Drilldown: Medicines

Psilocybin (1)

COMP360 (Compass Pathways, investigational synthesized clinical formulation) (1)

[[:Category:Classical Psychedelics (Serotonergic)|Serotonergic psychedelic]] (1) · [[:Category:Psychedelics|Psychedelic]] (1) · [[:Category:Tryptamines|Tryptamine]] (1)

Prodrug to [[Psilocin|psilocin]] (4-hydroxy-N,N-dimethyltryptamine), a partial agonist at the [[Receptor:5-HT2A|5-HT2A]] serotonin receptor; the action that defines the classical-psychedelic mechanism (1)

(investigational) '"`UNIQ--vote-000000EF-QINU`"', '"`UNIQ--vote-000000F0-QINU`"', '"`UNIQ--vote-000000F1-QINU`"', '"`UNIQ--vote-000000F2-QINU`"', '"`UNIQ--vote-000000F3-QINU`"' (1)

Modern clinical-trial standard: 25 mg synthesized psilocybin, single oral dose with psychological support (1)

Synthesized psilocybin capsules (COMP360 and other investigational formulations); dried whole [[Psilocybe|Psilocybe]] mushrooms (variable potency, no legal supply chain in most jurisdictions); psilocybin truffles (Psilocybe sclerotia, legal in the Netherlands) (1)

None · Indication-specific · 40 mg/d · 10 mg/d · 20 mg/d · 80 mg/d · 10 mg/d (adults) · 100 mg/d · 4 g/d · 400 mg/d · 40 mg/d typical; up to 240 mg/d for Zollinger-Ellison · 5 mg/d · 50 mg/d · 600 mg/d · No fixed ceiling; titrate to clinical effect and tolerability with CDC opioid prescribing guidance constraints on morphine-milligram-equivalent (MME) totals · No fixed maximum; titrated to TSH target · TID per eye · Titrated to glucose; no fixed ceiling · Titrated to glucose; no fixed maximum · '''20 mg/day in adults >60 years''' per FDA's 2011-2012 QT-prolongation warning; 40 mg/day in adults ≤60

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Oral (1)

20-45 min subjective onset; psilocin formation from psilocybin requires intestinal and hepatic alkaline phosphatase (1)

4-6 hours (1)

None · ~12 hours · ~27 days · ~5 h (caffeine) · '''Autoinduction''': 25-65 hours initially, falling to 12-17 hours after 2-3 weeks of dosing as carbamazepine induces its own CYP3A4 metabolism. Major clinical implication: doses require re-titration after the autoinduction period'"`UNIQ--ref-0000001D-QINU`"' · 0.5-1.5 hours (plasma); pharmacodynamic effect persists 24+ hours'"`UNIQ--ref-000000DE-QINU`"' · 1-1.3 hours'"`UNIQ--ref-000001A1-QINU`"' · 1-1.5 hours'"`UNIQ--ref-00000DE3-QINU`"' · 1-2 hours (parent compound)'"`UNIQ--ref-00000029-QINU`"' · 1-2 hours (parent); 18-30 hours for active metabolite oxypurinol'"`UNIQ--ref-0000030F-QINU`"' · 1-2 hours'"`UNIQ--ref-00000017-QINU`"' · 1-3 hours (normal liver); markedly prolonged in overdose with glutathione depletion'"`UNIQ--ref-000006A5-QINU`"' · 1-3 minutes (very short)'"`UNIQ--ref-00000C0F-QINU`"' · 1.4 hours (parent); 13-24 hours for active metabolite canrenone'"`UNIQ--ref-00000354-QINU`"' · 1.5-2 hours (longer in renal failure)'"`UNIQ--ref-00000222-QINU`"' · 1.5-2 hours'"`UNIQ--ref-00000020-QINU`"' · 10-11 hours (benazeprilat, the active metabolite)'"`UNIQ--ref-00000A22-QINU`"' · 11-13 h (immediate-release); 11-16 h (extended-release) · 11-15 hours'"`UNIQ--ref-00000842-QINU`"' · 12-15 hours (intermediate); '''no active metabolites''' (key clinical feature)'"`UNIQ--ref-00000023-QINU`"'

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Oral bioavailability of psilocin from administered psilocybin approximately 50% (1)

Not studied in human pregnancy; no approved clinical use in any population (1)

None (1)