Content
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1The drug "Allopurinol reviews of doctors, indications for use, side effects
- 1.1Pharmacological characteristics of the drug
- 1.2Allopurinol: indications for use
- 1.3Features of the drug
- 1.4Contraindications to the appointment of "Allopurinol"
- 1.5Allopurinol: side effects
- 1.6Form release and dosage
- 1.7Poisoning and drug overdose
- 1.8Reviews
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2Allopurinol - instructions for use, indications, composition, side effects, analogues and price
- 2.1Allopurinol tablets
- 2.2Pharmacodynamics and pharmacokinetics
- 2.3Indications for use
- 2.4Special instructions to the host Allopurinol
- 2.5Allopurinol and alcohol
- 2.6Drug Interactions
- 2.7Side effects and overdose
- 2.8Contraindications for use
- 2.9Terms of Sale and Storage
- 2.10Price Allopurinol
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3Allopurinol tablets
- 3.1Clinical and pharmacological group
- 3.2Conditions of leave from pharmacies
- 3.3Price list
- 3.4Form of issue and composition
- 3.5pharmachologic effect
- 3.6Indications for use
- 3.7Contraindications with intolerance
- 3.8Application in pregnancy and lactation
- 3.9Instructions for use Allopurinol
- 3.10Dosing for patients of certain groups
- 3.11Dosing for children
- 3.12Possible side effects
- 3.13special instructions
- 3.14Interaction with other drug groups
- 3.15Analogs similar in composition
- 3.16Terms and conditions of storage
- 4Allopurinol
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5Allopurinol, description and reviews of the drug
- 5.1pharmachologic effect
- 5.2Indications
- 5.3Contraindications to therapy
- 5.4Price
- 5.5Drug analogues
- 5.6Patient Reviews
The drug "Allopurinol reviews of doctors, indications for use, side effects
To date, the drug "Allopurinol" is the basic (basic and pathogenetic reasonable) drug that is used in the complex therapy of such a disease, as gout.
Each person before trying something new, trying to find the maximum useful information about it. Therefore, we propose to understand in more detail when the "Allopurinol" should be used.
The comments of patients and doctors will be presented in our material, and also you will learn what to be afraid of when taking this medication.
Pharmacological characteristics of the drug
"Allopurinol" belongs to the group of antidotal drugs. The main active ingredients are allopurinol and its active metabolite, oxipurinol.
Their pharmacodynamic effects are due to a violation of the synthesis of uric acid with the development of the urostatic effect.
Ultimately, this leads to a decrease in its concentration, followed by dissolution of urate.
Due to its good solubility, "Allopurinol" has a high bioavailability. The drug is well absorbed in the lumen of the small intestine. In the stomach, the systemic blood stream does not enter.
Presence in the blood plasma is observed after half an hour after administration, and the maximum concentration is noted after, hours.
Accordingly, the maximum concentration of the metabolite of allopurinol - oxypurinol, is observed three hours after oral administration.
The drug has a long half-life and is therefore capable of cumulation.
In patients at the beginning of therapy, there is an increase in the concentration of the drug, which stabilizes after one to two weeks of therapy.
Due to the long-term excretion of "Allopurinol" (the doctors' testimonies confirm this), it is not recommended for use by persons with renal insufficiency. In patients with preserved renal excretory function cumulation is not observed.
Allopurinol: indications for use
The opinion of the doctors prescribing this drug claims that its use is most effective and justified in cases of hyperuricemia (increased uric acid content per unit of blood volume) with:
- gouty arthritis (gout);
- urate diseases of the genitourinary tract (nephropathy, urolithiasis);
- oncological diseases of blood;
- congenital anomalies of the enzymatic system.
In some cases, it is possible to administer the drug to children for treatment of urate nephropathy, which arose on the background of therapy leukemia, with congenital diseases associated with impaired uric acid metabolism, secondary hyperuricemia of various origin.
Features of the drug
Tablets "Allopurinol" (reviews warned about strict adherence to recommendations when taking medication) are taken after food, they can not be chewed in any way, but on the contrary, they are drunk entirely and washed down with at least a glass of warm water.
People who take this medicine should always monitor their diet, and in cases inaccuracies in the diet must adjust its dosage, but only under the control of its treating specialist.
The necessary dose of the drug "Allopurinol" is determined depending on the content of uric acid in the bloodstream.
As a rule, it is from 100 to 300 mg per one dose of the drug "Allopurinol".
Reviews of patients and doctors regarding this dosing are positive, since the medicine is taken only once a day.
Gout therapy begins with the appointment of 100 mg of the drug once a day.
In the case of insufficient efficiency and a weak decrease in the level of uric acid, the dosage is gradually increased (by 100 mg every two to three weeks), leading to an effective therapeutic under laboratory control of urinary acid.
In such cases, the average dosage and further maintenance dose is 200 to 400 mg, but in certain situations the dose of the drug may be up to 800 mg. In this case, it is broken several times a day.
When appointing the drug to patients with renal insufficiency, it is necessary to focus on the clearance of creatinine.
Contraindications to the appointment of "Allopurinol"
The drug is contraindicated for patients with severe kidney failure, as well as pregnant and lactating.
It is also not recommended to prescribe this drug to patients who have allergic reactions or hypersensitivity to one or several components of the drug.
