药品详细
Proguanil(氯胍)
化学结构式图
中文名
氯胍
英文名
Proguanil
分子式
C11H16ClN5
化学名
(E)-1-({amino[(4-chlorophenyl)amino]methylidene}amino)-N'-(propan-2-yl)methenimidamide
分子量
Average: 253.731
Monoisotopic: 253.109423244
Monoisotopic: 253.109423244
CAS号
500-92-5
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
Proguanil is a prophylactic antimalarial drug, which works by stopping the malaria parasite, Plasmodium falciparum and Plasmodium vivax, from reproducing once it is in the red blood cells. It does this by inhibiting the enzyme, dihydrofolate reductase, which is involved in the reproduction of the parasite.
生产厂家
封装厂家
- A-S Medication Solutions LLC
- GlaxoSmithKline Inc.
- St Mary's Medical Park Pharmacy
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 causal prevention and suppression of malaria caused by susceptible strains of P. falciparum and other species of Plasmodium found in some geographical areas of the world. | ||||||||
| Pharmacodynamics | Proguanil is a biguanide derivative that is converted to an active metabolite called cycloguanil. It exerts its antimalarial action by inhibiting parasitic dihydrofolate reductase enzyme. It has causal prophylactic and suppressive activity against P. falciparum and cures the acute infection. It is also effective in suppressing the clinical attacks of vivax malaria. However it is slower compared to 4-aminoquinolines. | ||||||||
| Mechanism of action | Proguanil inhibits the dihydrofolate reductase of plasmodia and thereby blocks the biosynthesis of purines and pyrimidines, which are essential for DNA synthesis and cell multiplication. This leads to failure of nuclear division at the time of schizont formation in erythrocytes and liver. | ||||||||
| Absorption | Rapidly and well absorbed in humans following oral doses ranging from 50 to 500 mg. | ||||||||
| Volume of distribution | Not Available | ||||||||
| Protein binding | Approximately 75% | ||||||||
| Metabolism |
Variably metabolized in the liver by cytochrome P450 isoenzymes to the active triazine metabolite, cycloguanil. This variable metabolism of proguanil may have profound clinical importance in poor metabolizers such as the Asian and African populations at risk for malaria infection. Prophylaxis with proguanil may not be effective in these persons because they may not achieve adequate therapeutic levels of the active compound, cycloguanil, even after multiple doses.
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 | Approximately 20 hours | ||||||||
| Clearance | Not Available | ||||||||
| Toxicity | Not Available | ||||||||
| 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 |
|---|---|
| Artemether | Proguanil may increase the adverse effects of artemether. Combination therapy is contraindicated unless there are no other treatment options. |
| Lumefantrine | Proguanil may increase the adverse effects of lumefantrine. Combination therapy is contraindicated unless there are no other treatment options. |
食物相互作用
- Take with food.
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