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: Antidepressant

or Sedative-hypnotic

or Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism)

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None (10)

None (2) · 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) · Irreversible non-selective MAO inhibitor (3) · Melatonin receptor agonist (2) · Melatonin receptor agonist; 5-HT2C antagonist (1) · Mu-opioid agonist; modulates glutamate AMPA receptors (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) · Potent serotonin reuptake inhibitor; also NRI (1) · Reversible inhibitor of MAO-A (1) · Selective GABAA agonist (extrasynaptic delta subunit) (1) · Selective inverse agonist at 5HT2A receptors with weaker activity at 5HT2C. Has no significant dopamine D2 affinity, unique among approved antipsychotics. Inverse agonism (rather than antagonism) reduces constitutive 5HT2A receptor activity below baseline. (1) · Selective norepinephrine reuptake inhibitor (3) · Serotonin and norepinephrine reuptake inhibitor (3) · Serotonin reuptake inhibitor and 5-HT2A antagonist (1) · Serotonin–norepinephrine reuptake inhibition (balanced) (1) · Serotonin–norepinephrine reuptake inhibitor (2) · TrkB/BDNF'"`UNIQ--ref-00000084-QINU`"' '"`UNIQ--vote-00000085-QINU`"' (1) · Weak SRI; primarily H1/D2/alpha antagonist (1)

None (47) · Depression, anxiety, neuropathic pain, fibromyalgia, chronic musculoskeletal pain (1) · Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (1) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1)

None (47) · 25 mg (1) · 34 mg PO once daily (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

None (47) · 10 mg, 34 mg capsules/tablets (1) · 25 mg, 50 mg, 100 mg tablets; oral concentrate 20 mg/mL (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)

None (47) · 200 mg/d (1) · 34 mg/d (1) · N/A (never approved) (1)

None (46) · intranasal; rectal and IV reported. (1) · Oral (4) · sublingual (1)

None (46) · Anxiolysis classically 3-4 weeks, continuing improvement to 8-12 weeks (1) · Benefit over weeks of dosing (1) · Mood: 2–4 weeks. Pain: often within 1–2 weeks. (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (46) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Chronic daily dosing (1) · Daily dosing (1) · Long (1)

None (46) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~12 hours (1) · ~26 h (sertraline; range 13-45 h, longer in females); ~62-104 h (N-desmethylsertraline, weakly active) (1) · ~57 hours (parent), ~200 h (active metabolite) (1)

None (46) · Absolute bioavailability not precisely characterized; food modestly increases exposure (1) · Not characterized; oral dosing once daily (1) · Not formally characterized in humans. (1) · ~50% (highly variable) (1)

None (46) · 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 C (1) · Category C'"`UNIQ--ref-0000008F-QINU`"' (1) · Limited data; avoid (1)

None (47) · Rx-only (1) · Rx-only in US (1) · Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) (1)

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