotherapy, 400 mg is prescribed. Do not take more than 300 mg of the drug at a time, the dosage of more than 300 mg should be divided into several parts.
In the instructions for Allopurinol said, the dosage for children should be 10-20 mg per 1 kg of weight. The dosage should be divided into 3 parts and taken 3 times a day. For children older than 15 years, the maximum dosage is 400 mg per day.
Side Effects of Allopurinol
Allopurinol use rarely has side effects. At the initial stage of treatment, patients may experience gout attacks. The following side effects are possible:
- On the part of the hematopoietic system: eosinophilia, leukopenia, leukocytosis, thrombocytopenia;
- On the part of the hepatobiliary system: hepatic necrosis, granulomatous hepatitis, increase in liver enzymes;
- From the side of the central nervous system: ataxia, depression, headaches, paralysis, drowsiness, coma;
- From the senses: cataract, blurred vision, reduced taste sensations;
- Since the cardiovascular system: bradycardia, lowering blood pressure.
Regarding the effect of allopurinol on the body of pregnant women, no studies have been conducted. However, its use during pregnancy is not recommended. Since Allopurinol passes into breast milk, breastfeeding should be suspended for the period of treatment.
Allopurinol analogs are Ziloprim, Milurit, Allohexal.
Terms and conditions of storage
The drug should be stored at a temperature of 15 to 25 ° C in places isolated from light.