Amilorid
Amilorid Uses, Dosage, Side Effects, Food Interaction and all others data.
A pyrazine compound inhibiting sodium reabsorption through sodium channels in renal epithelial cells. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amilorid is used in conjunction with diuretics to spare potassium loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705)
Amilorid, an antikaliuretic-diuretic agent, is a pyrazine-carbonyl-guanidine that is unrelated chemically to other known antikaliuretic or diuretic agents. It is an antihypertensive, potassium-sparing diuretic that was first approved for use in 1967 and helps to treat hypertension and congestive heart failure. The drug is often used in conjunction with thiazide or loop diuretics. Due to its potassium-sparing capacities, hyperkalemia (high blood potassium levels) are occasionally observed in patients taking amiloride. The risk is high in concurrent use of ACE inhibitors or spironolactone. Patients are also advised not to use potassium-containing salt replacements.
| Trade Name | Amilorid |
| Availability | Prescription only |
| Generic | Amiloride |
| Amiloride Other Names | Amilorid, Amilorida, Amiloride, Amiloridum, Amipramidin, Amipramidine, Amyloride |
| Related Drugs | amlodipine, lisinopril, metoprolol, losartan, furosemide, carvedilol, hydrochlorothiazide, spironolactone, Lasix, chlorthalidone |
| Type | |
| Formula | C6H8ClN7O |
| Weight | Average: 229.627 Monoisotopic: 229.04788562 |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Amilorid is a pyrizine compound used to treat hypertension and congestive heart failure.
For use as adjunctive treatment with thiazide diuretics or other kaliuretic-diuretic agents in congestive heart failure or hypertension.
Amilorid is also used to associated treatment for these conditions: Ascites, Calcium Nephrolithiasis, Congestive Heart Failure (CHF), High Blood Pressure (Hypertension), Hypokalemia, Metabolic Alkalosis, Polyuria
How Amilorid works
Amilorid works by inhibiting sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys by binding to the amiloride-sensitive sodium channels. This promotes the loss of sodium and water from the body, but without depleting potassium. Amilorid 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. Amilorid is not an aldosterone antagonist and its effects are seen even in the absence of aldosterone.
Toxicity
No data are available in regard to overdosage in humans. The oral LD50 of amiloride hydrochloride (calculated as the base) is 56 mg/kg in mice and 36 to 85 mg/kg in rats, depending on the strain. The most likely signs and symptoms to be expected with overdosage are dehydration and electrolyte imbalance.
Food Interaction
- Avoid drastic dietary changes.
- Avoid natural licorice.
- Avoid potassium-containing products.
- Take with food. Food reduces irritation.
Amilorid Alcohol interaction
[Moderate]
Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.
Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.
Caution and close monitoring for development of hypotension is advised during coadministration of these agents.
Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.
Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.
Amilorid Drug Interaction
Unknown: aspirin, aspirin, apixaban, apixaban, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, furosemide, furosemide, atorvastatin, atorvastatin, pregabalin, pregabalin, levothyroxine, levothyroxine, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Amilorid Disease Interaction
Major: acidosis, diabetes, electrolytes/fluid, hyperkalemia, liver disease, renal dysfunction
Elimination Route
Readily absorbed following oral administration.
Half Life
Plasma half-life varies from 6 to 9 hours.
Elimination Route
Amilorid 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.
Innovators Monograph
You find simplified version here Amilorid
