Products
Cilazapril is commercially available in the form of film-coated tablets (Inhibace). Fixed combinations with hydrochlorothiazide are available (Inhibace plus). Cilazapril has been approved in many countries since 1990.
Structure and properties
Cilazapril (C22H31N3O5, Mr = 417.5 g/mol) exists as a white crystalline powder that is sparingly soluble in water. It is a prodrug that is rapidly hydrolyzed to the active form cilazaprilat after absorption. The prodrug was developed because it has higher bioavailability.
Effects
Cilazapril (ATC C09AA08) has antihypertensive properties and unloads the heart (preload and afterload). The effects are due to inhibition of angiotensin II formation from angiotensin I by inhibition of angiotensin converting enzyme (ACE). Cilazapril thus abolishes the effects of antiogensin II.
Indications
For the treatment of high blood pressure and chronic heart failure.
Dosage
According to the SmPC. The tablets are taken once daily, regardless of meals. They should always be administered at the same time of day.
Contraindications
- Hypersensitivity
- Previous angioedema while taking ACE inhibitors.
- Pregnancy and lactation
- Concurrent use of aliskiren in patients with diabetes mellitus or impaired renal function.
For complete precautions, see the drug label.
Interactions
Drug-drug interactions include those with antihypertensives, digoxin, lithium, diuretics, antidepressants, sympathomimetics, and certain hemodialysis membranes. Potassium, potassium-sparing diuretics, and other drugs that affect potassium levels may increase the risk for hyperkalemia.
Adverse effects
The most common possible adverse effects include nausea, dyspepsia, rash, a dry irritable cough, dyspnea, hypotension, palpitations, angina, headache, and fatigue. Rarely, hypersensitivity reactions and angioneurotic edema are possible.
