Acetazolamide

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Acetazolamide: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Acetazolamide

ATX code: S01EC01

Active ingredient: acetazolamide (Acetazolamide)

Manufacturer: LLC "OZON" (Russia)

Description and photo update: 2020-11-06

Prices in pharmacies: from 185 rubles.

Buy

Acetazolamide is a diuretic used for edematous syndrome, increased intraocular pressure (IOP), and excessive production of cerebrospinal fluid.

Release form and composition

The drug is produced in the form of tablets: white or almost white, round, flat-cylindrical, with a line and a chamfer (10, 12, 24 or 30 pieces in a blister strip, in a cardboard box 1, 2, 3, 4, 5 or 10 packages; 10, 12, 20, 24, 30, 40, 50 or 100 pieces in a can of polypropylene or polyethylene terephthalate, in a cardboard box 1 can and instructions for use of Acetazolamide).

1 tablet contains:

active substance: acetazolamide - 250 mg;
additional components: croscarmellose sodium, microcrystalline cellulose, magnesium stearate, povidone-K25, colloidal silicon dioxide.

Pharmacological properties

Pharmacodynamics

The active substance of Acetazolamide belongs to the systemic inhibitors of carbonic anhydrase (CA), an enzyme that participates in the hydration of carbon dioxide and dehydration of carbonic acid. The drug exhibits weak diuretic activity and, by inhibiting CA, reduces the formation of bicarbonate ions, which further reduces the movement of sodium into the cells. The effectiveness of acetazolamide depends on the point of application of the molecule: erythrocytes, the ciliary body of the eye, the proximal nephron, the choroid plexus of the brain.

The drug is used to treat intracranial hypertension and liquorodynamic disorders, since it helps to reduce the excess production of cerebrospinal fluid at the level of the vascular plexuses of the brain. Inhibition of CA in the ependymocytes of the choroid plexus reduces the excessive negative charge in the cells of the ependymal layer and decreases the gradient filtration of plasma into the cerebral ventricles.

The weak diuretic effect of acetazolamide is used in the treatment of edematous syndrome. Due to the suppression of CA activity in the proximal nephron, a decrease in the production of carbonic acid and a weakening of reabsorption by the epithelium of the tubules of bicarbonate and sodium ions are observed, which ultimately leads to a significant increase in the release of water.

A diuretic can cause metabolic acidosis due to increased excretion of hydrocarbons. Acetazolamide provides kidney elimination of magnesium, calcium, phosphates, which also aggravates the risk of metabolic disorders. During a 3-day course of treatment without interruptions, the reabsorption of sodium ions is compensatory activated in the distal tubules of the nephron, weakening the diuretic effect of the drug. Therefore, 3 days after the start of the intake, it loses its diuretic properties. After a few days of interruption in treatment, the activity of the CA of the proximal nephron is normalized and, as a result, when acetazolamide is resumed, its diuretic effect is restored.

Acetazolamide is also used to treat glaucoma. In the process of secretion of aqueous humor of the eye, hydrocarbonate ions (HCO ₃ ^-) intensively move from the cytoplasm of pigmented cells to the posterior chamber in order to replenish the gradient of positive ions caused by the active movement of sodium ions. By blocking the production of carbonic acid, CA inhibitors reduce the formation of HCO ₃ ^-… In the absence of a sufficient amount of these anions, the positive ionic gradient increases, which leads to a decrease in the production of aqueous humor. Inhibition of CA of the ciliary body reduces the formation of aqueous humor in the anterior chamber of the eye, and, as a result, lowers IOP. The development of tolerance to this effect is not recorded. After taking acetazolamide, the ophthalmotonus begins to decrease after 40-60 minutes, the maximum effect is noted after 3-5 hours, the IOP readings below the initial level (by about 40-60%) are determined for 6-12 hours.

Since the suppression of CA in nerve cells of the brain slows down pathological excitability, acetazolamide is used in the treatment of epilepsy as an adjuvant.

