Diacarb (acetazolamide) 250 mg, 30 pcs.

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.

Acetazolamide is a systemic carbonic anhydrase inhibitor with weak diuretic activity. Carbonic anhydrase (CA) is an enzyme involved in the hydration of carbon dioxide and dehydration of carbonic acid. Inhibition of carbonic anhydrase reduces the formation of bicarbonate ions with a subsequent decrease in sodium transport into cells. The effects of using the drug Diacarb ^{® are}  due to the point of application of the molecule: the vascular plexus of the brain, the proximal nephron, the ciliary body of the eye, erythrocytes.

Acetazolamide is used to treat cerebrospinal fluid disorders and intracranial hypertension by reducing excess cerebrospinal fluid production at the level of the vascular plexus of the brain. Inhibition of carbonic anhydrase in the ependymocytes of the choroid plexus lowers the excess negative charge in the cells of the ependyma and reduces the gradient filtration of plasma into the cavity of the cerebral ventricles.

Acetazolamide is used in the treatment of edema syndrome due to its weak diuretic effect. As a result of inhibition of carbonic anhydrase activity in the proximal nephron, there is a decrease in the formation of carbonic acid and a decrease in the reabsorption of bicarbonate and Na ^{+ by the}  epithelium of the tubules, in connection with which the release of water significantly increases. Acetazolamide increases the excretion of hydrocarbons, which can lead to the development of metabolic acidosis. Acetazolamide causes the excretion of phosphates, magnesium, calcium by the kidneys, which can also lead to metabolic disorders. During the next 3 days of therapy, Na ⁺ reabsorption  in the distal nephron is compensatory activated , reducing the diuretic effect of Diacarb ^® .

After 3 days from the start of application, acetazolamide loses its diuretic properties. After a break in treatment for several days, the newly prescribed acetazolamide resumes the diuretic effect due to the restoration of the normal activity of carbonic anhydrase of the proximal nephron.

Acetazolamide is used to treat glaucoma. During the formation of aqueous humor of the eye, bicarbonate ions are actively transported to the posterior chamber from the cytoplasm of pigmented cells in order to compensate for the positive ion gradient caused by the active transport of Na ⁺ ions . CA inhibitors block the formation of carbonic acid, thus reducing the production of HCO ₃ ^- . In the absence of a sufficient amount of НСО ₃ ^-the positive ionic gradient increases, which causes a decrease in the secretion of aqueous humor. Inhibition of ciliary body carbonic anhydrase reduces the secretion of aqueous humor in 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 effect 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 adjuvant in the treatment of epilepsy, because inhibition of carbonic anhydrase in nerve cells of the brain inhibits pathological excitability.

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

The drug is taken orally, strictly according to the doctor's prescription.

If you skip taking the drug, you should not increase the dose with the next dose.

Edematous syndrome

At the beginning of treatment, take 250 mg in the morning. To achieve the maximum diuretic effect, it is necessary to take Diacarb ^®  1 time / day every other day or 2 days in a row with a one-day break. Increasing the dose does not increase the diuretic effect.

Glaucoma

Diacarb ^®  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 exceeding 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 a short-term intake of the drug at a dose of 250 mg 2 times / day. In acute attacks of glaucoma - 250 mg 4 times / day.

Children over 3 years old with attacks of glaucoma - 10-15 mg / kg body weight / day in 3-4 doses.

After 5 days of admission, take a break for 2 days. With long-term treatment, it is necessary to prescribe potassium preparations, a potassium-sparing diet.

In preparation for the operation, appoint 250-500 mg the day before and in the morning of the operation.

Epilepsy

Doses for adults: 250-500 mg / day in 1 dose for 3 days, on the 4th day a break.

With the simultaneous use of acetazolamide with other anticonvulsants at the beginning of treatment, 250 mg is used 1 time / day, gradually increasing the dose if necessary.

Doses for children over 3 years old: 8-30 mg / kg / day, divided into 1-4 doses. The maximum daily dose is 750 mg.

Acute altitude illness

It is recommended to use the drug in a dose of 500-1000 mg / day. In the case of a rapid ascent - 1000 mg / day.

The drug should be used 24-48 hours before the ascent. In the event of symptoms of the disease, treatment is continued for the next 48 hours or longer if necessary.

CSF disorders, intracranial hypertension

It is recommended to use the drug in a dose of 250 mg / day or 125-250 mg every 8-12 hours. The maximum therapeutic effect is achieved when taking a dose of 750 mg / day. To achieve optimal therapeutic effect, daily non-interval drug intake may be required.

