Abstract:
:Cross-tolerance to the respiratory depression induced by i.c.v. [D-Ala2,D-Leu5]enkephalin (DADLE) and by s.c., i.c.v. and i.v. morphine was studied in anesthetized rats that had been rendered tolerant to s.c. sufentanil (4 micrograms/h per 7 days). Tolerance induced by i.c.v. sufentanil was also compared during withdrawal and its absence. Tolerance was evaluated by estimation of the changes in both the maximum attained reduction of respiratory frequency (Emax) and the area under the time-course curve for the effects (AUC). In contrast to the failure to develop tolerance, as estimated with the Emax, after i.c.v. sufentanil in the absence of abstinence (tolerance index: 1.1), rats displayed significant degrees of cross-tolerance to i.c.v. morphine (3.6), i.c.v. DADLE (4.3) and s.c. morphine (6.6). No tolerance, however, was obtained to i.v. morphine. Tolerance to i.c.v. sufentanil in non-abstinent rats was not present when the Emax was considered but was when AUC was considered. During withdrawal animals showed tolerance as estimated with both the Emax and AUC. These results complement previous findings and show that the appearance of dissimilar degrees of cross-tolerance to different agonists depends not only on their intrinsic activities but also on their pharmacokinetic properties. These observations, along with the critical influence of withdrawal upon the manifestation of tolerance, support the need to distinguish between the development of the tolerance state and the degree of tolerance that can be expressed under specific conditions.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Ayesta FJ,Flórez Jdoi
10.1016/0014-2999(90)90145-vsubject
Has Abstractpub_date
1990-01-03 00:00:00pages
1-12issue
1eissn
0014-2999issn
1879-0712pii
0014-2999(90)90145-Vjournal_volume
175pub_type
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