Acetazoleamide

General characteristics. Structure:

Active ingredient: 250 mg of acetazoleamide in 1 tablet.

The drug rendering inhibiting karboangidraza, diuretic, protivoglaukomny, antiepileptic action.

Pharmacological properties:

Pharmacodynamics. Selectively inhibits a karboangidraza (the enzyme catalyzing a reversible test of hydration of carbon dioxide and the subsequent dissociation of carbonic acid). The diuretic effect is connected with oppression of activity of a karboangidraza in kidneys (mainly in proximal renal tubules). As a result of oppression of a karboangidraza reduces a reabsorption of bicarbonate, ions of Na+, K+, does not influence excretion of ions of Cl-, strengthens a diuresis, raises urine pH, increases an ammonia reabsorption.

Oppression of a karboangidraza of a ciliary body leads to decrease in secretion of watery moisture and decrease in intraocular pressure.

Decrease of the activity of a karboangidraza in a brain causes braking of excessive paroxysmal categories of neurons and antiepileptic activity.

Pharmacokinetics. At intake it is well soaked up from a GIT. Cmax  in blood is reached in 2 h. Passes through a placenta, in small amounts gets into breast milk. It does not biotransformirutsya, removed by kidneys in not changed look. Action duration — to 12 h.

In pilot studies on animals (mice, rats, hamsters, rabbits) showed teratogenic and embriotoksichesky action at introduction of doses, by 10 times of the exceeding MRDCh.

Indications to use:

Glaucoma (chronic open-angle, secondary, acute closed-angle — short-term preoperative treatment for the purpose of decrease in intraocular pressure); epilepsy (big attacks and small attacks at children, the mixed forms) in a combination with anticonvulsant drugs; hypostases (against the background of a pulmonary heart or caused by medicines); a mountain disease (for reduction of time of acclimatization).

Route of administration and doses:

Inside, at glaucoma the dose is selected individually depending on indicators of intraocular pressure, by average doses — for 125–250 mg 1–3 times a day every other day within 5 days, then — a break 2 days.

At epilepsy adult — 250–500 mg of 1 times a day within 3 days, on the 4th — a break; to children — depending on body weight, in 1–2 receptions; at an acetazoleamide combination to anticonvulsants, an initial dose of 250 mg of 1 times a day (if necessary increase); at children it is not necessary to apply doses above, than 750 mg/days.

Hypostases — 250–375 mg a day in the morning; the maximum diuretic effect is reached at reception every other day or for 2 days in a row with a one-day break.

Mountain disease — on 250 mg 2–3 times a day, reception it is necessary to begin for 24–48 h before ascension and to continue during 48 h (if necessary — longer).

Features of use:

Use at pregnancy and feeding by a breast. It is not recommended at pregnancy (especially in the I trimester), in each separate case it is necessary to estimate the expected effect of therapy and potential risk for a fruit.

Category of action on a fruit on FDA — C. For the period of treatment it is necessary to stop breastfeeding.

In case of hypersensitivity to sulfonamides heavy side effects can develop: an anaphylaxis, fever, rash (including a mnogoformny exudative erythema, Stephens's syndrome — Johnson, a toxic epidermal necrolysis), a crystalluria, formation of stones in kidneys, oppression of marrow, a Werlhof's disease, hemolitic anemia, a leukopenia, a pancytopenia and an agranulocytosis.

In case of skin changes or changes in a blood picture drug needs to be cancelled immediately.

During long use monitoring of level of electrolytes in serum, and also control of a picture of peripheral blood is necessary.

The acetazoleamide applied in бóльших doses than it is recommended, does not increase a diuresis, and often reduces it, at the same time increases drowsiness and/or paresthesia. Under some circumstances, however, it is applied in very high doses together with other diuretics for the purpose of providing a reliable diuresis at completely refractory heart failure.

It is not necessary to apply in operating time to drivers of vehicles and people whose profession is connected with the increased concentration of attention.

Side effects:

From a nervous system and sense bodys: the drowsiness, disturbance a hearing/sonitus, taste disturbance passing short-sightedness, a disorientation, paresthesia, spasms.

From bodies of a GIT: appetite loss, nausea, vomiting, diarrhea, melena, liver failure.

From a metabolism: a metabolic acidosis and disturbance of electrolytic balance (at prolonged use).

Others: a small tortoiseshell, hypersensitivity to light, a polyuria, a hamaturia, a glucosuria.

Interaction with other medicines:

The diuretic effect amplifies theophylline, is weakened by acid-forming diuretics.

Acetazoleamide strengthens manifestations of the osteomalacy caused by reception of antiepileptic drugs. At simultaneous use acetazoleamide increases risk of manifestation of toxic effects of drugs of a foxglove, the carbamazepine, ephedrine which are not depolarizing muscle relaxants, salicylates.

It is necessary to be careful at simultaneous use of acetazoleamide with acetylsalicylic acid (in high doses) in view of a possibility of development of anorexia, a tachypnea, a lethargic state, a coma with a possible lethal outcome.

Contraindications:

Hypersensitivity (including to other sulfonamides), a hyponatremia, a hypopotassemia, insufficiency of adrenal glands, a renal and/or liver failure, cirrhosis (risk of development of encephalopathy), an urolithiasis (at a hypercalcuria), giperkhloremichesky acidosis, chronic dekompensirovanny closed-angle glaucoma (for long therapy), a diabetes mellitus, uraemia, feeding by a breast.

Restrictions to use. A pulmonary embolism, emphysema of lungs (strengthening of acidosis is possible), pregnancy.

Overdose:

Cases of overdose are not described. Symptoms: strengthening of side effects is possible.

Treatment: symptomatic and maintenance therapy.

Storage conditions:

To store in the dry, protected from light place, at a temperature of 15-25 °C. To hold far away from children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets on 250 mg, 10 tablets in each blister, on one, two or three blisters together with the application instruction in cardboard packaging.