A randomized comparative trial of the pharmacokinetics and pharmacodynamics of oral doses of mefloquine and of mefloquine in combination with artesunate was carried out on 20 Thai male patients with acute, uncomplicated falciparum malaria. The patients were randomized to receive either mefloquine alone (8 patients; 1250 mg of mefloquine--initial dose, 750 mg; followed 6 hours later by 500 mg), ...

OBJECTIVES To monitor the sensitivity of Plasmodium falciparum to the drugs used to treat severe malaria and to prevent malaria in Comoros and Madagascar. DESIGN We used the in vitro isotopic method to test the sensitivity of P. falciparum to quinine, mefloquine and cycloguanil. RESULTS We tested fresh isolates of P. falciparum, collected from patients living in urban, suburban and rural ar...

Mefloquine is an antimalarial drug that has been commonly used in military settings since its development by the US military in the late 1980s. Owing to the drug's neuropsychiatric contraindications and its high rate of inducing neuropsychiatric symptoms, which are contraindications to the drug's continued use, the routine prescribing of mefloquine in military settings may be problematic. Due t...

Peroxidic antimalarial agents including the sequiterpene artemisinins and the synthetic 1,2,4-trioxolanes function via initial intraparasitic reduction of an endoperoxide bond. By chemically coupling this reduction to release of a tethered drug species it is possible to confer two distinct pharmacological effects in a parasite-selective fashion, both in vitro and in vivo. Here we demonstrate th...

The effects of the antimalarial agent mefloquine on the release of marker enzymes, acid phosphatase and beta glucuronidase, from the rat liver lysosomes in a crude lysosomal preparation were investigated and compared with that of chloroquine whose membrane effects have been well-documented in the literature. At 10 microM, mefloquine decreased significantly the release of marker enzymes when com...

Mefloquine is a relatively new antimalarial drug which has been associated with a wide variety of adverse effects, including skin reactions. In order to evaluate the range and frequency of mefloquine's dermatological effects, we searched the scientific literature for published case reports of such effects. We found 74 case reports, published between the years 1983 and 1997. Pruritus and maculop...

Sir—The multicenter randomized trial reported by Overbosch and colleagues [1] is important for 2 reasons. First, the study shows that when taken as malaria prophylaxis, mefloquine is not well tolerated by many travelers. Of the study participants randomized to receive mefloquine, 67.1% reported 1 adverse event, and, in 6% of mefloquine users, these events were severe (defined as requiring medic...

The currently used treatments for leishmaniasis, a neglected parasitic disease, are associated with several side effects, high cost and resistance of the Leishmania parasites. Here we evaluated in vitro and in vivo the antileishmanial activity of five antimalarial drugs against Leishmania amazonensis. Mefloquine was effective against promastigotes in axenic cultures and showed an IC50 (concentr...

The efficacy of the combination of a single oral dose of 500 mg artemisinin with a single 500 mg oral dose of mefloquine (AM) in the treatment of uncomplicated falciparum malaria was compared to mefloquine therapy alone (M) in a double-'blind' randomized study in an endemic area in the south of Viet Nam where single low dose treatment was employed and where mefloquine had been recently introduc...