Benazepril

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Benazepril
Benazepril structure.svg
Benazepril-3D-balls.png
Systematic (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
Clinical data
Trade names Lotensin
AHFS/Drugs.com Monograph
MedlinePlus a692011
Pregnancy
category
  • D
Routes of
administration
Oral
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
CAS Number 86541-75-5 YesY
ATC code C09AA07 (WHO)
PubChem CID 5362124
IUPHAR/BPS 6374
DrugBank DB00542 YesY
ChemSpider 4514935 YesY
UNII UDM7Q7QWP8 YesY
ChEBI CHEBI:3011 YesY
ChEMBL CHEMBL838 YesY
Chemical data
Formula C24H28N2O5
Molar mass 424.49 g/mol
  (verify)

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.

Benazeprilat — the active metabolite of benazepril

Medical uses[edit]

Kidney disease[edit]

Patients with advanced renal insufficiency taking benazepril show "substantial" kidney benefits.[1] 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.[2] 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.[2]" 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.

Side effects[edit]

The most common side effects patients experience are a headache or a chronic cough. The chronic cough develops in about 20% of patients treated,[3] and those patients that experience it find it develops after a few months of use. Anaphylaxis, angioedema, and elevation of potassium levels are more serious side effects that can also occur.

Contraindications[edit]

Benazepril should be discontinued during pregnancy, as it can harm the fetus.

Dosage forms[edit]

It is also available in combination with hydrochlorothiazide, under the trade name Lotensin HCT', and with amlodipine (trade name Lotrel).

Veterinary use[edit]

Under the brand names Fortekor (Novartis) and VetACE (Jurox Animal Health),[citation needed] benazepril hydrochloride is used to treat congestive heart failure in dogs[4][5] and chronic renal failure in dogs and cats.[citation needed]

References[edit]

  1. ^ Hou F, Zhang X, Zhang G, Xie D, Chen P, Zhang W, Jiang J, Liang M, Wang G, Liu Z, Geng R (2006). "Efficacy and safety of benazepril for advanced chronic renal insufficiency". N Engl J Med. 354 (2): 131–40. doi:10.1056/NEJMoa053107. PMID 16407508. 
  2. ^ a b Hitti, Miranda; Chang, Louise (January 11, 2006). "Drug May Treat Advanced Kidney Disease". WebMD. Retrieved 2006-09-07. 
  3. ^ Dykewicz, Mark S. (April 2004). "Cough and Angioedema From Angiotensin-Converting Enzyme Inhibitors: New Insights Into Mechanisms and Management". Medscape. Retrieved 2 April 2014. 
  4. ^ King JN, Mauron C, Kaiser G (December 1995). "Pharmacokinetics of the active metabolite of benazepril, benazeprilat, and inhibition of plasma angiotensin-converting enzyme activity after single and repeated administrations to dogs". Am. J. Vet. Res. 56 (12): 1620–8. PMID 8599524. 
  5. ^ O'Grady MR, O'Sullivan ML, Minors SL, Horne R (2009). "Efficacy of benazepril hydrochloride to delay the progression of occult dilated cardiomyopathy in Doberman Pinschers". J. Vet. Intern. Med. 23 (5): 977–83. doi:10.1111/j.1939-1676.2009.0346.x. PMID 19572914. 

External links[edit]