for medical use
the Trade name
the International unlicensed
name Allopyrinolum Dosage Form
of the Tablet of 100 mg
One tablet contains
active agent – Allopyrinolum of 100 mg in terms of 100% dry matter,
excipients: lactoses monohydrate (granulak 200), magnesium stearate, cellulose microcrystalline, gipromeloza, starch corn.
of the Tablet of round shape, white or almost white color, with a flat surface, with a facet and risky
Antigouty drugs. Inhibitors of synthesis of uric acid. Allopyrinolum.
The ATX M04AA01 code
Pharmacokinetics At properties use inside about 90% of a dose of drug is absorbed from a digestive tract. The maximum concentration of Allopyrinolum in blood plasma is reached on average in 1.5 hours. Is exposed to biotransformation in a liver with formation of an active metabolite of uroxin. Elimination half-life of drug makes 1-2 hour, uroxin – about 15 hours therefore the inhibition of a xanthineoxidase can proceed within 24 hours after single dose of drug. About 20% of the accepted dose are removed through intestines, the rest of drug and its metabolites – kidneys.
Allopyrinolum – antigouty drug, the oppressing synthesis of uric acid and its salts in an organism. Drug has specific ability to inhibit enzyme a xanthineoxidase, the hypoxanthine participating in transformation into xanthine and xanthine in uric acid. Thereof the content of urates in blood serum goes down and adjournment of the last in fabrics and kidneys is prevented.
Against the background of effect of drug, discharge with urine of uric acid decreases and discharge of more readily soluble of hypoxanthine and xanthine raises.
Allopyrinolum in an organism turns into uroxin which also interferes with formation of uric acid, but on activity concedes to Allopyrinolum.
– primary and secondary gout
– a nephrolithiasis with formation of urates
– primary and secondary hyperuricemias taking place at the pathological processes which are followed by the strengthened disintegration of nucleoproteids and increase in content of uric acid in blood
– various haemo blastomas (acute leukosis, a lymphosarcoma, etc.)
– cytostatic and radiation therapy of tumors, psoriasis, massive therapy by corticosteroid drugs.
To Accept a route of administration and doses after a meal, without chewing, washing down with a large amount of water.
define the Daily dose individually depending on the level of uric acid in blood serum. Usually daily dose makes 100-300 mg. For reduction of risk of side reactions treatment it is necessary to begin with reception 100 mg of Allopyrinolum once a day.
If necessary gradually to increase an initial dose by 100 mg each 1-3 weeks before obtaining the maximum effect. The maintenance dose usually makes 200-600 mg/days.
If the daily dose exceeds 300 mg, it should be divided into 2-4 equal receptions.
At increase in a dose it is necessary to carry out control of level of an oksipurinol in blood serum which should not exceed 15 mkg/ml (100 µmol).
Use for children, generally when performing cytotoxic therapy of malignant new growths, especially leukemias and treatments of fermental disturbances (for example, Lesh-Niyena’s syndrome). To children of 6 years to appoint 10 mg/kg of body weight in a daily dose.
A renal failure
Treatment it is necessary to begin 100 mg which is raised only in case of insufficient efficiency of drug with a daily dose. At selection of a dose it is necessary to be guided by an indicator of clearance of creatinine:
The clearance of creatinine
the Daily dose of Allopyrinolum
More than 20 ml/min.
the Standard dose of 100-300
mg 10-20 ml/min. 100-200 mg Less than 10 ml/min. 100 mg or higher doses with big intervals between receptions (in 1-2 and more days depending on a condition of the patient and functional capacity of kidneys)
Duration of treatment depends on a course of a basic disease.
Patients of advanced age
in the absence of specific data it is necessary to apply minimal effective doses.
In an abnormal liver function the dose should be reduced to the minimum effective.
by the Most widespread side reactions of Allopyrinolum are skin rashes. Frequency of side reactions increases in disorders from kidneys and/or a liver.
Side reactions can differ depending on a disease, from the received dose and also when assigning in combination with other medicines.
In an initiation of treatment reactive attacks of gout because of mobilization of uric acid from gouty small knots and other depots can arise Allopyrinolum.
– an itching, rash, including scaly, purpuropodobny, makulopapulezny
– reactions of hypersensitivity, including skin reactions
– nausea, vomiting (it is possible to avoid, accepting Allopyrinolum after a meal)
– asymptomatic increase in level of hepatic tests
– exfoliative dermatitis, Stephens-Johnson’s syndrome, a toxic epidermal necrolysis
Skin reactions are the most widespread reactions and can arise during any period of treatment, at their emergence the intake of Allopyrinolum should be stopped immediately. After reduction of symptoms it is possible to appoint drug in low doses (for example, 50 mg/days), if necessary gradually raising. At repeated manifestation of skin rash the administration of drug should be stopped forever as heavy generalized reactions of hypersensitivity can appear.
