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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
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Quality
