ABSTRACT
Base: MW 254; hydrochloride: MW 290; pKa: 2.3,10.4.1 g of the salt dissolves in 110 ml of water. The drug should be protected from light.
Pharmacology and mechanism of action
Proguanil (PG) was introduced as a prophylactic agent against malaria just after the Second World War. It is a pyrimidine derivative which is highly active against pre-erythrocytic forms of Plasmodium (P) falciparum making it suitable for casual prophylaxis. It is also effective in the erythrocytic phase (schizontocide) against all forms of malaria, but the action is too slow for the drug to be used for treatment. Proguanil prevents the formation of sporozoites in the mosquito, thus interfering with the spread of malaria (1). The drug acts through an active metabolite (cycloguanil). The mechanism of action is due to an inhibition of dihydropholate reductase (2).
