pharmacopeia
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Mechanism of action

Sourced from openFDA

Mechanism-of-action class: Sodium-Potassium Exchanging ATPase Interactions.

Indications

Sourced from openFDA
  • 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.ICD-10: E87.6, I10, I50.9

Contraindications

Sourced from openFDA
  • 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.contraindicated

Dosage & administration

Sourced from openFDA

Amiloride HCl should be administered with food. Amiloride HCl, one 5 mg tablet daily, should be added to the usual antihypertensive or diuretic dosage of a kaliuretic diuretic. The dosage may be increased to 10 mg per day, if necessary. More than two 5 mg tablets of amiloride HCl daily usually are not needed, and there is little controlled experience with such doses. If persistent hypokalemia is documented with 10 mg, the dose can be increased to 15 mg, then 20 mg, with careful monitoring of electrolytes. In treating patients with congestive heart failure after an initial diuresis has been achieved, potassium loss may also decrease and the need for amiloride HCl should be re-evaluated. Dosage adjustment may be necessary. Maintenance therapy may be on an intermittent basis. If it is necessary to use amiloride HCl alone (see INDICATIONS), the starting dosage should be one 5 mg tablet daily. This dosage may be increased to 10 mg per day, if necessary. More than two 5 mg tablets usually are not needed, and there is little controlled experience with such doses. If persistent hypokalemia is documented with 10 mg, the dose can be increased to 15 mg, then 20 mg, with careful monitoring of electrolytes.

Warnings & precautions

Sourced from openFDA

Hyperkalemia Like other potassium-conserving agents, amiloride may cause hyperkalemia (serum potassium levels greater than 5.5 mEq per liter) which, if uncorrected, is potentially fatal. Hyperkalemia occurs commonly (about 10%) when amiloride is used without a kaliuretic diuretic. This incidence is greater in patients with renal impairment, diabetes mellitus (with or without recognized renal insufficiency), and in the elderly. When amiloride is used concomitantly with a thiazide diuretic in patients without these complications, the risk of hyperkalemia is reduced to about 1-2%. It is thus essential to monitor serum potassium levels carefully in any patient receiving amiloride, particularly when it is first introduced, at the time of diuretic dosage adjustments, and during any illness that could affect renal function. The risk of hyperkalemia may be increased when potassium-conserving agents, including amiloride HCl, are administered concomitantly with an angiotensin-converting enzyme inhibitor, an angiotensin II receptor antagonist, cyclosporine or tacrolimus. (See PRECAUTIONS , Drug Interactions. ) Warning signs or symptoms of hyperkalemia include paresthesias, muscular weakness, fatigue, flaccid paralysis of the extremities, bradycardia, shock, and ECG abnormalities. Monitoring of the serum potassium level is essential because mild hyperkalemia is not usually associated with an abnormal ECG. When abnormal, the ECG in hyperkalemia is characterized primarily by tall, peaked T waves or elevations from previous tracings.

Adverse reactions

Sourced from openFDA

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: (1) incidence greater than one percent; and (2) incidence one percent or less. The incidence for group (1) was determined from clinical studies conducted in the United States (837 patients treated with amiloride HCl). The adverse effects listed in group (2) 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. *Reactions occurring in 3% to 8% of patients treated with amiloride HCl. (Those reactions occurring in less than 3% of the patients are unmarked.) **See WARNINGS.

Use in specific populations

Sourced from openFDA

Pregnancy Pregnancy Category B . Teratogenicity studies with amiloride HCl in rabbits and mice given 20 and 25 times the maximum human dose, respectively, revealed no evidence of harm to the fetus, although studies showed that the drug crossed the placenta in modest amounts. Reproduction studies in rats at 20 times the expected maximum daily dose for humans showed no evidence of impaired fertility. At approximately 5 or more times the expected maximum daily dose for humans, some toxicity was seen in adult rats and rabbits and a decrease in rat pup growth and survival occurred. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Overdosage

Sourced from openFDA

No data are available in regard to overdosage in humans. The oral LD 50 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.

Approval history

Sourced from openFDA
  • Oct 5, 1981NDANDA018200Padagis Us
  • Jan 22, 1986ANDAANDA070346Ph Health
  • May 10, 1988ANDAANDA071111Barr
  • Jan 30, 2009ANDAANDA079133Sigmapharm Labs Llc

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
907 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Dyspnoea727.9%
  2. 2Diarrhoea636.9%
  3. 3Nausea546.0%
  4. 4Vomiting465.1%
  5. 5Fall394.3%
  6. 6Malaise394.3%
  7. 7Fatigue374.1%
  8. 8Confusional State353.9%
  9. 9Drug Interaction353.9%
  10. 10Headache333.6%
  11. 11Hyperkalaemia333.6%
  12. 12Abdominal Pain323.5%
  13. 13Renal Failure Acute313.4%
  14. 14Pruritus303.3%
  15. 15Arthralgia293.2%

Literature

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Recent PubMed references pinned to Amiloride as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 74 ClinicalTrials.gov registrations naming Amiloride as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Amiloride work?
Mechanism-of-action class: Sodium-Potassium Exchanging ATPase Interactions.
What is Amiloride used for?
According to FDA labeling, Amiloride carries indications including: 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Amiloride?
Amiloride is classified as Other potassium-sparing agents, Potassium-sparing Diuretic, Sodium-Potassium Exchanging ATPase Interactions, Decreased Blood Pressure, Decreased Collecting Duct K+ Excretion, Decreased Distal Tubule K+ Excretion, Decreased Renal Ca++ Excretion, Decreased Renal K+ Excretion, Increased Collecting Duct Na+ Excretion, Increased Distal Tubule Na+ Excretion, Increased Diuresis, Increased Renal Mg++ Excretion.
What are the contraindications for Amiloride?
Amiloride labeling lists contraindications including: 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.. Always consult the full prescribing information and a clinician.
Note. Data for amiloride is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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