8 Pharmacology and Biochemistry 8.1 Pharmacology Amiloride, an antikalivretic dretic agent is a pyrazine-carbonyl-guanidine that is unelated chemically to other ‘now antikaliurtic or diuretic agents. tis an antihypertensive, potassum-sparing diuretic that was fst approved ‘or use in 1967 and helps to treat hypertension and congestive hear allure, The drug is often used in conjunction ith thiazide or loop diuretics. Due to its potassum-sparing capacities, hyperkalemia (high blood potassium levels) {are occasionally observed in patients taking amiloride. The risks high in concurrent use of ACE inhibitors or spitonolactone, Patients are also advised not to use potassuir-containing salt replacements. » from DrapBank co ‘Amilorde isa synthetic pyrazine derivative with antikaliuretic and diuretic properties. Amiloride inhibits sodium ‘channels located in the distal tubules and collecting ducts ofthe kidney, thereby preventing the absorption of Sodium and inceasing its excretion along with wate, to produce natures. In response to the typernatremic conditions in the kidney, the plasma membrane becomes hyperpolatized and electrochemical forces are reduced, which then prevents the excretion of potassium and hydrogen into the lumen, » from NOI 8.2 MeSH Pharmacological Classification ‘Acid Sensing Ton Channel Blockers ‘A subclass of sodium channel blockers that are specific for ACID-SENSING SODIUM CHANNELS. Soo alist of PubChem compounds matching this category » for Mest Diuretics ‘Agents that promote the excretion of urine through ther effects on kidney function. See 3 list of PubChem ‘compounds matching this category. e » from MeSH Epithelial Sodium Channel Blockers ‘Aubclass of sodium channel blockers that ae specific for EPITHELIAL SODIUM CHANNELS, See lst of PubChem ‘compounds matching this category » from Mest88 Mechanism of Action ‘Amiloride works by inhibiting sodium reabsorption inthe distal convoluted tubules and collecting ducts inthe ‘Kidneys by binding tothe amiloride-sensitive sodium channels. Tis promotes the loss of sodium and water from the ‘body, but without depleting potassium. Amiloride exerts its potassium sparing effect through the inhibition of sodium reabsorption atthe distal convoluted tubule, cortical collecting tubule and collecting duct this decreases the net negative potential ofthe tubular lumen and reduces both potassium and bycogen secretion and their subsequent excretion. Amiloride isnot an aldosterone antagonist and is effects are seen even in the absence of aldosterone. eet ‘Aeneid este soi ctu stu lts ‘Aeerdezenstvesodimctoanel tnt bets ‘Aner senstvesod cana stuit gana ‘Aone sense inet cppercetaing ‘Act sercrlonchevel2 ‘Acksesrgon chal Seaiunyaoes exchanger 1 riaceypeplamingen eat Proteln roten Protea Protein Dooon°**"! e i : DOOROTEOO: + from DrugBank resin Unocto fiman LIGNE tman SLATE Human 0165150 Human ROHS EEE EEE EVE