Instructions for use ALLOPURINOL

Indications and contraindications for taking Allopurironol

The main indications for prescribing the drug are the following conditions:

• Gout and kidney stones (pathologies accompanied by hyperuricemia).
• Psoriasis.
• Hemoblastoses (acute and chronic leukemia, lymphosarcoma).
• Urinary nephropathy and concomitant renal failure.

There are a number of absolute and relative contraindications to taking Allopurinol. The first include:

• Chronic kidney disease.
• Acute attack of gout.
• Pregnancy and breastfeeding period.
• Allergic reactions to one or more substances included in the drug.
• Hemochromatosis.

Relative contraindications are diabetes mellitus types 1 and 2, as well as arterial hypertension with high cardiovascular risk.

Special instructions for the use of the drug Allopurinol

It must be taken into account that on the 3rd–4th day after stopping Allopurinol, the indicators of uricosuria and uricemia return to the original, elevated level. Treatment should be long-term; an interval of more than 2-3 days between doses of the drug is undesirable. The drug should be used with caution in cases of mild renal failure (adults in a dose of no more than 0.2 g/day). During the use of Allopurinol, diuresis in adult patients should be maintained at a level of at least 2 l/day. It is necessary to ensure a neutral or slightly alkaline urine reaction to prevent the formation of stones. For this purpose, drugs that alkalize urine are used simultaneously with Allopurinol. To prevent possible attacks of gouty arthritis at the beginning of treatment, you can prescribe NSAIDs or colchicine (adults, 0.5 mg 3 times a day). At the beginning of treatment with Allopurinol, a systematic study of the functional state of the kidneys should be carried out.

Possible adverse reactions and symptoms of overdose

Adverse effects when taking Allopurinol can occur in various organs and systems, so side effects should be classified into groups:

1. On the part of sensitive analyzers: visual impairment, amblyopia, allergic conjunctivitis, taste perversion.
2. Gastrointestinal tract: dyspeptic syndrome, cholestasis, enlarged liver, hepatitis, hepatonecrosis.
3. CVS: decreased heart rate, hypertension, vasculitis, pericarditis.
4. From the central and peripheral nervous system: drowsiness or insomnia, paresis, disturbances in the emotional state, neuritis, paresthesia.
5. Musculoskeletal system: pain in muscles and joints.
6. Hematopoietic organs: anemia, thrombocyto-, leuko- and pancytopenia.
7. From the urinary and reproductive systems: edema, increased urea concentration, nephritis, impotence, enlarged mammary glands, changes in libido, infertility.

An overdose of the drug is accompanied by weakness, dizziness and typical symptoms of poisoning (nausea, vomiting, loose stools). It is also possible to reduce the daily volume of urine excreted.

Side effects of the drug Allopurinol

Treatment with Allopurinol is usually well tolerated by patients. In case of gout, at the beginning of treatment, an exacerbation may occur due to the mobilization of uric acid from gouty nodules and other depots. In some cases, the following are possible: dyspeptic symptoms - nausea, vomiting, epigastric pain, diarrhea; allergic reactions - skin rash, itching, hyperemia, rarely - exfoliative dermatitis, fever, arthralgia; from the blood system - leukopenia, leukocytosis, eosinophilia; from the central nervous system - neuritis, sleep disorders, depression, amnesia.

Instructions for use of the drug

Tablets are always taken orally with plenty of liquid and always after meals. The dosage, frequency and duration of administration are selected by the doctor and depend on the pathology.

For gout, the daily dose can vary from 200 to 600 milligrams of Allopurinol. In this case, the severity and degree of the disease are the main criteria for selecting the amount of medication.

For urate nephropathy and oncology, the drug is taken in the amount of 600-800 mg per day.

If it is necessary to prescribe medication to children, the dosage is calculated based on body weight. It is recommended to prescribe from 5 to 10 mg per kilogram of body weight per day, depending on the type and severity of the disease. Under the age of 15 years, the daily dosage should not exceed 300 milligrams.

Use of the drug Allopurinol

- inside after meals. Doses are set depending on the concentration of uric acid in the blood. The minimum daily therapeutic dose for adults is 0.1 g, the maximum is 0.8 g. Usually, for moderate hyperuricemia (70–100 mg/l), 0.2–0.4 g/day is prescribed 1–2 times a day. for 2–3 weeks, then switch to a maintenance dose of 0.2–0.3 g/day in 2–3 divided doses. In severe forms of gout, significant deposits of urate in tissues and severe hyperuricemia (over 80–100 mg/l), the drug is prescribed in fractions (no more than 0.2 g per dose) up to 0.6–0.8 g/day for 2– 4 weeks, and then switch to maintenance doses - 0.1–0.3 g / day, which are taken long-term, for several months. When using the drug to prevent hyperuricemia during radiation therapy and chemotherapy of tumors, the average daily dose is 0.4 g. The drug is taken 2-3 days before the start of therapy (or simultaneously) and continued for several more days after the end of specific therapy. For children under 6 years of age, the drug is prescribed at a daily dose of 5 mg/kg body weight; from 6 to 10 years - 10 mg/kg/day. The frequency of administration is 3-4 times a day. For complex treatment of epilepsy in children, the dose of the drug is 4–5 mg/kg 2 times a day for 10 days; the break between repeated courses is 1.5–2 months. If you miss the time to take the drug, take the next dose as quickly as possible. If the next dose of the drug is planned after 12 hours or more, it is necessary to take Allopurinol immediately, and the next dose at the appointed time. If there are less than 12 hours left before the next dose, the dose should be skipped and treatment should continue as usual.

