Diacarb pills 250 mg 30 pcs
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Active ingredients
Acetazolamide
Release form
Pills
Composition
Active ingredient: Acetazolamide (Acetazolamidum) Concentration of the active substance (mg): 250
Pharmacological effect
Acetazolamide is a carbonic anhydrase inhibitor with weak diuretic activity. The mechanism of action is associated with the inhibition of the release of sodium ions (Na +) and hydrogen (H +) in a carbonic acid molecule. Inhibition of carbonic anhydrase activity with acetazolamide inhibits the synthesis of carbonic acid in the proximal nephron tubule. 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 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 excretion of phosphate, magnesium, calcium by the kidneys, which can also lead to metabolic disorders. After 3 days from the start, 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 the normal activity of carbonic anhydrase. Acetazolamide is used to treat glaucoma. Inhibition of carbonic anhydrase 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 of action 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. as an adjunct in the treatment of epilepsy, because inhibition of carbonic anhydrase in the nerve cells of the brain inhibits pathological excitability. Acetazolamide is used to treat liquorodynamic disorders and intracranial hypertension. The drug inhibits 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
AbsorptionAfter oral administration, acetazolamide is well absorbed from the gastrointestinal tract. After taking Diacarb in a dose of 500 mg Cmax of the active substance is 12-27 mcg / ml and is reached after 1-3 hours. The minimum concentration of acetazolamide in plasma lasts for 24 hours after taking the drug. Distribution and metabolismDistributed mainly in erythrocytes, kidneys, muscles , tissues of the eyeball and the central nervous system. It penetrates the placental barrier, is excreted in small quantities with breast milk. It does not accumulate in the tissues and is not metabolized in the body. Excretion is excreted by the kidneys unchanged. About 90% of the dose is excreted in the urine within 24 hours.
Indications
- edema syndrome (mild or moderate severity, in combination with alkalosis); - relief of an acute attack of glaucoma, preoperative preparation of patients, persistent cases of glaucoma (in complex therapy); - in epilepsy as an additional therapy to antiepileptic drugs; - acute altitude sickness (the drug reduces the time of acclimatization); - intracranial hypertension (benign intracranial hypertension, intracranial hypertension after ventricular bypass) in complex therapy.
Contraindications
- acute renal failure; - liver failure; - liver cirrhosis; - hypokalemia; - acidosis; - hypocorticism; - Addison's disease; - uremia; - diabetes; - pregnancy; - lactation; - hypersensitivity to the components of the preparation.
Precautionary measures
Do not exceed the recommended dose. With caution: edema of the liver and kidney origin, simultaneous administration with acetylsalicylic acid (doses of more than 300 mg / day), pulmonary embolism and pulmonary emphysema (risk of developing acidosis), II and III trimesters of pregnancy.
Use during pregnancy and lactation
Well-controlled clinical trials of the use of the drug Diacarb in pregnant women have not been conducted. Therefore, 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 when the potential benefit to the mother outweighs the potential risk to the fetus. Acetazolamide is excreted in small amounts with breast milk, therefore, if necessary, use the drug Diakarb during lactation breastfeeding should be stopped.
Dosage and administration
Nutr. Otsechny syndrome: at the beginning of treatment - 250–375 mg / day (1–1.5 pills), in the morning. The maximum diuretic effect is achieved when taken every other day or for 2 days in a row with a one-day break. For open-angle glaucoma: 250 mg (1 tab.) 1–4 times a day. Doses of more than 1000 mg (4 tab.) Do not increase the effectiveness of treatment. In secondary glaucoma: 250 mg (1 tab.) Every 4 hours, with acute attacks of glaucoma - 250 mg (1 tab.) 4 times a day, Some patients are effective in taking 250 mg (1 tab.) 2 times a day (short-term therapy). For children - 10–15 mg / kg / day in 3–4 divided doses. For epilepsy: for adults –– 250–500 mg / day (1–2 pills) in 1 dose for 3 days, on the 4th one - break. For children: 4–12 months - 50 mg / day in 1–2 doses, 2–3 years - 50–125 mg / day in 1–2 doses, 4–18 years - 125–250 mg once in the morning. When acetazolamide is combined with anticonvulsants, the initial dose is 250 mg 1 time per day (if necessary, increased). Do not use doses higher than 750 mg / day in children. Mountain disease: prevention - 500–1000 mg / day in equal doses. In case of rapid ascent - 1000 mg / day in equal doses. The drug should be used 24–48 hours before climbing, in the case of the onset of symptoms of the disease, treatment is continued for 48 hours (longer if necessary). In case of skipping the drug, the next dose should not be increased.
Side effects
Hypokalemia, muscle weakness, convulsions, skin flushes, paresthesias, tinnitus, anorexia, metabolic acidosis, pruritus, myopia, urticaria. drowsiness, nausea, vomiting, diarrhea, allergic reactions.
Overdose
Symptoms of overdose are not described. Violations of water and electrolyte balance, metabolic acidosis, as well as disorders of the central nervous system can be probable symptoms of overdose. Treatment: There is no specific antidote. Conduct symptomatic and supportive therapy. The content of electrolytes in the blood, especially potassium, sodium, and blood pH should be monitored. In the case of metabolic acidosis, sodium bicarbonate is used. Acetazolamide is eliminated by hemodialysis.
Interaction with other drugs
Acetazolamide may enhance the action of antagonists of folic acid, hypoglycemic agents and oral anticoagulants. Some of the simultaneous use of acetazolamide and acetylsalicylic acid can cause metabolic acidosis and increase toxic effects on the CNS. increases the serum phenytoin content. Acetazolamide increases the manifestations of osteomalacia caused by taking counter use of acetazolamide and amphetamine, atropine or quinidine can increase their side effects. Potentiation of the diuretic effect occurs when combined with methylxanthines (aminophylline). Reducing the diuretic effect occurs when combined with ammonium chloride and other acid-forming diuretics. Strengthening in relation to intraocular pressure, it is possible with simultaneous use with cholinergic drugs and beta-blockers. Acetazolamide enhances the effect of ephedrine. Increases plasma concentration of carbamazepine, non-depolarizing muscle relaxants. Increases the elimination of lithium.
special instructions
In case of hypersensitivity to the drug, life-threatening side effects may occur, for example, Stevens-Johnson syndrome, Lyell's syndrome, fulminant hepatic necrosis, agranulocytosis, aplastic anemia and hemorrhagic diathesis. In the event of these symptoms should immediately stop taking the drug. Diacarb used in doses exceeding the recommended, does not increase diuresis, can increase drowsiness and paresthesia, and sometimes also reduce diuresis. The drug can cause acidosis, therefore it should be used with caution in patients with pulmonary embolism and emphysema. The preparation alkalizes urine. Diacarb should be used carefully in patients with diabetes mellitus due to an increased risk of hyperglycemia. If administered over 5 days, it is high risk of developing metabolic acidosis. It is recommended to monitor the blood and platelet patterns at the beginning of treatment, and at regular intervals during treatment,as well as periodic monitoring of electrolytes in serum. Influencing the ability to drive vehicles and control mechanisms Diacarb, especially in high doses, can cause drowsiness, rarely fatigue, dizziness, ataxia and disorientation, therefore during treatment patients should not drive vehicles and work with mechanisms requiring increased concentration and speed of psychomotor reactions.