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Medicines > classes : Research material or Tryptamine or [[:Category:Alpha-2 adrenergic agonists|Alpha-2 adrenergic agonist]]

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generic:
brand:
None (132) · (none, never marketed) (1) · Intuniv (extended-release), Tenex (immediate-release) (1) · Kapvay (ER, ADHD), Catapres (IR, antihypertensive), Catapres-TTS (transdermal patch), Duraclon (epidural injection) (1) · O-DSMT (1) · Zanaflex (1)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (27) · Monoamine releasing agent (9) · 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/norepinephrine/dopamine releasing agent (3) · None (2) · Cathinone analogue; monoamine reuptake inhibitor (2) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist (2) · Prodrug of GHB (2)
uses:
None (133) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"', '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"' (1) · '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (1) · '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"' (1)
starting dose:
None (133) · 2 mg PO every 6-8 hours; titrate by 2-4 mg per dose every 1-4 days; maximum single dose 16 mg, maximum daily dose 36 mg (1) · 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) · 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)
preparations:
None (133) · 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) · Tablets 2, 4 mg; capsules 2, 4, 6 mg ('''capsules and tablets are not bioequivalent''': capsules slower with food; tablets faster on empty stomach) (1)
fda max:
None (133) · 2.4 mg/day (HTN, IR); 0.4 mg/day (ADHD, Kapvay) (1) · 36 mg/day in three divided doses; single dose maximum 16 mg (1) · 7 mg/day in children and adolescents; weight-based ceiling (~0.12 mg/kg/day) applies in smaller patients (1) · N/A (never approved) (1)
routes:
None (133) · epidural injection (1) · intranasal; rectal and IV reported. (1) · Oral (4) · sublingual (1) · transdermal (1)
onset:
None (133) · 30-60 min (IR oral); 2-3 days to steady state (transdermal patch) (1) · 30-60 minutes (1) · Gradual; full clinical effect over 2-4 weeks of titration (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (133) · 3-6 hours per dose (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)
halflife:
None (133) · 12-16 hours'"`UNIQ--ref-00000026-QINU`"' (1) · 2.5 hours (short, requires TID-QID dosing)'"`UNIQ--ref-0000001D-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~17-18 hours (Intuniv ER); ~17 hours (immediate-release)'"`UNIQ--ref-00000020-QINU`"' (1)
bioavailability:
None (133) · Not formally characterized in humans. (1) · ~40% (oral); food and formulation substantially alter the absorption profile'"`UNIQ--ref-0000001E-QINU`"' (1) · ~58% (extended-release); ~80% (immediate-release)'"`UNIQ--ref-00000021-QINU`"' (1) · ~75-85% (oral); ~60% (transdermal at steady state)'"`UNIQ--ref-00000027-QINU`"' (1)
pregnancy:
None (133) · 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.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Older agent with substantial use experience but limited controlled data; case reports of neonatal sedation and transient hypertension with maternal use near term.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (134) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, distinguishing it from carisoprodol among muscle-spasm options'"`UNIQ--ref-0000001F-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)

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