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Pharmacokinetics and pharmacodynamics of morphine-3-glucuronide in rats and its influence on the antinociceptive effect of morphine

✍ Scribed by Marianne Ekblom; Marie Gårdmark; Margareta Hammarlund-Udenaes

Publisher
John Wiley and Sons
Year
1993
Tongue
English
Volume
14
Category
Article
ISSN
0142-2782

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✦ Synopsis

In this study the pharmacokinetics and pharmacodynamics of morphine-3-glucuronide (M3G) were investigated in rats after i.v. administration as a bolus dose (86.7 pmol kg-I) and as a constant rate infusion (2.9 pmol h-') over 5 days. After the bolus dose, the clearance (Cl) was 12.1 ~0.6mlmin-**kg, the volume of distribution at steady state (V,J 1-68+0.891kg-', the half-life of the first phase 13.2+1-8min and the halflife of the second phase 11.6+7-7 h. After the constant rate infusion, C1 was 10.5 + 1 *7 ml min-'*kg. The antagonistic effect of M3G on the antinociceptive effect of a bolus dose of morphine (35pmolkg-') was tested during steady state concentrations of M3G on day 4 and to M3G naive rats. No antinociceptive, hyperalgesic or withdrawal effects were observed as a result of M3G administration, but a significantly lower antinociceptive effect of morphine was found in the M3G infusion group compared to the control group. Systemically administered M3G antagonized the antinociceptive effect of morphine, but this cannot be the only explanation to the tolerance development observed after morphine administration.

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