Back to Search
Start Over
The pharmacology of cocaethylene in humans following cocaine and ethanol administration
- Source :
- Drug and alcohol dependence. 72(2)
- Publication Year :
- 2003
-
Abstract
- Background: Concurrent use of cocaine and alcohol results in formation of a cocaine homolog and metabolite—cocaethylene. Methods: To characterize cocaethylene pharmacology, ten paid volunteer subjects were given deuterium-labeled (d 5 ) cocaine (0.3, 0.6, and 1.2 mg/kg and cocaine placebo) by a 15-min constant rate intravenous injection 1 h after a single oral dose of ethanol (1 g/kg) or ethanol and cocaine placebo using a double-blind, crossover design. Six of the same volunteers subsequently received a 1.2 mg/kg dose of cocaine alone. A small (7.5 mg) nonpharmacologically active dose of deuterium-labeled cocaethylene-d 3 was concurrently administered with the cocaine to enable calculation of absolute cocaethylene formation and clearance. Plasma and urine cocaine, cocaethylene, and benzoylecgonine concentrations, physiologic and subjective effects were measured. Results: When co-administered with ethanol, 17±6% (mean±S.D.) of the cocaine was converted to cocaethylene. Cocaethylene peak plasma concentrations and AUC increased proportionally to the cocaine dose. Ethanol ingestion prior to cocaine administration decreased urine benzoylecgonine levels by 48% and increased urinary cocaethylene and ecgonine ethyl ester levels. Subjects liked and experienced more total intoxication after the combination of cocaine and ethanol than after either drug alone. Conclusions: In the presence of ethanol, the altered biotransformation of cocaine resulted in 17% of an intravenous cocaine dose being converted to cocaethylene and relatively lower urinary concentrations of benzoylecgonine.
- Subjects :
- Adult
Male
Metabolic Clearance Rate
Blood Pressure
Urine
Pharmacology
Toxicology
chemistry.chemical_compound
Cocaethylene
Pharmacokinetics
Cocaine
Dopamine Uptake Inhibitors
Double-Blind Method
Heart Rate
Medicine
Humans
Pharmacology (medical)
Drug Interactions
Volunteer
Chromatography
Ethanol
Cross-Over Studies
Dose-Response Relationship, Drug
business.industry
Crossover study
Psychiatry and Mental health
chemistry
Benzoylecgonine
Female
business
Ecgonine
medicine.drug
Subjects
Details
- ISSN :
- 03768716
- Volume :
- 72
- Issue :
- 2
- Database :
- OpenAIRE
- Journal :
- Drug and alcohol dependence
- Accession number :
- edsair.doi.dedup.....bdbabff84821bcdfae02e4f79033fd58