Allopurinol prescription. Course and duration of treatment. Treatment of gout with allopurinol

Self-medication can be harmful to your health.
It is necessary to consult a doctor, and also read the instructions before use.

Allopurinol: instructions for use

Compound

1 tablet contains 100 mg of allopurinol in terms of 100% dry matter; tablets round shape, white or almost white color, with a flat surface, with a chamfer and risk.

Indications for use

For adults: hyperuricemia (with levels uric acid in blood serum 500 µmol (8.5 mg / 100 ml) and above and not controlled by diet); diseases caused by an increase in the level of uric acid in the blood, especially with gout, urate nephropathy and urate urolithiasis; secondary hyperuricemia various etiologies; primary and secondary hyperuricemia in various hemoblastoses (acute leukemia, chronic myeloid leukemia, lymphosarcoma); cytostatic and radiation therapy of tumors; psoriasis; therapy with glucocorticosteroids.

For children: urate nephropathy caused by leukemia treatment; secondary hyperuricemia (various etiology); congenital enzyme deficiency, in particular the Lesch-Nien syndrome (partial or complete deficiency of hypoxanthine-guanine phosphoribosyltransferase) and congenital deficiency of adenine phosphoribosyltransferase.

Contraindications

Hypersensitivity to allopurinol or to other components of the drug; pronounced violations liver or kidney function; During pregnancy and breastfeeding; childhood up to 3 years. Precautions for use. Before starting treatment with Allopurinol, you should consult your doctor. Do not use the drug for longer than the prescribed period without consulting your doctor. If the signs of the disease do not begin to disappear, or, conversely, the state of health worsens, or undesirable effects appear, it is necessary to stop taking it and seek the advice of a doctor regarding the further use of the drug. In patients with renal insufficiency, if the dose is not reduced, vasculitis may develop with skin changes, then the process can spread to the kidneys and liver. If vasculitis occurs, Allopurinol should be discontinued immediately. Use during pregnancy or lactation. The use of Allopurinol during pregnancy is contraindicated. If necessary, the use of the drug by women who are breastfeeding, breastfeeding should be discontinued.

Children. Allopurinol is not used in children under 3 years of age.

Dosage and administration

Taken orally after meals, without chewing, drinking large quantity water (at least 200 ml). Children aged 3-6 years old are prescribed in a daily dose of 5 mg/kg of body weight, 6-10 years old - 10 mg/kg of body weight. The multiplicity of reception is 3 times a day. For adults and children over 10 years old, the daily dose is determined individually, depending on the level of uric acid in the blood serum. Usually daily dose ranges from 100 - 300 mg / day. If necessary, the initial dose is gradually increased by 100 mg every 1 to 3 weeks until maximum effect. The maintenance dose is usually 200-600 mg/day. In some cases, the dose of the drug can be increased to 600 - 800 mg / day. If the daily dose exceeds 300 mg, it should be divided into 2 to 4 equal doses. Maximum single dose is 300 mg, the maximum daily dose is 800 mg. When increasing the dose, it is necessary to monitor the level of oxypurinol in the blood serum. In patients with renal insufficiency, treatment begins with a daily dose of 100 mg, which is increased only if the drug is not effective enough. When choosing a dose, one should be guided by the value of creatinine clearance:

In patients on hemodialysis, each session of hemodialysis (2-3 times a week) may be accompanied by the use of 300 mg of Allopurinol. For the prevention of hyperuricemia in radiotherapy and chemotherapy of tumors Allopurinol is prescribed at 400 mg / day. The drug should be taken 2-3 days before the start or simultaneously with antiblastoma therapy and continue taking it for several days after the end specific treatment. The duration of treatment depends on the course of the underlying disease. Overdose. Symptoms: nausea, vomiting, diarrhea, dizziness, oliguria. Treatment: forced diuresis, hemodialysis and peritoneal dialysis. In case of overdose, seek immediate medical attention medical care!

