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Drilldown: Medicines

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Medicines > classes : Analgesic or Anticonvulsant or Anxiolytic

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generic:
Codeine (2)
brand:
None (9)
classes: (Click arrow to add another value)
mechanism:
AMPA receptor antagonist (1) · GABA enhancer; sodium channel blocker; histone deacetylase inhibitor (1) · GABA reuptake inhibitor (GAT-1 blocker) (1) · GABA-A positive allosteric modulator'"`UNIQ--ref-00000067-QINU`"' '"`UNIQ--vote-00000068-QINU`"' (1) · GABAA modulator; glycine receptor agonist (1) · GABAA positive allosteric modulator (6) · GABAA positive allosteric modulator; lactate dehydrogenase inhibitor (1) · GABAA positive allosteric modulator; low sedation (1) · GABAA positive allosteric modulator; prodrug of desmethyldiazepam (1) · GABAA potentiator and direct activator (1) · Irreversible GABA-T inhibitor (1) · Kappa agonist; mu antagonist (1) · Kappa agonist; mu partial agonist (1) · Kappa agonist; mu partial agonist/antagonist (1) · Kavalactones; GABAA modulator; sigma receptor activity (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) · Multiple mechanisms; GPR55 antagonist; TRPV1 agonist (1) · NMDA antagonist; GABAA potentiator (1) · Partial mu-opioid agonist; kappa antagonist (1) · Phosphodiesterase inhibitor; calcium channel blocker (1) · Potent mu-opioid receptor agonist (3) · Prodrug of phenytoin; sodium channel blocker (1) · Prodrug; converted to [[Morphine|morphine]] by [[Enzyme:CYP2D6|CYP2D6]] for analgesic action. (1) · Serotonin releaser; sigma-1 agonist (1) · Serotonin–norepinephrine reuptake inhibition (balanced) (1) · Slow-inactivation sodium channel enhancer; CRMP-2 ligand (1) · Sodium channel blocker (2) · Sodium channel blocker; GABAA positive allosteric modulator (1) · Sodium channel modulator (1) · Sodium/T-type calcium channel blocker; carbonic anhydrase inhibitor (1) · SV2A ligand (higher affinity than levetiracetam) (1) · T-type calcium channel blocker (1) · TrkB/BDNF'"`UNIQ--ref-00000084-QINU`"' '"`UNIQ--vote-00000085-QINU`"' (1)
uses:
None (46) · Depression, anxiety, neuropathic pain, fibromyalgia, chronic musculoskeletal pain (1) · Mild to moderate pain; cough suppression (low-dose). (1) · '"`UNIQ--vote-00000069-QINU`"', '"`UNIQ--vote-0000006A-QINU`"', '"`UNIQ--vote-0000006B-QINU`"' (1)
starting dose:
None (46) · 0.25 mg (1) · 25 mg (1) · Adult: 15–60 mg every 4 hours as needed. (1)
preparations:
None (46) · 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) · Tablet (15, 30, 60 mg); oral solution; combination products (with [[Acetaminophen|acetaminophen]] or ibuprofen). (1)
fda max:
None (46) · 10 mg/d (1) · 200 mg/d (1) · 360 mg/day (1)
routes:
None (45) · Oral (3) · PO (only formulation marketed in the US). (1)
onset:
None (45) · 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)
duration:
None (45) · 4–6 hours (1) · 6 h (immediate-release); ~11 h (extended-release) (1) · Chronic daily dosing (1) · Long (1)
halflife:
None (45) · 11-13 h (immediate-release); 11-16 h (extended-release) (1) · 2.5–3 hours (1) · ~12 hours (1) · ~26 h (sertraline; range 13-45 h, longer in females); ~62-104 h (N-desmethylsertraline, weakly active) (1)
bioavailability:
None (45) · 80-90% oral (1) · Absolute bioavailability not precisely characterized; food modestly increases exposure (1) · ~50% (highly variable) (1) · ~50% (variable, CYP2D6-dependent for analgesic effect). (1)
pregnancy:
None (45) · 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 (45) · 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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