It is forbidden to use the drug in people who have borderline uric acid in the blood plasma, as its reduction can be successfully achieved by adjusting the diet.
Allopurinol: side effects
Feedback from patients who used this drug for the first time indicate that enough often an exacerbation of the disease and an increase in gout symptoms with the emergence of so-called attacks.
But this phenomenon is short-lived, and one should not fear it enough to stop therapy.
But in cases of occurrence of any rashes, uncomfortable sensations or earlier missing symptoms, you should immediately inform the doctor about it.
In this case, the reception of "Allopurinol" should be stopped immediately, and as the symptomatology disappears, the specialist can again prescribe the drug, but at a lower dosage (starting from 50 mg). Reception should be conducted under the careful supervision of the attending physician and in conditions of separation.
Among the adverse reactions from the nervous system and higher mental functions, depression may occur. On the part of the hemopoietic system, there is rarely a development of oppression of bone marrow function with the emergence of thrombocytopenia, aplastic anemia.
When taking the drug may develop metabolic disorders in the form of diabetes, increasing levels of fatty acids in blood plasma.
From the side of the cardiovascular system, it is possible to develop arterial hypertension, bradycardia.
The incidence of adverse reactions to this drug is increased if the patient has renal failure.
Form release and dosage
"Allopurinol" is available in tablet form (30 or 50 pcs. Each). in the package) at a dosage of 100 and 300 mg of the active ingredient in one tablet.
In the domestic market there is "Allopurinol Sandoz 300".
Reviews about it are positive, since the drug in this dosage is prescribed only once a day, which practically negates the possibility of missing the medication.
Poisoning and drug overdose
Poisoning is extremely rare, but there are cases of a single intake of 20 grams of the drug. The following symptoms were observed: dizziness, vomiting, nausea, diarrhea.
With renal insufficiency and prolonged administration of large doses of the drug, severe symptoms of intoxication in the form of fever, hepatitis, and acute renal failure were noted.
Therapy of acute poisoning and overdose is symptomatic, aimed at accelerating the removal of the drug from the body. There is no specific antidote. To speedily remove the drug from the body, dialysis is effective.
Reviews
Given the fact that the period of accumulation of a given drug substance in the blood (in sufficient concentration to provide therapeutic action) is an average of one week, patients suffering from gout should practically lifelong apply Allopurinol. The comments of the doctors are unambiguous: the drug has proved itself well. But this is not a "miracle pill which you can drink and forget about the disease. Gout is rather a way of life, not a chronic disease. But it is "Allopurinol" that helps to control the level of lactic acid and prevent the aggravation of the disease and its further progression.
From the point of view of the convenience of prescribing the drug "Allopurinol the doctors' reviews are also positive, because the patient in most cases needs to take the medicine once a day. This minimizes the likelihood of missing the medication and, consequently, improves the effectiveness of the therapy.
Conclusion
Thus, the main cure for gout is "Allopurinol."
Feedback from experts and patients taking this drug is positive, and this again confirms the effectiveness of the drug in the treatment of gout and impaired uric acid metabolism.
Thanks to the use of this drug, a huge number of patients gain the hope of reducing the complications of diabetes.
A source: http://.ru/article/220517/preparat-allopurinol-otzyivyi-vrachey-pokazaniya-k-primeneniyu-pobochnyie-deystviya
Allopurinol - instructions for use, indications, composition, side effects, analogues and price
In the treatment of chronic nephropathy, stones in the genitourinary system is prescribed Allopurinol - the instruction for the use of medication indicates its effect on the synthesis of uric acid. Due to the active composition, the drug acts effectively, is appointed by the doctor to eliminate problems with urination. Read its instructions for use.
Allopurinol tablets
Pharmacological classification refers the drug Allopurinol to hypo-uricemic and antidotal drugs, acting on the functions and work of the genitourinary system.
The action of the drug is based on the work of the active substance allopurinol. It dissolves urate compounds in the urine, does not allow the formation of stones in tissues and kidneys.
The preparation is available in the form of tablets of round shape in white with a flat surface, facet and risk. Their composition is indicated in the table:
Concentration of allopurinol, mg per 1 pc. | 100 or 300 |
Additional components | Microcrystalline cellulose, corn starch, magnesium stearate, lactose, hypromellose |
Packaging | For 10 pieces in a blister, for 30 or 50 pieces in a cardboard bundle |
Pharmacodynamics and pharmacokinetics
Allopurinol refers to drugs that interfere with the synthesis of uric acid. This substance is a structural analogue of hypoxanthine, inhibits the enzyme xanthine oxidase, which participates in the metabolism of hypoxanthine to xanthine and xanthine to uric acid.
Due to this, the concentration of uric acid and its salts in the urine and other body fluids is reduced. At the same time, already existing deposits of urate are dissolved, they are not formed in tissues and kidneys.
Taking Allopurinol increases the release of hypoxanthine and excretion of xanthines with urine.
Getting inside, the tablets are absorbed 90% from the stomach. Metabolism occurs with the formation of alloxanthin.
The maximum concentration in the blood of the active substance reaches in, hours, alloxanthin - after, hours.
