ArticlePsychopharmacology2026
Neuropharmacology of levamisole and its phase I metabolites: lack of evidence for levamisole-cocaine interactions.
Article in Psychopharmacology, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
rationaleThe anthelmintic agent, levamisole, is a cocaine adulterant that causes serious adverse effects in humans. A number of hypotheses have been proposed to explain why levamisole is used as an adulterant. Here, we examined whether levamisole might enhance acute pharmacological effects of cocaine.
methodsLevamisole and its phase I metabolites were tested for in vitro activity at monoamine receptors and transporters. The effect of levamisole (0.1-10 µM) on cocaine-induced inhibition of [
resultsLevamisole displayed no measurable activity at monoamine receptors or transporters. The metabolite aminorex acted as a potent substrate at transporters for dopamine, norepinephrine and serotonin, whereas rexamino had affinity for adrenoreceptors and weak substrate activity at norepinephrine transporters. Levamisole did not alter cocaine-induced inhibition of dopamine uptake in vitro. Administration of cocaine, or cocaine plus levamisole, produced similar increases in extracellular dopamine and locomotor stimulation in vivo.
conclusionsWe found no evidence that levamisole alters the acute pharmacological effects of cocaine in male rats. The metabolite aminorex is a potent monoamine transporter substrate which could contribute to effects of levamisole under certain conditions (e.g., repeated, high-dose exposure), but most studies in human users of levamisole-adulterated cocaine have failed to detect measurable quantities of aminorex.
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