药品详细
Prochlorperazine(丙氯拉嗪)
化学结构式图
中文名
丙氯拉嗪
英文名
Prochlorperazine
分子式
C20H24ClN3S
化学名
2-chloro-10-[3-(4-methylpiperazin-1-yl)propyl]-10H-phenothiazine
分子量
Average: 373.943
Monoisotopic: 373.13794618
Monoisotopic: 373.13794618
CAS号
58-38-8
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 antipsychotic used principally in the treatment of nausea; vomiting; and vertigo. It is more likely than chlorpromazine to cause extrapyramidal disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612)
生产厂家
- Able laboratories inc
- Alpharma us pharmaceuticals division
- Baxter healthcare corp anesthesia and critical care
- Bedford laboratories div ben venue laboratories inc
- Cadista pharmaceuticals inc
- Duramed pharmaceuticals inc sub barr laboratories inc
- G and w laboratories inc
- Glaxosmithkline
- Hospira inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Marsam pharmaceuticals llc
- Morton grove pharmaceuticals inc
- Mylan pharmaceuticals inc
- Paddock laboratories inc
- Sandoz inc
- Smith and nephew solopak div smith and nephew
- Teva parenteral medicines inc
- Teva pharmaceuticals usa
- Watson laboratories inc
- Wyeth ayerst laboratories
封装厂家
- Apotheca Inc.
- A-S Medication Solutions LLC
- Barr Pharmaceuticals
- Baxter International Inc.
- Bedford Labs
- Ben Venue Laboratories Inc.
- Bryant Ranch Prepack
- Cadista Pharmaceuticals Inc.
- Cardinal Health
- Comprehensive Consultant Services Inc.
- Corepharma LLC
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- G & W Labs
- General Injectables and Vaccines Inc.
- H.J. Harkins Co. Inc.
- Heartland Repack Services LLC
- Hospira Inc.
- Ivax Pharmaceuticals
- Kaiser Foundation Hospital
- Liberty Pharmaceuticals
- Medisca Inc.
- Medvantx Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Nucare Pharmaceuticals Inc.
- Paddock Labs
- Palmetto Pharmaceuticals Inc.
- Par Pharmaceuticals
- Patient First Corp.
- PCA LLC
- PD-Rx Pharmaceuticals Inc.
- Pharma Pac LLC
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmedix
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Prescript Pharmaceuticals
- Rebel Distributors Corp.
- Redpharm Drug
- Remedy Repack
- Sandhills Packaging Inc.
- Sandoz
- Southwood Pharmaceuticals
- Stat Rx Usa
- Teva Pharmaceutical Industries Ltd.
- UDL Laboratories
- Vangard Labs Inc.
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 symptomatic management of psychotic disorders, short term management of nonpsychotic anxiety in patients with generalized anxiety disorder, and for the control of severe nausea and vomiting of various causes. |
| Pharmacodynamics | Prochlorperazine is a piperazine phenothiazine related to high-potency neuroleptics such as perphenazine. It shares many of the actions and adverse effects of the antipsychotics. |
| Mechanism of action | The mechanism of action of prochlorperazine has not been fully determined, but may be primarily related to its antidopaminergic effects. Prochlorperazine blocks the D2 somatodendritic autoreceptor, resulting in the blockade of postsynaptic dopamine receptors in the mesolimbic system and an increased dopamine turnover. Prochlorperazine also has anti-emetic effects, which can be attributed to dopamine blockade in the chemoreceptor trigger zone. Prochlorperazine also blocks anticholinergic and alpha-adrenergic receptors, the blockade of alpha(1)-adrenergic receptors resulting in sedation, muscle relaxation, and hypotension. |
| Absorption | Rapidly absorbed following oral administration |
| Volume of distribution | Not Available |
| Protein binding | 91-99% |
| Metabolism |
Hepatic. Undergoes metabolism in the gastric mucosa and on first pass through the liver, CYP2D6 and/or CYP3A4.
|
| Route of elimination | Not Available |
| Half life | 6 to 8 hours |
| Clearance | Not Available |
| Toxicity | Symptoms of central nervous system depression to the point of somnolence or coma. Agitation and restlessness may also occur. Other possible manifestations include convulsions, EKG changes and cardiac arrhythmias, fever and autonomic reactions such as hypotension, dry mouth and ileus; LD50=400mg/kg (orally in mice) |
| 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 pyschotic 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 pyschotic 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 | Prochlorperazine 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 pyschotic symptoms |
| Metrizamide | Increased risk of convulsions |
| Phendimetrazine | Decreased anorexic effect, may increase pyschotic symptoms |
| Phenmetrazine | Decreased anorexic effect, may increase pyschotic 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, Prochlorperazine, 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. |
| Trimethobenzamide | Trimethobenzamide and Prochlorperazine, 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, Prochlorperazine. 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 Prochlorperazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects. |
食物相互作用
- Avoid alcohol.
- Take with a full glass of water Avoid excessive quantities of coffee or tea (Caffeine).
- Take with food.
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