QuickView for Benazepril (compound)

Summary
General Info

PubChem

PubChem Compound 2311

Name:	benazepril
PubChem Compound ID:	2311
Molecular formula:	C₂₄H₂₈N₂O₅
Molecular weight:	424.49 g/mol

DrugBank

Identification

Name:	benazepril
Name (isomeric):	DB00542
Drug Type:	small molecule
Synonyms:	Benazepril HCl; Benazepril Hydrochloride; Benazeprilum [Latin]
Brand:	Cibacen, Briem, Lotensin, Cibacene
Brand name mixture:	Lotrel(benazepril hydrochloride + amlodipine besylate), Lotensin HCT(benazepril hydrochloride + hydrochlorothiazide)
Category:	Angiotensin-converting Enzyme Inhibitors, Antihypertensive Agents
CAS number:	86541-75-5

Pharmacology

Indication:	For the treatment of hypertension. It may be used alone or in combination with thiazide diuretics.
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. Ben... show more » 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. show less «
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 c... show more » 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. show less «
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.
Protein binding:	benazepril, 97%; benazeprilat, 95%
Biotransformation:	Cleavage of the ester group (primarily in the liver) converts benazepril to its active metabolite, benazeprilat. Benazepril and benazeprilat may be conjugated to glucuronic acid prior to urinary excretion.
Route of elimination:	Benazepril and benazeprilat are cleared predominantly by renal excretion in healthy subjects with normal renal function. Nonrenal (i.e., biliary) excretion accounts for approximately 11%-12% of benazeprilat excretion in healthy subjects.
Half Life:	10-11 hours
Clearance:	0.35 L/hr/kg [pediatric hypertensive patients receiving multiple daily doses of Benazepril hydrochloride 0.1 - 0.5 mg/kg] 0.13 L/hr/kg [healthy adults receiving a single dose of 10 mg]
Toxicity:	Most likely symptom of overdosage is severe hypotension. Most common adverse effects include headache, dizziness, fatigue, somnolence, postural dizziness, nausea, and cough.
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Food slows absorption without decreasing the quantity absorbed.

Benazepril may decrease the excretion of potassium. Salt um may increase the risk of hyperkalemia. substitutes containing potassi

High salt intake may attenuate the antihypertensive effect of benazepril.

Take without regard to meals.

Herbs that may attenuate the antihypertensive effect of benazepril include: bayberry, blue cohash, cayenne, ephedra, ginger, ginseng (American), kola and licorice.

Drug interaction:

Lithium	The ACE inhibitor increases serum levels of lithium
Tizanidine	Tizanidine increases the risk of hypotension with the ACE inhibitor
Tobramycin	Increased risk of nephrotoxicity
Spironolactone	Increased risk of hyperkalemia
Potassium	Increased risk of hyperkalemia

Targets

Angiotensin-converting enzyme

Enzymes

Methylenetetrahydrofolate reductase

Transporters

Oligopeptide transporter, small intestine isoform

Oligopeptide transporter, kidney isoform