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Medicines > classes : Antidepressant or Opioid or Triazolobenzodiazepine

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generic:
Codeine (2)
brand:
None (13)
classes: (Click arrow to add another value)
mechanism:
Active metabolite of tramadol; mu-opioid agonist (1) · Extremely potent mu-opioid receptor agonist (1) · GABA-A positive allosteric modulator'"`UNIQ--ref-00000067-QINU`"' '"`UNIQ--vote-00000068-QINU`"' (1) · Highly potent mu-opioid receptor agonist (1) · Irreversible non-selective MAO inhibitor (3) · Kappa agonist; mu antagonist (1) · Kappa agonist; mu partial agonist (1) · Kappa agonist; mu partial agonist/antagonist (1) · Melatonin receptor agonist; 5-HT2C antagonist (1) · 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; 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) · Opioid receptor partial agonist/antagonist; toxic alkaloid (1) · Partial mu-opioid agonist; kappa antagonist (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) · Potent serotonin reuptake inhibitor; also NRI (1) · Prodrug of morphine; mu-opioid receptor agonist (1) · Prodrug; converted to [[Morphine|morphine]] by [[Enzyme:CYP2D6|CYP2D6]] for analgesic action. (1) · Reversible inhibitor of MAO-A (1) · Selective mu-opioid receptor agonist (1) · Selective norepinephrine reuptake inhibitor (3) · Serotonin and norepinephrine reuptake inhibitor (3) · Serotonin reuptake inhibitor and 5-HT2A antagonist (1) · Serotonin–norepinephrine reuptake inhibition (balanced) (1) · Serotonin–norepinephrine reuptake inhibitor (2) · TrkB/BDNF'"`UNIQ--ref-00000084-QINU`"' '"`UNIQ--vote-00000085-QINU`"' (1) · Ultra-short-acting mu-opioid agonist (1) · Weak SRI; primarily H1/D2/alpha antagonist (1)
uses:
None (48) · Depression, anxiety, neuropathic pain, fibromyalgia, chronic musculoskeletal pain (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) · '"`UNIQ--vote-00000069-QINU`"', '"`UNIQ--vote-0000006A-QINU`"', '"`UNIQ--vote-0000006B-QINU`"' (1)
starting dose:
None (48) · 0.25 mg (1) · 25 mg (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)
preparations:
None (48) · 0.25 mg, 0.5 mg, 1 mg, 2 mg tablets (immediate-release and orally disintegrating); 0.5 mg, 1 mg, 2 mg, 3 mg extended-release tablets; 1 mg/mL oral concentrate (1) · 25 mg, 50 mg, 100 mg tablets; oral concentrate 20 mg/mL (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)
fda max:
None (48) · 10 mg/d (1) · 200 mg/d (1) · 360 mg/day (1) · N/A (never approved) (1)
routes:
None (47) · intranasal; rectal and IV reported. (1) · Oral (4) · PO (only formulation marketed in the US). (1) · sublingual (1)
onset:
None (47) · 30-60 min (immediate-release); 1-2 h (extended-release) (1) · 30–60 min (PO) (1) · Anxiolysis classically 3-4 weeks, continuing improvement to 8-12 weeks (1) · Mood: 2–4 weeks. Pain: often within 1–2 weeks. (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (47) · 4–6 hours (1) · 6 h (immediate-release); ~11 h (extended-release) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Chronic daily dosing (1) · Long (1)
halflife:
None (47) · 11-13 h (immediate-release); 11-16 h (extended-release) (1) · 2.5–3 hours (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~12 hours (1) · ~26 h (sertraline; range 13-45 h, longer in females); ~62-104 h (N-desmethylsertraline, weakly active) (1)
bioavailability:
None (47) · 80-90% oral (1) · Absolute bioavailability not precisely characterized; food modestly increases exposure (1) · Not formally characterized in humans. (1) · ~50% (highly variable) (1) · ~50% (variable, CYP2D6-dependent for analgesic effect). (1)
pregnancy:
None (47) · 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) · Category C (1) · Category C'"`UNIQ--ref-0000008F-QINU`"' (1) · Category D'"`UNIQ--ref-0000006C-QINU`"' (1)
legal:
None (48) · Rx-only (1) · Rx-only in US (1) · Schedule IV (US) (1) · US Schedule II (single-entity); Schedule III–V (combination products by content). (1)

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