Pharmacokinetics of epidurally administered nicomorphine with its metabolites and glucuronide conjugates in patients undergoing pulmonary surgery during combined epidural local anaesthetic block and general anaesthesia
✍ Scribed by Petronella M. Koopman-Kimenai; Tom B. Vree; Leo H. D. J. Booij; Marcel A. W. M. Hasenbos
- Publisher
- John Wiley and Sons
- Year
- 1995
- Tongue
- English
- Weight
- 701 KB
- Volume
- 16
- Category
- Article
- ISSN
- 0142-2782
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✦ Synopsis
After epidural administration of 15 mg 3,6-dinicotinoylmorphine (nicomorphine) in 10 patients undergoing pulmonary surgery, the parent compound was quickly metabolized into the metabolites 6-mononicotinoylmorphine and morphine. The mean apparent half-lives ( f SD) of elimination were 10min (0.165 h f 0.053 h) for 3,6dinicotinoylmorphine and 1.77 h f 1.23 h for 6-mononicotinoylmorphine. Morphine is subsequently metabolized into morphine-3-glucuronide and morphine-6-glucuronide. The apparent half-lives of morphine, morphine-3-glucuronide, and morphine-6-glucuronide are similar: 3.63 h f 1-63 h, 4.10 h f 0.57 h, and 4.20 h f 1.64 h respectively. The possible glucuronide conjugate of 6-mononicotinoylmorphine was not detected. The prodrug 3,6-dinicotinoylmorphine was biotransformed into three active compounds: 6mononicotinoylmorphine, morphine, and morphine-6-glucuronide.