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ATC Group: C09A ACE inhibitors, plain

Anatomical Therapeutic Chemical Classification System

Hierarchical Position

Level
Code
Title
1
C
Cardiovascular system
2
C09
Agents acting on the renin-angiotensin system
3
C09A
ACE inhibitors, plain

Contents

Code
Title
C09AA
ACE inhibitors, plain

Active Ingredients

Chemical substance
Description
Benazepril

Benazepril is a prodrug which, after hydrolysis to the active substance benazeprilat, inhibits the angiotensin-converting enzyme (ACE) and so blocks the conversion of angiotensin I to angiotensin II. This reduces all the effects mediated by angiotensin II – i.e. vasoconstriction and production of aldosterone, which promotes the reabsorption of sodium and water in the renal tubules – and elevates cardiac output.

Captopril

Captopril is a highly specific, competitive inhibitor of angiotensin-I converting enzyme (ACE inhibitors). Inhibition of ACE results in decreased plasma angiotensin-II, which leads to decreased vasopressor activity and to reduced aldosterone secretion. In patients with hypertension, captopril causes a reduction in supine and erect blood pressure, without inducing any compensatory increase in heart rate, nor water and sodium retention.

Cilazapril

Cilazapril is a specific, long-acting angiotensin-converting enzyme (ACE) inhibitor which suppresses the renin-angiotensin-aldosterone system and thereby the conversion of the inactive angiotensin I to angiotensin II, which is a potent vasoconstrictor.

Delapril
Enalapril

Enalapril is a derivative of two amino-acids, L-alanine and L-proline. After absorption, enalapril is hydrolysed to enalaprilat, which inhibits ACE. Inhibition of ACE results in decreased plasma angiotensin II, which leads to increased plasma renin activity (due to removal of negative feedback of renin release), and decreased aldosterone secretion.

Fosinopril

Fosinopril is the pro-drug (ester) of the long acting active ACE inhibitor fosinoprilat. After oral administration fosinopril is quickly and fully metabolised to the active fosinoprilat. Fosinopril contains a phosphinic group capable of a specific binding to the active site of the angiotensin converting enzyme, preventing the conversion of angiotensin I in angiotensin II.

Imidapril

The hypotensive effect of imidapril in hypertension appears to result primarily from the suppression of the plasma renin-angiotensin-aldosterone system.

Lisinopril

Lisinopril is a peptidyl dipeptidase inhibitor. It inhibits the angiotensin-converting enzyme (ACE) that catalyses the conversion of angiotensin I to the vasoconstrictor peptide, angiotensin II. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex. Inhibition of ACE results in decreased concentrations of angiotensin II which results in decreased vasopressor activity and reduced aldosterone secretion.

Perindopril

Perindopril is an inhibitor of the enzyme that converts angiotensin I into angiotensin II (Angiotensin Converting Enzyme ACE). The converting enzyme, or kinase, is an exopeptidase that allows conversion of angiotensin I into the vasoconstrictor angiotensin II as well as causing the degradation of the vasodilator bradykinin into an inactive heptapeptide. Inhibition of ACE results in a reduction of angiotensin II in the plasma, which leads to increased plasma renin activity (by inhibition of the negative feedback of renin release) and reduced secretion of aldosterone. Since ACE inactivates bradykinin, inhibition of ACE also results in an increased activity of circulating and local kallikrein-kinin systems (and thus also activation of the prostaglandin system).

Quinapril

Quinapril is a potent angiotensin-converting enzyme (ACE) inhibitor. The mode of action of quinapril in humans and animals is to inhibit circulating and tissue ACE activity, thereby decreasing vasopressor activity and aldosterone secretion.

Ramipril

Ramiprilat, the active metabolite of the prodrug ramipril, inhibits the enzyme dipeptidylcarboxypeptidase I (synonyms: angiotensin-converting enzyme; kininase II). In plasma and tissue this enzyme catalyses the conversion of angiotensin I to the active vasoconstrictor substance angiotensin II, as well as the breakdown of the active vasodilator bradykinin. Reduced angiotensin II formation and inhibition of bradykinin breakdown lead to vasodilatation.

Trandolapril

Trandolapril is a prodrug, which is rapidly, non-specifically hydrolysed to its potent, long-acting active metabolite, trandolaprilat (other metabolites are inactive) and acts as an orally-active angiotensin converting enzyme inhibitor (ACE inhibitor) without a sulphydryl group. In addition to inhibition of plasma ACE, trandolapril has been experimentally shown to inhibit tissue ACE (particularly vascular, cardial and adrenal). The clinical relevance of tissue ACE inhibition has not been established in humans.

Zofenopril

The beneficial effects of zofenopril in hypertension and acute myocardial infarction appear to result primarily from the suppression of the plasma renin-angiotensin aldosterone system. Inhibition of ACE (Ki 0.4nM in rabbit lung for arginine salt of zofenoprilat) results in decreased plasma angiotensin II, which leads to decreased vasopressor activity and to reduced aldosterone secretion.

Monographs

Monograph
Type
Country
ACCUPRIL Film-coated tablet
MPI, US: SPL/Old
US
ACCUPRO Film-coated tablet
MPI, EU: SmPC
UK
ALTACE Capsule
MPI, US: SPL/PLR
US
CAPOTEN Tablets
MPI, EU: SmPC
UK
COVERSYL ARGININE Film-coated tablets
MPI, EU: SmPC
UK
LOTENSIN Tablet
MPI, US: SPL/PLR
US
PRINIVIL Tablet
MPI, US: SPL/PLR
US
TANATRIL Tablet
MPI, EU: SmPC
UK
TRITACE Tablet
MPI, EU: SmPC
UK
VASCACE Film-coated tablet
MPI, EU: SmPC
UK
VASOTEC Tablet
MPI, US: SPL/Old
US
ZESTRIL Tablet
MPI, EU: SmPC
UK
ZESTRIL Tablet
MPI, US: SPL/PLR
US