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
    pills inwards 
    BORSHAGOVSKY HFZ NPC, CJSC     Ukraine
  • Allopurinol
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    ORGANICS, JSC     Russia
  • Allopurinol
    pills inwards 
    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:Each tablet contains 100 mg of allopurinol, auxiliary substances: sucrose (refined sugar) - 20 mg, potato starch - 77.68 mg, magnesium stearate (magnesium stearic acid) - 1 mg, gelatin of food - 1.32 mg.
    Description:

    Tablets are white or white with a creamy hue of a flat-cylindrical shape with a bevel.

    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 applying a single dose of the drug, its concentration in the plasma reaches a maximum level within 1.5 hours. About 20% of allopurinol and its metabolites are excreted through the intestine, 10% by the kidneys. In the liver under the influence of xanthine oxidase allopurinol turns into oxypurinol, which also inhibits the formation of uric acid. The half-life for allopurinol is 1 -2 hours, because it is rapidly metabolized into oxypurinol and is intensively excreted by the kidneys due to glomerular filtration. The elimination half-life for oxypurinol is about 15 hours. In the renal tubule allopurinol 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), arising from diseases, accompanied by an increased disintegration of nucleoproteins and an increase in the content of uric acid in the blood, incl. at various hematoblastoses (acute leukemia, chronic myeloleukemia, lymphosarcoma, etc.), with cytostatic and radiation therapy of tumors (including in children), psoriasis, extensive traumatic injuries, due to enzymatic disorders (Lesch-Nichin syndrome), as well as with massive therapy with glucocorticosteroids, when the amount of purines in the blood increases significantly as a result of intensive tissue decay.

    Urinary acid nephropathy with impaired renal function (renal failure). Recurrent mixed oxalate-calcium kidney stones (in the presence of uricosuria).

    Contraindications:

    Hypersensitivity, hepatic insufficiency, severe renal failure, primary (idiopathic) hemochromatosis, asymptomatic hyperuricemia, acute attack of gout, pregnancy, lactation.

    Carefully:Chronic renal failure, chronic heart failure, diabetes, arterial hypertension. Children under the age of 14 years (prescribe only during cytostatic therapy of leukemias and other malignant diseases, as well as treatment of enzymatic disorders).
    Pregnancy and lactation:

    Allopurinol during pregnancy should be taken only as prescribed by the doctor and only in the absence of a therapeutic alternative, when the disease presents a greater risk to the fetus and the mother than allopurinol. If you need to use allopurinol during lactation, you should decide whether to stop breastfeeding or refrain from prescribing.

    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 prescription of the drug for mild disease is performed in a daily dose of 100-200 mg, with diseases of moderate 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 in 24-48 hours. To reduce the risk of exacerbation of gout, treatment begins with 100-300 mg / day, with weekly, if necessary, increasing the dose by 100 mg / day. To prevent urate nephropathy with antitumor therapy allopurinol prescribe in 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 hyperuricosemia, the dose of the drug is 200-300 mg / day.

    Children from 10 to 15 years, appoint 10-20 mg / kg / day or 100-400 mg per day, children under 10 years at 5-10 mg / kg / day.

    Patients with impaired renal excretion function the daily dose of allopurinol should be reduced. The first 6-8 weeks of treatment requires regular examination of the liver function, with blood tests, regular laboratory monitoring is required. When CRF it is necessary to start with a daily dose of not more than 100 mg per day with an interval of more than one day, increasing it only with insufficient therapeutic effect.When added to uricosuric drugs, its dose gradually increases, and uricosuric drugs decreases. During treatment, it is necessary to provide daily diuresis of at least 2 liters, maintain the pH of urine at a neutral or slightly alkaline level. When creatinine clearance (CK) is above 20 ml / min, usual doses of allopurinol are prescribed; with CC below 10-20 ml / min daily dose should not exceed 200 mg.

    Side effects:

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

    From the side of the cardiovascular system: pericarditis, increased blood pressure (BP), bradycardia, vasculitis, thrombophlebitis.

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

    From the nervous system: headache, peripheral neuropathy, neuritis, paresthesia, paresis, depression, drowsiness, amnesia.

    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, gynecomastia.

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

    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, 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. Symptomatic therapy is indicated.

    Effective hemodialysis.

    Interaction:

    Urikozuric medicines (LS) increase the renal clearance of the active metabolite oxypurinol, thiazide diuretics slow (increase toxicity). Strengthens the effect of oral hypoglycemic drugs.

    Increases the concentration in the blood and toxicity (inhibits the metabolism) of azathioprine, mercaptopurine, 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, the hypoprothrombinemic effect increases.

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

    When combined with iron 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.

    Thiazide diuretics, furosemide, ethacrynic acid and thiophosphamide, pyrazinamide, uricosuric drugs reduce the anti-hyperuricemic effect.

    Special instructions:

    With adequate therapy, it is possible to dissolve large urate stones in the renal pelvis and get them into the ureters. 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.

    Effect on the ability to drive transp. cf. and fur:

    Allopurinol is used with caution in patients whose activity requires high concentration of attention and rapid psychomotor reactions. The degree of restriction or prohibition on driving and the work with mechanisms the doctor must determine for each patient individually.

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

    For 50 tablets in a can of light-protective glass or 5 contour-cell packs of 10 tablets together with instructions for use in a cardboard bundle.

    Storage conditions:In the dark place at a temperature of no higher than 30 ° C.
    Shelf life:

    5 years.Do not use at the end of the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-001485/08
    Date of registration:14.03.2008 / 02.11.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp10.07.2017
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