Goodman & Gilman's The Pharmacological Basis of Therapeutics, 11e
|III. Drugs Acting on the Central Nervous System >|
Opioid Agonist/Antagonists and Partial Agonists
Sections: Opioid Agonist/Antagonists
and Partial Agonists, Pentazocine, Pharmacological
Actions, Nalbuphine, Pharmacological
Actions and Side Effects, Tolerance and
Physical Dependence, Therapeutic
Uses, Butorphanol, Pharmacological
Actions and Side Effects, Therapeutic
Uses, Buprenorphine , Pharmacological
Actions and Side Effects, Physical Dependence, Therapeutic
Topics Discussed: buprenorphine; butorphanol; nalbuphine; opiate agonist-antagonist; opiate partial agonist; opioid analgesics; pain management; pentazocine.
Excerpt:"The drugs described in this section differ from clinically used -opioid receptor agonists. Drugs such
competitive -receptor antagonists
but exert their analgesic actions by acting as agonists at receptors.
Pentazocine qualitatively resembles these drugs, but it may be a
weaker -receptor antagonist or partial
agonist while retaining its -agonist activity.
Buprenorphine, on the other hand, is a partial agonist at receptors. The stimulus for the development
of mixed agonist–antagonist drugs was a need for analgesics
with less respiratory depression and addictive potential. The clinical
use of these compounds is limited by undesirable side effects and
limited analgesic effects.
Pentazocine was synthesized as part of a deliberate
effort to develop an effective analgesic with little or no abuse