British Journal of Anaesthesia, 1985, Vol. 57, No. 2 192-196
© 1985 The Board of Management and Trustees of the British Journal of Anaesthesia
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CLINICAL ACTIONS OF FENTANYL AND BUPRENORPHINE
The Significance of Receptor Binding
Section of Anaesthetics, and Department of Pharmacology and Clinical Pharmacology, University of Auckland School of Medicine Private Bag, Auckland, New Zealand
Receptor binding assays were undertaken in an attempt to elucidate the opioid binding characteristics of fentanyl and buprenorphine, and to investigate some of the differences between them. Buprenorphine showed slow receptor association (30 min), but with high affinity to multiple sites from which dissociation was very slow (T
= 166 min) and incomplete (50% binding after 1 h). This contrasted with the receptor binding of fentanyl, which achieved rapid equilibrium (within 10 min) and dissociated equally rapidly (T = 6.8 min) and completely (100% by 1 h). Competitive displacement showed buprenorphine displacement of fentanyl binding was concentration-and time-dependent over ranges encountered in clinical use, but buprenorphine binding was displaced with only very high concentrations of other opioids. These findings offer pharmacodynamic explanations for the differences in fentanyl and buprenorphine analgesic response profiles and suggest how binding interactions might be applied to therapeutic use.
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