ACETEC

COMPOSITION :

Each tablet contains : Enalapril maleate 5 mg and 20 mg

DOSAGE FORM AVAILABLE

ORAL : TABLETS 5 mg

TABLETS 20 mg

PRODUCT DESCRIPTION :

ACETEC TABLET 5 mg :

Heart shape, biconvex, white tablets, impressed "BIOLAB" on one face and bisected on the obverse.

ACETEC TABLET 20 mg :

Heart shape, biconvex, light orange tablets, impressed "BIOLAB" on one face and bisected on the obverse.

ACTIONS :

ACETEC is an angiotensin converting enzyme (ACE) inhibitor. The effect of a dose will gradually take place within one hour and will usually stay for 24 hours, daily dosage may be given in one or two single administrations. Enalapril is a prodrug and will be transformed to enalaprilat which is active by liver.

ACETEC can reduce blood pressure in normal and hypertensive person by reducing peripheral vascular resistant but has no effect to heart rate. For the patient without congestive heart failure, ACETEC has no effect or little effect to cardiac output and does not interfere renal blood flow or glomerular filtration rate.

Enalapril maleate is rapidly absorbed from gastro-intestinal tract, approximately 60% of a dose is absorbed and peak serum concentrations occur within about one hour. Enalapril absorption is not influenced by the presence of food. Enalapril is metabolited in the liver by hydrolysis to enalaprilat, the active metabolite. Excretion of enalaprilat and enalapril is primarily renal. Approximately 94% of the dose is recovered in the urine and feces as enalaprilat or enalapril. The principle components in urine are enalaprilat, accounting for about 40% of the dose, and intact Enalapril. The elimination half-life is approximately 11 hours, and is increased in patients with renal failure.

INDICATIONS :

-- High blood pressure, whether alone or in combination with other anti-hypertensive drugs especially diuretics.

-- Congestive heart failure : Should be used as an adjunctive therapy with digitalis and/or diuretics.

DOSAGE AND ADMINISTRATIONS :

Essential Hypertension : The initial dose is 10-20 mg, depending on the degree of hypertension, and is given once daily. In mild hypertension, the recommended initial dose is 10 mg daily. For other degrees of hypertension the initial dose is 20 mg daily. The usual maintenance dose is one 20 mg tab taken once daily. The dosage should be adjusted according to the needs of the patient to a maximum of 40 mg daily.

Renovascular Hypertension : Since blood pressure and renal function in such patients may be particularly sensitive to ACE inhibition, therapy should be initiated with a lower starting dose (e.g. 5 mg or less). The dosage should then be adjusted according to the needs of the patient. Most patients may be expected to respond to one 20 mg tab taken once daily. For patients with hypertension who have been treated recently with diuretics, caution is recommended.

Concomitant Diuretic Therapy in Hypertension : Symptomatic hypotension may occur following the initial dose of ACETEC ; this is more likely in patients who are being treated currently with diuretics. Caution is recommended, therefore, since these patients may be volume or salt-depleted. The diuretic therapy should be discontinued for 2-3 days prior to initiation of therapy with ACETEC. If this is not possible, the initial dose of ACETEC should be low (5 mg or less) to determine the initial effect on the blood pressure. Dosage should then be adjusted according to the needs of the patient.

Dosage in Renal Insufficiency : Generally, the intervals between the administration of enalapril should be prolonged and/or the dosage reduced. (See table).

Heart Failure and/or Symptomatic Left Ventricular Dysfunction : The initial dose of ACETEC in patients with symptomatic heart failure or symptomatic left ventricular dysfunction is 2.5 mg and it should be administered under close medical supervision to determine the initial effect on the blood pressure. In the absence of, or after effective management of, symptomatic hypotension following initiation of therapy with ACETEC in heart failure, the dose should be increased gradually to the usual maintenance dose of 20 mg, given in a single dose or 2 divided doses, as tolerated by the patient. This dose titration may be performed over a 2 to 4 weeks period, or more rapidly if indicated by the presence of residual signs and symptoms of heart failure. In patients with symptomatic heart failure, this dosage regimen was effective in reducing mortality. Blood pressure and renal function should be monitored closely both before and after starting treatment with ACETEC because hypotension and consequent renal failure have been reported. In patients treated with diuretics, the dose should be reduced if possible before beginning treatment with ACETEC. The appearance of hypotension after the initial dose of ACETEC does not imply that hypotension will recur during chronic therapy with ACETEC and does not preclude continued use of the drug. Serum potassium also should be monitored.

OVERDOSAGE-SYMPTOMS, TREATMENT, SUPPORTIVE THERAPY, ANTIDOTE (S) :

The common symptom is hypotension. The recommended treatment of overdosage is IV infusion of normal saline solution.

If ingestion is recent, induce emesis. ACETEC may be removed from the circulation by hemodialysis.

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