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Medicines > classes : Sedative-hypnotic or [[:Category:SV2A ligands|Synaptic vesicle protein 2A (SV2A) ligand]] & routes: Oral

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generic:
Bromazolam (1) · Levetiracetam (1)
brand:
(none, never marketed) (1) · Keppra (IR), Keppra XR, Spritam (3D-printed orally disintegrating), Roweepra (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-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"' (1)
starting dose:
Adult: 500 mg PO BID, titrate by 1000 mg/day every 2 weeks. Pediatric: 10-20 mg/kg/day divided BID, weight-titrated (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 250, 500, 750, 1000 mg; XR tablets 500, 750 mg; oral solution 100 mg/mL; injection 100 mg/mL; Spritam ODT 250, 500, 750, 1000 mg (1)
fda max:
3000 mg/day (1) · N/A (never approved) (1)
routes: (Click arrow to add another value)
onset:
Anticonvulsant effect within days at therapeutic plasma level; rapid titration possible (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:
6-8 hours'"`UNIQ--ref-0000001F-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1)
bioavailability:
Not formally characterized in humans. (1) · ~100% (oral)'"`UNIQ--ref-00000020-QINU`"' (1)
pregnancy:
'''Considered one of the safest anticonvulsants in pregnancy''', with reassuring monotherapy registry data comparable to lamotrigine and in sharp contrast to valproate, topiramate, and carbamazepine'"`UNIQ--ref-00000021-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)
legal:
None (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance'"`UNIQ--ref-00000022-QINU`"' (1)

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