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Medicines > classes : Research material or [[:Category:Tremor medicines|Tremor medicine]] & routes: Oral

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generic:
Bromazolam (1) · Primidone (1)
brand:
(none, never marketed) (1) · Mysoline (1)
classes: (Click arrow to add another value)
mechanism:
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) · '"`UNIQ--vote-00000013-QINU`"' Strong CYP3A4 induction via the phenobarbital metabolite produces many interactions (reduces oral contraceptives, warfarin, many psychotropics). Essential-tremor efficacy is the unique pharmacological selling point'"`UNIQ--ref-00000014-QINU`"'. (1)
uses:
No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000015-QINU`"', '"`UNIQ--vote-00000016-QINU`"' (1)
starting dose:
No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Seizures: 100-125 mg PO at bedtime x 3 days, then BID, then TID, escalating to 750-1500 mg/day. Essential tremor: 25-50 mg PO at bedtime, titrate slowly to 250-750 mg/day (1)
preparations:
Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Tablets 50, 250 mg (1)
fda max:
2 g/day (seizures); typically much lower for essential tremor (1) · N/A (never approved) (1)
routes: (Click arrow to add another value)
onset:
Anticonvulsant effect emerges with slow titration over weeks; tremor effect over weeks (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
6–10 h subjective; full pharmacologic effect considerably longer. (1) · BID-TID dosing (1)
halflife:
Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Primidone 5-15 hours; '''phenobarbital active metabolite 50-150 hours'''; PEMA (phenylethylmalonamide) active metabolite 16 hours'"`UNIQ--ref-00000017-QINU`"' (1)
bioavailability:
Not formally characterized in humans. (1) · ~90% (oral)'"`UNIQ--ref-00000018-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) · Substantial teratogenic signal (barbiturate class effects including neonatal withdrawal and hemorrhagic disease of newborn).<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. '''Federally non-controlled despite being a barbiturate''', a paradoxical situation given that its primary active metabolite phenobarbital is Schedule IV'"`UNIQ--ref-00000019-QINU`"' (1)

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