Diacarbum

General characteristics. Structure:

Active agent: acetazoleamide of 250 mg

Other ingredients: cellulose microcrystallic, povidone, silicon dioxide colloid anhydrous, kroskarmelloza, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Acetazoleamide is powerful inhibitor of a karboangidraza and renders weak diuretic effect. The mechanism of action is based on oppression of release of ions of sodium and hydrogen from carbonic acid. Karboangidraza catalyzes reaction as a result of which carbonic acid is formed. Oppression of this enzyme acetazoleamide leads to oppression of synthesis of carbonic acid in proximal tubules. Deficit of carbonic acid as source of ions of hydrogen strengthens removal of water and sodium. The effect of acetazoleamide is caused by strengthening of a natriuresis and a diuresis. Acetazoleamide loses the diuretic properties in 3 days of use. The short-term break in use leads to recovery of diuretic effect of acetazoleamide as activity of a karboangidraza renews. Acetazoleamide raises not only removal of sodium, but also bicarbonates that can cause a metabolic acidosis. Removal of a significant amount of sodium owing to reception of acetazoleamide leads to strengthening of removal of water with loss of potassium and development of a hypopotassemia. Acetazoleamide strengthens also removal of phosphates, magnesium and calcium with urine that can lead to the corresponding metabolic disturbances.
The extrarenal effect of acetazoleamide is used at treatment of glaucoma. Acetazoleamide reduces amount of intraocular liquid, reducing intraocular pressure.
Oppression of a karboangidraza in TsNS slows down abnormal neyronalny transfer owing to what drug is also used in complex treatment of epilepsy.

Pharmacokinetics. Acetazoleamide is well soaked up in a GIT. After intake in a dose of 500 mg of Cmax (12–27 mkg/ml) it is reached in 1–3 h. Low concentration of acetazoleamide is maintained in blood during 24 h.
Distribution. Acetazoleamide is widely distributed in an organism. Gets into erythrocytes, a blood plasma, kidneys and in a significant amount — into a liver, muscles, eyes and TsNS. Drug does not collect in fabrics.
Metabolism. Acetazoleamide is not metabolized.
Removal. Drug is emitted with kidneys in not changed look. After intake about 90% of the accepted dose are removed with urine during 24 h.

Indications to use:

Chronic open angle glaucoma, secondary glaucoma, closed-angle glaucoma (for decrease in intraocular pressure, at short-term preoperative treatment and before the ophthalmologic procedures capable to provoke a bad attack of closed-angle glaucoma); cardiac dropsies or caused by reception of medicines; epilepsy (in a combination with other anticonvulsants at small attacks (petit mal) at children and at big (grand mal) — at adults; at the mixed forms); a hypobaropathy (drug reduces acclimatization time, but its influence on displays of the disease is insignificant).

Route of administration and doses:

Treatment of glaucoma: the dose of drug is defined individually, depending on the size of intraocular pressure.

The recommended doses for adults:

At an open angle glaucoma	250 mg (1 tablet) 1–4 times a day. The dose> 1000 mg (4 tablets) does not raise a therapeutic effectiveness of drug
At secondary glaucoma	250 mg (1 tablet) each 4 h. At some patients therapeutic effect 2 times a day note after reception 250 mg (1 tablets) (prolonged treatment is not shown)
At bad attacks of closed-angle glaucoma	250 mg (1 tablet) 4 times a day

Treatment of epilepsy:

Adults and children	As a rule, 8–30 mg/kg of body weight a day in 1–4 receptions. The optimum dose makes 250–1000 mg (1–4 tablets)
At simultaneous use of acetazoleamide with other anticonvulsant drugs its initial dose has to make 250 mg (1 tablet) a day. The dose is gradually raised if necessary. At children the daily dose should not exceed 750 mg

Treatment of the cardiac dropsies and hypostases caused by reception of medicines: the initial dose of drug makes 250 mg/days (1 tablet) in the morning. The best diuretic effect is noted at use of drug in 1 or 2 days with a one-day break.
At treatment of heart failure acetazoleamide appoint against the background of the standard therapy (for example purposes of cardiac glycosides, diets with the reduced content of sodium, potassium drugs).
Treatment of a hypobaropathy: the recommended daily dose makes 500–1000 mg (2–4 tablets) in stages. In case of the expected bystry rise on height the recommended daily dose makes 1000 mg (4 tablets) in stages. Drug should be taken for 24–48 h before rise. In case of symptoms of an indisposition treatment should be continued ≥48 more h.