Side effect

On the part of metabolic processes: at the beginning of the course of treatment, an acute attack of gout may occur due to the mobilization of uric acid from gouty nodules and other depots. From the side gastrointestinal tract and liver: nausea, vomiting, diarrhea, reversible increase in transaminases and alkaline phosphatase in the blood, hepatitis, stomatitis, acute cholangitis. From the hemopoietic system: leukopenia, leukocytosis, eosinophilia; severe damage bone marrow(thrombocytopenia, agranulocytosis, aplastic anemia), especially in patients with renal insufficiency. From the side of cardio-vascular system: bradycardia, hypertension. From the side of the central nervous system: dizziness, headache, drowsiness, weakness, fatigue, ataxia, depression, convulsions, paresis, paresthesia, neuropathy, peripheral neuritis, myalgia. From the senses: blurred vision, cataracts, impaired taste sensations. From the urinary system: interstitial nephritis With lymphocytic infiltration, uremia, hematuria, xanthogenic stones. Allergic reactions: erythema, urticaria, itching, fever, chills, arthralgia, exudative erythema multiforme, Lyell's syndrome. Others: alopecia, impotence, gynecomastia, diabetes. In patients with renal insufficiency, if the dose is not reduced, vasculitis with skin changes may develop, then the process can spread to the kidneys and liver. If vasculitis occurs, Allopurinol should be discontinued immediately. In cases of adverse effects or other unusual reactions, the patient should consult a doctor regarding the further use of the drug!

Interaction with other drugs

If you are taking any other medications be sure to tell your doctor! The effectiveness of Allopurinol is reduced by the use of drugs with uricosuric action (sulfinpyrazone, probenecid and benzbromarone) and salicylates in high doses. Due to the ability of allopurinol to inhibit xanthine oxidase, the metabolism of purine derivatives such as azathioprine and mercaptopurine slows down, so they usual dose should be reduced by 50 - 75%. Allopurinol in high doses slows down the excretion of probenecid and inhibits the metabolism of theophylline. With the simultaneous use of Allopurinol with chlorpropamide, the dose of chlorpropamide should be reduced. With the simultaneous use of Allopurinol with coumarin-type anticoagulants, their dose should be reduced, and blood coagulation parameters should be monitored more often. With the simultaneous use of Allopurinol with captopril, the risk of skin reactions increases, especially in the presence of chronic kidney failure. The use of Allopurinol with cytostatics leads to more frequent changes blood counts than separate application these medicines, so blood tests should be done more frequently than usual. When using Allopurinol in combination with ampicillin and amoxicillin, the risk of allergic reactions increases.

Allopurinol is an anti-gout drug that inhibits the synthesis of uric acid and its salts in the body. The drug has a specific ability to inhibit the xanthine oxidase enzyme involved in the conversion of hypoxanthine to xanthine and xanthine to uric acid. As a result, the content of urates in the blood plasma decreases and their deposition in tissues and kidneys is prevented.
When using the drug, the excretion of uric acid in the urine decreases and the excretion of more readily soluble hypoxanthine and xanthine increases.
Allopurinol in the body turns into alloxanthin, which also prevents the formation of uric acid, but in terms of activity is inferior to allopurinol.
After oral administration, about 90% of the drug is absorbed into the digestive tract. The maximum concentration of allopurinol in the blood plasma is reached on average after 1.5 hours. The half-life of allopurinol is 1-2 hours, alloxanthin - about 15 hours, so inhibition of xanthine oxidase activity can last for 24 hours after a single dose of the drug. About 20% taken dose excreted in the feces, the rest of the drug and its metabolites - in the urine.

Indications for the use of Allopurinol

Diseases accompanied by hyperuricemia, including primary and secondary gout, urolithiasis (with the formation of urates), primary and secondary hyperuricemia that occurs when pathological processes accompanied by increased breakdown of nucleoproteins and an increase in the content of uric acid in the blood, including various hemoblastomas ( acute leukemia, lymphosarcoma, etc.), conditions with cytostatic and radiation therapy of tumors, psoriasis, massive therapy with corticosteroid drugs. There are data on the use of the drug in complex therapy epilepsy in children (increased serotonin biosynthesis).

The use of the drug Allopurinol

Inside after eating. Doses are set depending on the concentration of uric acid in the blood. Minimum daily therapeutic dose for adults is 0.1 g, the maximum is 0.8 g. Usually, with moderate hyperuricemia (70-100 mg / l), 0.2-0.4 g / day is prescribed 1-2 times a day for 2-3 weeks, then switch to a maintenance dose - 0.2-0.3 g / day in 2-3 doses.
At severe forms gout, significant deposits of urate in the tissues and severe hyperuricemia (over 80-100 mg / l), the drug is prescribed fractionally (not more than 0.2 g per dose) up to 0.6-0.8 g / day for 2-4 weeks, and then they switch to maintenance doses - 0.1-0.3 g / day, which are taken for a long time, for several months.
When using the drug to prevent hyperuricemia during radiation therapy and chemotherapy of tumors, the average daily dose is 0.4 g. The drug is taken 2-3 days before the start of therapy (or simultaneously) and continues to be taken for several more days after the end of specific therapy.
For children under the age of 6 years, the drug is prescribed in a daily dose of 5 mg / kg of body weight; from 6 to 10 years - 10 mg / kg / day. Multiplicity of reception - 3-4 times a day. At complex treatment epilepsy in children, the dose of the drug is 4-5 mg / kg 2 times a day for 10 days; break between repeated courses - 1.5-2 months.
If the time of taking the drug is missed, then take the next dose as soon as possible. If a next move the drug is planned in 12 hours or more, it is necessary to take Allopurinol immediately, and the next dose at the prescribed time. If less than 12 hours are left before taking the next dose, the dose should be skipped and further treatment should be continued as usual.

