Paludrine
Paludrine - General Information
Paludrine 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.
Pharmacology of Paludrine
Paludrine is a biguanide derivative that is converted to an active metabolite called cycloguanil pamoate. 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.
Additional information about Paludrine
Paludrine 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.
Mechanism Of Action: Paludrine 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Proguanil
Synonyms: Not Available
Drug Category: Antimetabolites; Antimalarials
Drug Type: Small Molecule; Approved
Other Brand Names containing Proguanil: Chloroguanide; Paludrine;
Absorption: Rapidly and well absorbed in humans following oral doses ranging from 50 to 500 mg.
Toxicity (Overdose): Not Available
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
Dosage Forms of Paludrine: Not Available
Chemical IUPAC Name: 1-[amino-[(4-chlorophenyl)amino]methylidene]-2-propan-2-ylguanidine
Chemical Formula: C11H16ClN5
Proguanil on Wikipedia: https://en.wikipedia.org/wiki/Proguanil
Organisms Affected: Plasmodium
