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Medicines > classes : Benzodiazepine or Research material or [[:Category:DOACs|Direct oral anticoagulant (DOAC)]]

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generic:
brand:
None (131) · (none, never marketed) (1) · Dalmane (1) · Doral (1) · Eliquis (1) · Halcion (1) · Lexotan (1) · Librium (1) · Mogadon (1) · O-DSMT (1) · Onfi (1) · ProSom (1) · Restoril (1) · Rohypnol (1) · Serax (1) · Tranxene (1) · Versed (1) · Xanax (1) · Xarelto (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-00000069-QINU`"', '"`UNIQ--vote-0000006A-QINU`"', '"`UNIQ--vote-0000006B-QINU`"' (1) · '"`UNIQ--vote-000001F8-QINU`"', '"`UNIQ--vote-000001F9-QINU`"', '"`UNIQ--vote-000001FA-QINU`"' (1) · '"`UNIQ--vote-0000050F-QINU`"', '"`UNIQ--vote-00000510-QINU`"', '"`UNIQ--vote-00000511-QINU`"', '"`UNIQ--vote-00000512-QINU`"' (1)
starting dose:
None (145) · 0.25 mg (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · NVAF: 20 mg PO once daily with the evening meal (15 mg if CrCl 15-50); acute VTE: 15 mg BID for 21 days, then 20 mg daily; CAD/PAD: 2.5 mg BID with aspirin (1) · NVAF: 5 mg PO BID (2.5 mg BID if 2 of 3: age ≥80, weight ≤60 kg, serum creatinine ≥1.5 mg/dL); acute VTE: 10 mg BID for 7 days, then 5 mg BID (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) · 2.5 mg, 5 mg tablets (1) · 2.5, 10, 15, 20 mg tablets (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (145) · 10 mg BID for the first 7 days of acute VTE; otherwise 5 mg BID (1) · 10 mg/d (1) · 30 mg/d (acute VTE first 21 days as 15 mg BID); otherwise 20 mg/d (1) · N/A (never approved) (1)
routes:
None (145) · intranasal; rectal and IV reported. (1) · Oral (4) · sublingual (1)
onset:
None (145) · 30-60 min (immediate-release); 1-2 h (extended-release) (1) · Peak anticoagulant effect 2-4 hours (1) · Peak anticoagulant effect 3-4 hours (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (145) · 12 hours (1) · 24 hours (1) · 6 h (immediate-release); ~11 h (extended-release) (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) · 5-9 hours (elderly: 11-13 hours)'"`UNIQ--ref-00000513-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~12 hours'"`UNIQ--ref-000001FB-QINU`"' (1)
bioavailability:
None (145) · 80-90% oral (1) · Not formally characterized in humans. (1) · ~50% (oral; not significantly affected by food)'"`UNIQ--ref-000001FC-QINU`"' (1) · ~80-100% with food at 15-20 mg doses (10 mg dose: ~80% without food); '''must be taken with food''' at therapeutic doses'"`UNIQ--ref-00000514-QINU`"' (1)
pregnancy:
None (146) · Avoid in pregnancy; switch to LMWH. Crosses placenta; warfarin-class concerns about fetal hemorrhage and teratogenicity make heparins the preferred class.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · 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)
legal:
None (146) · Schedule IV (US) (1) · [[USLegal:Prescription only|Rx-only]] in US (2)

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