Acetazolamide trade name analogues. Medicinal reference book geotar

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 in 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. Cmax in the blood is reached after 2 hours. Passes through the placenta, in small amounts passes into breast milk. Not biotransformed, excreted by the kidneys unchanged. Duration of action - up to 12 hours.

In experimental studies on animals (mice, rats, hamsters, rabbits), it 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.

There are contraindications. Please consult your doctor before taking.

Commercial names abroad (abroad) - Diamox, Diazomid, Diluran, Glaupax.

Currently, analogues (generics) of the drug are NOT SOLD in Moscow pharmacies.

All drugs used in cardiology,.

You can ask a question or leave a review about the medicine (please do not forget to indicate the name of the drug in the text of the message).

Preparations containing Acetazolamide (Acetazolamide, ATC code (ATC) S01EC01):

Diacarb (Acetazolamide) - instructions for use. Prescription drug, information intended for healthcare professionals only!

Clinico-pharmacological group:

Diuretic. Carbonic anhydrase inhibitor.

pharmachologic effect

A diuretic from the group of carbonic anhydrase inhibitors. Causes a weak diuretic effect. Inhibits the enzyme carbonic anhydrase in the proximal convoluted tubule of the nephron, increases the urinary excretion of sodium, potassium, bicarbonate ions, does not affect the excretion of chloride ions; causes an increase in urine pH. Violates the acid-base balance (metabolic acidosis). Inhibition of carbonic anhydrase in the ciliary body leads to a decrease in the secretion of aqueous humor and a decrease in intraocular pressure. Suppression of carbonic anhydrase activity in the brain determines the anticonvulsant activity of the drug.

Duration of action - up to 12 hours.

Pharmacokinetics

Suction

After oral administration, acetazolamide is well absorbed from the gastrointestinal tract. After taking Diakarba at a dose of 500 mg, Cmax of the active substance is 12-27 μg / ml and is reached after 1-3 hours. The determined plasma concentration of acetazolamide is maintained for 24 hours after taking the drug.

Distribution and metabolism

It is distributed mainly in erythrocytes, kidneys, muscles, tissues of the eyeball and the central nervous system. It binds to plasma proteins to a high degree. Penetrates through the placental barrier.

Acetazolamide is not biotransformed in the body.

breeding

Excreted by the kidneys unchanged. About 90% of the dose is excreted in the urine within 24 hours.

Indications for use of the drug DIACARB®

• edematous syndrome (mild and moderate severity, in combination with alkalosis);
• glaucoma (primary and secondary, as well as in acute attack);
• epilepsy (as part of combination therapy);
• acute high-altitude (mountain) disease.

Dosing regimen

With edematous syndrome at the beginning of treatment, the drug is prescribed at a dose of 250-375 mg (1-1.5 tablets) 1 time per day in the morning. The maximum diuretic effect is achieved when taking the drug every other day or 2 days in a row, and then a one-day break. When using Diakarb, therapy for circulatory insufficiency, including cardiac glycosides, should be continued, a diet with limited salt intake and replenish the lack of potassium should be continued.

For adults with open-angle glaucoma, the drug is prescribed in a single dose of 250 mg (1 tablet) 1-4 times a day. Doses exceeding 1 g do not increase the therapeutic effect. In secondary glaucoma, the drug is prescribed in a single dose of 250 mg (1 tablet) every 4 hours. In some patients, the therapeutic effect is manifested after a short-term administration of the drug at 250 mg 2 times a day. In acute attacks of glaucoma, the drug is prescribed 250 mg 4 times a day.

For children with attacks of glaucoma, Diakarb® is prescribed at a dose of 10-15 mg / kg of body weight per day for 3-4 doses.

With epilepsy, adults are prescribed 250-500 mg per day in one dose for 3 days, on the 4th day - a break. Children aged 4 to 12 months - 50 mg per day in 1-2 doses; children aged 2-3 years - 50-125 mg per day in 1-2 doses; children and adolescents aged 4 to 18 years - 125-250 mg 1 time per day in the morning. With the simultaneous use of Diakarba with other anticonvulsants, at the beginning of treatment, 250 mg (1 tablet) is used 1 time per day, if necessary, gradually increasing the dose. In children, doses exceeding 750 mg per day should not be used.

