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


CONCLUSIONS
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.
Barennes
H
H
Centre Muraz, Bobo Dioulasso, Burkina Faso.
Sterlingot
H
H
Nagot
N
N
Meda
H
H
Kaboré
M
M
Sanou
M
M
Nacro
B
B
Bourée
P
P
Pussard
E
E
D000208:Acute Disease; D000284:Administration, Oral; D000285:Administration, Rectal; D000349:Africa; D000962:Antimalarials / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D002648:Child; D002675:Child, Preschool; D006801:Humans; D007262:Infusions, Intravenous; D016778:Malaria, Falciparum / Q000097:blood / Q000188:drug therapy*; D011803:Quinine / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D013997:Time Factors
D000962:Antimalarials; D011803:Quinine