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Therapeutic Index

MEXOQUINE

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          Retailer        Stockiest
                                
240.00        192.00            172.80
 
       
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