21, Moronu Maduagwu Crescent, Off Ibezim Obiajulu Street, Off Adelabu Road, Surulere, Lagos, Nigeria
Tel: 234-1-7935274, 1-4710802, 806-6458005
Kwality Pharmaceuticals (P) Ltd. Nag Kalan, Majitha Road, Amritsar-India
Dosage Form, Composition & NAFDAC Registration Number (NRN)
Tablet (NRN: A4-8586): Amiloride hydrochloride USP 5 mg. (anhydrous equivalent), Hydrochlorothiazide USP 50 mg.
Pack size: Each strip of 10 tablets and 10 strips packed in a printed carton.
Amiloride hydrochloride and Hydrochlorothiazide tablets provide diuretic and antihypertensive activity (principally due to the hydrochlorothiazide component), while acting through the Amiloride component to prevent the excessive potassium loss that may occur in patients receiving a thiazide diuretic. Due to its amiloride component, the urinary excretion of magnesium is less with Amiloride and Hydrochlorothiazide than with a thiazide or loop diuretic used alone.The onset of the diuretic action of this product is within 1 to 2 hours and this action appears to be sustained for approximately 24 hours.
This is a potassium-conserving (antikaliuretic) drug that possesses weak (compared with thiazide diuretics) natriuretic, diuretic, and antihypertensive activity. These effects have been partially additive to the effects of thiazide diuretics in some clinical studies. Amiloride HCl has potassium-conserving activity in patients receiving kaliuretic-diuretic agents. Amiloride HCl is not an aldosterone antagonist and its effects are seen even in the absence of aldosterone. It 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. This mechanism accounts in large part for the potassium-sparing action of Amiloride.
It usually begins to act within two hours after an oral dose. Its effect on electrolyte excretion reaches a peak between 6 to 10 hours and lasts about 24 hours. Peak plasma levels are obtained in 3 to 4 hours and the plasma half-life varies from 6 to 9 hours. Effects on electrolytes increase with single doses of Amiloride hydrochloride up to approximately 15 mg.
Amiloride HCl is not metabolized by the liver but is excreted unchanged by the kidneys. About 50 percent of a 20 mg dose of Amiloride hydrochloride is excreted in the urine and 40 percent in the stool within 72 hours. Amiloride HCl has little effect on glomerular filtration rate or renal blood flow. Because Amiloride HCl is not metabolized by the liver, drug accumulation is not anticipated in patients with hepatic dysfunction, but accumulation can occur if the hepatorenal syndrome develops.
Hydrochlorothiazide is a diuretic and antihypertensive. It affects the distal renal tubular mechanism of electrolyte reabsorption. Hydrochlorothiazide increases excretion of sodium and chloride in approximately equivalent amounts. Natriuresis may be accompanied by some loss of potassium and bicarbonate.
After oral administration, diuresis begins within two hours, peaks in about four hours and lasts about 6 to 12 hours. It is not metabolized but is eliminated rapidly by the kidney. When plasma levels have been followed for at least 24 hours, the plasma half-life has been observed to vary between 5.6 and 14.8 hours. At least 61 percent of the oral dose is eliminated unchanged within 24 hours. Hydrochlorothiazide crosses the placental but not the blood-brain barrier and is excreted in breast milk.
Amiloride hydrochloride and Hydrochlorothiazide tablets are indicated in those patients with hypertension or with congestive heart failure who develop hypokalemia when thiazides or other kaliuretic diuretics are used alone, or in whom maintenance of normal serum potassium levels is considered to be clinically important, e.g., digitalized patients, or patients with significant cardiac arrhythmias.
This combination may be used alone or as an adjunct to other antihypertensive drugs, such as Methyldopa or beta-blockers. Since Amiloride hydrochloride and Hydrochlorothiazide enhance the action of these agents, dosage adjustments may be necessary to avoid an excessive fall in blood pressure and other unwanted side effects.
The fixed combination drug is not indicated for the initial therapy of edema or hypertension except in individuals in whom the development of hypokalemia cannot be risked.
- Potassium supplements,
- Renal impairmaent,
Special precautions should be taken with patients with hepatic impairment, diabetes, gout, bronchial asthma, metabolic or respiratory acidosis.
Pregnant women should be advised to contact physician before taking these medications, since routine use of diuretics during normal pregnancy is inappropriate and exposes mother and fetus to unnecessary hazards.
It is not known if Amiloride is distributed into breast milk. Hydrochlorothiazide is distributed into breast milk. The American Academy of Pediatrics recommends that nursing mothers avoid thiazide diuretics during the 1st month of lactation, due to reports of lactation suppression.
In some patients, the administration of a non-steroidal anti-inflammatory agent can reduce the diuretic, natriuretic, and antihypertensive effects of loop, potassium-sparing and thiazide diuretics.
Amiloride Hydrochlorothiazide: When Amiloride hydrochlorothiazide is administered concomitantly with an angiotensin-converting enzyme (ACE) inhibitor, Cyclosporine or Tacrolimus, the risk of hyperkalemia may be increased.
Hydrochlorothiazide: When given concurrently, the following drugs may interact with thiazide diuretics:
Alcohol, Barbiturates, or Narcotics: Potentiation of orthostatic hypotension may occur.
Antidiabetic Drugs (oral and insulin): Dosage adjustment of the antidiabetic drug may be required.
Cholestyramine and Colestipol Resins: Additive or potentiative effect maybe seen
Corticosteroids, ACTH: Intensified electrolyte depletion, particularly hypokalemia.
Electrolyte imbalance, anorexia, nausea, vomiting, gastic irritation, constipation and diarrhea, skin rash, urticaria, hyperglycemia, hyperuricaemia, leucopenia, thrombocytopenia, paraesthesis.
Dosage & Administration
Amiloride hydrochloride and Hydrochlorothiazide tablets should be administered with food. The usual starting dosage is 1 tablet a day. The dosage may be increased to 2 tablets a day, if necessary.
More than 2 tablets of Amiloride hydrochloride and Hydrochlorothiazide daily usually are not needed and there is no controlled experience with such doses.
Overdosage: Immediate evacuation of the stomach; symptomatic treatment; monitoring of serum electrolyte concentrations and renal function; immediate institution of appropriate treatment of hyperkalemia.
Store between temperature 8 - 25ºC. Protect from light.
Keep medicines out of the reach of children