Diakarb: instructions for use of the drug

Pharmacological action, pharmacodynamics and pharmacokinetics

The main therapeutic effects of the drug:

Decongestant.
Diuretic.

The drug inhibits the enzyme carbonic anhydrase, which affects water and sodium metabolism in the body. As a result, Diacarb helps eliminate edema of various origins, relieve an attack of acute glaucoma and compensate for the manifestations of a number of other conditions.

By participating in water-salt metabolism, the drug does not affect pH and does not disturb the acid-base balance. The duration of action is no more than 12 hours.

The maximum concentration of Diacarb is achieved in the blood 2 hours after its administration. It has a high ability to bind to protein structures of blood plasma. Able to overcome the placental barrier.

The drug is not metabolized in the body and is excreted in its original form by the kidneys within 24 hours.

Diacarb®

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 determined by the point of application of the molecule: the choroid plexuses of the brain, the proximal nephron, the ciliary body of the eye, red blood cells.

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

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 tubular epithelium, and therefore the release of water significantly increases. Acetazolamide increases the excretion of bicarbonates, which can lead to the development of metabolic acidosis. Acetazolamide causes the kidneys to excrete phosphates, magnesium, and calcium, which can also lead to metabolic disorders. Over the next three 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 use, acetazolamide loses its diuretic properties. After a break in treatment for several days, newly prescribed acetazolamide resumes its diuretic effect due to the restoration of normal carbonic anhydrase activity in the proximal nephron.

Acetazolamide is used to treat glaucoma. During the formation of aqueous humor of the eye, bicarbonate ions are actively transported into 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.

CA inhibitors block the formation of carbonic acid, thus reducing the production of HCO3-. In the absence of sufficient 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 in the anterior chamber of the eye, which reduces intraocular pressure. Tolerance to this effect does not develop. Iphthalmotonus 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 adjuvant in the treatment of epilepsy, because inhibition of carbonic anhydrase in nerve cells of the brain inhibits pathological excitability.

Indications and contraindications

The following is a list of indications for the use of Diacarb:

Edema of any origin (with mild or moderate severity).
Acute attack of primary glaucoma.
Epilepsy (as part of complex treatment of the disease).
Pathology of the respiratory system, characterized by the accumulation of carbon dioxide and bicarbonate compounds in the blood plasma.
Mountain sickness.

The drug is strictly prohibited for use in the following conditions:

Individual intolerance to one or more components of the drug.
Acidosis.
Diabetes mellitus type 1 and 2.
Addison's disease.
Acute or chronic liver and kidney failure.
Pregnancy.
Lactation.
Decreased potassium concentration in the blood.

Diacarb 250 mg No. 30 tablet.

