Mefloquine

MEFLOQUINE

USES OF MEFLOQUINE

• Indicated for the treatment of mild-to-moderate acute malaria caused by mefloquine-susceptible strains of P. falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax.
• For Prevention of Malaria.
• In places with resistance to Chloroquine and Mefloquine,prophylaxis is given by medicines Doxycycline or Proguanil/Atovaquone.
• Insufficient clinical data exist to document the effect of mefloquine in malaria caused by P. ovale or P. malariae.
• 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 derivative (eg, primaquine).

SIDE EFFECTS AND DRUG INTERACTIONS OF MEFLOQUINE

• May cause neuropsychiatric adverse reactions that can persist after mefloquine has been discontinued
• Should not be prescribed for prophylaxis in patients with major psychiatric disorders .
• May increase QT interval; Halofantrine or quinidine/quinine given to patients who have received mefloquine cause QTc lengthening -cardiac arrest may occur.
• Strong CYP3A4 inhibitors (eg, ketoconazole) should do not coadminister with or within 15 weeks after the last mefloquine dose.

PHARMACOLOGY OF MEFLOQUINE

Mechanism of Action

• Structural analog of quinine; exact mechanism unknown, acts as a blood schizonticide
• May increase intravesicular pH in parasites.

• Metabolism:

• Extensively metabolized in liver by CYP3A4

SAFETY OF USE OF MEFLOQUINE IN PREGNANCY AND LACTATION

• Pregnancy Category: B
• Lactation: Minimally excreted in human breast milk; low concentrations (3% to 4%) excreted; caution advised.