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: Analgesic

or Sedative-hypnotic

or Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism)

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Codeine (2)

None (14) · (multiple, generic dominant) (1) · (none, never marketed) (1) · Dalmane (1) · Darvon (1) · Demerol (1) · Dilaudid (1) · Doral (1) · Doriden (1) · Duragesic (1) · Halcion (1) · Hetlioz (1) · Imovane (1) · Lunesta (1) · Mogadon (1) · Nembutal (1) · Nubain (1) · Nucynta (1) · Nuplazid (1) · Opana (1) · Placidyl (1) · ProSom (1) · Quaalude (1) · Restoril (1) · Rohypnol (1) · Rozerem (1) · Seconal (1) · Sonata (1) · Stadol (1) · Talwin (1) · THIP (1) · Versed (1) · Vicodin (1) · Xyrem (1)

None (2) · 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) · Kappa agonist; mu antagonist (1) · Kappa agonist; mu partial agonist (1) · Kappa agonist; mu partial agonist/antagonist (1) · Melatonin receptor agonist (2) · Mu-opioid agonist; norepinephrine reuptake inhibitor (1) · Mu-opioid receptor agonist (4) · Mu-opioid receptor agonist; prodrug (metabolized to morphine) (1) · Mu-opioid receptor agonist; sodium channel blocker (1) · Mu/kappa/delta agonist; NMDA antagonist (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 (3) · Prodrug; converted to [[Morphine|morphine]] by [[Enzyme:CYP2D6|CYP2D6]] for analgesic action. (1) · Selective GABAA agonist (extrasynaptic delta subunit) (1) · Selective inverse agonist at 5HT2A receptors with weaker activity at 5HT2C. Has no significant dopamine D2 affinity, unique among approved antipsychotics. Inverse agonism (rather than antagonism) reduces constitutive 5HT2A receptor activity below baseline. (1)

None (44) · Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (1) · 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)

None (44) · 34 mg PO once daily (1) · Adult: 15–60 mg every 4 hours as needed. (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

None (44) · 10 mg, 34 mg capsules/tablets (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Tablet (15, 30, 60 mg); oral solution; combination products (with [[Acetaminophen|acetaminophen]] or ibuprofen). (1)

None (44) · 34 mg/d (1) · 360 mg/day (1) · N/A (never approved) (1)

None (44) · intranasal; rectal and IV reported. (1) · Oral (2) · PO (only formulation marketed in the US). (1) · sublingual (1)

None (44) · 30–60 min (PO) (1) · Benefit over weeks of dosing (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (44) · 4–6 hours (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Daily dosing (1)

None (44) · 2.5–3 hours (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~57 hours (parent), ~200 h (active metabolite) (1)

None (44) · Not characterized; oral dosing once daily (1) · Not formally characterized in humans. (1) · ~50% (variable, CYP2D6-dependent for analgesic effect). (1)

None (44) · 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 data; avoid (1)

None (45) · Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) (1) · US Schedule II (single-entity); Schedule III–V (combination products by content). (1)

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