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Medicines > routes : Topical ophthalmic or topical or transdermal

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brand:
classes:
[[:Category:Antibacterials|Antibacterial]] (6) · [[:Category:Corticosteroids|Corticosteroid]] (6) · [[:Category:Glaucoma_medications|Glaucoma medication]] (4) · [[:Category:Ocular_hypotensive_agents|Ocular hypotensive agent]] (4) · [[:Category:Fluoroquinolones|Fluoroquinolone antibiotic]] (3) · [[:Category:Glucocorticoids|Glucocorticoid]] (3) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist]] (3) · [[:Category:Mast_cell_stabilizers|Mast cell stabilizer]] (3) · [[:Category:Antifungals|Antifungal]] (2) · [[:Category:Inhaled_corticosteroids|Inhaled corticosteroid (ICS)]] (2) · [[:Category:Ophthalmic_antihistamines|Ophthalmic antihistamine]] (2) · [[:Category:Prostaglandin_analogs|Prostaglandin F2α analog]] (2) · [[:Category:Topical_antifungals|Topical antifungal]] (2)
mechanism:
None (32) · Norepinephrine–dopamine reuptake inhibition (DAT, NET) (1) · Tropane alkaloids: hyoscyamine (dominant; the racemic form is atropine), scopolamine. Competitive muscarinic antagonism. (1) · '"`UNIQ--vote-0000001D-QINU`"' Major Beers-list concern in elderly patients for cognitive and fall risks. CYP2D6 substrate. At massive overdose, also produces sodium channel blockade with cardiac toxicity'"`UNIQ--ref-0000001E-QINU`"'. '"`UNIQ--effect-0000001F-QINU`"' (1) · '"`UNIQ--vote-000009FD-QINU`"' Active against gram-positive cocci including MRSA; the unique target underlies the absence of cross-resistance with other antibiotic classes. High-level resistance (plasmid-mediated mupA) is rising and limits prolonged or repeated use'"`UNIQ--ref-000009FE-QINU`"'. (1) · '"`UNIQ--vote-00000D11-QINU`"' Same mechanistic family as amphotericin B but with prohibitive systemic toxicity at therapeutic doses, hence restriction to topical and luminal-gut indications. No clinically meaningful resistance after decades of use'"`UNIQ--ref-00000D12-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-00001014-QINU`"' Activates the glucocorticoid receptor to broadly remodel inflammatory, immune, and metabolic transcription. The dipropionate, valerate, and augmented dipropionate ester forms determine topical potency (high to super-high)'"`UNIQ--ref-00001015-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-00001233-QINU`"' Onychomycosis cure rates with nail lacquer are modest (mycologic cure ~30-50%, complete cure ~5-12% at 48 weeks); oral terbinafine remains substantially more effective when systemic therapy is acceptable'"`UNIQ--ref-00001234-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:
'"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (2)
starting dose:
None (2)
preparations:
fda max:
None (2) · '''4.5 mg/kg (without epinephrine), 7 mg/kg (with epinephrine)''' for infiltration; serum level monitoring required for prolonged IV antiarrhythmic use (1) · 1 drop per eye q8-12h (1) · 1 drop/eye/day (more frequent dosing reduces efficacy) (1) · 150 mg/day (oral); use lowest effective dose for shortest duration per FDA NSAID class guidance (1) · 2 sprays/nostril BID (1) · 2.4 mg/day (HTN, IR); 0.4 mg/day (ADHD, Kapvay) (1) · 23 mg/day (1) · 250 mg/d (1) · 30 mg/d (XL) typical (1) · 300 mg/day (depression, hospitalized); 150 mg/day outpatient; 6 mg/day for insomnia (1) · 300 mg/day (oral) (1) · 4 g/d (rarely tolerated due to GI effects) (1) · 4% topical; limit duration of use (1) · 4.8 g/d (IV severe infection) (1) · 400 mg/d (1) · 50 g/week (cream/ointment); 2-week continuous limit; 4-week maximum cumulative (1) · 750 mg/d (1) · BID topical; once daily nail lacquer (1) · ICS 880 mcg/d (asthma); intranasal 200 mcg/d (1) · Indication-specific (4) · Indication-specific; high-dose IV regimens for encephalitis or disseminated disease (1) · Indication-specific; lowest effective dose for shortest duration is the WHI-era standard (1) · Indication-specific; titrated to effect (1) · Intranasal 200 mcg/d (adults); inhaled 880 mcg/d (1) · Limit topical to 10-day courses to reduce resistance pressure (1) · Once daily (Pataday 0.7%); BID (other ophthalmic) (1) · One drop per eye per day (1) · Per formulation (1) · Single 200-400 mcg/kg per dose for systemic indications (1) · TID per eye (2) · Titrated; risk of hypercalcemia is the limiting factor (1) · Topical: BID; troche: 5×/day (1) · Topical: nightly; oral APL: 45 mg/m²/d (1) · Topical: nightly; systemic: regimen-specific (1) · Topical: per formulation; oral supplement age-dependent (1) · ~1500 mg/d (oral); 1200 mg/d (IV) (1) · ~4 g/d (severe systemic infection) (1)
