Drug Notebook

FDA Alerts

  • Hyperkalemia (i.e., serum potassium concentrations >5.5 mEq/L) may occur with all potassium-sparing agents, including amiloride.
  • Hyperkalemia occurs in about 10% of patients not receiving a kaliuretic diuretic and more frequently in patients with renal impairment or diabetes (even without evidence of renal impairment) and in geriatric patients. In patients without the mentioned complications, incidence of hypercalcemia is reduced to 1–2% by concomitant use of amiloride with a thiazide diuretic.
  • Uncorrected hyperkalemia may be fatal; monitor serum potassium concentrations carefully, especially during initial therapy or dosage adjustments, and in patients with concurrent illness that may affect renal function.

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amiloride
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(a MIL o ride)

Uses

Amiloride should rarely be used alone, because such use may result in increased risk of hyperkalemia. Use alone only when persistent hypokalemia has been documented.

Hypokalemia Induced by Kaliuretic Diuretics

Treatment or prevention of hypokalemia induced by thiazide or other kaliuretic diuretics in patients with CHF or hypertension.

May be particularly useful for preventing diuretic-induced hypokalemia in patients in whom the clinical consequences of hypokalemia represent an important risk, such as patients receiving cardiac glycosides or those with cardiac arrhythmias.

Also useful in patients with hypokalemia who do not respond to potassium supplements or those who cannot tolerate potassium supplements.

Potassium-sparing effect of amiloride generally persists during prolonged therapy with the drug, but may diminish with time in some patients.

Potassium-sparing effect of amiloride is additive with that of spironolactone. May be effective in some patients unresponsive to spironolactone; unlike spironolactone, diuretic effect of amiloride is independent of aldosterone concentrations.

Edema

Management of edema associated with CHF, cirrhosis of the liver, or secondary hyperaldosteronism.

Generally, use in combination with other more effective, rapidly acting diuretics, such as thiazides, chlorthalidone, or loop diuretics (e.g., furosemide), to decrease potassium excretion caused by kaliuretic diuretics.

Used in fixed combination with hydrochlorothiazide for treatment of edema in patients who require a thiazide diuretic and in whom the development of hypokalemia cannot be risked.

CHF

In the management of edema associated with CHF, generally used in conjunction with other more effective, rapidly acting diuretics (e.g., thiazides, chlorthalidone, loop diuretics).

Most experts state that all patients with symptomatic CHF who have evidence or a prior history of fluid retention generally should receive diuretic therapy in conjunction with moderate sodium restriction (≤3 g of sodium daily), an ACE inhibitor, and usually a β-adrenergic blocking agent, with or without a cardiac glycoside.

Most experts state that the diuretics of choice for most patients with CHF are loop diuretics (e.g., bumetanide, ethacrynic acid, furosemide, torsemide).

Do not use diuretics as monotherapy in CHF even if symptoms (e.g., peripheral edema, pulmonary congestion) are well controlled; diuretics alone do not prevent progression of heart failure.

Once fluid retention in CHF has resolved, diuretic therapy should be maintained to prevent its recurrence. Ideally, diuretic therapy should be adjusted according to changes in body weight (as an indicator of fluid retention) rather than maintained at a fixed dosage.

Diuretics should be continued in CHF and comorbid conditions (e.g., hypertension) where ongoing therapy with the drugs is indicated.

Hypertension

Amiloride alone has mild hypotensive activity.

In hypertensive patients, is used concomitantly with a thiazide diuretic mainly to prevent or treat diuretic-induced hypokalemia. (See Hypokalemia Induced by Kaliuretic Diuretics under Uses.)

The manufacturers state that amiloride produces little additive hypotensive activity when used concurrently with a thiazide diuretic.

JNC 7 recommends that thiazides be used as initial therapy for the treatment of uncomplicated hypertension in most patients, either alone or combined with other classes of antihypertensive drugs that have demonstrated benefit (e.g., ACE inhibitors, angiotensin II receptor antagonists, β-adrenergic blocking agents, calcium-channel blocking agents).

Used in fixed combination with hydrochlorothiazide for treatment of hypertension in patients who require a thiazide diuretic and in whom the development of hypokalemia cannot be risked.

Used in fixed combination with hydrochlorothiazide for treatment of hypertension in patients who develop hypokalemia during hydrochlorothiazide monotherapy.

Use the amiloride/hydrochlorothiazide fixed combination alone or as an adjunct to other antihypertensive agents (e.g., methyldopa, β-adrenergic blocking agent).

Hyperaldosteronism

Has been used to control hypertension and correct electrolyte abnormalities associated with primary hyperaldosteronism†.

Also has been used for the management of secondary hyperaldosteronism† (Bartter’s syndrome) to correct hypokalemia.

Diuretic-induced Metabolic Alkalosis

Has been used to correct the metabolic alkalosis† produced by thiazides and other kaliuretic diuretics.

Calcium Nephrolithiasis

Has been used in combination with hydrochlorothiazide in patients with recurrent calcium nephrolithiasis†.

Lithium-induced Polyuria

Has been used for the management of lithium-induced polyuria† (secondary to lithium-induced nephrogenic diabetes insipidus). (See Specific Drugs, Foods, and Laboratory Tests under Interactions.)

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