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Medicines > classes : Anticonvulsant or Benzodiazepine or Sedative-Hypnotic

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generic:
brand:
None (10)
classes: (Click arrow to add another value)
mechanism:
None (2) · AMPA receptor antagonist (1) · Extremely potent GABAA positive allosteric modulator (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 positive allosteric modulator (19) · GABAA positive allosteric modulator (non-benzodiazepine) (3) · GABAA positive allosteric modulator; lactate dehydrogenase inhibitor (1) · GABAA positive allosteric modulator; low sedation (1) · GABAA positive allosteric modulator; prodrug of desmethyldiazepam (1) · GABAA positive allosteric modulator; very long half-life (1) · GABAA potentiator (1) · GABAA potentiator and direct activator (3) · GABAB agonist; GHB receptor agonist (1) · Irreversible GABA-T inhibitor (1) · Melatonin receptor agonist (2) · Multiple mechanisms; GPR55 antagonist; TRPV1 agonist (1) · NMDA antagonist; GABAA potentiator (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) · Prodrug of phenytoin; sodium channel blocker (1) · Selective GABAA agonist (extrasynaptic delta subunit) (1) · Serotonin releaser; sigma-1 agonist (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)
uses:
None (53) · 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 (53) · 0.25 mg (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
None (53) · 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) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (53) · 10 mg/d (1) · N/A (never approved) (1)
routes:
None (53) · intranasal; rectal and IV reported. (1) · Oral (2) · sublingual (1)
onset:
None (53) · 30-60 min (immediate-release); 1-2 h (extended-release) (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (53) · 6 h (immediate-release); ~11 h (extended-release) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
None (53) · 11-13 h (immediate-release); 11-16 h (extended-release) (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1)
bioavailability:
None (53) · 80-90% oral (1) · Not formally characterized in humans. (1)
pregnancy:
None (53) · 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) · Category D'"`UNIQ--ref-0000006C-QINU`"' (1)
legal:
None (54) · Schedule IV (US) (1)

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