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Drilldown: Medicines

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Medicines > classes : NDRI or Research material & routes: Oral

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generic:
Bromazolam (1) · Dexmethylphenidate (1) · Methylphenidate (1)
brand:
(none, never marketed) (1) · Focalin, Focalin XR (1) · Ritalin, Ritalin LA, Concerta, Metadate CD, Daytrana, Quillivant XR (1)
classes: (Click arrow to add another value)
mechanism:
Norepinephrine–dopamine reuptake inhibition (DAT, NET) (1) · Norepinephrine–dopamine reuptake inhibition (DAT, NET), d-threo enantiomer of methylphenidate (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:
ADHD, narcolepsy (1) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000150-QINU`"', '"`UNIQ--vote-00000151-QINU`"' (1)
starting dose:
None (2) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
None (2) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (2) · N/A (never approved) (1)
routes: (Click arrow to add another value)
onset:
20–60 min (oral) (1) · 30–60 min (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
6–10 h subjective; full pharmacologic effect considerably longer. (1) · IR 3–5 h; LA/SR 6–8 h; Concerta 10–12 h; Daytrana ~9 h wear time (1) · IR 4–6 h; XR 8–12 h (1)
halflife:
2.2 h (IR parent); ~3 h (XR parent) (1) · 2–3 h (parent compound) (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1)
bioavailability:
Not formally characterized in humans. (1) · ~22–25% (1) · ~30% (high first-pass) (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) · Category C (1) · Pregnancy categories were retired by FDA in 2015. Limited reproductive data with small observational signal for cardiac malformations; risk-benefit decision, with many patients deferring ADHD treatment during pregnancy. See pregnancy_details for the full discussion. (1)
legal:
None (1) · Schedule II (2)

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