Allopyrinolum

General characteristics. Structure:

Active ingredient: 100 mg of Allopyrinolum.

Excipients: sucrose (the granulated sugar refined); potato starch; magnesium stearate (magnesium stearate); edible gelatin.

The medicine applied to dissolution of uric concrements.

Pharmacological properties:

Pharmacodynamics. The means breaking synthesis of uric acid. Is a structural analog of hypoxanthine. Enzyme inhibits a xanthineoxidase which participates in transformation of hypoxanthine into xanthine and xanthine in uric acid. It caused reduction of concentration of uric acid and its salts in fluid mediums of an organism and urine that promotes dissolution of the available uratny deposits and prevents their education in fabrics and kidneys. At reception of Allopyrinolum allocation with urine of hypoxanthine and xanthine increases.

Pharmacokinetics. After intake almost completely (for 90%) it is absorbed from a GIT. It is metabolized with formation of uroxin which keeps ability it is rather long to inhibit a xanthineoxidase. Cmax of Allopyrinolum in a blood plasma is reached on average in 1.5 h, uroxin - in 4.5 h after a single dose.

T1/2 of Allopyrinolum makes 1-2 h, uroxin - about 15 h. About 20% of the accepted dose are removed through intestines, other part - kidneys.

Indications to use:

Treatment and prevention of gout and hyperuricemia of various genesis (including in combination with a nephrolithiasis, a renal failure, an uratny nephropathy). The recurrent mixed oxalic and calcium nephroliths in the presence of a hyper uricosuria. The increased formation of urates owing to fermental disturbances. Prevention of an acute nephropathy at cytostatic and radiation therapy of tumors and leukoses, and also at complete medical starvation.

Route of administration and doses:

Establish individually, under control of concentration of urates and uric acid in blood and in urine. The adult at intake - 100-900 mg/days, depending on weight of a course of a disease. Frequency of reception is 2-4 times/days after food. To children aged up to 15 years - 10-20 mg/kg/days or 100-400 mg/days.

Maximum doses: at renal failures (including caused by an uratny nephropathy) - 100 mg/days. Increase in a dose is possible when against the background of the carried-out therapy the increased concentration of urates in blood and urine remains.

Features of use:

With care it is necessary to apply Allopyrinolum at abnormal liver functions and/or kidneys (in both cases the dose decline is necessary), hypofunction of a thyroid gland. During an initial stage of a course of therapy by Allopyrinolum systematic evaluating indicators of function of a liver is necessary.

During treatment by Allopyrinolum the daily amount of the consumed liquid has to be not less than 2 l (under control of a diuresis).

At the beginning of a course of treatment of gout there can be an exacerbation of a disease. It is possible to apply NPVS or colchicine to prevention (on 0.5 mg of 3 times/days). It is necessary to consider that at adequate therapy by Allopyrinolum dissolution of large uratny stones in a renal pelvis and the subsequent their hit in an ureter is possible.

The symptomless hyperuricemia is not the indication to use of Allopyrinolum.

At children apply only at malignant new growths (especially leukoses), and also at some fermental disturbances (Lesh-Nikhena's syndrome).

At patients with tumoral diseases Allopyrinolum is recommended to be applied to correction of a hyperuricemia before an initiation of treatment cytostatics. In such cases it is necessary to apply a minimal effective dose. Besides, for reduction of risk of adjournment of xanthines in urinary tract it is necessary to take measures for maintenance of an optimum diuresis and alkalization of urine. At simultaneous use of Allopyrinolum and tsitostatik more frequent control of a picture of peripheral blood is necessary.

During reception of Allopyrinolum alcohol intake is not allowed.

With care to apply at patients whose activity demands high concentration of attention and bystry psychomotor reactions.

At children apply only at malignant new growths (especially leukoses), and also at some fermental disturbances (Lesh-Nikhena's syndrome).

The mode of dosing is set individually, under control of concentration of urates and uric acid in blood and in urine: to children aged up to 15 years - 10-20 mg/kg/days or 100-400 mg/days.

Side effects:

From cardiovascular system: in isolated cases - arterial hypertension, bradycardia.

From the alimentary system: the dispeptic phenomena (including nausea, vomiting), diarrhea, tranzitorny increase in activity of transaminases in blood serum are possible; seldom - hepatitis; in isolated cases - stomatitis, abnormal liver functions (passing increase in activity of transaminases and ShchF), a steatorrhea.

From TsNS and peripheral nervous system: in isolated cases - weakness, increased fatigue, a headache, dizziness, an ataxy, drowsiness, a depression, a coma, paresis, paresthesias, spasms, neuropathies, vision disorders, a cataract, changes of a nipple of an optic nerve, disturbance of flavoring feelings.

From system of a hemopoiesis: in some cases - thrombocytopenia, an agranulocytosis and aplastic anemia, a leukopenia (are most probable at patients with renal failures).

From an urinary system: seldom - intersticial nephrite; in isolated cases - hypostases, uraemia, a hamaturia.

From endocrine system: in isolated cases - infertility, impotence, a gynecomastia, a diabetes mellitus.

From a metabolism: in isolated cases - a lipidemia.

Allergic reactions: skin rash, hyperemia, itch; in some cases - an angioimmunoblastny lymphadenopathy, an arthralgia, temperature increase, an eosinophilia, fever, Stephens-Johnson's syndrome, a Lyell's disease.

Dermatological reactions: in isolated cases - a furunculosis, an alopecia, decolouration of hair.

Interaction with other medicines:

At simultaneous use Allopyrinolum strengthens effect of coumarinic anticoagulants, adenine of an arabinozid, and also hypoglycemic drugs (especially at renal failures).

Uricosuric means and salicylates in high doses reduce activity of Allopyrinolum.

At simultaneous use of Allopyrinolum and tsitostatik myelotoxic action is more often shown, than at separate use.

At simultaneous use of Allopyrinolum and Azathioprinum or Mercaptopurinum cumulation of the last in an organism since in connection with inhibition Allopyrinolum of activity of a xanthineoxidase necessary for biotransformation of medicines, slows down their metabolism and elimination is observed.

Contraindications:

The expressed abnormal liver functions and/or kidneys, pregnancy, a lactation, hypersensitivity to Allopyrinolum.

At an abnormal liver function and kidneys the dose decline is necessary.

Overdose:

Symptoms: at reception of 20 g of Allopyrinolum at the patient with normal function of kidneys development of vomiting and nausea, and also dizziness and disturbances of a chair was noted. The case of reception of 22,5 g of Allopyrinolum which was not followed by development of side effects is described. At patients with disturbances of functions of kidneys at long reception of 200-400 mg of Allopyrinolum a day development of skin reactions, eosinophilias, hepatitis, a hyperthermia and an exacerbation of a disease of kidneys was noted.

Treatment: the specific antidote of Allopyrinolum is unknown. At overdose performing symptomatic therapy is recommended. The hemodialysis reduces plasma concentration of Allopyrinolum.

Storage conditions:

In the place protected from light at a temperature not above 30 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets on 100 mg. 10 pieces - planimetric strip packagings (5) - packs cardboard. 50 pieces - banks of dark glass (1) - a pack cardboard. 50 pieces - banks polymeric (1) - packs cardboard.