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Medicines > classes : Benzodiazepine or Research material or [[:Category:Antisecretory_agents|Gastric acid suppressant]]

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generic:
brand:
None (131) · (none, never marketed) (1) · Dalmane (1) · Doral (1) · Halcion (1) · Lexotan (1) · Librium (1) · Mogadon (1) · Nexium, Nexium 24HR (OTC) (1) · O-DSMT (1) · Onfi (1) · Pepcid, Pepcid AC, Pepcid Complete (1) · Prilosec, Losec, Zegerid (1) · ProSom (1) · Protonix (1) · Restoril (1) · Rohypnol (1) · Serax (1) · Tranxene (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-00000069-QINU`"', '"`UNIQ--vote-0000006A-QINU`"', '"`UNIQ--vote-0000006B-QINU`"' (1) · '"`UNIQ--vote-000000DA-QINU`"', '"`UNIQ--vote-000000DB-QINU`"', '"`UNIQ--vote-000000DC-QINU`"', '"`UNIQ--vote-000000DD-QINU`"' (1) · '"`UNIQ--vote-00000119-QINU`"', '"`UNIQ--vote-0000011A-QINU`"', '"`UNIQ--vote-0000011B-QINU`"', '"`UNIQ--vote-0000011C-QINU`"' (1) · '"`UNIQ--vote-00000257-QINU`"', '"`UNIQ--vote-00000258-QINU`"', '"`UNIQ--vote-00000259-QINU`"', '"`UNIQ--vote-0000025A-QINU`"' (1) · '"`UNIQ--vote-000008E3-QINU`"', '"`UNIQ--vote-000008E4-QINU`"', '"`UNIQ--vote-000008E5-QINU`"', '"`UNIQ--vote-000008E6-QINU`"', '"`UNIQ--vote-000008E7-QINU`"' (1)
starting dose:
None (145) · 0.25 mg (1) · 20 mg PO once daily 30-60 minutes before breakfast (1) · 20 mg PO twice daily, or 40 mg at bedtime (1) · 20-40 mg PO once daily, 30-60 minutes before breakfast (1) · 40 mg PO or IV once daily (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) · 10 mg, 20 mg, 40 mg tablets; chewables; 40 mg/5 mL oral suspension; 10 mg/mL IV (1) · 10, 20, 40 mg delayed-release capsules and tablets; 2 mg/mL oral suspension; immediate-release combo with sodium bicarbonate (Zegerid) (1) · 20 mg, 40 mg delayed-release tablets; 40 mg IV vial; oral suspension 40 mg/packet (1) · 20, 40 mg delayed-release capsules; 2.5, 5, 10, 20, 40 mg oral suspension packets; 20, 40 mg IV (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (145) · 10 mg/d (1) · 160 mg/d (Zollinger-Ellison); 80 mg/d for routine indications (1) · 40 mg/d typical; up to 240 mg/d for Zollinger-Ellison (2) · 40 mg/d typical; up to 360 mg/d for Zollinger-Ellison (1) · N/A (never approved) (1)
routes:
None (145) · intranasal; rectal and IV reported. (1) · IV (4) · Oral (6) · sublingual (1)
onset:
None (145) · 1 hour PO; minutes IV (1) · 2-3 hours per dose; full acid suppression after 3-5 days (1) · 30-60 min (immediate-release); 1-2 h (extended-release) (1) · Acid suppression within hours; full effect after 3-5 days of dosing (1) · Symptom relief 1-4 days; full acid suppression after 3-5 days of dosing (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (145) · 24+ hours (irreversible enzyme binding) (1) · 24-72 hours per dose (irreversible enzyme binding) (1) · 24-72 hours per dose (irreversible enzyme binding; effect outlasts plasma exposure) (1) · 6 h (immediate-release); ~11 h (extended-release) (1) · 6-12 hours (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
None (145) · 0.5-1.5 hours (plasma); pharmacodynamic effect persists 24+ hours'"`UNIQ--ref-000000DE-QINU`"' (1) · 11-13 h (immediate-release); 11-16 h (extended-release) (1) · 2.5-3.5 hours; longer in renal impairment'"`UNIQ--ref-0000025B-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~1 hour (plasma); pharmacodynamic effect persists 24+ hours'"`UNIQ--ref-0000011D-QINU`"' (1) · ~1.5 hours (plasma); pharmacodynamic effect 24+ hours via target turnover'"`UNIQ--ref-000008E8-QINU`"' (1)
bioavailability:
None (145) · 30-40% (oral; increases with repeated dosing as gastric pH rises)'"`UNIQ--ref-000000DF-QINU`"' (1) · 40-45% (oral; not significantly affected by food)'"`UNIQ--ref-0000025C-QINU`"' (1) · 80-90% oral (1) · Not formally characterized in humans. (1) · ~64-90% (oral; increases at higher doses and with multi-day dosing)'"`UNIQ--ref-000008E9-QINU`"' (1) · ~77% (oral; not affected by food or antacids)'"`UNIQ--ref-0000011E-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) · Generally considered safe; widely used in obstetric reflux.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe; widely used. Cleared in lactation at low levels.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Widely used in obstetric reflux; reassuring data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Widely used in pregnancy; meta-analyses do not show increased malformation risk.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (146) · OTC (10-20 mg) and [[USLegal:Prescription only|Rx-only]] (higher doses) in US (1) · OTC (20 mg) and [[USLegal:Prescription only|Rx-only]] (higher doses) in US (1) · OTC (20 mg, 14-day course) and [[USLegal:Prescription only|Rx-only]] (higher and longer durations) in US (1) · Schedule IV (US) (1) · [[USLegal:Prescription only|Rx-only]] in US (1)

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