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
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
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Route of elimination | Not Available | ||||||
Half life | Not Available | ||||||
Clearance | Not Available | ||||||
Toxicity | Not Available | ||||||
Affected organisms | Not Available | ||||||
Pathways |
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理化性质
Properties | |||||||||||||||||||||||||||||||||||||||||||
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State | solid | ||||||||||||||||||||||||||||||||||||||||||
Experimental Properties | Not Available | ||||||||||||||||||||||||||||||||||||||||||
Predicted Properties |
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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.