Active substances

Acetazolamide

Chemical name

N-5- (Aminosulfonyl) -1,3,4-thiadiazol-2-yl-acetamide

Chemical properties

Acetazolamide is a diuretic that selectively inhibits an enzyme. carbonic anhydrase. The substance is on the list of essential and vital medicines. It is rarely used as a diuretic, more often as a decongestant.

The molecular weight of the compound = 222.3 grams per mole. The substance is synthesized in the form of a white crystalline powder, which is odorless. The product is slightly soluble in alcohol, water, acetoneinsoluble in chloroform, carbon tetrachloride. The substance is easily soluble in solutions. alkalis.

Pharmachologic effect

Diuretic, antiepileptic, antiglaucoma.

Pharmacodynamics and pharmacokinetics

The substance is a selective enzyme inhibitor carbonic anhydrase (in the kidneys). This enzyme is responsible for stimulating the reaction. carbon dioxide hydration and is a reaction catalyst dissociation carbonic acid.

The result is a decrease in reabsorption bicarbonate, potassium ions and sodium, urine output increases, urine pH increases, the reabsorption process is stimulated ammonia. The tool does not affect the allocation processes chlorine ions.

The ability of a substance to inhibit an enzyme carbonic anhydrase of the ciliary body leads to a significant decrease in the secretion of aqueous humor and pressure inside the eye. There is also a noticeable slowdown paroxysmal discharges of neurons, which causes the antiepileptic activity of the drug.

After taking the tablets, the substance is well absorbed by the gastrointestinal tract. Its maximum concentration, reaching within 120 minutes. Means overcomes placental barrierexcreted in breast milk.

The drug is not subjected to biotransformation, it is excreted from the body through the kidneys in an unchanged form. The duration of action of the substance is up to 12 hours.

When conducting experiments on animals, it was found that this tool exhibits embryotoxic and teratogenic effects when using dosages that are 10 times the maximum recommended.

Indications for use

The medicine is prescribed:

  • at edematous syndrome any degree of severity, combined with alkalosis;
  • patients with cranial hypertension;
  • with primary and secondary glaucoma;
  • as part of short-term treatment glaucomabefore surgery to lower intraocular pressure;
  • in mixed forms epilepsy in combination with anticonvulsants;
  • during small and large epileptic seizures in children;
  • for removal edemathat are caused by taking other medications or pulmonary heart disease;
  • to reduce tourist acclimatization time with mountain sickness.

Contraindications

Acetazolamide is not recommended for use:

  • at allergies on substance or other sulfonamides;
  • patients with hyponatremia and hypokalemia;
  • with insufficient adrenal function;
  • persons with a diseased kidney or liver;
  • at cirrhosis of the liver or urolithiasis;
  • patients with hyperchloremic acidosis;
  • for a long time in chronic decompensated angle-closure glaucoma;
  • breast-feeding women;
  • at uremia and diabetes.

Side effects

During treatment with the drug can be observed:

  • drowsinessviolation of taste and hearing, myopia, crampsdisorientation in space, tinnitus, paresthesia;
  • hypokalemiaimbalance electrolytes, metabolic acidosis;
  • vomiting diarrhealoss of appetite, liver disease, melenanausea
  • allergic reactions hives, polyuria, photophobia, glucosuria, hematuria.

Acetazolamide, instructions for use (Method and dosage)

The tablets are taken orally.

At edema use 250 mg of the drug 1-2 times a day. The medicine is taken in courses of 5 days, with a 2-day break between them.

For stopping and treatment epileptic seizures appoint from 250 to 500 mg of the substance per day, at one time. The drug is taken for 3 days, then take a break for 4 days and resume therapy.

For children from 4 months to a year, it is recommended to use 50 mg per day, distributed in 2 doses.

At the age of 3 to 5 years, use from 50 to 125 mg of the drug, for 2 doses.

Children over 5 are prescribed from 125 to 250 mg of the drug once a day.

For treatment chronic glaucoma appoint 125-500 mg of the drug 1-3 times a day. The course of treatment is 5 days.

Also for the treatment of various types glaucoma can be used ophthalmic solutionAcetazolamide. As a rule, apply 0.2-0.3% solution cellulose and hydroxyethyl cellulosesometimes add beta blockers.

At The miner (mountain sickness) It is recommended to take the medicine 2-3 times a day. It is recommended to start treatment 1-2 days before the ascent, and continue for another 2 days or more.

Overdose

In case of an overdose, an increase in the frequency and strength of adverse reactions will most likely occur. Supportive and symptomatic therapy is recommended.

Interaction

The drug increases plasma concentration cyclosporinethat is accompanied by toxic effects on the kidneys.

With the combined use of medication and primidina the plasma concentration of the latter decreases, its anticonvulsant effect is weakened.

Ammonium chloride weakens the action of acetazolamide, may cause acidosis.

The combination of a substance with other diuretics (theophylline) leads to potentiation of their diuretic effect.

Anticholinesterase agentsincrease manifestations of muscle weakness in patients with patients myasthenia and taking this medicine.

When combined with salicylates, digitalis preparations, ephedrine, carbamazepine, non-depolarizing muscle relaxants the likelihood of developing intoxication increases.

Combination of substance with lithium preparations may lead to increased lithium in urine. Acute intoxication may also develop.

The medicine increases the effectiveness insulin and other oral hypoglycemic drugs.

The combined intake of a substance with phenobarbital or phenytoin causes pronounced osteomalacia.

Special instructions

Acetazolamide may cause osteomalacia.

To avoid metabolic acidosis the medicine is not recommended to be taken for more than 5 days without a break.

Particular care should be taken during the treatment of elderly patients or patients with impaired renal function.

If during the course of treatment the patient has changes in blood counts, serum electrolytes, then treatment must be stopped.

During pregnancy and lactation

The medicine is not recommended for use in the first 3 months of pregnancy. During breastfeeding, treatment should be interrupted.

Preparations Containing (Acetazolamide Analogs)

Matches for ATX Level 4 code:DorzoptAzoptDiacarbTrusopt

Trade Name Acetazolamide: Diacarb, Acetazolamide.

Reviews on Acetazolamide

Some drug reviews Diacarb:

  • ... I was found to have increased intracranial pressure. The doctor prescribed Diakarb diuretic tablets. The medicine coped with its task, and only managed to reach the toilet. Pressure decreased, bruises under the eyes disappeared, swelling subsided from the legs and fingers. In addition, in order to prevent disturbances in the electrolyte balance, I was prescribed Asparkam. The effect is generally satisfied”;
  • ... The medicine for my child at 4 months was prescribed for a mild hydrocephalic syndrome. During treatment, the child was restless, excited, slept poorly. However, after drinking the entire course, an ultrasound scan showed that the child’s health is normal”.

Acetazolamide price, where to buy

The cost of 30 tablets Diacarb, a dosage of 250 mg is approximately 200-260 rubles.

Watch the video: Acetazolamide: Carbonic Anhydrase Inhibitor (February 2020).

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