title: A randomized, double-blind, placebo-controlled trial of RBP-8000 in cocaine abusers: pharmacokinetic profile of rbp-8000 and cocaine and effects of RBP-8000 on cocaine-induced physiological effects.
abstract: RBP-8000 is a double mutant cocaine esterase that rapidly metabolizes cocaine. This study was conducted to assess the pharmacokinetics of cocaine and cocaine-induced physiological effects in the absence (placebo) or presence of RBP-8000. Twenty-nine cocaine abusers were randomized 1:1 (active: placebo) to 4 sequences and 2 treatment periods. In the presence of RBP-8000, cocaine plasma exposures dropped by 90% within 2 min; cocaine-induced physiological effects were significantly reduced with higher extent and faster decrease in systolic blood pressure and pulse rate compared to placebo. This study provides strong evidence in support to use RBP-8000 as a pharmacotherapy for cocaine intoxication.
authors.affiliation: a Reckitt Benckiser Pharmaceuticals Inc. , Richmond , Virginia , USA.
authors.forename: Azmi F
authors.initials: AF
authors.lastname: Nasser
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Fudala
authors.forename: Bo
authors.initials: B
authors.lastname: Zheng
authors.forename: Yongzhen
authors.initials: Y
authors.lastname: Liu
authors.forename: Christian
authors.initials: C
authors.lastname: Heidbreder
mesh_terms: D000328:Adult; D001794:Blood Pressure / Q000187:drug effects* / Q000502:physiology; D002265:Carboxylic Ester Hydrolases / Q000493:pharmacokinetics*; D003042:Cocaine / Q000097:blood*; D019970:Cocaine-Related Disorders / Q000188:drug therapy*; D018592:Cross-Over Studies; D018765:Dopamine Uptake Inhibitors / Q000097:blood*; D004311:Double-Blind Method; D005260:Female; D006339:Heart Rate / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D008297:Male; D008875:Middle Aged; D016896:Treatment Outcome; D055815:Young Adult
chemical_list: D018765:Dopamine Uptake Inhibitors; D002265:Carboxylic Ester Hydrolases; C019921:cocaine esterase; D003042:Cocaine
keywords: (–)ecgonine methyl ester; Pharmacokinetics; cocaine; cocaine esterase; cocaine-abuse