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Cardace

CLINICAL PHARMACOLOGY:
Enalapril is an ACE inhibitor. ACE inhibitors are antihypertensive drugs that act as vasodilators resulting in the reduction of peripheral resistance. They inhibit angiotensin-converting enzyme (ACE), which is involved in the conversion of angiotensin I to angiotensin II. Angiotensin II stimulates the synthesis and secretion of aldosterone and raises blood pressure via a potent direct vasoconstrictor effect.

Pharmacokinetics:
Enalapril acts as a prodrug of the diacid enalaprilat, its active form, which is poorly absorbed by mouth. Following oral administration about 60% of a dose of Enalapril is absorbed from the gastro-intestinal tract and peak plasma concentrations are achieved within about 1 hour. Enalapril is extensively hydrolysed in the liver to enalaprilat; peak plasma concentrations of enalaprilat are achieved 3 to 4 hours after an oral dose of Enalapril. Enalaprilat is 50 to 60% bound to plasma proteins. Its elimination is multiphasic but the effective half-life for accumulation following multiple doses of Enalapril is reported to be about 11 hours in patients with normal renal function.

USES:
Cardace???? is used in the treatment of hypertension and heart failure.

DOSAGE AND ADMINISTRATION:
In the treatment of hypertension: An initial dose of 5mg daily may be given by mouth. The usual maintenance dose is 10 to 20mg given once daily.
For patients with renal impairment: A dose of 2.5mg should be given or to those who are receiving a diuretic.
In the management of heart failure: In patients with heart failure or asymptomatic left ventricular dysfunction, Cardace???? is given as an initial dose of 2.5mg daily. The usual maintenance dose is 20mg daily as a single dose or in 2 divided doses. Treatment should be initiated with a low dose under close medical supervision.

CONTRA-INDICATIONS AND WARNINGS:

Precautions:
Cardace???? should not be used in patients with aortic stenosis or outflow tract obstruction. It should not generally be used in patients with renovascular disease or suspected renovascular disease, but is occasionally necessary for severe resistant hypertension. In such patients then it should only be given with great caution and under close specialist supervision. Patients with heart failure and patients who are likely to be salt or water depleted for example, those receiving concomitant treatment with diuretics or dialysis may experience symptomatic hypotenson during the initial stages of ACE inhibitor therapy. Treatment should therefore be started under close medical supervision using a low dose.

Adverse Effects:
Adverse effects generally include hypotension, dizziness, fatigue, headache, gastro-intestinal disturbances, taste disturbances, persistant dry cough and other upper respiratory tract symptoms, skin rashes, angioedema, hypersensitivity reactions, renal impairment, hyperkalaemia, hyponatraemia and blood disorders.

Overdosage:
The main adverse effects is hypotension which usually responds to supportive treatment and volume expansion. Pressor agents are rarely required. Infusion of angiotensin amide may be considered if hypotension persists.

Interactions:
Excessive hypotension may occur when ACE inhibitors are used concurrently with diuretics, other antihypertensives, or other agents including alcohol that lower blood pressure. Potassium-sparing diuretics and potassium supplements should be stopped before initiating ACE inhibitors in patients with heart failure. The adverse effects of ACE inhibitors on the kidneys may be potentiated by other drugs such as NSAIDs, that can affect renal function.

PHARMACEUTICAL PRECAUTIONS:
Store in a dry place below 25????C. Protect from light. Keep all medicines out of the reach of children.

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