Acetazolamide

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Available since: 2019-09-19

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Clinical Pharmacology

Acetazolamide is a systemic carbonic anhydrase inhibitor with weak diuretic activity. Carbonic anhydrase (CA) is an enzyme involved in the process of hydrating carbon dioxide and dehydrating carbonic acid. Inhibition of carbonic anhydrase reduces the formation of bicarbonate ions, followed by a decrease in sodium transport into the cells. The effects of the use of the drug Diakarb® are due to the point of application of the molecule: the choroid plexus of the brain, the proximal nephron, the ciliary body of the eye, the red blood cells. Acetazolamide is used to treat liquorodynamic disorders and intracranial hypertension by reducing excessive production of cerebrospinal fluid at the level of the vascular plexus of the brain. Inhibition of carbonic anhydrase in ependymocytes of the choroid plexus reduces the excess negative charge in ependyma cells and reduces the gradient filtration of plasma into the cavity of the ventricles of the brain. Acetazolamide is used in the treatment of edema syndrome due to a weak diuretic effect. As a result of inhibition of the activity of carbonic anhydrase in the proximal nephron, there is a decrease in the formation of carbonic acid and a decrease in the reabsorption of bicarbonate and Na + tubule epithelium, due to which the excretion of water significantly increases. Acetazolamide increases the excretion of bicarbonates, which can lead to the development of metabolic acidosis. Acetazolamide causes excretion of phosphate, magnesium, calcium by the kidneys, which can also lead to metabolic disorders. Over the next 3 days of therapy, reabsorption of Na + in the distal nephron is compensatory activated, reducing the diuretic effect of Diacarb®. After 3 days from the start of the application, acetazolamide loses its diuretic properties. After a break in treatment for several days, the newly prescribed acetazolamide resumes its diuretic effect due to the restoration of the normal activity of carbonic anhydrase of the proximal nephron. Acetazolamide is used to treat glaucoma. In the process of formation of aqueous humor of the eye, bicarbonate ions are actively transported from the cytoplasm of non-pigmented cells to the back chamber to compensate for the gradient of positive ions caused by the active transport of Na + ions. KA inhibitors block the formation of carbonic acid, thus reducing the production of HCO3-. In the absence of a sufficient number of HCO3- ions, the positive ion gradient increases, which causes a decrease in the secretion of aqueous humor. Inhibition of ciliary body carbonic anhydrase reduces the secretion of aqueous humor of the anterior chamber of the eye, which reduces intraocular pressure. Tolerance to this effect does not develop. Ophthalmotonus when taking acetazolamide begins to decrease after 40-60 minutes, the maximum of action is observed after 3-5 hours, the intraocular pressure remains below the initial level for 6-12 hours. On average, the intraocular pressure decreases by 40-60% from the initial level. The drug is used as an adjunct in the treatment of epilepsy, because inhibition of carbonic anhydrase in the nerve cells of the brain inhibits pathological excitability.

Suggested use

The drug is taken orally, strictly on doctor's prescription. In case of skipping the drug, the next dose should not increase the dose. Edema syndrome At the beginning of treatment, take 250 mg in the morning. For maximum diuretic effect, it is necessary to take Diacarb® 1 time per 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 Diakarb® should be taken as part of complex therapy. For adults with open-angle glaucoma, the drug is prescribed at a dose of 250 mg 1-4 times / day. Doses in excess of 1000 mg do not increase the therapeutic effect. In secondary glaucoma, the drug is prescribed at a dose of 250 mg every 4 hours during the day. In some patients, the therapeutic effect is manifested after short-term administration of the drug at a dose of 250 mg 2 times / day.In acute attacks of glaucoma - 250 mg 4 times / day. Children older than 3 years with attacks of glaucoma - 10-15 mg / kg body weight / day in 3-4 doses. After 5 days of taking a break for 2 days. With long-term treatment, it is necessary to prescribe potassium, a potassium-saving diet. In preparation for the operation, 250-500 mg are prescribed the day before and in the morning of the operation. Epilepsy Doses for adults: 250-500 mg / day in 1 reception for 3 days, on the 4th day of a break. With the simultaneous use of acetazolamide with other anticonvulsants at the beginning of treatment, 250 mg 1 time / day is used, gradually increasing the dose if necessary. Doses for children over 3 years: 8-30 mg / kg / day, divided into 1-4 doses. The maximum daily dose is 750 mg. Acute Altitude Disease The use of the drug in a dose of 500-1000 mg / day is recommended. In the case of rapid ascent - 1000 mg / day. The drug should be used 24-48 hours before climbing. In the event of symptoms of the disease, treatment is continued for the next 48 hours or longer, if necessary. Liquorodynamic disorders, intracranial hypertension The use of the drug in a dose of 250 mg / day or 125-250 mg every 8-12 hours is recommended. The maximum therapeutic effect is achieved when taking a dose of 750 mg / day. In order to achieve the optimal therapeutic effect, it may be necessary to take the medication daily without interval.

Indications

edematous syndrome (mild or moderate severity, in combination with alkalosis); relief of an acute attack of glaucoma, preoperative preparation of patients, persistent cases of the course of glaucoma (in complex therapy); with epilepsy as an additional therapy to antiepileptic drugs; acute "altitude" disease (the drug reduces the time of acclimatization); liquorodynamic disorders, intracranial hypertension (benign intracranial hypertension, intracranial hypertension after ventricular shunting) in complex therapy.

