Diacarb, pills 250mg, 30pcs

Composition

Auxiliary substances:

microcrystalline cellulose – 80.76 mg,

povidone-8.64 mg,

colloidal silicon dioxide-1.8 mg,

croscarmellose sodium-7 mg,

magnesium stearate-1.8 mg

Pharmacological action

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 the dehydration of carbonic acid. Inhibition of carbonic anhydrase reduces the formation of bicarbonate ions, followed by a decrease in sodium transport into cells. The effects of using Diacarb® are determined by the point of application of the molecule: the vascular plexus of the brain, the proximal nephron, the ciliary body of the eye, and red blood cells.

Acetazolamide is used to treat CSF-dynamic disorders and intracranial hypertension by reducing excess CSF production at the level of the cerebral choroid plexuses. Inhibition of carbonic anhydrase in vascular plexus ependymocytes reduces the excess negative charge in ependymal cells and reduces the gradient filtration of plasma into the ventricular cavity of the brain.

Acetazolamide is used in the treatment of edematous syndrome due to a weak diuretic effect. As a result of inhibition of carbonic anhydrase activity in the proximal nephron, the formation of carbonic acid decreases and the reabsorption of bicarbonate and Na+ by the tubular epithelium decreases, which significantly increases the release of water. Acetazolamide increases the excretion of bicarbonates, which can lead to the development of metabolic acidosis. Acetazolamide causes the excretion of phosphates, magnesium, and 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 compensatorily activated, reducing the diuretic effect of Diacarb®.

After 3 days from the start of use, 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 normal activity of the proximal nephron carbonic anhydrase.

Acetazolamide is used to treat glaucoma. During the formation of watery eye moisture, bicarbonate ions are actively transported to the posterior chamber from the cytoplasm of non-pigmented cells to compensate for the positive ion gradient 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 amountof HCO3-ions, the positive ion gradient increases, which causes a decrease in the secretion of aqueous humor. Inhibition of carbonic anhydrase of the ciliary body 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 effect is observed after 3-5 hours, intraocular pressure remains below the initial level for 6-12 hours. On average, 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.

Indications

• edematous syndrome (mild or moderate symptoms, combined with alkalosis);
• relief of acute attack of glaucoma, preoperative preparation of patients, persistent cases of current glaucoma (in the complex therapy);
• epilepsy as adjunctive therapy to antiepileptic drugs;
• acute vysotnyy disease (drug reduces the time of acclimatization);
• liquorodynamic disorders, intracranial hypertension (intracranial hypertension, intracranial hypertension after bypass surgery ventricles) in the complex therapy.

Recommendations for use

The drug is taken orally, strictly as prescribed by a doctor.

If you miss taking the drug, do not increase the dose at 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 consecutive days with a one-day break. Increasing the dose does not increase the diuretic effect.

Glaucoma

Diacarb® should be taken as part of a 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 use of the drug at a dose of 250 mg 2 times a day. In acute attacks of glaucoma-250 mg 4 times / day.

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

After 5 days of admission, they 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,250-500 mg is prescribed the day before and in the morning on the day 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 of age: 8-30 mg / kg / day, divided into 1-4 doses. The maximum daily dose is 750 mg.

Acute “high-altitude” disease

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

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

Liquorodynamic disorders, intracranial hypertension

It is recommended to use the drug at 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 an optimal therapeutic effect, it may be necessary to take the drug daily without interruptions.

Contraindications

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

With caution:  edema of hepatic and renal origin, concomitant use with acetylsalicylic acid (doses greater than 300 mg / day), pulmonary embolism and emphysema of the lungs (risk of acidosis), II and III trimesters of pregnancy.

Side effects

Undesirable 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, <1/10); infrequently (><1/100); rarely (>1/10 000, <1/100); rarely (><1/1000); very rarely (

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

From the immune system:  frequency unknown – anaphylactic reactions.

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

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

Nervous system disorders:  often – dizziness, paresthesia, in particular a tingling sensation in the extremities; infrequently-hot flashes, headache; very rarely-drowsiness, peripheral paresis, convulsions; frequency unknown-ataxia.

From the side of the visual organ:  rarely-transient myopia (this condition completely disappeared when the dose was reduced or the drug was discontinued).

From the side of the hearing organ:  rarely – hearing disorders and ringing in the ears.

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

Skin and subcutaneous tissue disorders:  rarely-photosensitization; frequency unknown-pruritus, rash, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria.

Musculoskeletal disorders:  the frequency is unknown-arthralgia.

From the urinary system:  the frequency is unknown – kidney stone formation, crystalluria, renal and ureteral colic and kidney damage, polyuria, hematuria, and renal failure.

From the genitals and breast:  infrequently-decreased libido.

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

Interaction

Acetazolamide may enhance the effects of folic acid antagonists, hypoglycemic agents, and oral anticoagulants.

Concomitant use of acetazolamide and acetylsalicylic acid may 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 content of phenytoin in the blood serum.

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

Concomitant 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.

An increase in the hypotensive effect on intraocular pressure is possible when used simultaneously with cholinergic drugs and beta-blockers.

Acetazolamide enhances the effect of ephedrine.

Increases plasma concentrations of carbamazepine, a non-depolarizing muscle relaxant.

Increases the elimination of lithium.

Overdose

Overdose symptoms are not described. Possible symptoms of overdose may include impaired water-electrolyte balance, metabolic acidosis, and central nervous system disorders.

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

Description

Tablets are white, round, biconvex.

Functional features

Suction

Acetazolamide is well absorbed from the gastrointestinal tract. After oral use of the drug at a dose of 500 mg_{, the cmax}of the Active ingredient is 12-27 mcg/ml and is reached in 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 red blood cells, blood plasma and kidneys, to a lesser extent-in the liver, muscles, eyeball and central nervous system. It penetrates the placental barrier and is excreted in small amounts in breast milk.

It does not accumulate in tissues and is not metabolized in the body.

Deduction

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

Special instructions

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

Diacarb®, used in doses higher than recommended, does not increase diuresis, may increase drowsiness and paresthesia, and sometimes also reduce diuresis.

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

The drug alkalizes the urine.

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

If prescribed for more than 5 days, there is a high risk of developing metabolic acidosis.

Monitoring of blood and platelet counts is recommended 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 motor vehicles and manage 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 of attention and speed of psychomotor reactions.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Shelf

life is 5 years. Do not use the drug after the expiration date.

Active ingredient

Acetazolamide

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Epilepsy, Glaucoma