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Drilldown: Medicines

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Medicines > classes : Cardioselective (β1) + vasodilator or Sedative-Hypnotic & routes: Oral

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generic:
Bromazolam (1) · Nebivolol (1)
brand:
(none, never marketed) (1) · Bystolic (1)
classes: (Click arrow to add another value)
mechanism:
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) · The d-enantiomer is a highly β1-selective antagonist; the l-enantiomer triggers endothelial nitric-oxide–mediated vasodilation. Unique among beta blockers for this NO mechanism. (1)
uses:
No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-0000059D-QINU`"' (1)
starting dose:
5 mg daily (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
2.5, 5, 10, 20 mg tabs (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
40 mg/d (1) · N/A (never approved) (1)
routes: (Click arrow to add another value)
onset:
1–2 h (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
24 h (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers) (1)
bioavailability:
Not formally characterized in humans. (1) · ~12% (extensive metabolizers); ~96% (poor metabolizers) (1)
pregnancy:
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)
legal:
None (1) · Rx-only in US (1)

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