药品详细
Chlorpheniramine(扑尔敏)
化学结构式图
中文名
扑尔敏
英文名
Chlorpheniramine
分子式
C16H19ClN2
化学名
[3-(4-chlorophenyl)-3-(pyridin-2-yl)propyl]dimethylamine
分子量
Average: 274.788
Monoisotopic: 274.123676325
Monoisotopic: 274.123676325
CAS号
132-22-9
ATC分类
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 histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than promethazine. [PubChem]
生产厂家
- Alza corp
- Anabolic inc
- Avanthi inc
- Bayer pharmaceuticals corp
- Bel mar laboratories inc
- Bell pharmacal corp
- Elkins sinn div ah robins co inc
- Glaxosmithkline
- Halsey drug co inc
- Impax laboratories inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Kv pharmaceutical co
- Lannett co inc
- Lederle laboratories div american cyanamid co
- Mutual pharmaceutical co inc
- Newtron pharmaceuticals inc
- Panray corp sub ormont drug and chemical co inc
- Pharmaceutical assoc inc div beach products
- Pharmavite pharmaceuticals
- Pharmeral inc
- Pioneer pharmaceuticals inc
- Pliva inc
- Private formulations inc
- Purepac pharmaceutical co
- Roxane laboratories inc
- Sandoz inc
- Schering corp sub schering plough corp
- Schering plough healthcare products inc
- Vitarine pharmaceuticals inc
- Watson laboratories inc
- West ward pharmaceutical corp
- Wockhardt eu operations (swiss) ag
封装厂家
- Amend
- Anip Acquisition Co.
- A-S Medication Solutions LLC
- Breckenridge Pharmaceuticals
- C.O. Truxton Inc.
- Cardinal Health
- Consolidated Midland Corp.
- Contract Pharm
- Cypress Pharmaceutical Inc.
- Deltex Pharmaceuticals Inc.
- Direct Dispensing Inc.
- Dispensing Solutions
- Edwards Pharmaceuticals
- Hi Tech Pharmacal Co. Inc.
- Iopharm Laboratories Inc.
- Ivax Pharmaceuticals
- Kowa Pharmaceuticals America Inc.
- Kraft Pharmaceutical Co. Inc.
- Larken Laboratories Inc.
- Liberty Pharmaceuticals
- Magna Pharmaceuticals
- Major Pharmaceuticals
- Mallinckrodt Inc.
- McNeil Laboratories
- Meda AB
- Misemer Pharmaceuticals Inc.
- Mismer Pharmace
- Nucare Pharmaceuticals Inc.
- PD-Rx Pharmaceuticals Inc.
- Pecos Pharmaceutical Inc.
- Perrigo Co.
- Physicians Total Care Inc.
- Prepackage Specialists
- Provident Pharmaceuticals LLC
- Qualitest
- Rico Pharmacal
- River's Edge Pharmaceuticals
- Rugby Laboratories
- S&P Healthcare
- Schering-Plough Inc.
- Time-Cap Labs
- Tya Pharmaceuticals
- Watson Pharmaceuticals
- Wockhardt Ltd.
参考
| Synthesis Reference | Not Available |
| General Reference |
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 rhinitis, urticaria, allergy, common cold, asthma and hay fever. |
| Pharmacodynamics | In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Chlorpheniramine, is a histamine H1 antagonist (or more correctly, an inverse histamine agonist) of the alkylamine class. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies. |
| Mechanism of action | Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. |
| Absorption | Well absorbed in the gastrointestinal tract. |
| Volume of distribution | Not Available |
| Protein binding | 72% |
| Metabolism |
Primarily hepatic via Cytochrome P450 (CYP450) enzymes.
|
| Route of elimination | Not Available |
| Half life | 21-27 hours |
| Clearance | Not Available |
| Toxicity | Oral LD50 (rat): 306 mg/kg; Oral LD50 (mice): 130 mg/kg; Oral LD50 (guinea pig): 198 mg/kg [Registry of Toxic Effects of Chemical Substances. Ed. D. Sweet, US Dept. of Health & Human Services: Cincinatti, 2010.] Also a mild reproductive toxin to women of childbearing age. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| State | liquid | |||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Donepezil | Possible antagonism of action |
| Ethotoin | The antihistamine increases the effect of hydantoin |
| Fosphenytoin | The antihistamine increases the effect of hydantoin |
| Galantamine | Possible antagonism of action |
| Mephenytoin | The antihistamine increases the effect of hydantoin |
| Phenytoin | The antihistamine increases the effect of hydantoin |
| Rivastigmine | Possible antagonism of action |
| Tacrine | The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Chlorpheniramine, 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. |
| Telithromycin | Telithromycin may reduce clearance of Chlorpheniramine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Chlorpheniramine if Telithromycin is initiated, discontinued or dose changed. |
| Trimethobenzamide | Trimethobenzamide and Chlorpheniramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects. |
| Triprolidine | Triprolidine and Chlorpheniramine, 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 Chlorpheniramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects. |
| Voriconazole | Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of chlorpheniramine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of chlorpheniramine if voriconazole is initiated, discontinued or dose changed. |
食物相互作用
- Avoid alcohol.
- Take with food.
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