Correlation Engine 2.0
Clear Search sequence regions
Bookmark Forward

QuickView for proguanil (compound)


PubChem
Name: Proguanil
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
DrugBank
Identification
Name: Proguanil
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
Pharmacology
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.
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...
show more »
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
Interactions
Food interaction:
Take with food.
Drug interaction:
LumefantrineProguanil may increase the adverse effects of lumefantrine. Combination therapy is contraindicated unless there are no other treatment options.
ArtemetherProguanil may increase the adverse effects of artemether. Combination therapy is contraindicated unless there are no other treatment options.

Targets


Enzymes