Diacarb (Acetazolamide) diuretic 250 mg 30 tablet

Composition Diacarb:

One tablet contains:
active substance: 
acetazolamide in terms of 100% substance - 250 mg;
excipients:
microcrystalline cellulose - 83.15 mg, 
povidone (type K90) - 6.25 mg, 
colloidal silicon dioxide - 1.8 mg,
croscarmellose sodium - 7 mg,
magnesium stearate - 1.8 mg.

Pharmacodynamics Diacarb:

Acetazolamide is a systemic carbonic anhydrase inhibitor with weak diuretic activity. Carbonic anhydrase (KA) is an enzyme involved in the process of hydration of carbon dioxide and 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 the use of the drug Diacarb are determined by the point of application of the molecule: the vascular plexuses of the brain, the proximal nephron, the ciliary body of the eye, red blood cells.

Acetazolamide is used to treat cerebrospinal fluid disorders and intracranial hypertension by reducing excess cerebrospinal fluid production at the level of the vascular plexuses of the brain. The inhibition of carbonic anhydrase in the ependymocytes of the vascular plexus reduces the excess negative charge in the 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 edematous syndrome due to a weak diuretic effect. As a result of the inhibition of the activity of carbonic anhydrase 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 tubule epithelium, and therefore, the release of water increases significantly. Acetazolamide/Diacarb increases the excretion of bicarbonates, which can lead to the development of metabolic acidosis. Acetazolamide causes the kidneys to excrete phosphates, magnesium, calcium, which can also lead to metabolic disorders.

Over the next three days of therapy, Na + reabsorption in the distal nephron is compensatoryly activated, reducing the diuretic effect of the drug 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 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 into the posterior chamber from the cytoplasm of non-pigment cells in order to compensate for the gradient of positive ions due to the active transport of Na + ions. Diacarb

CA inhibitors block the formation of carbonic acid, thus reducing the production of NS (V ~. In the absence of a sufficient amount of HCO3 ions, the positive ion gradient increases, which causes a decrease in the secretion of aqueous humor. Inhibition of the 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.

Ophthalmotonus when taking acetazolamide begins to decline after 40-60 minutes, the maximum action is observed after 3-5 hours, intraocular pressure remains below the initial level for 6-12 hours. On average, intraocular pressure is reduced 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 brain nerve cells inhibits pathological excitability.

Pharmacokinetics Diacarb:

Acetazolamide is well absorbed from the gastrointestinal tract. After oral administration in a dose of 500 mg, the maximum concentration (12-27 μg / ml) is achieved after 1-3 hours. In minimal concentrations, it is retained in the blood for 24 hours from the time of administration. Acetazolamide is distributed in red blood cells, blood plasma and in the kidneys, to a lesser extent - in the liver, muscles, eyeball and central nervous system.

Acetazolamide crosses the placental barrier, in a small amount excreted in breast milk. It does not accumulate in tissues and is not metabolized in the body. It is excreted by the kidneys unchanged. After oral administration, about 90% of the dose Diacarb taken is excreted by the kidneys within 24 hours.

Side effects Diacarb:

Undesirable effects are classified according to the frequency of occurrence and according to 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, <1/1 000); very rarely (<1/10 000), the frequency is unknown (cannot be determined on the basis of agranulocytosis, leukopenia, thrombocytopenic purpura, myelosuppression, pancytopenia.

Immune system disorders:
frequency unknown - anaphylactic reactions.
Violation of the metabolism and nutrition:
often - loss of appetite, taste disturbances, metabolic acidosis, metabolic acidosis and electrolyte disturbances (this can usually be corrected by prescribing bicarbonate); infrequently - thirst; rarely - glucosuria; frequency is unknown - hypokalemia, hyponatremia.

Mental disorders: infrequently - depression, irritability; frequency unknown - agitation, confusion, disorientation. Violations of the nervous system: often - dizziness, paresthesia, in particular a tingling sensation in the limbs; infrequently - hot flashes, headache; very rarely - drowsiness, peripheral paresis, convulsions; frequency unknown - ataxia. Diacarb

Violations of the organ of vision: rarely - transient myopia (this condition completely disappeared with a dose reduction or drug withdrawal). Hearing impairment and labyrinth disorders: rarely, hearing impairment and tinnitus. Violations of the gastrointestinal tract: infrequently - nausea, vomiting, diarrhea, melena; frequency unknown - dry mouth, dysgeusia.

