Yeh S Y, Krebs H A, Changchit A
J Pharm Sci. 1981 Aug;70(8):867-70. doi: 10.1002/jps.2600700808.
The urine of male and female mice, rats, guinea pigs, rabbits, cats, and dogs, given meperidine hydrochloride, 20--40 mg/kg ip, was analyzed by GLC for meperidine, normeperidine, p-hydroxymeperidine, and total (free and conjugated) meperidinic and normeperidinic acids. More than 90% of the excreted drugs was found in the 24-hr urine. Meperidine was observed in the urine of mice, rats, guinea pigs, and cats, but only a trace amount was observed in the urine of rabbits and dogs. Normeperidine, p-hydroxymeperidine (except in the mice), and total meperidinic and normeperidinic acids were observed in all species. All of the species studied have the capacity to N-demethylate meperidine to normeperidine and to hydrolyze meperidine and normeperidine to their respective acids. The male has a higher N-demethylating activity that the female with the exception of mice. Ester hydrolysis is a major metabolic pathway for meperidine metabolism.
给雄性和雌性小鼠、大鼠、豚鼠、兔子、猫和狗腹腔注射20 - 40毫克/千克盐酸哌替啶后，用气相色谱法分析其尿液中的哌替啶、去甲哌替啶、对羟基哌替啶以及总的（游离和结合的）哌替啶酸和去甲哌替啶酸。超过90%的排泄药物在24小时尿液中被发现。在小鼠、大鼠、豚鼠和猫的尿液中观察到了哌替啶，但在兔子和狗的尿液中仅观察到微量。在所有物种中均观察到了去甲哌替啶、对羟基哌替啶（小鼠除外）以及总的哌替啶酸和去甲哌替啶酸。所有研究的物种都有将哌替啶N - 去甲基化为去甲哌替啶以及将哌替啶和去甲哌替啶水解为各自酸的能力。除小鼠外，雄性的N - 去甲基化活性高于雌性。酯水解是哌替啶代谢的主要代谢途径。
