AMILORIDE HYDROCHLORIDE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

AMILORIDE HYDROCHLORIDE (UNII: FZJ37245UC) (AMILORIDE - UNII:7DZO8EB0Z3)

Available from:

Physicians Total Care, Inc.

INN (International Name):

AMILORIDE HYDROCHLORIDE

Composition:

AMILORIDE HYDROCHLORIDE 5 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Amiloride HCl is indicated as adjunctive treatment with thiazide diuretics or other kaliuretic-diuretic 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). Amilo

Product summary:

Amiloride HCl Tablets, 5 mg, are off-white to light yellow, diamond-shaped, compressed tablets, embossed with "P291". They are supplied in Protect from moisture, freezing and excessive heat. Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]

Authorization status:

New Drug Application

Summary of Product characteristics

AMILORIDE HYDROCHLORIDE - AMILORIDE HYDROCHLORIDE TABLET
PHYSICIANS TOTAL CARE, INC.
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AMILORIDE HCL TABLETS, USP
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 C H ClN O•HCl•2H O and its structural formula is:
Amiloride HCl is available for oral use as tablets containing 5 mg of
anhydrous amiloride HCl. Each
tablet contains the following inactive ingredients: calcium phosphate,
lactose, magnesium stearate and
starch.
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 HCl has been shown to decrease the
enhanced urinary excretion of
magnesium which occurs when a thiazide or loop diuretic is used alone.
Amiloride HCl has potassium-
conserving activity in patients receiving kaliuretic-diuretic agents.
Amiloride HCl is not an aldosterone antagonist and its effects are
seen even in the absence of
aldosterone.
Amiloride HCl 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 HCl usually begins to act within 2 hours after an oral dose.
Its effect on electrolyte
excretion reaches a peak between 6 and