PCaution when used during lactation : Caution when used during pregnancy

LCaution when used during lactation : Caution when used during lactation

Molecule Info

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WARNING

Like other potassium-conserving agents, amiloride may cause hyperkalemia (serum potassium levels greater than 5.5 mEq per liter) which, if uncorrected, 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 the elderly. When amiloride HCl is used concomitantly with a thiazide diuretic in patients without these complications, the risk of hyperkalemia is reduced to about 1-2 percent. It is thus essential to monitor serum potassium levels carefully in any patient receiving amiloride, particularly when it is first introduced, at the time of diuretic dosage adjustments, and during any illness that could affect renal function.

Indication(s)

Potassium-conserving agent; diuretic. Although amiloride may be used alone, its principal indication is as concurrent therapy with thiazides or more potent diuretics to conserve potassium during periods of vigorous diuresis and during long-term maintenance therapy. It is indicated for use in:

1) Congestive heart failure.

2) Hypertension.

3) Hepatic cirrhosis with ascites.

Oedema
Adult: Initially, 5-10 mg orally daily. Start with 2.5 mg once daily if used with other diuretics or antihypertensives. Max: 20 mg daily. 
Renal impairment: Avoid use.

Dosage & Administration

MonotherapyInitially 10mg which may be given as a single or divided dose. This may be increased if necessary to a maximum of 20mg daily. When diuresis has been achieved, the dosage may be reduced by 5mg increments to the least amount required.

In conjunction with other diuretic therapy: When amiloride is used with a diuretic which is given on an intermittent basis, it should be given at the same time as the diuretic.

Congestive heart failure: Initially 5-10mg daily, together with the usual dosage of the diuretic concurrently employed. Where diuresis is not achieved dosage of both agents may be increased if necessary, however, the maximum dose for amiloride is 20mg a day. Once diuresis is achieved, reduction in dosage of both agents may be attempted for maintenance therapy. The dosage of both drugs is determined by diuresis and the level of plasma potassium.

Hypertension: 5-10mg daily, together with the usual antihypertensive dosage of the thiazide concurrently employed. It is not usually necessary to exceed 10mg of amiloride daily; in any event, not more than 20mg a day should be given.

Hepatic cirrhosis with ascites: When used in conjunction with another diuretic, treatment should be commenced with a small amiloride dose of 5mg, plus a low dosage of the other diuretic agent. If necessary, dosage of both agents may gradually be increased until there is effective diuresis. The maximum dose for amiloride is 20mg daily. Maintenance doses may be lower than those required to initiate diuresis; reduction in the daily dosage should therefore be attempted when the patient's weight is stabilised.

Elderly: Dosage in the elderly should be carefully adjusted according to renal function, blood electrolytes and diuretic response. The elderly are more susceptible to electrolyte imbalance and more likely to experience hyperkalaemia since renal reserve may be reduced.

Children: The use of amiloride in children is contraindicated.

Should be taken with food.

Overdosage

No data are available; it is not known whether the drug is dialysable. No specific antidote is available.

The most likely signs and symptoms are dehydration and electrolyte imbalance which should be treated by established methods. Therapy should be discontinued and the patient closely observed. Emesis should be induced or gastric lavage performed if ingestion is recent. Treatment is symptomatic and supportive. If hyperkalaemia occurs, active measures should be taken to reduce plasma potassium levels.

Contraindications Hyperkalaemia.
Special Precautions DM, elderly, pregnancy and lactation. Discontinue at least 3 days before glucose-tolerance tests are performed. Monitor serum electrolytes regularly.
Adverse Drug Reaction(s)

Amiloride is usually well tolerated, although minor side-effects are reported relatively frequently. Apart from hyperkalaemia, significant adverse reactions have been infrequently reported. Nausea/anorexia, abdominal pain, flatulence and mild skin rash are probably due to amiloride; but other side-effects are generally associated with diuresis or with the underlying disease being treated.

Body as a whole:Headache, weakness, fatigue, back pain, chest pain, neck/shoulder ache, pain in the extremities.

