Amiloride

Amiloride

Clinical data
Routes of administration	oral
ATC code	C03DB01 (WHO)
Pharmacokinetic data
Bioavailability	Readily absorbed
Metabolism	none
Elimination half-life	6 to 9 hours
Excretion	unchanged in urine
Identifiers
IUPAC name 3,5-diamino-6-chloro-N- (diaminomethylidene)pyrazine-2-carboxamide
CAS Number	2016-88-8
PubChem CID	16231
DrugBank	APRD00790
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C6H8ClN7O
Molar mass	229.627 g/mol

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Amiloride is a potassium-sparing diuretic, first approved for use in 1967 (then known as MK 870), used in the management of hypertension and congestive heart failure.

Structure

Amiloride is a guanidinium group containing pyrazine derivative.

Mode of action

Amiloride works by directly blocking the epithelial sodium channel (ENaC) thereby inhibiting sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys (this mechanism is the same for triamterene). This promotes the loss of sodium and water from the body, but without depleting potassium. The drug is often used in conjunction with thiazide (e.g. co-amilozide) or loop diuretics (e.g. co-amilofruse). 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.

A fraction of the effects of amiloride is inhibition of cyclic GMP-gated cation channels in the inner medullary collecting duct.

References

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