Диакарб®

General characteristics. Structure:

Deystvuyushchey substance: 250 mg of acetazoleamide.

Excipients: cellulose microcrystallic, povidone, silicon dioxide colloid, kroskarmelloza sodium salt, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Acetazoleamide is karboangidraza inhibitor with weak diuretic activity. The mechanism of action is connected with oppression of release of ions of sodium (Na+) and hydrogen (N +) in a molecule of carbonic acid. The inhibition of activity of a karboangidraza acetazoleamide suppresses synthesis of carbonic acid in a proximal tubule of nephron. The lack of carbonic acid which is a source of the ions of H+ necessary for replacement by Na+ ions raises excretion kidneys of sodium and water. As a result of allocation of large amounts of sodium in a distal part of the nephron caused by acetazoleamide substitution of ions of Na4 with potassium ions increases (To *) that leads to big losses of K+ and development of a hypopotassemia.

Acetazoleamide raises excretion of hydrocarbonates that can lead to development of a metabolic acidosis, Acetazoleamide causes removal by kidneys of phosphates, magnesium, calcium that can also lead to metabolic disturbances.

In 3 days from the beginning of use acetazoleamide loses the diuretic properties. After a break in treatment for several days again appointed acetazoleamide resumes diuretic action because of recovery of normal activity of a karboangidraza.

Acetazoleamide is used for treatment of glaucoma. Oppression of a karboangidraza of a ciliate body reduces secretion of watery moisture of an anterior chamber of an eye that reduces intraocular pressure. Tolerance to this effect does not develop. Intraocular tension at reception of acetazoleamide begins to decrease in 40-60 min., the maximum of action is observed in 3-5 hours, intraocular pressure remains below initial level within 6-12 hours. On average intraocular pressure decreases by 40-60% of initial level.

Drug is used as supportive application at treatment of epilepsy since the karboangidraza inhibition in nervous cells of a brain brakes pathological excitability.

Acetazoleamide is used for treatment of liquorodynamic disturbances and intracranial hypertensia. Drug suppresses activity of a karboangidraza in a brain, in particular, in a vascular texture of ventricles with decrease in products of cerebrospinal fluid.

Pharmacokinetics. Acetazoleamide is well soaked up from digestive tract. After intake in a dose of 500 mg the maximum concentration (12-27 mkg/ml) is reached in 1-3 hours. In the minimum concentration keeps in blood within 24 hours from the moment of introduction. Acetazoleamide is distributed in erythrocytes, a blood plasma and in kidneys, to a lesser extent - in a liver, muscles, an eyeglobe and the central nervous system. Acetazoleamide gets through a placental barrier, in a small amount is emitted with breast milk. Does not kumulirut in fabrics and it is not metabolized in an organism. It is removed by kidneys in not changed look. After intake about 90% of the accepted dose are allocated with kidneys within 24 hours.

Indications to use:

- An edematous syndrome (weak or moderate expressiveness, in combination with an alkalosis);

- Stopping of a bad attack of glaucoma, preoperative training of patients, persistent cases of a course of glaucoma (in complex therapy);

- At epilepsy as additional therapy to antiepileptic means;

- An acute "high-rise" disease (drug reduces acclimatization time);

- Intracranial hypertensia (benign intracranial hypertensia, intracranial hypertensia after shunting of ventricles) in complex therapy.

Route of administration and doses:

Drug is accepted inside, strictly on doctor's orders. In case of the admission of administration of drug, at the next reception not to increase a dose.

• Edematous syndrome. In an initiation of treatment of 250 mg in the morning. For achievement of the maximum diuretic effect it is necessary to accept Diakarb® of 1 times a day every other day or 2 days in a row with one-day a break. Increase in a dose does not strengthen diuretic effect.

• Glaucoma.  Диакарб® it is necessary to accept as a part of complex therapy. Adult at an open angle glaucoma drug is appointed 250 mg by 1-4 times a day. Doses of more than 1000 mg, do not increase therapeutic effect. At secondary glaucoma drug is appointed 250 mg by each 4 hours during the day. At some patients the therapeutic effect is shown after short-term administration of drug in a dose of 250 mg 2 times a day. At bad attacks of glaucoma: 250 mg 4 times a day. To children, is more senior than 3 years at glaucoma attacks: 10-15 mg/kg of body weight a day in 3 - 4 receptions.

After 5 days of reception do a break for 2 days. At prolonged treatment purpose of drugs of potassium, a kaliysberegayushchy diet is necessary. At a preparation for surgery appoint 250-500 mg the day before and in the morning in day of operation.

• Epilepsy. Doses for adults: 250 - 500 mg/days in one step within 3 days, for the 4th day a break. At simultaneous use of acetazoleamide with other anticonvulsant drugs in an initiation of treatment apply 250 mg of 1 times a day, gradually increasing a dose in case of need.

Doses for children are more senior than 3 years: 8-30 mg/kg a day divided into 1-4 receptions. The maximum daily dose - 750 mg.

• Acute "high-rise" disease. Use of drug in a dose of 500 - 1000 mg a day is recommended. In case of bystry ascension — 1000 mg a day. Drug should be used in 24 - 48 hours before ascension. In case of symptoms of a disease treatment is continued within the next 48 hours or longer if it is necessary.

• Intracranial hypertensia. Use of drug in a dose of 250 mg a day is recommended or to 125-250 mg there are each 8-12 hours. The maximum therapeutic effect is reached at reception of a dose of 750 mg a day.