In case of mountain sickness, it is recommended to use the drug at a dose of 500-1000 mg (2-4 tablets) per day; in case of rapid ascent - 1000 mg per day. The daily dose is divided into several doses in equal doses. The drug should be used 24-48 hours before the ascent, and in case of symptoms of the disease, continue treatment for the next 48 hours or more, if necessary.

If you miss taking the drug, you should not increase the dose at the next dose.

Side effect

From the side of the central nervous system and peripheral nervous system: convulsions, paresthesia, tinnitus, myopia; with prolonged use - disorientation, impaired touch, drowsiness.

On the part of the hematopoietic system: in some cases, with prolonged use - hemolytic anemia, leukopenia, agranulocytosis.

From the side of water and electrolyte balance and acid-base balance: hypokalemia, metabolic acidosis.

From the urinary system: in some cases, with prolonged use - nephrolithiasis, transient hematuria and glucosuria.

From the digestive system: anorexia; with prolonged use - nausea, vomiting, diarrhea.

Dermatological reactions: skin hyperemia, itching, urticaria.

Other: muscle weakness, with prolonged use - allergic reactions.

Contraindications to the use of the drug DIACARB®

• acute renal failure;
• liver failure;
• hypokalemia;
• acidosis;
• hypocorticism;
• Addison's disease;
• uremia;
• diabetes;
• pregnancy;
• lactation;
• hypersensitivity to the components of the drug.

With caution, the drug is prescribed for edema of the hepatic and renal origin and when taken together with acetylsalicylic acid in high doses.

The use of the drug DIACARB® during pregnancy and lactation

Diakarb® is contraindicated for use during pregnancy and lactation.

Application for violations of liver function

Contraindicated in liver failure.

Application for violations of kidney function

Contraindicated in acute renal failure. With caution, the drug should be used in patients with impaired renal function due to an increased risk of developing metabolic acidosis.

Use in children

The drug is used according to indications and in a dose adjusted according to age.

special instructions

When prescribing the drug for more than 5 days in a row, the risk of developing metabolic acidosis increases.

With prolonged use of the drug, the picture of peripheral blood, indicators of water-electrolyte and acid-base balance should be monitored.

Influence on the ability to drive vehicles and control mechanisms

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

Overdose

Cases of drug overdose or acute poisoning have not been described.

Symptoms: possible increase in the described side effects.

Treatment: carry out symptomatic therapy.

drug interaction

When used together with antiepileptic drugs, Diacarb increases the manifestations of osteomalacia.

With the combined use of Diakarba with other diuretics and theophylline, the diuretic effect is enhanced.

With the simultaneous use of Diakarb with acid-forming diuretics, the diuretic effect decreases.

With the simultaneous use of Diakarb® increases the risk of manifestation of the toxic effects of salicylates, digitalis preparations, carbamazepine, ephedrine, non-depolarizing muscle relaxants.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

List B. The drug should be stored in a dry, dark place and out of the reach of children at a temperature not exceeding 25°C. Shelf life - 5 years.

Acetazolamide (Latin name Acetazolamide) is a drug with diuretic properties. The drug is used to treat edema caused by fluid retention and sodium salts in the body. The drug is used as part of the treatment of increased intraocular and intracranial pressure and epilepsy. In patients, blood pressure, the activity of the heart and kidneys are normalized as a result of the action of Acetazolamide. The trade name of the drug is Diakarb.

Composition and form of release

The composition of the drug includes 250 mg of the active substance acetazolamide, as well as auxiliary components: sodium glycolate, potato starch, talc.

The active substance is a white powder with a crystalline structure, odorless. Acetazolamide is poorly soluble in water.

The drug has a diuretic, antiglaucoma, antiepileptic action. The active substance inhibits the production of carbonic anhydrase in the kidneys. As a result, there is an increase in diuresis, an increase in the level of acidity of the urine and the reabsorption of ammonia. A decrease in the amount of carbonic anhydrase helps to reduce the secretion of intraocular fluid and lower intraocular pressure.

