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None (9)

None (2) · Butyrophenone D2 antagonist (1) · Cardioselective β1-adrenergic antagonist. Selectivity is dose-dependent and partially lost at higher doses. (1) · D2 receptor antagonist; also H1, alpha-1, muscarinic antagonist (1) · D2/5-HT2A antagonist (1) · D2/5-HT2A antagonist; 5-HT7 antagonist (1) · D2/5-HT2A antagonist; active metabolite of risperidone (1) · D2/5-HT2A antagonist; SRI and NRI (1) · Dibenzoxazepine D2/5-HT2 antagonist (1) · Dihydroindolone D2 antagonist (1) · Diphenylbutylpiperidine D2 antagonist (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) · Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (1) · Melatonin receptor agonist (2) · Multi-receptor antagonist (D2, 5-HT2A, H1, alpha) (1) · Multi-receptor antagonist; low D2 affinity (1) · Phenothiazine D2 antagonist (5) · 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) · Thioxanthene D2 antagonist (1)

None (46) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-000004F5-QINU`"', '"`UNIQ--vote-000004F6-QINU`"', '"`UNIQ--vote-000004F7-QINU`"', '"`UNIQ--vote-000004F8-QINU`"', '"`UNIQ--vote-000004F9-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1)

None (46) · 2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) · 25–50 mg BID (tartrate); 25–100 mg daily (succinate); 12.5 mg daily in HFrEF (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

None (46) · 5, 10 mg tabs (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Tartrate: 25, 50, 100 mg tabs; 1 mg/mL IV. Succinate ER: 25, 50, 100, 200 mg. (1)

None (46) · 20 mg/d (1) · 400 mg/d (1) · N/A (never approved) (1)

None (46) · intranasal; rectal and IV reported. (1) · IV (1) · Oral (3) · sublingual (1)

None (46) · 1–2 h (1) · 1–2 h (PO); immediate (IV) (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (46) · 24 h (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · 6–12 h (tartrate); 24 h (succinate) (1)

None (46) · 3–7 h (1) · 9–12 h (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1)

None (46) · Not formally characterized in humans. (1) · ~50% (1) · ~90% (low first-pass) (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 (2)

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