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Medicines > classes : Benzodiazepine or Research material or [[:Category:Benzodiazepines|Benzodiazepine (long-acting)]]

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generic:
brand:
None (131) · (none, never marketed) (1) · Dalmane (1) · Doral (1) · Halcion (1) · Lexotan (1) · Librium (1) · Mogadon (1) · O-DSMT (1) · Onfi (1) · ProSom (1) · Restoril (1) · Rohypnol (1) · Serax (1) · Tranxene (1) · Valium (oral, IV/IM, rectal), Diastat (rectal gel for breakthrough seizures), Valtoco (nasal spray for breakthrough seizures), Libervant (buccal film) (1) · Versed (1) · Xanax (1)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (26) · GABAA positive allosteric modulator (21) · 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) · Serotonin/norepinephrine/dopamine releasing agent (3) · Cathinone analogue; monoamine reuptake inhibitor (2) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist (2) · Prodrug of GHB (2)
uses:
None (145) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"' (1) · '"`UNIQ--vote-00000069-QINU`"', '"`UNIQ--vote-0000006A-QINU`"', '"`UNIQ--vote-0000006B-QINU`"' (1)
starting dose:
None (145) · 0.25 mg (1) · Anxiety: 2-10 mg PO 2-4 times daily. Alcohol withdrawal: 10-20 mg PO/IV every 4-6 hours, symptom-triggered. Status epilepticus: 5-10 mg IV. Breakthrough seizures: Diastat rectal 0.2-0.5 mg/kg or Valtoco intranasal 5-20 mg (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
None (145) · 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) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Tablets 2, 5, 10 mg; oral solution 1, 5 mg/mL; injection 5 mg/mL; Diastat rectal gel 2.5, 5, 10, 20 mg; Valtoco nasal spray 5, 7.5, 10 mg/dose; Libervant buccal film (1)
fda max:
None (145) · 10 mg/d (1) · 40 mg/day (oral, anxiety) (1) · N/A (never approved) (1)
routes:
None (145) · buccal (1) · IM (1) · intranasal (1) · intranasal; rectal and IV reported. (1) · IV (1) · Oral (3) · rectal (1) · sublingual (1)
onset:
None (145) · 15-60 minutes (oral); 1-5 minutes (IV); 4-10 minutes (rectal or intranasal) (1) · 30-60 min (immediate-release); 1-2 h (extended-release) (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (145) · 6 h (immediate-release); ~11 h (extended-release) (1) · 6-24 hours (parent); much longer when accounting for the long-lived active metabolites (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
None (145) · 11-13 h (immediate-release); 11-16 h (extended-release) (1) · Diazepam 20-50 hours; '''N-desmethyldiazepam (nordazepam) 30-200 hours''' is the major active metabolite and accumulates substantially with chronic dosing'"`UNIQ--ref-00000026-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1)
bioavailability:
None (145) · 80-90% oral (1) · Not formally characterized in humans. (1) · ~93% (oral); ~90% (rectal)'"`UNIQ--ref-00000027-QINU`"' (1)
pregnancy:
None (145) · 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) · Category D'"`UNIQ--ref-0000006C-QINU`"' (1) · Some signal for cleft palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (146) · Schedule IV (US) (1) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the benzodiazepine class '''Boxed Warning''' for risk of fatal respiratory depression, coma, and death when combined with opioids'"`UNIQ--ref-00000028-QINU`"' (1)

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