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Medicines > classes : Research material or [[:Category:Schedule IV controlled substances|Schedule IV controlled substance]] & routes: Sublingual

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generic:
Bromazolam (1) · Zolpidem (tartrate) (1)
brand:
(none, never marketed) (1) · Ambien (IR), Ambien CR (biphasic-release), Edluar (sublingual), Intermezzo (low-dose sublingual for middle-of-night awakening), Zolpimist (oral spray) (1)
classes: (Click arrow to add another value)
mechanism:
None (1) · Positive allosteric modulator of the GABA<sub>A</sub> receptor at the benzodiazepine binding site; increases frequency of Cl<sup>−</sup> channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1)
uses:
No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"' (1)
starting dose:
'''5 mg PO at bedtime for women, 5-10 mg for men''' (per FDA's 2013 sex-specific dose reduction for women due to slower clearance). Ambien CR 6.25 mg women / 6.25-12.5 mg men. Intermezzo SL 1.75 mg women / 3.5 mg men (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · IR tablets 5, 10 mg; CR tablets 6.25, 12.5 mg; SL tablets 1.75, 3.5, 5, 10 mg; oral spray (1)
fda max:
10 mg/day (IR); 12.5 mg/day (CR) (1) · N/A (never approved) (1)
routes: (Click arrow to add another value)
onset:
15-30 minutes (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
6-8 hours (IR); 8 hours (CR via biphasic release) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~2.5 hours'"`UNIQ--ref-0000001A-QINU`"' (1)
bioavailability:
Not formally characterized in humans. (1) · ~70% (oral)'"`UNIQ--ref-0000001B-QINU`"' (1)
pregnancy:
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) · Limited human data; case reports of neonatal sedation with late-pregnancy exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (1) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the FDA '''Boxed Warning''' for '''complex sleep behaviors''' (sleep-driving, sleep-walking, sleep-eating, other parasomnias) added in 2019'"`UNIQ--ref-0000001C-QINU`"' (1)

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