Pussard Eric, Straczek Celine, Kaboré Idrissa, Bicaba Auguste, Balima-Koussoube Tatiana, Bouree Patrice, Barennes Hubert
Service de Pharmacologie, Hôpital de Bicêtre, 78 rue du Général Leclerc, 94275 Le Kremlin-Bicêtre, France.
Antimicrob Agents Chemother. 2004 Nov;48(11):4422-6. doi: 10.1128/AAC.48.11.4422-4426.2004.
The pharmacokinetics of increasing doses of an intrarectal Cinchona alkaloid combination containing 96.1% quinine, 2.5% quinidine, 0.68% cinchonine, and 0.67% cinchonidine (Quinimax) was compared to that of parenteral regimens in 60 children with moderate malaria. Quinine exhibited a nonlinear pharmacokinetics, suggesting a saturation of rectal resorption. When early rejections appeared, blood quinine concentrations decreased by 30 to 50% and were restored by an immediate half-dose administration of the drug. Rectal administration of doses of 16 or 20 mg/kg of body weight led to concentration-time profiles in blood similar to those of parenteral regimens and could be an early treatment of childhood malaria.
在60名中度疟疾患儿中,将含96.1%奎宁、2.5%奎尼丁、0.68%辛可宁和0.67%辛可尼定的递增剂量直肠用金鸡纳生物碱组合(Quinimax)的药代动力学与肠胃外给药方案的药代动力学进行了比较。奎宁呈现非线性药代动力学,提示直肠吸收饱和。当出现早期排异反应时,血液中奎宁浓度下降30%至50%,通过立即给予半剂量药物可使其恢复。直肠给予16或20mg/kg体重的剂量导致血液中的浓度-时间曲线与肠胃外给药方案相似,可作为儿童疟疾的早期治疗方法。