Violations of the liver and biliary tract: rarely fulminant necrosis of the liver, impaired liver function, hepatitis, cholestatic jaundice; frequency unknown - liver failure, hepatic colic. Disorders from the skin and subcutaneous tissues: rarely - photosensitivity; frequency unknown - pruritus, skin rash, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria. Violations of the musculoskeletal and connective tissue: frequency unknown - arthralgia.

Disorders from the kidneys and urinary tract: the frequency is unknown - the formation of calculi in the kidneys, crystalluria, renal and ureteral colic and kidney damage, polyuria, hematuria, renal failure.

Violations of the genitals and mammary gland: infrequently - decreased libido. General disorders and disorders at the injection site: often - fatigue; infrequently - fever, weakness

Special conditions Diacarb:

In case of hypersensitivity to the drug Diacarb, life-threatening hypersensitivity reactions to acetazolamide (sulfonamides) 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 and consult a doctor. The drug Diakarb®, used in doses exceeding the recommended, does not increase diuresis, but can increase drowsiness and paresthesia, and sometimes also reduce diuresis.

When using acetazolamide for more than 5 days, the risk of developing metabolic acidosis is high. Acetazolamide should be used with caution in patients with bronchial obstruction and emphysema (conditions accompanied by impaired alveolar ventilation) due to the possibility of increased acidosis. Acetazolamide alkalizes urine.

In patients with a history of urolithiasis, a balance of the benefits of treatment and the risk of stone formation should be assessed. If transient hearing loss occurs, you should stop taking acetazolamide. The combined use of acetazolamide/Diacarb with high doses of acetylsalicylic acid (more than 300 mg per day) is not recommended due to the high risk of serious side effects.

In the treatment of epilepsy with specific antiepileptic drugs, there is a slight increase in the risk of suicidal ideation and suicidal behavior.

The mechanism of this phenomenon is unknown, but existing data do not exclude such a risk with the use of acetazolamide. Therefore, when using acetazolamide for the treatment of epilepsy, patients should be monitored, possible signs of suicidal behavior and thinking should be identified, and, if necessary, immediately seek medical help. Diacarb should be used with caution in patients with diabetes mellitus due to the increased risk of hyperglycemia. In case of administration for more than 5 days, the risk of developing metabolic acidosis is high.

It is recommended to monitor the picture of blood and platelets at the beginning of treatment, and at regular intervals during treatment, as well as periodic monitoring of electrolytes in blood serum. Impact on the ability to drive vehicles and mechanisms:

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

Indications Diacarb:

Edema 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 additional therapy for antiepileptic drugs;
• Acute altitude sickness (the drug reduces the time of acclimatization);
• Liquorodynamic disturbances, intracranial hypertension (benign intracranial hypertension, intracranial hypertension after ventricular bypass surgery) in complex therapy.

Contraindications Diacarb:

Hypersensitivity to acetazolamide/Diacarb (or other sulfonamides), as well as any other components of the drug; acute renal failure;
uremia;
liver failure (risk of developing encephalopathy); refractory hypokalemia and hyponatremia;
metabolic acidosis;
hypocorticism;
Addison's disease;
decompensated diabetes mellitus;
pregnancy (I trimester);
lactation period;
children's age up to 3 years (solid dosage form).

Precautions: Edema of hepatic and renal origin, simultaneous administration with acetylsalicylic acid (doses above 300 mg / day), pulmonary embolism and pulmonary emphysema (risk of acidosis), pregnancy (II and III trimester), old age, disturbance of water-electrolyte balance , impaired liver function, in patients at risk of urinary tract obstruction.

Use during pregnancy and during breastfeeding. During pregnancy, the drug Diacarb is contraindicated in the first trimester, and in the second and third trimesters it is used with caution and only in cases where the potential benefit to the mother outweighs the potential risk to the fetus. Acetazolamide in a small amount is excreted in breast milk, so if it is necessary to use the drug Diacarb, breastfeeding must be stopped.

