药品详细
Amodiaquine(阿莫地喹)
化学结构式图
中文名
阿莫地喹
英文名
Amodiaquine
分子式
C20H22ClN3O
化学名
4-[(7-chloroquinolin-4-yl)amino]-2-[(diethylamino)methyl]phenol
分子量
Average: 355.861
Monoisotopic: 355.145140048
Monoisotopic: 355.145140048
CAS号
86-42-0
ATC分类
P01B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A 4-aminoquinoquinoline compound with anti-inflammatory properties. [PubChem]
生产厂家
- Parke davis div warner lambert co
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference |
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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 treatment of acute malarial attacks in non-immune subjects. | ||||||||
| Pharmacodynamics | Amodiaquine, a 4-aminoquinoline similar to chloroquine in structure and activity, has been used as both an antimalarial and an anti-inflammatory agent for more than 40 years. Amodiaquine is at least as effective as chloroquine, and is effective against some chloroquine-resistant strains, although resistance to amodiaquine has been reported. The mode of action of amodiaquine has not yet been determined. 4-Aminoquinolines depress cardiac muscle, impair cardiac conductivity, and produce vasodilatation with resultant hypotension. They depress respiration and cause diplopia, dizziness and nausea. | ||||||||
| Mechanism of action | The mechanism of plasmodicidal action of amodiaquine is not completely certain. Like other quinoline derivatives, it is thought to inhibit heme polymerase activity. This results in accumulation of free heme, which is toxic to the parasites. The drug binds the free heme preventing the parasite from converting it to a form less toxic. This drug-heme complex is toxic and disrupts membrane function. | ||||||||
| Absorption | Rapidly absorbed following oral administration. | ||||||||
| Volume of distribution | Not Available | ||||||||
| Protein binding | Not Available | ||||||||
| Metabolism |
Hepatic biotransformation to desethylamodiaquine (the principal biologically active metabolite) is the predominant route of amodiaquine clearance with such a considerable first pass effect that very little orally administered amodiaquine escapes untransformed into the systemic circulation.
Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.
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| Route of elimination | Not Available | ||||||||
| Half life | 5.2 ± 1.7 (range 0.4 to 5.5) minutes | ||||||||
| Clearance | Not Available | ||||||||
| Toxicity | LD50 (mouse, intraperitoneal) 225 mg/kg, LD50 (mouse, oral) 550 mg/kg. Symptoms of overdose include headache, drowsiness, visual disturbances, vomiting, hypokalaemia, cardiovascular collapse and cardiac and respiratory arrest. Hypotension, if not treated, may progress rapidly to shock. Electrocardiograms (ECG) may reveal atrial standstill, nodal rhythm, prolonged intraventricular conduction time, broadening of the QRS complex, and progressive bradycardia leading to ventricular fibrillation and/or arrest. | ||||||||
| 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
食物相互作用
Not Available
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