This plant was likely to have been used by pastoralists and hunter-gatherers as a mood-altering substance from prehistoric times. The earliest written records of the use of the plant date back to 1662 and 1685. The traditionally prepared dried plant material is chewed, or smoked, or powdered and inhaled as a snuff. Sceletium elevates mood and decreases anxiety, stress and tension. In intoxicating doses it can cause a euphoria, initially with stimulation and later with sedation. The plant is not hallucinogenic, and no severe adverse effects have been documented.

The active constituents of the plant are alkaloids, including mesembrine, mesembrenone, mesembrenol and tortuosamine. The alkaloid concentration in the dry material ranges from 0.05 to 2.3%. Mesembrine is usually the major alkaloid present, and has been demonstrated in laboratory studies to be a very potent serotonin-uptake inhibitor. This receptor-specific activity, and some receptor activities found on nicotinic, dopamine and nor-adrenaline sites certainly validate the traditional uses, and suggest additional therapeutic potential.

CAUTION!!!The National Institute of Mental Health in the United States have found Memembrine the principle alkaloid responsible for psychoactivity in Sceletium Tortuosum to be a serotonin-uptake inhibitor, keeping more serotonin in circulation, like Prozac. Since Prozac/SSRI's are contraindicated with MAOI, this would also go for Mesembrine. Also the results of taking it ontop of other SSRI's are unpredictable, and it is known that alcohol can also cause side effects combined with many SSRI's. Headaches in conjunction with alcohol have been noted with sceletium use.