Amiloride



Amiloride
Systematic (IUPAC) name
3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide
Identifiers
CAS number 2016-88-8
ATC code C03DB01
PubChem 16231
DrugBank APRD00790
Chemical data
O 
Mol. mass 229.627 g/mol
Pharmacokinetic data
Bioavailability Readily absorbed
Metabolism none
Half life 6 to 9 hours
Excretion unchanged in urine
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes oral

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 derivative.

Mode of action

Amiloride works by directly blocking the epithelial sodium channel (ENaC) thereby inhibiting spironolactone. Patients are also advised not to use potassium-containing salt replacements.[1]

A fraction of the effects of amiloride is inhibition of cyclic GMP-gated cation channels in the inner medullary collecting duct.[2]

References

  1. ^ LoSalt Advisory Statement (PDF)
  2. ^ Walter F., PhD. Boron. Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3.  page 875
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