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药品详细

Physostigmine(毒扁豆碱)

化学结构式图
中文名
毒扁豆碱
英文名
Physostigmine
分子式
C15H21N3O2
化学名
(3aS,8aR)-1,3a,8-trimethyl-1H,2H,3H,3aH,8H,8aH-pyrrolo[2,3-b]indol-5-yl N-methylcarbamate
分子量
Average: 275.3461
Monoisotopic: 275.163376931
CAS号
57-47-6
ATC分类
S01E 抗青光眼制剂及缩瞳药;V03A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. [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
    • Indoles and Indole Derivatives
    • Phenethylamines
    • Phenylpropylamines
    Substructures
    • Indoles and Indole Derivatives
    • Carbamates and Derivatives
    • Phenols and Derivatives
    • Pyrrolidines
    • Ethers
    • Benzene and Derivatives
    • Aminals and Derivatives
    • Phenethylamines
    • Heterocyclic compounds
    • Aromatic compounds
    • Anisoles
    • Phenylpropylamines
    • Phenyl Esters
    • Anilines
    • Pyrrolines
    适应症
    药理
    Indication For the treatment of glaucoma, and in the treatment of severe anticholinergic toxicity.
    Pharmacodynamics Physostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor which effectively increases the concentration of acetylcholine at the sites of cholinergic transmission. Physostigmine is used to treat glaucoma. Because it crosses the blood-brain barrier, it is also used to treat the central nervous system effects of atropine overdose and other anticholinergic drug overdoses. Physostigmine can reverse both central and peripheral anticholinergia.
    Mechanism of action Physostigmine inhibits acetylcholinesterase, the enzyme responsible for the breakdown of used acetylcholine. By interfering with the metabolism of acetylcholine, physostigmine indirectly stimulates both nicotinic and muscarinic receptors due to the consequential increase in available acetylcholine at the synapse.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Quickly hydrolyzed by cholinesterases
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Side effects include increased sweating, loss of bladder control, muscle weakness, nausea, vomiting, diarrhea, or stomach cramps or pain, shortness of breath, tightness in chest, or wheezing, slow or irregular heartbeat, unusual tiredness or weakness, watering of mouth, blurred vision or change in near or distant vision, and eye pain.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 105.5 °C PhysProp
    water solubility 7760 mg/L Not Available
    logP 1.58 HANSCH,C ET AL. (1995)
    pKa 6.12 MERCK INDEX (1996)
    Predicted Properties
    Property Value Source
    water solubility 9.92e-01 g/l ALOGPS
    logP 1.8 ALOGPS
    logP 2.23 ChemAxon
    logS -2.4 ALOGPS
    pKa (strongest acidic) 14.77 ChemAxon
    pKa (strongest basic) 6.59 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 3 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 44.81 ChemAxon
    rotatable bond count 2 ChemAxon
    refractivity 78.4 ChemAxon
    polarizability 30.62 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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