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Intrarectal pharmacokinetics of two formulations of quinine in children with falciparum malaria.

Author(s): Barennes H, Sterlingot H, Nagot N, Meda H, Kabore M, Sanou M, Nacro B, Bouree P, Pussard E

Affiliation(s): Centre Muraz, Bobo Dioulasso, Burkina Faso.

Publication date & source: 2003-02, Eur J Clin Pharmacol., 58(10):649-52. Epub 2003 Jan 29.

Publication type: Clinical Trial; Comparative Study ; Randomized Controlled Trial; Research Support, Non-U.S. Gov't

OBJECTIVE: To compare the intrarectal bioavailabilities of two parenteral formulations of quinine most available in French- (Cinchona alkaloid mixture) and English (hydrochloride salt) -speaking areas of Africa. METHODS: The pharmacokinetics of quinine was investigated in four groups of 12 children with acute Plasmodium falciparum malaria receiving 8 mg/kg quinine base every 8 h either as hydrochloride salt or Cinchona alkaloid mixture by a slow 4-h intravenous infusion or intrarectal administration. Body temperature and parasitaemia were monitored, and blood quinine concentrations were measured by means of high-performance liquid chromatography. RESULTS: At 72 h, all the children were aparasitaemic and apyretic. Quinine C(max) values were higher after intravenous infusion of the hydrochloride salt and Cinchona alkaloid mixture (6.9+/-1.9 micro g/ml and 5.2+/-1.3 micro g/ml) than after intrarectal administration (3.5+/-1.4 micro g/ml and 3.1+/-1.6 micro g/ml), but t(max) values were similar (3.6+/-1.5, 4.2+/-1.0, 4.0+/-1.9, and 4.7+/-2.0 h, respectively). Intrarectal relative bioavailabilities of hydrochloride salt solution (57%) and Cinchona alkaloid mixture (62%) were similar. CONCLUSION: Whatever the parenteral formulation of quinine, the blood concentration-time profiles of quinine were similar after intrarectal administration. Intrarectal administration of hydrochloride salt solution is a possible mode of quinine delivery in remote rural areas of Africa.

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