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药品详细

Thioproperazine(Thioproperazine)

化学结构式图
中文名
Thioproperazine
英文名
Thioproperazine
分子式
C22H30N4O2S2
化学名
N,N-dimethyl-10-[3-(4-methylpiperazin-1-yl)propyl]-10H-phenothiazine-2-sulfonamide
分子量
Average: 446.629
Monoisotopic: 446.181017604
CAS号
316-81-4
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

Thioproperazine is a potent neuroleptic with antipsychotic properties. Thioproperazine has a marked cataleptic and antiapomorphine activity associated with relatively slight sedative, hypothermic and spasmolytic effects. It is virtually without antiserotonin and hypotensive action and has no antihistaminic property. It is used for the treatment of all types of acute and chronic schizophrenia, including those which did not respond to the usual neuroleptics; manic syndromes.
Overdosage may result in severe extrapyramidal symptoms with dysphagia, marked sialorrhea, persistent and rapidly increasing hyperthermia, pulmonary syndrome, state of shock with pallor and profuse sweating, which may be followed by collapse and coma. LD50 in mice is 70 mg/kg I.V., 120 mg/kg I.P., 500 mg/kg S.C. and 830 mg/kg P.O.

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    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
    • Sulfonyls
    • Piperazines
    • Thiazines
    • Benzene and Derivatives
    • Benzenesulfonamides
    • Heterocyclic compounds
    • Aromatic compounds
    • Sulfanilamides
    • Sulfonamides
    • Anilines
    适应症
    药理
    Indication For the treatment of all types of acute and chronic schizophrenia, including those which did not respond to the usual neuroleptics; manic syndromes.
    Pharmacodynamics Thioproperazine is a potent neuroleptic with antipsychotic properties. Thioproperazine has a marked cataleptic and antiapomorphine activity associated with relatively slight sedative, hypothermic and spasmolytic effects. It is virtually without antiserotonin and hypotensive action and has no antihistaminic property.
    Mechanism of action Thioproperazine 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 Not Available
    Clearance Not Available
    Toxicity Overdosage may result in severe extrapyramidal symptoms with dysphagia, marked sialorrhea, persistent and rapidly increasing hyperthermia, pulmonary syndrome, state of shock with pallor and profuse sweating, which may be followed by collapse and coma. LD50 in mice is 70 mg/kg I.V., 120 mg/kg I.P., 500 mg/kg S.C. and 830 mg/kg P.O.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 140 °C PhysProp
    Predicted Properties
    Property Value Source
    water solubility 5.69e-02 g/l ALOGPS
    logP 3.09 ALOGPS
    logP 2.83 ChemAxon
    logS -3.9 ALOGPS
    pKa (strongest basic) 8.36 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 5 ChemAxon
    hydrogen donor count 0 ChemAxon
    polar surface area 47.1 ChemAxon
    rotatable bond count 5 ChemAxon
    refractivity 126.95 ChemAxon
    polarizability 49.62 ChemAxon
    药物相互作用
    Drug Interaction
    Donepezil Possible antagonism of action
    Galantamine Possible antagonism of action
    Rivastigmine Possible antagonism of action
    食物相互作用
    • Avoid alcohol
    • Take with food to avoid irritation

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