Comparative Pharmacology
Head-to-head clinical analysis: CHLOROQUINE PHOSPHATE versus MEFLOQUINE HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CHLOROQUINE PHOSPHATE versus MEFLOQUINE HYDROCHLORIDE.
CHLOROQUINE PHOSPHATE vs MEFLOQUINE HYDROCHLORIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Chloroquine is a 4-aminoquinoline that acts as a blood schizonticide. It inhibits heme polymerase in malaria parasites, preventing the conversion of toxic heme to hemozoin, leading to accumulation of toxic heme and parasite death. It also has anti-inflammatory and immunomodulatory effects via inhibition of toll-like receptors and cytokine production.
Mefloquine is a quinoline antimalarial agent that acts as a blood schizontocide. Its exact mechanism is unknown but is thought to involve forming toxic heme complexes or inhibiting heme polymerase, leading to parasite death.
600 mg base (1 g phosphate) orally once daily for 2 days, then 300 mg base (500 mg phosphate) orally once daily for 3 days for malaria. For extraintestinal amebiasis: 600 mg base (1 g phosphate) orally once daily for 2 days, then 300 mg base (500 mg phosphate) orally once daily for 2-3 weeks.
250 mg (1 tablet) orally once weekly for prophylaxis; 1250 mg (5 tablets) as a single oral dose for treatment of uncomplicated malaria.
None Documented
None Documented
Terminal elimination half-life: 30-60 days (range 20-100 days); prolonged due to extensive tissue distribution and slow release from lysosomes.
~2-4 weeks (terminal half-life); clinical context: long half-life allows weekly dosing for prophylaxis, but accumulation can occur with repeated doses.
Renal: 50-70% as unchanged drug; hepatic/biliary: 20-30% as metabolites; fecal: up to 20%.
~83% (fecal/biliary), ~9% (renal unchanged), ~2.5% (renal as metabolite).
Category C
Category A/B
Antimalarial
Antimalarial