Acetazolamide-Acry® (Acetazolamide-Akri®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceAcetazolamideAcetazolamide
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  • Acetazolamide-Acry®
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    AKRIKHIN HFK, JSC     Russia
  • Diakarb®
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    Pharmaceutical factory "POLFARMA" JSC     Poland
    • Dosage form: & nbsptabscesses
    Composition:

    One tablet contains:

    active substance: acetazolamide in recalculation on a 100% substance - 250 mg;

    Excipients: cellulose microcrystalline - 83.15 mg, povidone (type K90) - 6.25 mg, silicon colloidal dioxide - 1.8 mg, croscarmellose sodium - 7 mg, magnesium stearate - 1.8 mg.

    Description:

    Round, flat cylindrical tablets white or white with a yellowish or grayish hue, with a facet and a risk.

    Pharmacotherapeutic group:Diuretics
    ATX: & nbsp

    S.01.E.C   Inhibitors of carbonic anhydrase

    S.01.E.C.01   Acetazolamide

    Pharmacodynamics:

    Acetazolamide is an inhibitor of carbonic anhydrase with weak diuretic activity. The mechanism of action is associated with inhibition of the release of sodium ions (Na+) and hydrogen (H+) in the molecule of carbonic acid. Inhibition of carbonic anhydrase activity acetazolamide inhibits the synthesis of carbonic acid in the proximal tubule of the nephron. The lack of carbonic acid, which is the source of H ions+, necessary for replacement by ions Na+, increases the excretion of sodium and water by the kidneys. As a result of the release of large amounts of sodium in the distal part of the nephron caused by acetazolamide, the replacement of ions Na+ on potassium ions (K+), which leads to large losses of K+ and the development of hypokalemia. Acetazolamide increases the excretion of hydrocarbonates, which can lead to the development of metabolic acidosis. Acetazolamide causes the excretion of phosphates, magnesium, calcium by the kidneys, which can also lead to metabolic disturbances.

    In 3 days from the beginning of application acetazolamide loses its diuretic properties. After a break in treatment for several days, the newly appointed acetazolamide resumes diuretic action due to the restoration of normal activity of carbonic anhydrase.

    Acetazolamide is used to treat glaucoma. Inhibition of the carbonic anhydrase of the ciliated body reduces the secretion of watery moisture in the anterior chamber of the eye, which reduces intraocular pressure. Tolerance to this effect does not develop. Ophthalmotonus begins to decrease after taking acetazolamide after 40-60 minutes, the maximum action is observed after 3-5 hours, the intraocular pressure remains below the initial level within 6-12 hours. On average, intraocular pressure decreases by 40-60% of the baseline.

    The drug is used as an auxiliary in the treatment of epilepsy, since inhibition of carbonic anhydrase in the nerve cells of the brain inhibits pathological excitability.

    Acetazolamide is used to treat liquorodynamic disorders and intracranial hypertension. The drug inhibits the activity of carbonic anhydrase in the brain, in particular in the vascular plexus of the ventricles with a decrease in the production of cerebrospinal fluid.

    Pharmacokinetics:

    Acetazolamide is well absorbed from the gastrointestinal tract. After oral administration at a dose of 500 mg, the maximum concentration (12-27 μg / ml) is achieved after 1-3 hours. In minimal concentrations it is retained in the blood for 24 hours from the moment of administration. Acetazolamide is distributed in red blood cells, blood plasma and in the kidneys, to a lesser extent - in the liver, muscles, eyeball and central nervous system. Acetazolamide penetrates through the placental barrier, in a small amount is excreted in breast milk. Do not cumulate in tissues and is not metabolized in the body. It is excreted by the kidneys unchanged. After oral administration, about 90% of the dose taken is excreted by the kidneys within 24 hours.

    Indications:

    - Edema syndrome (mild or moderate in combination with alkalosis);

    - relief of acute attack of glaucoma, preoperative preparation of patients, persistent cases of glaucoma (in complex therapy);

    - with epilepsy as an additional therapy for antiepileptic drugs;

    - acute "altitude" disease (the drug shortens the time of acclimatization);

    - intracranial hypertension (benign intracranial hypertension, intracranial hypertension after ventricular shunting) in complex therapy.

