Pharmacokinetics and metabolism of amopyroquin after administration of two doses of 6 mg/kg im 24 h apart to healthy volunteers.
Twelve healthy volunteers received two doses of amopyroquin 6 mg/kg im 24 h apart. Blood and plasma concentrations of amopyroquin and two metabolites were assayed by HPLC from 0 to 48 h. Half-life values for amopyroquin, calculated from 0 to 48 h whole-blood and plasma samples were 13.9 +/- 9.1 and 18.3 +/- 6.8 h respectively. Two metabolites were detected in blood and they had very low in-vitro activity against Plasmodium falciparum compared with the parent drug. Neither hypotension nor lengthening of QRS complex were observed in any volunteers and hepatic enzymes remained in the normal range despite a transitory increase. These results confirm that unchanged amopyroquin accounts for antimalarial activity in vivo and that two doses of 6 mg/kg are well tolerated.
Pussard
E
E
Institut National de la Santé et de la Recherche Médicale, Unité 13, Hôpital Claude Bernard, Paris, France.
Chassard
D
D
Clavier
F
F
Bry
P
P
Verdier
F
F
D000328:Adult; D000634:Aminoquinolines / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000493:pharmacokinetics*; D006207:Half-Life; D006801:Humans; D007273:Injections, Intramuscular; D008297:Male; D010963:Plasmodium falciparum / Q000187:drug effects
D000634:Aminoquinolines; D000962:Antimalarials; C009846:amopyroquine