The half-life of the drug is 1-2 hours, metabolites - 15 hours. 20% of the dose is excreted by the intestine, 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 administered to patients:
- treatment and prevention of hyperuricemia;
- combination of hyperuricemia with nephrolithiasis, renal insufficiency, urate nephropathy;
- relapse of mixed oxalate-calcium kidney stones against the background of hyperuricosuria;
- increased urate formation when the enzyme function is disturbed;
- prevention of gout, acute nephropathy in cytostatic and radiation therapy of tumors, leukemia, complete medical starvation.
The dosage of tablets is set individually, according to the instructions. Doctors control the concentration of urate and uric acid in the blood and urine. Adults are assigned 100-900 mg / day, divided 2-4 times. Tablets should be drunk after eating.
Children under the age of 15 years 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 a high concentration of urate in the blood and urine.
Special instructions to the host Allopurinol
The section of special instructions in the instructions for use should be studied especially closely for all patients taking Allopurinol:
- the drug is administered with caution in cases of impaired renal function, kidney function, hypothyroidism of the thyroid gland; during the initial period of therapy with Allopurinol, liver function parameters are evaluated;
- when treating the drug, patients should consume at least 2 liters of water per day, under the control of daily diuresis;
- at the beginning of therapy, an exacerbation of gout may be possible, for the prevention of which non-steroidal anti-inflammatory drugs or colchicine are used;
- with adequate treatment with Allopurinol, it is possible to dissolve large urate stones in the renal pelvis and get them into the ureter;
- the indication to use is not asymptomatic hyperuricemia;
- for children, treatment with medication is indicated for malignant diseases, leukemia, Lesch-Nichin syndrome;
- in the presence of tumor diseases in the patient, the agent is used before the start of treatment with cytostatics, for reduction of risk of xanthine deposition in the urinary tract, measures are taken to support diuretics and alkaline urine reactions;
- the drug affects the speed of psychomotor reactions, so driving and handling 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 banned throughout the treatment of the drug.
The combination of ethanol and the active ingredient of the drug leads to toxic poisoning, influence on the liver and kidneys, increased risk of drug overdose and negative reactions.
Drug Interactions
In the instruction on the use of Allopurinol it is said about drug interaction of the drug with other medicines:
- strengthens the effect of doses of anticoagulants coumarin type, adenine arabinoside, hypoglycemic agents;
- when combined with cytostatics enhances myelotoxic effect;
- Urikozuric drugs and high doses of salicylates reduce the effectiveness of the medication;
- causes an increase in the cumulation of Azathioprine, Mercaptopurine.
Side effects and overdose
The instructions indicate the presence of the following possible side effects when applying Allopurinol:
- arterial hypertension, bradycardia;
- nausea, vomiting, diarrhea, hepatitis, stomatitis;
- weakness, increased fatigue, headaches, dizziness, drowsiness;
- depression, coma, convulsions, impaired vision or taste;
- anemia, leukopenia, thrombocytopenia;
- nephritis, edema, uremia, hematuria;
- infertility, impotence, gynecomastia (enlargement of mammary glands), diabetes mellitus;
- allergic reactions, skin rash, hyperemia, itching, arthralgia, fever, fever;
- furunculosis, alopecia, hypopigmentation of hair.
Overdose of a dose of 20 g in patients may manifest nausea, vomiting, diarrhea, dizziness.
With prolonged intake of 200-400 mg per day, severe intoxication is observed - skin reactions, hepatitis, fever, exacerbation of renal insufficiency.
Treatment is carried out in process of display of signs, doctors show adequate hydration for support of diuresis. If necessary, hemodialysis is prescribed, there is no specific antidote.
Contraindications for use
The use of allopurinol, according to the instructions, is banned in the presence of the following contraindications in patients:
- expressed violations of the liver, kidneys, their insufficiency;
- pregnancy, the period of breastfeeding;
- hypersensitivity to the constituent components of the drug;
- acute attacks of gout;
- childhood.
Terms of Sale and Storage
Shelf life of the drug is five years. The drug is stored at a temperature of up to 25 degrees outside the access of light, children. The drug is dispensed from pharmacies on prescription.
Analogues
On the shelves of pharmacies you can find direct analogs of Allopurinol, known under the names Allopurinol-Aegis, Allopurinol Sandoz, Allogexal or Purinol.
They are similar in composition, active substance.
Indirect analogues of the drug, showing the same therapeutic effect, are the following medicines:
- Adenurik;
- Phoebus-40;
- Phoebus-80.
Price Allopurinol
The cost of funds depends on the number of tablets in the package, the accepted trade mark-up of the enterprise. On the Internet, buy the drug will be cheaper. Approximate prices for medicines are indicated in the table:
Name, characteristics | Internet price, rubles | Pharmacy price, rubles |
Tablets 100 mg 50 pcs. | 91 | 100 |
Egis 100 mg 50 pcs. | 106 | 120 |
Egis 300 mg 30 pcs. | 139 | 150 |
Tablets 300 mg 30 pcs. | 97 | 104 |
A source: http://vrachmedik.ru/676-allopurinol-instrukciya-po-primeneniyu.html
Allopurinol tablets
Allopurinol is used to treat gout.
It reduces the rate of synthesis of lactic acid, thereby reducing the severity of the symptoms of the disease and preventing exacerbation. Medical research in clinical conditions has proved a positive effect in the treatment of gout, especially the root causes of its occurrence.
