Acetazolamide: indications, contraindications, use. Acetazolamide analogues Effective and safe treatment

Gross formula

Pharmacological group of the substance Acetazolamide

Nosological classification (ICD-10)

CAS code

Characteristics of the substance Acetazolamide

White crystalline powder, odorless. Very slightly soluble in water, alcohol, acetone, practically insoluble in carbon tetrachloride, chloroform, ether, freely soluble in alkali solutions.

Pharmacology

Selectively inhibits carbonic anhydrase (an enzyme that catalyzes the reversible reaction of carbon dioxide hydration and subsequent dissociation of carbonic acid). The diuretic effect is associated with inhibition of carbonic anhydrase activity in the kidneys (mainly in the proximal renal tubules). As a result of the inhibition of carbonic anhydrase, it reduces the reabsorption of bicarbonate, Na +, K + ions, does not affect the excretion of Cl - ions, increases diuresis, increases the pH of urine, and increases the reabsorption of ammonia.

Inhibition of carbonic anhydrase of the ciliary body leads to a decrease in the secretion of aqueous humor and a decrease in intraocular pressure.

A decrease in the activity of carbonic anhydrase in the brain causes inhibition of excessive paroxysmal discharges of neurons and antiepileptic activity.

When taken orally, it is well absorbed from the gastrointestinal tract. C max in the blood is reached after 2 hours. Passes through the placenta, in small quantities passes into breast milk. Not biotransformed, excreted by the kidneys unchanged. Duration of action - up to 12 hours.

In experimental animal studies (mice, rats, hamsters, rabbits) showed teratogenic and embryotoxic effects when administered at doses 10 times higher than the MRDC.

Application of the substance Acetazolamide

Glaucoma (chronic open-angle, secondary, acute angle-closure - short-term preoperative treatment to reduce intraocular pressure); epilepsy (grand seizures and small seizures in children, mixed forms) in combination with anticonvulsants; edema (against the background of pulmonary heart failure or caused by drugs); mountain sickness (to reduce acclimatization time).

Contraindications

Hypersensitivity (including to other sulfonamides), hyponatremia, hypokalemia, adrenal insufficiency, renal and / or liver failure, liver cirrhosis (risk of encephalopathy), urolithiasis (with hypercalciuria), hyperchloremic acidosis, chronic decompensated angle-closure glaucoma (for long-term therapy), diabetes mellitus, uremia, breastfeeding.

Application restrictions

Pulmonary embolism, pulmonary emphysema (possibly increased acidosis), pregnancy.

Use during pregnancy and lactation

At the time of treatment should stop breastfeeding.

Side effects of acetazolamide

From the nervous system and sensory organs: drowsiness, hearing loss/tinnitus, taste disturbance, transient myopia, disorientation, paresthesia, convulsions.

From the digestive tract: loss of appetite, nausea, vomiting, diarrhea, melena, liver failure.

From the side of metabolism: metabolic acidosis and electrolyte imbalance (with prolonged use).

Others: urticaria, hypersensitivity to light, polyuria, hematuria, glucosuria.

Interaction

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

Acetazolamide enhances the manifestations of osteomalacia caused by taking antiepileptic drugs. With the simultaneous use of acetazolamide increases the risk of manifestation of the toxic effects of digitalis, carbamazepine, ephedrine, non-depolarizing muscle relaxants, salicylates.

Caution should be exercised with the simultaneous use of acetazolamide with acetylsalicylic acid (in high doses) due to the possibility of developing anorexia, tachypnea, lethargy, coma with a possible fatal outcome.

Overdose

Cases of overdose are not described.

Symptoms: possible increased side effects.

Treatment: symptomatic and supportive therapy.

Routes of administration

inside.

Substance Precautions Acetazolamide

In case of hypersensitivity to sulfonamides, severe side effects may develop: anaphylaxis, fever, rash (including exudative erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis), crystalluria, formation of kidney stones, bone marrow suppression, thrombocytopenic purpura , hemolytic anemia, leukopenia, pancytopenia and agranulocytosis.

