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Pharmacokinetics of morphine are not altered in subjects with Gilbert's syndrome.


ABSTRACT: AIMS:To verify that Gilbert's syndrome, which is caused by decreased glucuronidation capacity of the UDP-glucuronosyl transferase (UGT)1A1, does not account for impaired morphine clearance. METHODS:Noncompartmental pharmacokinetic parameters for morphine and its glucuronide metabolites were compared between five carriers of Gilbert's syndrome and six noncarriers after a 7.5 mg (19.8 micro mol) intravenous injection of morphine sulphate pentahydrate. To estimate the amount of morphine-6-glucuronide (M6G) formed from morphine, 1 mg of deuterized M6G was injected intravenously at the same time. RESULTS:No differences were detected between carriers and noncarriers of Gilbert's syndrome in the clearance of morphine (80.1 +/- 12 l h(-1) vs 87.9 +/- 22 l h(-1)) and in the percentage of morphine that was metabolized to M6G (10.9 +/- 1.4 vs 13 +/- 2). The areas under the plasma concentration vs time curves of morphine, M6G and morphine-3-glucuronide also did not differ between carriers and noncarriers of Gilbert's syndrome. CONCLUSIONS:Gilbert's syndrome is not a factor to be considered when prescribing morphine.

SUBMITTER: Skarke C 

PROVIDER: S-EPMC1884272 | biostudies-literature | 2003 Aug

REPOSITORIES: biostudies-literature

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Pharmacokinetics of morphine are not altered in subjects with Gilbert's syndrome.

Skarke Carsten C   Schmidt Helmut H   Geisslinger Gerd G   Darimont Jutta J   Lötsch Jörn J  

British journal of clinical pharmacology 20030801 2


<h4>Aims</h4>To verify that Gilbert's syndrome, which is caused by decreased glucuronidation capacity of the UDP-glucuronosyl transferase (UGT)1A1, does not account for impaired morphine clearance.<h4>Methods</h4>Noncompartmental pharmacokinetic parameters for morphine and its glucuronide metabolites were compared between five carriers of Gilbert's syndrome and six noncarriers after a 7.5 mg (19.8 micro mol) intravenous injection of morphine sulphate pentahydrate. To estimate the amount of morph  ...[more]

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