Allopurinol-EGIS - Instructions For Use, Price, Reviews, 100 Mg

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Allopurinol-EGIS

Allopurinol-EGIS: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Allopurinol-EGIS

ATX code: M04AA01

Active ingredient: allopurinol (Allopurinol)

Manufacturer: CJSC "Pharmaceutical Plant" EGIS "(Hungary)

Description and photo updated: 30.11.2018

Prices in pharmacies: from 89 rubles.

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Allopurinol-EGIS is an anti-gout drug that has a hypouricemic effect.

Release form and composition

The drug is available in the form of tablets: grayish-white or white, round, flat, with a chamfer, little or no odor, a dividing line on one side and engraving "E 351" (dosage 100 mg) or "E 352" (dosage 300 mg) to another (dosage 100 mg: 50 pieces in a brown glass bottle, in a cardboard box 1 bottle; dosage 300 mg: 30 pieces in a brown glass bottle, in a cardboard box 1 bottle; each pack also contains instructions for use of Allopurinol-EGIS).

1 tablet contains:

• active ingredient: allopurinol - 100 or 300 mg;
• auxiliary components: dosage 100 mg - povidone K25, lactose monohydrate, magnesium stearate, potato starch, sodium carboxymethyl starch (type A), talc; dosage of 300 mg - gelatin, magnesium stearate, microcrystalline cellulose, anhydrous colloidal silicon dioxide, sodium carboxymethyl starch (type A).

Pharmacological properties

Pharmacodynamics

Allopurinol-EGIS is a drug with anti-gout and hypouricemic action. Its active component is a structural analogue of hypoxanthine. The mechanism of action of the drug is due to the property of allopurinol and oxypurinol, its main active metabolite, to inhibit xanthine oxidase. Xanthine oxidase is an enzyme that is required to convert hypoxanthine to xanthine and xanthine to uric acid.

By helping to reduce the concentration of uric acid in blood serum and urine, allopurinol prevents the deposition of uric acid crystals in tissues, including potentiating their dissolution. Along with the suppression of purine catabolism, in patients with hyperuricemia (not all, only some), a large amount of hypoxanthine and xanthine is involved in the re-formation of purine bases. This causes inhibition of de novo purine biosynthesis by a feedback mechanism, which is mediated by inhibition of the enzyme hypoxanthine-guanine phosphoribosyltransferase.

Pharmacokinetics

After oral administration, allopurinol is rapidly absorbed from the upper gastrointestinal tract. Its activity in oral administration is confirmed by the results of pharmacokinetic studies. In the blood, allopurinol is determined after 0.5-1 hour, and the maximum concentration (C _max) reaches 1.5 hours after administration. The bioavailability of allopurinol ranges from 67 to 90%. After reaching C _{max, the} level of allopurinol decreases rapidly, after 6 hours from the moment of administration in blood plasma it is found only in trace concentrations.

Allopurinol practically does not bind to blood plasma proteins.

The apparent V _d (volume of distribution) is approximately 1.6 L / kg. This indicates a fairly pronounced absorption of the drug by tissues. It is assumed that the highest accumulation of allopurinol and its main active metabolite (oxypurinol) occurs in the intestinal mucosa and liver; it is here that the high activity of xanthine oxidase is recorded.

Biotransformation of allopurinol proceeds under the action of xanthine oxidase and aldehyde oxidase with the formation of a metabolite of oxypurinol, which suppresses the activity of xanthine oxidase. C _{max of} oxypurinol in blood plasma is reached after 3-5 hours. It is characterized by a less pronounced inhibitory activity against xanthine oxidase, but a slower decrease in the level of concentration in the blood and a longer half-life (T _1/2) compared to allopurinol. These properties of oxypurinol cause the preservation of effective suppression of xanthine oxidase activity within 24 hours after taking Allopurinol-EGIS in a single daily dose. With normal renal function, the level of oxypurinol in the blood plasma increases slowly until an equilibrium concentration is reached. After taking 300 mg of allopurinol per day, its plasma concentration is usually in the range of 5 to 10 mg / L.

In addition to oxypurinol, the metabolites of allopurinol are allopurinol-riboside and oxypurinol-7-riboside.

Through the kidneys, 70% of the daily dose of allopurinol is excreted in the form of oxypurinol and about 10% unchanged. The rest (~ 20%) is excreted unchanged through the intestines. T _{1/2 of} allopurinol is 1-2 hours, oxypurinol - from 13 to 30 hours.

