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药品详细

Benazepril(贝那普利)

化学结构式图
中文名
贝那普利
英文名
Benazepril
分子式
C24H28N2O5
化学名
2-[(3S)-3-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]acetic acid
分子量
Average: 424.4895
Monoisotopic: 424.199822016
CAS号
86541-75-5
ATC分类
C09A 未知
药物类型
small molecule
阶段
approved
商品名
Briem (Pierre Fabre (France));Cibacen (Novartis (Belgium, Philippines, Switzerland, Turkey), Meda (Denmark, Germany, Greece, Ireland, Italy, Netherlands, Spain));Cibacene (Meda (France));Lotensin (Novartis Pharmaceuticals);
同义名
Benazepril HCl;Benazepril Hydrochloride;Benazeprilum [Latin];
基本介绍

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.

生产厂家
  • Apotex inc etobicoke site
  • Aurobindo pharma ltd
  • Biokey inc
  • Genpharm inc
  • Huahai us inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mylan pharmaceuticals inc
  • Novartis pharmaceuticals corp
  • Ranbaxy laboratories ltd
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc florida
  • Zydus pharmaceuticals usa inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Chan KK, Buch A, Glazer RD, John VA, Barr WH: Site-differential gastrointestinal absorption of benazepril hydrochloride in healthy volunteers. Pharm Res. 1994 Mar;11(3):432-7. Pubmed
  2. De Feo P, Torlone E, Perriello G, Fanelli C, Epifano L, Di Vincenzo A, Modarelli F, Motolese M, Brunetti P, Bolli GB: Short-term metabolic effects of the ACE-inhibitor benazepril in type 2 diabetes mellitus associated with arterial hypertension. Diabete Metab. 1992 Jul-Aug;18(4):283-8. Pubmed
  3. Gengo FM, Brady E: The pharmacokinetics of benazepril relative to other ACE inhibitors. Clin Cardiol. 1991 Aug;14(8 Suppl 4):IV44-50; discussion IV51-5. Pubmed
  4. Hou FF, Zhang X, Zhang GH, Xie D, Chen PY, Zhang WR, Jiang JP, Liang M, Wang GB, Liu ZR, Geng RW: Efficacy and safety of benazepril for advanced chronic renal insufficiency. N Engl J Med. 2006 Jan 12;354(2):131-40. Pubmed
  5. Ishimitsu T, Akashiba A, Kameda T, Takahashi T, Ohta S, Yoshii M, Minami J, Ono H, Numabe A, Matsuoka H: Benazepril slows progression of renal dysfunction in patients with non-diabetic renal disease. Nephrology (Carlton). 2007 Jun;12(3):294-8. Pubmed
  6. MacNab M, Mallows S: Safety profile of benazepril in essential hypertension. Clin Cardiol. 1991 Aug;14(8 Suppl 4):IV33-7; discussion IV51-5. Pubmed
  7. Szekacs B, Vajo Z, Dachman W: Effect of ACE inhibition by benazepril, enalapril and captopril on chronic and post exercise proteinuria. Acta Physiol Hung. 1996;84(4):361-7. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Phenylpropylamines
  • Lactams
  • Benzazepines
Substructures
  • Carboxylic Acids and Derivatives
  • Hydroxy Compounds
  • Acetates
  • Aliphatic and Aryl Amines
  • Amino Ketones
  • Ethers
  • Benzene and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Phenylpropylamines
  • Amino Acids
  • Lactams
  • Benzazepines
  • Anilines
适应症
ANTIHYPERTENSIVES 降血压;
药理
Indication For the treatment of hypertension. It may be used alone or in combination with thiazide diuretics.
Pharmacodynamics 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.
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.
Volume of distribution Not Available
Protein binding benazepril, 97%; benazeprilat, 95%
Metabolism
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.

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Benazepril
    		benazeprilat Details
    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
    Pathways
    Pathway Name SMPDB ID
    Smp00145 Benazepril Pathway SMP00145
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 148.5 °C PhysProp
    water solubility 2.229 mg/L Not Available
    logP 3.3 Not Available
    Predicted Properties
    Property Value Source
    water solubility 1.05e-02 g/l ALOGPS
    logP 1.14 ALOGPS
    logP 1.54 ChemAxon
    logS -4.6 ALOGPS
    pKa (strongest acidic) 3.53 ChemAxon
    pKa (strongest basic) 5.36 ChemAxon
    physiological charge -1 ChemAxon
    hydrogen acceptor count 5 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 95.94 ChemAxon
    rotatable bond count 10 ChemAxon
    refractivity 115.23 ChemAxon
    polarizability 44.98 ChemAxon
    药物相互作用
    Drug Interaction
    Amiloride Increased risk of hyperkalemia
    Azilsartan medoxomil Pharmacodynamic synergism: dual blockade of renin-angiotensin system. Increases risks of hypotension, hyperkalemia, renal impairment.
    Drospirenone Increased risk of hyperkalemia
    Icatibant Icatibant may attenuate the antihypertensive effect of ACE inhibitors by pharmacodynamic antagonism. Monitor concomitant therapy closely.
    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
    食物相互作用
    • Benazepril may decrease the excretion of potassium. Salt um may increase the risk of hyperkalemia. substitutes containing potassi
    • Food slows absorption without decreasing the quantity absorbed.
    • Herbs that may attenuate the antihypertensive effect of benazepril include: bayberry, blue cohash, cayenne, ephedra, ginger, ginseng (American), kola and licorice.
    • High salt intake may attenuate the antihypertensive effect of benazepril.
    • Take without regard to meals.

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