Pharmacokinetics

After oral administration, acetazolamide is rapidly absorbed from the gastrointestinal tract (GIT), the maximum concentration of 12-27 mcg / ml is noted after 1-3 hours. From the moment of administration, the agent in minimum concentrations is determined in the blood for 24 hours.

The diuretic is distributed mainly in the blood plasma, erythrocytes, kidneys, and to a lesser extent in the central nervous system (CNS), muscles, liver, eyeball. The drug passes through the placenta, in a small amount is excreted in breast milk.

Acetazolamide does not accumulate in tissues and does not undergo metabolic transformation in the body. Eliminated unchanged in the urine. After oral administration, approximately 90% of the dose is excreted by the kidneys within 24 hours.

Indications for use

an acute attack of glaucoma (for the purpose of relief), preoperative preparation; glaucoma characterized by a severe persistent course (in complex therapy);
mild / moderate edema syndrome (in combination with alkalosis);
intracranial hypertension after ventricular shunting, benign intracranial hypertension, CSF dynamics (as part of a combination treatment);
epilepsy (as a means of additional therapy to antiepileptic drugs);
an acute form of altitude sickness (in order to reduce the acclimatization period).

Contraindications

Absolute:

chronic renal failure (CRF) late stage, with creatinine clearance (CC) below 10 ml / min;
uremia;
acute renal failure;
liver failure;
metabolic acidosis;
refractory hypokalemia / hyponatremia;
Addison's disease;
hypocorticism;
decompensated form of diabetes mellitus;
chronic angle-closure glaucoma in the case of a long course of treatment (reduced IOP can mask worsening glaucoma and lead to organic closure of the angle);
age up to 3 years;
I trimester of pregnancy, lactation period;
hypersensitivity to any component of the drug, as well as other sulfonamides.

Relative (use Acetazolamide with extreme caution):

pulmonary emphysema and pulmonary embolism (against the background of conditions occurring with impaired alveolar ventilation, the threat of acidosis is aggravated);
edema of renal and / or hepatic origin;
impaired liver function;
violation of water and electrolyte balance;
diabetes mellitus (the risk of hyperglycemia increases);
the presence of a risk of obstruction of the urinary tract;
elderly age;
II – III trimesters of pregnancy;
combined use with acetylsalicylic acid in daily doses of more than 300 mg (since there are reports of tachypnea, anorexia, lethargy, coma and death when carrying out this combination).

Acetazolamide, instructions for use: method and dosage

Acetazolamide tablets are taken orally, strictly as directed by the attending physician.

Recommended dosing regimen based on indications:

glaucoma (as part of complex treatment): adults - against the background of open-angle glaucoma 1–4 times / day, 250 mg (1 tablet), taking in doses over 1000 mg (4 tablets) does not enhance the therapeutic effect; with secondary glaucoma, every 4 hours throughout the day, 250 mg, sometimes it is possible to achieve a therapeutic effect after taking 2 times / day, 250 mg; in acute attacks 4 times / day, 250 mg; children - for the treatment of glaucoma attacks in a daily dose of 10-15 mg / kg in 3-4 doses; after 5 days of the course, you should take a break for 2 days, in the case of long-term therapy, it is necessary to use potassium preparations, adherence to a potassium-sparing diet; to prepare for the operation the day before and on the morning of the operation - 250-500 mg;
edematous syndrome: at the beginning of the course - 250 mg in the morning, the maximum diuretic effect is achieved when using Acetazolamide 1 time / day every other day or for 2 consecutive days with a one-day interval; with a decrease in the previously recorded therapeutic effect, the drug should be discontinued for 1 day in order to restore renal CA activity; taking the drug does not exempt from the need to limit the consumption of sodium chloride, adherence to bed rest and the use of other prescribed drugs;
intracranial hypertension, liquorodynamic disorders: at a dose of 250 mg / day or every 8–12 hours at 125–250 mg, to achieve the maximum effect - at a dose of 750 mg / day; to achieve optimal therapeutic effect, daily intake can be prescribed without interruption;
epilepsy: adults - 1 time / day, 250-500 mg for 3 days, then 1 day break, in the case of using acetazolamide in combination with other anticonvulsants, its initial dose should be 250 mg / day, if necessary, a further gradual increase in the dose is possible; children - 8-30 mg / kg / day in 1-4 doses; for adults, the maximum daily dose should not exceed 1000 mg, for children - 750 mg;
acute altitude sickness: 24–48 hours before the ascent, 500–1000 mg / day, with a rapid change in altitude zones - 1000 mg / day; if symptoms of the disease reappear, treatment should be continued for the next 48 hours or more.

