Drug intelligence / Profile preview

quinethazone

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Quinethazone is a thiazide-like diuretic primarily used to treat hypertension. It acts by inhibiting sodium and chloride reabsorption in the distal convoluted tubules of the kidney via the sodium-chloride symporter (solute carrier family 12 member 3), leading to increased excretion of sodium, chloride, and water. This results in reduced extracellular fluid and plasma volume, thereby lowering blood pressure. Quinethazone also increases potassium excretion through the sodium-potassium exchange mechanism. While its short-term antihypertensive effects are well understood, involving direct renal action, its long-term blood pressure-lowering mechanisms may include inhibition of carbonic anhydrases in vascular smooth muscle and activation of large-conductance calcium-activated potassium channels (KCa) in smooth muscle tissue[1][5][6]. Common side effects include dizziness, dry mouth, nausea, hypokalemia (low potassium), and increased serum uric acid[1][3][8].

Brand names
Hydromox
Other names
chinetazonequinetazonaquinethazonquinethazonum
02

Targets

CA2 (Carbonic Anhydrase 2)CA1 (Carbonic anhydrase 1)KCNMA1 (Calcium-activated potassium channel subfamily M alpha member 1)SLC12A3 (Thiazide-sensitive sodium-chloride cotransporter)

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