Contraindications to the use of the drug Allopurinol

Renal failure, pregnancy and lactation, allergy to the components of the drug.

Side effects of Allopurinol

Treatment with Allopurinol is usually well tolerated by patients. With gout, at the beginning of treatment, an exacerbation may occur due to the mobilization of uric acid from gouty nodules and other depots.
In some cases, it is possible:
dyspeptic symptoms - nausea, vomiting, epigastric pain, diarrhea;
allergic reactions - skin rash, itching, hyperemia, rarely - exfoliative dermatitis, fever, arthralgia;
from the blood system - leukopenia, leukocytosis, eosinophilia;
from the side of the central nervous system - neuritis, sleep disturbances, depression, amnesia.

Special instructions for the use of the drug Allopurinol

It should be borne in mind that on the 3rd-4th day after stopping Allopurinol, the indicators of uricosuria and uricemia return to the original, elevated level. Treatment should be long, an interval of more than 2-3 days between doses of the drug is undesirable.
The drug should be used with caution in mild renal failure (adults at a dose of not more than 0.2 g / day). During the use of Allopurinol, diuresis in adult patients should be maintained at a level of at least 2 l / day. It is necessary to ensure a neutral or slightly alkaline urine reaction to prevent the formation of calculi. For this purpose, drugs that alkalize urine are used simultaneously with Allopurinol.
For the prevention of possible seizures at the beginning of treatment gouty arthritis you can prescribe NSAIDs or colchicine (adults 0.5 mg 3 times a day).
At the beginning of treatment with Allopurinol, a systematic study should be carried out functional state kidneys.

Allopurinol drug interactions

In the treatment of hemoblastoma anticancer drugs(methotrexate, mercaptopurine, etc.) it should be taken into account that the simultaneous use of Allopurinol not only inhibits the enzymatic oxidation of these drugs and enhances their antitumor activity, but also significantly increases toxicity. Doses anticancer drugs in such cases should be reduced by 50%.
Under the influence of Allopurinol, it is also possible to enhance the effects (including undesirable) of anticoagulants. indirect action, antipyrine, diphenine, theophylline, since their inactivation in the liver slows down.
With simultaneous use with ampicillin preparations, the risk of a rash on the skin increases.
Under the influence of thiazide diuretics, furosemide, ethacrynic acid, the antihyperuricemic effect of Allopurinol is weakened, since these drugs increase the level of uric acid in the blood plasma.
Allopurinol should not be used in combination with iron-containing drugs due to the possible accumulation of iron in the liver.

Allopurinol overdose, symptoms and treatment

Symptoms: nausea, vomiting, diarrhea, dizziness, oliguria.
Treatment: forced diuresis, hemodialysis and peritoneal dialysis.

Storage conditions of the drug Allopurinol

In a dry, dark place at a temperature not exceeding 25 ° C. Shelf life - 5 years.

List of pharmacies where you can buy Allopurinol:

  • St. Petersburg

In the treatment of chronic nephropathy, stones in the genitourinary system, Allopurinol is prescribed - the instruction for the use of the drug indicates its action in relation to the synthesis of uric acid. Due active composition medicine works effectively, is prescribed by a doctor to eliminate problems with urination. Check out its instructions for use.

Allopurinol tablets

Pharmacological classification classifies Allopurinol as a hypouricemic and anti-gout drug that affects function and function genitourinary system. Action medication based on the work of the active substance allopurinol. It dissolves urate compounds in the urine, prevents the formation of stones in the tissues and kidneys.

Compound

The drug is available in the form of round white tablets with a flat surface, a chamfer and a risk. Their composition is shown in the table:

Pharmacodynamics and pharmacokinetics

Allopurinol refers to drugs that disrupt the synthesis of uric acid. This substance is a structural analogue of hypoxanthine, inhibits the xanthine oxidase enzyme involved in the metabolism of hypoxanthine to xanthine and xanthine to uric acid. Due to this, a decrease in the concentration of uric acid and its salts in the urine and other body fluids is caused. At the same time, existing urate deposits are dissolved, they are not formed in the tissues and kidneys. Taking Allopurinol increases the excretion of hypoxanthine and the excretion of xanthines in the urine.

