Allopurinol (Allopurinol)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceAllopurinolAllopurinol
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  • Allopurinol
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    BORSHAGOVSKY HFZ NPC, CJSC     Ukraine
  • Allopurinol
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    ORGANICS, JSC     Russia
  • Allopurinol
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    ORGANICS, JSC     Russia
  • Allopurinol
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    ATOLL, LLC     Russia
  • Allopurinol-Aegis
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    Egis Pharmaceutical Plant OJSC     Hungary
    • Dosage form: & nbsppills
    Composition:

    For one tablet:

    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.

    Description:Tablets of round form white or almost white, with a flat surface, with a facet and a risk.
    Pharmacotherapeutic group:Antifungal agent - xanthine oxidase inhibitor
    ATX: & nbsp

    M.04.A.A   Inhibitors of uric acid synthesis

    Pharmacodynamics:

    Antifungal agent, inhibiting xanthine oxidase, prevents the transition of hypoxanthine to xanthine and the further formation of uric acid from it. Reduces the concentration of uric acid and its salts in body fluids, promotes dissolution of available urate deposits, prevents their formation in tissues and kidneys.Reducing the transformation of hypoxanthine and xanthine, enhances their use for the synthesis of nucleotides and nucleic acids. Accumulation in the plasma of xanthines does not disrupt the normal exchange of nucleic acids, precipitation and precipitation of xanthines in the plasma does not occur (high solubility). Kidney clearance of xanthines is 10 times higher than uric acid clearance, an increase in excretion of xanthines with urine is not accompanied by an increased risk of nephrourolythiasis.

    Pharmacokinetics:

    Allopurinol is rapidly and well absorbed from the gastrointestinal tract (up to 90%). When a single dose of the drug is used, its concentration in plasma reaches a maximum level within 1.5 hours. About 20% of allopurinol and its metabolites are excreted through the intestine, 10 % kidneys. In the liver under the influence of xanthine oxidase allopurinol turns into oxypurinol, which also inhibits the formation of uric acid. T1/2 for allopurinol is 1 to 2 hours, as it is rapidly metabolized to oxypurinol and is intensively excreted by the kidneys due to glomerular filtration. T1/2 for oxypurinol for about 15 hours. In the renal tubules, oxypurinol is actively reabsorbed. Allopurinol and its metabolites do not bind to proteins, being distributed in the tissue fluid. The drug penetrates into breast milk.

    Indications:

    Diseases accompanied by hyperuricemia (treatment and prevention): gout (primary and secondary), urolithiasis (with the formation of urates).

    Hyperuricemia (primary and secondary) that occurs in diseases involving enhanced dissolution of nucleoproteins and increased levels of uric acid in the blood, including the various gematoblastozah (acute leukemia, chronic myeloid leukemia, lymphosarcoma, and others), in cytostatic and radiotherapy of tumors (including number of children), psoriasis, extensive traumatic injuries, due to enzymatic disorders (Lesch-Nichin syndrome), as well as with massive therapy with glucocorticosteroids, when due to intensive dissolution hell tissues significantly increases the number of purines in the blood.

    Urinary acid nephropathy with impaired renal function (renal failure).

    Contraindications:

    Hypersensitivity, liver failure, chronic renal failure (stage of azotemia), primary (idiopathic) hemochromatosis, asymptomatic hyperuricemia, acute attack of gout, pregnancy, lactation.Patients with rare hereditary diseases, such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take the drug.

    Children under 3 years of age are also contraindicated.

    Carefully:

    Chronic renal failure, chronic heart failure, diabetes, arterial hypertension; Children's age (up to 14 years is prescribed only during cytostatic therapy of leukemia and other malignant diseases, as well as symptomatic treatment of enzyme disorders).

    Dosing and Administration:

    Inside. The drug should be taken after meals, washed down with plenty of water. The daily volume of urine should be more than 2 liters, and the urine reaction is neutral or slightly alkaline. A daily dose of more than 300 mg should be divided into several doses.

    Adults the administration of the drug for mild disease is carried out at a daily dose of 100-200 mg; at diseases of average severity - 300 - 600 mg / day; in severe cases, 700-900 mg / day. The dose of the drug is selected individually, the effectiveness of therapy is controlled at the initial stages by re-determining the level of uric acid in the blood (the desired level is less than 0.36 mmol / l).The decrease in the level of uric acid under the influence of the drug occurs after 24 - 48 hours. To reduce the risk of exacerbation of gout, treatment is prescribed from 100 to 300 mg / day, with a daily, if necessary, dose increase of 100 mg / day. To prevent urate nephropathy with antitumor therapy allopurinol appoint a daily dose of 600 - 800 mg and continue treatment with this drug for 2-3 days. With recurrent oxalate kidney stones in patients with hyperuricemia, the dose of the drug is 200-300 mg / day.

    Children the drug is only shown during cytostatic therapy of leukemia and other malignant diseases, as well as symptomatic treatment of enzymatic disorders:

    - from 10 to 15 years appoint 10-20 mg / kg / day or 100 - 400 mg per day,

    - from 3 to 10 years - 5 to 10 mg / kg / day.

