Amiloride Hydrochloride (Amiloride Hydrochloride) Drug Information: Overdosage and Contraindications

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May 24, 2012

Amiloride hydrochloride

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What are diuretics and how do they work?

The amount of fluid (water) retained by the body is controlled primarily by the kidneys. This occurs due to the kidney's ability to control the retention and elimination of sodium and chloride, because the amounts of sodium, chloride, and water in the body are carefully balanced. Thus, if sodium and chloride are eliminated from the body, water also is eliminated. Conversely, if sodium and chloride are retained by the body, so is water.

The elimination of sodium, chloride, and water from the body is somewhat complex. In the kidneys, sodium, chloride, and other small molecules are filtered out of the blood and into the tubules of the kidney where urine is formed. Most of the sodium, chloride, and water are reabsorbed into the blood before the filtered fluid leaves the kidney in the form of urine. To make matters even more complex, there are different mechanisms that are active in different parts of the tu...

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Amiloride Hydrochloride

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OVERDOSE

No data are available in regard to overdosage in humans.

The oral LD₅₀ of amiloride HCl (calculated as the base) is 56 mg/kg in mice and 36 to 85 mg/kg in rats, depending on the strain.

It is not known whether the drug is dialyzable.

The most likely signs and symptoms to be expected with overdosage are dehydration and electrolyte imbalance. These can be treated by established procedures. Therapy with amiloride HCl should be discontinued and the patient observed closely. There is no specific antidote. Emesis should be induced or gastric lavage performed.Treatment is symptomatic and supportive. If hyperkalemia occurs, active measures should be taken to reduce the serum potassium levels.

CONTRAINDICATIONS

Hyperkalemia

Amiloride HCl should not be used in the presence of elevated serum potassium levels (greater than 5.5 mEq per liter).

Antikaliuretic Therapy or Potassium Supplementation

Amiloride HCl should not be given to patients receiving other potassium-conserving agents, such as spironolactone or triamterene. Potassium supplementation in the form of medication, potassium-containing salt substitutes or a potassium-rich diet should not be used with amiloride HCl except in severe and/or refractory cases of hypokalemia. Such concomitant therapy can be associated with rapid increases in serum potassium levels. If potassium supplementation is used, careful monitoring of the serum potassium level is necessary.

Impaired Renal Function

Anuria, acute or chronic renal insufficiency, and evidence of diabetic nephropathy are contraindications to the use of amiloride HCl. Patients with evidence of renal functional impairment (blood urea nitrogen [BUN] levels over 30 mg per 100 mL or serum creatinine levels over 1.5 mg per 100 mL) or diabetes mellitus should not receive the drug without careful, frequent and continuing monitoring of serum electrolytes, creatinine, and BUN levels. Potassium retention associated with the use of an antikaliuretic agent is accentuated in the presence of renal impairment and may result in the rapid development of hyperkalemia.