Once inside, the tablets are 90% absorbed from the stomach. Metabolism occurs with the formation of alloxanthin. The maximum concentration in the blood of the active substance reaches after 1.5 hours, alloxanthin - after 4.5 hours. The half-life of the drug is 1-2 hours, metabolites - 15 hours. 20% of the dose is excreted by the intestines, the remaining 80% - by the kidneys with urine.

Indications for use

The instructions for use indicate the presence of the following indications in which Allopurinol can be prescribed to patients:

  • treatment and prevention of hyperuricemia;
  • a combination of hyperuricemia with nephrolithiasis, renal failure, urate nephropathy;
  • recurrence of mixed oxalate-calcium kidney stones against the background of hyperuricosuria;
  • increased formation of urates in violation of the function of enzymes;
  • prevention of gout, acute nephropathy with cytostatic and radiation therapy of tumors, leukemia, complete therapeutic starvation.

How to take Allopurinol

The dosage of tablets is set individually, according to the instructions. Doctors monitor the concentration of urate and uric acid in the blood and urine. Adults are prescribed 100-900 mg / day, divided into 2-4 times. Tablets should be taken after meals. Children under 15 years of age receive 10-20 mg/kg/day or 100-400 mg/day. The maximum daily dose of Allopurinol for violations of renal clearance is 100 mg / day. The increase in dosage is prescribed by the doctor while maintaining increased concentration urates in blood and urine.

special instructions

Chapter special instructions in the instructions for use, it is worth studying especially closely for all patients taking Allopurinol:

  • the drug is prescribed with caution in case of violations of the function of the kidneys, kidneys, hypofunction thyroid gland, in initial period Allopurinol therapy evaluates indicators of liver function;
  • when treating with medication, patients should consume at least 2 liters of water per day, under control daily diuresis;
  • at the beginning of therapy, an exacerbation of gout is possible, for the prevention of which non-steroidal anti-inflammatory drugs or colchicine are used;
  • at adequate treatment Allopurinol may dissolve large urate stones in the renal pelvis and enter them into the ureter;
  • indication for use is not asymptomatic hyperuricemia;
  • for children, drug treatment is indicated for malignant diseases, leukemia, Lesch-Nychen syndrome;
  • if patients have neoplastic diseases the drug is used before starting treatment with cytostatics, to reduce the risk of xanthine deposition in urinary tract measures are taken to support diuretics and alkaline reaction urine;
  • the drug affects the speed of psychomotor reactions, so driving vehicles and operating mechanisms during the treatment of gout is prohibited.

Allopurinol and alcohol

According to the instructions for the use of Allopurinol, alcohol and alcohol-containing drinks are prohibited throughout the course of drug therapy. The combination of ethanol and active active substance drug leads to toxic poisoning, pernicious influence on the liver and kidneys, increase the risk of drug overdose and the manifestation of negative reactions.

drug interaction

The instructions for use of Allopurinol say about the drug interaction of the drug with other medicines:

  • enhances the effect of doses of anticoagulants of the coumarin type, adenine arabinoside, hypoglycemic agents;
  • when combined with cytostatics, it enhances the myelotoxic effect;
  • uricosuric drugs and high doses of salicylates reduce the effectiveness of the drug;
  • causes an increase in the accumulation of Azathioprine, Mercaptopurine.

Side effects and overdose

The instructions indicate the presence of the following possible side effects when using Allopurinol:

  • arterial hypertension, bradycardia;
  • nausea, vomiting, diarrhea, hepatitis, stomatitis;
  • weakness, fatigue, headaches, dizziness, drowsiness;
  • depression, coma, seizures, impaired vision or taste;
  • anemia, leukopenia, thrombocytopenia;
  • nephritis, edema, uremia, hematuria;
  • infertility, impotence, gynecomastia (breast enlargement), diabetes mellitus;
  • allergic reactions, skin rash, hyperemia, itching, arthralgia, fever, fever;
  • furunculosis, alopecia, hair hypopigmentation.

Overdose with a dose of 20 g in patients may experience nausea, vomiting, diarrhea, dizziness. At long-term use 200-400 mg per day, severe intoxication is observed - skin reactions, hepatitis, fever, exacerbation of renal failure. Treatment is carried out as symptoms appear, doctors show adequate hydration to support diuresis. If necessary, hemodialysis is prescribed, there is no specific antidote.

Contraindications

The use of Allopurinol, according to the instructions, is prohibited in the presence of the following contraindications in patients:

Terms of sale and storage

The shelf life of the drug is five years. The drug is stored at temperatures up to 25 degrees out of light, children. The drug is dispensed from pharmacies by prescription.

