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Metab Brain Dis. 2012 Mar;27(1):1-5. doi: 10.1007/s11011-011-9274-6. Epub 2011 Dec 24.

Morphine metabolism, transport and brain disposition.

Author information

1
Clinical Pharmacokinetics Unit in Transplantation and Autoimmune Disease, Foundation IRCCS Policlinico San Matteo, 7100 Pavia, Italy. degregor@unipv.it

Abstract

The chemical structures of morphine and its metabolites are closely related to the clinical effects of drugs (analgesia and side-effects) and to their capability to cross the Blood Brain Barrier (BBB). Morphine-6-glucuronide (M6G) and Morphine-3-glucuronide (M3G) are both highly hydrophilic, but only M6G can penetrate the BBB; accordingly, M6G is considered a more attractive analgesic than the parent drug and the M3G. Several hypotheses have been made to explain these differences. In this review we will discuss recent advances in the field, considering brain disposition of M6G, UDP-glucoronosyltransferases (UGT) involved in morphine metabolism, UGT interindividual variability and transport proteins.

PMID:
22193538
PMCID:
PMC3276770
DOI:
10.1007/s11011-011-9274-6
[Indexed for MEDLINE]
Free PMC Article

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