Acetazolamide is a diuretic that belongs to carbonic anhydrase inhibitors.

Pharmacological action of the diuretic Acetazolamide

The drug Acetazolamide has a mild diuretic effect. It inhibits the enzyme carbonic anhydrase directly in the proximal tubules of the renal nephron. Promotes an increase in urinary excretion of sodium, potassium, and does not affect the excretion of chloride ions.

The drug increases the pH of urine. With prolonged use of this drug, the patient may develop metabolic acidosis, this condition will require medical correction. In addition, acetazolamide lowers intraocular pressure, affects the reduction of cerebrospinal fluid.

After oral administration, the diuretic is well absorbed from the gastrointestinal tract. After taking 500 mg - the maximum concentration is reached after one hour or after three. The determined concentration of the drug in the blood is maintained throughout the day.

This diuretic is distributed mainly in erythrocytes, in the central nervous system, in the kidneys and in muscles, as well as in the tissues of the eyeball. Plasma protein binding is quite high. The drug can easily cross the placental barrier, this point should be considered during pregnancy.

Acetazolamide is excreted from the body mainly by the kidneys unchanged within one day.

What are the acetazolamide diuretic for use?

Assign a diuretic in the presence of edematous syndrome;
Acetazolamide is used for chronic heart failure, as well as pulmonary insufficiency, prescribing the drug as part of complex treatment;
Increased intracranial pressure is also an indication for the use of this diuretic;
A history of glaucoma, both primary and secondary.

What diuretic contraindications for use?

Among the contraindications of Acetazolamide, the instructions for use list the following conditions:

The presence of diabetes;
Acute renal failure;
The use of Acetazolamide is contraindicated in severe pathological processes in the kidneys;
Impaired liver function is also a contraindication;
History of hypocorticism;
hypokalemia;
In the presence of metabolic acidosis, it is also forbidden to use this diuretic drug.

In addition, the drug should not be used during the first trimester of pregnancy.

Use of the diuretic Acetazolamide and dosage

With edematous syndrome, the patient is usually prescribed 250 mg once or twice a day, while a course is carried out for three, four days, with breaks of several days. In the presence of epilepsy, the dosage of the diuretic is the same, but up to four times a day.

In an acute attack of glaucoma, the initial dosage may be increased to 500 mg, after which it is reduced by half every six hours. The use of the drug in children is carried out taking into account the weight of the child, and only under strict supervision by a pediatrician.

With the simultaneous use of Acetazolamide with anticholinesterase agents, there is an increase in muscle weakness, especially in the category of people diagnosed with myasthenia gravis.

With the simultaneous use of acetazoline with lithium preparations, the excretion of this mineral element in the urine may increase. When combined with insulin and with some hypoglycemic oral agents, their clinical efficacy may be enhanced.

What are the side effects of a diuretic?

The use of Acetazolamide can provoke the occurrence of side effects, among which may be the following manifestations: hypokalemia, pruritus, muscle weakness joins, convulsions develop, the skin may acquire a reddish tint, there is no appetite, and in addition, metabolic acidosis begins.

With long-term administration of this drug, nephrolithiasis may develop, laboratory changes can also be detected in the form of transient hematuria, leukopenia, and glucosuria. In addition, the patient develops hemolytic anemia, parasthesia, agranulocytosis is noted, disorientation increases.

If the side effects become more pronounced, it is necessary to cancel the use of Acetazolamide for some time, not forgetting to consult a doctor first.

special instructions

With caution, a diuretic is used in old age, as well as in violation of kidney function. This drug may increase the development of osteomalacia, which is caused by the use of certain anticonvulsant drugs. In addition, Acetazolamide increases the risk of toxic effects of ephedrine, salicylates, digitalis, carbamazepine.

Preparations containing Acetazolamide (analogues)

Acetazolamide is present in the drug Diakarb, its dosage form is represented by tablets, they are packed in cardboard boxes, on which the date of manufacture of the drug is affixed. At the end of the implementation period, the drug can not be used.

