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Frequently Asked Questions

How does acetazolamide (Diamox, Avva) work?

Short Answer

Acetazolamide decreases the production of the fluid that fills the back of the eye; this helps to reduce the pressure caused by excessive fluid buildup.

Long Answer

Acetazolamide (a-set-a-ZOLE-a-mide), sold as Diamox and Avva, reduces the activity of a protein called carbonic anhydrase. By decreasing the production of the fluid that fills the back of the eye, this medication helps to reduce the pressure caused by excessive fluid buildup.

Acetazolamide also acts as a diuretic (water pill) to reduce edema (excess water retention), and has been used to help control seizures in certain types of epilepsy.

Additional Information

The Parkinsn's List Drug Database: acetazolamide, Diamox
Carbonicanhydrase is an enzyme responsible for forming hydrogen and bicarbonate ions from carbon dioxide and water. By inhibiting this reaction, acetazolamide reduces the availability of these ions for active transport. Hydrogen ion concentrations in the renal tubule lumen are reduced by acetazolamide, leading to analkaline urine and an increased excretion of bicarbonate, sodium,potassium, and water. A reduction in plasma bicarbonate results in metabolic acidosis, which rapidly reverses the diuretic effect. Reduced intraocular pressure (IOP) is the result of a 50-60% reduction in aqueous humor production by acetazolamide and is likely due to decreased bicarbonate ion concentrations inocular fluid.

The anticonvulsant activity of acetazolamide may depend on a direct inhibition of carbonic anhydrase in theCNS, which increases carbon dioxide tension and inhibits neuronal transmission. The successful treatment of altitude sickness involves production of respiratory and metabolic acidosis, which increases ventilation and binding of oxygen to hemoglobin. This occurs because the drug decreases carbon dioxide tension in the pulmonary alveoli, thus increasing arterial oxygen tension.
Wikipedia: Acetazolamide
Acetazolamide is a carbonic anhydrase inhibitor, which means that it forces the kidneys to excrete bicarbonate (HCO3-), thus re-acidifying the blood.

Carbonic anhydrase (CA) catalyzes the forward motion of molecules in the following equation: "CO2 + H2O >> CA >> H2CO3 >> H+ + HCO3-" where CA converts carbon dioxide (CO2) and water (H2O) to carbonic acid (H2CO3), but this is only the case when the current concentration of carbonic acid is less than it would be at equilibrium. Enzymes DO NOT catalyze only one direction of a chemical reaction. Nevertheless, in situations where pCO2 is increased, CA does catalyze the formation of carbonic acid which then dissociates to a hydrogen ion (H+, an acidic proton), and a bicarbonate ion (HCO3-, a basic anion). In some tissues (particularly plants), the steady state displacement from equilibrium is such that the net reaction catalyzed by CA is conversion of carbonic acid to carbon dioxide and water.

Carbonic acid inhibitors, such as acetazolamide, inhibit CA in tissue and fluid, causing less movement of carbonic acid toward CO2 production. In the kidneys, blocking CA leads to bicarbonate wasting in the tubules (alkalizes urine), loss of bicarbonate subsequently leads to a metabolic acidosis. In the meantime, H+ backs up due to acetazolamide CA inhibition in the tubule and enters the cell with Cl-, then passes into the bloodstream, creating a hyperchloremic metabolic acidosis. This effect can also be used for therapeutic correction of respiratory alkalosis.
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