Abstract
A double-blind randomized comparative study of the pharmacokinetics and pharmacodynamics of a single oral dose of 750 mg or 1250 mg of mefloquine was carried out on 20 Thai male patients with acute uncomplicated falciparum malaria. In the 750-mg group, one patient exhibited an RII response, while the others responded to the treatment with a mean fever clearance time of 50.2 +/- 28.2 hours and a mean parasite clearance time of 70.2 +/- 17.3 hours. The main adverse effects were dizziness, nausea, vomiting, abdominal pain, and diarrhoea. Electrocardiogram monitoring detected sinus bradycardia in three patients and sinus arrhythmia in three others. In the 1250-mg group, one patient exhibited an RII response, while the others responded to the treatment with a mean fever clearance time of 43.4 +/- 36.6 hours and a mean parasite clearance time of 73.4 +/- 25.2 hours. However, during the follow-up period, two patients recrudesced on day 23 and on day 31 (RI response). Dizziness, nausea, vomiting, abdominal pain, and diarrhoea were the major adverse effects, with dizziness being more frequent compared with the 750-mg group. Sinus bradycardia occurred in four patients and sinus arrhythmia in four others. The pharmacokinetics of the two regimens were similar, with the absorption of mefloquine increasing linearly with the dose; however, vomiting within an hour of taking the drug reduced the whole blood mefloquine concentrations. The results do not indicate that there is any advantage in using a single dose of 1250 mg of mefloquine rather than 750 mg.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Doberstyn E. B., Phintuyothin P., Noeypatimanondh S., Teerakiartkamjorn C. Single-dose therapy of falciparum malaria with mefloquine or pyrimethamine-sulfadoxine. Bull World Health Organ. 1979;57(2):275–279. [PMC free article] [PubMed] [Google Scholar]
- Harinasuta T., Bunnag D., Vanijanond S., Charoenlarp P., Suntharasmai P., Chitamas S., Sheth U. K., Wernsdorfer W. H. Mefloquine, sulfadoxine, and pyrimethamine in the treatment of symptomatic falciparum malaria: a double-blind trial for determining the most effective dose. Bull World Health Organ. 1987;65(3):363–367. [PMC free article] [PubMed] [Google Scholar]
- Harinasuta T., Bunnag D., Wernsdorfer W. H. A phase II clinical trial of mefloquine in patients with chloroquine-resistant falciparum malaria in Thailand. Bull World Health Organ. 1983;61(2):299–305. [PMC free article] [PubMed] [Google Scholar]
- Juma F. D., Ogeto J. O. Mefloquine disposition in normals and in patients with severe Plasmodium falciparum malaria. Eur J Drug Metab Pharmacokinet. 1989 Jan-Mar;14(1):15–17. doi: 10.1007/BF03190836. [DOI] [PubMed] [Google Scholar]
- Karbwang J., Molunto P., Na Bangchang K., Bunnag D. Determination of mefloquine in biological fluids using high performance liquid chromatography. Southeast Asian J Trop Med Public Health. 1989 Mar;20(1):55–60. [PubMed] [Google Scholar]
- Mu J. Y., Israili Z. H., Dayton P. G. Studies of the disposition and metabolism of mefloquine HCl (WR 142,490), a quinolinemethanol antimalarial, in the rat. Limited studies with an analog, WR 30,090. Drug Metab Dispos. 1975 May-Jun;3(3):198–210. [PubMed] [Google Scholar]
- de Souza J. M., Heizmann P., Schwartz D. E. Single-dose kinetics of mefloquine in Brazilian male subjects. Bull World Health Organ. 1987;65(3):353–356. [PMC free article] [PubMed] [Google Scholar]