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.
- 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.
- 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