Acetazolamide (Diacarb) - diuretic (diuretic). Selectively inhibits the enzyme carbonic anhydrase.
Acetazolamide | |
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Acetazolamide | |
Chemical compound | |
IUPAC | N- [5- (Aminosulfonyl) -1,3,4-thiadiazol-2-yl] acetamide |
Gross formula | C 4 H 6 N 4 O 3 S 2 |
Molar mass | 222.245 g / mol |
CAS | |
Pubchem | |
Drugbank | |
Classification | |
ATH | |
Pharmacokinetics | |
Metabolism | None |
The period is half out. | from 3 to 9 hours |
Excretion | by the kidneys |
Dosage Forms | |
pills | |
Mode of administration | |
inside , intravenous | |
Other names | |
Diacarb | |
As a conventional diuretic, acetazolamide is used relatively rarely, as there are more effective drugs, but it is well suited for edema due to pulmonary heart disease, when it is necessary to reduce elevated levels of carbon dioxide and bicarbonates in the blood (to restore normal pH and sensitivity to βloopbacksβ). "Diuretics such as furosemide ). [one]
Acetazolamide is included in the list of essential and essential drugs .
Content
Pharmacological action
A diuretic from the group of carbonic anhydrase inhibitors . It causes diuresis by removing certain electrolytes , in quantitative terms not violating a significant degree of electrolyte balance in the body . The mechanism of this action is to inhibit the function of the carbonic anhydrase enzyme, which plays a serious role in the transport of ions and preserves the ionic balance of the organism. Inhibits carbonic anhydrase in the proximal convoluted nephron tubule, increases the excretion of Na + , K + , bicarbonate with urine , does not affect the excretion of Cl - , alkalizes urine . Violates acid-base balance (metabolic acidosis ). Inhibition of carbonic anhydrase ciliary body leads to a decrease in the secretion of aqueous humor and lower intraocular pressure . Suppression of carbonic anhydrase in the brain causes the anticonvulsant activity of the drug. Reduces the formation of cerebrospinal fluid and intracranial pressure . Duration of action - up to 12 hours.
Pharmacokinetics
Absorption - high, C max in the blood - 2 hours after administration at a dose of 500 mg. It penetrates the placental barrier . Communication with plasma proteins is high. Excreted by the kidneys in unchanged form.
Indications
Edematous syndrome (mild and moderate severity, in combination with alkalosis ). Brain hypertension ; glaucoma (primary and secondary, acute attack), epilepsy (minor epileptic seizures in children, rare abscesses ), mountain sickness , Meniere's disease , tetany , premenstrual syndrome , gout .
Contraindications
Hypersensitivity , acute renal failure , liver failure , hypokalemia , acidosis , hypocorticism , Addison's disease , uremia , diabetes mellitus , pregnancy (I term).
Be careful
Swelling of the liver and kidney genesis .
Dosing regimen
Inside When edematous syndrome - 250 mg 1-2 times a day in courses for 5 days, followed by a two-day break. With epilepsy - 250-500 mg / day in one dose for 3 days, on the 4th day of a break. With an attack of glaucoma, the initial dose is 250-500 mg; then every 6 hours at 250 mg, after 1-2 days, the frequency of administration is first reduced to 3, then 2 times per day. Children 4-12 months - 50 mg / day in 1-2 doses; 3-5 years - 50-125 mg / day in 1-2 doses; 4-18 years old - 125-250 mg once in the morning. In chronic glaucoma, 125-250 mg 1-3 times every other day for 5 days. For glaucoma treatment, an ophthalmic solution containing acetazolamide, solubilized in an aqueous medium in the presence of hydroxypropyl-beta-cyclodextrin and a water-soluble stabilizing polymer, is proposed. For prolonged action using a 0.2-0.3% solution of hydroxyethylcellulose and methylcellulose. Beta-blockers are administered as an additional active substance. [2]
Side Effects
Hypokalemia , myasthenia gravis , convulsions , skin flushing , paresthesia , tinnitus, loss of appetite , metabolic acidosis , pruritus. With prolonged use - nephrourolithiasis , hematuria , glycosuria , hemolytic anemia , leukopenia , agranulocytosis , disorientation, violation of touch, drowsiness, nausea , vomiting , diarrhea , allergic reactions , paresthesia.
Special instructions
In case of appointment for more than 5 days, the risk of developing metabolic acidosis is high. With prolonged use should be monitored water and electrolyte balance, a picture of peripheral blood, acid-base state.
Interaction
Strengthens manifestations of osteomalacia caused by taking antiepileptic drugs. Other diuretics and theophylline increase the severity of the diuretic action of acetazolamide, acid-forming diuretics weaken. GCS increases the risk of hypokalemia. Increases toxicity of salicylates, digitalis preparations, carbamazepine , ephedrine and non-polarizing muscle relaxants .
Notes
- β Mashkovsky, 2005 , p. 505.
- β Π ΠΠ₯ΠΈΠΌ., 03.08. 19Π268
Literature
- Mashkovsky M. D. Medicinal products. - 15th ed. - M .: New Wave, 2005. - p. 505-506. - 1200 s. - ISBN 5-7864-0203-7 .