Drilldown: Medicines
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generic:
brand:
classes: (Click arrow to add another value)
mechanism:
None (4) ·
Active metabolite of tramadol; mu-opioid agonist (1) ·
Extremely potent GABAA positive allosteric modulator (1) ·
Extremely potent mu-opioid receptor agonist (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) ·
Highly potent mu-opioid receptor agonist (1) ·
Kappa agonist; mu antagonist (1) ·
Kappa agonist; mu partial agonist (1) ·
Kappa agonist; mu partial agonist/antagonist (1) ·
Melatonin receptor agonist (2) ·
Mitragynine/7-hydroxymitragynine; mu-opioid partial agonist (1) ·
Mu-opioid agonist; modulates glutamate AMPA receptors (1) ·
Mu-opioid agonist; norepinephrine reuptake inhibitor (1) ·
Mu-opioid receptor agonist (4) ·
Mu-opioid receptor agonist; fentanyl analogue (1) ·
Mu-opioid receptor agonist; prodrug (metabolized to morphine) (1) ·
Mu-opioid receptor agonist; sodium channel blocker (1) ·
Mu/kappa/delta agonist; NMDA antagonist (1) ·
Opioid receptor partial agonist/antagonist; toxic alkaloid (1) ·
Partial mu-opioid receptor agonist; alpha-2 agonist (1) ·
Phosphodiesterase inhibitor; calcium channel blocker (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) ·
Potent mu-opioid receptor agonist (6) ·
Prodrug of morphine; mu-opioid receptor agonist (1) ·
Prodrug; converted to [[Morphine|morphine]] by [[Enzyme:CYP2D6|CYP2D6]] for analgesic action. (1) ·
Selective GABAA agonist (extrasynaptic delta subunit) (1) ·
Selective mu-opioid receptor agonist (1) ·
Ultra-short-acting mu-opioid agonist (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)
uses:
None (58) ·
Mild to moderate pain; cough suppression (low-dose). (1) ·
No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) ·
'"`UNIQ--vote-00000013-QINU`"' (1) ·
'"`UNIQ--vote-00000015-QINU`"', '"`UNIQ--vote-00000016-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 (58) ·
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) ·
Adult: 15–60 mg every 4 hours as needed. (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)
preparations:
None (58) ·
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) ·
Tablet (15, 30, 60 mg); oral solution; combination products (with [[Acetaminophen|acetaminophen]] or ibuprofen). (1)
fda max:
None (58) ·
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) ·
360 mg/day (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)
routes:
onset:
None (58) ·
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) ·
30–60 min (PO) (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)
duration:
None (58) ·
10-12 hours (smoother profile than immediate-release amphetamine salts) (1) ·
24 hours (once-daily or split BID dosing) (1) ·
4–6 hours (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 (58) ·
12-16 hours'"`UNIQ--ref-00000026-QINU`"' (1) ·
2.5–3 hours (1) ·
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) ·
~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)
bioavailability:
None (58) ·
Not formally characterized in humans. (1) ·
~50% (variable, CYP2D6-dependent for analgesic effect). (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)
pregnancy:
None (58) ·
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) ·
Avoid; risk of neonatal opioid withdrawal with chronic use; UM-mother breastfeeding contraindicated. (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.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Limited human data.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (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.">[[[Pharmacopedia:Citation needed|citation needed]]]</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.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1)
legal:
None (59) ·
US Schedule II (single-entity); Schedule III–V (combination products by content). (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)
Showing below up to 64 results in range #1 to #64.