药品详细
Trimeprazine(异丁嗪)
化学结构式图
中文名
异丁嗪
英文名
Trimeprazine
分子式
C18H22N2S
化学名
dimethyl[2-methyl-3-(10H-phenothiazin-10-yl)propyl]amine
分子量
Average: 298.446
Monoisotopic: 298.150369404
Monoisotopic: 298.150369404
CAS号
84-96-8
ATC分类
D04A 未知;R06A 未知;R06A 未知;R06A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A phenothiazine derivative that is used as an antipruritic. [PubChem]
生产厂家
- Allergan herbert skin care div allergan inc
- Alpharma us pharmaceuticals division
- Morton grove pharmaceuticals 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 |
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| Substructures |
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适应症
药理
| Indication | Used to prevent and relieve allergic conditions which cause pruritus (itching) and urticaria (some allergic skin reactions). |
| Pharmacodynamics | Trimeprazine (also known as Alimemazine) is a tricyclic antihistamine, similar in structure to the phenothiazine antipsychotics, but differing in the ring-substitution and chain characteristics. Trimeprazine is in the same class of drugs as chlorpromazine (Thorazine) and trifluoperazine (Stelazine); however, unlike the other drugs in this class, trimeprazine is not used clinically as an anti-psychotic. It acts as an anti-histamine, a sedative, and an anti-emetic (anti-nausea). Trimeprazine is used principally as an anti-emetic, to prevent motion sickness or as an anti-histamine in combination with other medications in cough and cold preparations. Tricyclic antihistamines are also structurally-related to the tricyclic antidepressants, explaining the antihistaminergic adverse effects of these two drug classes and also the poor tolerability profile of tricyclic H1-antihistamines. |
| Mechanism of action | Trimeprazine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. |
| Absorption | Well absorbed in the digestive tract. |
| Volume of distribution | Not Available |
| Protein binding | Not Available |
| Metabolism |
Hepatic
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| Route of elimination | Not Available |
| Half life | Not Available |
| Clearance | Not Available |
| Toxicity | Symptoms of overdose clumsiness or unsteadiness, seizures, severe drowsiness, flushing or redness of face, hallucinations, muscle spasms (especially of neck and back), restlessness, shortness of breath, shuffling walk, tic-like (jerky) movements of head and face, trembling and shaking of hands, and insomnia. |
| 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 |
| Guanethidine | Trimeprazine 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 |
| Pramlintide | The anticholinergic effects of Trimeprazine may be enhanced by Pramlintide. Additive effects of reduced GI motility may occur. Pramlintide slows gastic emptying and should not be used with drugs that alter GI motility (e.g. anticholinergics). Consider alternative treatments or use caution during concomitant therapy. |
| Tacrine | The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Trimeprazine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents. |
| Terfenadine | Increased risk of cardiotoxicity and arrhythmias |
| Trimethobenzamide | Trimethobenzamide and Trimeprazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects. |
| Triprolidine | Triprolidine and Trimeprazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects. |
| Trospium | Trospium and Trimeprazine, 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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