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amiloride (Midamor)

 

Classes: Diuretics, Potassium-Sparing

Dosing and uses of Midamor (amiloride)

 

Adult dosage forms and strengths

tablet

  • 5mg

 

Congestive Heart Failure

5-10 mg/day PO qDay OR divided q12hr

 

Hypertension

5-10 mg/day PO qDay OR divided q12hr

 

Thiazide-Induced Hypokalemia

5-10 mg/day PO qDay OR divided q12hr

 

Renal Impairment

CrCl 10-50 mL/minute: 50% normal dose

CrCl <10 mL/minute: Not recommended

 

Overdose Management

May use normal saline for volume replacement

May use dopamine or norepinephrine to treat hypotension

Treat hyperkalemia with IV glucose (dextrose 25% in water) with rapid acting insulin with concurrent IV sodium bicarbonate and use oral or rectal solutions of kayexalate in sorbitol if needed

If dysrhythmia due to decreased K+ or Mg+ suspected replace aggressively

Discontinue treatment if no symptoms after 6hr

 

Other Information

Take with food

Monitor: Serum potassium

See also combo with hydrochlorothiazide

 

Other Indications & Uses

Off-label: cystic fibrosis, Li-induced polyuria

 

Pediatric dosage forms and strengths

tablet

  • 5mg

 

Hypertension (Off-label)

0.4-0.625 mg/kg/day PO; not to exceed 20 mg/day

 

Geriatric dosage forms and strengths

5-10 mg/day PO qDay OR every other day

Maximum dosage limit: 20 mg PO qDay; 40 mg PO qDay has been used

Elderly patients may be more sensitive to the diuretic effects of the drug and are more likely to have age-associated renal dysfunction

 

Midamor (amiloride) adverse (side) effects

1-10%

Hyperkalemia (10%)

Anorexia (3-8%)

Diarrhea (3-8%)

Headache (3-8%)

Nausea (3-8%)

Vomiting (3-8%)

Abdominal pain (<3%)

Appetite changes (<3%)

Constipation (<3%)

Cough (<3%)

Dizziness (<3%)

Dyspnea (<3%)

Encephalopathy (<3%)

Fatigue (<3%)

Gas pain (<3%)

Impotence (<3%)

Muscle cramps (<3%)

Weakness (<3%)

 

Warnings

Black box warnings

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.

When amiloride is used concomitantly with a thiazide diuretic in patients without these complications, the risk of hyperkalemia is reduced to about 1-2%. Monitoring serum potassium levels carefully in any patient receiving amiloride is essential, particularly when it is first introduced, at the time of diuretic dosage adjustments, and during any illness that could affect renal function.

 

Contraindications

Hypersensitivity to amiloride

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]) diabetes

 

Cautions

Anuria, DM, diabetic nephropathy, electrolyte imbalance and increases BUN, metabolic or respiratory acidosis

 

Pregnancy and lactation

Pregnancy category: B

Lactation: excretion in milk unknown/not recommended

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Midamor (amiloride)

Mechanism of action

Direct effect on renal distal convoluted tubule to inhibit Na+ reabsorption from the lumen

Inhibits Na/K-ATPase, decreases Ca++, Mg++ and hydrogen excretion

 

Pharmacokinetics

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

Bioavailability: 30-90%

Protein Bound: 23%

Vd: 350-380 L

Metabolism: NOT metabolized in the liver; no active metabolites

Excretion

  • Urine: 50%
  • Feces: 40-50%