Amiloride

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Cyprus: Alverix; France: Modamide; Malta: Amiloride; Slovakia: Amiclaran; Sweden: Amilorid; UK: Amilamont, Amiloride.

North America

Canada: Amiloride, Midamor; USA: Amiloride, Midamor.

Drug combinations

Amiloride and Bendroflumethiazide

Amiloride and Chlorthalidone

Amiloride and Furosemide

Amiloride and Hydrochlorothiazide

Amiloride, Atenolol, and Hydrochlorothiazide

Amiloride, Hydrochlorothiazide, and Timolol

Chemistry

Amiloride Hydrochloride: C~6~H~8~ClN~7~O HCl 2H~2~O. Mw: 302.12. (1) Pyrazinecarboxamide, 3,5-diamino-N-(aminoiminomethyl)-6-chloro-, monohydrochloride dihydrate; (2) N-Amidino-3,5-diamino-6-chloropyrazinecarboxamide monohydrochloride dihydrate. CAS-17440-83-4; CAS-2016-88-8 (anhydrous); CAS-2609-46-3 (amiloride)(1967).

Pharmacologic Category

Diuretics; Potassium-Sparing Diuretics. (ATC-Code: C03DB01).

Mechanism of action

Reduces potassium and hydrogen excretion by inhibiting renal-sodium reabsorption, resulting in weak natriuretic, diuretic, and antihypertensive activity. Increases sodium loss. Increases potassium retention. Decreases calcium excretion. Decreases magnesium loss.

Therapeutic use

Counteracts potassium loss induced by other diuretics in the treatment of hypertension or edematous conditions (CHF, hepatic cirrhosis, hypoaldosteronism). Normally used in conjunction with more potent diuretics (thiazides or loop diuretics).

Pregnancy and lactiation implications

Teratogenic effects were not observed in animal studies. Administration is not recommended during lactation (excretion in breast milk unknown).

Unlabeled use

Cystic fibrosis. Reduction of lithium-induced polyuria. Pediatric hypertension.

Contraindications

Hypersensitivity to amiloride or any component of the formulation. Elevated serum potassium levels (>5.5 mEq/L). Administration of other potassium-conserving agents (e.g. spironolactone, triamterene), or potassium supplementation (medicine, potassium-containing salt substitutes, potassium-rich diet). Anuria. Renal insufficiency. Diabetic nephropathy.

Warnings and precautions

Fluid/electrolyte loss (with excess amounts of drug). Hyperkalemia can occur (increased risk in renal impairment, diabetes, the elderly, and the severely ill). In cirrhosis electrolyte and acid/base imbalances should be avoided (may lead to hepatic encephalopathy). Use with caution in diabetes mellitus and in patients at risk for metabolic or respiratory acidosis (e.g. cardiopulmonary disease or uncontrolled diabetes).

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