Acetazolamide (Acetazolamidum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Diuretics

Included in the formulation
  • Acetazolamide-Acry®
    pills inwards 
    AKRIKHIN HFK, JSC     Russia
  • Diakarb®
    pills inwards 
    Pharmaceutical factory "POLFARMA" JSC     Poland
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    S.01.E.C   Inhibitors of carbonic anhydrase

    S.01.E.C.01   Acetazolamide

    Pharmacodynamics:

    Has a diuretic, antiglaucomal, antiepileptic effect. Selectively inhibits carbonic anhydrase in the proximal renal tubule decreasing the reabsorption of sodium ions and potassium bicarbonate. Does not affect the excretion of chloride ions, raises the pH of urine, increases the reabsorption of ammonia.

    Inhibition of carbonic anhydrase ciliary body thereby reducing the secretion of aqueous humor, thereby reducing intraocular pressure.

    Inhibition of brain carbonic anhydrase inhibition causes paroxysmal neuronal discharges, kupiruya seizure activity.

    Pharmacokinetics:

    After oral administration, it is absorbed in the digestive tract. The maximum concentration of the drug in the blood plasma is achieved in 1-3 hours. It is bound by plasma proteins in 90%.

    Half-Elimination (half-life) of the drug is 10-15 hours.

    Penetrates through the placenta and enters the breast milk. Do not undergo biotransformation, is excreted in the urine unchanged.The duration of action is 12 hours.

    Indications:

    It is used in ophthalmology, with edematic syndrome in combination with alkalosis, increased intracranial pressure. Used for glaucoma, small epileptic seizures, as part of complex therapy for chronic heart failure. It is used for the prevention of mountain sickness.

    ICD-10

    VI.G40-G47.G40   Epilepsy

    VI.G90-G99.G93.2   Benign intracranial hypertension

    VII.H40-H42.H40   Glaucoma

    IX.I26-I28.I27.9   Pulmonary heart disease, unspecified

    IX.I30-I52.I50.0   Congestive heart failure

    XVIII.R50-R69.R60   Edema, not elsewhere classified

    XIX.T66-T78.T70.2   Other and unspecified influence of high altitude

    Contraindications:

    Acute renal failure, hepatic insufficiency, acidosis, hypokorticism, hypokalemia, Addison's disease, diabetes, uremia.

    Individual intolerance.

    Carefully:

    Edemas of renal and hepatic genesis.

    Pregnancy and lactation:

    Pregnancy and lactation: recommendations for Food and Drug Administration (US Food and Drug Administration) - Category C. Contraindicated in I trimester of pregnancy, in II-III trimester is prescribed in emergency situations, when the risk from taking the drug is justified by the effectiveness of the action of acetazolamide.

    During treatment with acetazolamide, it is recommended to stop breastfeeding.

    Dosing and Administration:

    Ocular syndrome - 250 mg 1-2 times a day for 2-4 days, with interruptions for 1-2 days.

    Epilepsy - 250 mg 3-4 times a day.

    Attack glaucoma: 250-500 mg - the initial dose, then 250 mg every 6 hours.

    Prevention of mountain sickness: 250 mg 3 times a day, the beginning of admission for 2-3 days before climbing, taking the drug for 48 hours and longer, as needed.

    The highest daily dose: 1.5 g.

    The highest single dose: 500 mg.

    Use in children

    Newborn infants, children aged 1 month - 12 years: intravenously or in tablets of 10-20 mg / kg per day, the maximum dose - 750 mg per day. From 12 to 18 years: intravenously or in tablets of 0.5-1 g per day for 2-4 admission.

    Side effects:

    Central and peripheral nervous system: drowsiness, disorientation, paresthesia, spasms of calf muscles.

    Metabolic acidosis, electrolyte balance disturbance.

    Gastrointestinal tract nausea, loss of appetite, vomiting, diarrhea.

    Organs of the senses: hearing loss, transient myopia, photophobia.

    Allergic reactions.

    Overdose:

    Increased side effects.

    Treatment: symptomatic.

    Interaction:

    Strengthens the diuretic effect of diuretics and theophylline.

    With simultaneous application increases the toxic effects of carbamazepide, digitalis preparations, salicylates, ephedrine, nondepolarizing muscle relaxants.

    Strengthens the action of insulin and oral hypoglycemic drugs.

    Simultaneous use with anticholinesterase drugs increases muscle weakness in patients with myasthenia gravis.

    Increases the excretion of lithium in the urine.

    Weaken the action of acetazolamide with simultaneous application of ammonium chloride.

    Expressed osteomalacia is noted with concurrent administration of acetazolamide with primidon and barbiturates.

    The use of high doses of acetylsalicylic acid concomitantly with acetazolamide can lead to tachypnea, anorexia, a lethargic state, the development of a coma with a possible fatal outcome.

    Special instructions:

    To avoid the development of metabolic acidosis, the use of acetazolamide is not recommended for more than 5 consecutive days.

    The most pronounced diuretic effect is observed with the drug every other day or two days in a row with a break in one day.

    Instructions
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