• acute renal failure;
• uremia;
• liver failure (risk of developing encephalopathy);
• hypokalemia;
• hyponatremia;
• metabolic acidosis;
• hypocorticism;
• Addison's disease;
• diabetes;
• I trimester of pregnancy;
• lactation period;
• children under 3 years old;
• hypersensitivity to drug components.

With care: edema of hepatic and renal genesis, simultaneous administration with acetylsalicylic acid (doses over 300 mg / day), pulmonary embolism and pulmonary emphysema (risk of acidosis), II and III trimesters of pregnancy.

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 rare (<1/10 000), frequency unknown (cannot be determined from available data).

From the hematopoietic system: rarely - aplastic anemia, thrombocytopenia, agranulocytosis, leukopenia, thrombocytopenic purpura, myelosuppression, pancytopenia.

From the immune system: the frequency is unknown - anaphylactic reactions.

From the side of metabolism and nutrition: often - decreased appetite, taste disturbances, metabolic acidosis, metabolic acidosis and electrolyte disturbances (usually can be corrected by the appointment of bicarbonate); infrequently - thirst; rarely - glucosuria; frequency unknown - hypokalemia, hyponatremia.

Mental disorders: infrequently - depression, irritability; frequency unknown - agitation, confusion, disorientation.

From the nervous system: often - dizziness, paresthesia, 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 completely disappeared with a dose reduction or drug withdrawal).

From the side of the organ of hearing: rarely - hearing impairment and ringing in the ears.

From the digestive system: infrequently - nausea, vomiting, diarrhea, melena; rarely - fulminant liver necrosis, liver dysfunction, hepatitis, cholestatic jaundice; frequency unknown - dry mouth, dysgeusia, hepatic failure, hepatic colic.

On the part of the skin and subcutaneous tissue: rarely - photosensitivity; frequency unknown - pruritus, rash, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria.

From the musculoskeletal system: the frequency is unknown - arthralgia.

From 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 genitals and breast: infrequently - decreased libido.

General disorders and disorders at the injection site: often - fatigue; infrequently - fever, weakness.

Acetazolamide can potentiate the action of folic acid antagonists, hypoglycemic agents, and oral anticoagulants.

The simultaneous use of acetazolamide and acetylsalicylic acid can cause metabolic acidosis and enhance toxic effects on the central nervous system.

When used together with cardiac glycosides or drugs that increase blood pressure, the dose of acetazolamide should be adjusted.

Acetazolamide increases serum phenytoin levels.

Acetazolamide enhances the manifestations of osteomalacia caused by taking antiepileptic drugs.

The simultaneous use of acetazolamide and amphetamine, atropine or quinidine may increase 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 action of ephedrine.

Increases plasma concentration of carbamazepine, non-depolarizing muscle relaxants.

Increases the excretion of lithium.

Overdose symptoms are not described. Probable symptoms of an overdose may be disturbances in water and electrolyte balance, metabolic acidosis, as well as disorders of the central nervous system.

Treatment: there is no specific antidote. Symptomatic and supportive therapy is performed. The content of electrolytes in the blood, especially potassium, sodium, and blood pH should be monitored. In case of metabolic acidosis, sodium bicarbonate is used. Acetazolamide is eliminated by hemodialysis.

Suction

Acetazolamide is well absorbed from the gastrointestinal tract. After taking the drug orally at a dose of 500 mg, C _{max of the} active substance is 12-27 μg / ml and is reached after 1-3 hours. The minimum concentration of acetazolamide in plasma is maintained for 24 hours after taking the drug.

Distribution and metabolism

It is distributed mainly in erythrocytes, blood plasma and in the kidneys, to a lesser extent in the liver, muscles, eyeball and central nervous system. Penetrates through the placental barrier, in a small amount excreted in breast milk.

Does not accumulate in tissues and is not metabolized in the body.

Withdrawal

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

In case of hypersensitivity to the drug, life-threatening side effects may appear, for example, Stevens-Johnson syndrome, Lyell's syndrome, fulminant liver necrosis, agranulocytosis, aplastic anemia, and hemorrhagic diathesis. In case of manifestation of these symptoms, you should immediately stop taking the drug.

Diacarb ^® , used in doses exceeding the recommended ones, does not increase urine output, may increase drowsiness and paresthesia, and sometimes also reduce urine output.

The drug can cause acidosis, so it should be used with caution in patients with pulmonary embolism and pulmonary emphysema.

The drug alkalizes the urine.

Diakarb ^®  should be used cautiously in patients with diabetes mellitus due to the increased risk of hyperglycemia.

If administered for more than 5 days, the risk of developing metabolic acidosis is high.

It is recommended to monitor blood counts and platelets at the beginning of treatment and at regular intervals during treatment, as well as periodic monitoring of serum electrolytes.

Influence on the ability to drive vehicles and use mechanisms

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