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Drilldown: Medicines

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Medicines > classes : Analgesic or Empathogen or Sedative-Hypnotic

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generic:
Codeine (2)
brand:
None (30) · (multiple, generic dominant) (1) · (none, never marketed) (1) · Dalmane (1) · Darvon (1) · Demerol (1) · Dilaudid (1) · Dolophine (1) · Doral (1) · Doriden (1) · Duragesic (1) · Halcion (1) · Hetlioz (1) · Imovane (1) · Lunesta (1) · Mogadon (1) · Nembutal (1) · Nubain (1) · Nucynta (1) · Opana (1) · Placidyl (1) · ProSom (1) · Quaalude (1) · Restoril (1) · Rohypnol (1) · Rozerem (1) · Seconal (1) · Sonata (1) · Stadol (1) · Suboxone (1) · Talwin (1) · THIP (1) · Versed (1) · Vicodin (1) · Xyrem (1)
classes: (Click arrow to add another value)
mechanism:
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) · MAO inhibitor; monoamine releasing agent (1) · MAO inhibitor; serotonin releasing agent (1) · Melatonin receptor agonist (2) · Monoamine releasing agent (3) · Monoamine releasing agent; 5-HT2A agonist (1) · Monoamine releasing agent; serotonergic at higher doses (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 mu-opioid agonist; kappa 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) · Serotonin releasing agent (2) · Serotonin releasing agent; 5-HT2A agonist (3) · Serotonin/dopamine/norepinephrine releasing agent; 5-HT2A agonist (1) · Serotonin/norepinephrine/dopamine releasing agent (3)
uses:
None (62) · 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)
starting dose:
None (62) · 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)
preparations:
None (62) · 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)
fda max:
None (62) · 360 mg/day (1) · N/A (never approved) (1)
routes:
None (62) · intranasal; rectal and IV reported. (1) · Oral (1) · PO (only formulation marketed in the US). (1) · sublingual (1)
onset:
None (62) · 30–60 min (PO) (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (62) · 4–6 hours (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
None (62) · 2.5–3 hours (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1)
bioavailability:
None (62) · Not formally characterized in humans. (1) · ~50% (variable, CYP2D6-dependent for analgesic effect). (1)
pregnancy:
None (62) · 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)
legal:
None (63) · US Schedule II (single-entity); Schedule III–V (combination products by content). (1)

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