Name: | Proguanil |
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PubChem Compound ID: | 4923 |
Description: | A biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent. |
Molecular formula: | C11H16ClN5 |
Molecular weight: | 253.731 g/mol |
Name: | Proguanil |
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Name (isomeric): | DB01131 |
Drug Type: | small molecule |
Description: | A biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent. |
Brand: | Paludrine, Chloroguanide |
Category: | Antimetabolites, Antimalarials |
CAS number: | 500-92-5 |
Indication: | For the causal prevention and suppression of malaria caused by susceptible strains of <i>P. falciparum</i> and other species of Plasmodium found in some geographical areas of the world. |
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Pharmacology: |
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 a...
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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. |
Protein binding: | Approximately 75% |
Biotransformation: | 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. |
Half Life: | Approximately 20 hours |
Affected organisms: | Plasmodium |
Food interaction: |
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