Drug/Small Molecule:
benazepril

2D structure

Overview

Generic Names: benazepril
Trade Names: Benazepril HCl; Benazepril Hydrochloride; Benazeprilum [Latin]; Briem; Cibacen; Cibacene; Lotensin
Brand Mixtures: Lotensin HCT (Benazepril Hydrochloride + Hydrochlorothiazide); Lotrel (Benazepril Hydrochloride + Amlodipine Besylate)
PharmGKB Accession Id: PA448561

Description

Benazepril, brand name Lotensin®, is a medication used to treat high blood pressure (hypertension), congestive heart failure, and chronic renal failure. Upon cleavage of its ester group by the liver, benazepril is converted into its active form benazeprilat, a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor. (source: Drug Bank)

Indication

For the treatment of hypertension. It may be used alone or in combination with thiazide diuretics. (source: Drug Bank)

ATC Therapeutic Category

  • C09AA:ACE inhibitors, plain

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Benazeprilat, the active metabolite of Benazepril, competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. Inhibition of ACE results in decreased plasma angiotensin II. As angiotensin II is a vasoconstrictor and a negative-feedback mediator for renin activity, lower concentrations result in a decrease in blood pressure and stimulation of baroreceptor reflex mechanisms, which leads to decreased vasopressor activity and to decreased aldosterone secretion. Benazeprilat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin. (source: Drug Bank)

Pharmacology

Benazepril, an angiotensin-converting enzyme (ACE) inhibitor, is a prodrug which, when hydrolyzed by estarases to its active Benazeprilat, is used to treat hypertension and heart failure, to reduce proteinuria and renal disease in patients with nephropathies, and to prevent stroke, myocardial infarction, and cardiac death in high-risk patients. Benazepril and Benazeprilat inhibit angiotensin-converting enzyme (ACE) in human subjects and animals. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex. (source: Drug Bank)

Food Interactions

Food slows absorption without decreasing the quantity absorbed.
Take without regard to meals. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Cleavage of the ester group (primarily in the liver) converts benazepril to its active metabolite, benazeprilat. (source: Drug Bank)

Protein Binding

96.7% (source: Drug Bank)

Absorption

Peak in plasma within 0.5-1.0 hours. The extent of absorption is at least 37% as determined by urinary recovery and is not significantly influenced by the presence of food in the GI tract. (source: Drug Bank)

Toxicity

Symptoms of overdose include swelling of face, mouth, hands, or feet, trouble in swallowing or breathing (sudden), hoarseness, fever and chills. (source: Drug Bank)

Isomeric SMILES Code:

CCOC(=O)[C@H](CCC1=CC=CC=C1)N[C@H]2CCC3=CC=CC=C3N(C2=O)CC(=O)O (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs4961 at chr4:2876505 in ADD1
    Ina study of 954 Chinese hypertensives, systolic blood pressure of those with ACE:I/D DD and ADD1:Gly460Trp Gly/Gly genotypes was significantly higher than carriers of ACE:I or ADD1:460Trp. However, genotype was not related to benazepril treatment response.
    Variant Name:
    ADD1:Gly460Trp, rs4961 G>T, alpha-adducin Gly460Trp
    Related Drugs:
    benazepril
    Related Diseases:
    Hypertension
    Evidence:
    PMID:15773232
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ACE
  •   
  • PD
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ADD1
  •   
  • PD
  •   
  •   
  • GN
Publications, Variants

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
ACE Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
amiloride Uncurated Annotation Increased risk of hyperkaliemia (source: Drug Bank)
lithium Uncurated Annotation The ACE inhibitor increases serum levels of lithium (source: Drug Bank)
potassium Uncurated Annotation Increased risk of hyperkaliemia (source: Drug Bank)
spironolactone Uncurated Annotation Increased risk of hyperkaliemia (source: Drug Bank)
tizanidine Uncurated Annotation Tizanidine increases the risk of hypotension with the ACE inhibitor (source: Drug Bank)
triamterene Uncurated Annotation Increased risk of hyperkaliemia (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Diabetes Mellitus, Type 2
  •   
  • PD
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Proteinuria
  •   
  • PD
  •   
  •   
  • GN
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00542
ChEBI ID:
3011
KEGG Compound ID:
C06843
PubChem Compound ID:
5362124
PubChem Substance ID:
205187

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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