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Medicines > classes

: Phenethylamine

or Sedative-Hypnotic

or [[:Category:ADHD medicines|ADHD medicine]]

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None (4) · 5-HT2A agonist (12) · 5-HT2A agonist; long duration (1) · 5-HT2A agonist; MAO inhibitor (1) · 5-HT2A agonist; milder than other 2C-x (1) · 5-HT2A partial agonist (1) · Extremely potent 5-HT2A agonist; vasoconstrictor (1) · Extremely potent 5-HT2A agonist; very long duration (1) · Extremely potent GABAA positive allosteric modulator (1) · GABAA positive allosteric modulator (15) · GABAA positive allosteric modulator (non-benzodiazepine) (3) · GABAA positive allosteric modulator; very long half-life (1) · GABAA potentiator (1) · GABAA potentiator and direct activator (2) · GABAB agonist; GHB receptor agonist (1) · Melatonin receptor agonist (2) · Positive allosteric modulator of the GABAA receptor at the benzodiazepine binding site; increases frequency of Cl− channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1) · Potent 5-HT2A agonist (5) · Potent 5-HT2A agonist; no oral activity (1) · Potent 5-HT2A agonist; very long duration (1) · Selective GABAA agonist (extrasynaptic delta subunit) (1) · Very potent 5-HT2A agonist; long duration (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) · '"`UNIQ--vote-00000019-QINU`"' Sedation and hypotension are the dose-limiting effects; gradual titration and bedtime or split dosing mitigate both. Abrupt discontinuation can precipitate rebound hypertension, particularly with long-standing use'"`UNIQ--ref-0000001A-QINU`"'. (1)

None (55) · ADHD (Kapvay ER): 0.1 mg PO at bedtime, titrate weekly to 0.4 mg/day divided BID. HTN (IR): 0.1 mg PO BID, titrate by 0.1 mg increments (1) · 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) · Children ≤70 kg: 0.5 mg/kg/day, titrate to 1.2 mg/kg/day after 3 days. Adults and children >70 kg: 40 mg PO once daily for 3 days, then 80 mg/day, then if needed 100 mg/day after 2-4 weeks (1) · Intuniv ER 1 mg PO once daily; titrate by 1 mg/week as tolerated to clinical response (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

None (55) · Capsules 10, 18, 25, 40, 60, 80, 100 mg (1) · Capsules 10, 20, 30, 40, 50, 60, 70 mg; chewable tablets 10, 20, 30, 40, 50, 60 mg (1) · Extended-release tablets 1, 2, 3, 4 mg (Intuniv); immediate-release tablets 1, 2 mg (Tenex) (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · IR tablets 0.1, 0.2, 0.3 mg; ER tablets 0.1, 0.2 mg (Kapvay); transdermal patches 0.1, 0.2, 0.3 mg/24h (TTS-1/2/3, weekly); epidural injection (Duraclon) (1)

None (55) · 100 mg/day (adult); 1.4 mg/kg/day or 100 mg total (pediatric, whichever lower) (1) · 2.4 mg/day (HTN, IR); 0.4 mg/day (ADHD, Kapvay) (1) · 7 mg/day in children and adolescents; weight-based ceiling (~0.12 mg/kg/day) applies in smaller patients (1) · 70 mg/day (1) · N/A (never approved) (1)

None (54) · epidural injection (1) · insufflated (1) · intranasal; rectal and IV reported. (1) · Oral (6) · PR (1) · sublingual (1) · transdermal (1)

None (54) · 1-2 hours (slower than immediate-release amphetamine because activation requires enzymatic cleavage in red blood cells) (1) · 30-60 min (IR oral); 2-3 days to steady state (transdermal patch) (1) · 45-75 min (oral) (1) · ADHD effect emerges over 1-2 weeks (slower than psychostimulants); full effect 4-6 weeks (1) · Gradual; full clinical effect over 2-4 weeks of titration (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (54) · 10-12 hours (smoother profile than immediate-release amphetamine salts) (1) · 24 hours (once-daily or split BID dosing) (1) · 4-8 h (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · 8-12 hours (IR); ~7 days (transdermal patch) (1) · ~24 hours (ER formulation supports once-daily dosing) (1)

None (54) · 12-16 hours'"`UNIQ--ref-00000026-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Not well characterized (1) · Parent lisdexamfetamine <1 hour; dextroamphetamine 10-12 hours after release'"`UNIQ--ref-00000017-QINU`"' (1) · ~17-18 hours (Intuniv ER); ~17 hours (immediate-release)'"`UNIQ--ref-00000020-QINU`"' (1) · ~5 hours in extensive CYP2D6 metabolizers; ~21 hours in CYP2D6 poor metabolizers'"`UNIQ--ref-00000014-QINU`"' (1)

None (54) · Not formally characterized in humans. (1) · Not well characterized (1) · ~58% (extended-release); ~80% (immediate-release)'"`UNIQ--ref-00000021-QINU`"' (1) · ~63% (oral; extensive first-pass)'"`UNIQ--ref-00000015-QINU`"' (1) · ~75-85% (oral); ~60% (transdermal at steady state)'"`UNIQ--ref-00000027-QINU`"' (1) · ~96% after red blood cell hydrolytic cleavage releases dextroamphetamine'"`UNIQ--ref-00000018-QINU`"' (1)

None (54) · 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. Animal studies show fetal effects at maternally toxic doses; use only if benefits justify the potential risk.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Limited human data.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Limited human data; the amphetamine class is associated with intrauterine growth restriction and neonatal withdrawal symptoms.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Not established (1) · Older agent with substantial use experience but limited controlled data; case reports of neonatal sedation and transient hypertension with maternal use near term.[[[Pharmacopedia:Citation needed|citation needed]]] (1)

None (55) · [[USLegal:DEA Schedule I|Schedule I]] (United States) (1) · [[USLegal:Prescription only|Rx-only]] in US. '''Not a controlled substance''', the principal clinical selling point versus psychostimulant ADHD options. Carries the antidepressant-class '''Boxed Warning''' for suicidal ideation in pediatric patients'"`UNIQ--ref-00000016-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, like guanfacine and unlike the psychostimulant alternatives for ADHD'"`UNIQ--ref-00000028-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, which is a meaningful contrast to the psychostimulant alternatives for ADHD'"`UNIQ--ref-00000022-QINU`"' (1) · [[USLegal:Schedule II|Schedule II controlled substance]] in US'"`UNIQ--ref-00000019-QINU`"' (1)

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