Szeto H H, Inturrisi C E, Houde R, Saal S, Cheigh J, Reidenberg M M
Ann Intern Med. 1977 Jun;86(6):738-41. doi: 10.7326/0003-4819-86-6-738.
Concentrations of meperidine and its active metabolite, normeperidine, were measured in plasma of patients receiving the drug for analgesia. Meperidine levels in cancer patients were 0.10 to 0.55 microng/ml 1 h after a dose and were 0.05 to 0.14 in patients in the oliguric period after renal transplantation. Normeperidine levels were 0.05 to 0.28 microng/ml in the cancer patients and 0.13 to 0.36 in the renal failure patients. The ratio of normeperidine to meperidine levels was always higher in the renal failure patients than in the cancer patients. Additionally, two patients receiving multiple doses of meperidine had high normeperidine levels and very high normeperidine/meperidine ratios when they showed signs of central nervous system excitation. These data indicate that normeperidine can contribute to the excitatory effects seen after multiple doses of meperidine and suggest that patients with renal failure are particularly susceptible to this problem.
在接受哌替啶镇痛治疗的患者血浆中测定了哌替啶及其活性代谢物去甲哌替啶的浓度。癌症患者用药1小时后血浆中哌替啶水平为0.10至0.55微克/毫升,肾移植后少尿期患者的哌替啶水平为0.05至0.14微克/毫升。癌症患者的去甲哌替啶水平为0.05至0.28微克/毫升,肾衰竭患者为0.13至0.36微克/毫升。肾衰竭患者去甲哌替啶与哌替啶水平的比值始终高于癌症患者。此外,两名接受多次哌替啶给药的患者在出现中枢神经系统兴奋迹象时,去甲哌替啶水平较高,去甲哌替啶/哌替啶比值非常高。这些数据表明,去甲哌替啶可导致多次使用哌替啶后出现兴奋作用,并提示肾衰竭患者尤其易受此问题影响。