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QuickView for amiloride (compound)


PubChem
Name: Amiloride
PubChem Compound ID: 16230
Description: 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)
Molecular formula: C6H9Cl2N7O
Molecular weight: 266.088 g/mol
Synonyms:
Pyrazinecarboxamide, N-amidino-3,5-diamino-6-chloro-, monohydrochloride; MLS000028442; Amiloride hydrochloride anhydrous; CCRIS 5959; EU-0100111; Amiloride chloride; SMR000058414; 2016-88-8; 2609-46-3; NCGC00024443-04.
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DrugBank
Identification
Name: Amiloride
Name (isomeric): DB00594
Drug Type: small molecule
Description: 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)
Synonyms:
Amilorida [INN-Spanish]; AMR; Amyloride; Amiloridum [INN-Latin]; Amiloride hydrochloride; Amiloride hydrochloride hydrate; Amiloride HCL
Brand: Midamor, Amipramizide, Amipramizid, Amipramidin, Guanamprazine, Amiprazidine, Guanamprazin
Brand name mixture:
Nu-Amilzide 5/50 mg Tab(Amiloride Hcl + Hydrochlorothiazide), Alti-Amiloride HCTZ(Amiloride Hcl + Hydrochlorothiazide), Novamilor Tab USP(Amiloride Hcl + Hydrochlorothiazide), Ami-Hydro Tab(Amiloride Hcl + Hydrochlorothiazide), Moduret(Amiloride Hcl + Hydrochlorothiazide), Riva-Amilzide 5/50 mg(Amiloride Hcl + Hydrochlorothiazide), Gen-Amilazide...
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Category: Diuretics, Sodium channel blockers
CAS number: 2016-88-8
Pharmacology
Indication: For use as adjunctive treatment with thiazide diuretics or other kaliuretic-diuretic agents in congestive heart failure or hypertension.
Pharmacology:
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 heart failure. The drug is often used in conjunction...
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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 sparing effect through the inhibition of sodium reabso...
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Absorption: Readily absorbed following oral administration.
Biotransformation: Amiloride is not metabolized by the liver but is excreted unchanged by the kidneys.
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.
Half Life: Plasma half-life varies from 6 to 9 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 electrolyte imbalance.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take with food to reduce irritation.
Avoid salt substitutes containing potassium.
Avoid natural licorice.
Avoid drastic changes in dietary habit.
Drug interaction:
BenazeprilIncreased risk of hyperkalemia
TasosartanIncreased risk of hyperkalemia
RamiprilIncreased risk of hyperkalemia
SpiraprilIncreased risk of hyperkalemia
QuinidineAmiloride may decrease the therapeutic effect of quinidine. Monitor for changes in the therapeutic and adverse effects of quinidine if amiloride if initiated, discontinued or dose changed.
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