Instructions for medical use of the drug DIAKARB Trade name Diakarb International nonproprietary name Acetazolamide Dosage form Tablets 250 mg Composition One tablet contains the active substance: acetazolamide 250 mg excipients: microcrystalline cellulose, povidone, colloidal silicon dioxide, croscarmellose sodium, magnesium stearate. Description Tablets are white, round, biconvex. Pharmacotherapeutic group Drugs for the treatment of eye diseases. Antiglaucoma drugs and miotics. Carbonic anhydrase inhibitors. Acetazolamide. ATC code S01EC01 Pharmacological properties Pharmacokinetics Acetazolamide is well absorbed from the gastrointestinal tract. After oral administration at a dose of 500 mg, the maximum concentration (12-27 mcg/ml) is reached within 1-3 hours. In minimal concentrations it is retained in the blood for 24 hours from the moment of administration. Acetazolamide penetrates the placental barrier and passes into breast milk in small quantities. Does not accumulate in tissues and is not metabolized in the body. It is excreted unchanged by the kidneys. After oral administration, about 90% of the dose taken is excreted in the urine within 24 hours. Pharmacodynamics Acetazolamide is a potent carbonic anhydrase inhibitor with weak diuretic activity. The mechanism of action is associated with inhibition of the release of Na+ and H+ ions in the carbonic acid molecule. Inhibition of carbonic anhydrase activity by acetazolamide suppresses the synthesis of carbonic acid in the proximal tubule of the nephron. The lack of carbonic acid, which is a source of H+ ions necessary for replacement with Na+ ions, increases the excretion of sodium and water by the kidneys. As a result of the release of large amounts of sodium in the distal part of the nephron, caused by acetazolamide, the replacement of Na+ ions with K+ ions increases, which leads to large losses of potassium and the development of hypokalemia. Acetazolamide increases bicarbonate excretion, which can lead to the development of metabolic acidosis. Acetazolamide causes the excretion of phosphates, magnesium, and calcium in the urine, which can also lead to metabolic disorders. After 3 days from the start of use, acetazolamide loses its diuretic properties. After a break in treatment for several days, newly prescribed acetazolamide resumes its diuretic effect due to the restoration of normal carbonic anhydrase activity. The extrarenal action of acetazolamide is used to treat glaucoma. Inhibition of carbonic anhydrase of the ciliary body reduces the secretion of aqueous humor in the anterior chamber of the eye, which lowers intraocular pressure. The drug is used as an adjuvant in the treatment of epilepsy. Inhibition of carbonic anhydrase in nerve cells of the brain inhibits pathological excitability. Acetazolamide is used to treat CSF leaks and intracranial hypertension. The drug suppresses the activity of carbonic anhydrase in the brain, in particular in the ventricular plexuses, with a decrease in the production of cerebrospinal fluid. Acetazolamide changes the acid-base state towards metabolic acidosis, which is used to treat respiratory disorders, including central sleep apnea. Indications for use - edema syndrome, including heart failure, edema caused by drugs and (mild and moderate severity, in combination with alkalosis) - chronic open-angle glaucoma, secondary glaucoma, closed-angle glaucoma (to reduce intraocular pressure during short-term preoperative treatment and before ophthalmological procedures , capable of triggering an acute attack of angle-closure glaucoma) - epilepsy (in combination with other anticonvulsants) with petit mal seizures in children and grand mal seizures in adults, with mixed forms - increased intracranial pressure (benign intracranial hypertension, intracranial hypertension after ventricular bypass). Method of administration and dosage The drug is taken orally. If you miss a dose of the drug, do not increase the dose at the next dose. Edema syndrome The initial dose of the drug is 250 - 375 mg (1 - 1½ tablets) 1 time per day in the morning. If the patient's edema does not improve after the initial dose, increasing the dose is not recommended. The maximum diuretic effect is achieved when taking the drug every other day or two days in a row, then a one-day break. In the treatment of heart failure, Diacarb is prescribed against the background of conventional therapy (for example, the administration of cardiac glycosides, potassium supplements, a diet with a reduced sodium content). Glaucoma The dose of the drug should be determined individually in accordance with the value of intraocular pressure. Open-angle glaucoma: 250 mg (1 tablet) 1 - 4 times a day. Doses above 1000 mg (4 tablets) do not increase the therapeutic effect. Secondary glaucoma: 250 mg (1 tablet) every 4 hours. In some patients, the therapeutic effect appears after a dose of 250 mg (1 tablet) 2 times a day (with short-term therapy). Epilepsy Dosage for adults: 250 – 500 mg/day in one dose for 3 days, break on the 4th day. When using acetazolamide simultaneously with other anticonvulsants, at the beginning of treatment, use 250 mg (1 tablet) 1 time per day, gradually increasing the dose if necessary. Dosages in children: 2 – 3 years: 50 – 125 mg/day in 1 – 2 doses; 4 – 18 years: 125 – 250 mg once in the morning. In children, doses higher than 750 mg per day should not be