Reviews about Allopurinol

Most of the patient reviews about the drug are positive. Consumers note the high effectiveness of the drug, rapid relief of symptoms of the disease, and a noticeable decrease in the level of uric acid in the blood according to test results. Patients also note that the drug works better as part of complex therapy and when following a diet.

However, there are also reviews of a different nature on the Internet, both neutral and negative. For some patients, Allopurinol either did not help or caused undesirable reactions, which served as a reason to cancel the course of treatment.

Pharmacological properties of the drug Allopurinol

Allopurinol is an anti-gout drug that inhibits the synthesis of uric acid and its salts in the body. The drug has the specific ability to inhibit the enzyme xanthine oxidase, which is involved in the conversion of hypoxanthine to xanthine and xanthine to uric acid. As a result, the urate content in the blood plasma is reduced and their deposition in tissues and kidneys is prevented. When using the drug, the excretion of uric acid in the urine decreases and the excretion of more easily soluble hypoxanthine and xanthine increases. Allopurinol in the body is converted into alloxanthin, which also prevents the formation of uric acid, but is inferior in terms of activity to allopurinol. After oral administration, about 90% of the drug is absorbed in the digestive tract. The maximum concentration of allopurinol in the blood plasma is achieved on average after 1.5 hours. The half-life of allopurinol is 1–2 hours, alloxanthin is about 15 hours, so inhibition of xanthine oxidase activity can last for 24 hours after a single dose of the drug. About 20% of the dose taken is excreted in feces, the rest of the drug and its metabolites are excreted in urine.

Allopurinol

Use during pregnancy and breastfeeding

Contraindicated for use during pregnancy and lactation (breastfeeding).

Use for liver dysfunction

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

Use for renal impairment

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

Use in children

In children, it is used only for malignant neoplasms (especially leukemia), as well as for certain enzyme 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: 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. During the initial period of allopurinol therapy, systematic assessment of liver function parameters is necessary.

During 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 a day). It should be taken into account that with adequate therapy with allopurinol, large urate stones in the renal pelvis may dissolve and subsequently 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 certain enzyme disorders (Lesch-Nychen syndrome).

To correct hyperuricemia in patients with tumor diseases, allopurinol is recommended 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 diuresis and alkalinization of urine. With the simultaneous use of allopurinol and cytostatics, more frequent monitoring of peripheral blood patterns is necessary.

During the period of taking allopurinol, alcohol consumption is not allowed.

Impact on the ability to drive vehicles and operate machinery

Use with caution in patients whose activities require high concentration and rapid psychomotor reactions.

Drug interactions Allopurinol

When treating hemoblastomas with antitumor drugs (methotrexate, mercaptopurine, etc.), it should be taken into account that the simultaneous use of Allopurinol not only inhibits the enzymatic oxidation of these drugs and enhances their antitumor activity, but also significantly increases toxicity. Doses of antitumor drugs in such cases should be reduced by 50%. Under the influence of Allopurinol, it is also possible to enhance the effects (including unwanted) of indirect anticoagulants, antipyrine, diphenine, theophylline, since their inactivation in the liver slows down. When used simultaneously with ampicillin drugs, the risk of developing a skin rash increases. Under the influence of thiazide diuretics, furosemide, ethacrynic acid, the antihyperuricemic effect of Allopurinol is weakened, since these drugs increase the level of uric acid in the blood plasma. Allopurinol should not be used in combination with iron-containing drugs due to the possible accumulation of iron in the liver.

Allopurinol (Allopurinolum)

Diseases accompanied by hyperuricemia (treatment and prevention). Gout (primary and secondary). Mild symptoms of gout - 200-300 mg/day, severe gout with tophi - 400-600 mg/day, for a lesser risk of exacerbation of gout - 100 mg/day with a weekly increase of 100 mg (until the uric acid level in plasma decreases to 6 mg/dl). The onset of action is 2-3 days, the maximum effect develops after 1-3 weeks of continuous use, the duration of action is 1-2 weeks after cessation of therapy. Kidney stone disease (with the formation of urates). 200-300 mg/day, for chronic renal failure the dose is reduced: for CC 10-20 ml/min - 200 mg, 10 ml/min - 100 mg, ‹3 ml/min - 100 mg after 36-72 hours. Hyperuricemia (primary and secondary). For diseases accompanied by increased breakdown of nucleoproteins and increased levels of uric acid in the blood, including various hemoblastoses (acute leukemia, chronic myeloid leukemia, lymphosarcoma). For cytostatic and radiation therapy of tumors (including in children) (weak and unreliable evidence of effectiveness in the treatment of oral mucositis). During the first 2-3 days, 600-800 mg/day, plenty of fluid intake. For psoriasis. For extensive traumatic injuries. Due to enzyme disorders (Lesch-Nychen syndrome). Purine metabolism disorders in children. Uric acid nephropathy with impaired renal function (renal failure). Recurrent mixed oxalate-calcium kidney stones (in the presence of uricosuria). Orally after meals in 2 doses or once. Doses exceeding 300 mg are taken in fractions. The minimum effective dose is 100-200 mg/day, the maximum is 800-900 mg/day.

When adding allopurinol to uricosuric drugs, its dose should be gradually increased, and the dose of uricosuric drugs should be reduced. Daily diuresis is at least 2 liters, urine pH is neutral or slightly alkaline.

Use in children

Prevention of hyperuricemia associated with antitumor chemotherapy, prevention of urate nephropathy, Lesch-Nyhan syndrome (enzyme-mediated hyperuricemia). Orally. 1 month-15 years: 10-20 mg/kg/day (maximum 400 mg) after meals. 15-18 years: starting from 100 mg/day after meals, the dose is selected depending on the concentration of uric acid in the blood/urine (maximum 900 mg), doses of more than 300 mg are taken in several doses.