If the next dose of acetazolamide is missed, the dose should not be increased at the next dose as usual.

Side effects

immune system: with unknown frequency - anaphylactic reactions;
blood and lymphatic system: rarely - leukopenia, aplastic anemia, thrombocytopenic purpura, thrombocytopenia, agranulocytosis, myelosuppression, pancytopenia;
nervous system: often - dizziness, paresthesia, especially a tingling sensation in the extremities; infrequently - headache, hot flashes; extremely rarely - drowsiness, convulsions, peripheral paresis; with an unknown frequency - ataxia;
mental disorders: infrequently - irritability, depression; with an unknown frequency - agitation, disorientation, confusion;
metabolism and nutrition: often - taste disturbance, impaired appetite, metabolic acidosis, including with concomitant electrolyte disturbances (as a rule, they are eliminated when sodium bicarbonate is prescribed); infrequently - thirst; rarely - glucosuria; with an unknown frequency - hyponatremia, hypokalemia;
labyrinthine disorders and the organ of hearing: rarely - ringing in the ears and hearing impairment;
organ of vision: rarely - transient myopia (stops with a dose reduction or withdrawal of Acetazolamide);
hepatobiliary system: rarely - cholestatic jaundice, liver dysfunction, fulminant liver necrosis, hepatitis; with an unknown frequency - hepatic colic, liver failure;
digestive tract: infrequently - nausea, diarrhea, vomiting, melena; with an unknown frequency - dry mouth, dysgeusia;
genitals and mammary gland: infrequently - decreased libido;
kidneys and urinary tract: with an unknown frequency - crystalluria, the occurrence of calculi in the kidneys, polyuria, renal and ureteral colic, hematuria, kidney damage, renal failure;
skin and subcutaneous tissue: rarely - photosensitization; with an unknown frequency - urticaria, skin rash, pruritus, Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis;
violations at the injection site and general disorders: often - fatigue; infrequently - weakness, fever;
musculoskeletal and connective tissue: with an unknown frequency - arthralgia.

Overdose

Possible symptoms of acetazolamide overdose may include metabolic acidosis, disturbances in water and electrolyte balance, and disorders of the central nervous system.

There is no specific antidote, symptomatic and supportive treatment is recommended. It is required to monitor the plasma levels of electrolytes in the blood, especially sodium and potassium, as well as the pH of the blood. When metabolic acidosis is detected, sodium bicarbonate is prescribed. Acetazolamide is eliminated during hemodialysis.

special instructions

If it is necessary to use acetazolamide for a long time, a complete blood count should be done before taking it, to determine the number of leukocytes, erythrocytes, platelets. During treatment, it is also recommended to regularly monitor the blood picture and serum electrolyte levels in the blood.

If, against the background of therapy, the development of toxic skin reactions and / or a decrease in the number of blood corpuscles is observed, you must immediately stop taking the drug. If you have any skin rash, you need to consult a doctor.

An increase in the dose of acetazolamide does not cause an increase in the diuretic effect, but it can provoke an increase in unwanted side reactions (dizziness and / or paresthesia). The use of the drug in high doses in many cases causes a decrease in urine output.

Against the background of treatment with Acetazolamide for more than 5 days, the threat of metabolic acidosis is aggravated.

Reception of acetazolamide must be completed if transient hearing impairment develops.

