Cocaethylene (CE)

Cocaethylene is a psychoactive metabolite produced in the liver when cocaine and ethanol are consumed simultaneously [1.2.1, 1.2.2]. It is formed through the transesterification of cocaine by the enzyme carboxylesterase 1, representing a rare instance of a new drug being synthesized entirely within the human body [1.2.4, 1.4.1]. Biologically, it functions as a triple reuptake inhibitor (SNDRI), blocking the transporters for dopamine, serotonin, and norepinephrine [1.2.2, 1.3.1]. This action increases synaptic concentrations of these monoamines, leading to enhanced euphoria and reinforcing effects [1.2.1, 1.4.2]. However, cocaethylene is significantly more toxic than cocaine, particularly to the cardiovascular system and the liver [1.1.2, 1.2.4]. It has a longer elimination half-life than cocaine, which prolongs the duration of its physiological and toxic effects [1.2.2, 1.4.2]. Clinical risks associated with its formation include an 18- to 25-fold increase in the risk of sudden cardiac death compared to cocaine use alone [1.2.2, 1.2.5]. It also contributes to increased rates of seizures, hepatotoxicity, and impulsive or violent behavior [1.1.2, 1.2.5]. In forensic and clinical settings, the detection of cocaethylene in blood, urine, or hair serves as a definitive biomarker for the co-ingestion of alcohol and cocaine [1.2.2, 1.3.1]. Understanding its pharmacology is essential for managing polydrug overdose and assessing long-term health risks in substance users [1.2.4, 1.4.1].

Other names

EthylbenzoylecgonineBenzoylecgonine ethyl esterEthylcocaineCocaine ethyl ester

Inhibition of dopamine, serotonin, and norepinephrine transporters (SNDRI)