Composition

1 tab. acetazolamide 250 mg Excipients: microcrystalline cellulose - 80.76 mg, povidone - 8.64 mg, colloidal silicon dioxide - 1.8 mg, croscarmellose sodium - 7 mg, magnesium stearate - 1.8 mg.

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Adverse reactions

Adverse effects are classified according to the frequency of occurrence and by organs and systems. The following definition of the frequency of occurrence of undesirable effects is accepted: very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (> 1/10 000, <1/1000); very rarely (<1/10 000), the frequency is unknown (cannot be determined based on the available data). On the part of the hematopoietic system: rarely - aplastic anemia, thrombocytopenia, agranulocytosis, leukopenia, thrombocytopenic purpura, myelosuppression, pancytopenia. On the part of the immune system: the frequency is unknown - anaphylactic reactions. Metabolism and nutrition: often - loss of appetite, taste disturbances, metabolic acidosis, metabolic acidosis and electrolyte disturbances (usually can be corrected by administration of bicarbonate); infrequently - thirst; rarely - glycosuria; frequency is unknown - hypokalemia, hyponatremia. Mental Disorders: Infrequently - depression, irritability; frequency unknown - arousal, confusion, disorientation. On the part of the nervous system: often - dizziness, paresthesias, in particular, a tingling sensation in the extremities; infrequently - "hot flashes", headache; very rarely - drowsiness, peripheral paresis, convulsions; frequency unknown - ataxia. On the part of the organ of vision: rarely - transient myopia (this condition disappeared completely with a dose reduction or drug withdrawal). On the part of the organ of hearing: rarely - hearing loss and tinnitus. On the part of the digestive system: infrequently - nausea, vomiting, diarrhea, melena; rarely - fulminant liver necrosis, abnormal liver function, hepatitis, cholestatic jaundice; frequency is unknown - dry mouth, dysgeusia, liver failure, hepatic colic. Skin and subcutaneous tissue: rarely - photosensitivity; frequency is unknown - itching, rash, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria. On the part of the musculoskeletal system: the frequency is unknown - arthralgia. On the part of the urinary system: the frequency is unknown - the formation of calculi in the kidneys, crystalluria, renal and ureteral colic and kidney damage, polyuria, hematuria, renal failure. On the part of the genital organs and the mammary gland: infrequently - decreased libido. General disorders and disorders at the injection site: often - fatigue; infrequently - fever, weakness.

Contraindications

acute renal failure; uremia; liver failure (risk of developing encephalopathy); hypokalemia; hyponatremia; metabolic acidosis; hypocorticoidism; Addison's disease; diabetes; I trimester of pregnancy; lactation period; children up to 3 years; hypersensitivity to the drug. With caution: edema of the liver and kidney origin, simultaneous administration with acetylsalicylic acid (doses of more than 300 mg / day), pulmonary embolism and pulmonary emphysema (risk of developing acidosis), II and III trimesters of pregnancy.

Drug interactions

Acetazolamide may enhance the action of folate antagonists, hypoglycemic agents, and oral anticoagulants. The simultaneous use of acetazolamide and acetylsalicylic acid can cause metabolic acidosis and increase 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 serum phenytoin content. Acetazolamide increases the manifestations of osteomalacia caused by taking antiepileptic drugs. The simultaneous use of acetazolamide and amphetamine, atropine or quinidine may 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. Strengthening the hypotensive effect on intraocular pressure is possible with simultaneous use with cholinergic drugs and beta-blockers. Acetazolamide enhances the effect of ephedrine. Increases plasma concentration of carbamazepine, non-depolarizing muscle relaxants. Increases the elimination of lithium.

Special instructions

In case of hypersensitivity to the drug, life-threatening side effects may occur, for example, Stevens-Johnson syndrome, Lyell's syndrome, fulminant hepatic necrosis, agranulocytosis, aplastic anemia and hemorrhagic diathesis. In the event of these symptoms should immediately stop taking the drug. Diakarb®, used in doses higher than recommended, does not increase diuresis, can increase drowsiness and paresthesias, and sometimes also reduce diuresis. The drug can cause acidosis, so it should be used with caution in patients with pulmonary embolism and pulmonary emphysema. The drug leaches urine. Diacarb® should be used carefully in patients with diabetes due to an 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 the blood and platelet patterns at the beginning of treatment and at regular intervals during treatment, as well as periodic monitoring of electrolytes in the blood serum. Influence on ability to drive motor transport and control mechanisms Diacarb®, especially in high doses, can cause drowsiness, less often fatigue, dizziness, ataxia and disorientation, so during treatment, patients should not drive vehicles and work with mechanisms that require increased concentration and psychomotor speed.

Overdosage

Symptoms of overdose are not described. Disorders of water and electrolyte balance, metabolic acidosis, as well as disorders of the central nervous system can be probable symptoms of overdose. Treatment: there is no specific antidote. Conduct symptomatic and supportive therapy. The content of electrolytes in the blood, especially potassium, sodium, and blood pH should be monitored. In the case of metabolic acidosis, sodium bicarbonate is used. Acetazolamide is eliminated by hemodialysis.