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Medicines > classes : Benzodiazepine or [[:Category:Barbiturates|Barbiturate (parent compound)]] & routes: Oral

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generic:
Alprazolam (1) · Primidone (1)
brand:
Mysoline (1) · Xanax (1)
classes: (Click arrow to add another value)
mechanism:
GABA-A positive allosteric modulator'"`UNIQ--ref-00000067-QINU`"' '"`UNIQ--vote-00000068-QINU`"' (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:
'"`UNIQ--vote-00000015-QINU`"', '"`UNIQ--vote-00000016-QINU`"' (1) · '"`UNIQ--vote-00000069-QINU`"', '"`UNIQ--vote-0000006A-QINU`"', '"`UNIQ--vote-0000006B-QINU`"' (1)
starting dose:
0.25 mg (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:
0.25 mg, 0.5 mg, 1 mg, 2 mg tablets (immediate-release and orally disintegrating); 0.5 mg, 1 mg, 2 mg, 3 mg extended-release tablets; 1 mg/mL oral concentrate (1) · Tablets 50, 250 mg (1)
fda max:
10 mg/d (1) · 2 g/day (seizures); typically much lower for essential tremor (1)
routes: (Click arrow to add another value)
onset:
30-60 min (immediate-release); 1-2 h (extended-release) (1) · Anticonvulsant effect emerges with slow titration over weeks; tremor effect over weeks (1)
duration:
6 h (immediate-release); ~11 h (extended-release) (1) · BID-TID dosing (1)
halflife:
11-13 h (immediate-release); 11-16 h (extended-release) (1) · Primidone 5-15 hours; '''phenobarbital active metabolite 50-150 hours'''; PEMA (phenylethylmalonamide) active metabolite 16 hours'"`UNIQ--ref-00000017-QINU`"' (1)
bioavailability:
80-90% oral (1) · ~90% (oral)'"`UNIQ--ref-00000018-QINU`"' (1)
pregnancy:
Category D'"`UNIQ--ref-0000006C-QINU`"' (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:
Schedule IV (US) (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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