Since the drug alkalizes urine, before using it, patients with a history of urolithiasis need to assess the relationship between the benefits of therapy and the risk of urinary calculi formation.

In patients taking antiepileptic drugs, a slight increase in the risk of suicidal ideation and manifestations of suicidal activity was found. The mechanism of this phenomenon has not been established, however, based on existing data, the possibility of the development of such effects during drug treatment cannot be excluded. Therefore, when taking acetazolamide, it is necessary to ensure careful monitoring of patients in order to timely identify them with possible signs of suicidal thinking / behavior and provide the necessary medical care.

Influence on the ability to drive vehicles and complex mechanisms

Due to the fact that taking acetazolamide, especially in large doses, can lead to drowsiness, fatigue, ataxia, dizziness and disorientation, you should not drive vehicles and other complex moving mechanisms during the course of treatment.

Application during pregnancy and lactation

In pregnant women, strictly controlled clinical studies of the use of the drug have not been conducted. As a result, in the first trimester of pregnancy, taking Acetazolamide is contraindicated, in the second and third trimesters, it is possible only in cases where the expected effect of treatment for the mother exceeds the possible threat to the fetus.

Since the drug in a small amount penetrates into breast milk, if it is necessary to take acetazolamide during lactation, it is necessary to stop breastfeeding.

Pediatric use

For children under 3 years of age, therapy with Acetazolamide is contraindicated.

In children from 3 years of age and older, the drug can be used according to the dosage regimen.

With impaired renal function

In the presence of severe chronic renal failure (CC less than 10 ml / min), uremia or acute renal failure, Acetazolamide is contraindicated.

Patients with renal edema should be treated with caution.

For violations of liver function

In the presence of liver failure, drug treatment due to the threat of encephalopathy is contraindicated.

Patients with functional disorders of the liver, including with hepatic edema, should use Acetazolamide with caution.

Use in the elderly

Elderly patients should be treated with extreme caution with acetazolamide.

Drug interactions

atropine, quinidine, amphetamine: the threat of increased side reactions of these substances is aggravated;
cardiac glycosides; drugs that increase blood pressure: dose adjustment of acetazolamide is required;
methylxanthines (aminophylline): the diuretic effect of acetazolamide is enhanced;
acetylsalicylic acid: the risk of increased toxic effects on the central nervous system and the appearance of metabolic acidosis is aggravated;
phenytoin: the serum level of this substance in the blood increases;
hypoglycemic drugs, folic acid antagonists, oral anticoagulants: the effect of these drugs is potentiated;
cyclosporine: its concentration increases;
ephedrine: the effect of this substance is enhanced;
antiepileptic drugs: the manifestations of osteomalacia, caused by the intake of these drugs, increase;
acid-forming diuretics, including ammonium chloride: weaken the diuretic effect of acetazolamide;
lithium: its excretion increases;
β-blockers, cholinergic drugs: increased hypotensive effect on IOP;
non-depolarizing muscle relaxants, carbamazepine: the content of these drugs in the blood plasma increases;
methenamine: the antiseptic effect of this agent on the urinary system is weakened;
sodium bicarbonate: the threat of renal calculi increases;
primidone: its absorption in the gastrointestinal tract decreases, which can cause a decrease in the plasma concentration of this substance and its metabolites and reduce its anticonvulsant effect; special care should be taken with this combination.

Analogs

Analogs of Acetazolamide are Diacarb, Acetazolamide-Acri.

Terms and conditions of storage

Store out of the reach of children at a temperature not exceeding 25 ° C.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Acetazolamide

Currently, there are no patient reviews on Acetazolamide on specialized sites, on the basis of which it would be possible to objectively assess its effectiveness and disadvantages.

Price for Acetazolamide in pharmacies

The price for acetazolamide, in the form of tablets, can be 180-210 rubles. for 30 pcs. packaged.

Acetazolamide: prices in online pharmacies

Drug name

Price

Pharmacy

Acetazolamide 250 mg tablets 30 pcs.

RUB 185

Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!