DIAKARB

Active material: Aцetazolamid
When ATH: S01EC01
CCF: Diuretic. Carbonic anhydrase inhibitors
ICD-10 codes (testimony): G40, G93.2, H40.1, H40.2, H40.3, H40.4, H40.5, I50.0, K74, N18, T70
When CSF: 01.08.04
Manufacturer: Pharmaceutical Works POLPHARMA S.A. (Poland)

Pharmaceutical form, composition and packaging

Pills white, round, flat.

Excipients: potato starch, talc, krahmalynыy sodium glycolate.

12 PC. – blisters (2) – packs cardboard.

Pharmacological action

Diuretic group of carbonic anhydrase inhibitors. It causes a slight diuretic effect. It inhibits the enzyme carbonic anhydrase in the proximal convoluted tubules of the nephron, It increases the urinary excretion of sodium ions, Potassium, bicarbonate, It does not affect the excretion of chloride ions; It causes an increase in urine pH. It violates the acid-base balance (metabolic acidosis). Inhibition of carbonic anhydrase of ciliary body reduces the secretion of aqueous humor and reduce intraocular pressure. Inhibition of carbonic anhydrase activity in the brain causes the anticonvulsant activity of the drug.

Duration of action – to 12 no.

Pharmacokinetics

Absorption

After oral acetazolamide is well absorbed from the gastrointestinal tract. After receiving Diamox^® dose 500 mg C_max the active substance is 12-27 ug / ml achieved after 1-3 no. Determine the concentration of acetazolamide in plasma is maintained for 24 h after dosing.

Distribution and metabolism

Distributed mainly in erythrocytes, kidney, muscle, tissues of the eyeball and the CNS. Bound to plasma proteins to a high degree. It penetrates through the placental barrier.

Acetazolamide not biotransformed in the body.

Deduction

Excreted by the kidneys in unchanged form. About 90% the dose is excreted in the urine within 24 no.

Testimony

- Edema syndrome (mild to moderate severity, in combination with alkalosis);

- Glaucoma (primary and secondary, as well as an acute attack);

- Epilepsy (in a combination therapy);

- Acute altitude (mountain) disease.

Dosage regimen

At Edema syndrome at the beginning of the treatment drug is prescribed in a dose 250-375 mg (1-1.5 tab.) 1 time / day in the morning. The maximum diuretic effect is achieved while taking the drug every other day, or 2 days in a row, and then – a one-day break. When using Diamox^® should continue treatment of circulatory failure, including cardiac glycosides, a diet with restriction of salt intake and compensate for the deficiency of potassium.

Adults at open-angle glaucoma drug administered in a single dose 250 mg (1 tab.) 1-4 times / day. Doses, exceeding 1 g, do not increase the therapeutic effect. At secondary glaucoma drug administered in a single dose 250 mg (1 tab.) every 4 no. In some patients, the therapeutic effect is shown after administration of the drug at short 250 mg 2 times / day. At acute attacks of glaucoma the drug is prescribed for 250 mg 4 times / day.

Babies at glaucoma attack Diakarʙ^® administered at a dose rate of 10-15 mg / kg of body weight per day for 3-4 admission.

At epilepsy adult appoint 250-500 mg / day at one time for 3 days, on 4th day – break. Children under the age of 4 to 12 Months – 50 mg / day 1-2 admission; for children 2-3 years – 50-125 mg / day 1-2 admission; children and adolescents between the ages of 4 to 18 years – by 125-250 mg 1 time / day in the morning. With simultaneous application of Diamox^® other anticonvulsant used in the early treatment 250 mg (1 tab.) 1 time / day, if necessary, gradually increasing the dose. Children should not use doses, exceeding 750 mg / day.

At mountain sickness It recommends the use of the drug at a dose of 500-1000 mg (2-4 tab.) per day; when rapid ascent – by 1000 mg / day. The daily dose is divided into several stages in equal doses. The drug should be used for 24-48 hours before climbing, and in case of the onset of symptoms – continue treatment for the following 48 h or more, if necessary.

If you missed doses should not increase the dose when the next reception.

Side effect

From the central and peripheral nervous system: convulsions, paresthesia, noise in ears, myopia; prolonged use – disorientation, paraphia, drowsiness.

From the hematopoietic system: in some cases with prolonged use – gemoliticheskaya anemia, leukopenia, agranulocytosis.

From the water-electrolyte balance and acid-base balance: kaliopenia, metabolic acidosis.

From the urinary system: in some cases with prolonged use – nephrolithiasis, transient hematuria and glycosuria.

From the digestive system: anorexia; prolonged use – nausea, vomiting, diarrhea.

Dermatological reactions: dermahemia, itch, hives.

Other: muscular weakness, prolonged use – allergic reactions.

Contraindications

- Acute renal failure;

- Liver failure;

- Hypokalemia;

- Acidosis;

- Gipokorticizm;

- Addison's disease;

- Uremia;

- Diabetes;

- Pregnancy;

- Lactation;

- Hypersensitivity to the drug.

FROM caution prescribers edema hepatic and renal origin and a joint reception with acetylsalicylic acid in high doses.

Pregnancy and lactation

Diakarʙ^® contraindicated during pregnancy and lactation.

Cautions

In appointing the drug more 5 consecutive days increases the risk of metabolic acidosis.

With prolonged use of the drug should be monitored picture peripheral blood, Indicators of water-electrolyte and acid-base balance.

Effects on ability to drive vehicles and management mechanisms

Diakarʙ^®, especially in high doses, may cause drowsiness, fatiguability, dizziness and disorientation, so during treatment, patients should not drive vehicles and use machines, require high concentration and speed of psychomotor reactions.

Overdose

No cases of overdose or acute poisoning.

Symptoms: may increase the side effects described.

Treatment: symptomatic therapy.

Drug Interactions

In a joint application with antiepileptic drugs Diakarb^® increase the expression of osteomalacia.

If concomitant use of Diamox^® other diuretics and theophylline enhanced diuretic effect.

With simultaneous application of Diamox^® with acid-diuretic diuretic effect decreases.

In an application Diakarb^® It increases the risk of symptoms of toxic effects of salicylates, Digitalis preparations, karʙamazepina, ephedrine, non-depolarizing muscle relaxants.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored in a dry, protected from light and away from children at a temperature no higher than 25 ° C. Shelf life – 5 years.