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Medicines > duration : 12 hours or 24 hours (HS dosing) or 8-12 hours

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classes:
[[:Category:Antidepressants|Antidepressant]] (4) · [[:Category:Antibacterials|Antibacterial]] (2) · [[:Category:Fluoroquinolones|Fluoroquinolone antibiotic]] (2) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist]] (2) · [[:Category:Mast_cell_stabilizers|Mast cell stabilizer]] (2) · [[:Category:Migraine prophylactics|Migraine prophylactic]] (2) · [[:Category:Neuropathic pain medicines|Neuropathic pain medicine]] (2) · [[:Category:Tricyclic antidepressants|Tricyclic antidepressant (TCA)]] (2)
mechanism:
None (12) · '"`UNIQ--vote-00000019-QINU`"' Therapeutic plasma-level monitoring is standard practice for TCAs given the narrow therapeutic index and the established plasma-level-efficacy correlation. CYP2D6 substrate; CPIC PGx guidance applies for dose individualization'"`UNIQ--ref-0000001A-QINU`"'. (1) · '"`UNIQ--vote-000001F6-QINU`"' CYP3A4 (primary) and P-glycoprotein substrate; strong dual inhibitors or inducers materially shift exposure. Reversal: andexanet alfa for life-threatening bleeding; 4F-PCC commonly used off-label when andexanet unavailable'"`UNIQ--ref-000001F7-QINU`"'. (1) · '"`UNIQ--vote-0000113A-QINU`"' Concomitant β-blocker or CCB is required when used for AF to prevent 1:1 atrial flutter conduction (flecainide can slow atrial rate to a level where AV conduction allows dangerous ventricular rates). CYP2D6 substrate'"`UNIQ--ref-0000113B-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) · '"`UNIQ--vote-000014BC-QINU`"' Topical ophthalmic and otic formulations remain widely used in ENT and ophthalmology. Subject to all fluoroquinolone-class restrictions (tendinitis/rupture, peripheral neuropathy, QT prolongation)'"`UNIQ--ref-000014BD-QINU`"'. (1) · '"`UNIQ--vote-00001580-QINU`"' First FDA-approved treatment for PBA. The 10 mg quinidine daily dose is far below antiarrhythmic levels but sufficient to nearly fully inhibit CYP2D6, the basis of the combination's pharmacokinetic rationale'"`UNIQ--ref-00001581-QINU`"'. (1)
uses:
'"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (2) · '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"' (1) · '"`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`"' (1) · '"`UNIQ--vote-000001F8-QINU`"', '"`UNIQ--vote-000001F9-QINU`"', '"`UNIQ--vote-000001FA-QINU`"' (1) · '"`UNIQ--vote-00000475-QINU`"', '"`UNIQ--vote-00000476-QINU`"', '"`UNIQ--vote-00000477-QINU`"', '"`UNIQ--vote-00000478-QINU`"', '"`UNIQ--vote-00000479-QINU`"', '"`UNIQ--vote-0000047A-QINU`"', '"`UNIQ--vote-0000047B-QINU`"', '"`UNIQ--vote-0000047C-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-00000BE3-QINU`"', '"`UNIQ--vote-00000BE4-QINU`"', '"`UNIQ--vote-00000BE5-QINU`"', '"`UNIQ--vote-00000BE6-QINU`"', '"`UNIQ--vote-00000BE7-QINU`"', '"`UNIQ--vote-00000BE8-QINU`"', '"`UNIQ--vote-00000BE9-QINU`"', '"`UNIQ--vote-00000BEA-QINU`"' (1) · '"`UNIQ--vote-00000C8F-QINU`"', '"`UNIQ--vote-00000C90-QINU`"', '"`UNIQ--vote-00000C91-QINU`"' (1) · '"`UNIQ--vote-00000E91-QINU`"', '"`UNIQ--vote-00000E92-QINU`"', '"`UNIQ--vote-00000E93-QINU`"' (1) · '"`UNIQ--vote-00000FCF-QINU`"', '"`UNIQ--vote-00000FD0-QINU`"', '"`UNIQ--vote-00000FD1-QINU`"' (1) · '"`UNIQ--vote-00000FF3-QINU`"', '"`UNIQ--vote-00000FF4-QINU`"', '"`UNIQ--vote-00000FF5-QINU`"', '"`UNIQ--vote-00000FF6-QINU`"', '"`UNIQ--vote-00000FF7-QINU`"', '"`UNIQ--vote-00000FF8-QINU`"' (1) · '"`UNIQ--vote-000010CE-QINU`"', '"`UNIQ--vote-000010CF-QINU`"', '"`UNIQ--vote-000010D0-QINU`"' (1) · '"`UNIQ--vote-0000113C-QINU`"', '"`UNIQ--vote-0000113D-QINU`"', '"`UNIQ--vote-0000113E-QINU`"' (1) · '"`UNIQ--vote-00001286-QINU`"' (1) · '"`UNIQ--vote-000013B3-QINU`"', '"`UNIQ--vote-000013B4-QINU`"', '"`UNIQ--vote-000013B5-QINU`"' (1) · '"`UNIQ--vote-000013CF-QINU`"', '"`UNIQ--vote-000013D0-QINU`"' (1) · '"`UNIQ--vote-000014BE-QINU`"', '"`UNIQ--vote-000014BF-QINU`"', '"`UNIQ--vote-000014C0-QINU`"', '"`UNIQ--vote-000014C1-QINU`"', '"`UNIQ--vote-000014C2-QINU`"' (1) · '"`UNIQ--vote-00001582-QINU`"' (1)
starting dose:
1 capsule (20/10 mg dextromethorphan/quinidine) PO once daily × 7 days, then 1 capsule BID (1) · 100 mg PO BID; rickettsial 200 mg/d; doxy-PEP 200 mg within 72 hours after condomless sex (1) · 15 mg PO at bedtime, titrate to 30-45 mg/day after 1-2 weeks. '''Counterintuitive dose paradox''': lower doses (7.5-15 mg) are more sedating than higher doses because H1 antihistamine effect dominates at low dose (1) · 2 g PO BID with meals (4 g/d total) (1) · 250-500 mg PO BID × 7-14 days; IV 1.5 g q8h for serious infections (1) · 4 mg PO initially, then 2 mg after each loose stool, '''not to exceed 16 mg/d''' (8 mg OTC); chronic-use lower (1) · 50 mg PO BID; titrate to 100-200 mg BID; pill-in-pocket 200-300 mg PO single dose for AF conversion (1) · 500 mg PO TID × 7-10 days (most indications); 2 g single dose for trichomoniasis; 500 mg IV q8h for severe anaerobic infection; rectal 1 g BID (1) · 500-750 mg PO BID; 400 mg IV q8-12h (1) · ACS/PCI: 180 mg PO loading dose, then 90 mg PO BID for 12 months; long-term post-MI: 60 mg BID (1) · Depression (rarely used now): 25-75 mg PO at bedtime, titrate to 150 mg/day. Neuropathic pain / migraine prophylaxis: 10-25 mg at bedtime, titrate by 10-25 mg weekly to 50-100 mg/day. Elderly: 10 mg at bedtime (Beers-list cautions apply) (1) · Depression: 25 mg PO TID-QID or 75 mg at bedtime, titrate to 75-150 mg/day. Neuropathic pain: 10-25 mg at bedtime, titrate to 50-100 mg/day. Elderly: 10 mg at bedtime (Beers-list cautions, though less than amitriptyline) (1) · Depression: 25-75 mg/day to start, titrate to 75-150 mg/day at bedtime. Insomnia (Silenor): 3 mg PO 30 minutes before bedtime, max 6 mg. Topical (Prudoxin): apply to affected area every 3-4 hours (1) · Intranasal 0.1% or 0.15%: 1-2 sprays/nostril BID; ophthalmic 0.05%: 1 drop in each eye BID (1) · NVAF: 5 mg PO BID (2.5 mg BID if 2 of 3: age ≥80, weight ≤60 kg, serum creatinine ≥1.5 mg/dL); acute VTE: 10 mg BID for 7 days, then 5 mg BID (1) · Ophthalmic 1 drop in affected eye(s) TID; topical Mirvaso 0.33% gel applied to face daily (1) · Ophthalmic 1 drop in each eye every 8-12 hours (1) · Oral 200-400 mg BID; ophthalmic 1-2 drops in affected eye(s) q2-4h initially, then taper; otic 5-10 drops in affected ear BID (1) · Treatment: 75 mg PO BID × 5 days (adult); pediatric weight-based; prophylaxis: 75 mg PO once daily × 7-10 days (1)
preparations:
