Acute, tolerance to cocaine in humans

John J. Ambre*, Steven M. Belknap, John Nelson, Tsuen Ih Ruo, Sang Goo Shin, Arthur J. Atkinson

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

103 Scopus citations

Abstract

There is controversy as to whether acute tolerance develops to the principal effects of cocaine in humans. The studies described here demonstrate the phenomenon of acute tolerance to cocaine chronotropic and subjective effects and the rate and extent of tolerance development. Stable plasma cocaine concentrations were produced and then maintained in volunteer cocaine users by administering an intravenous cocaine injection. followed by a cocaine infusion designed to compensate for the plasma clearance of cocaine. The euphoric effect (high) intensified to a peak at about 1 hour and then declined toward baseline at 4 hours despite the presence of constant plasma cocaine levels. The chronotropiic effect reached a peak within 10 minutes and then declined, with a half-life of 31 ± 13 (mean ± SD) minutes toward a plateau at 33% ± 7.1% of its peak intensity. Tolerance development was quantified as an exponential process, with a rate constant (tolerance factor) accounting for the progressive alteration of the cocaine concentration-effect relationship.

Original languageEnglish (US)
Pages (from-to)1-8
Number of pages8
JournalClinical pharmacology and therapeutics
Volume44
Issue number1
DOIs
StatePublished - Jul 1988

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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