Products
Enalapril is commercially available in tablet form (Reniten, generics). It has been approved in many countries since 1984. The active ingredient is also combined fixed with hydrochlorothiazide.
Structure and properties
Enalapril (C20H28N2O5, 376.45 g/mol) is present in drugs as enalapril maleate, a white powder that is sparingly soluble in water. Enalapril is the prodrug of the active metabolite enalaprilat, which is rapidly formed by ester hydrolysis after absorption of the more lipophilic precursor. Enalapril is a peptidomimetic and has approximately the structure of the tripeptide Phe-Ala-Pro.
Effects
Enalapril (ATC C09AA02) has antihypertensive properties and unloads the heart (preload and afterload). The effects are due to inhibition of the formation of angiotensin II from angiotensin I by inhibition of angiotensin converting enzyme (ACE). Enalapril thus abolishes the effects of antiogensin II.
Indications
For the treatment of high blood pressure and heart failure (myocardial insufficiency) and for the prevention of heart failure in patients with weakened hearts (asymptomatic left ventricular dysfunction).
Dosage
According to the SmPC. Tablets are usually taken once daily, independent of meals.
Contraindications
- Hypersensitivity
- Patients with hereditary or idiopathic angioedema.
- Angioedema on ACE inhibitors or sartans in patient history.
- Pregnancy
- Concurrent use of aliskiren in patients with diabetes mellitus or impaired renal function.
For complete precautions, see the drug label.
Interactions
Drug-drug interactions are possible with other antihypertensives, antidiabetics, lithium, NSAIDs, sympathomimetics, alcohol, and gold therapeutics. Concomitant administration of potassium or potassium-sparing diuretics may result in hyperkalemia.
Adverse effects
The most common possible adverse effects include weakness, nausea, irritable cough, dizziness, and visual disturbances. Other common adverse reactions include diarrhea, abdominal pain, difficulty breathing, pneumonia, hyperkalemia, low blood pressure, headache, depression, syncope, taste impairment, fatigue, hypersensitivity reactions, and angioneurotic edema. If angioedema occurs, the drug should be discontinued immediately and a physician contacted.
Cf.
ACE inhibitors
