Metabolism of lysergic acid diethylamide (LSD): an update

Lysergic acid diethylamide (LSD), the most potent known hallucinogen, exerts its pharmacological effects by stimulating central serotonin receptors (5-HT2). Despite its low toxicity and physiological safety, renewed therapeutic interest has emerged. This review discusses LSD metabolism, detailing all metabolites and their clinical and toxicological relevance. LSD is rapidly and extensively metabolized into inactive metabolites, which have a longer detection window than the parent compound. The major human metabolite, 2-oxo-3-hydroxy LSD, is crucial for clinical and forensic toxicology. However, information on LSD pharmacokinetics in humans remains limited, highlighting the need for further research.

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Abstract

Lysergic acid diethylamide (LSD) is the most potent hallucinogen known and its pharmacological effect results from stimulation of central serotonin receptors (5-HT2). Since LSD is seen as physiologically safe compound with low toxicity, its use in therapeutics has been renewed during the last few years. This review aims to discuss LSD metabolism, by presenting all metabolites as well as clinical and toxicological relevance. LSD is rapidly and extensively metabolized into inactive metabolites; whose detection window is higher than parent compound. The metabolite 2-oxo-3-hydroxy LSD is the major human metabolite, which detection and quantification is important for clinical and forensic toxicology. Indeed, information about LSD pharmacokinetics in humans is limited and for this reason, more research studies are needed.