药品详细
Bepridil(苄普地尔)
化学结构式图
中文名
苄普地尔
英文名
Bepridil
分子式
C24H34N2O
化学名
N-benzyl-N-[3-(2-methylpropoxy)-2-(pyrrolidin-1-yl)propyl]aniline
分子量
Average: 366.5396
Monoisotopic: 366.26711372
Monoisotopic: 366.26711372
CAS号
64706-54-3
ATC分类
C08E 未知
药物类型
small molecule
阶段
approved, withdrawn
商品名
同义名
基本介绍
A long-acting, non selective, calcium channel blocker with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist. [PubChem] It is no longer marketed in the United States, as it has been implicated in causing ventricular arrhythmias (ie. Torsade de pointes).
生产厂家
- Johnson and johnson pharmaceutical research and development llc
- Medpointe pharmaceuticals medpointe healthcare inc
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 |
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| Substructures |
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适应症
药理
| Indication | For the treatment of hypertension, and chronic stable angina (classic effort-associated angina). |
| Pharmacodynamics | Bepridil is a calcium channel blocker that has well characterized anti-anginal properties and known but poorly characterized type 1 anti-arrhythmic and anti-hypertensive properties. It is not related chemically to other calcium channel blockers such as diltiazem hydrochloride, nifedipine and verapamil hydrochloride. |
| Mechanism of action | Bepridil has inhibitory effects on both the slow calcium (L-type) and fast sodium inward currents in myocardial and vascular smooth muscle, interferes with calcium binding to calmodulin, and blocks both voltage and receptor operated calcium channels. Bepridil inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle. This has been demonstrated in isolated myocardial and vascular smooth muscle preparations in which both the slope of the calcium dose response curve and the maximum calcium-induced inotropic response were significantly reduced by bepridil. In cardiac myocytes in vitro, bepridil was shown to be tightly bound to actin. Bepridil regularly reduces heart rate and arterial pressure at rest and at a given level of exercise by dilating peripheral arterioles and reducing total peripheral resistance (afterload) against which the heart works. |
| Absorption | Rapidly and completely absorbed after oral administration. |
| Volume of distribution | Not Available |
| Protein binding | 99% |
| Metabolism |
Hepatic.
|
| Route of elimination | Not Available |
| Half life | 24-50 hours |
| Clearance | Not Available |
| Toxicity | There has been one experience with overdosage in which a patient inadvertently took a single dose of 1600 mg of bepridil. The patient was observed for 72 hours in intensive care, but no significant adverse experiences were noted. |
| Affected organisms |
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| 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 |
|---|---|
| Amprenavir | Amprenavir may increase the effect and toxicity of bepridil. |
| Artemether | Additive QTc-prolongation may occur. Concomitant therapy should be avoided. |
| Astemizole | Increased risk of cardiotoxicity and arrhythmias |
| Atazanavir | Atazanavir may increase the effect and toxicity of bepridil. |
| Cisapride | Increased risk of cardiotoxicity and arrhythmias |
| Etravirine | Bepridil (withdrawn from US. market), when used concomitantly with etravirine, may experience a decrease in serum concentration. If possible, it is recommended to monitor for decreased bepridil concentrations and therapeutic efficacy. |
| Fosamprenavir | Amprenavir increases the effect and toxicity of bepridil |
| Gatifloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Grepafloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Levofloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Lumefantrine | Additive QTc-prolongation may occur. Concomitant therapy should be avoided. |
| Moxifloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Ritonavir | Ritonavir increases the effect and toxicity of bepridil |
| Sparfloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Telavancin | Additive QTc-prolongation may occur. Concomitant therapy should be avoided. |
| Terfenadine | Increased risk of cardiotoxicity and arrhythmias |
| Tipranavir | Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Bepridil. Concomitant therapy is contraindicated. |
食物相互作用
- Alcohol may further decrease blood pressure and increase dizziness and drowsiness
- Take with food to reduce nausea.
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