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Primaquine
is the only drug available for use as anti-relapse
antimalarial for prophylactic in P.vivax
malaria. However, this drug is not without side
effects and most commonly cited effect is methaemoglobinaemia
in patients with G6PD deficiency. Higher doses
of primaquine cause methaemoglobinaemia in most
subjects and leukopenia in some. However, there
is a small fraction of black population with G6PD
deficiency who develop anaemia due to intravascular
haemolysis at daily dose levels of 15 mg (base)
and above.
It is being increasingly felt that the eroding efficacy of commonly used antimalarials has
contributed substantially to the resurgency of malaria during last three decades. Although
new antimalarials have appeared in the market during this time but none has yet
supplemented chloroquine. There are no drugs in the market at any cost or in advanced
development that appear to be as well tolerated as chloroquine.
Combinations of existing antimalarials especially those now available in rural clinics and
market hold great potential for effective, self administered therapies for uncomplicated
malaria particularly where relapses are frequently encountered. Applying combined
therapies to the problem should demand a high standard of proof of safety and efficacy in
randomised double blind, placebo controlled trials.
The Central Drug Research Institute has
developed a compound - given in house number "Compound
80/53" and allotted International Nonproprietary
Name (INN) as Bulaquin - which is a primaquine
derivative.
Bulaquin is without any side effects observed
with primaquine. Comparative data on initial (0
day pre drug) and final (+7 day post drug) values
of haemoglobin, methaemoglobin, prothrombin time,
partial thromboplastin time and fibrinogen in
healthy human subject treated with primaquine
(15 mg OD x7 days) and Bulaquin (25 mg OD x7 days)
have shown that one week primaquine treatment
leads to rise in methaemoglobin levels from 3.97%
to 16.32%, which is highly significant in comparison
to the 2.29% and 3.02% levels of methaemoglobin
before and after 7 days treatment with Bulaquin
respectively. Thus, it is evident that primaquine
treatment produces rise in methaemoglobin. While
Bulaquine does not produce rise in methaemoglobin
levels offering an advantage over primaquine.
Bulaquin has been licenced to Nicholas Piramal
India Ltd., Mumbai for marketing . Nicholas Piramal
has introduced Bulaquin alongwith chloroquine
into the market as a combination pack under the
trade name Aablaquine. The objective of
the combined therapy is to control P.vivax
malaria more effectively by providing initial
cure and thereafter preventing relapses by use
of this combination pack. It is hoped that the
introduction of this combination pack of Bulaquin
should contribute substantially to the ongoing
National Malaria action programme advocated by
Government of India.
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