The drug is rapidly absorbed from the gastrointestinal tract and enters the systemic circulation. The maximum amount of the active substance in the blood plasma is observed after two hours. The action of the drug begins 60-90 minutes after administration. After 4 hours, the remains of the drug are excreted from the body along with urine.

Instructions for use Acetazolamide

The instruction prescribes the main diseases for the treatment and prevention of which the drug is used:

Acetazolamide is for oral use. The medicine is taken one tablet once a day or in courses of 2-4 days every other day. With longer use or increase in dose, a decrease in the diuretic effect may be observed. To relieve edematous syndrome, the drug is taken one tablet in the morning. For maximum diuretic action, medicine should be used daily or for two days with a break of one day.

In glaucoma, Acetazolamide is used strictly according to the doctor's prescription in the complex treatment of the disease.

Adult patients are prescribed 250 mg of the drug up to 4 times a day. In some cases, the therapeutic effect occurs after a short use of the drug.

For the treatment of children after three years, the dose of the drug depends on the body weight of the child and is 10 mg per kilogram of body weight 3-4 times a day. 5 days after the start of treatment, you need to take a break . Prolonged use of the product requires additional potassium supplements and a potassium-sparing diet.

Before surgery Acetazolamide is taken the day before surgery and on the day of surgery.

In the treatment of epilepsy, the drug is taken one tablet for three days. Sharing with other anticonvulsants, if necessary, requires a gradual increase in dose.

To relieve symptoms of mountain sickness, 500 mg of the drug is prescribed, and in case of rapid ascent, the dose can be increased to 1000 mg. The medicine begins to be taken 24 hours before the start of the ascent. In case of manifestation of symptoms of the disease, the drug is continued for the next 48 hours. If necessary, longer use of the drug is allowed.

In case of increased intracranial pressure, the drug should be taken every 8 hours. The maximum therapeutic dose should not exceed 750 mg per day.

In the event of a patient showing skin reactions should stop taking the medicine and seek the advice of a doctor.

Long-term use of the drug requires constant monitoring of the clinical picture of peripheral blood.

If the dose is increased, the patient experiences weakness and drowsiness, while the diuretic effect of the drug does not increase, and in some cases decreases. In heart failure, acetazolamide is very often used with other diuretics to provide more diuresis. If a dose is missed, do not increase the next dose.

Currently, there are no data from clinical studies on the effect of the drug on fetal development, so treatment with Acetazolamide in the first trimester of pregnancy is not carried out. The use of the drug at a later date is carried out strictly according to the doctor's prescription in case of emergency. To avoid the risk of harm to the child, constant monitoring of blood pressure and the activity of the internal organs of a woman is necessary.

It is known that active the substance can pass into breast milk Therefore, the medicine is not used during breastfeeding.

When using Acetazolamide in childhood, the dosage is adjusted by a pediatric neurologist on an individual basis, taking into account the age and severity of the child's condition. As a rule, the duration of the course of treatment does not exceed three days. The drug is taken in the morning. Usually, Acetazolamide is prescribed together with Asparkam, which is a complementary agent and replenishes the destructive effect of Acetazolamide.

Contraindications and side effects

The instruction prohibits the use of the drug if the following diseases are diagnosed in patients:

Acetazolamide is a low-toxic drug, and therefore short-term use does not cause side effects.

Prolonged use of the product can cause myopia, weakness, drowsiness, tingling sensations in the extremities, headache and dizziness, nausea, vomiting, stool disturbance. Some patients experience a violation of taste sensations, a decrease or loss of appetite, irritability. In more severe cases, the development of a depressive state, the development of phobias, confusion of consciousness is possible.

In the case of the development of metabolic acidosis, patients are prescribed corrective therapy with sodium preparations.

In rare cases, acetazolamide can cause the rapid development of aplastic anemia, leukopenia, agranulocytosis, pancytopenia, crystalluria, renal colic, reduced bone marrow activity, liver tissue necrosis.

Analogues and price

If the use of the drug for any reason is not possible, you should seek the advice of a specialist who will prescribe an analog similar in action to Acetazolamide. Diacrab has similar properties. The drug has no other analogues.

