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Drilldown: Medicines

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Medicines > classes : Cathinone or Sedative-Hypnotic or the first approved

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generic:
brand:
None (23) · (none, never marketed) (1) · Belsomra (1) · Dalmane (1) · Doral (1) · Doriden (1) · Halcion (1) · Hetlioz (1) · Imovane (1) · Lunesta (1) · Mogadon (1) · Nembutal (1) · Placidyl (1) · ProSom (1) · Quaalude (1) · Restoril (1) · Rohypnol (1) · Rozerem (1) · Seconal (1) · Sonata (1) · THIP (1) · Versed (1) · Xyrem (1)
classes: (Click arrow to add another value)
mechanism:
None (2) · Cathinone analogue; monoamine reuptake inhibitor (2) · Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1) · Extremely potent GABAA positive allosteric modulator (1) · GABAA positive allosteric modulator (15) · GABAA positive allosteric modulator (non-benzodiazepine) (3) · GABAA positive allosteric modulator; very long half-life (1) · GABAA potentiator (1) · GABAA potentiator and direct activator (2) · GABAB agonist; GHB receptor agonist (1) · Melatonin receptor agonist (2) · Monoamine releasing agent (4) · Monoamine releasing agent; active ingredient in khat (1) · Norepinephrine and dopamine releasing agent (1) · Norepinephrine/dopamine releasing agent (1) · Norepinephrine/dopamine reuptake inhibitor (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) · Selective GABAA agonist (extrasynaptic delta subunit) (1) · Serotonin releasing agent; monoamine reuptake inhibitor (1) · Serotonin/norepinephrine/dopamine releasing agent (3)
uses:
None (43) · Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1)
starting dose:
None (43) · 10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
None (43) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (43) · 20 mg/d (1) · N/A (never approved) (1)
routes:
None (43) · intranasal; rectal and IV reported. (1) · Oral (2) · sublingual (1)
onset:
None (43) · ~20–40 min PO; faster sublingual/intranasal. (1) · ~30 min (1)
duration:
None (43) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · ~7-8 hours (1)
halflife:
None (43) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~12 hours (1)
bioavailability:
None (43) · Not formally characterized in humans. (1) · ~82% (1)
pregnancy:
None (43) · 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) · Limited data; avoid (1)
legal:
None (44) · Rx, Schedule IV (US) (1)

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