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Medicines > classes : Sedative-hypnotic or [[:Category:Mood stabilizers|Mood stabilizer (off-label)]] & routes: Oral

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generic:
Bromazolam (1) · Oxcarbazepine (1)
brand:
(none, never marketed) (1) · Trileptal (IR), Oxtellar XR (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:
Adult monotherapy: 300 mg PO BID, titrate by 300 mg every 3 days. Pediatric: weight-based titration starting 8-10 mg/kg/day divided BID (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 150, 300, 600 mg; oral suspension 60 mg/mL; XR tablets 150, 300, 600 mg (Oxtellar) (1)
fda max:
2400 mg/day (adult) (1) · N/A (never approved) (1)
routes: (Click arrow to add another value)
onset:
Anticonvulsant effect within days at therapeutic plasma level (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
6–10 h subjective; full pharmacologic effect considerably longer. (1) · BID dosing (IR); once-daily (XR) (1)
halflife:
Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Oxcarbazepine 2 hours; '''10-monohydroxy active metabolite (MHD) ~9 hours''' (the agent that produces essentially all of the clinical effect)'"`UNIQ--ref-0000001A-QINU`"' (1)
bioavailability:
Not formally characterized in humans. (1) · ~100% (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) · Teratogenic signal less than carbamazepine but present; folate supplementation and effective contraception are appropriate in reproductive-age patients'"`UNIQ--ref-0000001C-QINU`"' (1)
legal:
None (1) · [[USLegal:Prescription only|Rx-only]] in US (1)

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