used. Intracranial hypertension It is recommended to use Diacarb at a dose of 250 mg (1 tablet) per day or 125 -250 mg (1/2 - 1 tablet) every 8 -12 hours. The maximum therapeutic effect is achieved when taking a dose of 750 mg (3 tablets) per day in equal doses. If repeated lumbar punctures are ineffective, it is possible to use the drug at a dosage of 500 mg 3 times a day. Side effects - paresthesia, hearing loss or tinnitus, drowsiness and disorientation, flaccid paralysis, photophobia - loss of appetite, nausea, vomiting, diarrhea, taste disturbance, thirst, diarrhea, polyuria, melena - metabolic acidosis and electrolyte imbalance - temporary myopia - urticaria, anaphylaxis, anaphylactic shock - hepatic colic, hepatitis, cholestatic jaundice, liver failure up to fulminant liver necrosis - renal colic, hepatic and renal failure - crystalluria, nephrolithiasis, urolithiasis, hematuria, glycosuria - elevated temperature - headache, dizziness , fatigue, irritability, depression, decreased libido, drowsiness - hearing loss and ringing in the ears - hematuria, glycosuria, agranulocytosis, thrombocytopenia, leukopenia and aplastic anemia, platelet purpura, bone marrow failure, pancytopenia, rash in the form of erythema multiforme - Stevens syndrome - Johnson, Lyell's syndrome. Contraindications - hypersensitivity to the components of the drug or to sulfonamides - with reduced levels of sodium and potassium in the blood serum - impaired liver and kidney function - adrenal insufficiency - hyperchloremic acidosis - chronic decompensated angle-closure glaucoma (in long-term therapy) - urolithiasis - pregnancy and lactation Drug interactions Acetazolamide may enhance the effects of folic acid antagonists, hypoglycemic agents and oral anticoagulants. The simultaneous use of acetazolamide and acetylsalicylic acid can cause severe acidosis and increase toxic symptoms from the central nervous system. During concomitant use of digitalis glycosides or drugs that increase blood pressure, it is necessary to modify the dosage of acetazolamide. Acetazolamide alters the metabolism of phenytoin, increasing its serum concentration. Severe osteomalacia has been observed in several patients taking acetazolamide concomitantly with certain anticonvulsants (phenytoin, primidone). Concomitant use of acetazolamide with amphetamines, atropine or quinidine may increase their side effects. Acetazolamide may increase or decrease blood glucose concentrations, which should be taken into account when treating diabetes mellitus. Dosage adjustments to insulin or oral hypoglycemic agents may be necessary. Acetazolamide increases the excretion of lithium and may reduce its effect. Acetazolamide may increase plasma concentrations of carbamazepine and cyclosporine. Acetazolamide may reduce the antiseptic effect of methenamine in urology. The simultaneous administration of acetazolamide and sodium bicarbonate increases the risk of kidney stones. Special instructions The drug can cause acidosis, so it should be used with caution in patients with pulmonary embolism and emphysema. The drug alkalizes urine. Acetazolamide should be used cautiously in patients with diabetes mellitus due to the increased risk of hyperglycemia. Increasing the dose does not increase urine output, but may increase the incidence of drowsiness and/or paresthesia. Special precautions are recommended when planning long-term therapy with acetazolamide. The patient should be warned to consult a doctor if any unusual skin rash appears. It is recommended to monitor blood and platelet counts at the beginning of treatment and regularly during treatment, as well as regularly monitor water-electrolyte and acid-base balance. If there is a sharp decrease in the number of formed elements of blood cells or the appearance of toxic skin manifestations, it is necessary to immediately stop therapy with acetazolamide. The behavior of patients taking acetazolamide should be monitored due to the possibility of depressive episodes with suicidal thoughts. Caution should be exercised in elderly patients due to the risk of urinary tract obstruction. Features of the effect of the drug on the ability to drive vehicles and maintain moving mechanisms While taking the drug, patients should not drive vehicles or work with mechanisms that require increased concentration and speed of psychomotor reactions. Overdose Symptoms: increased symptoms of side effects. Treatment: symptomatic. In case of acidosis, bicarbonates are used. Hemodialysis removes acetazolamide from the body. Release form and packaging 10 tablets in a blister pack, made of polyvinyl chloride film and aluminum foil. 3 blister packs together with instructions for medical use in the state and Russian languages are placed in a cardboard box. Storage conditions Store in a dry place, protected from light, at a temperature not exceeding 25°C. Keep out of the reach of children. Shelf life: 5 years Do not use after expiration date. Conditions for dispensing from pharmacies By prescription Manufacturer/packer Pharmaceutical JSC, Poland Owner of the registration certificate "Khimpharm" JSC, Kazakhstan Address of the organization that accepts claims from consumers on the quality of products (products) in the territory of the Republic of Kazakhstan Khimpharm JSC, Republic of Kazakhstan, Shymkent , st. Rashidova, 81, tel/fax +7 7252 (561342) email address [email protected]

