Amiloride

Amiloride Pharmacology
 
Amiloride
About Amiloride
Potassium-Sparing Diuretic , a pyrazine-carbonyl-guanidine, Diuretic, Antihypertensive.
Mechanism of Action of Amiloride
Amiloride is a guanidine derivative which exerts its diuretic action by interacting with renal epithelial Na+ channels in distal tubules and collecting duct and prevents sodium reabsorption. It prevents potassium lose. It also increases chloride, bicarbonate, and water excretion and decreases H+ excretion. The drug augment the natriuretic and anti hypertensive response of other drugs. It is used in the management of edema associated with congestive heart failure, hepatic cirrhosis and idiopathic edema. It is used mainly in combination with other drugs in the management of hypertension and to correct hypokalemia caused by other diuretic drugs.
Pharmacokinets of Amiloride
Absorption: Orally absorbed up to 50%. Food decreases absorption. Distribution: Widely distributed extravascularly. Metabolism: It is not metabolized in the body. Excretion: Excreted mainly through urine.
Onset of Action for Amiloride
2hours
Duration of Action for Amiloride
24 hours.
Half Life of Amiloride
6 to 9 hours
Side Effects of Amiloride
1.Headache
2.Orthostatic hypotension
3.Confusion
4.Nausea
5.Diarrhoea
6.Anorexia
7.Weakness
8.Hyperkalemia
9.Hyponatremia
10.Aplastic anaemia
11.Neutropenia
12.Impotence
13.Altered liver function tests
14.Altered kidney function tests
15.Gastro intestinal disturbances
16.Constipation
17.Dyspnoea
18.Rashes
19.Ototoxicity
Contra-indications of Amiloride
1.Hypersensitivity to the drug
2.Renal impairment
3.Hyper kalemia
4.Along with other potassium sparing diuretics
5.Anuria
6.Diabetic nephropathy.
Special Precautions while taking Amiloride
1.Hepatic impairment
2.Diabetes mellitus
3.Along with other diuretics
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution.
Breast Feeding Related Information
Contraindicated.
Children Related Information
Contraindicated
Indications for Amiloride
1.Adjunctive in treatment of Hypertension
2.Edema associated with heart failure with potassium conservation
3.Edema where potassium conservation is needed.
4.Liddle`s syndrome
Interactions for Amiloride
Lithium: Increaes serum lithium levels and toxicity.
Ace inhibitors: Increased risk of potassium retention.
Digoxin: Increased renal clearance of digoxin.
Typical Dosage for Amiloride
5mg 1 to 2 times daily. Increased to 10mg 1 to 2 times if required.
Schedule of Amiloride
H
Storage Requirements for Amiloride
Store in a well closed container at a temperature range of 15 to 30 degree C. Protects from light, moisture and freezing.
Effects of Missed Dosage of Amiloride
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Amiloride
Treatment is supportive and symptomatic. Drug is removed by induced emesis or gastric lavage. Monitor & support serum electrolyte level and blood acidosis. To reduce potassium levels administer I.V. sodium bicarbonate or glucose with insulin. Potassium levels can be also lowered by cation exchange resins like sodium polystyrene sulfonate given orally or as retention enema.

 

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