Tolerance to analgesia and dependence liability by topical application of dihydroetorphine to hairless rats.

Abstract:

:The tolerance to analgesia and dependence liability of dihydroetorphine following topical application were investigated in hairless rats with and without formalin-induced inflammation. The analgesic effect of dihydroetorphine (s.c.) was 4600- to 7200-fold more potent than that of morphine. In non-inflamed rats, the analgesic effect of 24-h topical application of dihydroetorphine tape (35 microg) and 4-day repeated tape applications (20 microg/5 h/day) decreased with time after the start of application, even though the plasma dihydroetorphine concentrations did not decrease. In formalin-inflamed rats, however, the tolerance to analgesia diminished. Naloxone-precipitated weight loss was observed after 24-h infusion of dihydroetorphine but not after the tape application in non-inflamed rats. A significant rewarding effect was found in the non-inflamed rats conditioned by s.c. injection and tape application but not in the formalin-inflamed rats. These results indicate that topical application of dihydroetorphine has a tolerance and dependence liability when there is no pain, and therefore, it should be used only for pain relief.

journal_name

Eur J Pharmacol

authors

Ohmori S,Fang L,Kawase M,Saito S,Morimoto Y

doi

10.1016/s0014-2999(01)01098-6

keywords:

subject

Has Abstract

pub_date

2001-07-06 00:00:00

pages

157-66

issue

2-3

eissn

0014-2999

issn

1879-0712

pii

S0014299901010986

journal_volume

423

pub_type

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