Proguanil Systematic (IUPAC) name 1-(4-chlorophenyl)-2-(N'-propan-2-ylcarbamimidoyl) guanidine Clinical data AHFS/Drugs.com Pregnancy cat. ? Legal status ? Routes Oral Pharmacokinetic data Half-life ~20 h Identifiers CAS number ATC code P01 PubChem DrugBank ChemSpider UNII KEGG ChEBI ChEMBL Chemical data Formula C11H16ClN5 Mol. mass 253.731 g/mol SMILES & (what is this?)
Proguanil (chlorguanide, chloroguanide) is a prophylactic antimalarial drug.
Proguanil is effective against sporozoites.
Proguanil hydrochloride is marketed as Paludrine by AstraZeneca.
It does this by inhibiting the enzyme dihydrofolate reductase, which catalyzes the formation of tetrahydrofolate, the main one carbon unit carrier in our body, required for dTMP and purine base synthesis.
Malarone has fewer side effects than mefloquine, but can be more expensive because it is taken daily.
Proguanil is taken with atovaquone for chloroquine-resistant and multidrug resistant strains of P. falciparum and P. vivax. Proguanil combined with atovaquone is sold under the tradename Malarone (GlaxoSmithKline)
General precaution regarding Proguanil involves watching out for feelings of sullenness and anxiety to a level that is outside the ordinary, when taking over a period of several months. These may come on gradually and may not be immediately attributable to anything in particular.
- ^ Sutherland CJ, Laundy M, Price N, et al. (November 2008). "Mutations in the Plasmodium falciparum cytochrome b gene are associated with delayed parasite recrudescence in malaria patients treated with atovaquone-proguanill". Malar. J. 7 (1): 240. doi:10.1186/1475-2875-7-240. PMC 2640403. PMID 19021900. http://www.malariajournal.com/content/7/1/240.
- ^ Payen C, Monnin L, Pulce C, Descotes J (December 2008). "Bone marrow aplasia following acute poisoning with chloroquine-proguanil". Clin Toxicol (Phila) 46 (10): 1085–7. doi:10.1080/15563650601182925. PMID 19065311. http://www.informaworld.com/openurl?genre=article&doi=10.1080/15563650601182925&magic=pubmed%7C%7C1B69BA326FFE69C3F0A8F227DF8201D0.
Antiparasitics – antiprotozoal agents – Chromalveolate antiparasitics (P01) Alveo-
(antifols)Sulfadoxine • sulfamethoxypyrazineCoformulationFansidar# (sulfadoxine/pyrimethamine)OtherCombi-
nationsFixed-dose (coformulated) ACTsOther combinations
(not co-formulated)artesunate/SP • artesunate/mefloquine •
quinine/tetracycline • quinine/doxycycline • quinine/clindamycin
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