Drilldown: Medicines

Brimonidine (1) · Bromazolam (1) · Dorzolamide (1)

(none, never marketed) (1) · Alphagan P (ophthalmic glaucoma), Mirvaso (topical rosacea) (1) · Trusopt; with timolol as Cosopt (1)

Designer benzodiazepine (1) · Research material (1) · Sedative-Hypnotic (1) · Triazolobenzodiazepine (1) · [[:Category:Alpha-2_agonists|Alpha-2 adrenergic agonist]] (1) · [[:Category:Carbonic_anhydrase_inhibitors|Carbonic anhydrase inhibitor (topical)]] (1) · [[:Category:Glaucoma_medications|Glaucoma medication]] (2) · [[:Category:Ocular_hypotensive_agents|Ocular hypotensive agent]] (2)

None (2) · 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-00000B08-QINU`"', '"`UNIQ--vote-00000B09-QINU`"' (1) · '"`UNIQ--vote-000010CE-QINU`"', '"`UNIQ--vote-000010CF-QINU`"', '"`UNIQ--vote-000010D0-QINU`"' (1)

1 drop in affected eye(s) TID (monotherapy); BID with timolol (Cosopt) (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Ophthalmic 1 drop in affected eye(s) TID; topical Mirvaso 0.33% gel applied to face daily (1)

0.1%, 0.15%, 0.2% ophthalmic solutions; 0.33% topical gel; combinations with timolol (Combigan) and brinzolamide (Simbrinza) (1) · 2% ophthalmic solution (Trusopt); 2%/0.5% fixed combination with timolol (Cosopt, Cosopt PF) (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (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:

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

IOP lowering at 1 hour; max at 2-3 hours (1) · IOP lowering at 2 hours; max at 4 hours (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

6–10 h subjective; full pharmacologic effect considerably longer. (1) · 8-12 hours (1) · 8-12 hours (TID dosing needed) (1)

Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~3 hours'"`UNIQ--ref-000010D1-QINU`"' (1) · ~4 months in erythrocytes (carbonic anhydrase binding in red cells; not relevant to topical IOP duration)'"`UNIQ--ref-00000B0A-QINU`"' (1)

Not formally characterized in humans. (1) · Topical with measurable systemic absorption (small CA inhibition observed clinically with chronic use)'"`UNIQ--ref-00000B0B-QINU`"' (1) · Topical; clinically meaningful systemic absorption can produce systemic α2 effects (somnolence, hypotension), especially in children'"`UNIQ--ref-000010D2-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) · Limited data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; 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) · [[USLegal:Prescription only|Rx-only]] in US (2)