4.6 Article

Urinary, biliary and faecal excretion of rocuronium in humans

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BRITISH JOURNAL OF ANAESTHESIA
卷 85, 期 5, 页码 717-723

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ELSEVIER SCI LTD
DOI: 10.1093/bja/85.5.717

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neuromuscular block, rocuronium; pharmacokinetics, rocuronium; metabolism, rocuronium

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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.

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