Mechanism of action, pharmacokinetics, adverse effects, and therapeutic uses of amiloride hydrochloride, a new potassium-sparing diuretic.

Amiloride hydrochloride is a new, orally administered, potassium-sparing diuretic with mild natriuretic and diuretic properties. Its primary site of action is the distal tubule of the nephron where it selectively blocks sodium transport, thereby inhibiting sodium-potassium exchange. The mechanism of action of amiloride is independent of aldosterone. It is excreted unmetabolized in the urine and feces. Peak serum levels are seen at three hours, and the serum half-life is six hours. The drug can probably be safely administered to patients with hepatic dysfunction but should be used cautiously, if at all, in patients with renal insufficiency. Amiloride is well tolerated, and serious toxicity is rare. It should prove useful in edematous states and hypertension. When amiloride is used in fixed combination with a thiazide diuretic the risk of hypokalemia is minimal.