Features of use:

In case of development of complications, life-threatening the patient, for example Stephens's syndrome — Johnson, a Lyell's disease, a fulminant necrosis of a liver, aplastic anemia and hemorrhagic diathesis, it is necessary to stop administration of drug immediately. With care appoint to the patients accepting acetylsalicylic acid (in high doses) as there is a probability of development of anorexia, a tachypnea, lethargic state, coma and even death. In the doses exceeding recommended acetazoleamide does not raise a diuresis (sometimes even reduces it), but can cause drowsiness and paresthesia. Drug can strengthen acidosis therefore it with care is appointed in case of an embolism or emphysema of lungs. At drug use> 5 days the risk of development of a metabolic acidosis increases. Acetazoleamide raises рН urine.
It is recommended to carry out the developed blood test before the beginning and throughout a course of treatment. Periodic control of electrolytes of a blood plasma is shown.
Acetazoleamide gets through a placental barrier. Adequate clinical trials of teratogenecity of drug during pregnancy were not conducted, it is not necessary to appoint it pregnant, especially in the I trimester. Anyway at purpose of drug pregnant women should weigh carefully expected advantage for mother and potential risk for a fruit. Acetazoleamide in a small amount is emitted with breast milk therefore during administration of drug feeding by a breast should be stopped.
To children Diacarbum is appointed only from 3-year age as a part of complex treatment of epilepsy.
Acetazoleamide in high doses can cause drowsiness, is more rare — increased fatigue, dizziness, an ataxy and a disorientation. Therefore during treatment drug should not be managed vehicles or to work with potentially dangerous mechanisms.

Side effects:

- from a GIT: appetite loss, change of flavoring feelings, nausea, vomiting, diarrhea, liver failure;
- from metabolism: acidosis and disturbance of electrolytic balance;
- from a nervous system: paresthesias, spasms, paresis, sometimes — drowsiness and a disorientation;
- from organs of sight and hearing: passing myopia, hearing disorder or sonitus;
- from system of blood and lymphatic system: agranulocytosis, thrombocytopenia, leukopenia and aplastic anemia, insufficiency of marrow, pancytopenia;
- from an urinary system: polyuria, hamaturia, renal colic;
- others: an anaphylaxis, urticaria, a glucosuria, a photosensitization, fever, a multiformny erythema, Stephens's syndrome — Johnson, a Lyell's disease.

Interaction with other medicines:

Acetazoleamide can strengthen action of antagonists of folic acid, hypoglycemic means and anticoagulants for intake. Simultaneous use of acetazoleamide with acetylsalicylic acid can lead to heavy acidosis and exert toxic impact on TsNS. At simultaneous use of acetazoleamide with the cardiac glycosides or medicines raising the ABP, the dose of the first has to be lowered. Acetazoleamide breaks metabolism of Phenytoinum, increasing its concentration in a blood plasma. At some patients accepting acetazoleamide with a number of anticonvulsants (Phenytoinum, Primidonum) noted a severe form of osteomalacy.

Contraindications:

Hypersensitivity to drug components; hyponatremia, hypopotassemia; abnormal liver function (risk of development of encephalopathy); renal failure; insufficiency of adrenal glands; acidosis with a hyperchloremia; the chronic dekompensirovanny closed-angle glaucoma demanding prolonged treatment; diabetes mellitus; Addison's disease.

Overdose:

It is shown by disturbance of electrolytic balance, acidosis and disturbances from TsNS. There is no specific antidote. Symptomatic treatment. In case of acidosis to the patient appoint bicarbonates. The hemodialysis is shown.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tab. of 250 mg, No. 24
Tab. of 250 mg, No. 30.