Side effects and clinical manifestations of overdose

Short-term use of Diacarb can provoke the development of hypokalemia, paresthesia and limb cramps, muscle weakness, acidosis, visual and auditory disturbances, appetite disorders, itching, and an allergic reaction such as urticaria.

Long-term treatment with the drug causes drowsiness, dyspeptic syndrome, hemolytic anemia, leukopenia and agranulocytosis in some patients.

Overdose symptoms are similar to adverse reactions. Treatment is symptomatic. Immediate discontinuation of the drug and contact a doctor is necessary.

Instructions for use Diacarb

The daily dosage and treatment regimen may vary. Features of admission depend on the presence of concomitant diseases, the age of the patient, as well as the type and severity of the underlying pathology.

For mild and moderate swelling, you should take 250 to 400 mg of the drug per day once.

For the treatment of an acute attack of glaucoma, adult patients are prescribed 250 milligrams of Diacarb every 4 hours. For pediatric patients, the dosage is calculated at 10-15 mg per kilogram of weight.

To prevent mountain sickness, it is recommended to take 500 mg of the drug 1-2 days before and during the ascent.

For patients with epilepsy, Diacarb is prescribed in a dosage of 250 to 500 mg per day for three days.

Reviews about the medication

Reviews from patients and doctors about the drug Diacarb are very different, both positive and negative.

Most patients note the high effectiveness of the drug, as well as its affordable cost.

Some patients speak negatively about Diakarb. For some it did not help at all, but for others it caused undesirable reactions, due to which they had to stop taking the drug. Most often, patients experience severe muscle weakness and cramps as a result of hypokalemia.

On thematic forums, the question often arises about the possibility of treatment with Diacarb during pregnancy and lactation. Currently, medical professionals do not prescribe it to expectant and nursing mothers, since there is no reliable data on the safety of its use in this category of patients.

Diakarb

Acetazolamide is a carbonic anhydrase inhibitor with weak diuretic activity. The mechanism of action is associated with inhibition of the release of sodium (Na+) and hydrogen (H+) ions in the carbonic acid molecule. Inhibition of carbonic anhydrase activity by acetazolamide suppresses carbonic acid synthesis in the proximal nephron tubule. The lack of carbonic acid, which is a source of H+ ions needed to be replaced by Na+ ions, increases the excretion of sodium and water by the kidneys. As a result of the release of large amounts of sodium in the distal part of the nephron, caused by acetazolamide, the replacement of Na+ ions with potassium ions (K+) increases, which leads to large losses of K+ and the development of hypokalemia. Acetazolamide increases the excretion of bicarbonates, which can lead to the development of metabolic acidosis. Acetazolamide causes the kidneys to excrete phosphates, magnesium, and calcium, which can also lead to metabolic disorders.

Acetazolamide is used to treat glaucoma. Inhibition of carbonic anhydrase of the ciliary body reduces the secretion of aqueous humor in the anterior chamber of the eye, which reduces intraocular pressure. Tolerance to this effect does not develop. Iphthalmotonus 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% of 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.

Acetazolamide is used to treat CSF leaks and intracranial hypertension. The drug suppresses the activity of carbonic anhydrase in the brain, in particular in the choroid plexus of the ventricles, with a decrease in the production of cerebrospinal fluid.

Pharmacokinetics

Suction

After oral administration, acetazolamide is well absorbed from the gastrointestinal tract. After taking Diacarb at a dose of 500 mg, the Cmax of the active substance is 12-27 mcg/ml and is achieved after 1-3 hours. The minimum concentration of acetazolamide in plasma remains for 24 hours after taking the drug.

Distribution and metabolism

Distributed mainly in red blood cells, kidneys, muscles, eyeball tissues and the central nervous system. Penetrates the placental barrier and is excreted in small amounts in breast milk.

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

Removal

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