Influence of phendimetrazine maintenance on the reinforcing, subjective, performance, and physiological effects of intranasal cocaine

Psychopharmacology (Berl). 2019 Sep;236(9):2569-2577. doi: 10.1007/s00213-019-05227-x. Epub 2019 Mar 21.

Abstract

Rationale: No pharmacotherapies are approved for cocaine use disorder. Phendimetrazine, a prodrug of the monoamine-releaser phenmetrazine, attenuates the reinforcing effects of cocaine in preclinical models, has minimal abuse potential, and is safe when combined with cocaine.

Objectives: This study determined the influence of phendimetrazine maintenance on the reinforcing effects of cocaine (i.e., choice to self-administer cocaine), along with the subjective, performance, and physiological effects of cocaine. We hypothesized that phendimetrazine would attenuate the reinforcing effects of cocaine.

Methods: Twenty-nine subjects with cocaine use disorder completed this within-subject, inpatient study. The subjects were maintained on placebo and 210 mg phendimetrazine in a counterbalanced order. After at least 7 days of maintenance on the target dose, the subjects completed experimental sessions in which the effects of single doses of 0, 20, 40, and 80 mg of intranasal cocaine were determined.

Results: Cocaine functioned as a reinforcer, producing significant dose-related increases in self-administration. Cocaine increased prototypic effects (e.g., ratings of stimulated and blood pressure). Phendimetrazine attenuated ratings on a select set of subjective outcomes (e.g., ratings of talkative/friendly), but failed to reduce the reinforcing effects of cocaine or a majority of positive subjective cocaine effects. Phendimetrazine increased heart rate, indicating a physiologically active dose was tested, but heart rate increases were not clinically significant.

Conclusions: These results indicate that although phendimetrazine can safely be combined with cocaine, it does not attenuate the abuse-related effects of cocaine. It is unlikely, then, that phendimetrazine will be an effective standalone treatment for cocaine use disorder.

Keywords: Behavioral economic demand; Cocaine; Humans; Pharmacotherapy; Phendimetrazine; Self-administration.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Administration, Intranasal
  • Adult
  • Blood Pressure / drug effects
  • Blood Pressure / physiology
  • Central Nervous System Stimulants / administration & dosage*
  • Cocaine / administration & dosage*
  • Dopamine Uptake Inhibitors / administration & dosage*
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Drug Synergism
  • Female
  • Humans
  • Male
  • Middle Aged
  • Morpholines / administration & dosage*
  • Psychomotor Performance / drug effects*
  • Psychomotor Performance / physiology
  • Reinforcement, Psychology*
  • Self Administration

Substances

  • Central Nervous System Stimulants
  • Dopamine Uptake Inhibitors
  • Morpholines
  • phendimetrazine
  • Cocaine