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Healthcare Communications

Mefloquine

 

Malaria - a killer returns

- Incidence of malaria on the rise due to resistance of mosquito (the vector) to insecticides and of Plasmodium (the parasite) to antimalarial drugs
- Sharp increase in deaths from malaria

 

 

Antimalarial Therapy

- Chloroquine is the mainstay of therapy
- Quinine is old yet effective
- Other antimalarials are amodiaquine, proguanil, pyrimethamine, mepacrine
- Primaquine for falciparum malaria
- Mefloquine, artemisinin, artemether, artesunate are newer agents
- Sulfonamides, trimethoprim, tetracyclines and quinolone have some antimalarial activity

 

Limitations of Existing Antimalarial Therapy

- Resistance to chloroquine is common
- Plasmodium falciparum infections are particularly a threat because of severity of infection and drug resistance
- Adverse effects with quinine
- Other agents are not as effective as first line therapy

 

Mefloquine

- Acts against malarial parasite at erythrocytic phase
- Schizonticidal
- Effective against P. falciparum and P. vivax
- Effective even in chloroquine and quinine resistant cases

 

Pharmacokinetics

Absorption
- Well absorbed from GI tract
- Peak concentrations in 6 hours

Distribution
- Widely distributed

Elimination
- Half life : 21 days
- Drug persists in the body
- Mefloquine and metabolite mainly excreted in bile anf faeces

 

 

Dosage

Single dose 1000 mg or 15 mg/kg body wt.

In multidrug resistant cases 25 mg/kg in 2 divided doses

Administer with a 250 ml water (vomiting following administration reduces the drug availability in the body)

For prophylaxis
250 mg or 5 mg/kg once weekly 1-2 weeks before entering a malarial area and continuing for 4 months after leaving

 

 

Contraindications

- Pregnancy - 1st trimester
- Children < 3 months age or < 5 kg weight

 

Indications

- Chloroquine and multi drug resistant Plasmodium falciparum or vivax infection
- Prophylaxis in endemic areas

 

Salient Features

- Used in treatment of chloroquine resistant and multi drug resistant malaria due to P.falciparum or P.vivax
- Near 100% success rates
- A drug of choice in cerebral malaria
- Convenient single dose administration
- Long half life, hence persistence of drug in the body, preventing recrudescence
- May be used alone or with other antimalarial drugs, if necessary
- May be used for prophylaxis