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Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
CYP2D6 plays an important role in the metabolism of many indolealkylamines agents, which are 5-hydroxytryptamine (5-HT/serotonin) analogs that mainly act on the serotonin system (Yu 2008). Structurally, this group of compounds contains an indole moiety and a basic nitrogen atom, which are connected by an alkyl chain usually of two carbons in length. They mainly act on the 5-HT receptors, and some indolealkylamines such as ergotamine and a series of triptans including sumatriptan, zolmitriptan, naratriptan, almotriptan, frovatriptan, and rizatriptan have been developed for the clinical treatment of migraine (Saper and Silberstein 2006). However, many other indolealkylamine agents are widely abused compounds in developed countries although some have demonstrated therapeutic potential in psychopharmacotherapy. These include the notorious lysergic acid amides such as D-lysergic acid diethylamide and ergine; tryptamine derivatives such as psilocybin (O-phosphoryl-4-hydroxy-N,N-dimethyltryptamine), N,N-dimethyltryptamine (DMT), bufotenine (5-hydroxy-dimethyltryptamine), 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT), and 5-methoxy-N,N-diisopropyltryptamine (5-MeO-DIPT, “Foxy,” or “Foxy Methoxy”); and β-carbolines such as harman, harmaline, harmine, and ibogaine (Yu 2008). All these compounds produce hallucinogenic and stimulant activities and high doses of administration will cause mydriasis, nausea, jaw clenching, and overt hallucinations with auditory and visual distortions.
Hallucinogen persisting perceptual disorder: a scoping review covering frequency, risk factors, prevention, and treatment
Published in Expert Opinion on Drug Safety, 2022
Marcus A. Doyle, Susan Ling, Leanna M.W. Lui, Paul Fragnelli, Kayla M. Teopiz, Roger Ho, Joshua D. Di Vincenzo, Joshua D. Rosenblat, Emily S. Gillissie, Danica Nogo, Felicia Ceban, Muhammad Youshay Jawad, Roger S. McIntyre
Psilocybin [31,37,45], phencyclidine, ibogaine [43], and 5-methoxy-N,N-diisopropyltryptamine (5-MeO DiPT) [38] have all been associated with HPPD onset. Ibogaine and 5-MeO DiPT were associated with HPPD onset [38,43]; meanwhile, psilocybin and phencyclidine were found to be associated with HPPD only when used in combination with other drugs [31,37,45]. However, each of the aforementioned drugs was indicated in three or fewer case reports, making it hard to interpret whether they are frequently associated with HPPD alone or when used in combination with other drugs.