Cardiovascular:Angina pectoris, orthostatic hypotension, arrhythmias, palpitation, one patient with partial heart block developed complete heart block.

Digestive:Anorexia, nausea, vomiting, diarrhoea, constipation, abdominal pain, GI bleeding, jaundice, thirst, dyspepsia, flatulence.

Metabolic:Elevated plasma potassium levels above 5.5mmol/l, hyponatraemia.

Musculoskeletal:Muscle cramps, joint pain. Serum uric acid levels may rise during treatment with amiloride and acute attacks of gout may be precipitated.

Nervous:Dizziness, vertigo, paraesthesia, tremors, encephalopathy.

Psychiatric:nervousness, mental confusion, insomnia, decreased libido, depression, somnolence.

Respiratory:Cough, dyspnoea.

Special senses:Nasal congestion, visual disturbances, increased intra-ocular pressure, tinnitus.

Urogenital:Impotence, polyuria, dysuria, bladder spasms, frequency of micturition.

Reactions in which no causal relationship could be established were activation of probable pre-existing peptic ulcer, aplastic anaemia, neutropenia and abnormal liver function tests. In a few cirrhotic patients, jaundice associated with the underlying disease has deepened, but the drug relationship is unknown.

Drug Interactions

Lithium should not generally be given with diuretics because they reduce it renal clearance and add a high risk of lithium toxicity.

When combined with thiazide diuretics, amiloride can act synergistically with chlorpropamide to increase the risk of hyponatraemia.

When amiloride is administered concurrently with an angiotensin-converting enzyme inhibitor, NSAIDs or ciclosporin the risk of hyperkalaemia may be increased. Therefore, if concomitant use of these agents is indicated because of demonstrated hypokalaemia, they should be used with caution and with frequent monitoring of serum potassium.In patients receiving amiloride with NSAIDs or ciclosporin the risk of nephrotoxcity may also be increased.

Lithium should not generally be given with diuretics because they reduce it renal clearance and add a high risk of lithium toxicity.

When combined with thiazide diuretics, amiloride can act synergistically with chlorpropamide to increase the risk of hyponatraemia.

When amiloride is administered concurrently with an angiotensin-converting enzyme inhibitor, NSAIDs or ciclosporin the risk of hyperkalaemia may be increased. Therefore, if concomitant use of these agents is indicated because of demonstrated hypokalaemia, they should be used with caution and with frequent monitoring of serum potassium.In patients receiving amiloride with NSAIDs or ciclosporin the risk of nephrotoxcity may also be increased.

Lab Interference Rise in blood-urea-nitrogen concentrations.
Pregnancy Category (FDA) and use in Specific Population

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1sttrimester (and there is no evidence of a risk in later trimesters).
Category D
: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Amiloride is not recommended for use during pregnancy due to limited clinical experience. The potential benefits must be weighed against the possible hazard to the foetus if administered to a woman of childbearing age.

The routine use of diuretics in otherwise healthy pregnant women with or without mild oedema is not indicated because they may be associated with hypovolaemia, increased blood viscosity and decreased placental perfusion. Foetal and neonatal jaundice, foetal bone depression and thrombocytopenia have also been described.

It is not known whether amiloride is excreted in human milk. Therefore, due to the risk that it may take this route of excretion, and possibly cause serious adverse reactions to the nursing infant, the mother should either stop breast-feeding or cease taking the drug.

Storage Oral: Store at 15-30°C.
Pharmacology Amiloride is a weak diuretic which acts mainly on the distal renal tubules. It increases the excretion of sodium and reduces the excretion of potassium. It diminishes kaliuretic effects of other diuretics, and may produce an additional natriuretic effect.
Onset: 2 hr.
Duration: 24 hr.
Absorption: Bioavailability: about 50%.
Excretion: Plasma half-life: 6-9 hr and terminal half-life: about 20 hr or more. Excreted unchanged by the kidneys.
ATC Classification C03DB01 - amiloride; belongs to the class of other potassium-sparing agents. Used as diuretics.

 

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