Features of use:

Use at pregnancy and in the period of a lactation. Well controlled clinical trials of use of the drug DIAKARB® for pregnant women were not conducted. Therefore during pregnancy the drug DIAKARB® is contraindicated in the I trimester, and in II and III trimesters - is applied with care and only when the potential advantage for mother exceeds potential risk for a fruit.

Acetazoleamide in a small amount is emitted with breast milk therefore in need of use of the drug DIAKARB® in the period of a lactation, breastfeeding needs to be stopped.

In case of hypersensitivity to drug life-threatening side effects, for example, Stephens-Johnson's syndrome, a Lyell's disease, a fulminantny necrosis of a liver, an agranulocytosis, aplastic anemia and hemorrhagic diathesis can be shown. In case of manifestation of these symptoms it is necessary to stop administration of drug immediately. DIACARBUM applied in the doses exceeding recommended does not raise a diuresis, and can increase drowsiness and paresthesias, and sometimes also to lower a diuresis. Drug can cause acidosis therefore it has to be applied with care at patients with a pulmonary embolism and emphysema of lungs.

Drug alkalinizes urine. DIACARBUM should be applied carefully at patients with a diabetes mellitus in connection with the increased risk of a hyperglycemia. In case of appointment for more than 5 days the risk of development of a metabolic acidosis is high. Control of a picture of blood and thrombocytes in an initiation of treatment, and in regular intervals of time is recommended during treatment, and also periodic control of electrolytes in blood serum.

Influence on ability to driving of the car and to control of mechanisms. Acetazoleamide, especially in high doses, can cause drowsiness, fatigue, dizziness and a disorientation therefore during treatment patients should not manage motor transport and work with the mechanisms demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the central nervous system - paresthesia, hearing disorder or a sonitus, fatigue, dizziness, an ataxy, drowsiness and a disorientation, spasms, sluggish paralysis and a photophobia, touch disturbance, hepatic encephalopathy (against the background of a liver failure).

From the alimentary system nausea, vomiting, diarrhea, a loss of appetite, taste disturbance, a fulminantny necrosis of a liver are possible.

From an urinary system - the speeded-up urination, a nephrolithiasis.

From the hemopoietic system - an agranulocytosis, thrombocytopenia, a leukopenia and aplastic anemia, insufficiency of a marrowy hemopoiesis, a pancytopenia, hemorrhagic diathesis.

Allergic reactions - skin rash in the form of a polymorphic erythema, a small tortoiseshell, Stephens-Johnson's syndrome, a Lyell's disease, an anaphylaxis.

Laboratory indicators - a hamaturia, a glucosuria, a hyperglycemia, a hypopotassemia, a hyponatremia, disturbance of water and electrolytic balance and an acid-base state (metabolic acidosis).

Others - passing short-sightedness, muscular weakness.

Interaction with other medicines:

Acetazoleamide can strengthen action of antagonists of folic acid, hypoglycemic means and peroral anticoagulants.

Simultaneous use of acetazoleamide and acetylsalicylic acid can cause a metabolic acidosis and strengthen toxic effects on the central nervous system.

At combined use with the cardiac glycosides or drugs increasing arterial pressure it is necessary to adjust an acetazoleamide dose.

Acetazoleamide, increases the maintenance of Phenytoinum in blood serum. Acetazoleamide strengthens manifestations of the osteomalacy caused by reception of antiepileptic medicines.

Simultaneous use of acetazoleamide and amphetamine, atropine or quinidine can strengthen their side effect. Potentsiirovany diuretic effect arises at combined use by methylxanthines (Aminophyllinum).

Reduction of diuretic effect happens at the combined use to ammonium chloride and other acid-forming diuretics. Strengthening of hypotensive effect concerning intraocular pressure is possible at simultaneous use with cholinergic drugs and beta adrenoblockers.

Acetazoleamide strengthens effect of ephedrine. Increases concentration in a blood plasma of carbamazepine, not depolarizing muscle relaxants.

Increases lithium removal.

Contraindications:

- Hypersensitivity to drug components;
- acute renal failure;
- uraemia;
- liver failure (risk of development of encephalopathy);
- hypopotassemia;
- hyponatremia;
- metabolic acidosis;
- hypocorticoidism;
- Addison's disease;
- diabetes mellitus;
- pregnancy (I trimester);
- lactation period;
- children's age up to 3 years.

With care: hypostases of hepatic and renal genesis, a concomitant use with acetylsalicylic acid (doses over 300 mg/days), a pulmonary embolism and emphysema of lungs (risk of development of acidosis), pregnancy (II and the III trimester).

Overdose:

Symptoms of overdose are not described. Disturbances of water and electrolytic balance, a metabolic acidosis, and also disturbances from the central nervous system can be probable symptoms of overdose. Treatment: the specific antidote does not exist.

Treatment has to be symptomatic and supporting. It is necessary to control the content of electrolytes in blood, especially potassium, sodium, and also рН blood. In case of a metabolic acidosis hydrosodium carbonate is applied. Acetazoleamide is removed by means of a hemodialysis.

Storage conditions:

List B. To store in dry, protected from light and the place, unavailable to children, at a temperature below 25 to the °sena to use after the period of validity specified on packaging. A period of validity - 5 years.

Issue conditions:

According to the recipe

Packaging:

Tablets on 250 mg. On 12 tablets in the blister from a foil of A1/PVC. 2 blisters (24 tablets) together with the Application instruction place in a cardboard pack.