On this page you will find all information about the Allopurinol: the full instructions for use for this medicine medium, average prices in pharmacies, complete and incomplete analogs of the drug, as well as reviews of people who have already applied Allopurinol. Want to leave your opinion? Please write in the comments.
Clinical and pharmacological group
The drug belongs to the pharmacological group of xanthine oxidase inhibitors. Antifungal drug.
Conditions of leave from pharmacies
The drug is released by prescription.
Price list
How much is Allopurinol? The average price in pharmacies is at the level of 100 rubles.
Form of issue and composition
The preparation is available in the form of tablets of round shape in white with a flat surface, facet and risk.
Their composition is indicated in the table:
Concentration of allopurinol, mg per 1 pc. | 100 or 300 |
Additional components | Microcrystalline cellulose, corn starch, magnesium stearate, lactose, hypromellose |
Packaging | For 10 pieces in a blister, for 30 or 50 pieces in a cardboard bundle |
pharmachologic effect
The main action is a decrease in the synthesis of uric acid in the human body. Uric acid is the result of the metabolism of foods containing purines.
When the formation of uric acid is excessive, or the excretory system does not cope with its excretion, the uric acid content in the blood will increase.
When supersaturation will be formed urate - crystals of uric acid, which can cause the formation of stones in the bladder, kidneys or deposited in the joints.
So there are characteristic signs of gouty arthritis (gout): joint inflammation, swelling, pain, redness, mobility restriction, fever.
That is why it is so important to control the level of uric acid, and not to exceed the norm.
When taking allopurinol, the activity of a special enzyme that promotes the formation of uric acid is inhibited. The drug reduces the synthesis of uric acid, and accelerates the dissolution of already deposited urate salts.
Indications for use
The main indications for the use of Allopurinol tablets are the following:
- Gout;
- Psoriasis;
- In the complex treatment of acute leukemia;
- In the complex treatment of lymphosarcoma;
- Disorders of metabolic processes in the body, namely purines and pyrimidines;
- As part of complex therapy for acute and chronic myeloid leukemia;
- Numerous injuries and pathologies of the motor apparatus, which can lead to numerous violations of metabolic processes in the body;
- Side effects that develop in the patient as a result of prolonged or uncontrolled treatment with glucocorticoids or their analogues of synthetic origin;
- An increased concentration of uric acid in the blood serum - this condition is checked by means of blood tests that are given up on an empty stomach;
- Identified stones and sand in the urinary tract and kidneys - the drug is shown only if the stone does not overlap the ureter, and its size does not exceed 2 mm in diameter;
- After the passed course of chemotherapy of cancers in order to prevent the formation of urate stones in the organs of urination.
Contraindications with intolerance
The use of allopurinol is contraindicated in people with intolerance to the active ingredient or the auxiliary components of the drug.
Other contraindications are severe violations of liver function, renal failure with creatinine clearance less than 2 ml / min, age up to 15 years.
Allopurinol is not prescribed in cases where the level of uric acid in the plasma can be regulated by diet.
With caution, the drug is prescribed for patients with hematopoietic disorders, with hepatic and renal insufficiency.
Also with arterial hypertension and heart failure, when the patient is treated with angiotensin-converting enzyme inhibitors and diuretics.
Allopurinol is not prescribed to people suffering from acute gout attacks, the drug can be treated only when the patient's condition improves.
Application in pregnancy and lactation
Studies of allopurinol in pregnant women have not been conducted, use of the drug during pregnancy is not recommended.
Allopurinol is found in breast milk. Taking the drug Allopurinol during lactation is undesirable.
Instructions for use Allopurinol
The instructions for use indicate that Allopurinol tablets are intended for oral administration. They are recommended to swallow without chewing, drinking with a lot of drinking water. It is advisable to take Allopurinol after meals.
When taking the drug Allopurinol, you must use a large amount of fluid to maintain normal diuresis, if necessary, alkalinization of urine can also be carried out (in this case, excretion of urinary acid).
The average maintenance dose is 200-600 mg of allopurinol per day. In some cases, high-dose treatment (600-800 mg of allopurinol per day) may be required.
If the daily dose of the drug Allopurinol exceeds 300 mg it should be divided into several receptions (not more than 300 mg of allopurinol per reception).
With an increase in the dose of allopurinol, the level of the main metabolite in the blood (oxypurinol), which should not exceed 15 μg / ml (100 μmol), should also be monitored.
The maximum daily dose of allopurinol is 800 mg.
Dosing for patients of certain groups
Patients with renal insufficiency, allopurinol is prescribed in an initial dose of 100 mg per day.
The effectiveness of the drug is determined depending on the level of uric acid in the plasma 1-3 weeks after the start of treatment.
If the effectiveness of the drug Allopurinol is not enough - the dose is gradually increased (with careful monitoring of the level of oxypurinol in the plasma).
- Patients with a creatinine clearance greater than 20 mL / min should not be prescribed more than 300 mg of allopurinol per day.
- Patients with a creatinine clearance of 10-20 ml / min should not be prescribed more than 200 mg of allopurinol per day.
- Patients with a creatinine clearance of less than 10 ml / min should be prescribed allopurinol at a dose of 100 mg per day.
If necessary, increase the dose, increasing the intervals between allopurinol (100-300 mg every 48-72 hours).