You can buy the drug at a pharmacy with a doctor's prescription. The average price for a package of medicine is from 250 rubles.

pharmachologic effect

Weak diuretic. Inhibits carbonic anhydrase in the proximal convoluted tubule of the nephron, increases the excretion of Na +, K +, bicarbonate in the urine, does not affect the excretion of Cl-, alkalinizes the urine. Violates KOS (metabolic acidosis). Inhibition of carbonic anhydrase in the ciliary body leads to a decrease in the secretion of aqueous humor and a decrease in intraocular pressure. The ability to suppress the activity of carbonic anhydrase in the brain determines the presence of some antiepileptic activity in the drug. Reduces the formation of cerebrospinal fluid and reduces intracranial pressure. Duration of action - up to 12 hours.
Pharmacokinetics

Absorption is high, Cmax in the blood is 2 hours after taking a dose of 500 mg. Penetrates through the placental barrier. Communication with plasma proteins is high. Excreted by the kidneys unchanged.
Indications for use

Edema syndrome (mild and moderate severity, in combination with alkalosis). Cranial hypertension; glaucoma (primary and secondary, acute attack), epilepsy (small epileptic seizures in children, rare absences), altitude sickness, Meniere's disease, tetany, premenstrual syndrome, gout.
Contraindications

Hypersensitivity, acute renal failure, liver failure, hypokalemia, acidosis, hypocorticism, Addison's disease, uremia, diabetes mellitus, pregnancy (I trimester).
Carefully

Edema of hepatic and renal genesis.
Dosing regimen

inside. With edematous syndrome - 250 mg 1-2 times a day in courses of 5 days, followed by a two-day break. With epilepsy - 250-500 mg / day in one dose for 3 days, on the 4th day a break. With an attack of glaucoma, the initial dose is 250-500 mg; then every 6 hours, 250 mg, after 1-2 days, gradually reduce the frequency of administration, first to 3, then to 2 times a day. Children 4-12 months - 50 mg / day in 1-2 doses; 3-5 years - 50-125 mg / day in 1-2 doses; 4-18 years - 125-250 mg once in the morning. In chronic glaucoma - 125-250 mg 1-3 times a day for 5 days.
Side effect

Hypokalemia, myasthenia gravis, convulsions, skin flushing, paresthesia, tinnitus, decreased appetite, metabolic acidosis, pruritus.

With prolonged use - nephrourolithiasis, hematuria, glucosuria, hemolytic anemia, leukopenia, agranulocytosis, disorientation, impaired sense of touch, drowsiness, nausea, vomiting, diarrhea, allergic reactions, paresthesia.
Interaction

Enhances the manifestations of osteomalacia caused by taking antiepileptic drugs.

Dr. diuretics and theophylline enhance the severity of the diuretic effect of acetazolamide, acid-forming diuretics weaken.

GCS increase the risk of developing hypokalemia.

Increases the toxicity of salicylates, digitalis preparations, carbamazepine, ephedrine and non-polarizing muscle relaxants.
special instructions

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

With prolonged use, it is necessary to control the water-electrolyte balance, the picture of peripheral blood, CBS.

Formula: C4H6N4O3S2, chemical name: N-acetamide.
Pharmacological group: metabolites/enzymes and antienzymes; organotropic agents / agents that regulate the function of the organs of the genitourinary system and reproduction / diuretics; neurotropic drugs / antiepileptic drugs.
Pharmachologic effect: diuretic, inhibitory carbonic anhydrase, antiepileptic, antiglaucoma.

Pharmacological properties

Acetazolamide inhibits (selectively) the enzyme carbonic anhydrase (is a catalyst for the reversible reaction of carbon dioxide hydration and further decomposition of carbonic acid). The diuretic effect of acetazolamide is associated with inhibition of carbonic anhydrase activity in the kidneys (mainly in the proximal tubules of the kidneys). This leads to a decrease in the reabsorption of K+, Na+, bicarbonate ions, an increase in diuresis, an increase in urine pH, and an increase in ammonia reabsorption. Acetazolamide does not affect the excretion of Cl- ions. Inhibition of carbonic anhydrase in the ciliary body by acetazolamide reduces the secretion of aqueous humor, which leads to a decrease in intraocular pressure. A decrease in the activity of carbonic anhydrase in the brain by acetazolamide leads to inhibition of paroxysmal excessive discharges of neurons and causes antiepileptic activity.

