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: Anticonvulsant

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or [[:Category:AUD medicines|Alcohol use disorder medicine]]

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None (9)

None (3) · 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) · GABAA positive allosteric modulator (16) · GABAA positive allosteric modulator (non-benzodiazepine) (3) · GABAA positive allosteric modulator; lactate dehydrogenase inhibitor (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)

None (49) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1)

None (49) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

None (48) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Oral tablets 50 mg (ReVia, Depade, generics); Vivitrol extended-release IM suspension 380 mg single-dose vial; Contrave (naltrexone 8 mg + bupropion 90 mg ER tablets); compounded 1, 2, 3, 4.5 mg tablets/capsules for LDN (1)

None (48) · 50 mg/day oral; 380 mg/4 weeks IM (Vivitrol); 32 mg + 360 mg naltrexone/bupropion daily (Contrave maximum after titration) (1) · N/A (never approved) (1)

None (48) · intramuscular (depot) (1) · intranasal; rectal and IV reported. (1) · Oral (2) · sublingual (1)

None (48) · Oral peak plasma 1 hour; therapeutic opioid blockade within hours of first dose. IM Vivitrol: peak plasma 2-3 days; therapeutic blockade through the dosing interval. (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (48) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Oral mu-blockade clinically meaningful for 24-72 hours; IM Vivitrol blockade through 4 weeks. (1)

None (48) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Naltrexone parent ~4 hours (oral); 6-beta-naltrexol (active metabolite) ~13 hours. Vivitrol depot terminal half-life 5-10 days with sustained release from microspheres maintaining blockade for the 4-week dosing interval.'"`UNIQ--ref-0000004F-QINU`"' (1)

None (48) · Not formally characterized in humans. (1) · ~5-40% (oral, highly variable due to extensive first-pass metabolism; mean ~5-10% for parent naltrexone with the majority of pharmacologic effect coming from 6-beta-naltrexol). IM Vivitrol bypasses first-pass entirely.'"`UNIQ--ref-00000050-QINU`"' (1)

None (49) · 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)

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