Serious generalized reactions of hypersensitivity, including the skin reactions associated with exfoliation, fever, a lymphadenopathy, an arthralgia and/or an eosinophilia arise seldom. The vasculites associated with reactions of hypersensitivity and reaction of fabrics can have various manifestations, including hepatitis, damage of kidneys (interstitial nephrite) and very seldom a spasm. These reactions can arise at any moment of treatment, at their emergence Allopyrinolum should be cancelled immediately.
– hepatitis (including gepatonekroz and granulematozny hepatitis), an acute cholangitis.
Liver dysfunction (usually reversible at drug withdrawal) can arise without strong indications of generalized reactions of hypersensitivity.
– a lymphadenopathy, including an angioimmunoblastny lymphadenopathy (usually reversible at drug withdrawal), an anaphylaxis, including an acute anaphylaxis
– an alopecia, an angioedema, decolouration of hair, the fixed medicamentous erythema
– a furunculosis
– heavy injury of marrow (thrombocytopenia, an agranulocytosis, aplastic anemia)
– diabetes, a lipidemia
– a depression
– an ataxy, a coma, a headache, neuropathy, spasms, peripheral neuritis, paresthesias, paralyzes, drowsiness, distortion of flavoring feelings
– a cataract (especially at patients of advanced age, at prolonged use of high doses), macular changes, a disorder of vision
– stenocardia, bradycardia, arterial hypertension
– change of a rhythm of defecation, stomatitis, a steatorrhea, gematomezis
– interstitial nephrite, a hamaturia, uraemia
– a gynecomastia, impotence, male infertility
– an asthenia, fever, feeling of an indisposition, hypostases, myopathy/myalgia, ksantinovy deposits in fabrics, including in muscles
the Fever can arise with/without symptoms of generalized reactions of hypersensitivity.
Frequency is unknown
– the skin reactions associated with an eosinophilia, urticaria
– an arthralgia
– a leukopenia, a leukocytosis, an eosinophilia, hemolytic anemia, disturbance of blood clotting. It was reported about a case of the acute clean erythrocyte aplasia connected with therapy by Allopyrinolum
– in an initiation of treatment reactive attacks of gout
– diarrhea, abdominal pain
– a nephrolithiasis
– nocturnal emission
of the Contraindication
– Hypersensitivity to Allopyrinolum and to other components of drug
– heavy disturbances of functions of a liver or kidneys (clearance of creatinine less than 2 ml/min.)
– a bad attack of gout
– intolerance of a galactose, insufficiency of lactase, a syndrome of glyukozo-galaktozny malabsorption
– pregnancy and the period of a lactation
– children’s age up to 6 years are possible.
Anticoagulants of coumarinic type – strengthening of effect of warfarin and other coumarins therefore more frequent control of indicators of coagulation is required and also is possible a dose decline of anticoagulants.
Azathioprinum, Mercaptopurinum – as Allopyrinolum inhibits a xanthineoxidase, metabolism of these derivatives of purine slows down, effects are prolonged, the toxicity increases therefore their usual dose should be lowered by 50-75% (up to ¼ usual doses).
Vidarabin (adenine arabinozid) – is extended elimination half-life of the last with risk of increase in its toxicity. This combination should be applied with care.
Salicylates (high doses), uricosuric drugs (for example, Sulfinpyrazonum, probenetsid, benzbromaron) – decrease in efficiency of Allopyrinolum because of acceleration of removal of its main metabolite of an oksipurinol is possible. Also Allopyrinolum slows down removal of a probenitsid. It is necessary to correct Allopyrinolum doses.
Chlorpropamide – in a renal failure raises risk of a long hypoglycemia that can demand a chlorpropamide dose decline.
Phenytoinum – disturbance of metabolism of Phenytoinum in a liver is possible, the clinical importance of it is unknown.
Theophylline, caffeine – Allopyrinolum in high doses suppresses metabolism and increases plasma concentration of theophylline, caffeine. Follows in an initiation of treatment Allopyrinolum or at increase in its dose to control theophylline level in blood plasma.
Ampicillin, amoxicillin – raises risk of emergence of allergic reactions, including skin rashes therefore the patients accepting Allopyrinolum should apply other antibiotics.
Cyclosporine – increase in concentration of cyclosporine in blood plasma and, respectively, increase in risk of development of side reactions, especially nephrotoxicity is possible.
Cytostatics (for example, cyclophosphamide, doxorubicine, bleomycin, Procarbazinum, mekhloretamin) – the risk of bone marrow suppression at patients with neoplastic diseases (except leukemia) is increased, than at separate use of these medicines therefore indicators of blood should be controlled through short intervals of time.
Didanozin – Allopyrinolum increases concentration in blood plasma of a didanozin, increasing risk of its toxicity, it is necessary to avoid their combined use.
Kapetsitabin – is recommended to avoid combined use of a kapetsitabin with Allopyrinolum.
