Yes

Diuretic, Potassium Sparing

Counteracts potassium loss induced by other diuretics in the treatment of hypertension or edematous conditions including CHF, hepatic cirrhosis, and hypoaldosteronism; usually used in conjunction with more potent diuretics such as thiazides or loop diuretics

B

Hypersensitivity to amiloride or any component; presence of elevated serum potassium levels (>5.5 mEq/L); if patient is receiving other potassium-conserving agents (eg, spironolactone, triamterene) or potassium supplementation (medicine, potassium-containing salt substitutes, potassium-rich diet); anuria; acute or chronic renal insufficiency; evidence of diabetic nephropathy. Patients with evidence of renal impairment or diabetes mellitus should not receive this medicine without close, frequent monitoring of serum electrolytes and renal function.

May cause hyperkalemia (patients with renal impairment, diabetes and the elderly are at greatest risk). Should be stopped at least 3 days before glucose tolerance testing. Use caution in severely ill patients in whom respiratory or metabolic acidosis may occur.

1% to 10%:

Central nervous system: Headache, fatigue, dizziness

Endocrine & metabolic: Hyperkalemia, hyperchloremic metabolic acidosis, dehydration, hyponatremia, gynecomastia

Gastrointestinal: Nausea, diarrhea, vomiting, abdominal pain, gas pain, appetite changes, constipation

Genitourinary: Impotence

Neuromuscular & skeletal: Muscle cramps, weakness

Respiratory: Cough, dyspnea

<1% (Limited to important or life-threatening symptoms): Orthostatic hypotension, arrhythmias, palpitations, chest pain, alopecia, GI bleeding, polyuria, bladder spasms, dysuria, jaundice, increased intraocular pressure, shortness of breath

Clinical signs are consistent with dehydration and electrolyte disturbance; large amounts may result in life-threatening hyperkalemia (>6.5 mEq/L)

This can be treated with I.V. glucose (dextrose 25% in water), with rapid-acting insulin, with concurrent I.V. sodium bicarbonate and, if needed, Kayexalate® oral or rectal solutions in sorbitol; persistent hyperkalemia may require dialysis.

Amoxicillin's absorption may be reduced; avoid concurrent use or observe for clinical response.

Angiotensin-converting enzyme inhibitors can cause hyperkalemia, especially in patients with renal impairment, potassium-rich diets, or on other drugs causing hyperkalemia; avoid concurrent use or monitor closely.

Potassium supplements may further increase potassium retention and cause hyperkalemia; avoid concurrent use.

Quinidine and amiloride together may increase risk of malignant arrhythmias; avoid concurrent use.

Interferes with potassium/sodium exchange (active transport) in the distal tubule, cortical collecting tubule and collecting duct by inhibiting sodium, potassium-ATPase; decreases calcium excretion; increases magnesium loss

Onset of action: 2 hours

Duration: 24 hours

Absorption: Oral: ~15% to 25%; Onset: 2 hours; Duration: 24 hours

Distribution: V_d: 350-380 L

Protein binding: 23%

Metabolism: No active metabolites

Half-life: Normal renal function: 6-9 hours; End-stage renal disease: 8-144 hours

Peak serum concentration: 6-10 hours

Elimination: Unchanged equally in the urine and the feces

Oral:

Adults: 5-10 mg/day (up to 20 mg)

Elderly: Initial: 5 mg once daily or every other day

Dosing adjustment in renal impairment:

Cl_cr 10-50 mL/minute: Administer at 50% of normal dose.

Cl_cr <10 mL/minute: Avoid use.

This diuretic does not cause you to lose potassium; because salt substitutes and low-salt milk may contain potassium, do not use these products without checking with your physician, too much potassium can be as harmful as too little

I & O, daily weights, blood pressure, serum electrolytes, renal function

potassium (S)

Amiloride may cause hyperkalemia, the EKG manifestations of which include peaked T waves, QRS prolongation, and cardiac conduction abnormalities.

May cause drowsiness; rarely may cause insomnia and depression

May cause impotence and orthostatic hypotension which may be exacerbated by psychotropics; effective agent for the treatment of lithium induced diabetes insipidus

No information available to require special precautions

No effects or complications reported

Take as directed, preferably early in day. Do not increase dietary intake of potassium unless instructed by prescriber (too much potassium can be as harmful as too little). You may experience dizziness or fatigue; use caution when driving or engaging in tasks that require alertness until response to drug is known. You may experience constipation (increased dietary fluid, fiber, or fruit may help), impotence (reversible), or loss of head hair (rare). Report muscle cramping or weakness, unresolved nausea or vomiting, palpitations, or difficulty breathing. Breast-feeding precautions: Do not breast-feed.

Assess fluid status via daily weights, I & O ratios, standing and supine blood pressures; observe for hyperkalemia; if ordered once daily, dose should be given in the morning

Tablet, as hydrochloride: 5 mg

Jaffey L and Martin A, "Malignant Hyperkalemia After Amiloride/Hydrochlorothiazide Treatment," Lancet, 1981, 1(8232):1272.

Kleyman TR and Cragoe EJ Jr, "The Mechanism of Action of Amiloride," Semin Nephrol, 1988, 8(3):242-8.

Wang L, Sheldon RS, Mitchell LB, et al, "Amiloride-Quinidine Interaction: Adverse Outcomes," Clin Pharmacol Ther, 1994, 56(6 Pt 1):659-67.

Westphal JF, Jehl F, Brogard JM, et al,"Amoxicillin Intestinal Absorption Reduction by Amiloride: Possible Role of the Na⁺-H⁺ Exchanger," Clin Pharmacol Ther 1995, 57(3):257-64.