In case of impaired renal function, the excretion of the drug is significantly slowed down; with prolonged therapy, this can lead to an increase in the concentration of allopurinol and oxypurinol in the blood plasma. Therefore, in patients with impaired renal function, a reduced dose of allopurinol should be used for treatment. It should be borne in mind that allopurinol and its derivatives are removed from the body during hemodialysis.

For elderly patients, dose adjustment is not required, provided that there is no concomitant renal pathology.

Indications for use

The use of Allopurinol-EGIS is indicated for the suppression of the formation of uric acid and its salts under the following conditions, which may be accompanied by the accumulation of uric acid and its salts:

• idiopathic gout;
• urolithiasis, accompanied by the formation of 2,8-dihydroxyadenine (2,8-DHA) calculi from uric acid due to the decreased activity of adenine phosphoribosyltransferase;
• acute uric acid nephropathy;
• hyperuricemia, the spontaneous occurrence of which is due to tumor diseases and myeloproliferative syndrome with a high rate of cell renewal, or after cytotoxic therapy;
• enzymatic disorders accompanied by overproduction of uric acid salts, including Lesch-Nychen syndrome, decreased activity of hypoxanthine-guanine phosphoribosyltransferase, glucose-6-phosphatase (including glycogenose), adenine phosphoribosyltransferase.

In addition, Allopurinol-EGIS is prescribed to patients with hyperuricosuria for the prevention and treatment of urolithiasis, accompanied by the formation of mixed calcium-oxalate calculi, in which diet and increased fluid intake did not give the desired result.

Contraindications

Absolute:

• acute attack of gout;
• liver failure;
• stage of azotemia of chronic renal failure;
• primary hemochromatosis;
• asymptomatic hyperuricemia;
• period of pregnancy;
• breast-feeding;
• age up to 3 years;
• hypersensitivity to drug components.

In addition, Allopurinol-EGIS 100 mg tablets are contraindicated for patients with hereditary galactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.

It is recommended with caution to prescribe Allopurinol-EGIS in case of liver dysfunction, hypothyroidism, diabetes mellitus, arterial hypertension, concomitant therapy with angiotensin-converting enzyme (ACE) inhibitors, diuretics, in old age.

For children under 15 years of age, the use of the drug is indicated only for the symptomatic treatment of enzyme disorders or during the period of cytostatic therapy of leukemia and other malignant neoplasms.

Allopurinol-EGIS, instructions for use: method and dosage

Allopurinol-EGIS tablets are taken orally, after meals and washed down with plenty of water.

Depending on the dosage regimen, Allopurinol-EGIS tablets 100 mg or 300 mg should be used.

The prescribed dose is taken once a day. In cases where the daily dose is higher than 300 mg or the patient has symptoms of gastrointestinal intolerance, the prescribed dose should be taken in several doses.

Recommended dosage:

• adults: the initial dose is 100 mg once a day. In the absence of sufficient clinical action (if the level of uric acid concentration in the blood serum remains elevated), a gradual increase in the daily dose of the drug is shown until the desired effect is achieved. With a mild course of the disease, the daily dose of Allopurinol-EGIS is usually 100-200 mg, with a moderate course - 300-600 mg, with a severe course - 700-900 mg. When determining the individual dose, the patient's body weight can be taken into account. In this case, the daily dose of allopurinol should be in the range from 2 to 10 mg per 1 kg of patient weight;
• children from 3 to 10 years old: at the rate of 5-10 mg per 1 kg of the child's body weight per day;
• children from 10 to 15 years old: 10–20 mg per 1 kg of body weight per day. The maximum daily dose is 400 mg.

If the prescribed dose is less than 100 mg, then two doses of 50 mg each can be obtained using the separating risks on the tablet.

For the treatment of elderly patients, the minimum effective dose of Allopurinol-EGIS should be used.

Care should be taken when choosing a dose in patients with impaired renal function, especially in the elderly. Increasing the dose of allopurinol should be accompanied by regular monitoring of the serum uric acid concentration at intervals of 7–21 days.

In severe renal failure and other renal pathologies, including impaired renal function due to the development of acute uric acid nephropathy, the dose of allopurinol should not exceed 100 mg once a day or at intervals of more than one day. It is desirable that the dose of Allopurinol-EGIS maintains the level of concentration of oxypurinol in the blood plasma below 100 μmol / l (15.2 mg / l).