    Patients with impaired renal excretion function the daily dose of allopurinol should be reduced.

    Treatment begins with a daily dose of 100 mg, which is increased only when the effectiveness of the drug is inadequate. When determining the dose of the drug, the amount of creatinine clearance is guided:

    Creatinine clearance

    Daily dose of allopurinol

    More than 20 ml / min

    100-300 mg

    10-20 ml / min

    100-200 mg

    Less than 10 ml / min

    100 mg or higher doses at large intervals (eg 1-2 or more days depending on the condition of the patient and the functional capacity of the kidneys)

    The first 6-8 weeks of treatment requires regular examination of the liver function, with blood tests, regular laboratory monitoring is required.

    Side effects:

    From the digestive system: dyspepsia, diarrhea, nausea, vomiting, abdominal pain, stomatitis, hyperbilirubinemia, cholestatic jaundice, increased activity of "liver" transaminases and alkaline phosphatase, rarely - hepatonecrosis, hepatomegaly, granulomatous hepatitis.

    From the side of the cardiovascular system: pericarditis, increased blood pressure, bradycardia, vasculitis.

    From the side of the musculoskeletal system: myopathy, myalgia, arthralgia.

    From the nervous system: headache, peripheral neuropathy, neuritis, paresthesia, paresis of various muscle groups, depression, drowsiness.

    From the sense organs: perversion of taste, loss of taste, visual impairment, cataract, conjunctivitis, toxic damage to the optic nerve.

    From the genitourinary system: acute renal failure, interstitial nephritis, increased urea concentration (in patients with initially decreased renal function), peripheral edema, hematuria, proteinuria, decreased potency, infertility, ginecomastia.

    On the part of the organs of hematopoiesis: agranulocytosis, anemia, aplastic anemia, thrombocytopenia, eosinophilia, leukocytosis, and leukopenia.

    Allergic reactions: skin rash, skin itch, urticaria, multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), purpura, bullous dermatitis, eczematous dermatitis, exfoliative dermatitis, rarely bronchospasm.

    Other: furunculosis, alopecia, diabetes mellitus, dehydration, nasal bleeding, necrotic angina, lymphadenopathy, hyperthermia, hyperlipidemia.

    Overdose:

    The main symptoms: nausea, vomiting, diarrhea and dizziness. Usually no treatment is required if the drug is discontinued and adequate fluid is taken to accelerate the excretion of the drug. In clinical conditions hemodialysis is effective if necessary.

    Interaction:

    Uricosuric medicines increase the renal clearance of the active metabolite of oxypurinol and, as a consequence, may decrease the effectiveness of allopurinol; thiazide diuretics, furosemide, ethacrynic acid and thiophosphamide, pyrazinamide slow the renal clearance of oxypurinol and may increase the toxic effect preparation.

    Strengthens the effect of oral hypoglycemic drugs.

    Increases the concentration in the blood and toxicity (inhibits the metabolism) of azathioprine, mercaptopurine, requiring a reduction in the doses of drugs on 1/3-1/4. Increases the concentration of methotrexate, adenine arabinoside, xanthines (theophylline, aminophylline).

    Colchicine, acetylsalicylic acid increase the effectiveness (salicylates in high doses reduce the effectiveness).

    Lengthens the half-life of indirect anticoagulants of the coumarin series, increases the hypoprothrombinemic effect.

    Ampicillin, amoxicillin increase the incidence of skin rashes; cyclophosphamide, doxorubicin, bleomycin, procarbazine increase the risk of developing bone marrow aplasia.

    When combined with iron-containing preparations, iron can be accumulated in the liver tissues.

    Increased risk of toxicity when combined with angiotensin-converting enzyme inhibitors, especially captopril; This is most clearly manifested in renal failure. Increases the concentration of cyclosporine in the plasma, which increases the risk of nephrotoxicity.

    Special instructions:

    With adequate therapy, it is possible to dissolve large urate stones in the renal pelvis and get them into the ureter. Asymptomatic uricosuria is not an indication for the purpose. If the kidney and liver function is impaired, the dose is reduced. The use of azathioprine or 6-mercaptopurine on the background of allopurinol allows the reduction of their doses 4 times. With caution combine with vidarabinom.

    Form release / dosage:Tablets of 100 mg.
    Packaging:

    10 tablets in a planar cell package; 5 packs per pack of cardboard with instructions for use.

    Storage conditions:

    List B. In a dry, dark place out of the reach of children, at a temperature of no higher than 25 ° C.

    Shelf life:

    5 years. The drug should not be used after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N010930
    Date of registration:30.09.2009 / 18.05.2012
    Expiration Date:Unlimited
    The owner of the registration certificate:BORSHAGOVSKY HFZ NPC, CJSCBORSHAGOVSKY HFZ NPC, CJSC Ukraine
    Manufacturer: & nbsp
    Information update date: & nbsp10.07.2017
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