Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2015 Publisher: Mercury Pharmaceuticals Ltd, Capital House, 85 King William Street, London EC4N 7BL, UK
Pharmacotherapeutic group: Carbonic anhydrase inhibitors
ATC Code: S01EC01
Acetazolamide is an inhibitor of carbonic anhydrase. By inhibiting the reaction catalysed by this enzyme in the renal tubules, acetazolamide increases the excretion of bicarbonate and of cations, chiefly sodium and potassium, and so promotes alkaline diuresis.
Continuous administration of acetazolamide is associated with metabolic acidosis and resultant loss of diuretic activity. Therefore, the effectiveness of Acetazolamide tablets in diuresis diminishes with continuous use.
By inhibiting carbonic anhydrase in the eye, acetazolamide decreases intra-ocular pressure and is therefore useful in the treatment of glaucoma.
Acetazolamide is fairly rapidly absorbed from the gastro-intestinal tract with peak plasma concentrations occurring about 2 hours after administration by mouth. It has been estimated to have a plasma half-life of about 4 hours. It is tightly bound to carbonic anhydrase and accumulates in tissues containing this enzyme, particularly red blood cells and the renal cortex. It is also bound to plasma proteins. It is excreted unchanged in the urine; renal clearance being enhanced in alkaline urine.
Not applicable.
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