APURILL [Allopurinol] 300 mg Tablets
APURILL
instructions for medical use of the medicinal product
Tradename
Apurill, Apurill
International non-proprietary name
allopurinol, allopurinol
Composition
Each film-coated tablet contains:
active substance: allopurinol 300 mg
excipients: starch, dextrin, microcrystalline cellulose, hypromellose, magnesium stearate, talc
Dosage form
Tablets.
Pharmacotherapeutic group
Antigout agent, xanthine oxidase inhibitor.
Pharmacological properties
Pharmacodynamics
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 contributes to the dissolution of existing urate deposits and prevents their formation in tissues and kidneys. When taking allopurinol, the excretion of hypoxanthine and xanthine in the urine increases.
Pharmacokinetics
After oral administration, it is almost completely (90%) absorbed from the gastrointestinal tract. It is metabolized with the formation of alloxanthin, which retains the ability to inhibit xanthine oxidase for a sufficiently long time. Cmax of allopurinol in plasma is achieved on average after 1.5 hours, alloxanthin - 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.
Indications for use
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 leukemia, as well as with complete therapeutic starvation.
Contraindications
Hypersensitivity to allopurinol or any of the excipients that make up the drug.
Liver failure, chronic renal failure (azotemia stage), primary hemochromatosis, asymptomatic hyperuricemia, acute gout attack, children under 3 years of age (including solid dosage form)
Pregnancy, breastfeeding period.
Dosage and administration
Inside, after eating. The tablets are swallowed whole, without chewing, with plenty of water.
If the daily dose exceeds 300 mg or symptoms of intolerance are observed from Gastrointestinal tract, then the dose must be divided into several doses.
Adults. In order to reduce the risk of side effects, it is recommended to use Apurill at an initial dose of 100 mg 1 time per day. If this dose is not enough to properly reduce the concentration of uric acid in the blood serum, then the daily dose of the drug can be gradually increased until the desired effect is achieved. Special care should be taken in case of impaired renal function.
When increasing the dose of the drug every 1-3 weeks, it is necessary to determine the concentration of uric acid in the blood serum.
The recommended dose of the drug is 100-200 mg / day for mild disease; 300-600 mg / day for moderate course; 600–900 mg/day in severe cases. Maximum daily dose - 900 mg.
Children and teenagers up to 15 years old. Recommended dose for children aged 3 to 10 years - 5-10 mg / kg / day. At a calculated dose of less than 100 mg, 100 mg scored tablets should be used. The recommended dose for children aged 10 to 15 years is 10-20 mg/kg/day. The daily dose of the drug should not exceed 400 mg.
Apurillo is rarely used in pediatric therapy. The exceptions are malignant oncological diseases (especially leukemia) and some enzymatic disorders (for example, Lesch-Nychen syndrome).
Elderly age. For the treatment of such patients, the drug should be used in the minimum dose that provides a sufficient decrease in the concentration of uric acid in the blood serum. Particular attention should be paid to recommendations on the selection of the dose of the drug for patients with impaired renal function.
Kidney dysfunction. In severe renal insufficiency, it is recommended to use Apurill at a dose below 100 mg / day or to use single doses of 100 mg with an interval of more than one day.
Special instructions and precautions
With caution, Apurill should be used for violations of the liver and / or kidneys (in both cases, a dose reduction is necessary), hypofunction of the thyroid gland. In the initial period of the course of therapy, a systematic assessment of liver function indicators is necessary.
During the period of treatment, the daily amount of fluid consumed should be at least 2 liters (under the control of diuresis).
At the beginning of the course of gout treatment, an exacerbation of the disease may occur. For prophylaxis, NSAIDs or colchicine (0.5 mg 3 times / day) can be used. It should be borne in mind that with adequate therapy with Apurill, dissolution of large urate stones in the renal pelvis and their subsequent entry into the ureter is possible.
Asymptomatic hyperuricemia is not an indication for the use of Apurill.
In children, it is used only for malignant neoplasms (especially leukemia), as well as for some enzymatic disorders (Lesch-Nychen syndrome).
To correct hyperuricemia in patients with neoplastic diseases, Apurill is recommended to be used before starting treatment with cytostatics. In such cases, the lowest 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 the urine. With the simultaneous use of allopurinol and cytostatics, more frequent monitoring of the peripheral blood picture is necessary.
During the period of taking the drug, alcohol is not allowed.
Influence on the ability to drive vehicles and mechanisms
Use with caution in patients whose activities require a high concentration of attention and rapid psychomotor reactions.
Use during pregnancy and during breastfeeding
Contraindicated in pregnancy and during breastfeeding .
Interaction with other drugs
With the simultaneous use of allopurinol, it enhances the effect of coumarin anticoagulants, adenine arabinoside, and 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, a myelotoxic effect is more often manifested than with separate use.
With the simultaneous use of allopurinol and azathioprine or mercaptopurine, cumulation of the latter in the body is observed, tk. due to the inhibition of xanthine oxidase activity by allopurinol, which is necessary for the biotransformation of drugs, their metabolism and elimination slows down.
Side effect
The classification of the incidence of side effects is based on an approximate estimate. Their frequency may vary depending on the dose and whether the drug was prescribed as monotherapy or in combination with other drugs.
From the side of the cardiovascular system: arterial hypertension, angina pectoris, bradycardia.
On the part of the digestive system: nausea, vomiting, diarrhea, stomatitis, liver dysfunction (transient increase in transaminases and alkaline phosphatase), hepatitis.
From the side of the central nervous system and peripheral nervous system: weakness, fatigue, headache, dizziness, ataxia, drowsiness, depression, coma, paresis, paresthesia, convulsions, neuropathy, visual impairment, cataracts, macular changes, taste disturbances.
From the urinary system: edema, uremia, hematuria.
From the reproductive system and mammary gland : infertility, impotence, gynecomastia.
From the hemopoietic system: thrombocytopenia, agranulocytosis and aplastic anemia, leukopenia.
From the side of metabolism and nutrition: diabetes mellitus, hyperlipidemia.
Allergic reactions: skin rash, hyperemia, itching, lymphadenopathy, arthralgia, fever, eosinophilia, fever, Stevens-Johnson syndrome, Lyell's syndrome.
Others: furunculosis, alopecia, hair bleaching.
If any of the side effects listed in the instructions get worse, or if you notice any other side effects not listed in the instructions, tell your doctor.
Overdose
Symptoms: nausea, vomiting, diarrhea and dizziness. Severe overdose can lead to significant inhibition of xanthine oxidase activity.
Treatment: The specific antidote for allopurinol is unknown. Adequate hydration, maintaining optimal diuresis, promotes the excretion of allopurinol and its derivatives in the urine. If clinically indicated, hemodialysis is performed.
Storage conditions
Store in a cool and dry place, at a temperature not exceeding 30 0 C.
Keep out of the reach of children.
Best before date
3 years. Do not use after the expiry date stated on the package.
Holiday conditions
Released by prescription.
Release form
10 tablets in an aluminum foil blister. 5 blisters with instructions for use in a cardboard box.