If the patient is on hemodialysis with an interval between sessions of 1–3 days, then it is advisable to consider switching to an alternative therapy regimen, which involves taking allopurinol at a dose of 300–400 mg immediately after a hemodialysis session. In this case, Allopurinol-EGIS is not taken between hemodialysis sessions.

In case of impaired renal function, special care should be taken if it is necessary to combine therapy with thiazide diuretics. The lowest effective dose of allopurinol should be used and renal function closely monitored.

For the treatment of patients with impaired liver function, a reduced dose of the drug should be used and laboratory indicators of liver function should be monitored at an early stage of therapy.

In patients with tumor diseases, Lesch-Nyhan syndrome and other conditions accompanied by an increase in the metabolism of uric acid salts, the existing hyperuricemia and (or) hyperuricosuria is corrected before starting therapy with cytotoxic agents using allopurinol. The dose of Allopurinol-EGIS should be in the range of the lower limit of the recommended dosage. It is recommended to carry out adequate hydration, which helps to maintain optimal diuresis, and alkalinization of urine, which increases the solubility of uric acid and its salts.

To adjust the dose of Allopurinol-EGIS, the level of uric acid salts in the blood serum, the concentration of uric acid and urate in urine should be assessed regularly, observing the optimal interval between studies.

Side effects

• infections and parasitic diseases: very rarely - furunculosis;
• from the immune system: infrequently - hypersensitivity reactions; rarely - severe hypersensitivity reactions (skin reactions with epidermal detachment, fever, lymphadenopathy, arthralgia and / or eosinophilia, including Stevens-Johnson syndrome, toxic epidermal necrolysis), concomitant vasculitis / skin reactions, the manifestations of which may be hepatitis, acute cholangitis, kidney damage, xanthine calculi, in quite rare cases - convulsions; very rarely - the development of anaphylactic shock. With drug hypersensitivity syndrome, various combinations of symptoms may appear, such as skin rash, lymphadenopathy, arthralgia, eosinophilia, altered liver test results, hepatosplenomegaly, leukopenia, pseudolymphoma, vasculitis, fever,disappearing bile duct syndrome (these reactions cause drug therapy to be canceled). In patients with impaired renal / hepatic function, there were cases of generalized hypersensitivity reactions (sometimes fatal), very rarely - angioimmunoblastic lymphadenopathy;
• on the part of the blood and lymphatic system: very rarely - leukopenia, leukocytosis, aplastic anemia, agranulocytosis, thrombocytopenia, granulocytosis, eosinophilia and aplasia related to erythrocytes;
• from the heart: very rarely - bradycardia, angina pectoris;
• from the side of the vessels: very rarely - increased blood pressure (BP);
• on the part of metabolism and nutrition: very rarely - hyperlipidemia, diabetes mellitus;
• mental disorders: very rarely - depression;
• on the part of the organ of vision: very rarely - visual impairments, cataracts, macular changes;
• from the organ of hearing and labyrinth disorders: very rarely - dizziness, including vertigo;
• from the nervous system: very rarely - perversion of taste, drowsiness, headache, paresthesia, ataxia, neuropathy, coma, paralysis;
• from the gastrointestinal tract: infrequently - nausea, vomiting, diarrhea; very rarely - stomatitis, recurrent bloody vomiting, changes in the frequency of bowel movements, steatorrhea; frequency not established - abdominal pain;
• from the hepatobiliary system: infrequently - an asymptomatic increase in the level of alkaline phosphatase and the concentration of hepatic transaminases in the blood serum; rarely - hepatitis (including necrotic and granulomatous forms);
• dermatological reactions: often - rash; rarely - toxic epidermal necrolysis, Stevens-Johnson syndrome; very rarely - local drug rash, angioedema, hair discoloration, alopecia;
• from the urinary system: very rarely - uremia, renal failure, hematuria; frequency not established - urolithiasis;
• from the reproductive system and breast: very rarely - erectile dysfunction, male infertility, gynecomastia;
• on the part of the musculoskeletal system and connective tissue: very rarely - myalgia;
• general disorders: very rarely - general weakness, general malaise, edema, fever.

Overdose

Symptoms: nausea, vomiting, dizziness, diarrhea. A significant overdose of allopurinol can cause a pronounced inhibition of xanthine oxidase activity, which, having no obvious manifestations, may affect concomitant therapy with 6-mercaptopurine, azathioprine and other drugs.

