The DOI matches its Crossref record; 65 of the 65 references it cites were found in a registry or an index.
Metabolism of psilocybin and psilocin: clinical and forensic toxicological relevance
Abstract
Psilocybin and psilocin are controlled substances in many countries. These are the two main hallucinogenic compounds of the “magic mushrooms” and both act as agonists or partial agonists at 5-hydroxytryptamine (5-HT)2A subtype receptors. During the last few years, psilocybin and psilocin have gained therapeutic relevance but considerable physiological variability between individuals that can influence dose-response and toxicological profile has been reported. This review aims to discuss metabolism of psilocybin and psilocin, by presenting all major and minor psychoactive metabolites. Psilocybin is primarily a pro-drug that is dephosphorylated by alkaline phosphatase to active metabolite psilocin. This last is then further metabolized, psilocin-O-glucuronide being the main urinary metabolite with clinical and forensic relevance in diagnosis.
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Basic and Clinical Pharmacology
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Items 201–225 of 225
Primjena psihodelika u psihijatriji
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Psychotropic Substances and Sleep
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Psychedelic Drugs as Treatment Agents
Yehuda, R., Lepow, L., Bonnano, P. A., Zaretsky, T. G., Antonio, J. H., & Jagodnik, K. M. (2025) · doi:10.1093/med/9780197640654.003.0074
Exploring psilocybin’s role in mental health and palliative medicine: a path to improved well-being
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“After oral administration it is rapidly depho-sphorylated upon reaching an acidic environment, thus converting to psilocin [62].”
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The therapeutic use of psychedelic drugs: Legal, policy, and neuroscientific perspectives
Rahmani, S., Crupi, R., Riley, A. L., & Davidson, T. L. (2025) · Pharmacology Biochemistry and Behavior · doi:10.1016/j.pbb.2025.174087
Oo, A. P., Tseu, S., & Ponnusamy, A. (2025) · Cureus · doi:10.7759/cureus.96718
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The Potential Therapeutic Effects of MEAI in the Treatment of Alcohol Use Disorder
Ekhlasi, M., Frytz, A., & Nia, A. B. (2025) · Current Addiction Reports · doi:10.1007/s40429-025-00700-4
“After 24 h, almost 20% of psilocybin is excreted as psilocin-O-glucuronide, involving the UDP-glucuronyl transferase enzymes UGT1A9 and UGT1A10 [ 90, 94, 96].”
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“…minor oxidation metabolic pathway yielding a deep blue colour product with an o-quinone or iminoquinone structure, catalysed by hydroxyindole oxidases (e.g. ceruloplasmin, the copper containing oxidase of mammalian plasma and cytochrome oxidase) or non-enzymatically by Fe 3+ (Dinis-Oliveira 2017).”
InfluentialMushroom Waste Valorization: From By-products to High-Value Bioactives
Mahajan, A., Kamal, T., Mohana, T., Satheesh, N., & El-Mogy, M. M. (2025) · Springer eBooks · doi:10.1007/978-3-032-00789-6_12
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Psilocibina en depresión: mecanismos neurobiológicos y cambios cognitivos
Arias, A. V., Ramírez, M. C., López, A. H., & Becerra-Hernández, L. V. (2026) · Acta neurológica colombiana · doi:10.22379/anc.v42i1.1926
Synthesis and Characterization of Psilocybin Metabolites and Deuterated Analogs
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Psilocybin: Chemical Foundations and Emerging Therapeutic Potential
Patil, S. A., & Hunsberger, H. C. (2026) · Mini-Reviews in Medicinal Chemistry · doi:10.2174/0113895575429775260119043318 · Cited by 1
Zauberpilze im Fokus von Ökologie und Pharmazie
Hille‐Rehfeld, A. (2026) · Chemie in unserer Zeit · doi:10.1002/ciuz.70056
Salgaço, M. K., Farias, D. D. P., de Souza, M. Z., Sartoratto, A., Bottino, F., Barud, H. D. S., de Oliveira, F. L., de Medeiros, A. I., Raimundo, B. V. B., Nascimento, V. H., et al. (2026) · Drugs and Drug Candidates · doi:10.3390/ddc5030046
Microbiome: Artifacts in forensic toxicology qualitative and quantitative analysis
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Self-citationThomas, J. E., & Saxena, J. (2026) · Elsevier eBooks · doi:10.1016/b978-0-443-44037-3.00043-9
Tai, M. L., Szigeti, B., Downey, A. E., Aday, J. S., Fredenburg, L., Sakai, K., Molina, C., Fernandes‐Osterhold, G., Bradley, E., Pantoni, M. M., et al. (2026) · Journal of Psychopharmacology · doi:10.1177/02698811261478603
P31-17 Psilocin as a Broad CYP450 Inhibitor: Evidence from Enzymatic Assays and Molecular Dynamics
da Silva, D. D., Brito-da-Costa, A. M., Carvalho, M., Dinis‐Oliveira, R. J., Madureira-Carvalho, Á., & Sousa, S. F. (2026) · Toxicology Letters · doi:10.1016/j.toxlet.2026.112868
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“…PSI is a prodrug with negligible activity of its own: following oral administration, it is rapidly and almost completely dephosphorylated by alkaline phosphatases and non-specific esterases in the intestine, liver, and kidneys such that virtually no intact PSI is detectable in human plasma [16,17].”
InfluentialŻełabowski, K., Wieczorek, T., & Hamed, A. (2026) · Frontiers in Pharmacology · doi:10.3389/fphar.2026.1852799
“According to the review by Dinis-Oliveira, psilocin becomes detectable in plasma within 20–40 min of oral psilocybin administration and subjective effects subside after 4–6 h (Dinis-Oliveira, 2017).”
Clinical Evidence on Psilocybin and Its Representation in Media Reporting
Madden, K., Flood, B., Kashir, I., Ahmad, R., Ali, H., Petranker, R., MacKillop, J., & Adili, A. F. (2026) · JAMA Network Open · doi:10.1001/jamanetworkopen.2026.38843
Metadata
- Authors
- Dinis-Oliveira, R. J.
- Affiliations
- Department of Sciences, IINFACTS – Institute of Research and Advanced Training in Health Sciences and Technologies, University Institute of Health Sciences (IUCS), CESPU, CRL, Gandra, Portugal;
- Venue
- Drug Metabolism Reviews
- Publisher
- Informa UK Limited
- Published
- 2017-01-02
- Volume
- 49
- Issue
- 1
- Pages
- 84-91
- ISSN
- 0360-2532 (ISSN-L)
- 1097-9883
- OpenAlex
- W2572835720
- Cited by
- 224
- References
- 65
- Citations by year
- 2026: 21 · 2025: 48 · 2024: 41 · 2023: 38 · 2022: 36 · 2021: 10 · 2020: 17 · 2019: 7 · 2018: 6
- FWCI
- 1.17
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Drug Metabolism Reviews (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Fundação para a Ciência e a Tecnologia
- FCT (IF/01147/2013)
- FEDER (UID/QUI/50006/2013)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Toxicology › Forensic Toxicology and Drug Analysis
- Social Sciences › Psychology › Clinical Psychology › Psychedelics and Drug Studies
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Keywords
- psilocybin, psilocin, drug metabolism, alkaline phosphatase, prodrugs, urinary metabolites, forensic toxicology, clinical toxicology, 5-HT2A receptor agonists, magic mushrooms, hallucinogens
- MeSH terms
- Hallucinogens, Humans, Prodrugs, Psilocybin, Metabolomics
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