Amiloride

Amiloride
Clinical data
Trade namesMidamor, others
Other namesMK-870
AHFS/Drugs.comMonograph
Pregnancy
category
  • AU: C
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
Pharmacokinetic data
BioavailabilityReadily absorbed, 15–25%
Protein binding~23%
MetabolismNil
Onset of action2 hours (peak at 6–10 hours, duration ~24 hours)
Elimination half-life6 to 9 hours
Excretionurine (20–50%), feces (40%)
Identifiers
  • 3,5-diamino-6-chloro-N-(diaminomethylene)pyrazine-2-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.018.205 Edit this at Wikidata
Chemical and physical data
FormulaC6H8ClN7O
Molar mass229.63 g·mol−1
3D model (JSmol)
Melting point240.5 to 241.5 °C (464.9 to 466.7 °F)
  • Clc1nc(C(=O)\N=C(/N)N)c(nc1N)N
  • 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) checkY
  • Key:XSDQTOBWRPYKKA-UHFFFAOYSA-N checkY
  (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.[1][2] Amiloride is classified as a potassium-sparing diuretic. Amiloride is often used together with another diuretic, such as a thiazide or loop diuretic.[2] It is taken by mouth.[1] Onset of action is about two hours and it lasts for about a day.[2]

Common side effects include high blood potassium, vomiting, loss of appetite, rash, and headache.[1] The risk of high blood potassium is greater in those with kidney problems, diabetes, and those who are older.[1] Amiloride blocks the epithelial sodium channel (ENaC) in the late distal tubule, connecting tubule, and collecting duct of the nephron,[3] which both reduces absorption of sodium ion from the lumen of the nephron and reduces excretion of potassium ion into the lumen.[2]

Amiloride was developed in 1967.[4] It is on the World Health Organization's List of Essential Medicines.[5]

  1. ^ a b c d "Amiloride Hydrochloride". The American Society of Health-System Pharmacists. Archived from the original on 27 December 2016. Retrieved 8 December 2016.
  2. ^ a b c d World Health Organization (2009). Stuart MC, Kouimtzi M, Hill SR (eds.). WHO Model Formulary 2008. World Health Organization. pp. 328, 330. hdl:10665/44053. ISBN 9789241547659.
  3. ^ Nesterov V, Dahlmann A, Krueger B, Bertog M, Loffing J, Korbmacher C (November 2012). "Aldosterone-dependent and -independent regulation of the epithelial sodium channel (ENaC) in mouse distal nephron". American Journal of Physiology. Renal Physiology. 303 (9): F1289–F1299. doi:10.1152/ajprenal.00247.2012. PMID 22933298.
  4. ^ Progress in Drug Research/Fortschritte der Arzneimittelforschung/Progrés des recherches pharmaceutiques. Birkhäuser. 2013. p. 210. ISBN 9783034870948. Archived from the original on 2016-12-28.
  5. ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.