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药品详细

Acepromazine(乙酰丙嗪)

化学结构式图
中文名
乙酰丙嗪
英文名
Acepromazine
分子式
C19H22N2OS
化学名
1-{10-[3-(dimethylamino)propyl]-10H-phenothiazin-2-yl}ethan-1-one
分子量
Average: 326.456
Monoisotopic: 326.145284026
CAS号
61-00-7
ATC分类
N05A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Acepromazine is one of the phenothiazine derivative psychotropic drugs, used little in humans, however frequently in animals as a sedative and antiemetic.

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
    • Phenothiazines
    Substructures
    • Ethers
    • Phenothiazines
    • Aliphatic and Aryl Amines
    • Thiazines
    • Benzene and Derivatives
    • Heterocyclic compounds
    • Aromatic compounds
    • Benzoyl Derivatives
    • Anilines
    • Ketones
    适应症
    药理
    Indication Acepromazine was first used in humans in the 1950s as an antipsychotic agent. It is now rarely used in humans. Acepromazine is frequently used in animals as a sedative and antiemetic. Its principal value is in quietening and calming anxious animals.
    Pharmacodynamics Acepromazine is one of the phenothiazine derivative psychotropic drugs. Acepromazine has actions at all levels of the central nervous system-primarily at subcortical levels-as well as on multiple organ systems. Acepromazine has strong antiadrenergic and weaker peripheral anticholinergic activity; ganglionic blocking action is relatively slight. It also possesses slight antihistaminic and antiserotonin activity.
    Mechanism of action Acepromazine acts as an antagonist (blocking agent) on different postsysnaptic receptors -on dopaminergic-receptors (subtypes D1, D2, D3 and D4 - different antipsychotic properties on productive and unproductive symptoms), on serotonergic-receptors (5-HT1 and 5-HT2, with anxiolytic, antidepressive and antiaggressive properties as well as an attenuation of extrapypramidal side-effects, but also leading to weight gain, fall in blood pressure, sedation and ejaculation difficulties), on histaminergic-receptors (H1-receptors, sedation, antiemesis, vertigo, fall in blood pressure and weight gain), alpha1/alpha2-receptors (antisympathomimetic properties, lowering of blood pressure, reflex tachycardia, vertigo, sedation, hypersalivation and incontinence as well as sexual dysfunction, but may also attenuate pseudoparkinsonism - controversial) and finally on muscarinic (cholinergic) M1/M2-receptors (causing anticholinergic symptoms like dry mouth, blurred vision, obstipation, difficulty/inability to urinate, sinus tachycardia, ECG-changes and loss of memory, but the anticholinergic action may attenuate extrapyramidal side-effects).
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life 3 hours in horses.
    Clearance Not Available
    Toxicity Agitation, coma, convulsions, difficulty breathing, difficulty swallowing, dry mouth, extreme sleepiness, fever, intestinal blockage, irregular heart rate, low blood pressure, restlessness
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State liquid
    Experimental Properties
    Property Value Source
    melting point < 25 °C PhysProp
    boiling point 230 °C at 5.00E-01 mm Hg PhysProp
    Predicted Properties
    Property Value Source
    water solubility 9.80e-03 g/l ALOGPS
    logP 4.32 ALOGPS
    logP 3.49 ChemAxon
    logS -4.5 ALOGPS
    pKa (strongest acidic) 16.06 ChemAxon
    pKa (strongest basic) 8.5 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 3 ChemAxon
    hydrogen donor count 0 ChemAxon
    polar surface area 23.55 ChemAxon
    rotatable bond count 5 ChemAxon
    refractivity 99.35 ChemAxon
    polarizability 37.17 ChemAxon
    药物相互作用
    Drug Interaction
    Donepezil Possible antagonism of action
    Galantamine Possible antagonism of action
    食物相互作用
    • Avoid alcohol
    • Take with food to reduce irritation

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