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Drilldown: Medicines

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Medicines > classes : GABAergic or Opioid or Sedative-Hypnotic

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generic:
Codeine (2)
brand:
None (28)
classes: (Click arrow to add another value)
mechanism:
GABAA positive allosteric modulator (15) · Potent mu-opioid receptor agonist (6) · Mu-opioid receptor agonist (4) · GABAA positive allosteric modulator (non-benzodiazepine) (3) · None (2) · GABAA potentiator and direct activator (2) · Melatonin receptor agonist (2) · Prodrug of GHB (2)
uses:
None (67) · 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 (67) · 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 (67) · 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 (67) · 360 mg/day (1) · N/A (never approved) (1)
routes:
None (67) · intranasal; rectal and IV reported. (1) · Oral (1) · PO (only formulation marketed in the US). (1) · sublingual (1)
onset:
None (67) · 30–60 min (PO) (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (67) · 4–6 hours (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
None (67) · 2.5–3 hours (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1)
bioavailability:
None (67) · Not formally characterized in humans. (1) · ~50% (variable, CYP2D6-dependent for analgesic effect). (1)
pregnancy:
None (67) · 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 (68) · US Schedule II (single-entity); Schedule III–V (combination products by content). (1)

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