Composition
RepresTM SR Tablet: Each sustained release tablet contains
Indapamide BP 1.5 mg.
Pharmacology
Indapamide is an oral antihypertensive agent. The mechanism
whereby Indapamide exerts its antihypertensive action has not been
completely elucidated; both vascular and renal actions have been
implicated. The possible beneficial pharmacological effects of
Indapamide in the treatment of hypertension include a reduction in
cardiac hypertrophy and a reduction in the thickening of arterial walls,
a prevention of the accumulation of the embryonic isoform of
fibronectin in coronary vessels, free radical scavenging leading to
stimulation of vasodilator eicosanoid formation, and interaction with
renal carbonic anhydrase. The renal site of action of Indapamide is the
proximal segment of the distal tubule. Indapamide appears to have
natriuretic properties (sodium and chloride being excreted in equivalent
amounts) with less effect on kaliuresis or uric acid excretion. Only at
doses greater than 1.5 mg Indapamide sustained release tablet/day is
an appreciable increase in urinary volume observed in man. No
significant changes in plasma sodium levels have been observed in
clinical studies. Significant hypokalemia (plasma potassium <3.2
mmol/L) has been reported in 4% of patients.
Pharmacokinetics
Absorption: The fraction of Indapamide released is rapidly and totally
absorbed via the gastrointestinal digestive tract. Ingestion with food
slightly increases the rate and extent of absorption. These changes are
unlikely to be clinically significant. Peak serum level following a single
dose occurs about 12 hours after ingestion; repeated administration
reduces the variation in serum levels between 2 doses. Distribution:
Indapamide is widely distributed throughout the body, with extensive
binding to some specific sites. In blood, it is highly bound to red blood
cells (80%) and more specifically to carbonic anhydrase (98%) without
having any significant inhibiting activity on this enzyme. Binding of
Indapamide to plasma proteins is 79%. The plasma elimination
half-life is 14 to 24 hours (mean 18 hours). The drug has a volume of
distribution of approximately 60L. Steady state is achieved after 7 days.
Repeated administration does not lead to accumulation. Metabolism:
The drug is extensively metabolized in the liver, with only 5 to 7% of
the dose excreted in the urine as unchanged drug. Elimination:
Elimination is essentially urinary (70% of the dose) and faecal (22%) in
the form of inactive metabolites.
Indications and Uses
RepresTM SR is indicated in the treatment of essential hypertension. It
is effective in treating hypertension in patients with renal function
impairment, although its diuretic effect is reduced. RepresTM SR is also
indicated for the treatment of salt and fluid retention associated with
congestive heart failure.
Dosage & Administration
One tablet daily, preferably in the morning. In more severe cases,
RepresTM SR can be combined with other categories of antihypertensive agents.
Contraindications
This drug must not be taken in the following conditions: known
allergy to this drug or to sulphonamides, renal failure, serious
liver disease, hypokalemia.
Side Effects
Side effects include dizziness, headache, anorexia, nausea,
vomiting, constipation, diarrhea and postural hypotension.
Electrolyte imbalances include hypochloremic alkalosis, hyponatremia,
hypokalemia and hyperuricemia; hypersensitivity reactions which
include skin rashes, cholestatic jaundice and blood dyscrasias
including thrombocytopenia, leucopenia, aplastic anemia.
Precautions
The drug should be used cautiously in the following situations- disturbed
water/electrolyte balance, diabetes, gout and kidney problems. Monitoring
of potassium and uric acid serum levels is also recommended.
Drug Interactions
Other Antihypertensive: Indapamide may add to or potentiate the
action of other antihypertensive drugs. In limited controlled trials
that compared the effect of Indapamide combined with other
antihypertensive drugs with the effect of the other drugs administered
alone, there was no notable change in the nature or frequency of
adverse reactions associated with the combined therapy.
Norepinephrine: Indapamide, like the thiazides, may decrease
arterial responsiveness to norepinephrine, but this diminution is
not sufficient to preclude effectiveness of the pressor agent for
therapeutic use.
Use in Pregnancy and Lactation
There is no adequate and well-controlled studies in pregnant
women and so Indapamide is not recommended. Mothers taking
Indapamide should not breastfeed.
Use in Pediatric Patients
The safety and effectiveness in pediatric patients have not been
established.
Storage Condition
Keep below 300
C, away from light and moisture.
How Supplied
RepresTM SR Tablet: Each box contains 30 tablets in blister pack.
RepresTM
SR
Indapamide BP
Brand: Square Pharmaceuticals Ltd
