Drilldown: Medicines

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Medicines (732)

Medicines > classes

: Anticonvulsant

or Sedative-Hypnotic

or [[:Category:Anesthetics|Anesthetic]]

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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 (48) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (1)

None (48) · Infiltration: 1-2% solution; '''4.5 mg/kg ceiling without epinephrine, 7 mg/kg with epinephrine'''. IV antiarrhythmic: 1-1.5 mg/kg bolus then infusion 1-4 mg/minute. Lidoderm patch: up to 3 patches per 12 hours (1) · 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) · Injection 0.5-4% solutions (with and without epinephrine); topical cream 4-5%; transdermal patch 5% (Lidoderm), 1.8% (ZTLido); oral 2% viscous solution; jelly 2%; ophthalmic (1)

None (48) · '''4.5 mg/kg (without epinephrine), 7 mg/kg (with epinephrine)''' for infiltration; serum level monitoring required for prolonged IV antiarrhythmic use (1) · N/A (never approved) (1)

None (48) · epidural (1) · infiltration (1) · intranasal; rectal and IV reported. (1) · intravenous (1) · nerve block) (1) · Oral (1) · oral mucosal (1) · regional anesthesia (spinal (1) · sublingual (1) · Topical (1)

None (48) · <1 minute (IV); 1-2 minutes (infiltration); 30+ minutes (patch on adult skin, faster on thinner pediatric skin) (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (48) · 30-90 minutes (infiltration without epinephrine); 90-200 minutes (with epinephrine); 12 hours (patch) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)

None (48) · 1.5-2 hours'"`UNIQ--ref-00000020-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1)

None (48) · Not formally characterized in humans. (1) · ~35% (oral, extensive first-pass; not used orally for systemic effect); ~100% (IV)'"`UNIQ--ref-00000021-QINU`"' (1)

None (48) · 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) · Extensive use experience in obstetric anesthesia; broadly considered safe'"`UNIQ--ref-00000022-QINU`"' (1)

None (49) · [[USLegal:Prescription only|Rx-only]] for most formulations; some low-concentration topical formulations are [[USLegal:Over-the-counter|OTC]] (4% cream) (1)