药品详细
Neostigmine(新斯的明)
化学结构式图
中文名
新斯的明
英文名
Neostigmine
分子式
C12H19N2O2
化学名
3-[(dimethylcarbamoyl)oxy]-N,N,N-trimethylanilinium
分子量
Average: 223.2915
Monoisotopic: 223.144652862
Monoisotopic: 223.144652862
CAS号
59-99-4
ATC分类
N07A 未知;S01E 抗青光眼制剂及缩瞳药
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike physostigmine, does not cross the blood-brain barrier. [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 |
|
| Substructures |
|
适应症
药理
| Indication | Neostigmine is used for the symptomatic treatment of myasthenia gravis by improving muscle tone. |
| Pharmacodynamics | Neostigmine is a cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike physostigmine, does not cross the blood-brain barrier. By inhibiting acetylcholinesterase, more acetylcholine is available in the synapse, therefore, more of it can bind to the fewer receptors present in myasthenia gravis and can better trigger muscular contraction. |
| Mechanism of action | Neostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. The drug inhibits acetylcholinesterase which is responsible for the degredation of acetylcholine. So, with acetylcholinesterase inhibited, more acetylcholine is present By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors which are involved in muscle contraction.. It does not cross the blood-brain barrier. |
| Absorption | Neostigmine bromide is poorly absorbed from the gastrointestinal tract following oral administration |
| Volume of distribution | Not Available |
| Protein binding | Protein binding to human serum albumin ranges from 15 to 25 percent. |
| Metabolism |
Neostigmine undergoes hydrolysis by cholinesterase and is also metabolized by microsomal enzymes in the liver.
|
| Route of elimination | Not Available |
| Half life | The half-life ranged from 42 to 60 minutes with a mean half-life of 52 minutes. |
| Clearance | Not Available |
| Toxicity | Overdosage of Neostigmine can cause cholinergic crisis, which is characterized by increasing muscle weakness, and through involvement of the muscles of respiration, may result in death. The LD 50 of neostigmine methylsulfate in mice is 0.3 ± 0.02 mg/kg intravenously, 0.54 ± 0.03 mg/kg subcutaneously, and 0.395 ± 0.025 mg/kg intramuscularly; in rats the LD 50 is 0.315 ± 0.019 mg/kg intravenously, 0.445 ± 0.032 mg/kg subcutaneously, and 0.423 ± 0.032 mg/kg intramuscularly. |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Experimental Properties | Not Available | ||||||||||||||||||||||||||||||||||||
| Predicted Properties |
|
||||||||||||||||||||||||||||||||||||
药物相互作用
| Drug | Interaction |
|---|---|
| Dexamethasone | The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, neostigmine. |
| Fludrocortisone | The corticosteroid, fludrocortisone, may decrease the effect of the anticholinesterase, neostigmine. |
| Hydrocortisone | The corticosteroid, hydrocortisone, may decrease the effect of the anticholinesterase, neostigmine. |
| Prednisolone | The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, neostigmine. |
| Prednisone | The corticosteroid, prednisone, may decrease the effect of the anticholinesterase, neostigmine. |
| Triamcinolone | The corticosteroid, triamcinolone, may decrease the effect of the anticholinesterase, neostigmine. |
食物相互作用
Not Available
收藏