Analogues

On the shelves of pharmacies you can find direct analogues of Allopurinol, known as Allopurinol-Egis, Allopurinol Sandoz, Allohexal or Purinol. They are similar in composition active substance. Indirect analogues of the drug, showing the same therapeutic effect are the following medicines:

  • Adenuric;
  • Febux-40;
  • Febux-80.

Allopurinol price

The cost of funds depends on the number of tablets in the package, the accepted trade margin of the enterprise. It will be cheaper to buy the drug on the Internet. Approximate prices for medicines are shown in the table.

Allopurinol: instructions for use and reviews

Latin name: Allopurinol

ATX code: M04AA01

Active substance: allopurinol (allopurinol)

Producer: CJSC NPC "Borshchagovsky CPP" (Ukraine), LLC "Atoll", JSC "Organika" (Russia)

Description and photo update: 26.07.2018

Allopurinol is an anti-gout drug that helps to reduce the concentration of uric acid.

Release form and composition

The drug is available in the form of tablets: round, flat-cylindrical, white or almost white, with a chamfer and a risk (in blister packs of 10, 14, 25 and 30 pieces, in a carton pack 1, 2, 3, 4, 5, 6 , 7, 8, 9 or 10 packs; in cans of 10, 20, 30, 40, 50 and 100 pieces, in a carton pack 1 can).

Composition of 1 tablet:

  • active ingredient: allopurinol - 100 or 300 mg;
  • auxiliary components: lactose monohydrate (milk sugar), magnesium stearate, food gelatin, sodium carboxymethyl starch (primogel), colloidal silicon dioxide (aerosil), microcrystalline cellulose.

Pharmacological properties

Pharmacodynamics

Allopurinol is structural analogue hypoxanthine. This drug, as well as its main pharmacologically active metabolite, oxypurinol, inhibit xanthine oxidase, the enzyme responsible for the transition of xanthine to uric acid and hypoxanthine to xanthine.

Allopurinol reduces the content of uric acid in urine and blood serum, thus ensuring the dissolution of uric acid crystals in tissues and / or preventing their deposition. In addition to inhibition of purine catabolism, in some (but not all) patients with hyperuricemia, large concentrations of hypoxanthine and xanthine are available for re-formation. purine bases. The latter process causes inhibition of de novo purine biosynthesis, which is carried out according to the mechanism feedback, which is caused by the suppression of the activity of the enzyme hypoxanthine-guanine phosphoribosyltransferase.

Pharmacokinetics

When administered orally, the activity of allopurinol is quite high. It is rapidly absorbed from upper divisions GIT. According to the results of pharmacokinetic studies, allopurinol is found in the blood within 30-60 minutes after ingestion. The bioavailability of the substance is 67–90%. The maximum plasma concentration is usually determined approximately 1.5 hours after ingestion, then the level decreases rapidly. 6 hours after ingestion, only a trace concentration of the active substance is recorded in the blood plasma. The maximum concentration of the pharmacologically active metabolite - oxypurinol - is mainly determined 3-5 hours after allopurinol is taken orally. The content of oxypurinol in blood plasma decreases much more slowly.

Allopurinol practically does not bind to plasma proteins, therefore, varying the degree of protein binding should not have a significant effect on drug clearance. The apparent volume of distribution of allopurinol is approximately 1.6 l / kg, which indicates a fairly pronounced absorption of the substance by tissues. The concentration of the drug in various tissues of the body has not been studied, but it is quite possible that allopurinol and oxypurinol in maximum concentrations accumulate in the intestinal mucosa and liver, where it is noted increased activity xanthine oxidase.

Allopurinol is involved in metabolic processes under the action of aldehyde oxidase and xanthine oxidase, resulting in the formation of oxypurinol. The latter inhibits the activity of xanthine oxidase. At the same time, oxypurinol is not such a powerful xanthine oxidase inhibitor as allopurinol itself, but its half-life is significantly longer. This fact explains the fact that a single daily dose of the drug leads to an effective suppression of xanthine oxidase activity, which lasts about 24 hours. In patients with normal function kidneys, the concentration of oxypurinol in the blood plasma gradually increases until an equilibrium concentration is reached. After taking the drug at a daily dose of 300 mg, the content of allopurinol in the blood plasma is usually 5-10 mg / l. Other metabolites of allopurinol include oxypurinol-7-riboside and allopurinol-riboside.

