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Behavioral and toxicological effects of propofol
Michael B Gatch1, Michael J Forster
1Department of Pharmacology and Neuroscience, University of North Texas Health Science Center, 3500 Camp Bowie Blvd, Fort Worth, TX 76107-2699, USA. michael.gatch@unthsc.edu
Behavioural Pharmacology
|September 17, 2011
Summary
Propofol, a common anesthetic, shows abuse potential in rats, mimicking drugs like carisoprodol. High mortality rates and cardiovascular issues in the study highlight concerns about propofol abuse.
Area of Science:
- Neuroscience
- Pharmacology
- Drug Abuse Research
Background:
- Propofol is a widely used anesthetic and sedative.
- Currently, propofol is not a controlled substance, raising concerns about its potential for abuse.
- Understanding the abuse liability and mechanisms of propofol is crucial.
Purpose of the Study:
- To establish a rat model for studying the psychoactive effects of subanesthetic doses of propofol.
- To assess the abuse liability of propofol using a discriminative-stimulus paradigm.
- To investigate the neurobiological mechanisms underlying propofol's effects.
Main Methods:
- Sprague-Dawley rats were trained to discriminate propofol from a vehicle.
- Substitution tests were conducted with known psychoactive drugs (carisoprodol, chlordiazepoxide, dizocilpine) and pentylenetetrazol.
- Propofol was also tested for its discriminative effects in rats trained to discriminate carisoprodol.
Main Results:
- Propofol successfully served as a discriminative stimulus in rats.
- Carisoprodol and chlordiazepoxide showed some substitution for propofol's effects, while dizocilpine did not.
- A significant mortality rate (38%) was observed during propofol training, with postmortem findings of cardiovascular abnormalities.
- Propofol's effects were more aligned with GABA-A receptor modulators than NMDA receptor antagonists.
Conclusions:
- Propofol can be modeled as a discriminative stimulus, indicating potential abuse liability.
- The study highlights similarities between propofol's discriminative effects and those of known drugs of abuse.
- The high mortality rate and observed cardiovascular effects underscore the risks associated with propofol abuse.
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