Treatment: for the elimination of allopurinol and its derivatives in the urine, it is necessary to carry out appropriate measures to maintain optimal diuresis, including the appointment of hemodialysis in the presence of clinical indications. There is no specific antidote for allopurinol.

special instructions

The frequency of side effects with monotherapy differs from that with the use of Allopurinol-EGIS in combination with other drugs, in addition, it depends on the dose of the drug and the state of kidney and liver function in the patient.

Treatment with allopurinol should be discontinued immediately if delayed multi-organ hypersensitivity reactions (or drug hypersensitivity syndrome) develop and should never be resumed. The manifestation of the syndrome can be a different combination of the following symptoms: skin rash, fever, vasculitis, arthralgia, lymphadenopathy, pseudolymphoma, leukopenia, hepatosplenomegaly, eosinophilia, impaired liver function test results, vanishing bile duct syndrome.

It should be borne in mind that in patients with impaired renal and / or liver function, the development of generalized hypersensitivity reactions can be fatal.

The development of liver dysfunctions can occur without obvious signs of generalized hypersensitivity.

Most often, against the background of the use of allopurinol, adverse reactions from the skin occur, which are usually manifested by itching, maculopapular or scaly rash, purple, in rare cases - exfoliative skin lesions (toxic epidermal necrolysis or Stevens-Johnson syndrome). If skin reactions occur, therapy with allopurinol should be discontinued immediately. If they were mild, then after the disappearance of the symptoms, treatment is resumed with a lower dose of allopurinol, which, if necessary, can be gradually increased. In case of recurrence of skin reactions, further use of allopurinol is contraindicated in the patient.

The manifestation of any reactions of individual intolerance to allopurinol is a clinical diagnosis that requires appropriate decisions.

Angioimmunoblastic lymphadenopathy regresses after discontinuation of therapy with allopurinol.

A relationship was established between the presence of the HGA-B * 5801 allele in the patient and the development of hypersensitivity reactions to allopurinol. Therefore, if it is known that the patient is a carrier of the HGA-B * 5801 allele, then Allopurinol-EGIS should be prescribed only in cases where the expected effect of treatment outweighs the potential risk. In this case, the patient should be informed about the symptoms of the development of hypersensitivity syndrome, toxic epidermal necrolysis and Stevens-Johnson syndrome and the need to immediately stop taking pills at the first signs of their appearance.

In addition to addressing the underlying cause of hyperuricemia, changes in diet and fluid intake should be made to improve patients with asymptomatic hyperuricemia.

An acute attack of gout may occur at the beginning of allopurinol use. To avoid this complication, it is recommended to carry out prophylactic therapy with colchicine or non-steroidal anti-inflammatory drugs (NSAIDs) for at least 30 days before the appointment of Allopurinol-EGIS. With the development of an acute attack of gout during therapy with allopurinol, its administration should be continued at the same dose and an appropriate NSAID should be additionally prescribed.

With malignant neoplasms and appropriate antitumor therapy, Lesch-Nychen syndrome, the formation of uric acid is enhanced, in rare cases this causes a significant increase in the absolute concentration of xanthine in the urine and the deposition of xanthine in the tissues of the urinary tract. To prevent or minimize the likelihood of this complication, the patient should be provided with adequate hydration for optimal dilution of urine.

Against the background of adequate therapy with allopurinol, it is possible to dissolve large stones from uric acid in the renal pelvis, but their wedging into the ureters is unlikely.

Due to the fact that the effect of allopurinol can affect the content and excretion of iron deposited in the liver, patients with hemochromatosis (including their blood relatives) should be prescribed the drug with caution.

Influence on the ability to drive vehicles and complex mechanisms

During the period of taking Allopurinol-EGIS, patients should refuse to drive vehicles and complex mechanisms for a period sufficient to make sure that there are no adverse drug reactions such as drowsiness, dizziness (vertigo), ataxia.

Application during pregnancy and lactation

The use of Allopurinol-EGIS is contraindicated during gestation and breastfeeding.

An exception during pregnancy is when taking the drug poses less threat to the mother and fetus than the disease itself, and there are no less dangerous alternative methods of treatment.

Pediatric use

The use of Allopurinol-EGIS in children under the age of 15 is indicated only for the symptomatic treatment of enzyme disorders or during the period of cytostatic therapy of leukemia and other malignant neoplasms.

The use of tablets for the treatment of children under the age of three is contraindicated.

With impaired renal function

The use of Allopurinol-EGIS is contraindicated for the treatment of patients with chronic renal failure at the stage of azotemia.

