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Drilldown: Medicines

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Medicines > classes : Non-selective or Research material & routes: Oral

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generic:
Bromazolam (1) · Propranolol (1)
brand:
(none, never marketed) (1) · Inderal (1)
classes: (Click arrow to add another value)
mechanism:
Non-selective competitive antagonist at β1 and β2 adrenergic receptors. Lipophilic; significant blood–brain barrier penetration, accounting for its CNS effects. (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)
uses:
No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-000005E7-QINU`"', '"`UNIQ--vote-000005E8-QINU`"', '"`UNIQ--vote-000005E9-QINU`"', '"`UNIQ--vote-000005EA-QINU`"', '"`UNIQ--vote-000005EB-QINU`"' (1)
starting dose:
10–40 mg (situational anxiety); 40 mg BID (HTN) (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
10, 20, 40, 60, 80 mg tabs; 60/80/120/160 mg ER caps; 1 mg/mL IV (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
640 mg/d (HTN); 240 mg/d (migraine) (1) · N/A (never approved) (1)
routes: (Click arrow to add another value)
onset:
1–2 h (PO), immediate (IV) (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
6–10 h subjective; full pharmacologic effect considerably longer. (1) · 6–12 h (IR); 24 h (ER) (1)
halflife:
3–6 h (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1)
bioavailability:
Not formally characterized in humans. (1) · ~25% (extensive hepatic first-pass) (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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