Goromaru T, Matsuura H, Yoshimura N, Miyawaki T, Sameshima T, Miyao J, Furuta T, Baba S
Anesthesiology. 1984 Jul;61(1):73-7.
Although fentanyl has been used widely as a short-acting narcotic analgesic, its metabolism in humans has not been clarified. In this study, three fentanyl metabolites were identified in the urine of eight surgical patients receiving 0.3-0.5 mg of fentanyl intravenously. The metabolites 4-N-(N-propionylanilino)piperidine, 4-N-(N-hydroxypropionylanilino)piperidine and 1-(2-phenethyl)-4-N-(N-hydroxypropionylanilino)piperidine, and unchanged fentanyl were identified by GC-mass spectrometry in urine collected 6 h after administration. Fentanyl and its main metabolite, 4-N-(N-propionylanilino)piperidine, were determined quantitatively in the urine of five additional patients receiving 0.5 mg fentanyl intravenously. Urinary excretion of fentanyl and 4-N-(N-propionylanilino)-piperidine during the first 12 h after injection accounted for 0.3-4.0% and 26 to 55% of the dose, respectively.
尽管芬太尼已被广泛用作短效麻醉性镇痛药，但其在人体内的代谢情况尚未明确。在本研究中，在8名静脉注射0.3 - 0.5毫克芬太尼的外科手术患者的尿液中鉴定出了三种芬太尼代谢物。通过气相色谱 - 质谱法在给药后6小时收集的尿液中鉴定出代谢物4 - N -（N - 丙酰苯胺基）哌啶、4 - N -（N - 羟基丙酰苯胺基）哌啶和1 -（2 - 苯乙基）- 4 - N -（N - 羟基丙酰苯胺基）哌啶以及未变化的芬太尼。在另外5名静脉注射0.5毫克芬太尼的患者的尿液中对芬太尼及其主要代谢物4 - N -（N - 丙酰苯胺基）哌啶进行了定量测定。注射后前12小时内，芬太尼和4 - N -（N - 丙酰苯胺基）哌啶的尿排泄量分别占给药剂量的0.3 - 4.0%和26%至55%。