Patients on hemodialysis are prescribed 300-400 mg of allopurinol after each dialysis session (2-3 times per week).
In the treatment of urolithiasis and gout, daily diuresis should be at least 2 liters.
Dosing for children
The daily dose of allopurinol for children is calculated by the formula 10-20 mg / kg of weight.
The received dose should be divided into 3 doses. The maximum daily dose of allopurinol for children older than 15 years is 400 mg.
Possible side effects
The drug is easily tolerated and usually does not have side effects, however, in rare cases, the following unwanted side effects may develop:
- Central nervous system: development of depressive conditions, headache, neuropathy.
- Cardiovascular system: high blood pressure, the probability of bradycardia, anemia, vasculitis, leukocytosis, leukopenia.
- Gastrointestinal tract: development of dyspeptic disorders (nausea, vomiting, abdominal pain, diarrhea); stomatitis.
- Genitourinary system: development of acute renal failure, the formation of peripheral edema, weakening of potency.
- Development of allergic reactions. Allopurinol can cause the formation of skin rash, itching, urticaria, multiforme exudative erythema, toxic epidermal necrolysis, purpura, bullous dermatitis. In rare cases, the development of bronchospasm is possible.
When observing these symptoms, it is necessary to stop using the drug and consult a doctor.
special instructions
At the beginning of the course of treatment of gout, there may be an exacerbation of the disease. For prevention, you can use NSAIDs or colchicine (0.5 mg 3 times / day).
It should be taken into account that with adequate therapy with allopurinol, it is possible to dissolve large urate stones in the renal pelvis and subsequently to enter the ureter.
With caution should use allopurinol for violations of the liver and / or kidney function (in both cases, a dose reduction is necessary), hypothyroidism of the thyroid gland.
In the initial period of the course of therapy with allopurinol, systematic evaluation of liver function parameters is necessary.
During the treatment with allopurinol, the daily amount of fluid consumed should be at least 2 liters (under the control of diuresis).
Asymptomatic hyperuricemia is not an indication for the use of allopurinol. Children are only used for malignant neoplasms (especially leukemia), also for certain enzymatic disorders (Lesch-Nian syndrome).
For the correction of hyperuricemia in patients with tumorous diseases, it is recommended that allopurinol be used before treatment with cytostatics. In such cases, the minimum effective dose should be used.
In addition, in order to reduce the risk of xanthine deposition in the urinary tract, measures should be taken to maintain optimal diuresis and urine alkalinization.
With the simultaneous use of allopurinol and cytostatics, more frequent monitoring of the peripheral blood pattern is necessary.
During the reception of allopurinol, do not drink alcohol.
Interaction with other drug groups
The drug can promote an increase in the content of cyclosporine in the blood plasma, which can lead to the development of nephrotoxicity.
When used simultaneously with furosemide, ethacrynic acid, thiophosphamide, preparations of the group of thiazide diuretics, a decrease in the pharmacological effect of Allopurinol is possible. The combination with vydabarine should be carried out with extreme caution and under the supervision of the attending physician.
Simultaneous use with ampicillin and amoxicillin may increase the risk of allergic reactions.
Analogs similar in composition
On the shelves of pharmacies you can find direct analogs of Allopurinol, known under the names Allopurinol-Aegis, Allopurinol Sandoz, Allogexal or Purinol. They are similar in composition, active substance.
Indirect analogues of the drug, showing the same therapeutic effect, are the following medicines:
- Adenurik;
- Phoebus-40;
- Phoebus-80.
Before using analogues, consult your doctor.
Terms and conditions of storage
Store in a place protected from light and inaccessible to children at a temperature of no higher than 30 ° C. Shelf life of tablets 100 mg - 5 years, 300 mg - 3 years.
A source: http://simptomy-lechenie.net/tabletki-allopurinol/
Allopurinol
Name:Allopurinol
Name:Allopurinolum (Allopurinolum)
Indications for use:
Diseases accompanied by hyperuricemia (treatment and prevention): gout (primary and secondary), nephrolithiasis (with the formation of urates).
Hyperuricemia (primary and secondary) that occurs in diseases accompanied by increased disintegration of nucleoproteins and an increase in the content of uric acid in the blood, incl.
with various hematoblastomas (acute leukemia, chronic myelogenous leukemia, lymphosarcoma, etc.), with cytostatic and radiation therapy of tumors (incl.
in babies), psoriasis, extensive traumatic injuries, due to enzymatic disorders (Lesch-Niehen syndrome), also with massive therapy of SCS, when, due to the intensive decay of tissues, the amount of purines in blood.
Violations of purine metabolism in babies. Urinary acid nephropathy with impaired renal function (renal failure). Recurrent mixed oxalate-calcium kidney stones (in the presence of uricosuria).
Pharmachologic effect:
Anti-arthritis agent. Pharmacodynamics. Allopurinol-EGIS is an inhibitor of xanthine oxidase, an enzyme catalyzing conversion hypoxanthine to xanthine and xanthine to uric acid, which is the final product of purine metabolism in rights.
Allopurinol inhibits the oxidation of endogenous purines with xanthine oxidase, resulting in a concentration uric acid in the serum and urine decreases, and the excretion of xanthine and hypoxanthine in the urine increases.
