Premium
Analgesic effects of codeine‐6‐glucuronide after intravenous administration
Author(s) -
Srinivasan V.,
Wielbo D.,
Tebbett I.R.
Publication year - 1997
Publication title -
european journal of pain
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.305
H-Index - 109
eISSN - 1532-2149
pISSN - 1090-3801
DOI - 10.1016/s1090-3801(97)90103-8
Subject(s) - codeine , analgesic , glucuronide , pharmacology , morphine , chemistry , opioid , medicine , receptor , metabolite , biochemistry
Centrally administered codeine glucuronide has been shown to exhibit antinociceptive properties with decreased immunosuppressive effects compared to codeine. In this study, codeine‐6‐glucuronide was administered to rats, and its analgesic effect was compared to that of codeine. The concentrations of codeine and its metabolites in plasma and brain were also determined at the peak response time after administration of each compound. Receptor‐binding studies with rat brain homogenates and affinity profiles were also determined. Intravenous administration of codeine‐6‐glucuronide resulted in approximately 60% of the analgesic response elicited by codeine itself. Analysis of plasma and brain showed that codeine‐6‐glucuronide is relatively stable in vivo , with only small amounts of morphine‐6‐glucuronide being detected in addition to unchanged codeine‐6‐glucuronide. The receptor affinity of codeine‐6‐glucuronide was similar to that of codeine. It is concluded that intravenously administered codeine‐6‐glucuronide possesses analgesic activity similar to that of codeine, and may have clinical benefit in the treatment of pain