Adult: Initially, 1 mg once daily; adjust dose according to response. Usual dose: 2.5-5 mg once daily. Elderly: Initially, 0.5 mg once daily; titrate according to response, tolerability, and clinical status.
Oral Chronic heart failure
Adult: Initially, 0.5 mg once daily to be maintained for a week. If tolerated, may increase at weekly intervals to 1-2.5 mg once daily. Max: 5 mg once daily. Elderly: Initially, 0.5 mg once daily; titrate according to response, tolerability, and clinical status.
Special Patient Group
Patients with strongly activated renin-angiotensin-aldosterone system; cirrhosis without ascites; receiving diuretics: Initially, 0.5 mg once daily.
Renal Impairment
CrCl (mL/min)
Dosage
<10
Not recommended.
10-40
Initially, 0.5 mg once daily; Max: 2.5 mg once daily.
>40
Initially, 1 mg once daily; Max: 5 mg once daily.
Administration
May be taken with or without food.
Contraindications
Hypersensitivity to cilazapril or any other ACE inhibitor; hereditary or idiopathic angioedema; angioedema related to previous treatment with an ACE inhibitor; ascites, anuria, hereditary problems of galactose intolerance, glucose-galactose malabsorption, or congenital lactase deficiency. Concomitant use with aliskiren-containing products in patients with diabetes mellitus or moderate to severe renal impairment (GFR <60 mL/min); sacubitril/valsartan within 36 hours of use. Pregnancy and lactation.
Special Precautions
Patient with diabetes mellitus, collagen vascular disease (e.g. SLE), severe aortic stenosis, mitral valve stenosis, ischaemic heart disease, acute cardiac decompensation, severe degrees of heart failure, cerebrovascular disease, angina pectoris, hypertrophic cardiomyopathy, outflow tract obstruction, cirrhosis without ascites, unstented unilateral or bilateral renal artery stenosis; volume-depletion, metabolic acidosis. Black patients. Patients undergoing major surgery. Concomitant use with medications that may increase K (e.g. K-sparing diuretics, K supplements, K-containing salts, heparin); immunosuppressants, allopurinol, procainamide. Renal and hepatic impairment. Elderly.
Adverse Reactions
Significant: Cough, hyperkalaemia, hypotension, syncope, deterioration of renal function and/or increases in serum creatinine. Rarely, angioedema of the face, lips, glottis, and/or intestine; neutropenia, agranulocytosis, thrombocytopenia, anaemia; proteinuria in patients with pre-existing renal impairment. Gastrointestinal disorders: Dysgeusia, nausea, aphthous stomatitis, dry mouth, vomiting, diarrhoea. General disorders and administration site conditions: Fatigue, asthenia. Metabolism and nutrition disorders: Decreased appetite. Musculoskeletal and connective tissue disorders: Muscle cramps, arthralgia, myalgia. Nervous system disorders: Headache, dizziness. Rarely, cerebral ischaemia, transient ischaemic attack, ischaemic stroke. Psychiatric disorders: Sleep disorders. Reproductive system and breast disorders: Impotence. Respiratory, thoracic and mediastinal disorders: Bronchospasm, rhinitis, dyspnoea. Skin and subcutaneous tissue disorders: Rash, maculopapular rash, hyperhidrosis. Vascular disorders: Flushing. Potentially Fatal: Rarely, severe anaphylactoid reactions during haemodialysis (eg, CVVHD) with high-flux dialysis membranes (e.g. AN 69), LDL apheresis with dextran sulfate cellulose; and desensitisation treatment with Hymenoptera (bee or wasp) venom. Very rarely, angioedema associated with laryngeal or tongue oedema; cholestatic jaundice which may progress to fulminant hepatic necrosis.
Patient Counseling Information
This drug may cause dizziness and fatigue; if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor blood pressure; serum creatinine, BUN, electrolytes, LFTs (at baseline and periodically thereafter in patients with pre-existing hepatic impairment), serum glucose (diabetic patients), CBC (patients with renal impairment and/or collagen vascular disease). Assess pregnancy status. Monitor for signs of angioedema.
Overdosage
Symptoms: Cough, dizziness, electrolyte disturbances, palpitations, tachycardia, bradycardia, anxiety, hyperventilation, hypotension, renal failure, and circulatory shock. Management: IV infusion of 0.9% NaCl. If hypotension occurs, place the patient in the shock position or consider treatment with angiotensin II infusion or IV catecholamines, if available. May place pacemaker for therapy-resistant bradycardia. May perform haemodialysis, if indicated. Monitor vital signs, serum electrolytes and creatinine concentrations continuously.
Drug Interactions
Increased risk of angioedema with sacubitril/valsartan, racecadotril, mammalian target of rapamycin (mTOR) inhibitors (e.g. sirolimus, everolimus, temsirolimus). May increase the serum concentration of lithium. Enhanced therapeutic effect with other antihypertensives. Enhanced hyperkalaemic effect with K-sparring diuretics (e.g. spironolactone, triamterene, amiloride), K supplements, K containing salt substitutes, heparin, trimethoprim, trimethoprim/sulfamethoxazole, ciclosporin. Enhanced hypotensive effect with thiazide or loop diuretics, TCAs, antipsychotics, anaesthetics, and narcotics. Enhanced hyperkalaemic, hypotensive and nephrotoxic effects with angiotensin receptor blockers. Reduced antihypertensive effect with sympathomimetics. Diminished antihypertensive effect, enhanced hyperkalaemic and nephrotoxic effects with NSAIDs. May potentiate the hypoglycaemic effect of insulins and oral hypoglycaemic agents. May cause nitritoid reactions with Na aurothiomalate (gold) inj. Potentially Fatal: Increased risk of hyperkalaemia, hypotension and changes in renal function with aliskiren in patients with diabetes mellitus and renal impairment.
Food Interaction
Decreased absorption with food.
Lab Interference
May cause false-negative aldosterone/renin ratio.
Action
Description: Mechanism of Action: Cilazapril, a prodrug of cilazaprilat, is a long-acting angiotensin-converting enzyme (ACE) inhibitor that prevents the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, thereby increasing plasma renin activity and reducing aldosterone secretion. Onset: Approx 1-2 hours. Duration: Up to 24 hours. Pharmacokinetics: Absorption: Rapidly absorbed. Food delays and reduces absorption to a minor extent. Bioavailability: Approx 60% (cilazaprilat). Time to peak plasma concentration: Within 2 hours (cilazaprilat). Metabolism: Rapidly hydrolysed in the liver to its active metabolite (cilazaprilat). Excretion: Cilazaprilat: Via urine (53%, as unchanged). Terminal elimination half-life: Cilazaprilat: 36-49 hours (single dose); approx 54 hours (multidose).
Chemical Structure
Cilazapril Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 56330, Cilazapril. https://pubchem.ncbi.nlm.nih.gov/compound/Cilazapril. Accessed Apr. 26, 2022.
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