Cilazapril


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Hypertension
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.
Nhóm bệnh nhân đặc biệt
Patients with strongly activated renin-angiotensin-aldosterone system; cirrhosis without ascites; receiving diuretics: Initially, 0.5 mg once daily.
Suy thận
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.

Cách dùng
May be taken with or without food.
Chống chỉ định
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.
Thận trọng
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.
Tác dụng không mong muốn
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.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness and fatigue; if affected, do not drive or operate machinery.
Chỉ số theo dõi
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.
Quá liều
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.
Tương tác
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.
Tương tác với thức ăn
Decreased absorption with food.
Ảnh hưởng đến kết quả xét nghiệm
May cause false-negative aldosterone/renin ratio.
Tác dụng
Description: 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).
Đặc tính

Chemical Structure Image
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.

Bảo quản
Store at 25°C.
Phân loại MIMS
Thuốc ức chế men chuyển angiotensin/Thuốc ức chế trực tiếp renin
Phân loại ATC
C09AA08 - cilazapril ; Belongs to the class of ACE inhibitors. Used in the treatment of cardiovascular disease.
Tài liệu tham khảo
Anon. Cilazapril. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/04/2022.

Buckingham R (ed). Cilazapril. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/04/2022.

Cilazapril 2.5 mg Film-coated Tablets (Activase Pharmaceuticals Limited). MHRA. https://products.mhra.gov.uk. Accessed 01/04/2022.

Mylan New Zealand Ltd. Zapril, 0.5 mg, 2.5 mg, 5 mg, Film Coated Tablets data sheet 18 June 2019. Medsafe. http://www.medsafe.govt.nz. Accessed 01/04/2022.

Preston CL (ed). Ciclosporin - Cilazapril Drug Interaction. Stockley’s Drug Interactions [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/04/2022.

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