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Medicines (732)

Medicines > classes

: Sedative-Hypnotic

or [[:Category:Cardiovascular_agents|Cardiovascular agent]]

& routes: Oral

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Amiodarone (1) · Bromazolam (1)

(none, never marketed) (1) · Cordarone, Pacerone, Nexterone (IV) (1)

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)

No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000CB0-QINU`"', '"`UNIQ--vote-00000CB1-QINU`"', '"`UNIQ--vote-00000CB2-QINU`"' (1)

No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Oral load 800-1600 mg/d in divided doses for 1-3 weeks, then 600-800 mg/d for 1 month, then 200-400 mg/d maintenance; IV 150 mg over 10 min then 1 mg/min for 6 hours then 0.5 mg/min (1)

100, 200, 400 mg tablets; 50 mg/mL IV (with polysorbate 80 in older formulations causing hypotension); 1.5 mg/mL Nexterone IV (PVC-free, lower hypotension risk) (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)

N/A (never approved) (1) · Oral maintenance 400 mg/d typical; higher in refractory cases (1)

IV: minutes; oral: weeks to load (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

6–10 h subjective; full pharmacologic effect considerably longer. (1) · Weeks after discontinuation (extremely long half-life) (1)

Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~58 days (parent); ~61 days (desethylamiodarone, active metabolite)'"`UNIQ--ref-00000CB3-QINU`"' (1)

Not formally characterized in humans. (1) · ~50% (oral; highly variable)'"`UNIQ--ref-00000CB4-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) · Generally avoided; fetal goiter/hypothyroidism risk (iodine load). Used only for life-threatening arrhythmia.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1)

None (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries '''Boxed Warnings''' for pulmonary toxicity (interstitial pneumonitis, fibrosis), hepatotoxicity, and proarrhythmia'"`UNIQ--ref-00000CB5-QINU`"' (1)

Showing below up to 2 results in range #1 to #2.

A

Amiodarone

B

Bromazolam

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