BUTYRYLCHOLINESTERASE - AN ENZYME ANTIDOTE FOR COCAINE INTOXICATION

Cocaine-associated toxicity is the result of effects on the cardiovasc ular and central nervous systems. Since the primary route of cocaine i nactivation is enzymatic degradation by butyrylcholinesterase (BChE), we sought to determine if the administration of purified human enzyme would ameliorate the lethal effects of cocaine. While the cardiovascul ar, autonomic or central nervous systems were unaffected by BChE, the enzyme reduced the adverse effects of cocaine including hypertension, hyperactivity and convulsions. BChE decreased both the brain and blood levels of cocaine and shifted the metabolites towards the production of the inactive product ecgonine methyl ester and away from the physio logically active metabolites, norcocaine and benzoylecgonine. We concl ude that BChE would appear to be an ideal antidote in the treatment of cocaine intoxication and has potential therapeutic application.