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Medicines > classes : Classic Psychedelic or Dissociative or [[:Category:Direct_vasodilators|Direct arteriolar vasodilator]]

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generic:
brand:
None (86) · Apresoline (historical); mostly generic; combination with isosorbide dinitrate marketed as BiDil for self-identified Black patients with HFrEF (1) · Delysid (historical, Sandoz, withdrawn 1965) (1) · DXM (1) · DXO (1) · Spravato (1)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (26) · Potent 5-HT2A agonist (5) · LSD analogue; 5-HT2A agonist (4) · Prodrug of LSD; 5-HT2A agonist (4) · NMDA antagonist (3) · None (2) · Contains LSA (2) · Contains mescaline (2) · NMDA antagonist; sigma receptor agonist (2)
uses:
None (89) · Treatment-resistant depression (TRD) in adults, as adjunct to oral antidepressant (FDA-approved March 2019). Depressive symptoms in adults with MDD with acute suicidal ideation or behavior (FDA-approved Aug 2020). (1) · '"`UNIQ--vote-00000683-QINU`"', '"`UNIQ--vote-00000684-QINU`"', '"`UNIQ--vote-00000685-QINU`"', '"`UNIQ--vote-00000686-QINU`"' (1)
starting dose:
None (89) · Induction (TRD): 56 mg intranasal twice weekly × 4 weeks. Maintenance: 56-84 mg once weekly × 4 weeks, then 56-84 mg every 1-2 weeks. For acute suicidality: 84 mg twice weekly × 4 weeks. Administered under medical supervision in REMS-certified site. (1) · PO 10 mg QID; IV 5-10 mg every 20-30 minutes for hypertensive emergency (1)
preparations:
None (89) · 10, 25, 50, 100 mg tablets; 20 mg/mL IV (1) · 28 mg/device (each dose uses 2 devices) (1)
fda max:
None (89) · 300 mg/d typical practical limit (toxicity rises sharply above) (1) · 84 mg per session (1)
routes:
None (88) · IM (1) · Intranasal (under direct medical supervision) (1) · IV (1) · Oral (2)
onset:
None (88) · 30–60 minutes (1) · IV: 5-20 minutes; PO: 30-60 minutes (1) · Within hours of first administration (1)
duration:
None (88) · 8–12 hours (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1) · IV: 1-4 hours; PO: 3-8 hours (1)
halflife:
None (88) · 3-7 hours (slow acetylators) vs 1-3 hours (rapid acetylators) via NAT2 polymorphism'"`UNIQ--ref-00000687-QINU`"' (1) · 3–5 hours (1) · ~7-12 hours (1)
bioavailability:
None (88) · 70–90% (oral) (1) · ~25-50% (oral; substantial first-pass via NAT2 acetylation, phenotype-dependent)'"`UNIQ--ref-00000688-QINU`"' (1) · ~48% intranasal (1)
pregnancy:
None (88) · Avoid; may cause fetal harm (1) · Not established (1) · One of the historically preferred IV agents for severe hypertension in pregnancy alongside labetalol and nifedipine.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (88) · Rx, Schedule III (US). REMS program required. (1) · Schedule I (United States) (1) · [[USLegal:Prescription only|Rx-only]] in US (1)

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