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药品详细

Chlorprothixene(氯普噻吨)

化学结构式图
中文名
氯普噻吨
英文名
Chlorprothixene
分子式
C18H18ClNS
化学名
[3-(2-chloro-9H-thioxanthen-9-ylidene)propyl]dimethylamine
分子量
Average: 315.86
Monoisotopic: 315.084847978
CAS号
113-59-7
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

Chlorprothixene is a typical antipsychotic drug of the thioxanthene (tricyclic) class. Chlorprothixene exerts strong blocking effects by blocking the 5-HT2 D1, D2, D3, histamine H1, muscarinic and alpha1 adrenergic receptors.

生产厂家
  • Hoffmann la roche inc
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 Not Available
Substructures Not Available
适应症
药理
Indication For treatment of psychotic disorders (e.g. schizophrenia) and of acute mania occuring as part of bipolar disorders.
Pharmacodynamics Chlorprothixene is a typical antipsychotic drug of the thioxanthine class. It has a low antipsychotic potency (half to 2/3 of chlorpromazine). An intrinsic antidepressant effect of chlorprothixene has been discussed, but not proven yet. Likewise, it is unclear, if chlorprothixene has genuine analgesic effects. An antiemetic effect, as with most antipsychotics, exists. It is used in the treatment of nervous, mental, and emotional conditions. Improvement in such conditions is thought to result from the effect of the medicine on nerve pathways in specific areas of the brain. Chlorprothixene has a strong sedative activity with a high incidence of anticholinergic side-effects. Chlorprothixene is structurally related to chlorpromazine, with which it shares in principal all side effects. Allergic side-effects and liver damage seem to appear with an appreciable lower frequency.
Mechanism of action Chlorprothixene 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 Incomplete bioavailability.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Hepatic
Route of elimination Not Available
Half life 8 to 12 hours
Clearance Not Available
Toxicity Symptoms of overdose include difficulty in breathing (severe), dizziness (severe), drowsiness (severe), muscle trembling, jerking, stiffness, or uncontrolled movements (severe), small pupils, unusual excitement, and unusual tiredness or weakness (severe).
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 97.5 °C PhysProp
water solubility 0.295 mg/L Not Available
logP 5.18 HANSCH,C ET AL. (1995)
Predicted Properties
Property Value Source
water solubility 3.66e-04 g/l ALOGPS
logP 5.42 ALOGPS
logP 5.07 ChemAxon
logS -5.9 ALOGPS
pKa (strongest basic) 9.76 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 1 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 3.24 ChemAxon
rotatable bond count 3 ChemAxon
refractivity 104.66 ChemAxon
polarizability 35.85 ChemAxon
药物相互作用
Drug Interaction
Donepezil Possible antagonism of action
Galantamine Possible antagonism of action
Guanethidine Chlorprothixene may decrease the effect of guanethidine.
Rivastigmine Possible antagonism of action
食物相互作用
  • Avoid alcohol.
  • Take with food to reduce irritation.

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