The pharmacokinetics of mefloquine in man: lack of effect of mefloquine on antipyrine metabolism.

Riviere, J E; Back, DJ; Breckenridge, AM; Re, Howells

doi:10.1111/j.1365-2125.1985.tb05099.x

Cited by 26 publications

(9 citation statements)

References 12 publications

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“…The pharmacokinetics of racMQ show marked variability of absorption and metabolism between subjects and between ethnic groups. Karbwang et al [1] found plasma concentrations in healthy Thai volunteers to be twice as high as those reported by Riviere et al [2] in healthy Caucasian volunteers. In contrast, a study by Juma et al [3] [2].…”

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confidence: 53%

Whole blood concentrations of mefloquine enantiomers in healthy Thai volunteers

Martin

Gimenez

Bangchang

et al. 1994

Eur J Clin Pharmacol

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We studied the pharmacokinetics of the enantiomers of mefloquine in whole blood in healthy Thai volunteers after administration of a single oral dose of 750 mg of the racemic mixture. Mefloquine pharmacokinetics were stereoselective. The peak concentrations and areas under the curve of the (-) enantiomer were significantly higher than those of its antipode (0.79 versus 0.46 microgram.ml-1 and 402 versus 94 micrograms.h.ml-1). The half-lives of (-)MQ were significantly longer than those of (+)MQ (531 versus 206 h). No stereoselectivity was observed for tmax values.

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confidence: 53%

Whole blood concentrations of mefloquine enantiomers in healthy Thai volunteers

Martin

Gimenez

Bangchang

et al. 1994

Eur J Clin Pharmacol

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“…The HPLC method of Riviere et al (6) was used to assay mefloquine from biological fluid. The within assay coefficient of variation was 3.5% at l00nglml and 2.5% at 500nglml and between assay it was 5.4% at 500nglml and 5.5% at 75Onglml.…”

Section: Methodsmentioning

confidence: 99%

Mefloquine disposition in normals and in patients with severePlasmodium falciparum malaria

Juma

Ogeto

1989

Eur. J. Drug Metab. Pharmacokinet.

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Mefloquine pharmacokinetics were studied in Kenyan African normal volunteers and in patients with severe acute attack of Plasmodium falciparum malaria. Peak concentrations were achieved in both groups at 20-24 hours. The mean half-life of elimination was 385 +/- 150 hours (mean +/- SD) in normal subjects while in severe malaria it was 493 +/- 215 hours which was significantly longer (P less than or equal to 0.001). The volume of distribution was significantly smaller in severe malaria where it was 30.76 +/- 10.50 l/kg (mean +/- SD) while in the normal subjects it was 40.90 +/- 20.70 l/kg (mean +/- SD) (P less than or equal to 0.001). The total body clearance in severe malaria was 3.75 +/- 1.51 l/h (mean +/- SD). This was significantly lower than in the normal subjects where it was 5.15 +/- 1.50 l/h (mean +/- SD) (P less than or equal to 0.001).

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“…; Riviere et al, 1985). For the assay of mefloquine in whole blood the extraction procedure was modified as follows; To samples of blood (1 ml) containing WR 184,806 as internal standard ([±-2,8-bis-trifluoromethyl)-4-[1-hydroxy-3-(Ntertbutylamino)-propyl]quinoline] phosphate; 400 ng) was added acetonitrile (2 ml) followed by vortex mixing for 30 s and centrifugation at 1000 g for 5 min.…”

Section: Discussionmentioning

confidence: 99%

“…After vortex mixing for 15 s the mixture was extracted with dichloromethane (6 ml) and the extracts assayed by h.p.l.c. (Riviere et al, 1985). Standard curves were prepared by adding known quantities of mefloquine (50-1000 ng) to either plasma or whole blood containing internal standard (400 ng).…”

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confidence: 99%

Plasma and whole blood mefloquine concentrations during treatment of chloroquine‐resistant falciparum malaria with the combination mefloquine‐sulphadoxine‐pyrimethamine.

Karbwang

Phillips

Wattanagoon

et al. 1987

Brit J Clinical Pharma

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Mefloquine-sulphadoxine-pyrimethamine (MSP) in combination has proved effective against multiple-drug-resistant falciparum malaria, but nothing is known about mefloquine absorption when it is given in this formulation. Nine Thai patients, aged 15-51 years with uncomplicated chloroquine-resistant falciparum malaria, took 11.2-16.7 mg of mefloquine base per kilogram bodyweight as MSP tablets. All patients responded to treatment with fever and parasite clearance times of 61 ± 29 h (mean ± s.d.) and 52 ± 24 h, respectively.The mean apparent absorption half-time (t½/2abs) of mefloquine was 4.89 h (range 2.25-9.72) and mean peak plasma concentration was 1815 ng ml-' (range 725-3368). Peak plasma mefloquine concentrations in three patients who vomited within 2 h of treatment were 725, 956 and 1972 ng ml-1. There was no significant difference between plasma and whole blood mefloquine concentrations during the first 48 h of treatment. Based on the elimination of parasitaemia, the plasma mefloquine concentrations are adequate for therapy of uncomplicated falciparum malaria although the relationship between plasma concentrations and therapeutic efficacy of mefloquine requires further study.

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The pharmacokinetics of mefloquine in man: lack of effect of mefloquine on antipyrine metabolism.

Cited by 26 publications

References 12 publications

Whole blood concentrations of mefloquine enantiomers in healthy Thai volunteers

Whole blood concentrations of mefloquine enantiomers in healthy Thai volunteers

Mefloquine disposition in normals and in patients with severePlasmodium falciparum malaria

Plasma and whole blood mefloquine concentrations during treatment of chloroquine‐resistant falciparum malaria with the combination mefloquine‐sulphadoxine‐pyrimethamine.

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