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.

Autor: Koopman-Kimenai PM; Department of Clinical Pharmacy, Academic Hospital Nijmegen Sint Radboud, Geert Grooteplein Zuid 8, GA Nijmegen, The Netherlands., Vree TB, Booij LH, Hasenbos MA
Jazyk: angličtina
Zdroj: Biopharmaceutics & drug disposition [Biopharm Drug Dispos] 1995 Aug; Vol. 16 (6), pp. 507-20.
DOI: 10.1002/bdd.2510160608
Abstrakt: 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 (+/- SD) of elimination were 10 min (0.165 h +/- 0.053 h) for 3,6-dinicotinoylmorphine and 1.77 h +/- 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 +/- 1.63 h, 4.10 h +/- 0.57 h, and 4.20 h +/- 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: 6-mononicotinoylmorphine, morphine, and morphine-6-glucuronide.
Databáze: MEDLINE
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