The drug lowers the urate content in the blood serum and prevents their deposition in tissues and kidneys. Due to this, the product is effective both in primary (gout) and secondary (associated with tumors) hyperuricemia.
The decrease in uric acid production depends on the dose of allopurinol. Pharmacokinetics. After ingestion, allopurinol is well and rapidly absorbed into the blood. The peak values of its concentration in the plasma in humans are usually observed after 1 - 1 hours after the reception.
Approximately 20% of the dose taken is excreted with feces. Allopurinol is excreted from the body mainly with urine.
It has a very short half-life (within 2 hours), since it has a high renal clearance due to the glomerular filtration and, in addition, rapidly turns into oxypurinol, an active metabolite with a longer half-life (~ 15 hours).
Metabolic conversion of allopurinol under the influence of xanthine oxidase occurs at a high rate, and the ratio of allopurinol to oxypurinol in plasma changes rapidly. Neither allopurinol nor oxypurinol binds to plasma proteins and is distributed in the tissue fluid.
In patients with renal insufficiency, uric acid and oxypurinol are poorly isolated. In gouty nephropathy, the dose of allopurinol should be reduced in order to maintain an adequate level of oxypurinol to inhibit xanthine oxidase.
There are nomograms for the calculation of adequate doses of allopurinol in violation of the clearance of oxypurinol. After 5-7-day oral administration of allopurinol, 60-70% of the dose is detected in the urine in the form of oxypurinol, 6-12% is excreted in the urine as unchanged allopurinol. Only a very small part (within 3% of the dose) is released as allopurinol-1-ribonucleoside or oxypurinol-7-ribonucleoside.
Allopurinol route of administration and dose:
Take allopurinol inside (after eating). Doses are set depending on the content of uric acid in the blood. The minimum therapeutic dose, g per day, the largest g.
Usually, with moderate (up to 10 mg%) hyperuricemia take on, g per day for 2 to 3 weeks, then go to the maintenance dose, g per day (in 2 to 3 doses).
In severe cases of gout, with significant deposition of urate in tissues and high hyperuricemia (above 7 mg%), it is prescribed up to, g fractional (not more than, g at the reception) for 2 to 4 weeks, then go on maintenance doses (, g every day), which give a long time (for several months).
When discontinuing allopurinol, uricemia and uricosuria return on day 3 to day 4 to the baseline, so treatment should be long. Leaks in taking the product beyond 2 to 3 days are undesirable.
For the prevention of hyperuricemia with radiation therapy and chemotherapy, tumors are prescribed approximately in grams per day; product is taken for 2 - 3 days before the start of treatment or at the same time and continue for several days after the end of the specific therapy.
There are data on the efficacy of allopurinol in the complex therapy of infants with epilepsy. It is believed that the effect is due to the inhibitory effect of the product on tryptophan pyrolase and the increase in serotonin biosynthesis. Allopurinol (in addition to antiepileptic drugs) was administered at a dose of 4 to 5 mg / kg 2 times a day with 10-day courses with a break, -2 months.
Allopurinol contraindications:
Increased susceptibility to allopurinol. Pronounced violations of the liver and kidneys (azotemia). Pregnancy and lactation. Primary (idiopathic) hemochromatosis (or its presence in a family anamnesis).
Treatment with allopurinol is absolutely not indicated for asymptomatic hyperuricemia. Treatment with allopurinol can not be started during an acute attack of gout. Drug interaction.
The drug should be used with caution in conjunction with:
6-mercaptopurine and azathioprine (allopurinol depresses their metabolism and thereby increases toxicity) with methotrexate, cyclophosphamide, anticoagulants indirect action, antipyrine, diphekin, theophylline (due to the possibility of enhancing their effects [including unwanted] due to a slowdown in their inactivation in liver);
antitumor drugs (increased risk of damage to the hematopoiesis system);
Chlorpropamide (increased risk of permanent hypoglycemia in the event of a decrease in kidney function);
sulfinpyrazone (the effectiveness of allopurinol decreases);
products of ampicillin (due to increased risk of skin rash), iron products (due to the possible accumulation of iron in the liver);
Under the influence of thiazide diuretics, furosemide, ethacrynic acid, also thiophosphamide The antihyperuricemic effect of allopurinol is reduced, as these products increase the level of urinary acids in the blood serum.
Overdose.
Most of the overdose symptoms, such as nausea, vomiting and diarrhea, can be weakened by increasing renal excretion of allopurinol and its metabolites with abundant fluid intake and corresponding enhancement diuresis. In a clinical setting, dialysis can be used.
Allopurinol side effects:
From the digestive system: indigestion, diarrhea, nausea, vomiting, abdominal pain, stomatitis, hyperbilirubinemia, cholestatic jaundice increased activity of "liver" transaminases and alkaline phosphatase, not often - hepatonecrosis, hepatomegaly, granulomatous hepatitis.
From the cardiovascular system: pericarditis, increased blood pressure, bradycardia, vasculitis. From the musculoskeletal system: myopathy, myalgia, arthralgia.
From the side of the nervous system: headache, peripheral neuropathy, neuritis, paresthesia, paresis, depression, drowsiness. From the senses: a taste distortion, loss of taste, visual impairment, cataract, conjunctivitis, amblyopia.
