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Home / Drugs / Starting with B / Benazepril
 
Benazepril
 

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.
BrandsBriem
Cibacen
Cibacene
Lotensin
CategoriesAntihypertensive Agents
Angiotensin-converting Enzyme Inhibitors
ManufacturersApotex inc etobicoke site
Aurobindo pharma ltd
Biokey inc
Genpharm inc
Huahai us inc
Ivax pharmaceuticals inc sub teva pharmaceuticals usa
Mylan pharmaceuticals inc
Ranbaxy laboratories ltd
Sandoz inc
Teva pharmaceuticals usa inc
Watson laboratories inc florida
Zydus pharmaceuticals usa inc
Novartis pharmaceuticals corp
PackagersAdvanced Pharmaceutical Services Inc.
Amneal Pharmaceuticals
Apotex Inc.
Apotheca Inc.
A-S Medication Solutions LLC
Atlantic Biologicals Corporation
Aurobindo Pharma Ltd.
Bryant Ranch Prepack
Cardinal Health
Caremark LLC
Corepharma LLC
Direct Dispensing Inc.
Direct Pharmaceuticals Inc.
Dispensing Solutions
Diversified Healthcare Services Inc.
Doctor Reddys Laboratories Ltd.
Eon Labs
Ethex Corp.
Greenstone LLC
H.J. Harkins Co. Inc.
Heartland Repack Services LLC
International Laboratories Inc.
Ivax Pharmaceuticals
KV Pharmaceutical Co.
Lake Erie Medical and Surgical Supply
Liberty Pharmaceuticals
Lupin Pharmaceuticals Inc.
Murfreesboro Pharmaceutical Nursing Supply
Mylan
Novartis AG
Nucare Pharmaceuticals Inc.
Ohm Laboratories Inc.
Palmetto Pharmaceuticals Inc.
PCA LLC
PD-Rx Pharmaceuticals Inc.
Pharmaceutical Utilization Management Program VA Inc.
Physicians Total Care Inc.
Preferred Pharmaceuticals Inc.
Prepak Systems Inc.
Ranbaxy Laboratories
Rebel Distributors Corp.
Resource Optimization and Innovation LLC
Sandoz
Southwood Pharmaceuticals
Stat Rx Usa
Teva Pharmaceutical Industries Ltd.
UDL Laboratories
SynonymsBenazepril HCl
Benazepril Hydrochloride
Benazeprilum [Latin]

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. 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.

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.

toxicity

Most likely symptom of overdosage is severe hypotension. Most common adverse effects include headache, dizziness, fatigue, somnolence, postural dizziness, nausea, and cough.

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.

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.

half life

10-11 hours

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.

drug interactions

Amiloride: Increased risk of hyperkalemia

Drospirenone: Increased risk of hyperkalemia

Lithium: The ACE inhibitor increases serum levels of lithium

Potassium: Increased risk of hyperkalemia

Spironolactone: Increased risk of hyperkalemia

Tizanidine: Tizanidine increases the risk of hypotension with the ACE inhibitor

Tobramycin: Increased risk of nephrotoxicity

Treprostinil: Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.

Triamterene: Increased risk of hyperkalemia