Drug intelligence / Profile preview

acetazolamide + loop diuretics

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Acetazolamide + loop diuretics is a combination therapy used primarily in the management of acute decompensated heart failure with volume overload. Acetazolamide is a carbonic anhydrase inhibitor that acts on the proximal renal tubule to inhibit sodium and bicarbonate reabsorption, leading to increased excretion of sodium, bicarbonate, and water. Loop diuretics (such as furosemide or torsemide) act on the thick ascending limb of the loop of Henle to inhibit sodium-potassium-chloride cotransporters, resulting in potent natriuresis and diuresis. When combined, acetazolamide enhances the efficacy of loop diuretics by increasing distal delivery of sodium, thereby overcoming compensatory mechanisms that can limit response to loop diuretic monotherapy. This combination has been shown in clinical trials (e.g., ADVOR) to improve early decongestion rates and increase urine output without significantly increasing adverse events compared with loop diuretic monotherapy[1][3][4][5][9].

02

Targets

CA1 (Carbonic anhydrase 1)CA2 (Carbonic Anhydrase 2)CA7 (Carbonic anhydrase VII)CA12 (Carbonic anhydrase XII)CA14 (Carbonic Anhydrase 14)NKCC2 (Sodium-potassium-chloride cotransporter 2)CA4 (Carbonic anhydrase 4)NKCC (Sodium-potassium-chloride cotransporter)

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