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Medicines > classes : Research material or [[:Category:Amphetamines|Amphetamine]] & routes: Oral

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generic:
Bromazolam (1) · Lisdexamfetamine (dimesylate) (1)
brand:
(none, never marketed) (1) · Vyvanse, Elvanse (EU) (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`"' Once converted, dextroamphetamine acts by displacing dopamine and norepinephrine from presynaptic vesicles via VMAT-2 and reversing DAT and NET transport, the shared mechanism of all amphetamine-class agents'"`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:
ADHD: 30 mg PO once daily in the morning; titrate by 10-20 mg weekly to clinical effect. Binge-eating disorder: 30 mg/day, titrate to 50-70 mg/day (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
Capsules 10, 20, 30, 40, 50, 60, 70 mg; chewable tablets 10, 20, 30, 40, 50, 60 mg (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
70 mg/day (1) · N/A (never approved) (1)
routes: (Click arrow to add another value)
onset:
1-2 hours (slower than immediate-release amphetamine because activation requires enzymatic cleavage in red blood cells) (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
10-12 hours (smoother profile than immediate-release amphetamine salts) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Parent lisdexamfetamine <1 hour; dextroamphetamine 10-12 hours after release'"`UNIQ--ref-00000017-QINU`"' (1)
bioavailability:
Not formally characterized in humans. (1) · ~96% after red blood cell hydrolytic cleavage releases dextroamphetamine'"`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) · Limited human data; the amphetamine class is associated with intrauterine growth restriction and neonatal withdrawal symptoms.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (1) · [[USLegal:Schedule II|Schedule II controlled substance]] in US'"`UNIQ--ref-00000019-QINU`"' (1)

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