Each uncoated tablet contains:
Composition:
Mefloquine Hydrochloride equivalent to
Mefloquine........................................................................250
mg
Indications :
Mexoquine is for use as a second line
treatment in chloroquine resistant
malaria, severe malaria due to P.
falciparum and P. vivax including
cerebral malaria. Not to be used as a
first line treatment for malaria.
Description:
Mefloquine is an antimalarial agent that
acts as a blood schizonticide. It is
effective against all species of malaria
(P. falciparum, P. vivax, P. malariae
and P. ovale). Its exact mechanism of
action is not known. Mefloquine is
active against the erythrocytic stages
of Plasmodium species. However, the drug
has no effect against the
exoerythrocytic (hepatic) stages of the
parasite and mature gametocytes.
Mefloquine is effective against malaria
parasites resistant to chloroquine and
other
4-aminoquinoline derivatives, proguanil,
pyrimethamine and
pyrimethamine-sulphonamide combinations.
Similar
to chloroquine and quinine, mefloquine
appears to interfere with the parasite's
ability to metabolize and utilise
erythrocyte hemoglobin. The antimalarial
activity of mefloquine may depend on the
ability of the drug to form hydrogen
bonds with cellular constituents.
Mefloquine binds to high-density
lipoproteins in serum, specifically
polypeptide apo A and is delivered to
the erythrocytes where it interacts with
a specific erythrocyte membrane protein,
stromatin and is then transferred to the
intracellular parasite by a pathway used
for exogenous phospholipids. Mefloquine
may exert its antimalarial action by
disrupting the membrane trafficking
events involved in the uptake of
phospholipids.
Cross
resistance between mefloquine and
halofantrine and cross-resistance
between mefloquine and quinine have been
observed in some regions.
In
vitro and in vivo studies with
mefloquine showed no haemolysis
associated with glucose-6-phosphate
dehydrogenase deficiency.
CONTRA-INDICATIONS:
Use of
mefloquine is contraindicated in
patients with a known hypersensitivity
to mefloquine or related compounds (eg,
quinine and quinidine). Mefloquine
should not be prescribed for prophylaxis
in patients with active depression, a
recent history of depression,
generalized anxiety disorder, psychosis,
or schizophrenia or other major
psychiatric disorders, or with a history
of convulsions. The use of mefloquine is
contraindicated in persons who have
received treatment with mefloquine in
the previous 4 weeks.
WARNINGS:
Patients
with acute P. vivax malaria, treated
with mefloquine, are at high risk of
relapse because mefloquine does not
eliminate exoerythrocytic (hepatic
phase) parasites. To avoid relapse,
after initial treatment of the acute
infection with mefloquine, patients
should subsequently be treated with an
8-aminoquinoline (eg, primaquine).
In case
of life-threatening, serious or
overwhelming malaria infections due to
P. falciparum, patients should be
treated with an intravenous antimalarial
drug. Following completion of
intravenous treatment, mefloquine may be
given to complete the course of therapy.
Data on
the use of halofantrine subsequent to
administration of mefloquine suggest a
significant, potentially fatal
prolongation of the QTc interval of the
ECG. Therefore, halofantrine must not be
given simultaneously with or subsequent
to mefloquine.
Mefloquine may cause psychiatric
symptoms in a number of patients,
ranging from anxiety, paranoia, and
depression to hallucinations and
psychotic behavior. On occasions, these
symptoms have been reported to continue
long after mefloquine has been stopped.
Rare cases of suicidal ideation and
suicide have been reported though no
relationship to drug administration has
been confirmed. Mefloquine should be
used with caution in patients with a
previous history of depression.
During
prophylactic use, if psychiatric
symptoms such as acute anxiety,
depression, restlessness or confusion
occur, these may be considered prodromal
to a more serious event. In these cases,
the drug must be discontinued and an
alternative medication should be
substituted.
Concomitant administration of mefloquine
and quinine or quinidine may produce
electrocardiographic abnormalities.
Concomitant administration of mefloquine
with quinine or chloroquine may increase
the risk of convulsions.
PRECAUTIONS:
General
Hypersensitivity reactions ranging from
mild cutaneous events to anaphylaxis
cannot be predicted.
In patients with epilepsy, mefloquine
may increase the risk of convulsions.
The drug should therefore be prescribed
only for curative treatment in such
patients and only if there are
compelling medical reasons for its use.
Caution
should be exercised with regard to
activities requiring alertness and fine
motor coordination such as driving,
piloting aircraft, operating machinery,
and deep-sea diving, as dizziness, a
loss of balance, or other disorders of
the central or peripheral nervous system
have been reported during and following
the use of mefloquine. These effects may
occur after therapy is discontinued due
to the long half-life of the drug.
Mefloquine should be used with caution
in patients with psychiatric
disturbances because mefloquine use has
been associated with emotional
disturbances.
In
patients with impaired liver function
the elimination of mefloquine may be
prolonged, leading to higher plasma
levels.This drug has been administered
for longer than 1 year. If the drug is
to be administered for a prolonged
period, periodic evaluations including
liver function tests should be
performed.
Mefloquine should be used with caution
in patients with renal impairment.
Dosage
:
Mexoquine should be taken with plenty of
water and preferably with food. The
dosage depends on the immune status and
body weight of the patient.
Adults:
15-25 mg per kg body weight or as per
the physician’s advice.
Presentations: 6
tablets
MRP
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