On the part of the genitourinary system: acute renal failure, interstitial nephritis, increased urea concentration (in patients with initially reduced 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, and leukopenia. Allergic reactions: skin rash, skin itching, urticaria, multiforme exudative erythema (incl.
Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), purpura, bullous dermatitis, eczematous dermatitis, exfoliative dermatitis, and not often bronchospasm.
Other: furunculosis, alopecia, diabetes mellitus, dehydration, nasal bleeding, necrotic angina, lymphadenopathy, hyperthermia, hyperlipidemia. Overdose. Symptoms: nausea, vomiting, diarrhea, dizziness, oliguria. Treatment: forced diuresis, hemo- and peritoneal dialysis.
Form of issue:
Tablets in a pack of 30 and 50 pcs.
Synonyms:
Milurit, Apurin, Zilorik, Allopur, Atizuril, Foligan, Gotikur, Lizurin, Petrazin, Prinol, Piral, Purinol, Uridozide, Uriprim, Xanturate, Allopurinola-EGIS, Colchicine.
List B. In the dark place. Shelf life: 5 years. Do not use the product after the expiration date indicated on the package.
Allopurinol formulation:
1-H-pyrazolo [(-d) -pyrimidin-4-ol. White or white with a creamy shade of fine crystalline powder. Virtually nerastvorim in water and alcohol.1 tablet contains 100 mg or 300 mg of allopurinol (the active substance), also auxiliary ingredients: lactose, starch, polyvidone, talc, magnesium stearate, sodium amylopectin glycolate.
Additionally:
With caution should use allopurinol for violations of the liver and / or kidney function (in both cases, a dose reduction is necessary), hypothyroidism of the thyroid gland. In the initial period of the course of therapy with allopurinol, systematic evaluation of liver function parameters is necessary.
During the treatment with allopurinol, the daily amount of fluid consumed must be at least 2 liters (under the control of diuresis). At the beginning of the course of treatment of gout, the disease may become exacerbated. For prevention, you can use NSAIDs or colchicine (0.5 mg 3 times / day).
It should be taken into account that with adequate therapy with allopurinol, it is possible to dissolve large urate stones in the renal pelvis and subsequently to enter the ureter. Asymptomatic hyperuricemia is not an indication for the use of allopurinol.
In toddlers are used only for malignant neoplasms (especially leukemia), also for certain enzymatic disorders (syndrome Lesha-Nyana). To correct hyperuricemia in patients with tumorous diseases, allopurinol is recommended to be used before treatment cytostatics.
In such cases, the minimum effective dose should be used. In addition, in order to reduce the risk of xanthine deposition in the urinary tract, measures should be taken to maintain optimal diuresis and urine alkalinization.
With the simultaneous use of allopurinol and cytostatics, more frequent monitoring of the peripheral blood pattern is necessary. During the reception of allopurinol, do not drink alcohol.
Influence on the ability to drive vehicles and manage mechanisms in patients whose activity requires high concentration of attention and rapid psychomotor reactions.
Attention!
Before using the medicationAllopurinolit is necessary to consult a doctor.
The instruction is provided solely for acquaintance with "Allopurinol".
A source: http://medprep.info/drug/medicament/52
Allopurinol, description and reviews of the drug
Allopurinol, a drug used in the treatment of gout, is a real salvage from the reviews of most patients.
However, treatment with the drug requires great care and compliance with the instructions, since it can cause adverse reactions and complications, sometimes life-threatening, and should be carried out strictly according to the purpose doctor.
Allopurinol releases several manufacturers to the market. The most famous are the following:
- Salutas Pharma, Germany;
- PAO SPC "Borshchagovsky Chemical and Pharmaceutical Plant Kiev, Ukraine;
- CJSC "Pharmaceutical Plant EGIS Budapest, Hungary;
- Joint Stock Company "Organica Novokuznetsk, Russia.
The drug is in the form of tablets for internal use. Tablets may contain 100 or 300 mg of allopurinol.
Do not choose a dosage yourself, it should be prescribed by a doctor, based on the results of the patient's tests.
pharmachologic effect
The main action is a decrease in the synthesis of uric acid in the human body. Uric acid is the result of the metabolism of foods containing purines.
When the formation of uric acid is excessive, or the excretory system does not cope with its excretion, the uric acid content in the blood will increase.
When supersaturation will be formed urate - crystals of uric acid, which can cause the formation of stones in the bladder, kidneys or deposited in the joints.
So there are characteristic signs of gouty arthritis (gout): joint inflammation, swelling, pain, redness, mobility restriction, fever. That is why it is so important to control the level of uric acid, and not to exceed the norm.
When taking allopurinol, the activity of a special enzyme that promotes the formation of uric acid is inhibited.
The drug reduces the synthesis of uric acid, and accelerates the dissolution of already deposited urate salts.
Indications
Allopurinol is indicated for the treatment of hyperuricemia (increased uric acid in the blood) of any genesis, especially when the correction of such conditions is ineffective diet. As a rule, values of 500 μmol and higher are considered dangerous.
Allopurinol can be prescribed for all diseases that are accompanied by an elevated level of uric acid, for example, gout, urate-type kidney disease, urate nephropathy, hemoblastosis.
In pediatrics, allopurinol is prescribed from the age of 15 with conditions of enzymatic insufficiency, leukemia with impaired renal function and other conditions of hyperuricemia.
