2010/09/17

Allopurinol-Egis

Composition, structure and packing

Tablets are round, flat, white or grayish-white color.

Tablets are round, flat, white or grayish-white color.

1 tab. allopurinol 300 mg.

Clinico-pharmacological group: drugs affecting the exchange of uric acid.

Arthrifuge drug.

Pharmacological action

Arthrifuge drug. Allopurinol - an inhibitor of xanthine oxidase - an enzyme catalyzing the conversion of hypoxanthine to xanthine and xanthine to uric acid, an end product of purine metabolism in humans. Allopurinol inhibits the oxidation of endogenous purines xanthine oxidase, as a result of the concentration of uric acid in serum and urine decreased, and excretion of xanthine and hypoxanthine in the urine increases.

The drug reduces the content of uric acid in the blood and prevents the deposition of acid and its salts in the tissues and the kidneys.

This drug is effective both in primary (gout), and secondary hyperuricemia.

Pharmacokinetics

Absorption

After oral allopurinol is well and rapidly absorbed into the blood. Cmax of allopurinol in the blood plasma are usually achieved in 1-1.5 h after ingestion.

Distribution

Neither allopurinol nor oksipurinol not bind to plasma proteins and distributed in the tissue fluid.

Metabolism

Allopurinol is rapidly converted to oksipurinol - the active metabolite with a longer T1 / 2 - 15 h. The metabolic conversion of allopurinol under the influence of xanthine oxidase occurs at high speed and the ratio of allopurinol to oksipurinolu in plasma is rapidly changing.

Withdrawal

About 20% of the dose excreted in the feces. Allopurinol excreted mainly in urine. T1 / 2 allopurinol - about 2 hours

Renal clearance of high due to glomerular filtration.

After a 5-7-day oral administration of allopurinol 60-70% of the dose is determined in the urine in the form of oksipurinola. 6-12% is excreted in the urine as unchanged allopurinol. Only a very small portion (about 3% of the dose) is displayed in the form of allopurino-1-ribonucleoside or oksipurino-7-ribonucleosides.

Pharmacokinetics in special clinical situations

In patients with renal insufficiency and uric acid output oksipurinol bad. In gouty nephropathy dose of allopurinol should be reduced in order to maintain an adequate level oksipurinola for inhibiting xanthine oxidase. There are charts for calculating adequate doses of allopurinol in violation clearance oksipurinola.

Statement
gout;
treatment of primary hyperuricemia;
prevention and treatment of urate nephropathy with signs of gout or without them;
treatment of secondary hyperuricemia associated with blood diseases;
prevention and treatment of secondary hyperuricemia which develops during radio-and / or chemotherapy for leukemia, lymphoma and other malignant diseases;
prevention and treatment giperurikozurii.

Dosage regimen

Drugs are taken by mouth after meals, drinking plenty of water. Daily urine volume should be higher than 2 liters, and the reaction of urine - a neutral or slightly alkaline. For adults the initial dose is 100-300 mg 1 time / day.

If necessary, the daily dose can be gradually increased to 100 mg every 1-3 weeks to achieve the desired effect under the control of the content of uric acid in blood serum.

Maintenance dose is usually 200-600 mg / day, but if necessary it can be increased to 800 mg / day. If the daily dose exceeds 300 mg, it should be shared equally by 2-4 single admission.

The prevention of hyperuricemia in tumor therapy for 1-2 days before the beginning Allopurinol-Aegis administered in doses of 600-800 mg daily for 2-3 days.

Maintenance dose of allopurinol depend on the level of uric acid.

Children with secondary hyperuricemia in malignant blood diseases and tumors, as well as changes in enzymatic activity of the drug administered in daily doses at the rate of 10-20 mg / kg body weight. The choice of a daily dose is given the size of the tumor, the number of blast forms in the peripheral blood and bone marrow infiltration.

Side effect
On the part of the digestive system: nausea, vomiting, abdominal pain, diarrhea, rarely - granulomatous hepatitis, transient disturbances of liver function with increased levels of alkaline phosphatase, transaminases, blood.
On the part of the hemopoietic system: possible thrombocytopenia, eosinophilia, leukopenia, leukocytosis, aplastic anemia, hemolytic anemia, reticulocytosis, lymphocytosis.
On the part of metabolism: at the beginning of treatment may develop an acute attack of gout because of the mobilization of uric acid from gouty nodules and other tissue depots.
Since the cardiovascular system: rarely - vasculitis, pericarditis, bradycardia, thrombophlebitis.
From the side of the central nervous system: possible neuritis, sleep disorders, depression, amnesia.
On the part of the organ of vision: can katarkta, conjunctivitis, amblyopia.
On the part of the urinary system: rarely - interstitial nephritis, hematuria, proteinuria, peripheral edema. Allergic reactions: possible rash, fever, rarely - bronchospasm.

Patients with liver disease or kidney may itch, Makulo-papular lesions, purpura, rarely - exfoliative dermatitis, accompanied by fever, lymphadenopathy, arthralgia, and eosinophilia, similar to Stevens-Johnson syndrome and / or Lyell's syndrome.

These reactions require the discontinuation of the drug and treatment with corticosteroids.

Contraindications
severe liver problems;
severe renal dysfunction (azotemia);
Primary (idiopathic) hemochromatosis (or its presence in the family history);
acute attack of gout;
Pregnancy
lactation (breastfeeding);
Hypersensitivity to allopurinol.

Pregnancy and lactation

Allopurinol-Aegis is contraindicated in pregnancy and lactation (breastfeeding).

Cautions

In order to prevent acute attacks of gout, which can be triggered by the use of allopurinol, in addition to it within 1 month from the start of treatment should be prescribed NSAIDs or colchicine.

Elderly patients with hepatic or renal insufficiency the dose should be reduced in connection with an increased risk of intoxication.

In the first 6-8 weeks of treatment, regular liver function tests.

When blood diseases need regular monitoring of the laboratory parameters.

Precautions should be prescribed Allopurinol-Egis along with 6-mercaptopurine, azathioprine, methotrexate, cyclophosphamide, anticoagulants of indirect action, antipyrine, phenytoin, theophylline, hlorpropamidom, sulfinpirazon with iron preparations, thiazide diuretics, furosemide, ethacrynic acid, thiophosphamide.

Overdose

Symptoms: nausea, vomiting, diarrhea.

Treatment: Symptoms of intoxication are reduced by increasing the renal excretion of allopurinol and its metabolites with abundant fluid intake and consequently enhance diuresis. In the clinical setting can be used dialysis.

Drug Interactions
With simultaneous use of allopurinol with anti-Aegis means increased risk of hemopoietic system.
With the simultaneous use of allopurinol-Aegis with 6-mercaptopurine and azathioprine are the oppression of their metabolism and due to this increased toxicity.
With the simultaneous use of allopurinol-Aegis with methotrexate, cyclophosphamide, anticoagulants of indirect action, antipyrine, phenytoin, theophylline may enhance their effects (including side) in connection with the slowing of inactivation in the liver.
At simultaneous application with hlorpropamidom increased risk of persistent hypoglycemia in patients with impaired renal function.
At simultaneous application with sulfinpirazon decreases the effectiveness of allopurinol.
With simultaneous use of allopurinol-Aegis with iron supplementation may be the accumulation of iron in the liver.

Under the influence of thiazide diuretics, furosemide, ethacrynic acid, and thiotepa antigiperurikemicheskoe effects of allopurinol decreases, because These drugs increase levels of uric acid in blood serum.

Terms and Conditions of storage

The drug should be stored under normal conditions at room temperature (15 ° to 25 ° C). Shelf life - 5 years.