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Medicines > routes : intra-articular or intranasal; rectal and IV reported. or topical ophthalmic

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mechanism:
None (8) · 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) · '"`UNIQ--vote-00000860-QINU`"' Activates the glucocorticoid receptor to broadly remodel inflammatory, immune, and metabolic transcription. Unlike prednisone, it does not require hepatic activation, making it the preferred oral choice in severe hepatic dysfunction'"`UNIQ--ref-00000861-QINU`"'. (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-000011D5-QINU`"' Minimal systemic absorption and the dual mechanism underlie its first-line role in seasonal allergic conjunctivitis. Comfort drops without preservatives are available for sensitive patients'"`UNIQ--ref-000011D6-QINU`"'. (1) · '"`UNIQ--vote-00001284-QINU`"' Systemic oral ketotifen (available outside US) has historical use for asthma adjunct therapy via the same dual mechanism, but oral use produces sedation and weight gain — the topical ophthalmic application largely avoids both'"`UNIQ--ref-00001285-QINU`"'. (1) · '"`UNIQ--vote-000013B1-QINU`"' Topical application minimizes systemic antihistaminic burden; the characteristic bitter taste with nasal use (drainage to oropharynx) is the main tolerability issue'"`UNIQ--ref-000013B2-QINU`"'. (1)
uses:
No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000415-QINU`"', '"`UNIQ--vote-00000416-QINU`"' (1) · '"`UNIQ--vote-00000661-QINU`"', '"`UNIQ--vote-00000662-QINU`"', '"`UNIQ--vote-00000663-QINU`"', '"`UNIQ--vote-00000664-QINU`"', '"`UNIQ--vote-00000665-QINU`"' (1) · '"`UNIQ--vote-00000862-QINU`"', '"`UNIQ--vote-00000863-QINU`"', '"`UNIQ--vote-00000864-QINU`"', '"`UNIQ--vote-00000865-QINU`"', '"`UNIQ--vote-00000866-QINU`"' (1) · '"`UNIQ--vote-00000932-QINU`"', '"`UNIQ--vote-00000933-QINU`"', '"`UNIQ--vote-00000934-QINU`"', '"`UNIQ--vote-00000935-QINU`"', '"`UNIQ--vote-00000936-QINU`"', '"`UNIQ--vote-00000937-QINU`"' (1) · '"`UNIQ--vote-00000B08-QINU`"', '"`UNIQ--vote-00000B09-QINU`"' (1) · '"`UNIQ--vote-00000CEF-QINU`"', '"`UNIQ--vote-00000CF0-QINU`"', '"`UNIQ--vote-00000CF1-QINU`"', '"`UNIQ--vote-00000CF2-QINU`"', '"`UNIQ--vote-00000CF3-QINU`"', '"`UNIQ--vote-00000CF4-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-00000D9E-QINU`"', '"`UNIQ--vote-00000D9F-QINU`"', '"`UNIQ--vote-00000DA0-QINU`"' (1) · '"`UNIQ--vote-00000E23-QINU`"', '"`UNIQ--vote-00000E24-QINU`"', '"`UNIQ--vote-00000E25-QINU`"', '"`UNIQ--vote-00000E26-QINU`"', '"`UNIQ--vote-00000E27-QINU`"', '"`UNIQ--vote-00000E28-QINU`"', '"`UNIQ--vote-00000E29-QINU`"', '"`UNIQ--vote-00000E2A-QINU`"' (1) · '"`UNIQ--vote-000010CE-QINU`"', '"`UNIQ--vote-000010CF-QINU`"', '"`UNIQ--vote-000010D0-QINU`"' (1) · '"`UNIQ--vote-000011D7-QINU`"', '"`UNIQ--vote-000011D8-QINU`"' (1) · '"`UNIQ--vote-00001286-QINU`"' (1) · '"`UNIQ--vote-000013B3-QINU`"', '"`UNIQ--vote-000013B4-QINU`"', '"`UNIQ--vote-000013B5-QINU`"' (1)
starting dose:
preparations:
0.005% ophthalmic solution (50 mcg/mL); typical 2.5 mL bottle (1) · 0.01%, 0.03% ophthalmic solution (1) · 0.025%, 0.035% ophthalmic solutions (1) · 0.1% (Patanol), 0.2% (Pataday once-daily original), 0.7% (Pataday 24-hour) ophthalmic solutions; 0.6% nasal spray (1) · 0.1%, 0.15% intranasal spray; 0.05% ophthalmic solution; combination Dymista (azelastine 0.137 mg + fluticasone 50 mcg/spray) (1) · 0.1%, 0.15%, 0.2% ophthalmic solutions; 0.33% topical gel; combinations with timolol (Combigan) and brinzolamide (Simbrinza) (1) · 0.5, 0.75, 1, 1.5, 2, 4, 6 mg tablets; oral solution; 4, 10, 20, 100 mg/mL IV; intravitreal implant (Ozurdex) (1) · 2% ophthalmic solution (Trusopt); 2%/0.5% fixed combination with timolol (Cosopt, Cosopt PF) (1) · 2, 4, 8, 16, 32 mg oral tablets; 40, 125, 500, 1000 mg IV vials; Depo-Medrol 20, 40, 80 mg/mL IM depot (1) · 250, 500, 750 mg IR tablets; 500, 1000 mg ER tablets (XR); 250, 500 mg/5 mL oral suspension; 200, 400 mg IV; 0.3% ophthalmic solution and ointment; 0.2% otic (1) · 250, 500, 750 mg tablets; 25 mg/mL oral solution; 25 mg/mL IV (premix bags 250, 500, 750 mg); 0.5%, 1.5% ophthalmic solutions (1) · 400 mg tablets; 400 mg/250 mL IV; 0.5% ophthalmic solution (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Topical creams, ointments, lotions, dental paste (0.025-0.5%); Kenalog 10 mg/mL, 40 mg/mL injection; Nasacort 55 mcg/spray intranasal; oral inhaler discontinued in US (1)
routes: (Click arrow to add another value)
pregnancy:
'''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 in pregnancy where alternatives exist''' (animal cartilage toxicity; class-wide concern).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · '''Avoid in pregnancy where alternatives exist''' (animal cartilage toxicity; class-wide concern); use only when benefit clearly outweighs.<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) · Generally considered safe (minimal systemic exposure).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe; minimal systemic exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (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; second-line to intranasal corticosteroids or PO loratadine/cetirizine.<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, though systemic exposure is low.<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> (2) · Topical/intranasal generally low-risk; intra-articular and high-dose injection: weigh risk individually.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Use when benefits outweigh; small association with oral clefts in first trimester debated.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Used in antenatal lung maturation (24-34 weeks gestation; 6 mg IM q12h × 4 doses); broader use weighs benefits against fetal HPA suppression.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

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