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Drilldown: Medicines

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Medicines > classes : Anxiolytic or Dissociative or Research material

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generic:
brand:
None (138) · (none, never marketed) (1) · Cymbalta, Drizalma Sprinkle, Irenka, Yentreve (1) · DXM (1) · DXO (1) · Lexotan (1) · Librium (1) · Miltown (1) · O-DSMT (1) · Serax (1) · Spravato (1) · Tranxene (1) · Xanax (1) · Zoloft (1)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (26) · GABAA positive allosteric modulator (11) · Monoamine releasing agent (9) · 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 (147) · Depression, anxiety, neuropathic pain, fibromyalgia, chronic musculoskeletal pain (1) · 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-00000069-QINU`"', '"`UNIQ--vote-0000006A-QINU`"', '"`UNIQ--vote-0000006B-QINU`"' (1)
starting dose:
None (147) · 0.25 mg (1) · 25 mg (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 (147) · 0.25 mg, 0.5 mg, 1 mg, 2 mg tablets (immediate-release and orally disintegrating); 0.5 mg, 1 mg, 2 mg, 3 mg extended-release tablets; 1 mg/mL oral concentrate (1) · 25 mg, 50 mg, 100 mg tablets; oral concentrate 20 mg/mL (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 (147) · 10 mg/d (1) · 200 mg/d (1) · 84 mg per session (1) · N/A (never approved) (1)
routes:
None (146) · Intranasal (under direct medical supervision) (1) · intranasal; rectal and IV reported. (1) · Oral (4) · sublingual (1)
onset:
None (146) · 30-60 min (immediate-release); 1-2 h (extended-release) (1) · Anxiolysis classically 3-4 weeks, continuing improvement to 8-12 weeks (1) · Mood: 2–4 weeks. Pain: often within 1–2 weeks. (1) · Within hours of first administration (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (146) · 6 h (immediate-release); ~11 h (extended-release) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1) · Chronic daily dosing (1) · Long (1)
halflife:
None (146) · 11-13 h (immediate-release); 11-16 h (extended-release) (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~12 hours (1) · ~26 h (sertraline; range 13-45 h, longer in females); ~62-104 h (N-desmethylsertraline, weakly active) (1) · ~7-12 hours (1)
bioavailability:
None (146) · 80-90% oral (1) · Absolute bioavailability not precisely characterized; food modestly increases exposure (1) · Not formally characterized in humans. (1) · ~48% intranasal (1) · ~50% (highly variable) (1)
pregnancy:
None (146) · 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) · Category C'"`UNIQ--ref-0000008F-QINU`"' (1) · Category D'"`UNIQ--ref-0000006C-QINU`"' (1)
legal:
None (147) · Rx, Schedule III (US). REMS program required. (1) · Rx-only (1) · Rx-only in US (1) · Schedule IV (US) (1)

Showing below up to 164 results in range #1 to #164.

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