Cilazapril
- Atc Codes:C09AA08
- CAS Codes:92077-78-6#88768-40-5
- PHARMGKB ID:92077-78-6#88768-40-5
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Cilazapril, Inhibace; Belgium: Inhibace; Bulgaria: Inhibace; Czech Republic: Cazaprol, Cilazapril, Inhibace; France: Cilazapril, Justor; Germany: Cilazapril, Dynorm; Greece: Vascase; Hungary: Inhibace; Ireland: Vascace; Italy: Inhibace, Initiss; Luxembourg: Inhibace; Netherlands: Cilazapril, Inhibace; Poland: Cazaprol, Cilan, Inhibace, Inhibestril; Portugal: Cilazapril, Inhibace, Vascase; Slovakia: Cilaprazil; Slovenia: Cilazil; Spain: Cilazapril, Inhibace, Inocar; Sweden: Inhibace; UK: Vascace.
North America
Canada: Cilazapril, Inhibace.
Latin America
Brazil: Vascase.
Asia
Japan: Cilazabace, Inhibace, Inhirock.
Drug combinations
Cilazapril and Hydroclorotiazide
Chemistry
Cilazapril: C~22~H~31~N~3~O~5~ H~2~O. Mw: 435.51. (1) 6H-Pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid, 9-[[1-(ethoxycarbonyl)-3-phenylpropyl]amino]octahydro-10-oxo-, monohydrate, [1S-[1α,9α(R*)]]-; (2)(1S,9S)-9-[[(S)-1-Carboxy-3-phenylpropyl]amino]octahydro-10-oxo-6H-pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid 9-ethyl ester monohydrate. CAS-92077-78-6; CAS-88768-40-5 (anhydrous)(1986).
Pharmacologic Category
Renin-Angiotensin-Aldosterone System Inhibitors; Angiotensin-Converting Enzyme Inhibitors. (ATC-Code: C09AA08).
Mechanism of action
Competitive inhibitor of angiotensin-converting enzyme. Prevents conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, resulting in lower levels of angiotensin II, and thus causing an increase in plasma renin activity and a reduction in aldosterone secretion.
Therapeutic use
Hypertension. Heart failure.
Pregnancy and lactiation implications
Contraindicated in pregnancy and in nursing women.
Unlabeled use
Contraindications
Hypersensitivity to cilazapril, any other ACE inhibitor, or any component of the formulation. Angioedema related to previous treatment with an ACE inhibitor. Ascites. Pregnancy. Breast-feeding.
Warnings and precautions
Angioedema may occur, involving the head and neck (potentially compromising the airway) or the intestine (presenting with abdominal pain)(African-Americans, patients with idiopathic or hereditary angioedema, and those with history of airway surgery may be at higher risk; use in previous angioedema associated with ACE inhibitor therapy is contraindicated). Cholestatic jaundice, which may progress to fulminant hepatic necrosis, may occur. May cause a dry, hacking, nonproductive cough usually within the first few months of treatment. Hyperkalemia may occur (risk factors include renal dysfunction, diabetes mellitus, concomitant use of potassium-sparing diuretics, potassium supplements, and/or potassium-containing salts). Anaphylactic/anaphylactoid reactions can occur with ACE inhibitors. Symptomatic hypotension with or without syncope can occur. Another ACE inhibitor, captopril, has been associated with rare cases of agranulocytosis, neutropenia, or leukopenia with myeloid hypoplasia. Patients with renal impairment are at high risk of developing neutropenia. Patients with both renal impairment and collagen vascular disease (e.g. systemic lupus erythematosus) are at an even higher risk of developing neutropenia. May be associated with deterioration of renal function and/or increases in serum creatinine, particularly in low renal blood flow (e.g. renal artery stenosis, heart failure). Use with caution in severe aortic stenosis (may reduce coronary perfusion resulting in ischemia). Potential consequences posed by falling blood pressure in ischemic heart disease or cerebrovascular disease. Use with caution in hypertrophic cardiomyopathy and outflow tract obstruction since reduction in afterload may worsen symptoms associated with this condition. Use with caution in unstented unilateral/bilateral renal artery stenosis. Use with caution in pre-existing renal insufficiency. Contains lactose (avoid use in galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption). ACE inhibitors can cause injury and death to the developing fetus when used in the second and third trimesters (use is contraindicated in pregnancy). Use with caution before, during, or immediately after major surgery. Cardiopulmonary bypass, intraoperative blood loss or vasodilating anesthesia increases endogenous renin release. Use of ACE inhibitors perioperatively will blunt angiotensin II formation and may result in hypotension.