After oral administration, acetazolamide is well absorbed from the gastrointestinal tract. After 2 hours, the maximum concentration is reached in the blood. Acetazolamide crosses the placenta and is excreted in breast milk in small amounts. Acetazolamide is not biotransformed, therefore it is excreted unchanged by the kidneys. The duration of action of acetazolamide is up to 12 hours. In experimental animal studies (rats, mice, rabbits, hamsters), acetazolamide has shown embryotoxic and teratogenic effects at doses that are 10 times the MRDC.

Indications

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

Method of administration of acetazolamide and dose

Acetazolamide is taken orally. In glaucoma, the dose, depending on intraocular pressure, is set individually, the average doses are 1-3 times a day, 125-250 mg every other day for 5 days, then a break of 2 days. Edema - 250 - 375 mg per day in the morning; the maximum diuretic effect develops when taking the drug for 2 days in a row with a break of one day or taking the drug every other day. Epilepsy, for adults - 1 time per day 250 - 500 mg for 3 days, take a break on the fourth day; for children, the dose is set depending on body weight, taken in 1-2 doses; when sharing acetazolamide with anticonvulsants, the initial dose of acetazolamide is 250 mg once a day (the dose is increased if necessary); for children: do not use doses greater than 750 mg per day. With mountain sickness - 2-3 times a day, 250 mg, the reception should be started 1-2 days before the ascent and continue for 2 days (if necessary - longer).

With hypersensitivity to sulfonamides, the following severe adverse reactions may occur: anaphylaxis, rash (including erythema multiforme exudative, toxic epidermal necrolysis, Stevens-Johnson syndrome), fever, crystalluria, bone marrow depression, kidney stones, thrombocytopenic purpura, leukopenia, hemolytic anemia, agranulocytosis, pancytopenia. In case of development of changes in the picture of the blood or skin changes, the use of acetazolamide should be urgently canceled. During prolonged use, it is necessary to control the content of electrolytes in the blood serum, as well as to monitor the picture of peripheral blood. Acetazolamide, which is used in higher doses than recommended, does not increase diuresis, but often, on the contrary, reduces it, along with this, it increases paresthesia and/or drowsiness. But in some circumstances, acetazolamide is used in very high doses along with other diuretics to provide reliable diuresis in completely refractory heart failure. It is not recommended to use acetazolamide for drivers of vehicles during work, as well as for people whose activities are associated with increased concentration.

Contraindications for use

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

Application restrictions

Emphysema and pulmonary embolism (due to the possibility of increased acidosis), pregnancy.

Use during pregnancy and lactation

The use of acetazolamide during pregnancy (especially in the 1st trimester) is not recommended, in each individual case it is necessary to evaluate the expected benefit of treatment for the mother and the possible risk to the fetus. During therapy with acetazolamide, breastfeeding should be discontinued.

Side effects of acetazolamide

Sense organs and nervous system: drowsiness, tinnitus or hearing impairment, taste disturbance, disorientation, transient myopia, convulsions, paresthesia;
digestive system: loss of appetite, diarrhea, nausea, melena, vomiting, liver failure; metabolism: electrolyte imbalance and metabolic acidosis (with prolonged use);
others: polyuria, urticaria, hematuria, hypersensitivity to light, glucosuria.

Interaction of acetazolamide with other substances

The diuretic effect of acetazolamide is weakened by acid-forming diuretics, enhanced by theophylline. With the combined use of acetazolamide, the likelihood of developing toxic reactions of carbamazepine, digitalis preparations, ephedrine, salicylates, non-depolarizing muscle relaxants. Acetazolamide potentiates the manifestations of osteomalacia, which are caused by taking antiepileptic drugs. Care must be taken when sharing acetazolamide and high doses of acetylsalicylic acid because of the possibility of developing tachypnea, anorexia, coma, lethargy and death.