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More popularly known as proguanil, this drug was developed
by British antimalarial research in 1945. It 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.
Chloroguanide
is slowly but adequately absorbed from the gastrointestinal tract. Peak plasma levels are
attained within 5 hours and elimination half-time is about 16-20 hours.
Chloroguanide is available as tablets,
each containing 100 mg of the drug. The dose for prophylaxis is 100-200 mg daily.
Chloroguanide along with chloroquine is
used as prophylaxis effective against P. falciparum malaria.
At the prophylactic doses, it produces
occasional nausea and diarrhoea. It is otherwise a safe drug and can be used in pregnancy.
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