Amiloride
1128211
221482983
2008-06-24T18:21:53Z
BOT-Superzerocool
338065
robot Adding: [[es:Amilorida]]
{{drugbox
| IUPAC_name = 3,5-diamino-6-chloro-''N''-(diaminomethylene)pyrazine-2-carboxamide
| image = Amiloride structure.svg
| width=250
| CAS_number = 2016-88-8
| ATC_prefix = C03
| ATC_suffix = DB01
| ATC_supplemental =
| PubChem = 16231
| DrugBank = APRD00790
| C=6 | H=8 | Cl=1 | N=7 | O=1
| molecular_weight = 229.627 g/mol
| bioavailability = Readily absorbed
| protein_bound =
| metabolism = none
| elimination_half-life = 6 to 9 hours
| excretion = unchanged in urine
| pregnancy_category =
| legal_status =
| routes_of_administration = oral
}}
'''Amiloride''' is a [[potassium-sparing diuretics|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 [[guanidine|guanidinium]] group containing [[pyrazine]] [[derivative (chemistry)|derivative]].
==Mode of action==
Amiloride works by directly blocking the [[epithelial sodium channel]] (ENaC) thereby inhibiting [[sodium]] reabsorption in the [[distal convoluted tubule]]s and collecting ducts in the [[kidney]]s (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 diuretic]]s (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 inhibitor]]s or [[spironolactone]]. Patients are also advised not to use potassium-containing salt replacements.<ref>LoSalt [http://www.losalt.com/docs/lo_salt_web_advice.pdf Advisory Statement] (PDF)</ref> Amiloride also carries the risk of developing an [[acidosis]].
A fraction of the effects of amiloride is inhibition of [[cyclic GMP-gated cation channel]]s in the [[inner medullary collecting duct]].<ref name=boron875> {{cite book |author=Walter F., PhD. Boron |title=Medical Physiology: A Cellular And Molecular Approaoch |publisher=Elsevier/Saunders |location= |year= |pages= |isbn=1-4160-2328-3 |oclc= |doi=}} page 875 </ref>
==See also==
*[[Benzamil]]
==References==
<references/>
{{Antihypertensives and diuretics}}
{{pharma-stub}}
[[Category:Potassium-sparing diuretics]]
[[Category:Pyrazines]]
[[Category:Guanidines]]
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