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Drilldown: Medicines

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Medicines > classes : Cardioselective (β1) + vasodilator or Dissociative or Research material

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generic:
brand:
None (137) · (none, never marketed) (1) · Bystolic (1) · DXM (1) · DXO (1) · O-DSMT (1) · Spravato (1)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (26) · Monoamine releasing agent (9) · GABAA positive allosteric modulator (8) · CB1/CB2 agonist (7) · Dopamine/norepinephrine reuptake inhibitor (5) · Potent 5-HT2A agonist (5) · LSD analogue; 5-HT2A agonist (4) · Prodrug of LSD; 5-HT2A agonist (4) · NMDA antagonist (3) · Serotonin/norepinephrine/dopamine releasing agent (3) · Cathinone analogue; monoamine reuptake inhibitor (2) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist; sigma receptor agonist (2) · Prodrug of GHB (2)
uses:
None (140) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · 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-0000059D-QINU`"' (1)
starting dose:
None (140) · 5 mg daily (1) · 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) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
None (140) · 2.5, 5, 10, 20 mg tabs (1) · 28 mg/device (each dose uses 2 devices) (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (140) · 40 mg/d (1) · 84 mg per session (1) · N/A (never approved) (1)
routes:
None (140) · Intranasal (under direct medical supervision) (1) · intranasal; rectal and IV reported. (1) · Oral (2) · sublingual (1)
onset:
None (140) · 1–2 h (1) · Within hours of first administration (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (140) · 24 h (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1)
halflife:
None (140) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers) (1) · ~7-12 hours (1)
bioavailability:
None (140) · Not formally characterized in humans. (1) · ~12% (extensive metabolizers); ~96% (poor metabolizers) (1) · ~48% intranasal (1)
pregnancy:
None (140) · Avoid. Benzodiazepines are associated with neonatal sedation, floppy-infant syndrome, and withdrawal; teratogenic signal weak but non-zero. Designer benzo with no safety data, assume worst-case. (1) · Avoid; may cause fetal harm (1) · Category C (1)
legal:
None (141) · Rx, Schedule III (US). REMS program required. (1) · Rx-only in US (1)

Showing below up to 153 results in range #1 to #153.

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