Antimalarial Agents 351cated falciparum malaria but is not recom-
mended for prophylaxis.
8-AMINOQUINOLINESPRIMAQUINE
Primaquine, a 8-aminoquinoline, is a
poor erythrocytic schizontocide. It is
highly effective against gametocytes and
exoerythrocytic stages.
It disrupts the parasites mitochondria
and binds to native DNA, resulting in
inhibition of gametocytes and exoeryth-
rocytic forms.
Adverse effects include nausea, vom-
iting, weakness, abdominal pain and
methaemoglobinaemia. Haemolytic
anaemia in patients with G-6-PD defi-
ciency. Passage of dark urine is indica-
tion of haemolysis. In larger dose it can
cause leucopenia.
It is effective in radical cure of P. vivax
and P. ovale malaria.
QUINOLINE-METHANOL DERIVATIVESMEFLOQUINE
It is a highly effective erythrocytic
schizonticide especially against mature
trophozoite and schizont forms of malarial
parasite.
It behaves like quinine in many ways
but does not inhibit haem polymerase. It
probably acts by forming toxic complexes
with free haem that damages membranes
and interacts with other plasmodial
components.
It is absorbed after oral administration
and presence of food may enhance the
absorption. It is extensively metabolised in
liver and primarily secreted in bile.
Adverse reactions include nausea,
vomiting, dizziness, diarrhoea, abdominal
pain, anxiety disorder, sinus bradycardia,
ataxia. It is reported that mefloquine is
teratogenic in nature so should not be given
in first trimester of pregnancy.
It is used in multiresistant P. falciparum
malaria. It is not useful in complicated/
cerebral malaria.BULAQUINE
Bulaquine is a mixture of 3{-1-4-6(-
methoxy-8-quinolinyl) aminopentyl}
ethylidenedihydro-2-(3H) furanone and it’s
tautomers.
The exact action is not fully eluci-
dated. However, bulaquine inhibits
protein synthesis in protozoa and
indirectly inhibits polymerisation of
amino acids by the plasmodia. Treat-
ment prevents emergence of either
primary or secondary liver stage para-
sitaemia and the disease.
Since bulaquine is a tissue schizonto-
cide it is effective against the dormant
hepatic stages of P. vivax only. It has to be
combined with chloroquine which acts on
the erythrocytic stage of the plasmodium.
For convenience bulaquine is available
along with chloroquine as an anti-relapse
treatment pack.
It is an erythrocytic schizontocide used
in the treatment and prevention of P. vivax
malaria relapse.