Diuretics, including thiazide, and related drugs – risk of development of reactions of hypersensitivity, especially at patients with renal failures increases.
APF inhibitors, including captopril – the increased risk of development of gematotoksichesky reactions, such as leukopenia, and reactions of hypersensitivity, especially in renal failures.
Antacids – it is desirable to accept Allopyrinolum in 3 hours prior to intake of aluminum hydroxide.
it is not recommended to use Drug at the level of uric acid lower than 500 µmol/l (there correspond 8.5 mg / 100 to ml) at observance of recommendations about a diet and lack of severe damage of kidneys. Not to use products with the high content of purines (for example, an offal: kidneys, brain, liver, heart and language, meat profits and alcohol, especially beer).
At treatment it is necessary to support by Allopyrinolum a diuresis at the level of not less than 2 l/days, at the same time reaction of urine has to be neutral or alkalescent as it prevents precipitation of urates, formation of concrements. For this purpose it is possible to appoint Allopyrinolum in combination with the drugs alkalizing urine.
At the first manifestations of skin rash or any other signs of hypersensitivity the administration of drug should be stopped immediately to prevent development of more serious reactions of hypersensitivity (including Stephens-Johnson’s syndrome, a toxic epidermal necrolysis).
It is necessary to apply Allopyrinolum with extra care:
– in a renal failure and a liver – constant observation of the doctor is necessary, doses of Allopyrinolum should be reduced, considering the corresponding recommendations
– at earlier established disturbances of a hematopoiesis
– to patients with arterial hypertension or heart failure, receiving APF inhibitors and/or diuretics, because of the possible accompanying renal failure.
The asymptomatic hyperuricemia, as a rule, is not considered the indication for Allopyrinolum use as there is usually enough observance of the corresponding diet and the adequate drinking mode.
Bad attack of gout: treatment by Allopyrinolum should not be begun before its full stopping as further attacks can be provoked.
In an initiation of treatment Allopyrinolum, as well as other uricosuric drugs, bad attacks of gout because of mobilization of a large amount of uric acid are possible. Therefore it is desirable within the first 4 weeks for the purpose of prevention at the same time to apply non-steroidal anti-inflammatory drugs (except aspirin or salicylates) or colchicine.
If the bad attack of gout arises at the patients who are already accepting Allopyrinolum, treatment should be continued in the same dose, and a bad attack to treat the appropriate anti-inflammatory drugs.
At adequate therapy the dissolution of large uratny stones in kidneys, their hit in urinary tract (renal colic) with their possible obstruction is possible.
For prevention of a hyperuricemia the patients with neoplastic diseases, Lesh-Niyena’s syndrome are recommended to appoint Allopyrinolum prior to the beginning of radiotheraphy or chemotherapy. In such cases it is necessary to apply a minimal effective dose. For minimization of risk of adjournment of xanthines in urinary tract the adequate hydration is necessary for maintenance of an optimum diuresis, urine alkalization.
Tablets of Allopyrinolum contain lactose. Patients with rare hereditary problems of intolerance of a galactose, deficiency of lactase or a syndrome of glyukozo-galaktozny malabsorption should not take the drug.
Use during pregnancy or feeding by a breast.
Use of Allopyrinolum during pregnancy is contraindicated.
In need of drug use the breastfeeding should be stopped.
The feature of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms
Before clarification of individual reaction to drug needs to refrain from control of vehicles and work with other mechanisms because of possibility of dizziness or drowsiness.
Symptoms: nausea, vomiting, diarrhea, dizziness, headache, drowsiness, abdominal pain. In some cases – a renal failure, hepatitis.
Treatment: symptomatic, apply the supporting actions. Adequate hydration for maintenance of an optimum diuresis promotes excretion of Allopyrinolum and its metabolites. If necessary – a hemodialysis. Specific antidote is unknown.
A form of release and packing
On 10 tablets in blister strip packaging from a film of polyvinylchloride and aluminum foil with a unilateral covering thermovarnish and the press on the other hand. On 5 packs together with the instruction for medical use in the state and Russian languages in a pack from cardboard.
In original packing at a temperature not higher than 25 wasps.
To store out of children’s reach!
Not to use a period of storage of 5 years after expiry date.
According to the prescription
the Public joint stock company Producer “”Borshchagovsky Chemical and Pharmaceutical Plant” research and production center”,
03134, Ukraine, Kiev, Mira St. 17.
The owner of the registration certificate
“”Borshchagovsky Chemical and Pharmaceutical Plant” research and production center” Public joint stock company, Ukraine
the Address of the organization accepting claims in the territory of RK from consumers on quality
of the Representative Office of PJSC NPC Borshchagovskiy HFZ product in the territory of the Republic of Kazakhstan
050043, Almaty, mdt. Orbit-2, 28, quarter 30
Fax: +7 (272) 20-78-05, 55-18-53
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