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
  1. Should not be prescribed for prophylaxis in patients with major psychiatric disorders .
  2. 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
  1. Structural analog of quinine; exact mechanism unknown, acts as a blood schizonticide
  2. May increase intravesicular pH in parasites.
  3. 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.
Exam Question
  • Chemoprophylaxis in an Englishman visiting chloroquine and mefloquine ersistant malaria region is done with Doxycycline.
  • Mefloquine is contraindicated with Halofantrine/Quinine.
Don't Forget to Solve all the previous Year Question asked on Mefloquine