It is recommended to drink tablets with plenty of liquid. It is better to take the drug after eating.
It is very important to drink at least two liters of water a day to help dissolve urate stones and to facilitate their excretion by the kidneys.
After oral administration, the maximum concentration of the drug is detected within an hour. The withdrawal time depends on the individual characteristics of the patient and can vary significantly.
The daily dose is calculated by the doctor for each individual patient, depending on the concentration of uric acid in the blood. The average maintenance dose is 200-600 mg, which can be divided into several doses - from 2 to 4 times a day.
The maximum allowable dose for children (15 years) is 400 mg of allopurinol per day. Patients with renal insufficiency daily dose adjusted to a smaller side.
Contraindications to therapy
Contraindications to therapy with Allopurinol are the following conditions:
- Intolerance of the main or auxiliary components of the drug.
- Severe liver disorders.
- The age is under 15 years.
- Pregnancy.
- Severe kidney failure.
- The period of breastfeeding.
- Light states of hyperuricemia, which can be controlled by compliance with the right diet.
- Violations of the function of hematopoiesis.
- Heart failure and high blood pressure, especially when taking drugs from the group of diuretics or ACE inhibitors.
- Acute attack of gout (treatment should begin in a state of remission).
Unwanted reactions when taking the drug are observed quite rarely - in 5% of patients. However, in some cases:
- Disorders in the hematopoietic system: a decreased number of platelets, agranulocytosis, aplastic anemia, eosinophilia, leukocytosis, angioimmunoblastnaya lymphadenopathy, a low content of leukocytes and other qualitative and quantitative changes.
- Disorders in the liver and gallbladder: the appearance of stones, inflammation of the bile duct, changes in the activity of liver enzymes, hepatitis, and necrosis of the liver.
- Problems with metabolism: increased lipid levels in the blood, violation of carbohydrate metabolism and the detection of excess glucose in the blood.
- Dysfunction of the nervous system: the appearance of outbreaks of aggression, depressive state, neuropathy, headache, drowsiness, periodic paresthesia.
- Disturbances in the work of the senses: decreased visual acuity, changes in taste, pathology of the retina and lens of the eye.
- Pathology of the cardiovascular system: slowing of the heart rate, lowering of pressure.
- Allergic reactions: various rashes and dermatitis, swelling, vasculitis.
- Problems in the reproductive system: infertility, inflammation of the mammary glands, weakening of the erection.
- Other undesirable reactions: diarrhea, weakness, stomatitis, nausea, vomiting, swelling, arthralgia (joint pain) and myalgia (muscle pains).
The intensification of gout attacks at the beginning of treatment refers to undesirable reactions, but does not require the withdrawal of treatment.
The risk of the above described side effects increases if the patient has problems with the liver or kidneys.
Taking certain antibiotics, for example amoxicillin or ampicillin, can also contribute to the appearance of unwanted reactions.
Multiple excess daily dose (up to 20 g) can cause dizziness, nausea, vomiting, stool disorders. The risk of undesirable reactions will be insignificant with normal functioning of the liver and kidneys.
With renal failure, a long-term intake of conventional doses of allopurinol (200-400 mg) may result in more serious consequences: exacerbation of kidney diseases, the appearance of skin rashes, liver diseases.
There is no specific antidote that can neutralize the action of allopurinol. In case of drug overdose, symptomatic therapy, gastric lavage and sorbents are recommended. In a hospital, hemodialysis is possible.
Price
Allopurinol is an inexpensive drug. Its price depends on the manufacturer and dosage.
For Ukraine:
- domestic manufacturer, dosage of 100 mg - about 40 UAH for 50 tablets;
- Allopuronol-Sandoz, dosage of 300 mg - about 180 UAH for 50 tablets.
For Russia:
- domestic manufacturer, dosage of 100 mg - from 85 rubles per 50 tablets;
- Allopurinol-Aegis, a dosage of 100 mg - from 90 rubles for 50 tablets, a dosage of 300 mg - from 124 rubles for 30 tablets.
Drug analogues
Drugs of allopurinol that enter pharmacies may differ in their effectiveness and have different trade names, but they all contain the same main active ingredient.
- Among the analogs are the following drugs:
- Alopron;
- Allpol;
- Remid;
- Milurite;
- Sanfipourol;
- Purinol;
- Allozim.
Patient Reviews
Ольга, 57 years, Naberezhnye Chelny:
"I am retired and have long been suffering from gout. At first, did not attach importance to this pain, but over time it only intensified and became unbearable. It turns out that the fault is due to low-quality nutrition and age-related metabolic disorders.
The doctor prescribed Allopurinol 100 mg for three months. The drug was a great help! The pain was almost gone within a week, and by the end of the treatment laboratory parameters improved significantly.
Now I'll take a break, correct the diet and repeat the course in a few months. "
Виктор, 34 years old, Stavropol:
"The doctor said that I have a predisposition to gout and a cluster of urate stones.
To give up a good life and a sedentary way of life is still beyond my strength, so I was advised to drink Allopurinol prophylactically - half the minimum dosage tablets.
I do not drink it every day, but I regularly take tests to monitor my health. Thanks to this drug, I have no problems! "
A source: http://pomogispine.com/lechenie/lekarstva/allopurinol-instruktsiya.html