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Medicines > classes : 5HT2A or Analgesic or Phenethylamine

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generic:
Codeine (2)
brand:
None (30) · (multiple, generic dominant) (1) · Darvon (1) · Demerol (1) · Dilaudid (1) · Dolophine (1) · Duragesic (1) · Nexus, Eroxan (historical, late-1980s through mid-1990s) (1) · Nubain (1) · Nucynta (1) · Opana (1) · Rexulti (1) · Stadol (1) · Suboxone (1) · Talwin (1) · Vicodin (1)
classes: (Click arrow to add another value)
mechanism:
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) · Kappa agonist; mu antagonist (1) · Kappa agonist; mu partial agonist (1) · Kappa agonist; mu partial agonist/antagonist (1) · Mu-opioid agonist; norepinephrine reuptake inhibitor (1) · Mu-opioid receptor agonist (4) · Mu-opioid receptor agonist; NMDA antagonist (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) · Partial agonist at D2 and 5HT1A. Antagonist at 5HT2A, α1A, α1B, α2C. More potent 5HT2A antagonism, 5HT1A partial agonism, and α1 antagonism (relative to D2 partial agonism) than aripiprazole, proposed to reduce akathisia and enhance affective/cognitive effects. (1) · Partial mu-opioid agonist; kappa antagonist (1) · Phosphodiesterase inhibitor; calcium channel blocker (1) · Potent 5-HT2A agonist (5) · Potent 5-HT2A agonist; no oral activity (1) · Potent 5-HT2A agonist; very long duration (1) · Potent mu-opioid receptor agonist (3) · Prodrug; converted to [[Morphine|morphine]] by [[Enzyme:CYP2D6|CYP2D6]] for analgesic action. (1) · Very potent 5-HT2A agonist; long duration (1)
uses:
None (43) · Mild to moderate pain; cough suppression (low-dose). (1) · Schizophrenia (FDA-approved 2015). Adjunctive treatment of major depressive disorder (2015). '''Agitation associated with dementia due to Alzheimer disease''' (FDA-approved May 2023, first agent specifically approved for this problem). Investigational for PTSD (combined with sertraline). (1)
starting dose:
None (43) · Adult: 15–60 mg every 4 hours as needed. (1) · Schizophrenia: 1 mg PO daily × 4 days, then 2 mg daily × 3 days, then 4 mg daily. MDD adjunct: 0.5-1 mg daily, increase to 2 mg max. AD agitation: 0.5 mg daily, titrate to 2-3 mg daily. (1)
preparations:
None (43) · 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets (1) · Tablet (15, 30, 60 mg); oral solution; combination products (with [[Acetaminophen|acetaminophen]] or ibuprofen). (1)
fda max:
None (43) · 360 mg/day (1) · 4 mg/d (schizophrenia); 3 mg/d (AD agitation); 3 mg/d (MDD adjunct) (1)
routes:
None (42) · insufflated (1) · Oral (2) · PO (only formulation marketed in the US). (1) · PR (1)
onset:
None (42) · 30–60 min (PO) (1) · 45-75 min (oral) (1) · Weeks for psychosis/depression; AD agitation benefit emerges over weeks (1)
duration:
None (42) · 4-8 h (1) · 4–6 hours (1) · Daily dosing (1)
halflife:
None (42) · 2.5–3 hours (1) · Not well characterized (1) · ~91 hours (1)
bioavailability:
None (42) · Not well characterized (1) · ~50% (variable, CYP2D6-dependent for analgesic effect). (1) · ~95% (1)
pregnancy:
None (42) · Avoid; risk of neonatal opioid withdrawal with chronic use; UM-mother breastfeeding contraindicated. (1) · Limited data; National Pregnancy Registry available (1) · Not established (1)
legal:
None (42) · Rx (1) · US Schedule II (single-entity); Schedule III–V (combination products by content). (1) · [[USLegal:DEA Schedule I|Schedule I]] (United States) (1)

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