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An experimental study on dependence liability of zipeprol
V Moretti1, C Concettoni, P Giusti
1Institute of Experimental and Clinical Medicine, University of Ancona, Italy.
Pharmacological Research
|March 1, 1989
Summary
Zipeprol, a widely used antitussive, acts as a moderate opioid agonist. It also exhibits a direct anticholinergic effect, contrary to previous assumptions about its abuse liability.
Area of Science:
- Pharmacology
- Neuroscience
- Drug Abuse Studies
Background:
- Zipeprol is a piperazine ethanol derivative used as a pediatric antitussive.
- It is not legally recognized as having dependence or abuse potential.
Purpose of the Study:
- To investigate the pharmacological mechanisms underlying zipeprol's potential for abuse.
- To characterize zipeprol's interaction with opioid and cholinergic systems.
Main Methods:
- Radioligand binding assays using [3H]naloxone on rat brain homogenates.
- Field stimulation of guinea-pig ileum in the presence/absence of naloxone and yohimbine.
- In vitro inhibition of acetylcholine (ACh) response on guinea-pig ileum.
Main Results:
- Zipeprol demonstrated moderate opioid agonist activity, displacing [3H]naloxone.
- Zipeprol exhibited a direct anticholinergic effect on guinea-pig ileum.
- This anticholinergic effect was independent of presynaptic alpha 2 interactions.
Conclusions:
- Zipeprol possesses moderate opioid agonist properties.
- Zipeprol has a direct anticholinergic effect, contributing to its pharmacological profile.
- These findings suggest a potential for abuse liability not previously recognized.