In severe renal failure and other renal pathologies, including impaired renal function due to the development of acute uric acid nephropathy, the dose of allopurinol should not exceed 100 mg once a day or at intervals of more than one day. It is desirable that the dose of the drug maintains the level of concentration of oxypurinol in the blood plasma below 100 μmol / l (15.2 mg / l).

If the patient is on hemodialysis, the interval between sessions is 1–3 days, then you should consider switching to a therapy regimen in which allopurinol is taken in a dose of 300–400 mg immediately after a hemodialysis session, and the drug is not taken between hemodialysis sessions.

In case of impaired renal function, special care should be taken if it is necessary to combine therapy with thiazide diuretics. The lowest effective dose of Allopurinol-EGIS should be used and renal function should be closely monitored.

For violations of liver function

The appointment of Allopurinol-EGIS for the treatment of patients with hepatic insufficiency is contraindicated.

It should be used with caution in case of liver dysfunction.

Use in the elderly

Allopurinol-EGIS should be used with caution in elderly patients.

For treatment, the minimum effective dose of the drug should be used.

Drug interactions

• azathioprine, 6-mercaptopurine: if it is necessary to combine therapy with Allopurinol-EGIS, the dose of 6-mercaptopurine or azathioprine should be only ¼ of the usual dose. This is due to the fact that 6-mercaptopurine is inactivated by the enzyme xanthine oxidase, inhibition of xanthine oxidase activity contributes to a significant prolongation of the action of these compounds;
• vidarabine (adenine arabinoside): T1 _{/ 2 of} vidarabine increases, the risk of increased toxic effects increases, therefore, it is recommended to be especially careful with combination therapy;
• probenecid and other uricosuric agents, salicylates in high doses: can contribute to increased excretion of oxypurinol and a decrease in the therapeutic activity of Allopurinol-EGIS;
• chlorpropamide: increases the risk of prolonged hypoglycemia in patients with impaired renal function;
• warfarin and other anticoagulants - coumarin derivatives: increase their activity;
• phenytoin: allopurinol may suppress the oxidation of phenytoin in the liver;
• theophylline: inhibition of theophylline metabolism occurs, therefore, control of its concentration in the blood serum should be carried out both at the beginning of concomitant therapy and with an increase in the dose of allopurinol;
• ampicillin, amoxicillin: contribute to an increase in the risk of developing adverse reactions from the skin, therefore, it is recommended to use other antibiotics;
• bleomycin, cyclophosphamide, doxorubicin, procarbazine, mechlorethamine (cytotoxic agents): in patients with tumor diseases (except leukemia), an increased suppression of bone marrow activity by cytotoxic agents is observed, but their toxic effect when combined with allopurinol is not enhanced;
• cyclosporine: it is necessary to take into account the risk of increased toxicity of cyclosporine associated with an increase in its concentration in blood plasma;
• didanosine: a daily dose of allopurinol 300 mg causes an increase in the C _max in the blood plasma of didanosine by about 2 times, while the T _{1/2 of} didanosine does not change. It is recommended to avoid the combination of these drugs, but if concomitant therapy is clinically justified, the dose of didanosine should be reduced and the patient's condition should be carefully monitored;
• ACE inhibitors: prescribed with caution, as this is associated with an increased risk of leukopenia;
• thiazide diuretics, including hydrochlorothiazide: increase the likelihood of developing hypersensitivity reactions associated with allopurinol, especially with impaired renal function.

Analogs

Allopurinol-EGIS analogues are: Allopurinol, Adenurik, Azuriks, Allupol, Alopron, Purinol, Sanfipurol, etc.

Terms and conditions of storage

Keep out of the reach of children.

Store at temperatures up to 25 ° C.

The shelf life is 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Allopurinol-EGIS

Reviews about Allopurinol-EGIS are mostly positive. Patients point to the effectiveness of the drug in the treatment of gout: pains become much quieter, exacerbations of the disease occur less often. The rapid action of the drug is also noted. In some patients, undesirable phenomena of a different nature appeared. Many people recommend following an appropriate diet and drinking plenty of water at the same time as treatment with Allopurinol-EGIS.

Price for Allopurinol-EGIS in pharmacies

The price of Allopurinol-EGIS for a package containing 50 tablets at a dose of 100 mg can be 89–107 rubles, 30 tablets at a dose of 300 mg - 119–136 rubles.

Allopurinol-EGIS: prices in online pharmacies

Drug name Price Pharmacy

Allopurinol-Egis 100 mg tablets 50 pcs. 89 RUB Buy

Allopurinol-Egis 300 mg tablets 30 pcs. RUB 103 Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!