Comparison of intravenous cocaethylene and cocaine in humans.
BACKGROUND
Cocaethylene is a pharmacologically active homolog and metabolite of cocaine, formed by transesterification of cocaine in the presence of ethanol. Here we relate findings from a randomized, placebo-controlled, double-blind study in which we examined the physiological and subjective effects and pharmacokinetics of i.v. administered cocaethylene in human volunteers using cocaine as a comparator.


METHODS
Cocaine-dependent participants randomly received one study drug, cocaethylene (0.25 or 0.5 mg/kg), cocaine (0.25 or 0.5 mg/kg), or placebo, during each experimental session which occurred on separate days.


RESULTS
Cocaethylene was less potent in elevating heart rate than equivalent doses of cocaine. Similar differences between cocaine and cocaethylene were found for subjective measures ("Cocaine High", "Rush", "Stimulated" and "Good Drug Effects"). All active drug conditions produced significant increases in systolic blood pressure relative to placebo, but no significant effect on diastolic blood pressure was observed. Cocaethylene demonstrated a slower clearance, larger volume of distribution and correspondingly longer elimination half-life than cocaine.


CONCLUSIONS
The findings from this study confirm those of previous studies that show that cocaethylene has pharmacological properties in common with cocaine, but is less potent.
Hart
C L
CL
Yale University School of Medicine, Department of Psychiatry and Laboratory Medicine, West Haven, Connecticut, USA.
Jatlow
P
P
Sevarino
K A
KA
McCance-Katz
E F
EF
D000328:Adult; D001794:Blood Pressure / Q000187:drug effects; D003042:Cocaine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology*; D019970:Cocaine-Related Disorders / Q000378:metabolism / Q000503:physiopathology; D018765:Dopamine Uptake Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology; D004311:Double-Blind Method; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D014662:Vasoconstrictor Agents / Q000493:pharmacokinetics / Q000494:pharmacology
D018765:Dopamine Uptake Inhibitors; D014662:Vasoconstrictor Agents; C066444:cocaethylene; D003042:Cocaine