Intranasal Cocaine: Dose Relationships of Psychological Effects and Plasma Levels

Abstract

We compared the psychological effects of three doses of intranasal cocaine hydrochloride (.2, .75, and 1.5 mg/kg) with cocaine plasma concentrations in four volunteers. Intranasal lidocaine hydrochloride (.2 mg/kg) was used as a topically active placebo. Peak "high" ratings were related to both dose and peak plasma concentrations. At a given plasma concentration, "high" ratings were greater when plasma levels were increasing than when they were decreasing. This indicates that acute tolerance by tachphylaxis occurred after single doses. The cocaine "high" was a pleasant feeling but was without distinctive sensations. The dramatic effects of intranasal cocaine on the street may be related to larger or repeated doses as well as the setting.

Concurrent cocaine-ethanol ingestion in humans: pharmacology, physiology, behavior, and the role of cocaethylene

“…This may have contributed to the more intense behavioral effects of the cocaine/ ethanol administration. The findings for intranasal cocaine alone administration in this study are similar to those of Wilkinson et al (1980), Jatlow (1988), and Jeffcoat et al (1989 with respect to its pharmacokinetics and to those of Van Dyke et al (1982), Fischman et al (1983), and Higgins et al (1990) with respect to time course of euphoria ("high"). The mechanism underlying the higher cocaine concentrations observed during cocaine/ethanol administration cannot be determined with certainty from this study.…”

“…A series of measures designed to assess subjective drug effects were administered. Visual analog scales included the Self-Rated Analog Scale measuring "high", "rush", "sleepy", "pleasant", and "desire for cocaine" and a second subject-rated version of the High Scale which specifically assessed cocaine "high" (Van Dyke et al 1982). The "high" item on the Self-Rated Analog Scale asked subjects to rate the overall "high" state without regard to whether the "high" was more similar to that of cocaine or ethanol.…”

Gender Effects Following Repeated Administration of Cocaine and Alcohol in Humans

“…Visual analog scales (Fischman et al, 1993) consisted of lines anchored at 0 mm = minimal and 100 mm = maximal, measuring Any High, Rush, Sleepy, Paranoid, Sad, Depressed, Nervous, Crash, Desire for cocaine, and Feel Good (a measure of overall state of physical and mental well-being). A second subject-rated version of the High Scale, a single 100 mm line with 5 equidistant anchors characterizing the quality of the "Cocaine High" (Van Dyke, 1982), was also collected.…”

Cocaine Addiction: Psychology and Neurophysiology

“…In both reports from individuals addicted to cocaine and human laboratory investigations (in which cocaine is administered to nonaddicted cocaine users), cocaine initially induces profound subjective well-being together with alertness (6,7,12,13). The fundamental effect of cocaine is the magnification of the intensity of almost all normal pleasures.…”