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Allopurinol

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Allopurinol violates the synthesis of uric acid. It is a structural analogue of hypoxanthine. It inhibits the xanthine oxidase enzyme, which participates in the conversion of hypoxanthine to xanthine and xanthine to uric acid.

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ALLOPURINOL

A drug that violates the synthesis of uric acid. It is a structural analogue of hypoxanthine. It inhibits the xanthine oxidase enzyme, which participates in the conversion of hypoxanthine to xanthine and xanthine to uric acid. This causes a decrease in the concentration of uric acid and its salts in body fluids and urine, which promotes the dissolution of existing urate deposits and prevents their formation in tissues and kidneys. During receiving of allopurinol urinary excretion of hypoxanthine and xanthine is increased.

Allopurinol Indications

  • Treatment and prevention of gout and hyperuricemia of varying origin (including in combination with nephrolithiasis, renal failure, urate nephropathy).
  • Recurrent mixed calcium oxalate kidney stones in the presence of hyperuricosuria.
  • Increased production of urate due to enzyme disorders.
  • Prevention of acute nephropathy during cytostatic and radiation therapy of tumors and leukemia, as well as full medical fasting.

Allopurinol interactions

In case of simultaneous use allopurinol enhances the effect of coumarin anticoagulants, adenine arabinoside, and hypoglycemic drugs (especially in renal insufficiency).

Uricosuric agents and salicylates in high doses reduce the activity of allopurinol.

In case of simultaneous use of allopurinol and cytostatics a myelotoxic effect is manifested more often than in case of separate application.

In case of simultaneous use of allopurinol and azathioprine or mercaptopurine accumulation of the latter ones is observed in the body, because due to the allopurinol-induced inhibition of xanthine oxidase activity, necessary for the biotransformation of drugs, their metabolism and elimination are slowed down.

Allopurinol Pregnancy and lactation

This drug cannot be used during pregnancy and lactation (breastfeeding).

Allopurinol Side effects

Cardiovascular system: in isolated cases - arterial hypertension, bradycardia.

Digestive system: possible dyspeptic symptoms (including nausea, vomiting), diarrhea, transient elevation of transaminases in blood serum; rarely - hepatitis; in isolated cases - stomatitis, abnormal liver function (transient elevation of transaminases and alkaline phosphatase activity), steatorrhea.

CNS and peripheral nervous system: in isolated cases - weakness, fatigue, headache, dizziness, ataxia, drowsiness, depression, coma, pareses, paresthesias, cramps, neuropathies, visual disturbances, cataract, changes in the optic papilla, taste disturbances.

Hematopoietic system: in some cases - thrombocytopenia, agranulocytosis and aplastic anemia, leukopenia (most likely to occur in patients with impaired renal function).

Urinary system: rarely - interstitial nephritis; in isolated cases - edema, uremia, hematuria.

Endocrine system: in isolated cases - infertility, impotence, gynecomastia, diabetes.

Metabolism: in isolated cases - hyperlipidemia.

Allergic reactions: skin rash, hyperemia, itching; in some cases - angioimmunoblastic lymphadenopathy, arthralgia, rise of temperature, eosinophilia, fever, Stevens-Johnson syndrome, Lyell's syndrome.

Dermatological reactions: in isolated cases - furunculosis, alopecia, hair decoloration.

Allopurinol Contraindications

Pronounced liver and/or kidney diseases, pregnancy, lactation, hypersensitivity to allopurinol.

Allopurinol Cautions

Allopurinol should be used with caution in cases of the liver and/or kidney diseases (in both cases reduction of the dose is needed), hypothyroidism. In the initial period of therapy with allopurinol systematic assessment of liver function is necessary.

During treatment with allopurinol daily fluid intake should be at least 2 liters (under the control of diuresis).

At the beginning of treatment of gout disease exacerbation may occur. For prevention of that NSAIDs or colchicine can be used (0.5 mg 3 times per day). One should bear in mind that appropriate therapy with allopurinol can cause possible dissolution of large uric acid stones in the renal pelvis and their subsequent entry into the ureter.

Asymptomatic hyperuricemia is not an indication for the use of allopurinol.

Allopurinol is used in children only in case of malignancies (especially leukemia), and in case of some enzymatic disorders (Lesch–Nyhan syndrome).

For the correction of hyperuricemia in patients with neoplastic diseases allopurinol is recommended to be used before starting treatment with cytostatics. In such cases it is necessary to use the minimal effective dose. In addition, in order to reduce the risk of xanthine deposition in the urinary tract measures should be taken to maintain optimum diuresis and alkalinization of urine. In case of simultaneous use of allopurinol and cytostatics more frequent monitoring of peripheral blood picture is needed.

During treatment with allopurinol alcohol consumption is not allowed.

Effects on the ability to drive and use machines

To be used with caution in patients whose activities require high concentration levels and rapid psychomotor reactions.

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