Conclusion

Before using this diuretic drug, it is recommended to first get an exhaustive consultation with a qualified specialist.

Tradename

Monopreparations: Diakarb (Polpharma).

chemical name: N-acetamide
Molecular formula: C 4 H 6 N 4 O 3 S 2
Molar mass: 222.24
CAS number: 59-66-5
Solubility: Soluble in DMSO, methanol. Slightly soluble in ethanol.

Release form, composition

Diakarb - tablets, 250.0 mg of acetazolamide in blisters of 10 pcs. Round biconvex white tablets.

Excipients

Diacarb - dicalcium phosphate, magnesium stearate, corn starch, sodium starch glycolate, povidone.

Diakarb - pharmacological action

Acetazolamide refers to carboanhydrase inhibitors. By slowing down the reactions in the body catalyzed by this enzyme in the kidneys, it increases the excretion of sodium and potassium bicarbonate ions, water, providing alkaline diuresis. Inhibition of carbonic anhydrase in the tissues of the eye reduces IOP. Prolonged use of the drug causes metabolic acidosis and, as a result, a decrease in the diuretic effect.

Diacarb - pharmacokinetics

Acetazolamide is rapidly absorbed from the gastrointestinal tract, reaching peak plasma concentrations 2 hours after oral administration. The onset of hypotensive action is usually 1-1.5 hours after administration. The half-life is about 4 hours, the duration of the therapeutic effect is about 8-12 hours. Acetazolamide binds closely to carbonic anhydrase in tissues containing it (mainly erythrocytes and the renal cortex), as well as to plasma proteins. It is not metabolized in the body and is excreted unchanged in the urine (90%). Excretion increases with a shift in urine pH to the alkaline side.

Dosing regimen

Diacarb is prescribed 250-1000 mg (1-4 tablets) per day. A single dose is usually 250 mg.

Indications for use

In ophthalmology, diacarb is used for open-angle, secondary and acute attacks of angle-closure glaucoma (if necessary, reduce IOP before surgery).

Contraindications

Hypersensitivity to sulfa drugs. Diakarb is contraindicated in case of a decrease in the level of sodium and / or potassium in the blood, dysfunction or diseases of the liver and kidneys, adrenal glands, hyperchloremic acidosis. Should not be used in patients with cirrhosis of the liver as it may increase the risk of hepatic encephalopathy.

Precautions and Warnings

Acetazolamide (diacarb) should be used with caution in patients with chronic obstructive pulmonary disease, emphysema, diabetes, respiratory acidosis, liver damage, and while taking high doses of aspirin.

When taking the drug, it is possible to develop side effects common to sulfa drugs: Stevens-Jones syndrome, toxic epidermal necrolysis.

Increasing the dose of diacarb may cause drowsiness and / or paresthesia. Fatigue, headache and ataxia are less common. Some patients with edema due to cirrhosis of the liver experienced disorientation in space. Transient myopia was also noted.

An increase in dose often entails a decrease in diuresis. With prolonged use of diacarb, it is necessary to take into account the possibility of a skin rash. It is also recommended to regularly monitor the indicators of the general blood test and electrolyte balance.

In patients with urolithiasis, the drug increases the risk of its progression.

The risk category for the use of the drug during pregnancy according to the FDA is C. Acetazolamide had a teratogenic and embryotoxic effect in experiments on animals when administered orally or parenterally at doses 10 times higher than those recommended for humans. Given the lack of adequate studies in pregnant women, the use of the drug in this group of patients should be avoided, especially in the first trimester of gestation.

Acetazolamide was found in low concentrations in the milk of women. The drug is not recommended for the appointment during lactation.

Diacarb - side effects

With short-term use, side effects are usually not expressed. During the reception, paresthesias were noted (mainly a tingling sensation in the limbs), loss of appetite, taste disturbances, polyuria, hyperemia, thirst, headache, dizziness, fatigue, irritability, depression, decreased libido, drowsiness, confusion, rarely - photophobia.

With prolonged use, metabolic acidosis and electrolyte imbalance may develop, which is usually corrected by the appointment of sodium bicarbonate.

