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Medicines > classes : Empathogen or Research material or [[:Category:Psychostimulants|Psychostimulant]]

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generic:
brand:
None (140) · (none, never marketed) (1) · O-DSMT (1) · Provigil (US, 100 mg and 200 mg tablets); Alertec (Canada); Modiodal (France, original market). See also: Armodafinil (Nuvigil), the R-enantiomer, a related eugeroic approved 2007 with a longer effective half-life. (1) · Vyvanse, Elvanse (EU) (1)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (26) · Monoamine releasing agent (10) · GABAA positive allosteric modulator (8) · CB1/CB2 agonist (7) · Dopamine/norepinephrine reuptake inhibitor (5) · Potent 5-HT2A agonist (5) · LSD analogue; 5-HT2A agonist (4) · Prodrug of LSD; 5-HT2A agonist (4) · Serotonin releasing agent; 5-HT2A agonist (3) · Serotonin/norepinephrine/dopamine releasing agent (3) · Cathinone analogue; monoamine reuptake inhibitor (2) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist (2) · Prodrug of GHB (2) · Serotonin releasing agent (2)
uses:
None (142) · 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:
None (141) · 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) · Narcolepsy/OSA: 200 mg PO once daily in the morning. Shift work disorder: 200 mg PO approximately 1 hour before the start of the work shift. Lower starting dose (100 mg) can be considered in elderly patients or those with hepatic impairment. (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
None (141) · 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) · Oral tablets 100 mg and 200 mg (Provigil and generics). No IV or extended-release formulations available; compare armodafinil (Nuvigil) 50/150/250 mg tablets as the R-enantiomer alternative. (1)
fda max:
None (141) · 400 mg/day (though clinical trials and FDA label note that doses above 200 mg/day have not demonstrated additional benefit in controlled studies for the approved indications; 200 mg is the standard therapeutic dose).'"`UNIQ--ref-0000004B-QINU`"' (1) · 70 mg/day (1) · N/A (never approved) (1)
routes:
None (141) · intranasal; rectal and IV reported. (1) · Oral (2) · Oral only. (1) · sublingual (1)
onset:
None (141) · 1-2 hours (slower than immediate-release amphetamine because activation requires enzymatic cleavage in red blood cells) (1) · Peak plasma concentrations 2-4 hours after oral dose. Wakefulness-promoting effect onset correlates with peak plasma; subjective alertness typically reported within 1-2 hours of dosing. (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (141) · 10-12 hours (smoother profile than immediate-release amphetamine salts) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Effective wakefulness promotion through approximately 12-15 hours reflecting the half-life of the predominant R-enantiomer. For shift-work use, 200 mg taken 1 hour before shift provides coverage through most 8-12 hour shifts. (1)
halflife:
None (142) · 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:
None (141) · Approximately 80% (well-absorbed orally; not significantly affected by food, though food may delay Tmax by ~1 hour).'"`UNIQ--ref-0000004D-QINU`"' (1) · Not formally characterized in humans. (1) · ~96% after red blood cell hydrolytic cleavage releases dextroamphetamine'"`UNIQ--ref-00000018-QINU`"' (1)
pregnancy:
None (142) · 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 (143) · [[USLegal:Schedule II|Schedule II controlled substance]] in US'"`UNIQ--ref-00000019-QINU`"' (1)

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