Drilldown: Medicines

Bromazolam (1) · Flecainide (1) · Metoprolol (1) · Moxifloxacin (1)

(none, never marketed) (1) · Avelox (oral/IV brand discontinued US); Vigamox, Moxeza (ophthalmic) (1) · Lopressor (tartrate), Toprol XL (succinate) (1) · Tambocor (US brand discontinued) (1)

Beta Blocker (1) · Cardioselective (β1) (1) · Designer benzodiazepine (1) · Research material (1) · Sedative-Hypnotic (1) · Triazolobenzodiazepine (1) · [[:Category:Antiarrhythmics|Antiarrhythmic (Vaughan-Williams class IC)]] (1) · [[:Category:Antibacterials|Antibacterial]] (1) · [[:Category:Fluoroquinolones|Fluoroquinolone antibiotic]] (1)

Cardioselective β1-adrenergic antagonist. Selectivity is dose-dependent and partially lost at higher doses. (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) · '"`UNIQ--vote-00000D7A-QINU`"' Substantial QT-interval prolongation — the most QT-prolonging fluoroquinolone — limits use in patients on other QT-prolonging agents or with electrolyte abnormalities'"`UNIQ--ref-00000D7B-QINU`"'. (1) · '"`UNIQ--vote-0000113A-QINU`"' Concomitant β-blocker or CCB is required when used for AF to prevent 1:1 atrial flutter conduction (flecainide can slow atrial rate to a level where AV conduction allows dangerous ventricular rates). CYP2D6 substrate'"`UNIQ--ref-0000113B-QINU`"'. (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-00000D7C-QINU`"', '"`UNIQ--vote-00000D7D-QINU`"', '"`UNIQ--vote-00000D7E-QINU`"', '"`UNIQ--vote-00000D7F-QINU`"', '"`UNIQ--vote-00000D80-QINU`"', '"`UNIQ--vote-00000D81-QINU`"' (1) · '"`UNIQ--vote-0000113C-QINU`"', '"`UNIQ--vote-0000113D-QINU`"', '"`UNIQ--vote-0000113E-QINU`"' (1)

25–50 mg BID (tartrate); 25–100 mg daily (succinate); 12.5 mg daily in HFrEF (1) · 400 mg PO/IV once daily (1) · 50 mg PO BID; titrate to 100-200 mg BID; pill-in-pocket 200-300 mg PO single dose for AF conversion (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

400 mg tablets; 400 mg/250 mL IV; 0.5% ophthalmic solution (1) · 50, 100, 150 mg tablets (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 · Indication-specific · 40 mg/d · 10 mg/d · 20 mg/d · 80 mg/d · 10 mg/d (adults) · 100 mg/d · 4 g/d · 400 mg/d · 40 mg/d typical; up to 240 mg/d for Zollinger-Ellison · 5 mg/d · 50 mg/d · 600 mg/d · No fixed ceiling; titrate to clinical effect and tolerability with CDC opioid prescribing guidance constraints on morphine-milligram-equivalent (MME) totals · No fixed maximum; titrated to TSH target · TID per eye · Titrated to glucose; no fixed ceiling · Titrated to glucose; no fixed maximum · '''20 mg/day in adults >60 years''' per FDA's 2011-2012 QT-prolongation warning; 40 mg/day in adults ≤60

Other values:

Search

intranasal; rectal and IV reported. (1) · IV (2) · Oral (4) · sublingual (1) · topical ophthalmic (1)

1–2 h (PO); immediate (IV) (1) · AF conversion within hours of single PO dose (1) · Hours (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

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

3–7 h (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~12 hours'"`UNIQ--ref-00000D82-QINU`"' (1) · ~14 hours (adults); longer in elderly and renal impairment'"`UNIQ--ref-0000113F-QINU`"' (1)

Not formally characterized in humans. (1) · ~50% (1) · ~90% (oral)'"`UNIQ--ref-00001140-QINU`"' (1) · ~90% (oral; not affected by food but reduced by divalent cations)'"`UNIQ--ref-00000D83-QINU`"' (1)

'''Avoid in pregnancy where alternatives exist''' (animal cartilage toxicity).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (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 (1) · Use in fetal SVT (transplacental antiarrhythmic therapy) is established; otherwise weigh against alternatives.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

None (1) · Rx-only in US (1) · [[USLegal:Prescription only|Rx-only]] in US. '''Contraindicated in structural heart disease''' — CAST trial (1989) showed increased mortality from class IC agents in patients with prior MI; modern use is limited to structurally normal hearts'"`UNIQ--ref-00001141-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the same fluoroquinolone-class '''Boxed Warnings''' as ciprofloxacin/levofloxacin'"`UNIQ--ref-00000D84-QINU`"' (1)