Proguanil
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| Systematic (IUPAC) name | |
| 1-(4-chlorophenyl)-2-(N'-propan-2-ylcarbamimidoyl) guanidine | |
| Clinical data | |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
| Pregnancy cat. | ? |
| Legal status | ? |
| Routes | Oral |
| Pharmacokinetic data | |
| Half-life | ~20 h |
| Identifiers | |
| CAS number | 500-92-5  |
| ATC code | P01BB01 |
| PubChem | CID 4923 |
| DrugBank | APRD00188 |
| ChemSpider | 4754 |
| UNII | S61K3P7B2V |
| KEGG | D08428 |
| ChEBI | CHEBI:8455 |
| ChEMBL | CHEMBL1377 |
| Chemical data | |
| Formula | C11H16ClN5 |
| Mol. mass | 253.731 g/mol |
| SMILES | eMolecules & PubChem |
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Proguanil (chlorguanide, chloroguanide) is a prophylactic antimalarial drug. When taken it is converted to the active metabolite cycloguanil.
Proguanil is effective against sporozoites.
Proguanil hydrochloride is marketed as Paludrine by AstraZeneca.
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[edit] Mechanism
It works by stopping the malaria parasites, Plasmodium falciparum and Plasmodium vivax, from reproducing once they are inside red blood cells.
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.
[edit] Combinations
Proguanil is usually taken in combination with another anti-malarial drug such as atovaquone[1] (e.g., in the drug Malarone) or chloroquine.[2]
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)
[edit] Precautions
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.[citation needed] These may come on gradually and may not be immediately attributable to anything in particular.
[edit] References
- ^ 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.
[edit] External links
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