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药品详细

Cilazapril(西拉普利)

化学结构式图
中文名
西拉普利
英文名
Cilazapril
分子式
C22H31N3O5
化学名
(1S,9S)-9-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}-10-oxo-octahydro-1H-pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid
分子量
Average: 417.4986
Monoisotopic: 417.226371117
CAS号
92077-78-6
ATC分类
C09A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
Inhibace;
基本介绍

One of the angiotensin-converting enzyme inhibitors (ACE inhibitors) used for hypertension. It is a prodrug that is hydrolyzed after absorption to its main metabolite cilazaprilat. [PubChem]

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference Not Available
    剂型
    规格
    化合物类型
    Type small molecule
    Classes Not Available
    Substructures Not Available
    适应症
    ANTIHYPERTENSIVES 降血压;
    药理
    Indication Cilazapril is an ACE inhibtor class drug used in the treatment of hypertension and heart failure.
    Pharmacodynamics Cilazapril inhibits the production angiotensin II. By doing so, it decreases sodium and water reabsorption (via aldosterone) and it decreases vasoconstriction. The combined effect of this is a decrease in vascular resistance, and therefore, blood pressure.
    Mechanism of action Cilazapril is a pyridazine ACE inhibitor. It competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. As angiotensin II is a vasoconstrictor and a negative feedback mediator for renin activity, lower angiotensin II levels results in a decrease in blood pressure, an increase in renin activity, and stimulation of baroreceptor reflex mechanisms. Kininase II, an enzyme which degrades the vasodilator bradykinin, is identical to ACE and may also be inhibited.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Not Available
    Affected organisms Not Available
    Pathways
    Pathway Name SMPDB ID
    Smp00147 Cilazapril Pathway SMP00147
    理化性质
    Properties
    State solid
    Experimental Properties Not Available
    Predicted Properties
    Property Value Source
    water solubility 1.06e+00 g/l ALOGPS
    logP -0.2 ALOGPS
    logP -0.0079 ChemAxon
    logS -2.6 ALOGPS
    pKa (strongest acidic) 3.41 ChemAxon
    pKa (strongest basic) 5.35 ChemAxon
    physiological charge -1 ChemAxon
    hydrogen acceptor count 6 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 99.18 ChemAxon
    rotatable bond count 9 ChemAxon
    refractivity 110.56 ChemAxon
    polarizability 44.73 ChemAxon
    药物相互作用
    Drug Interaction
    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
    Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
    Triamterene Increased risk of hyperkalemia
    食物相互作用
    • Food decreases cilazapril absorption with no significant clinical impact.
    • Take without regard to meals.

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