Benazepril

Structural formula
General
Non-proprietary name	Benazepril
other names	(3 S ) -3 - {[(1 S ) -1-carboxy-3-phenylpropyl] amino} -2,3,4,5-tetrahydro-2-oxo-1 H -1-benzazepine-1-acetic acid- 3-ethyl ester; 3 - [(1 S ) -1-ethoxycarbonyl-3-phenylpropylamino] -2,3,4,5-tetrahydro-2-oxo-1 H -1-benzazepin-1-acetic acid;
Molecular formula	C 24 H 28 N 2 O 5
Brief description	colorless solid (hydrochloride)
External identifiers / databases
PubChem	5362124
ChemSpider	4514935
DrugBank	DB00542
Wikidata	Q592802
Drug information
ATC code	C09 AA07 Q C09AA07
Drug class	Antihypertensive drugs
Mechanism of action	ACE inhibitors
properties
Molar mass	424.49 g mol −1
Physical state	firmly
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS labeling of hazardous substances Hydrochloride;	no GHS pictograms
	no GHS pictograms
H and P phrases	H: no H-phrases
	P: no P-phrases
Toxicological data	> 5000 mg kg −1 ( LD 50 , rat , oral )
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Benazepril is a drug from the group of ACE inhibitors that is used to treat arterial hypertension (high blood pressure) and heart failure . Benazepril is a prodrug . After hydrolysis to benazeprilat, it inhibits the angiotensin converting enzyme (ACE).

pharmacology

application areas

Benazepril is used individually (monotherapy) and in combination with other antihypertensive agents (combination therapy, especially with diuretics or calcium channel blockers ), mainly for the treatment of high blood pressure . It can also be used to treat heart failure.

Mechanism of action

Benazepril leads as inhibitor of angiotensin converting enzyme in a decreased formation of angiotensin II from angiotensin I . This reduced formation of angiotensin II causes a decrease in the tone of the blood vessels and thus a decrease in blood pressure. The decrease in the angiotensin II level also leads to a reduction in the release of aldosterone from the adrenal cortex and thus to an influence on the water balance (see also renin-angiotensin-aldosterone system ).

Contraindications

Benazepril is contraindicated in hypersensitivity to other ACE inhibitors, with a vorberichtlich known angioneurotic edema due to an earlier use of an ACE inhibitor, in congenital or idiopathic angioneurotic edema, with bilateral renal artery stenosis after kidney transplants , with hemodynamically significant aortic or mitral valve stenosis and hypertrophic cardiomyopathy and used in primary aldosteronism . Concomitant use of aliskiren- containing medicinal products is contraindicated in patients with diabetes mellitus or renal insufficiency . The active substance must not be used in the second and third trimester of pregnancy , and use is not recommended in the first trimester either.

Pharmacokinetics

Benazeprilat - active metabolite of benazepril

Oral benazepril is rapidly absorbed and hydrolyzed to benazeprilat in the liver. It crosses the placental barrier . It is mainly excreted via the kidneys. The elimination half-life is 3.5 hours in dogs, the maximum effect sets in after 2 hours. The elimination half-life in humans is 10 to 11 hours.

Trade names

Human medicine

Benazeplus, Cibadrex, Cibacen and Generics

Veterinary medicine

Actikor, Benacep, Benadog, Benakor, Benazecare, Benefortin, Cardalis, Fortekor, Fortepril (except trade), Kelapril, Nelio, Prilben, Virbakor

Combination preparations

with Pimobendan : Fortekor Plus
with spironolactone : Cardalis

Individual evidence

↑ ^a ^b ^c Entry on benazepril at Vetpharm, accessed on May 19, 2016.
↑ ^a ^b ^c Datasheet Benazepril hydrochloride, European Pharmacopoeia (EP) Reference Standard from Sigma-Aldrich , accessed on May 21, 2016 ( PDF ).

[vetpharm-1] Entry on benazepril at Vetpharm, accessed on May 19, 2016.

[Sigma-2] Datasheet Benazepril hydrochloride, European Pharmacopoeia (EP) Reference Standard from Sigma-Aldrich , accessed on May 21, 2016 ( PDF ).