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Medicines > classes : Research material or [[:Category:Beta blockers|Beta blocker (cardioselective β1)]] & routes: Oral

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generic:
Atenolol (1) · Bromazolam (1)
brand:
(none, never marketed) (1) · Tenormin (1)
classes: (Click arrow to add another value)
mechanism:
None (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-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (1)
starting dose:
25-50 mg PO once daily; titrate to 100 mg/day (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Tablets 25, 50, 100 mg (1)
fda max:
100-200 mg/day depending on indication (1) · N/A (never approved) (1)
routes: (Click arrow to add another value)
onset:
BP effect within hours; full effect over 1-2 weeks (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
24 hours (once-daily dosing supported by long elimination) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
6-9 hours (substantially longer in renal impairment due to renal elimination)'"`UNIQ--ref-00000020-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1)
bioavailability:
Not formally characterized in humans. (1) · ~50% (oral)'"`UNIQ--ref-00000021-QINU`"' (1)
pregnancy:
'''Documented fetal growth restriction with chronic exposure'''; avoid in pregnancy if alternative β-blockers are appropriate. The β-blocker most consistently associated with intrauterine growth concerns'"`UNIQ--ref-00000022-QINU`"' (1) · 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)
legal:
None (1) · [[USLegal:Prescription only|Rx-only]] in US (1)

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