Approximately 20% of allopurinol taken orally is excreted through the intestines unchanged. Approximately 10% of the daily dose is excreted through the glomerular apparatus of the kidneys in the form of allopurinol, which has not undergone biotransformation, 70% of the daily dose of the drug is also excreted through the kidneys in the form of oxypurinol. Oxypurinol is excreted unchanged in the urine, but has a long half-life due to tubular reabsorption. The half-life of allopurinol is 1-2 hours, while this indicator for oxypurinol is in the range of 13-30 hours. Presumably, these significant differences are due to differences in creatinine clearance in patients and/or study design.

In patients with renal dysfunction, the rate of elimination of allopurinol and oxypurinol can be significantly reduced, which during a long course of treatment leads to an increase in the concentration of these substances in the blood plasma. In patients with impaired renal function and creatinine clearance ranging from 10 to 20 ml / min, after long-term therapy with the drug (daily dose was 300 mg), plasma levels of oxypurinol reached approximately 30 mg / l. A similar concentration of oxypurinol can be determined in patients with normal renal function with regular intake of allopurinol at a daily dose of 600 mg. In this regard, in the treatment of patients with kidney dysfunction, it is recommended to reduce the dose of the drug.

In elderly patients, significant changes in the pharmacokinetic parameters of allopurinol are considered unlikely, with the exception of patients with concomitant pathology kidneys.

Indications for use

The drug is prescribed for diseases that are characterized by increased content uric acid (hyperuricemia):

The indication for the use of Allopurinol tablets is primary and secondary hyperuricemia, which develops when:

  • Metabolic disorders of purines and pyrimidines;
  • Acute leukemia;
  • Lymphosarcoma;
  • Chronic myeloid leukemia;
  • Lesch-Nychen syndrome;
  • Psoriasis;
  • extensive injuries;
  • Adverse reactions during treatment with glucocorticoids and their synthetic analogues;
  • Chemotherapy of tumors.

Contraindications

  • Hypersensitivity to the components of the drug;
  • Severe renal and hepatic insufficiency;
  • Pregnancy and lactation.

The drug is not prescribed to children under 15 years of age, except in cases of cytostatic therapy. malignant formations and treatment of severe enzyme disorders.

Instructions for use Allopurinol: method and dosage

Allopurinol tablets should be taken orally after meals. The dosage is set individually and averages 100-900 mg per day for adults and 100-400 mg or 10-20 mg / kg per day for children, depending on the severity of the symptoms of the disease and general condition patient. daily rate the drug should be divided into 2-4 doses.

Side effects

  • From the digestive system: diarrhea, vomiting, nausea, dyspepsia, abdominal pain, increased activity of transaminases in the blood serum, hepatitis, stomatitis;
  • From the side of the cardiovascular system: bradycardia, arterial hypertension;
  • From the side of the central and peripheral nervous system: headaches, weakness, dizziness, drowsiness, convulsions, depression, neuropathy, blurred vision, cataracts;
  • From the genitourinary system: interstitial nephritis, hematuria, edema, uremia;
  • From the hematopoietic system: thrombocytopenia, aplastic anemia, agranulocytosis, leukopenia;
  • From the side endocrine system: impotence, infertility, diabetes mellitus, gynecomastia;
  • Allergic manifestations: rash, itching, hyperemia skin, arthralgia, fever, eosinophilia, Lyell's syndrome, Stevens-Johnson syndrome;
  • Dermatological reactions: alopecia, furunculosis, hair bleaching.

Overdose

Overdose symptoms are dizziness, diarrhea, nausea and vomiting. Severe overdose of the drug can cause significant inhibition of xanthine oxidase activity, however, by itself this effect should not be accompanied negative reactions, except for the effect on concomitant treatment especially on therapy with azathioprine and/or 6-mercaptopurine.

There is no specific antidote. Excretion of the drug and its metabolites in the urine is facilitated by adequate hydration, which maintains normal diuresis. If available clinical indications undergoing hemodialysis.

special instructions

With extreme caution, the drug should be used in persons with impaired renal and hepatic function and with hyperthyroidism.

During the course of treatment, it is necessary to exclude the use of alcohol.

Influence on the ability to drive vehicles and complex mechanisms

During treatment, it is necessary to exercise increased caution when driving vehicles and complex mechanisms.

Use during pregnancy and lactation

On the this moment data on the safety of treatment with Allopurinol during pregnancy are considered insufficient, although this drug has been widely used for many years without obvious negative consequences. Pregnant patients should not take the drug, except in cases where a less dangerous alternative treatment absent, and the disease poses a greater threat to the mother and fetus than taking Allopurinol.

The available research results confirm that allopurinol and oxypurinol are determined in breast milk. In women taking allopurinol at a daily dose of 300 mg, the content of allopurinol and oxypurinol in breast milk was 1.4 mg / ml and 53.7 mg / l, respectively. Data on the effects of allopurinol and its metabolites on pediatric patients breastfeeding are absent, so taking the drug during lactation is contraindicated.

