PT  - JOURNAL ARTICLE
AU  - Gilberto N. Carmona
AU  - Rebecca A. Jufer
AU  - Steven R. Goldberg
AU  - David A. Gorelick
AU  - Nigel H. Greig
AU  - Qian-Sheng Yu
AU  - Edward J. Cone
AU  - Charles W. Schindler
TI  - Butyrylcholinesterase Accelerates Cocaine Metabolism: In Vitro and In Vivo Effects in Nonhuman Primates and Humans
DP  - 2000 Mar 01
TA  - Drug Metabolism and Disposition
PG  - 367--371
VI  - 28
IP  - 3
4099  - http://dmd.aspetjournals.org/content/28/3/367.short
4100  - http://dmd.aspetjournals.org/content/28/3/367.full
SO  - Drug Metab Dispos2000 Mar 01; 28
AB  - Butyrylcholinesterase (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.