Dambisya Y M, Chan K, Wong C L
Department of Pharmacology, Faculty of Medicine, Chinese University of Hong Kong.
Methods Find Exp Clin Pharmacol. 1992 Dec;14(10):773-80.
The effects of ephedrine and phenylpropanolamine (PPA) on the 24 h urinary excretion of morphine, codeine and their metabolites, and on the plasma and brain disposition of morphine and codeine at steady state in mice were studied. Morphine-3-glucuronide was the major urinary metabolite in morphine treated animals, while for codeine treated animals norcodeine and morphine-3-glucuronide were the major metabolites. In all cases percentage of drug excreted unchanged was 10-15% of the administered dose. Ephedrine or PPA pretreatment had no apparent effect on these parameters. The metabolic ratios for the different pathways were comparable in all treatment groups. Steady-state plasma and brain concentration-time profiles of codeine and morphine also showed marked similarity in all treatment groups. Apparently, ephedrine or PPA pretreatment has no effect on the disposition of morphine and codeine in mice. The results are discussed from the perspective of our earlier findings of dependence on cough mixtures containing opioids and sympathomimetics.
研究了麻黄碱和去氧肾上腺素（PPA）对小鼠24小时内吗啡、可待因及其代谢产物尿排泄的影响，以及对稳态下吗啡和可待因在血浆和脑内分布的影响。在接受吗啡治疗的动物中，吗啡-3-葡萄糖醛酸是主要的尿代谢产物，而在接受可待因治疗的动物中，去甲可待因和吗啡-3-葡萄糖醛酸是主要代谢产物。在所有情况下，原形药物排泄的百分比为给药剂量的10%-15%。麻黄碱或PPA预处理对这些参数无明显影响。所有治疗组中不同代谢途径的代谢比相当。可待因和吗啡的稳态血浆和脑浓度-时间曲线在所有治疗组中也显示出明显的相似性。显然，麻黄碱或PPA预处理对小鼠体内吗啡和可待因的分布没有影响。结合我们早期对含有阿片类药物和拟交感神经药的止咳合剂依赖性的研究结果对这些结果进行了讨论。
