Drug information of Amiloride
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. Amilorideis used in conjunction with diuretics to spare potassium loss.
Mechanism of effect
Amiloride 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. 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.
Amiloride, 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 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.
Half-Life: 6-9 hr
Duration: 24 hr
Onset: initial effect: 2-3 hr, max effect: 6-10 hr
Peak Plasma Time: 3-4 hr
Protein Bound: 23%
Vd: 350-380 L
Metabolism: NOT metabolized in the liver; no active metabolites
Drug indicationspolyuria , cystic fibrosis patients
It is used to treat or prevent low potassium levels in ongestive heart failure or hypertension
Usual Adult Dose for Ascites, Congestive Heart Failure, Edema, Hypertension,
Initial dose: 5 mg orally once a day.
Maintenance dose: 5-10 mg once a day.
Renal Dose Adjustments
CrCl< 25 mL/min: Not recommended.
CrCl 25-80 mL/min: The usual dose is decreased by 50%.
Amilorideis used to prevent hypokalemia in patients receiving diuretics or digoxin. Doses as high as 15-20 mg divided 1-2 times a day have been used.
5-10 mg/day divided 1-2 times a day
5-10 mg/day PO qDay OR every other day
0.4-0.625 mg/kg/day PO; not to exceed 20 mg/day
Drug contraindicationsdiabetes , impairment of renal function , hypersensitivity to this drug , Hyperkalemia (K+ >5.5 mEq/L [5.5 mmol/L])
Concomitant use with K+-sparing diuretic, or K supplementation
Impaired renal function (Scr>1.5 mg/dL [132.6 umol/L], or BUN >30 mg/dL [10.7 mmol/L])
Side effectsDiarrhea , Headache , nausea , constipation , dizziness , vomiting , vertigo , asthenia , impotence , anorexia , flatulence , Muscle cramps , tiredness , Restlessness , Abdominal pain
InteractionsAmlodipine/Atorvastatine , Triamterene-H , eplerenone , Spironolactone , Potassium chloride , Drospirenone , Cyclosporine , Triamterene , potassium citrate , ethacrynic acid , Trimethoprim , Bumetanide , Eprosartan , Perindopril , Canagliflozin , Telmisartan , Sacubitril and valsartan , Azilsartan , Irbesartan , Olmesartan , Treprostinil , Benorilate , Blonanserin , xipamide
Like other potassium-conserving agents, amiloride may cause hyperkalemia (serum potassium levels greater than 5.5 mEq/L), which, if not corrected, 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 elderly persons.
Monitoring serum potassium levels carefully in any patient receiving amiloride is essential.
Anuria, DM, diabetic nephropathy, electrolyte imbalance and increases BUN, metabolic or respiratory acidosis
Points of recommendation
Take with food
Monitor: Serum potassium