Difference between revisions of "Amiloride"
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Latest revision as of 15:44, 19 September 2010
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| Systematic (IUPAC) name | |
|---|---|
|
3,5-diamino-6-chloro-N-(diaminomethylene)pyrazine-2-carboxamide | |
| Clinical data | |
| Pregnancy category |
|
| Routes of administration | oral |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Bioavailability | Readily absorbed |
| Metabolism | none |
| Biological half-life | 6 to 9 hours |
| Excretion | unchanged in urine |
| Identifiers | |
| CAS Number | 2016-88-8 |
| ATC code | C03DB01 (WHO) |
| PubChem | CID 16231 |
| IUPHAR/BPS | 2421 |
| DrugBank | APRD00790 |
| ChemSpider | 15403 |
| Chemical data | |
| Formula | C6H8ClN7O |
| Molar mass | 229.627 g/mol[[Script error: No such module "String".]] |
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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.
Mechanism of action
Amiloride works by directly blocking the epithelial sodium channel (ENaC) thereby inhibiting sodium reabsorption in the late distal convoluted tubules, connecting tubules, and collecting ducts in the kidneys (this mechanism is the same for triamterene).[1] 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.[2] Amiloride also carries the risk of developing an acidosis.
A fraction of the effects of amiloride is inhibition of cyclic GMP-gated cation channels in the inner medullary collecting duct.[3]
Amiloride has a second action on the heart, blocking Na+/H+ exchangers Sodium-hydrogen antiporter 1 or NHE-1. This minimizes reperfusion injury in ischemic attacks.
See also
References
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es:Amilorida fa:آمیلوراید fr:Amiloride hr:Amilorid it:Amiloride hu:Amilorid ja:アミロライド pl:Amiloryd pt:Amilorida
th:อะมิโลไรด์- ↑ Loffing, Johannes and Kaissling, Brigitte (2003). "Sodium and calcium transport pathways along the mammalian distal nephron: from rabbit to human". Am J Physiol Renal Physiol. 284: F628–F643. PMID 12620920.
- ↑ LoSalt Advisory Statement (PDF)
- ↑ Walter F., PhD. Boron. Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3. page 875
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- 2Fix
- Potassium-sparing diuretics
- Pyrazines
- Guanidines
- World Health Organization essential medicines
- Cardiovascular system drug stubs
- CS1 maint: Multiple names: authors list
