药品详细
Trifluoperazine(三氟拉嗪)
化学结构式图
中文名
三氟拉嗪
英文名
Trifluoperazine
分子式
C21H24F3N3S
化学名
10-[3-(4-methylpiperazin-1-yl)propyl]-2-(trifluoromethyl)-10H-phenothiazine
分子量
Average: 407.496
Monoisotopic: 407.164303088
Monoisotopic: 407.164303088
CAS号
117-89-5
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 with actions similar to chlorpromazine. It is used as an antipsychotic and an antiemetic. [PubChem]
生产厂家
- Duramed pharmaceuticals inc sub barr laboratories inc
- Glaxosmithkline
- Ivax pharmaceuticals inc
- Mylan pharmaceuticals inc
- Sandoz inc
- Watson laboratories inc
- Wockhardt eu operations (swiss) ag
封装厂家
- Apotheca Inc.
- Comprehensive Consultant Services Inc.
- Heartland Repack Services LLC
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Nucare Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Remedy Repack
- Sandhills Packaging Inc.
- Sandoz
- Stat Rx Usa
- UDL Laboratories
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 | For the treatment of anxiety disorders, depressive symptoms secondary to anxiety and agitation. |
| Pharmacodynamics | Trifluoperazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Trifluoperazine has not been shown effective in the management of behaviorial complications in patients with mental retardation. |
| Mechanism of action | Trifluoperazine 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 |
Hepatic.
|
| Route of elimination | Not Available |
| Half life | 10-20 hours |
| 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 |
|---|---|
| Amphetamine | Decreased anorexic effect, may increase psychotic symptoms |
| Benzphetamine | Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines. |
| Bromocriptine | The phenothiazine decreases the effect of bromocriptine |
| Cisapride | Increased risk of cardiotoxicity and arrhythmias |
| Dexfenfluramine | Decreased anorexic effect, may increase psychotic symptoms |
| Dextroamphetamine | 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 | Trifluoperazine may decrease the effect of guanethidine. |
| Levofloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Mazindol | Decreased anorexic effect, may increase psychotic symptoms |
| Methamphetamine | Decreased anorexic effect, may increase psychotic symptoms |
| Metrizamide | Increased risk of convulsions |
| Phendimetrazine | Decreased anorexic effect, may increase psychotic symptoms |
| Phenmetrazine | Decreased anorexic effect, may increase psychotic symptoms |
| Phentermine | Decreased anorexic effect, may increase psychotic symptoms |
| Phenylpropanolamine | Decreased anorexic effect, may increase psychotic symptoms |
| Rivastigmine | Possible antagonism of action |
| Sparfloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Tacrine | The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Trifluoperazine, 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. |
| Thiabendazole | The strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Trifluoperazine by decreasing Trifluoperazine metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Trifluoperazine if Thiabendazole is initiated, discontinued or dose changed. |
| Trimethobenzamide | Trimethobenzamide and Trifluoperazine, 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, Trifluoperazine. 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 Trifluoperazine, 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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