There were cases of transient myopia, which disappeared after discontinuation of the drug.

On the part of the gastrointestinal tract, nausea, vomiting, and diarrhea were noted.

As a member of the sulfa group, acetazolamide can cause fever, agranulocytosis, thrombocytopenia, thrombolytic purpura, leukopenia, aplastic anemia, pancytopenia, rash (including erythema multiforme, Stevens-Jones syndrome, toxic epidermal necrolysis), anaphylactic reactions, crystalluria, urolithiasis, renal colic, kidney damage, suppress the activity of bone marrow. Rarely, the development of fulminant necrosis of the liver was noted.

Incidental adverse reactions include urticarial rash, melena, hematuria, glucosuria, hearing loss and tinnitus, liver dysfunction, kidney damage, and, very rarely, renal or cholestatic jaundice, flaccid paralysis, or convulsions.

drug interaction

Acetazolamide may potentiate the effect of folic acid antagonists, hypoglycemic agents and oral anticoagulants.

The simultaneous administration of diacarb and aspirin can lead to the development of severe acidosis, increase toxicity to the central nervous system.

Dose adjustment is necessary when co-administered with cardiac glycosides and drugs that reduce blood pressure.

Simultaneous administration of acetazolamide and phenytoin leads to an increase in the concentration of the latter in the blood. There have been cases of severe osteomalacia when taking acetazolamide and anticonvulsants. There are also limited data on a decrease in the level of primidone and an increase in carbamazepine when they are co-administered with the drug.

By increasing the pH level of the primary urine, diacarb reduces the excretion of amphetamine and quinidine in the urine. This may lead to an increase in the severity and duration of the effect of these drugs.

Acetazolamide can increase blood levels of ciclosporin, reduce the antiseptic effect of methanamine in urine, increase lithium excretion and decrease blood levels.

The co-administration of acetazolamide and sodium bicarbonate increases the risk of urolithiasis.

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• ATH classification: Acetazolamide
• Active ingredients / composition: acetazolamide

Cheap analogues of Acetazolamide

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All analogs Acetazolamide

Analogues in composition and indications for use

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Analogues by indication and method of application

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Acetazolamide price

• Improves water-salt metabolism, supports acid-base balance.
  
  Indications for use.
  Retention of sodium and water in the body: edema resulting from circulatory failure, cirrhosis of the liver and renal failure; bronchial asthma; emphysema; glaucoma (to reduce intraocular pressure); some types of epilepsy; Meniere's disease; toxicosis of pregnant women; premenstrual syndrome; gout.
  
  Application rules.
  With edema of cardiac origin, take 1/2-1 tablet orally, less often - 2 tablets, 1 time per day or every other day in courses of 2-4 days with breaks of several days.
  With more frequent use, the diuretic effect is significantly reduced and increasing the dose does not lead to the desired result.
  In case of glaucoma, 1/2-1 tablet is administered orally 1-3 times a day, every other day. With epilepsy, usually take 1-2 tablets 1 time per day.
  
  Side effects.
  Rarely - drowsiness, disorientation, changes in skin sensitivity, allergic reactions in the form of skin rashes, and kidney damage.
  
  Contraindications.
  The drug can not be used for Addison's disease, severe liver and kidney damage (acute hepatitis and nephritis), diabetes mellitus, acidosis (pronounced change in the reaction of the blood to the acid side), as well as for some heart rhythm disturbances.
  
  Pregnancy and lactation.
  The drug is contraindicated in the first 3 months of pregnancy.
  
  Interaction with alcohol.
  No data.
  
  Special instructions.
  With long-term treatment with the drug, especially for the elderly, a diet rich in potassium is recommended: potatoes, carrots, beets, peas, beans, beans, peanuts, oranges, bananas, prunes, dried apricots, peaches, raisins, oatmeal.
  
  Storage conditions.
  Store at room temperature, in a dry place. Shelf life - 5 years.
  All information is presented for informational purposes and is not a reason for self-prescription or replacement of the drug.