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Opiate mixed agonist-antagonist interactions with histamine antagonists vs. morphine
Neurobehavioral Toxicology and Teratology
|September 1, 1985
Summary
Drug interactions between tripelennamine and mixed agonist-antagonists were studied in mice. Cyclazocine demonstrated a unique mechanism, distinct from other tested compounds, suggesting separate antinociceptive pathways.
Area of Science:
- Pharmacology
- Neuroscience
- Drug Interactions
Background:
- Polydrug abuse involving tripelennamine and pentazocine has been anecdotally reported.
- Mixed agonist-antagonists are used clinically, but their interactions with other drugs require further investigation.
Purpose of the Study:
- To investigate drug interactions between tripelennamine and various synthetic mixed agonist-antagonists in a mouse model.
- To elucidate the distinct mechanisms of action for different mixed agonist-antagonists.
Main Methods:
- Administered tripelennamine, morphine, and several mixed agonist-antagonists (pentazocine, nalbuphene, butorphanol, cyclazocine) to mice.
- Assessed antinociceptive activity and drug potentiation or blockade.
- Investigated the effect of cimetidine on drug responses.
Main Results:
- Pentazocine, nalbuphene, and butorphanol potentiated tripelennamine's antinociceptive effects.
- Cyclazocine, unlike other mixed agonist-antagonists, blocked tripelennamine's effects and abolished morphine's antinociception.
- Cimetidine blocked cyclazocine's response but not that of other mixed agonist-antagonists.
Conclusions:
- Cyclazocine exhibits a unique mechanism of action compared to other mixed agonist-antagonists studied.
- Findings suggest potential histaminergic involvement in antinociception.
- A distinct locus for antinociception separate from the opiate receptor may exist.