아밀로라이드

Pharmaceuticals -> Listed in ZINC15

Pharmaceuticals -> Diuretics

Pharmaceuticals

-0.3

-0.86

Slightly soluble

1.22e+00 g/L

Breast Feeding; Lactation; Milk, Human; Diuretics

Pharmaceuticals

Diuretics

240.5-241.5

240 °C

157.0 Ų [M+Na]+ [CCS Type: DT; Buffer gas: N2; Ionization: ESI+; Dataset: TOXCAST; Source Identifier: DTXSID2024452]

151.08 Ų [M+Na]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]

Danger

H300 (12.5%): Fatal if swallowed [Danger Acute toxicity, oral]

P264, P264+P265, P270, P273, P280, P301+P316, P301+P317, P302+P352, P305+P351+P338, P305+P354+P338, P317, P321, P330, P332+P317, P337+P317, P362+P364, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 40 reports by companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Not Classified

REACH registered substance: Amiloride (EC: 220-024-7)

REACH registered substance: N-amidino-3,5-diamino-6-chloropyrazinecarboxamide (EC: 926-801-3)

Acute Tox. 2 (12.5%)

Not Classified

Amiloride therapy has not been associated with serum aminotransferase elevations. Idiosyncratic, clinically apparent liver injury from amiloride is rare, but several instances have been reported as isolated case reports in which the combination of amiloride with hydrochlorothiazide was used (Case 1). The numbers of cases have been too few to characterize the clinical features, but the latency to onset was ranged from 2 to 12 months and the pattern of injury either hepatocellular or mixed. Immunoallergic features and autoantibodies have not been associated with the liver injury from amiloride.

C - Cardiovascular system

QC - Cardiovascular system

C03DB01

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 with thiazide or loop diuretics. Due to its potassium-sparing capacities, hyperkalemia (high blood potassium levels) are occasionally observed in patients taking amiloride. The risk is high in concurrent use of ACE inhibitors or spironolactone. Patients are also advised not to use potassium-containing salt replacements.

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 reabsorption at the distal convoluted tubule, cortical collecting tubule and collecting duct; this decreases the net negative potential of the tubular lumen and reduces both potassium and hydrogen secretion and their subsequent excretion. Amiloride is not an aldosterone antagonist and its effects are seen even in the absence of aldosterone.

7DZO8EB0Z3

AMILORIDE

Physiologic Effects [PE] - Decreased Renal K+ Excretion

Physiologic Effects [PE] - Increased Diuresis

Established Pharmacologic Class [EPC] - Potassium-sparing Diuretic

Amiloride is a Potassium-sparing Diuretic. The physiologic effect of amiloride is by means of Decreased Renal K+ Excretion and Increased Diuresis.