Description

Simple

A medication used to treat high blood pressure and heart failure.

Clinical

A pyrizine compound used to treat hypertension and congestive heart failure.

Overview

A pyrazine compound inhibiting sodium reabsorption through sodium channels in renal epithelial cells. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with diuretics to spare potassium loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705)

Pharmacology

Indication

For use as adjunctive treatment with thiazide diuretics or other kaliuretic-diuretic agents in congestive heart failure or hypertension.

Pharmacodynamic

Amiloride, an antikaliuretic-diuretic agent, is a pyrazine-carbonyl-guanidine that is unrelated chemically to other known antikaliuretic or diuretic agents. It is an antihypertensive, potassium-sparing diuretic that was first approved for use in 1967 and helps to treat hypertension and congestive he... Read more

Mechanism of action

Amiloride works by inhibiting sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys by binding to the amiloride-sensitive sodium channels. This promotes the loss of sodium and water from the body, but without depleting potassium. Amiloride exerts its potassium spar... Read more

Absorption

Readily absorbed following oral administration.

Protein binding

Information currently not available.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

Plasma half-life varies from 6 to 9 hours.

Route of elimination

Amiloride HCl is not metabolized by the liver but is excreted unchanged by the kidneys. About 50 percent of a 20 mg dose of amiloride HCl is excreted in the urine and 40 percent in the stool within 72 hours.

Toxicity

No data are available in regard to overdosage in humans. The oral LD50 of amiloride hydrochloride (calculated as the base) is 56 mg/kg in mice and 36 to 85 mg/kg in rats, depending on the strain. The most likely signs and symptoms to be expected with overdosage are dehydration and electro... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Nausea US
  • Kind: experimental
    • Percent: 3-8%
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 3-8%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 3-8%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 3-8%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 3-8%
  • Clinical Trial
    Gas pain US
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Appetite changes US
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Weakness US
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Encephalopathy US
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Cough US
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Elevated serum potassium levels US
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Muscle Cramps US
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Impotence US
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Back Pain US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Neck ache US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Shoulder ache US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Chest Pain US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Angina Pectoris US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Pain in extremities US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Palpitation US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Orthostatic Hypotension US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Arrhythmia US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Abdominal fullness US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    GI Bleeding US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Jaundice US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Thirst US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    GI Disturbance US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Dyspepsia US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Flatulence US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Heartburn US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Dryness of mouth US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Itching US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Skin Rash US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Pruritus US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Alopecia US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Joint Pain US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Leg ache US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Paresthesia US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Tremors US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Vertigo US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Nervousness US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Mental confusion US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Insomnia US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Depression US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing
    Decreased libido US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial Post Marketing

    Contraindications

    • Regions: US
    • With Categories Coadmin:
        • Name: Potassium-Sparing Diuretics
        • Drugbank Id: DBCAT002702
        • Mesh Id: D062865
    • Regions: US
    • With Therapies:
        • Name: Potassium supplementation
        • Drugbank Id: DBCOND0107850
    • Regions: US
    • Patient Conditions:
        • Name: Impaired Renal Function
        • Drugbank Id: DBCOND0038927
    • Regions: US
    • Patient Conditions:
        • Name: Hyperkalemia
        • Drugbank Id: DBCOND0003949

    Food Interactions

    Avoid drastic dietary changes.

    Avoid natural licorice.

    Avoid potassium-containing products.

    Take with food. Food reduces irritation.