Proost J H, Eriksson L I, Mirakhur R K, Roest G, Wierda J M
Department of Anaesthesiology, University Hospital, GZ Groningen, The Netherlands.
Br J Anaesth. 2000 Nov;85(5):717-23. doi: 10.1093/bja/85.5.717.
The excretion of rocuronium and its potential metabolites was studied in 38 anaesthetized patients, ASA I-III and 21-69 yr old. Rocuronium bromide was administered as an i.v. bolus dose of 0.3 or 0.9 mg kg-1. In Part A of the study, the excretion into urine and bile, and the liver content were studied. Plasma kinetics (n = 19) were similar to those reported previously. Urinary recovery within 48 h after administration was 26 (8)% (mean (SD)) (n = 8) of the dose. In bile obtained from T-drains, the recovery within 48 h was 7 (6)% (n = 11). The rocuronium concentration in bile declined bi-exponentially, with half-lives of 2.3 (0.7) and 16 (11) h respectively (n = 6). In three patients from whom stoma fluid was collected, the amount of rocuronium recovered ranged from 0.04 to 12.0% of the dose. In liver tissue obtained from four patients undergoing hemihepatectomy, the estimated amount of rocuronium at 2-5 h after administration ranged between 6.3 and 13.2% (n = 4). In the second part of the study (Part B), urine and faeces were collected over 4-8 days and the recovery was 27 (13)% and 31 (23)% of the dose respectively (n = 10). In most samples, irrespective of the type of biological material, only small amounts of the metabolite 17-desacetyl-rocuronium was found. The results demonstrate that rocuronium is taken up by the liver and excreted into bile in high concentrations. The faecal and urinary excretion of unchanged rocuronium are the major routes of rocuronium elimination.
在38例ASA I-III级、年龄在21至69岁的麻醉患者中研究了罗库溴铵及其潜在代谢物的排泄情况。静脉注射给予溴化罗库溴铵,剂量为0.3或0.9 mg·kg-1。在研究的A部分,研究了尿液和胆汁中的排泄情况以及肝脏中的含量。血浆动力学(n = 19)与先前报道的相似。给药后48小时内尿液回收率为剂量的26(8)%(均值(标准差))(n = 8)。从T形引流管获得的胆汁中,48小时内回收率为7(6)%(n = 11)。胆汁中罗库溴铵浓度呈双指数下降,半衰期分别为2.3(0.7)小时和16(11)小时(n = 6)。在3例收集了造口液的患者中,回收的罗库溴铵量占剂量的0.04%至12.0%。在4例接受半肝切除术的患者的肝脏组织中,给药后2至5小时罗库溴铵的估计量在6.3%至13.2%之间(n = 4)。在研究 的第二部分(B部分),在4至8天内收集尿液和粪便,回收率分别为剂量的27(13)%和31(23)%(n = 10)。在大多数样本中,无论生物材料类型如何,仅发现少量代谢物17-去乙酰基罗库溴铵。结果表明,罗库溴铵被肝脏摄取并以高浓度排泄到胆汁中。未改变的罗库溴铵的粪便和尿液排泄是罗库溴铵消除的主要途径。