- Overview
- Properties
- Genetics
- Related Genes
- Pathways
- Related Drugs
- Related Diseases
- Downloads/LinkOuts
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 (
)
-
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
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
|
ACE |
|
Publications |
|
|
ADD1 |
|
Publications, Variants |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| ACE |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| amiloride |
|
Increased risk of hyperkaliemia (source: Drug Bank) |
| lithium |
|
The ACE inhibitor increases serum levels of lithium (source: Drug Bank) |
| potassium |
|
Increased risk of hyperkaliemia (source: Drug Bank) |
| spironolactone |
|
Increased risk of hyperkaliemia (source: Drug Bank) |
| tizanidine |
|
Tizanidine increases the risk of hypotension with the ACE inhibitor (source: Drug Bank) |
| triamterene |
|
Increased risk of hyperkaliemia (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
Diabetes Mellitus, Type 2 |
|
Publications |
|
|
Proteinuria |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
