药品详细
Pralidoxime(解磷定)
化学结构式图
中文名
解磷定
英文名
Pralidoxime
分子式
C7H9N2O
化学名
2-[(1E)-(hydroxyimino)methyl]-1-methylpyridin-1-ium
分子量
Average: 137.1592
Monoisotopic: 137.07148792
Monoisotopic: 137.07148792
CAS号
6735-59-7
ATC分类
V03A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
Pralidoxime is an antidote to organophosphate pesticides and chemicals. Organophosphates bind to the esteratic site of acetylcholinesterase, which results initially in reversible inactivation of the enzyme. If given within 24 hours,after organophosphate exposure, pralidoxime reactivates the enzyme cholinesterase by cleaving the phosphate-ester bond formed between the organophosphate and acetylcholinesterase.
生产厂家
- Baxter healthcare corp anesthesia critical care
- Meridian medical technologies inc
- Wyeth ayerst laboratories
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
药理
| Indication | For the treatment of poisoning due to those pesticides and chemicals of the organophosphate class which have anticholinesterase activity and in the control of overdosage by anticholinesterase drugs used in the treatment of myasthenia gravis. |
| Pharmacodynamics | Pralidoxime is to reactivate cholinesterase (mainly outside of the central nervous system) which has been inactivated by phosphorylation due to an organophosphate pesticide or related compound. The destruction of accumulated acetylcholine can then proceed, and neuromuscular junctions will again function normally. Pralidoxime also slows the process of "aging" of phosphorylated cholinesterase to a nonreactivatable form, and detoxifies certain organophosphates by direct chemical reaction. The drug has its most critical effect in relieving paralysis of the muscles of respiration. Because pralidoxime is less effective in relieving depression of the respiratory center, atropine is always required concomitantly to block the effect of accumulated acetylcholine at this site. Pralidoxime relieves muscarinic signs and symptoms, salivation, bronchospasm, etc., but this action is relatively unimportant since atropine is adequate for this purpose. |
| Mechanism of action | Pralidoxime is an antidote to organophosphate pesticides and chemicals. Organophosphates bind to the esteratic site of acetylcholinesterase, which results initially in reversible inactivation of the enzyme. Acetylcholinesterase inhibition causes acetylcholine to accumulate in synapses, producing continuous stimulation of cholinergic fibers throughout the nervous systems. If given within 24 hours after organophosphate exposure, pralidoxime reactivates the acetylcholinesterase by cleaving the phosphate-ester bond formed between the organophosphate and acetylcholinesterase. |
| Absorption | Not Available |
| Volume of distribution | Not Available |
| Protein binding | No binding to plasma proteins |
| Metabolism |
Hepatic
|
| Route of elimination | The drug is rapidly excreted in the urine partly unchanged, and partly as a metabolite produced by the liver. |
| Half life | 74-77 minutes |
| Clearance | Not Available |
| Toxicity | Not Available |
| 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
食物相互作用
Not Available
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