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Medicines > classes : Sedative-Hypnotic or [[:Category:Immunomodulators|Immunomodulator]] & routes: Oral

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generic:
Bromazolam (1) · Hydroxychloroquine (1)
brand:
(none, never marketed) (1) · Plaquenil; mostly prescribed generically (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-000007E7-QINU`"', '"`UNIQ--vote-000007E8-QINU`"', '"`UNIQ--vote-000007E9-QINU`"', '"`UNIQ--vote-000007EA-QINU`"', '"`UNIQ--vote-000007EB-QINU`"' (1)
starting dose:
200-400 mg PO daily; '''dose by actual body weight ≤5 mg/kg/d''' to reduce retinopathy risk (AAO 2016 guideline) (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
200 mg tablets; 100 mg/5 mL suspension (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
400 mg/d typical maintenance; weight-adjusted ceiling per ophthalmology guidance (1) · N/A (never approved) (1)
routes: (Click arrow to add another value)
onset:
Rheumatologic effect at 6-12 weeks (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
6–10 h subjective; full pharmacologic effect considerably longer. (1) · Weeks (long half-life) (1)
halflife:
Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~40 days (terminal; reflects extensive tissue distribution)'"`UNIQ--ref-000007EC-QINU`"' (1)
bioavailability:
70-75% (oral)'"`UNIQ--ref-000007ED-QINU`"' (1) · Not formally characterized in humans. (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) · Long-considered safe in pregnancy for lupus and other rheumatologic indications; benefits typically outweigh.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (1) · [[USLegal:Prescription only|Rx-only]] in US (1)

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