    Contraindications:

    - Hypersensitivity to acetazolamide (or other sulfonamides), as well as any other components of the drug; acute renal insufficiency;

    uremia;

    - hepatic insufficiency (risk of encephalopathy); refractory hypokalemia and hyponatremia;

    metabolic acidosis;

    - hypokorticism;

    - Addison's disease;

    Decompensated diabetes mellitus;

    - pregnancy (I trimester);

    - lactation period;

    - Children's age under 3 years (solid dosage form).

    Carefully:ABOUTliver and renal genesis, concomitant administration with acetylsalicylic acid (doses above 300 mg / day), pulmonary embolism and emphysema (risk of acidosis development), pregnancy (II and III trimester), advanced age, disturbance of water-electrolyte balance, dysfunction liver, in patients with a risk of obstruction of the urinary tract.
    Pregnancy and lactation:

    During pregnancy, the drug Acetazolamide-Acry® is contraindicated in the I trimester, and in the II and III trimesters is used with caution and only in those cases where the potential benefit to the mother exceeds the potential risk to the fetus.

    Acetazolamide in a small amount excreted in breast milk, so if you need to use the drug Acetazolamide-Acry® breastfeeding should be discontinued.

    Dosing and Administration:

    The drug is taken orally, strictly according to the doctor's prescription.

    In case of skipping the drug, with the next admission should not increase the dose.

    Edema Syndrome

    At the beginning of treatment take 250 mg in the morning. To achieve maximum diuretic effect, it is necessary to take the drug Acetazolamide-Acry® once a day every other day or 2 days in a row with a one-day break. Increasing the dose does not enhance the diuretic effect.

    Glaucoma

    The drug Acetazolamide-Acry® should be taken as part of complex therapy.

    Adults with open-angle glaucomae the drug is prescribed in a dose of 250 mg 1-4 times a day. Doses exceeding 1000 mg, not increase the therapeutic effect.In secondary glaucoma, the drug is given in a dose of 250 mg every 4 hours during the day. In some patients, the therapeutic effect is manifested after a short-term dose of 250 mg twice a day.

    In acute attacks of glaucoma: 250 mg 4 times a day.

    Children older than 3 years with attacks of glaucoma: 10-15 mg / kg of body weight per day in 3-4 divided doses.

    After 5 days of taking a break for 2 days. With prolonged treatment, it is necessary to prescribe potassium preparations, a potassium-sparing diet.

    When preparing for surgery, appoint 250-500 mg on the eve and in the morning on the day of the operation.

    Epilepsy

    Doses for adultsx: 250-500 mg per day in one session for 3 days, on the 4th day break. With the simultaneous use of the drug Acetazolamide-Acry® with other anticonvulsants at the beginning of treatment, 250 mg once a day, gradually increasing the dose if necessary.

    Doses for children older than 3 years: 8-30 mg / kg per day, divided into 1-4 doses. The maximum daily dose is 750 mg.

    Acute "high altitude" disease

    It is recommended to use the drug in a dose of 500-1000 mg per day. In the case of rapid ascent - 1000 mg per day.

    The drug should be used 24-48 hours before climbing.If symptoms of the disease appear, the treatment is continued for the next 48 hours or longer, if necessary.

    Intracranial hypertension

    It is recommended to use the drug at a dose of 250 mg per day or 125-250 mg every 8-12 hours. The maximum therapeutic effect is achieved by taking a dose of 750 mg per day.

    Side effects:

    From the central nervous system: paresthesia, hearing impairment or tinnitus, fatigue, dizziness, ataxia, drowsiness and disorientation, convulsions, flaccid paralysis and photophobia, impaired touch, hepatic encephalopathy (against hepatic insufficiency).

    From the digestive system: nausea, vomiting, diarrhea, melena, decreased appetite, impaired taste, fulminant liver necrosis.

    From the urinary system: frequent urination, nephrolithiasis.

    On the part of the organs of hematopoiesis: agranulocytosis, thrombocytopenia, leukopenia and aplastic anemia, bone marrow hematopoiesis deficiency, pancytopenia, hemorrhagic diathesis.

