Morphine metabolism, transport and brain disposition

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 onl...

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Detalles Bibliográficos
Autores principales: De Gregori, Simona, De Gregori, Manuela, Ranzani, Guglielmina Nadia, Allegri, Massimo, Minella, Cristina, Regazzi, Mario
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer US 2011
Materias:
Review Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3276770/
https://www.ncbi.nlm.nih.gov/pubmed/22193538
http://dx.doi.org/10.1007/s11011-011-9274-6
Descripción
Sumario: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.

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