Lack of effect of sublingual salvinorin A, a naturally occurring kappa opioid, in humans: a placebo-controlled trial.
John Mendelson, Jeremy Coyle, Juan Carlos Lopez, Matthew J. Baggott, Keith Flower, E Thomas Everhart, Thomas A Munro, Gantt P. Galloway, Bruce M Cohen
Psychopharmacology April 1, 2011 DOI: 10.1007/s00213-010-2103-5 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Placebo-controlled ascending-dose design Peer reviewed |
|---|---|
| Sample size | 8 |
| Population | Salvia divinorum-experienced subjects |
| Intervention | Salvinorin A |
| Dose | up to 4 mg |
| Topics | Salvia divinorum |
| Keywords | Bioavailability Sublingual administration Pharmacology |
| Citations | 40 |
| Key points | Sublingual salvinorin A at doses up to 4 mg produced no greater physiological or subjective effects than placebo and had low bioavailability. |
Abstract
Salvinorin A (SA) is a highly selective kappa opioid receptor agonist and the putative psychoactive compound in Salvia divinorum (SD), an increasingly abused hallucinogenic plant. The objectives of this study were to characterize the physiological and subjective effects of SA versus placebo and measure drug and metabolite levels. Sublingual SA doses up to 4 mg were administered in dimethyl sulfoxide/polyethylene glycol 400 solution to eight SD-experienced subjects using a placebo-controlled ascending-dose design. No dose of SA produced significantly greater physiological or subjective effects than placebo. Furthermore, effects did not resemble reported "typical" effects of smoked SD. SA was detectable in plasma and urine, but was, in most cases, below the reliable limit of quantification (0.5 ng/mL). Our results suggest that the sublingual bioavailability of SA is low. Higher doses, alternate formulations, or alternate routes of administration will be necessary to study the effects of SA in humans.