Pharmacokinetics and Concentration-Effect Relationship of Oral LSD in Humans
OrthoEvidence Journal (OE Journal) - ACE Report
OE Journal. 2022;10(12):73 Int J Neuropsychopharmacol. 2015 23-Feb;():. 10.1093/ijnp/pyv072What this means for my practice?
The pharmacokinetic profile of LSD exhibits first-order kinetics up to 12 hours. The concentrations of LSD were maximal after 1.5 hours (median) and gradually declined to very low levels by 12 hours. LSD produces physiological and psychotropic effects lasting up to 12 hours, closely related to the plasma concentrations of LSD and inhibiting no acute tolerance.
Study Summary
Sixteen healthy subjects were included in this double-blind, placebo-controlled, cross-over study examining the single-dose kinetics and pharmacokinetic-pharmacodynamic relationships of oral lysergic acid diethylamide (LSD). Participants were given 200 μg LSD or placebo over 2 experimental test sessions with a washout period of at least 7 days between sessions. LSD and 2-oxo-3-hydroxy-lysergic acid diethylamide (O-H-LSD) concentrations in plasma and urine were determined using a validated liquid-chromatography-tandem mass-spectrometry, and drug effect was measured using the visual analogue scale. The acute subjective and sympathomimetic responses to lysergic acid diethylamide lasted up to 12 hours and were closely associated with the concentrations in plasma over time. Maximal concentrations of lysergic acid diethylamide were reached 1.5 (median, range 0.5-4) hours after administration. One percent of the orally administered LSD was eliminated in urine as LSD, and 13% was eliminated as O-H-LSD within 24 hours.
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