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Drilldown: Medicines

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Medicines > classes : Dissociative or Research material or [[:Category:Catecholamines|Catecholamine]]

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generic:
brand:
None (137) · (none, never marketed) (1) · DXM (1) · DXO (1) · EpiPen, EpiPen Jr, Auvi-Q, Adrenaclick, Symjepi; many generic (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-00000E4C-QINU`"', '"`UNIQ--vote-00000E4D-QINU`"', '"`UNIQ--vote-00000E4E-QINU`"', '"`UNIQ--vote-00000E4F-QINU`"', '"`UNIQ--vote-00000E50-QINU`"', '"`UNIQ--vote-00000E51-QINU`"' (1)
starting dose:
None (140) · Anaphylaxis IM 0.3-0.5 mg (adult) into lateral thigh, repeat q5-15 minutes prn; pediatric 0.01 mg/kg IM (max 0.3 mg, max 0.5 mg in adolescents); cardiac arrest 1 mg IV/IO q3-5 minutes; severe asthma neb 0.1 mg/kg up to 5 mg; never IV bolus for anaphylaxis outside critical care (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) · 28 mg/device (each dose uses 2 devices) (1) · Auto-injectors 0.15 mg (Jr/pediatric), 0.3 mg (adult); 1 mg/mL (1:1,000) ampules for IM/SC use; 0.1 mg/mL (1:10,000) for IV use; 2.25% racemic nebulizer (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (140) · 84 mg per session (1) · Indication-specific; ACLS no fixed cumulative ceiling (1) · N/A (never approved) (1)
routes:
None (140) · endotracheal (legacy ACLS (1) · IM (1) · intracardiac (historical only) (1) · Intranasal (under direct medical supervision) (1) · intranasal; rectal and IV reported. (1) · IV (1) · nebulized (1) · not preferred) (1) · Oral (1) · SC (less common) (1) · sublingual (1)
onset:
None (140) · IM: 5-10 minutes; IV: seconds; nebulized: 5-10 minutes (1) · Within hours of first administration (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (140) · 5-15 minutes (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) · ~2 minutes'"`UNIQ--ref-00000E52-QINU`"' (1) · ~7-12 hours (1)
bioavailability:
None (140) · IM/SC ~100%; oral negligible (extensive first-pass and gut metabolism — hence the no-oral route)'"`UNIQ--ref-00000E53-QINU`"' (1) · Not formally characterized in humans. (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) · Used in life-threatening obstetric anaphylaxis without hesitation; benefits clearly outweigh.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (141) · Rx, Schedule III (US). REMS program required. (1) · [[USLegal:Prescription only|Rx-only]] in US (1)

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