Application in childhood

In children, the drug is used only in case of malignant neoplasms(especially with leukemia), as well as with some violations of enzymatic processes (Lesch-Niechen syndrome).

The dosage regimen in such cases is selected individually, and the treatment process is accompanied by monitoring the concentration of uric acid and urates in the blood and urine.

For impaired renal function

With severe renal failure, the drug is contraindicated.

According to the instructions, Allopurinol is used with caution in patients with impaired renal function (dose reduction is recommended).

For impaired liver function

With severe liver failure, the drug is contraindicated.

The drug is prescribed with caution to patients with liver dysfunctions (dose adjustment is required downward).

drug interaction

Azathioprine is metabolized to form 6-mercaptopurine, the action of which is inactivated by the enzyme xanthine oxidase. In cases where azathioprine or 6-mercaptopurine is combined with allopurinol, patients are advised to prescribe only 1/4 of the recommended dose of azathioprine or 6-mercaptopurine, due to the suppression of xanthine oxidase activity, which increases the duration of action of these compounds.

When allopurinol is combined with vidarabine (adenine arabinoside), the half-life of the latter increases, so special care should be taken regarding the possible increase in the toxic effects of treatment.

Since the main pharmacologically active metabolite of allopurinol is oxypurinol, which is excreted through the kidneys like uric acid salts, drugs with uricosuric activity (salicylates in high concentrations, probenecid), can accelerate the excretion of oxypurinol. In turn, an increase in the rate of excretion of this compound is accompanied by a decrease in the therapeutic activity of allopurinol, however, the clinical significance of this type of interaction is assessed individually in each case.

The combination of chlorpropamide and allopurinol in patients with impaired renal function increases the risk of developing prolonged hypoglycemia, which is explained by the competition between chlorpropamide and allopurinol at the stage of tubular excretion.

When using anticoagulants (coumarin derivatives) together with allopurinol, an increase in the action of the former is observed. Therefore, it is recommended to carefully monitor the condition of patients who are prescribed concomitant therapy with these drugs.

Allopurinol may inhibit the hepatic oxidation of phenytoin, but the clinical significance of this interaction has not been determined.

There is evidence that allopurinol inhibits the metabolism of theophylline. This interaction is explained by the participation of xanthine oxidase in the process of biological transformation of theophylline in the human body. The content of theophylline in the blood serum should be monitored at the beginning of a concomitant course of treatment with allopurinol, as well as with an increase in the dose of the latter.

With the simultaneous use of allopurinol and ampicillin or amoxicillin, patients have an increased incidence of skin reactions compared with patients who have not undergone such concomitant therapy. The reason for this variety drug interaction is not precisely established, and therefore, patients receiving allopurinol are recommended to take other antibacterial drugs.

In patients with diagnosed oncological diseases(except leukemias) taking allopurinol, active suppression of bone marrow function by cyclophosphamide and other cytotoxic drugs (mechlorethamine, doxorubicin, procarbazine, bleomycin) has been reported. However, evidence from controlled studies in patients treated with the above drugs suggests that concomitant treatment with allopurinol did not increase the toxic effects of these cytotoxic drugs.

Some reports state that plasma levels of ciclosporin may increase with concomitant use of allopurinol. When combining these drugs, the risk of increasing the toxicity of cyclosporine should be taken into account.

In both healthy volunteers and HIV-infected patients taking didanosine, concomitant therapy with allopurinol (300 mg daily dose) results in an increase in AUC (area under the concentration-time curve) and a maximum plasma concentration of didanosine of about 2 times. At the same time, the half-life of this substance remains unchanged. In general, the concomitant use of allopurinol and didanosine is not recommended. If concomitant treatment is unavoidable, dose reduction of didanosine and careful monitoring of the patient's condition may be necessary.

The combination of allopurinol and ACE inhibitors may increase the risk of leukopenia, so this combination should be used with caution.

Concomitant use of allopurinol and thiazide diuretics, including hydrochlorothiazide, increases the risk of adverse reactions hypersensitivity associated with allopurinol, especially in patients with renal dysfunction.

Analogues

Analogues of Allopurinol are: Adenurik, Purinol, Allopurinol-Lugal, Allopurinol Sandoz, Allopurinol-Egis.

Terms and conditions of storage

Store protected from impact sunlight place at an air temperature not exceeding 30 ° C.

The shelf life of the drug is 3 years from the date of manufacture.

