Butyrylcholinesterase accelerates cocaine metabolism: in vitro and in vivo effects in nonhuman primates and humans
by
Carmona GN, Jufer RA, Goldberg SR, Gorelick DA,
Greig NH, Yu QS, Cone EJ, Schindler CW
Preclinical Pharmacology Section,
National Institute on Aging,
National Institutes of Health,
Baltimore, Maryland 21224, USA.
[email protected]
Drug Metab Dispos 2000 Mar; 28(3):367-71
ABSTRACTButyrylcholinesterase (BChE) is known to metabolize cocaine in humans. In the present study, three different experiments were performed to determine whether the addition of horse serum-derived BChE would accelerate the metabolism of cocaine. In the first experiment, the addition of BChE to squirrel monkey plasma in vitro reduced the half-life of cocaine by over 80%, decreased the production of the metabolic product benzoylecgonine, and increased ecgonine methyl ester formation. The effect of BChE on cocaine metabolism was reversed by a specific BChE inhibitor. In the second, in vivo, experiment, exogenously administered BChE reduced peak cocaine concentrations when given to anesthetized squirrel monkeys. Finally, incubation of cocaine with added BChE in human plasma in vitro resulted in a decrease in cocaine half-life similar to that observed with squirrel monkey plasma. The magnitude of the decrease in cocaine half-life was proportional to the amount of added BChE. Together, these results indicate that exogenously administered BChE can accelerate cocaine metabolism in such a way as to potentially lessen the behavioral and toxic effects of cocaine. Therefore, BChE may be useful as a treatment for cocaine addiction and toxicity.CART
Cocaine
Metabolism
Ketoconazole
Cocaine hotspots
The coke-craving brain
Freebasing flies go hyperkinetic
Cocaine, alcohol and cocaethylene
Cocaethylene and cocaine dependence
Butyrylcholinesterase (BChE) enhancement01 02 03 04 05 06 07 08 09 10 11 12
13 14 15 16 17 18 19 20 21 22 23 24
Refs
MORE
HedWeb
Future Opioids
BLTC Research
Wirehead Hedonism
Paradise-Engineering
Utopian Pharmacology
The Hedonistic Imperative
When Is It Best To Take Crack Cocaine?
The Good Drug Guide
The Responsible Parent's Guide
To Healthy Mood Boosters For All The Family
