药品详细

Acetophenazine(醋奋乃静)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

醋奋乃静

英文名

Acetophenazine

分子式

C₂₃H₂₉N₃O₂S

化学名

1-(10-{3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl}-10H-phenothiazin-2-yl)ethan-1-one

分子量

Average: 411.56
Monoisotopic: 411.198047877

CAS号

2751-68-0

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

Acetophenazine is an antipsychotic drug of moderate-potency. It is used in the treatment of disorganized and psychotic thinking. It is also used to help treat false perceptions (e.g. hallucinations or delusions). It primarily targets the dopamine D2 receptor.

生产厂家

Schering corp sub schering plough corp

封装厂家

参考

Synthesis Reference

Not Available

General Reference

Jones GL, Woodbury DM: Spin-label study of phenothiazine interactions with erythrocyte ghost membranes: a possible membrane-mediated antisickling action. J Pharmacol Exp Ther. 1978 Oct;207(1):203-11. Pubmed
Tam SW, Cook L: Sigma opiates and certain antipsychotic drugs mutually inhibit (+)-[3H] SKF 10,047 and [3H]haloperidol binding in guinea pig brain membranes. Proc Natl Acad Sci U S A. 1984 Sep;81(17):5618-21. Pubmed

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 disorganized and psychotic thinking. Also used to help treat false perceptions (e.g. hallucinations or delusions.)
Pharmacodynamics	Acetophenzine is a phenothiazine antipsychotic intended for the management of schizophrenia and other psychotic disorders.
Mechanism of action	Acetophenazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.
Absorption	Not Available
Volume of distribution	Not Available
Protein binding	Not Available
Metabolism	Not Available
Route of elimination	Not Available
Half life	Not Available
Clearance	Not Available
Toxicity	Not Available
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
logP	2.62	SANGSTER (1994)

Predicted Properties

Property	Value	Source
water solubility	6.01e-02 g/l	ALOGPS
logP	3.48	ALOGPS
logP	2.65	ChemAxon
logS	-3.8	ALOGPS
pKa (strongest acidic)	15.46	ChemAxon
pKa (strongest basic)	8.07	ChemAxon
physiological charge	1	ChemAxon
hydrogen acceptor count	5	ChemAxon
hydrogen donor count	1	ChemAxon
polar surface area	47.02	ChemAxon
rotatable bond count	7	ChemAxon
refractivity	121.7	ChemAxon
polarizability	46.68	ChemAxon

药物相互作用

Drug	Interaction
Bromocriptine	The phenothiazine decreases the effect of bromocriptine
Cisapride	Increased risk of cardiotoxicity and arrhythmias
Dexfenfluramine	Decreased anorexic effect, may increase psychotic symptoms
Diethylpropion	Decreased anorexic effect, may increase psychotic symptoms
Fenfluramine	Decreased anorexic effect, may increase psychotic symptoms
Guanethidine	Acetophenazine may decrease the effect of guanethidine.
Mazindol	Decreased anorexic effect, may increase psychotic symptoms
Phentermine	Decreased anorexic effect, may increase psychotic symptoms
Phenylpropanolamine	Decreased anorexic effect, may increase psychotic symptoms
Tacrine	The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Acetophenazine, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents.
Terfenadine	Increased risk of cardiotoxicity and arrhythmias
Tetrabenazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects. Similar pharmacologic properties thus combination therapy will worsen the severity of sedative, parkinsonian, and extrapyramidal adverse effects.
Trimethobenzamide	Trimethobenzamide and Acetophenazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine	The antihistamine, Triprolidine, may increase the arrhythmogenic effect of the phenothiazine, Acetophenazine. Monitor for symptoms of ventricular arrhythmias. Additive anticholinergic and CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
Trospium	Trospium and Acetophenazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.

食物相互作用

Not Available

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