routes: (Click arrow to add another value)
onset:
None (1) · 15 minutes (1) · 15-30 minutes (oral); 1-2 minutes (IV) (1) · 20–60 min (oral) (1) · 30-60 min (IR oral); 2-3 days to steady state (transdermal patch) (1) · 30-60 minutes (oral); slower for topical (1) · 30-60 minutes (PO) (1) · <1 minute (IV); 1-2 minutes (infiltration); 30+ minutes (patch on adult skin, faster on thinner pediatric skin) (1) · Caries reduction over months to years of consistent use (1) · Clinical and mycologic cure follows the full course; nail clearance over months of regrowth (1) · Cognitive effect emerges gradually over weeks to months; ceiling effect at the therapeutic dose (1) · Days (2) · Days for calcium effect; weeks for PTH suppression (1) · Days for dermatophyte clearance; nail clearance over months (1) · Hours (8) · Hours to days (1) · Hours to days for inflammation; substantial improvement within 1 week (1) · Inhaled: bronchial effect 1-2 weeks; nasal: symptom relief 12-24 hours; topical: hours (1) · Intranasal: symptom relief 12-24 hours; inhaled: bronchial effect 1-2 weeks (1) · IOP lowering at 1 hour; max at 2-3 hours (1) · IOP lowering at 2 hours; max at 4 hours (1) · IOP lowering at 3-4 hours; maximum at 8-12 hours (1) · IOP lowering at 4 hours, maximum at 8-12 hours; eyelash effect after 2 months (1) · Minutes (1) · SL/spray: 1-3 minutes; IV: minutes; patch: 30-60 minutes (1) · Sleep effect from first dose; antidepressant effect over 1-4 weeks (1) · Symptom relief within 24-48 hours of starting episodic treatment (1) · Symptom relief within 30-60 minutes (1) · Symptom relief within days (1) · Topical hours; intra-articular days to weeks (1) · Topical: inflammation, erythema, crusting at 2 weeks; complete response weeks to months after course (1) · Topical: irritation within days; acne improvement 6-12 weeks; oral APL response within days (1) · Vasomotor relief 2-4 weeks; bone density gains over months (1) · Visible lightening at 4-12 weeks (1) · Within minutes (1)
halflife:
bioavailability:
pregnancy:
None (3) · '''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 from 20 weeks gestation onward per FDA's 2020 expanded NSAID warning (fetal renal dysfunction, oligohydramnios); contraindicated from 30 weeks (risk of premature ductus arteriosus closure)'"`UNIQ--ref-0000002B-QINU`"' (1) · Contraindicated in pregnancy (use is not appropriate during gestation; class label X). Lactation considerations vary by indication.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Extensive use experience in obstetric anesthesia; broadly considered safe'"`UNIQ--ref-00000022-QINU`"' (1) · Generally avoided in pregnancy.<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 absorption).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · 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 after the first trimester; first-trimester use weighed against indication.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe in pregnancy (no systemic absorption).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe; commonly used in pregnancy.<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> (2) · Inhaled and intranasal generally considered safe; widely used in asthma in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Intranasal long considered acceptable; widely used in obstetric rhinitis.<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> (2) · Limited data; generally avoided in pregnancy for the cosmetic indication of onychomycosis.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; risk-benefit case by case; pregnancy is not a strict contraindication in WHO mass drug administration programs.<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) · Limited human data; rarely indicated in pregnancy given the patient population.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Older agent with substantial use experience but limited controlled data; case reports of neonatal sedation and transient hypertension with maternal use near term.