Each uncoated tablet contains:
Mefloquine Hydrochloride equivalent to
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.
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
derivatives, proguanil, pyrimethamine and
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
In vitro and in vivo
studies with mefloquine showed no haemolysis associated
with glucose-6-phosphate dehydrogenase deficiency.
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.
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 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.
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.
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
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
Mefloquine should be used
with caution in patients with renal impairment.
Mexoquine should be
taken with plenty of water and preferably with food. The
dosage depends on the immune status and body weight of
Adults: 15-25 mg per kg
body weight or as per the physician’s advice.
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