Amiloride

Amiloride
Clinical data
Trade names	Midamor, others
Other names	MK-870
AHFS/Drugs.com	Monograph
Pregnancy; category	AU: C;
Routes of; administration	By mouth
ATC code	C03DB01 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Bioavailability	Readily absorbed, 15–25%
Protein binding	~23%
Metabolism	Nil
Onset of action	2 hours (peak at 6–10 hours, duration ~24 hours)
Elimination half-life	6 to 9 hours
Excretion	urine (20–50%), feces (40%)
Identifiers
	IUPAC name 3,5-diamino-6-chloro-N-(diaminomethylene)pyrazine-2-carboxamide;
CAS Number	2016-88-8 ;
PubChem CID	16231;
IUPHAR/BPS	2421;
DrugBank	DB00594 ;
ChemSpider	15403 ;
UNII	7M458Q65S3;
KEGG	D07447 ;
ChEBI	CHEBI:2639 ;
ChEMBL	ChEMBL945 ;
CompTox Dashboard (EPA)	DTXSID9043853 ;
ECHA InfoCard	100.018.205
Chemical and physical data
Formula	C6H8ClN7O
Molar mass	229.63 g·mol−1
3D model (JSmol)	Interactive image;
Melting point	240.5 to 241.5 °C (464.9 to 466.7 °F)
	SMILES Clc1nc(C(=O)\N=C(/N)N)c(nc1N)N;
	InChI InChI=1S/C6H8ClN7O/c7-2-4(9)13-3(8)1(12-2)5(15)14-6(10)11/h(H4,8,9,13)(H4,10,11,14,15) ; Key:XSDQTOBWRPYKKA-UHFFFAOYSA-N ;
	(verify)

Amiloride, sold under the trade name Midamor among others, is a medication typically used with other medications to treat high blood pressure or swelling due to heart failure or cirrhosis of the liver. Amiloride is classified as a potassium-sparing diuretic. Amiloride is often used together with another diuretic, such as a thiazide or loop diuretic. It is taken by mouth. Onset of action is about two hours and it lasts for about a day.

Common side effects include high blood potassium, vomiting, loss of appetite, rash, and headache. The risk of high blood potassium is greater in those with kidney problems, diabetes, and those who are older. Amiloride blocks the epithelial sodium channel (ENaC) in the late distal tubule, connecting tubule, and collecting duct of the nephron, which both reduces absorption of sodium ion from the lumen of the nephron and reduces excretion of potassium ion into the lumen.

Amiloride was developed in 1967. It is on the World Health Organization's List of Essential Medicines.

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