Allopurinol rarely develops side effects. Predominantly at the beginning of treatment, patients may develop attacks of gout.
When taking the drug Allopurinol the possibility of developing such an undesirable influence cannot be ruled out:
On the blood system: agranulocytosis, thrombocytopenia, aplastic anemia, angioimmunoblastic lymphadenopathy, leukocytosis, leukopenia, eosinophilia.
On the hepatobiliary system: increased activity of liver enzymes, acute cholangitis, xanthine stones, granulomatous hepatitis, liver necrosis.

Metabolism: hyperglycemia, hyperlipidemia.
On the nervous system: depressive states, peripheral neuritis, ataxia, headache, paralysis, neuropathy. In addition, the development of coma, drowsiness and paresthesia is possible.
On the senses: decreased visual acuity, retinal degeneration, cataracts, changes in taste sensations.
On the heart and blood vessels: decrease blood pressure, bradycardia.
On the reproductive system: erectile dysfunction, infertility, gynecomastia.
Allergic reactions: Stevens-Johnson syndrome, urticaria, purpura, exfoliative dermatitis, Lyell's syndrome, vasculitis, epidermal necrolysis, joint pain, chills, anaphylactic shock, angioedema.

Others: sore throat, vomiting with blood, stomatitis, steatorrhea, stool disorders, nausea, alopecia, hair discoloration, furunculosis, myalgia, uremia, hematuria, edema and asthenia.
The risk of side effects is higher in patients with renal and liver failure and in patients receiving ampicillin or amoxicillin.
It should be borne in mind that if there are large urate stones in the renal pelvis when taking allopurinol, they can partially dissolve and enter the ureter or bladder.
With the development of side effects, it is necessary to stop taking Allopurinol and consult a doctor.







Allopurinol does not remove MK! It blocks the production of a new one in the body. And MK is already excreted by the kidneys, some are normal, some are bad. Tophi dissolves the body itself over time, in many people, if the kidneys have time to remove MK. From this principle of these tablets. And I don’t advise young men either ... It hits potency ... I checked it myself ... Well, the kidneys themselves must understand ... There are modern European analogues, fewer side effects, but they cost under 6000 for 28 tablets .. If the body did not quite have time to zasr @ t - it's better to stick to a diet and thump well, very rarely, from the word at all. In short, this is a hell of a disease. Goes under the handle with AG and SD, etc. I’m silent about joint diseases, and so it’s clear. High MK hits the whole body. Yes, and read specialized forums on gout, where people take allopurinol for 10-15 years, they write a lot of interesting things. So ladies and gentlemen...

I take the drug for attacks of gout. After several doses, a positive result is noticeable. The drug does not particularly show side effects, only in some cases a headache or a depressive state may appear. It helps me, so the drug is very good. disease, I recommend, but after visiting the doctor's office.

The drug is really very good, it helps me specifically with gout attacks. But in order to prevent attacks, you also need to follow a strict diet: completely abandon fatty alcohol, but by the way, what I'm telling you who suffers from this disease and so everyone knows perfectly well .Once again I repeat that the drug really has an effective effect.

Blemaren is more expensive, but better, I cleaned my kidneys in a month and a half, otherwise the urologist determined on the table

Not only the drug Allopurinol can not be drunk during an exacerbation of gout, that's all. You need to be treated properly. And not on the forums to look for answers, but to consult a doctor. But in our country, people begin to be treated when they get hot, and then they run around and, as a result, they write what bad medicines. No to go to the doctor, get an examination, if you need to take tests. I am personally very satisfied with Allopurinol. I do not care at least helps.

Do you know why our people are being treated on the forums - because there are no sensible doctors. And while you find this, you have to listen to about 5-10 dumb-headed pieces and each a couple of thousand per appointment and each has his own tests ...
And if you still need to feed your family. No one wants to feed parasites...

I agree with you 100%. This year alone, 66,000 doctors left. And who is left?

God, what kind of doctors are you talking about, you come to ours, but she doesn’t even want to look at you. And one answer; your age. I learn more through social media. networks. And you need to go to your doctors, and not to losers from whom you bought diplomas, although now mostly doctors good times two and counted, good ones have long been in America or Israel, but in Russia it is very difficult to find good doctor, although I live in a megapole

Allopurinol really good drug, but I want to say that it must be taken very carefully, and it is best that the doctor prescribes the dosage and regimen. Don't take it on your own. And if you still decide to take it yourself, without the advice of a doctor, then read the instructions carefully, they are written for a reason. The drug Allopurinol can give to the kidneys, you need to monitor this, plus it can be allergic reaction. It would be best to do a test before taking Allopurinol. Yes, I agree, Allopurinol has many side effects, but at the same time it is effective against gout. O helps to transfer gout much easier.

Similar posts