Drilldown: Medicines

Bisoprolol (1) · Bromazolam (1) · Metoprolol (1)

(none, never marketed) (1) · Lopressor (tartrate), Toprol XL (succinate) (1) · Zebeta (1)

Research material · Classic Psychedelic · Stimulant · Opioid · Sedative-Hypnotic · Phenethylamine · Tryptamine · Benzodiazepine · Botanical · [[:Category:Antihypertensives|Antihypertensive]] · Dissociative · Anticonvulsant · Antidepressant · Plant Medicine · Analgesic · Antiparkinsonian · Antipsychotic · Empathogen · Neuroleptic · Cathinone

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Cardioselective β1-adrenergic antagonist. Selectivity is dose-dependent and partially lost at higher doses. (1) · Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (1) · Positive allosteric modulator of the GABA_A receptor at the benzodiazepine binding site; increases frequency of Cl⁻ channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1)

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)

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)

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)

20 mg/d (1) · 400 mg/d (1) · N/A (never approved) (1)

None · Oral · IV · topical · IM · intranasal · rectal · Subcutaneous · topical ophthalmic · ophthalmic · intramuscular · intravenous · transdermal · vaginal · Subcutaneous (abdomen · sublingual · thigh · Inhaled · SC · intra-articular

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1–2 h (1) · 1–2 h (PO); immediate (IV) (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

24 h (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · 6–12 h (tartrate); 24 h (succinate) (1)

3–7 h (1) · 9–12 h (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1)

Not formally characterized in humans. (1) · ~50% (1) · ~90% (low first-pass) (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) · Category C (2)

None (1) · Rx-only in US (2)