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]] [[de:Amilorid]] [[es:Amilorida]] [[fr:Amiloride]] [[hr:Amilorid]] [[hu:Amilorid]] [[ja:アミロライド]] [[pt:Amilorida]] [[th:อะมิโลไรด์]]