99%+ Purity Amiloride Hydrochloride CAS No.: 2016-88-8
Product Summary:
| Amiloride HCl, an antikaliuretic-diuretic agent, is a pyrazine-carbonyl-guanidine that is unrelated chemically to other known antikaliuretic or diuretic agents. It is the salt of a moderately strong base (pKa 8.7). It is designated chemically as 3,5-diamino-6-chloro- N-(diaminomethylene) pyrazinecarboxamide monohydrochloride, dihydrate and has a molecular weight of 302.12. |
99%+ Purity Amiloride Hydrochloride CAS No.: 2016-88-8
Amiloride Hydrochloride Details:
Product Name: Amiloride hydrochloride dihydrate
Synonyms: AMILORIDE HYDROCHLORIDE (500 MG);AMILORIDE HCL DIHYDRATE;AMILORIDE HYDROCHLORIDE 2-HYDRATE;Pyrazinecarboxamide, 3,5-diamino-N-(aminoiminomethyl)-6-chloro-, monohydrochloride, dihydrate;AMILORIDEHYDROCHLORIDE,USP;3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide hydrochloride dihydrate;Amiloride hydrochloride dihydrate;Miloride hydrochloride dihydrate
CAS: 17440-83-4
MF: C6H8ClN7O.HCl.2H2O
MW: 302.12
EINECS: 217-958-2
Product Categories: MK-870
Mol File: 17440-83-4.mol
Chemical Properties Crystalline solid or very light yellow powder.
Amiloride Hydrochloride Description:
Amiloride HCl, an antikaliuretic-diuretic agent, is a pyrazine-carbonyl-guanidine that is unrelated chemically to other known antikaliuretic or diuretic agents. It is the salt of a moderately strong base (pKa 8.7). It is designated chemically as 3,5-diamino-6-chloro- N-(diaminomethylene) pyrazinecarboxamide monohydrochloride, dihydrate and has a molecular weight of 302.12. Its empirical formula is C6H8CIN7O•HCl•2H2O.
Each tablet for oral administration contains 5 mg of Amiloride HCI, calculated on the anhydrous basis. Each tablet contains the following inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, D&C yellow #10 lake, dibasic calcium phosphate dihydrate, FD&C yellow #6 lake, magnesium stearate, microcrystalline cellulose and silicon dioxide.
Amiloride Hydrochloride Indications:
Amiloride HCl is indicated as adjunctive treatment with thiazide diuretics or other kaliureticdiuretic agents in congestive heart failure or hypertension to:
help restore normal serum potassium levels in patients who develop hypokalemia on the kaliuretic diuretic.
prevent development of hypokalemia in patients who would be exposed to particular risk if hypokalemia were to develop, e.g., digitalized patients or patients with significant cardiac arrhythmias.
The use of potassium-conserving agents is often unnecessary in patients receiving diuretics for uncomplicated essential hypertension when such patients have a normal diet. Amiloride HCl has little additive diuretic or antihypertensive effect when added to a thiazide diuretic.
Amiloride HCl should rarely be used alone. It has weak (compared with thiazides) diuretic and antihypertensive effects. Used as single agents, potassium sparing diuretics, including amiloride HCl, result in an increased risk of hyperkalemia (approximately 10% with amiloride). Amiloride HCl should be used alone only when persistent hypokalemia has been documented and only with careful titration of the dose and close monitoring of serum electrolytes.
Amiloride Hydrochloride Side Effect:
Amiloride HCl is usually well tolerated and, except for hyperkalemia (serum potassium levels greater than 5.5 mEq liter - see WARNINGS), significant adverse effects have been reported infrequently. Minor adverse reactions were reported relatively frequently (about 20%) but the relationship of many of the reports to amiloride HCl is uncertain and the overall frequency was similar in hydrochlorothiazide treated groups. Nausea/anorexia, abdominal pain, flatulence, and mild skin rash have been reported and probably are related to amiloride. Other adverse experiences that have been reported with amiloride are generally those known to be associated with diuresis, or with the underlying disease being treated.
The adverse reactions for amiloride HCl listed in the following table have been arranged into two groups: incidence greater than one percent; and incidence one percent or less. The incidence for group was determined from clinical studies conducted in the United States (837 patients treated with amiloride HCl). The adverse effects listed in group (include reports from the same clinical studies and voluntary reports since marketing. The probability of a causal relationship exists between amiloride HCl and these adverse reactions, some of which have been reported only rarely.
Amiloride Hydrochloride Clinical Pharmacology:
Amiloride HCl is a potassium-conserving (antikaliuretic) drug that possesses weak (compared with thiazide diuretics) natriuretic, diuretic, and antihypertensive activity. These effects have been partially additive to the effects of thiazide diuretics in some clinical studies. When administered with a thiazide or loop diuretic, amiloride has been shown to decrease the enhanced urinary excretion of magnesium which occurs when a thiazide or loop diuretic is used alone. Amiloride has potassium-conserving activity in patients receiving kaliureticdiuretic agents.
Amiloride HCl is not an aldosterone antagonist and its effects are seen even in the absence of aldosterone.
Amiloride exerts its potassium sparing effect through the inhibition of sodium reabsorption at the distal convoluted tubule, cortical collecting tubule and collecting duct; this decreases the net negative potential of the tubular lumen and reduces both potassium and hydrogen secretion and their subsequent excretion. This mechanism accounts in large part for the potassium sparing action of amiloride.
Amiloride usually begins to act within 2 hours after an oral dose. Its effect on electrolyte excretion reaches a peak between 6 and 10 hours and lasts about 24 hours. Peak plasma levels are obtained in 3 to 4 hours and the plasma half-life varies from 6 to 9 hours. Effects on electrolytes increase with single doses of amiloride HCl up to approximately 15 mg.
Amiloride HCl is not metabolized by the liver but is excreted unchanged by the kidneys. About 50 percent of a 20 mg dose of amiloride HCl is excreted in the urine and 40 percent in the stool within 72 hours. Amiloride has little effect on glomerular filtration rate or renal blood flow. Because amiloride HCl is not metabolized by the liver, drug accumulation is not anticipated in patients with hepatic dysfunction, but accumulation can occur if the hepatorenal syndrome develops.
