Drilldown: Medicines

Bromazolam (1) · Esomeprazole (1) · Pantoprazole (1)

(none, never marketed) (1) · Nexium, Nexium 24HR (OTC) (1) · Protonix (1)

Designer benzodiazepine (1) · Research material (1) · Sedative-Hypnotic (1) · Triazolobenzodiazepine (1) · [[:Category:Antisecretory_agents|Gastric acid suppressant]] (2) · [[:Category:Proton_pump_inhibitors|Proton pump inhibitor (PPI)]] (2)

Positive allosteric modulator of the GABA_A receptor at the benzodiazepine binding site; increases frequency of Cl⁻ channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1) · '"`UNIQ--vote-00000117-QINU`"' Compared with omeprazole, pantoprazole has a more linear pharmacokinetic profile and is metabolized predominantly via CYP2C19 with CYP3A4 contribution; less CYP2C19-driven drug interaction with clopidogrel than omeprazole'"`UNIQ--ref-00000118-QINU`"'. (1) · '"`UNIQ--vote-000008E1-QINU`"' Like omeprazole, it is an acid-activated prodrug that covalently and irreversibly binds the H+/K+ ATPase. CYP2C19 PGx remains clinically relevant for both'"`UNIQ--ref-000008E2-QINU`"'. (1)

No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000119-QINU`"', '"`UNIQ--vote-0000011A-QINU`"', '"`UNIQ--vote-0000011B-QINU`"', '"`UNIQ--vote-0000011C-QINU`"' (1) · '"`UNIQ--vote-000008E3-QINU`"', '"`UNIQ--vote-000008E4-QINU`"', '"`UNIQ--vote-000008E5-QINU`"', '"`UNIQ--vote-000008E6-QINU`"', '"`UNIQ--vote-000008E7-QINU`"' (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)

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)

None · Indication-specific · 40 mg/d · 10 mg/d · 20 mg/d · 80 mg/d · 10 mg/d (adults) · 100 mg/d · 4 g/d · 400 mg/d · 40 mg/d typical; up to 240 mg/d for Zollinger-Ellison · 5 mg/d · 50 mg/d · 600 mg/d · No fixed ceiling; titrate to clinical effect and tolerability with CDC opioid prescribing guidance constraints on morphine-milligram-equivalent (MME) totals · No fixed maximum; titrated to TSH target · TID per eye · Titrated to glucose; no fixed ceiling · Titrated to glucose; no fixed maximum · '''20 mg/day in adults >60 years''' per FDA's 2011-2012 QT-prolongation warning; 40 mg/day in adults ≤60

Other values:

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intranasal; rectal and IV reported. (1) · IV (2) · Oral (3) · sublingual (1)

2-3 hours per dose; full acid suppression after 3-5 days (1) · Acid suppression within hours; full effect after 3-5 days of dosing (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

24+ hours (irreversible enzyme binding) (1) · 24-72 hours per dose (irreversible enzyme binding) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (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)

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)

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) · 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) · 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)

None (1) · OTC (20 mg, 14-day course) and [[USLegal:Prescription only|Rx-only]] (higher and longer durations) in US (1) · [[USLegal:Prescription only|Rx-only]] in US (1)