    Allergic reactions: skin rash in the form of polymorphic erythema, urticaria, Stevens-Johnson syndrome, Lyell's syndrome, anaphylaxis.

    Laboratory indicators: hematuria, glucosuria, hyperglycemia, hypokalemia, hyponatremia, disturbance of water-electrolyte balance and acid-base state (metabolic acidosis).

    Other: transient myopia, muscle weakness.

    Overdose:

    Symptoms overdoses are not described. Possible symptoms of overdose may be violations of water-electrolyte balance, metabolic acidosis, as well as violations from the central nervous system.

    Treatment: there is no specific antidote. Symptomatic and supportive therapy is recommended. It is necessary to control the content of electrolytes in blood plasma, especially potassium, sodium, and also the pH of the blood. In the case of metabolic acidosis, sodium hydrogencarbonate is used. Acetazolamide is output by hemodialysis.

    Interaction:

    Acetazolamide can enhance the action of antagonists of folic acid, hypoglycemic agents and oral anticoagulants.

    The simultaneous use of acetazolamide and acetylsalicylic acid can cause metabolic acidosis and enhance toxic effects on the central nervous system.

    When combined with cardiac glycosides or drugs that increase blood pressure, the dose of acetazolamide should be adjusted.

    Acetazolamide increases the content of phenytoin in the blood serum.

    Acetazolamide enhances manifestations of osteomalacia caused by the use of antiepileptic drugs.

    The simultaneous use of acetazolamide and amphetamine, atropine or quinidine can enhance their side effects.

    Potentiation of the diuretic effect occurs when combined with methylxanthines (aminophylline).

    A decrease in the diuretic effect occurs when combined with ammonium chloride and other acid-forming diuretics.

    Increased antihypertensive effect on intraocular pressure is possible with simultaneous application with cholinergic drugs and beta-blockers.

    Acetazolamide increases the effect of ephedrine.

    Increases the concentration in the blood plasma of carbamazepine, nondepolarizing muscle relaxants.

    Acetazolamide can increase the concentration of cyclosporine.

    Increases the excretion of lithium.

    Acetazolamide can reduce the antiseptic effect of methenamine on the genitourinary system.

    The simultaneous use of acetazolamide and sodium bicarbonate increases the risk of kidney stones.

    Special instructions:

    In case of hypersensitivity to the drug, life-threatening side effects may appear, for example, Stevens-Johnson syndrome, Lyell's syndrome, fulminant liver necrosis, agranulocytosis, aplastic anemia and hemorrhagic diathesis. If these symptoms occur, stop taking the medication immediately and consult a doctor.

    The drug Acetazolamide-Acry®, used in doses exceeding the recommended, does not increase diuresis, and may enhance drowsiness and paresthesia, and sometimes also reduce diuresis.

    The drug can cause acidosis, so it should be used with caution in patients with pulmonary embolism and emphysema.

    The drug becomes alkaline.

    Acetazolamide-Acry® should be used with caution in patients with diabetes mellitus because of the increased risk of hyperglycemia.

    In case of appointment for more than 5 days, the risk of developing metabolic acidosis is high.

    It is recommended to monitor blood and platelet patterns at the beginning of treatment, and at regular intervals during treatment,as well as periodic monitoring of electrolytes in blood serum.

    Effect on the ability to drive transp. cf. and fur:

    Acetazolamide-Acry®, especially in high doses, can cause drowsiness, less fatigue, dizziness, ataxia and disorientation, during treatment patients should not drive vehicles and work with mechanisms that require increased concentration and speed of psychomotor reactions.

    Form release / dosage:Tabletki, 250 mg.
    Packaging:

    10 tablets per contour cell packaging made of polyvinylchloride film and aluminum foil.

    3 contour mesh packages together with instructions for use are placed in a pack of cardboard.

    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003122
    Date of registration:30.07.2015 / 20.07.2016
    Expiration Date:30.07.2020
    The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia
    Manufacturer: & nbsp
    Representation: & nbspAKRIKHIN OJSC AKRIKHIN OJSC Russia
    Information update date: & nbsp02.10.2017
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