药品详细
Olmesartan(奥美沙坦)
化学结构式图
中文名
奥美沙坦
英文名
Olmesartan
分子式
C24H26N6O3
化学名
4-(2-hydroxypropan-2-yl)-2-propyl-1-({4-[2-(1H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-1H-imidazole-5-carboxylic acid
分子量
Average: 446.5016
Monoisotopic: 446.206638728
Monoisotopic: 446.206638728
CAS号
144689-63-4
ATC分类
C09C 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
Olmesartan is an antihypertensive agent, which belongs to the class of medications called angiotensin II receptor blockers. It is indicated for the treatment of high blood pressure and is marketed under the name Olmetec®. The FDA label includes a black-box warning of injury and death to the fetus, so women of child-bearing age need to be warned and take the necessary precautions. Olmesartan is also contraindicated in diabetes mellitus patients taking aliskiren.
生产厂家
- Daiichi Sankyo
- Daiichi sankyo inc
封装厂家
- Bryant Ranch Prepack
- Cardinal Health
- Daiichi Sankyo
- DispenseXpress Inc.
- Dispensing Solutions
- Lake Erie Medical and Surgical Supply
- Murfreesboro Pharmaceutical Nursing Supply
- Physicians Total Care Inc.
- Quality Care
- Resource Optimization and Innovation LLC
- Schering-Plough Inc.
- Southwood Pharmaceuticals
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
药理
| Indication | For the treatment of hypertension. |
| Pharmacodynamics | Olmesartan is a specific angiotensin II type 1 (AT1) receptor antagonist, which blocks the blood pressure increasing effects of angiotensin II via the renin-angiotensin-aldosterone system (RAAS). During sympathetic stimulation or when renal blood pressure or blood flow is reduced, renin is released from granular cells of the juxtaglomerular apparatus in the kidneys. Renin cleaves circulating angiotensinogen to angiotensin I, which is cleaved by angiotensin converting enzyme (ACE) to angiotensin II. Angiotensin II increases blood pressure by increasing total peripheral resistance, increasing sodium and water reabsorption in the kidneys via aldosterone secretion, and altering cardiovascular structure. Angiotensin II binds to two receptors: AT1 and AT2. AT1 is a G-protein coupled receptor (GPCR) that mediates the vasoconstrictive and aldosterone-secreting effects of angiotensin II. Angiotensin receptor blockers (ARBs) are non-peptide competitive inhibitors of AT1. ARBs block the ability of angiotensin II to stimulate pressor and cell proliferative effects. Unlike ACE inhibitors, ARBs do not affect bradykinin-induced vasodilation. The overall effect of ARBs is a decrease in blood pressure. |
| Mechanism of action | Olmesartan is an ARB that selectively inhibits the binding of angiotensin II to AT1, which is found in many tissues such as vascular smooth muscle and the adrenal glands. This effectively inhibits the AT1-mediated vasoconstrictive and aldosterone-secreting effects of angiotensin II and results in a decrease in vascular resistance and blood pressure. Olmesartan is selective for AT1 and has a 12,500 times greater affinity for AT1 than the AT2 receptor. Also unlike the well-known ARB losartan, olmesartan does not have an active metabolite or possess uricosuric effects. |
| Absorption | Bioavailability is about 26%. Food does not affect the bioavailability of olmesartan. |
| Volume of distribution | The volume of distribution is 17 L and olmesartan poorly crosses the blood brain barrier. |
| Protein binding | Highly bound to plasma proteins (99%) and does not penetrate red blood cells. |
| Metabolism |
Olmesartan is rapidly and completely bioactivated by ester hydrolysis to olmesartan during absorption from the gastrointestinal tract. There is virtually no further metabolism of olmesartan.
|
| Route of elimination | Olmesartan is elminated unchanged in the urine (35% to 50%) and the remainder in the feces. |
| Half life | The half life is approximately 13 hours. |
| Clearance |
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| Toxicity | The main symptoms of overdose include low blood pressure and fast heartbeat. |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Drospirenone | Increased risk of hyperkalemia |
| Tobramycin | Increased risk of nephrotoxicity |
| Trandolapril | The angiotensin II receptor blocker, Olmesartan, may increase the adverse effects of Trandolapril. |
| Treprostinil | Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. |
食物相互作用
- Food does not affect the bioavailability of olmesartan.
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