Drug Interactions Diacarb:

Acetazolamide may enhance the effects 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 combined with cardiac glycosides or drugs that increase blood pressure, the dose Diacarb of acetazolamide should be adjusted. Acetazolamide increases the content of phenytoin in the blood serum. Acetazolamide enhances the manifestations of osteomalacia caused by the use of antiepileptic drugs.

The simultaneous use of acetazolamide and amphetamine, atropine or quinidine can enhance 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 with respect to intraocular pressure is possible with simultaneous use with cholinergic drugs and beta-blockers. Acetazolamide enhances the effects of ephedrine.

Increases the concentration in the blood plasma of carbamazepine, non-depolarizing muscle relaxants.
Acetazolamide may increase the concentration of cyclosporine. Increases lithium excretion. Acetazolamide may reduce the antiseptic effect of methenamine on the genitourinary system. The simultaneous use of acetazolamide and sodium bicarbonate increases the risk of kidney stones. Diacarb

Dosage Diacarb:

The drug Diacarb is taken orally, strictly as prescribed by the doctor. In case of missing the drug Diacarb, do not increase the dose at the next dose. • Edema syndrome At the beginning of treatment, 250 mg is taken in the morning.

To achieve the maximum diuretic effect, the necessary diuretic effect is necessary to take Diacarb once a day every other day or 2 days in a row with a one-day break. Increasing the dose does not enhance the diuretic effect. With a decrease in the previously achieved response to acetazolamide therapy, the drug should be discontinued for a day (to restore the activity of renal carbonic anhydrase).
The use of acetazolamide does not eliminate the need for other drugs, bed rest (if recommended by a doctor) and restrictions on the intake of sodium chloride. • Glaucoma Diacarb should be taken as part of complex therapy. For adults with open-angle glaucoma, the drug is prescribed in a dose Diacarb of 250 mg 1-4 times a day.

Doses in excess of 1000 mg do not increase the therapeutic effect. In secondary glaucoma, the drug is prescribed in a dose of 250 mg every 4 hours during the day. In some patients, the therapeutic effect is manifested after short-term administration of the drug in a dose of 250 mg 2 times a day. In acute attacks of glaucoma: 250 mg 4 times a day. Children older than 3 years with glaucoma attacks: 10-15 mg / kg body weight per day in 3-4 doses.
After 5 days of admission, take a break for 2 days. With prolonged treatment Diacarb, it is necessary to prescribe potassium preparations, a potassium-safe diet. In preparation for the operation, 250-500 mg are prescribed on the eve and in the morning on the day of the operation.

Epilepsy Doses Diacarb for adults: 250-500 mg / day in one dose for 3 days, on the 4th day a break. With the simultaneous use of acetazolamide with other anticonvulsants, 250 mg 1 time per day is used at the beginning of treatment, gradually increasing the dose if necessary. The maximum daily dose for adults is 1000 mg. Doses for children over 3 years: 8-30 mg / kg per day, divided into 1-4 doses. The maximum daily dose is 750 mg. • Acute altitude sickness Recommended use of the drug Diacarb in a dose of 500-1000 mg per day. In case of rapid ascent - 1000 mg per day.

The drug should be used 24-48 hours before the ascent. In case of symptoms of the disease, treatment is continued for the next 48 hours or longer if necessary. • Liquorodynamic disturbances, intracranial hypertension. The use of the drug Diacarb in a dose of 250 mg per day or 125-250 mg every 8-12 hours is recommended.

The maximum therapeutic effect is achieved when taking a dose Diacarb of 750 mg per day. To achieve an optimal therapeutic effect, daily intake of the drug Diacarb without intervals may be required.

Overdose Diacarb:

Symptoms of an overdose are not described.

Possible symptoms of an overdose may be disturbances in the water-electrolyte balance, metabolic acidosis, as well as disorders of the central nervous system. Treatment: there is no specific antidote.

Symptomatic and supportive therapy is recommended. Plasma electrolytes should be monitored, especially potassium, sodium, as well as blood pH. In the case of metabolic acidosis, sodium bicarbonate is used. Acetazolamide/Diacarb is excreted by hemodialysis. Diacarb