Allopyrinolum

General characteristics. Structure:

International and chemical names: Allopurinol; 4-oksipirazolo [3,4-d] pyrimidine; main physical and chemical properties: tablets of a round form, white or almost white color, with a flat surface, with a facet and risky; structure: 1 tablet contains 0,1 g of Allopyrinolum in terms of 100% dry matter; excipients: lactoses monohydrate, cellulose microcrystallic, starch corn, gipromeloza, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. 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 allocation with urine of uric acid decreases and allocation of more readily soluble of hypoxanthine and xanthine increases.
Allopyrinolum in an organism turns into uroxin which also interferes with formation of uric acid, but on activity concedes to Allopyrinolum.

Pharmacokinetics. At use inside about 90% of a dose of drug are absorbed from a digestive tract. The maximum concentration of Allopyrinolum in a blood plasma is reached on average in 1,5 hours. The 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 a single dose of drug. About 20% of the accepted dose are removed through intestines, other part of drug and its metabolites – kidneys.

Indications to use:

Allopyrinolum is applied to treatment of the diseases which are followed by a hyperuricemia: at primary and secondary gout, a nephrolithiasis with formation of the urates, primary and secondary hyperuricemia taking place at the pathological processes which are followed by the strengthened disintegration of nucleoproteids and increase in content of uric acid in blood including various haemo blastomas (an acute leukosis, a lymphosarcoma, etc.) at cytostatic and radiation therapy of tumors, psoriasis, massive therapy by corticosteroid drugs. There are data on use of drug in complex therapy of epilepsy for children (increase in biosynthesis of serotonin).

Route of administration and doses:

Allopyrinolum is applied inside, after food.
Doses establish depending on amount of uric acid in blood. The minimum daily therapeutic dose for adults makes 0,1 g, maximum - 0,8 g. Usually at a moderate hyperuricemia (to 70-100 mg/l) the adult appoint 0,2-0,4 g a day, within 2-3 weeks, 1-2 times a day, then pass to a maintenance dose (0,2-0,3 g a day, into 2-3 receptions).
At severe forms of gout, considerable deposits of urates in fabrics and a high hyperuricemia (over 80-100 mg/l) appoint fractionally (no more than 0,2 g to reception), up to 0,6-0,8 g a day, within 2-4 weeks, then pass to maintenance doses (0,1-0,3 g a day) which accept it is long, within several months.
For prevention of a hyperuricemia during radiation therapy and chemotherapy of tumors the average daily dose is equal to 0,4 g. Drug is accepted in 2-3 days prior to therapy (or at the same time) and continue reception within several days after the end of specific therapy.
 To children under 6 years Allopyrinolum appoint 5 mg/kg in a daily dose; from 6 to 10 years – 10 mg/kg a day. Frequency rate of appointments – 3-4 times a day.
At complex treatment of epilepsy at children the dose of drug makes 4-5 mg/kg of body weight (2 times a day, 10-day courses with a break between them 1,5-2 months).
If timely administration of drug is missed, then Allopyrinolum needs to accept a dose as soon as possible. If the following reception is planned in 12 hours and more, then it is necessary to accept Allopyrinolum at once, and the following dose at the scheduled time. If before reception of the following dose there were less than 12 hours, reception should be missed and to further continue reception in the usual mode.

Features of use:

It is necessary to consider that after the termination of reception of Allopyrinolum for the 3-4th day indicators of an uricosuria and a lithemia therefore treatment has to be long are returned to the initial, increased level. The interval of more than 2-3 days between administrations of drug is undesirable.
Drug needs to be begun with care at unsharply expressed renal failure (the adult - in a dose no more than 0,2 g a day). During use of Allopyrinolum the diuresis at adults should be supported at the level of not less than 2 l a day. Reaction of urine has to be neutral or alkalescent - for prevention of formation of concrements. For this purpose drug is appointed in combination with drugs, alkaliziruyushchy I wet.
For prevention of possible attacks of gouty arthritis in an initiation of treatment it is possible to appoint non-steroidal anti-inflammatory drugs or colchicine (the adult on 0.5 mg 3 times a day).
At the beginning of therapy by Allopyrinolum it is necessary to conduct researches of a functional condition of kidneys systematically.

Side effects:

Allopyrinolum is usually well transferred. At gout in an initiation of treatment there can be an aggravation connected with mobilization of uric acid from gouty small knots and other depots. Are in some cases possible:
the dispeptic phenomena – nausea, vomiting, an abdominal pain, diarrhea;
allergic reactions – an enanthesis, an itch, a hyperemia, it is rare - exfoliative dermatitis, fever, arthralgias;
from system of a hemopoiesis – a leukopenia, a leukocytosis, an eosinophilia;
from a nervous system – neuritis, sleep disorders, a depression, amnesia.

Interaction with other medicines:

At use of Allopyrinolum in case of treatment of haemo blastomas antineoplastic drugs (the methotrexate, Mercaptopurinum, etc.) should be considered that Allopyrinolum not only oppresses euzymatic oxidation of the called drugs and increases their antineoplastic activity, but also considerably increases their toxicity. Therefore doses of the last have to be reduced (to 50%).
Under the influence of Allopyrinolum perhaps also strengthening of effects (including undesirable) anticoagulants of indirect action, antipyrine, dipheninum, theophylline as their inactivation in a liver is slowed down.
At simultaneous use with drugs of ampicillin the risk of emergence of an enanthesis increases.
Under the influence of thiazide diuretics, furosemide, Acidum etacrynicum antigiperurikemichesky action of Allopyrinolum decreases as these drugs increase the level of uric acid in blood serum.
It is not necessary to appoint Allopyrinolum along with ferriferous medicines in connection with possible accumulation of iron in a liver.

Contraindications:

Renal failure, pregnancy and lactation, hypersensitivity to drug.

Overdose:

Symptoms: nausea, vomiting, diarrhea, dizziness, oligouriya.
Treatment: artificial diuresis, hemodialysis and peritoneal dialysis.

Storage conditions:

To store in dry, protected from light and the place, unavailable to children, at a temperature not above 25ºС. A period of validity - 5 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging, on 5 packagings in a pack.