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Older agent with substantial use experience; broadly considered safe in pregnancy'"`UNIQ--ref-00000028-QINU`"' (1) · Pregnancy categories were retired by FDA in 2015. Limited reproductive data with small observational signal for cardiac malformations; risk-benefit decision, with many patients deferring ADHD treatment during pregnancy. See pregnancy_details for the full discussion. (1) · Safe at routine fluoride levels.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · TCA class signal; limited human data specific to doxepin.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Topical and vaginal generally considered safe; widely used.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Topical corticosteroids in pregnancy: use lowest potency and smallest area; super-potent agents like clobetasol are reserved for compelling indications.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · 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) · Topical: avoid; systemic: contraindicated in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Use when benefits outweigh; widely used at physiologic doses for adrenal insufficiency.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Used in obstetric emergencies (uterine relaxation, severe hypertension) when needed; otherwise limited routine use.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Used when needed for hypoparathyroidism or renal osteodystrophy in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Widely used in pregnancy for HSV/VZV indications; reassuring registry data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (1) · OTC (Astepro 0.15%) and [[USLegal:Prescription only|Rx-only]] (other intranasal, ophthalmic, Dymista) in US (1) · OTC (intranasal Flonase) and [[USLegal:Prescription only|Rx-only]] (inhaled, topical) in US (1) · OTC (low-dose topicals) and [[USLegal:Prescription only|Rx-only]] (other forms) in US (1) · OTC (lower strengths) and [[USLegal:Prescription only|Rx-only]] (combination with betamethasone) in US (1) · OTC (lower-concentration washes) and [[USLegal:Prescription only|Rx-only]] (Peridex oral rinse, ChloraPrep) in US (1) · OTC (lowest-strength topicals) and [[USLegal:Prescription only|Rx-only]] (higher strengths, injectable) in US (1) · OTC (most dentifrice and rinse) and [[USLegal:Prescription only|Rx-only]] (high-concentration paste/gel, supplements) in US (1) · OTC (Nasonex 24HR) and [[USLegal:Prescription only|Rx-only]] (other forms) in US (1) · OTC (ophthalmic ointment) and [[USLegal:Prescription only|Rx-only]] (other forms) in US (1) · OTC (Pataday ophthalmic) and [[USLegal:Prescription only|Rx-only]] (Patanase intranasal) in US (1) · OTC (topical) and [[USLegal:Prescription only|Rx-only]] (oral) in US (1) · OTC (transdermal patch in women) and [[USLegal:Prescription only|Rx-only]] (other forms) in US (1) · OTC in US (1) · Plant unrestricted; pharmaceutical atropine Rx-only (1) · Schedule II (1) · [[USLegal:Over-the-counter|OTC]] for most oral and topical formulations; [[USLegal:Prescription only|Rx-only]] for injectable (1) · [[USLegal:Prescription only|Rx-only]] for most formulations; some low-concentration topical formulations are [[USLegal:Over-the-counter|OTC]] (4% cream) (1) · [[USLegal:Prescription only|Rx-only]] for oral and most topical formulations in US; Voltaren Arthritis Pain 1% gel switched to [[USLegal:Over-the-counter|OTC]] in 2020 (1) · [[USLegal:Prescription only|Rx-only]] in US (17) · [[USLegal:Prescription only|Rx-only]] in US (the veterinary preparations are not for human use) (1) · [[USLegal:Prescription only|Rx-only]] in US since 2020 (OTC 2% formulations withdrawn under CARES Act due to safety concerns) (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries a '''Boxed Warning''' for Clostridioides difficile colitis (one of the most C. difficile-inducing antibiotic classes)'"`UNIQ--ref-00001444-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000022-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the same fluoroquinolone-class '''Boxed Warnings''' as ciprofloxacin/levofloxacin'"`UNIQ--ref-00000D84-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the same fluoroquinolone-class '''Boxed Warnings''' as ciprofloxacin: tendinitis/tendon rupture (especially elderly, corticosteroid co-use), peripheral neuropathy, CNS effects, worsening of myasthenia gravis'"`UNIQ--ref-00000CF7-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, like guanfacine and unlike the psychostimulant alternatives for ADHD'"`UNIQ--ref-00000028-QINU`"' (1)

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