An overview of cocaethylene, an alcohol-derived,
psychoactive, cocaine metabolite
by
MJ Landry
Training and Education Project,
Haight Ashbury Free Clinics.
J Psychoactive Drugs, 1992 Jul-Sep, 24:3, 273-6
ABSTRACTCocaethylene is a psychoactive ethyl homologue of cocaine, and is formed exclusively during the coadministration of cocaine and alcohol. Not a natural alkaloid of the coca leaf, cocaethylene can be identified in the urine, blood, hair, and neurological and liver tissue samples of individuals who have consumed both cocaine and alcohol. With a pharmacologic profile similar to cocaine, it can block the dopamine transporter on dopaminergic presynaptic nerve terminals in the brain. It increases dopamine synaptic content, provoking enhanced postsynaptic receptor stimulation, resulting in euphoria, reinforcement, and self-administration. Equipotent to cocaine with regard to dopamine transporter affinity, cocaethylene appears to be far less potent than cocaine with regard to serotonin transporter binding. Lacking the serotonergic-related inhibitory mechanism, cocaethylene appears to be more euphorigenic and rewarding than cocaine. Synthesized and administered cocaethylene has a behavioral stimulation profile similar to cocaine. Cocaethylene has been shown to be less potent and equipotent to cocaine, and alcohol plus cocaine produces more stimulatory locomotor behavior in mice than either drug alone. Equipotent to cocaine with regard to primate reinforcement and self-administration, cocaethylene can substitute for cocaine in drug discrimination studies, and can produce stimulation of operant conditioning in rats. With regard to lethality, cocaethylene has been shown to be more potent than cocaine in mice and rats. The combination of cocaine and alcohol appears to exert more cardiovascular toxicity than either drug alone in humans. Alcohol appears to potentiate cocaine hepatotoxicity in both humans and mice.Cocaine
Dopamine
Supercoke
Cocaethylene
Noradrenaline
Cocaine hotspots
Cocaine withdrawal
The coke-craving brain
Cocaethylene metabolism
The neural basis of addiction
Freebasing flies go hyperkinetic
Cocaine, alcohol and cocaethylene
Cocaethylene and cocaine dependence
The bacterial junkie: Rhodococcus sp. strain MB1
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