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Medicines > routes : rectal or topical or topical ophthalmic

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brand:
classes:
[[:Category:Antibacterials|Antibacterial]] (6) · [[:Category:Corticosteroids|Corticosteroid]] (6) · [[:Category:Analgesics|Analgesic]] (4) · [[: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:Antiemetics|Antiemetic]] (2) · [[:Category:Antifungals|Antifungal]] (2) · [[:Category:Antipyretics|Antipyretic]] (2) · [[:Category:Inhaled_corticosteroids|Inhaled corticosteroid (ICS)]] (2) · [[:Category:NSAIDs|Non-steroidal anti-inflammatory (NSAID)]] (2) · [[:Category:Ophthalmic_antihistamines|Ophthalmic antihistamine]] (2) · [[:Category:Prostaglandin_analogs|Prostaglandin F2α analog]] (2) · [[:Category:Topical_antifungals|Topical antifungal]] (2)
mechanism:
None (36) · 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-00001067-QINU`"' Chronic use is associated with cathartic colon (colonic dilation, loss of haustration), hypokalemia, and laxative dependence; reserved for short-term use or bowel prep with breaks between courses'"`UNIQ--ref-00001068-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`"' (3) · '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"' (2)
starting dose:
preparations:
fda max:
Indication-specific (4) · TID per eye (2)
routes: (Click arrow to add another value)
onset:
None (1) · 1-3 days (1) · 15 minutes (1) · 15-30 minutes (oral); 1-2 minutes (IV) (1) · 15-60 minutes (oral); 1-5 minutes (IV); 4-10 minutes (rectal or intranasal) (1) · 20 minutes (oral); 5 minutes (IV) (1) · 30-60 minutes (oral); rapid relief in acute gout (1) · 30-60 minutes (oral); slower for topical (1) · 5-10 minutes (IV); 30 minutes (oral IR); slower for ER and rectal (1) · <1 minute (IV); 1-2 minutes (infiltration); 30+ minutes (patch on adult skin, faster on thinner pediatric skin) (1) · Antiplatelet effect within 30-60 minutes; analgesic effect 30-60 minutes (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) · 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) · PO 6-12 hours; PR 15-60 minutes (1) · PO: 30-60 minutes; IV: 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) · Symptomatic improvement 2-4 weeks (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) · Visible lightening at 4-12 weeks (1) · Within minutes (1)
halflife:
bioavailability:
pregnancy:
None (3) · 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.<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> (2) · 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)
legal:
None (2) · 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 and [[USLegal:Prescription only|Rx-only]] (IV, combination products) in US (1) · OTC in US (3) · Plant unrestricted; pharmaceutical atropine Rx-only (1) · [[USLegal:Over-the-counter|OTC]] for most oral and topical formulations; [[USLegal:Prescription only|Rx-only]] for injectable (1) · [[USLegal:Over-the-counter|OTC]] in US at all standard strengths (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:Schedule II|Schedule II controlled substance]] in US; WHO essential medicine'"`UNIQ--ref-00000022-QINU`"' (1) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the benzodiazepine class '''Boxed Warning''' for risk of fatal respiratory depression, coma, and death when combined with opioids'"`UNIQ--ref-00000028-QINU`"' (1)

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