ACETEC

What it is

ACETEC tablets contain 2.5 mg, 5 mg, 10 mg or 20 mg enalapril maleate as the active ingredient. Enalapril maleate is a prodrug, which, when administered orally is hydrolysed to release the active converting enzyme inhibitor, enalaprilat, with the liver appearing to be the main site for this conversion.

Approved indications

— All grades of essential hypertension and renovascular hypertension. — Treatment of all degrees of symptomatic heart failure. — All degrees of left ventricular dysfunction where the left ventricular ejection fraction is less than 35%, irrespective of the presence or severity of obvious symptoms of heart failure.

Dosing overview

Dosing varies by indication and patient factors. For essential hypertension in patients not on diuretics, the recommended initial dose is 5 mg once a day, with dosage adjusted according to blood pressure response, and the usual dosage range being 10 to 40 mg/day administered in a single dose or two divided doses. For elderly patients over 65 years, the starting dose should be 2.5 mg. For congestive heart failure, the initial dose should be lower (2.5 mg or less), and in the absence of or after effective management of symptomatic hypotension, the dose should be gradually increased to the usual maintenance dose (10–20 mg) given in a single or divided dose. For patients with creatinine clearance ≤30 mL/min, the first dose is 2.5 mg once daily and may be titrated upward until blood pressure is controlled or to a maximum of 40 mg daily.

Key safety warnings

Angioedema of the face, extremities, lips, tongue, glottis and/or larynx has been reported in patients treated with ACETEC and may occur at any time during treatment, requiring prompt discontinuation and careful observation until the swelling disappears. Very rarely, fatalities have been reported due to angioedema associated with laryngeal oedema or tongue oedema, and where there is involvement of the tongue, glottis or larynx likely to cause airway obstruction, appropriate therapy including subcutaneous adrenaline solution and measures to ensure a patent airway should be promptly administered. Excessive hypotension is a possible consequence of ACETEC use in severely salt/volume depleted persons, and in patients with heart failure excessive hypotension has been observed and may be associated with oliguria and progressive azotaemia, therefore therapy should be started under very close medical supervision with such patients followed closely for the first two weeks of treatment and whenever the dose is increased. Diabetic patients treated with oral antidiabetic agents or insulin should be told to closely monitor for hypoglycaemia, especially during the first month of combined use. A persistent non-productive, ticklish cough has been reported in some patients undergoing treatment with ACETEC, is often worse when lying down, is commoner in women, and if the cough persists, the drug should be discontinued.

Contraindications

ACETEC is contraindicated in patients with a history of hypersensitivity to enalapril maleate or to any component of the formulation and in patients with a history of angioneurotic oedema relating to previous treatment with an ACE inhibitor and in patients with hereditary or idiopathic angioedema. ACETEC should not be used during pregnancy. ACETEC should not be administered with aliskiren in patients with diabetes. ACETEC is contraindicated in combination with a neprilysin inhibitor (e.g., sacubitril).

Regulatory history

ACETEC was first listed on the ARTG on 18 August 2000, with ARTG entries 75457 (2.5 mg), 75497 (5 mg), 75498 (10 mg) and 75499 (20 mg).