Benazepril

Benazepril
Clinical data


Trade names	Lotensin
AHFS/Drugs.com	Monograph
MedlinePlus	a692011
Pregnancy category	D
Routes of administration	Oral
ATC code	C09AA07 (WHO)
Legal status
Legal status	℞ (Prescription only)
Pharmacokinetic data
Protein binding	96.7%
Metabolism	Hepatic glucuronidation
Biological half-life	10-11 hours
Excretion	Renal and biliary
Identifiers
IUPAC name 2-[(3S)-3-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]-2-oxo-4,5-dihydro-3H-1-benzazepin-1-yl]acetic acid
CAS Number	86541-75-5^Y
PubChem (CID)	5362124
IUPHAR/BPS	6374
DrugBank	DB00542^Y
ChemSpider	4514935^Y
UNII	UDM7Q7QWP8^Y
ChEBI	CHEBI:3011^Y
ChEMBL	CHEMBL838^Y
Chemical and physical data
Formula	C₂₄H₂₈N₂O₅
Molar mass	424.49 g/mol
3D model (Jmol)	Interactive image
SMILES O=C(OCC)[C@@H](N[C@@H]2C(=O)N(c1ccccc1CC2)CC(=O)O)CCc3ccccc3
InChI InChI=1S/C24H28N2O5/c1-2-31-24(30)20(14-12-17-8-4-3-5-9-17)25-19-15-13-18-10-6-7-11-21(18)26(23(19)29)16-22(27)28/h3-11,19-20,25H,2,12-16H2,1H3,(H,27,28)/t19-,20-/m0/s1^Y Key:XPCFTKFZXHTYIP-PMACEKPBSA-N^Y

Benazepril, brand name Lotensin (Novartis), is an ACE inhibitor used primarily in treatment of hypertension, congestive heart failure, and heart attacks, and also in preventing the renal and retinal complications of diabetes.

ACE inhibitors relax blood vessels, and decrease blood volume, which lowers blood pressure and decreases oxygen demand from the heart. They inhibit angiotensin-converting enzyme, which is part of the renin–angiotensin–aldosterone system.

Benazepril is a prodrug which is metabolized by the liver into its active form benazeprilat via cleavage of the drug's ester group.

Patients with advanced renal insufficiency taking benazepril show "substantial" kidney benefits. A long-term study of patients' kidney disease revealed patients who took benazepril had better kidney function and slower progressions of kidney disease than their peers who took a placebo drug. This is notable because this category of pharmaceuticals has long been thought to cause further kidney damage or increase the rate of progression for kidney disease.

According to coverage of the study on WebMD: "ACE inhibitors can pose a potential threat to kidneys, as well. The key question was whether damaged kidneys would worsen if patients took ACE inhibitors. In a nutshell, concerns centered on blood levels of potassium and creatinine, waste products that are excreted by the kidneys. Testing creatinine levels in the blood is used as a way to monitor kidney function (...) kidney problems worsened more slowly in those taking Lotensin. Overall, there were no major differences in side effects between patients taking Lotensin or the placebo." This study marks the first indication that benazepril, and perhaps other ACE inhibitors, may actually be beneficial in the treatment of hypertension in patients with kidney disease.

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Wikipedia