Analgesic action of i.v. morphine-6-glucuronide in healthy volunteers.
The pharmacodynamics of morphine-6-glucuronide (M-6-G) i.v. were assessed in 12 healthy male volunteers in an open study. After a single bolus dose of M-6-G 5 mg i.v., we measured antinociceptive effects, using electrical and cold pain tests, and plasma concentrations of M-6-G, morphine-3-glucuronide (M-3-G) and morphine. Pain intensities during electrical stimulation (at 30, 60 and 90 min after injection) and ice water immersion (at 60 min) decreased significantly (P < 0.005) compared with baseline. Mean plasma peak concentrations of M-6-G were 139.3 (SD 38.9) ng ml-1, measured at 15 min. Our data demonstrate that M-6-G has significant analgesic activity.
Buetler
T M
TM
Department of Clinical Research, University of Bern, Switzerland.
Wilder-Smith
O H
OH
Wilder-Smith
C H
CH
Aebi
S
S
Cerny
T
T
Brenneisen
R
R
D000328:Adult; D000701:Analgesics, Opioid / Q000097:blood / Q000627:therapeutic use*; D003080:Cold Temperature; D004558:Electric Stimulation; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D008875:Middle Aged; D009022:Morphine Derivatives / Q000097:blood / Q000627:therapeutic use*; D010147:Pain Measurement; D010149:Postoperative Pain / Q000517:prevention & control*
D000701:Analgesics, Opioid; D009022:Morphine Derivatives; C035349:morphine-6-glucuronide