药品详细
Triflupromazine(三氟丙嗪)
化学结构式图
中文名
三氟丙嗪
英文名
Triflupromazine
分子式
C18H19F3N2S
化学名
dimethyl({3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl})amine
分子量
Average: 352.417
Monoisotopic: 352.122103923
Monoisotopic: 352.122103923
CAS号
146-54-3
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
A phenothiazine used as an antipsychotic agent and as an antiemetic. [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 |
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| Substructures |
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适应症
药理
| Indication | Used mainly in the management of psychoses. Also used to control nausea and vomiting. |
| Pharmacodynamics | Triflupromazine is a member of a class of drugs called phenthiazines, which are dopamine D1/D2 receptor antagonists. Phenothiazines are used to treat serious mental and emotional disorders, including schizophrenia and other psychotic disorders. It reduces anxiety, emotional withdrawal, hallucinations, disorganized thoughts, blunted mood, and suspiciousness. Triflupromazine is used particularly to control violent behavior during acute episodes of psychotic disorders. It can also be used to control severe nausea and vomiting, severe hiccups, and moderate to severe pain in some hospitalized patients. Triflupromazine acts on the central nervous system. |
| Mechanism of action | Triflupromazine binds to the dopamine D1 and dopamine D2 receptors and inhibits their activity. The mechanism of the anti-emetic effect is due predominantly to blockage of the dopamine D2 neurotransmitter receptors in the chemoreceptor trigger zone (CTZ) and vomiting centre. Triflupromazine blocks the neurotransmitter dopamine and the vagus nerve in the gastrointestinal tract. Triflupromazine also binds the muscarinic acetylcholine receptors (M1 and M2) and the tryptamine D receptors (5HT2B). |
| Absorption | Absorption may be erratic and peak plasma concentrations show large interindividual differences. |
| Volume of distribution | Not Available |
| Protein binding | Very high (90% or more). |
| Metabolism |
Hepatic.
|
| Route of elimination | Not Available |
| Half life | Not Available |
| Clearance | Not Available |
| Toxicity | Symptoms of overdose include agitation, coma, convulsions, difficulty breathing, difficulty swallowing, dry mouth, extreme sleepiness, fever, intestinal blockage, irregular heart rate, low blood pressure, and restlessness. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| State | solid | |||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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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 |
| Donepezil | Possible antagonism of action |
| Fenfluramine | Decreased anorexic effect, may increase psychotic symptoms |
| Galantamine | Possible antagonism of action |
| Gatifloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Grepafloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Guanethidine | Triflupromazine may decrease the effect of guanethidine. |
| Levofloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Mazindol | Decreased anorexic effect, may increase psychotic symptoms |
| Phentermine | Decreased anorexic effect, may increase psychotic symptoms |
| Phenylpropanolamine | Decreased anorexic effect, may increase psychotic symptoms |
| Terfenadine | Increased risk of cardiotoxicity and arrhythmias |
食物相互作用
Not Available
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