0.025%, 0.035% ophthalmic solutions (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 g, 1 g capsules (1) · 125, 250, 500 mg tablets; 125 mg/5 mL, 250 mg/5 mL suspension; 750 mg, 1.5 g IV vials (1) · 2 mg capsules and tablets; 1 mg/5 mL oral solution; combined with simethicone (Imodium Multi-Symptom) (1) · 2.5 mg, 5 mg tablets (1) · 20 mg dextromethorphan HBr / 10 mg quinidine sulfate capsules (1) · 200, 300, 400 mg tablets (mostly generic now); 0.3% ophthalmic solution; 0.3% otic solution (1) · 250, 500 mg tablets; 750 mg ER; 500 mg/100 mL IV; 0.75-1% topical gel/cream; 0.75% vaginal gel; suppository (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) · 30, 45, 75 mg capsules; 6 mg/mL oral suspension (1) · 50 mg, 75 mg, 100 mg, 150 mg tablets and capsules; delayed-release; suspension; IV (1) · 50, 100, 150 mg tablets (1) · 60, 90 mg tablets (1) · Capsules 10, 25, 50, 75 mg; oral solution 10 mg/5 mL (1) · Capsules 10, 25, 50, 75, 100, 150 mg; oral concentrate 10 mg/mL; Silenor tablets 3, 6 mg; topical cream 5% (Prudoxin, Zonalon) (1) · Tablets 10, 25, 50, 75, 100, 150 mg (1) · Tablets 7.5, 15, 30, 45 mg; orally disintegrating tablets (SolTab) 15, 30, 45 mg (1)
duration: (Click arrow to add another value)
halflife:
bioavailability:
Increased substantially via CYP2D6 inhibition'"`UNIQ--ref-00001584-QINU`"' (1) · Intranasal ~40% systemic; ophthalmic minimal'"`UNIQ--ref-000013B7-QINU`"' (1) · Substantially improved with high-fat meal; take with food'"`UNIQ--ref-000013D2-QINU`"' (1) · Topical with minimal systemic absorption'"`UNIQ--ref-00001288-QINU`"' (1) · Topical; clinically meaningful systemic absorption can produce systemic α2 effects (somnolence, hypotension), especially in children'"`UNIQ--ref-000010D2-QINU`"' (1) · ~0.3% (oral; extensive first-pass via CYP3A4 and P-glycoprotein-mediated efflux at the intestinal and blood-brain barriers limit systemic and CNS exposure at therapeutic doses)'"`UNIQ--ref-00000FD3-QINU`"' (1) · ~30% (oral)'"`UNIQ--ref-00000021-QINU`"' (1) · ~36% (oral)'"`UNIQ--ref-00000C93-QINU`"' (1) · ~37% (oral, as axetil prodrug; food modestly improves absorption)'"`UNIQ--ref-00000FFA-QINU`"' (1) · ~50% (oral)'"`UNIQ--ref-00000021-QINU`"' (1) · ~50% (oral)'"`UNIQ--ref-00000027-QINU`"' (1) · ~50% (oral; not significantly affected by food)'"`UNIQ--ref-000001FC-QINU`"' (1) · ~50% (oral; substantial first-pass)'"`UNIQ--ref-00000024-QINU`"' (1) · ~70% (oral; reduced by divalent cations — antacids, iron, calcium, dairy)'"`UNIQ--ref-00000939-QINU`"' (1) · ~75% (oral, as the active carboxylate after hepatic esterase activation)'"`UNIQ--ref-00000E95-QINU`"' (1) · ~80% (oral)'"`UNIQ--ref-00000BEC-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00001140-QINU`"' (1) · ~95% (oral)'"`UNIQ--ref-000014C4-QINU`"' (1) · ~95% (oral; reduced by dairy, antacids, iron via divalent-cation chelation, though less than for tetracycline itself)'"`UNIQ--ref-0000047E-QINU`"' (1)
pregnancy:
None (2) · '''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) · Generally considered acceptable when needed.<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) · 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.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally used when influenza treatment is indicated; pregnancy is a recognized risk factor for severe influenza.<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; quinidine has been used in pregnancy as antiarrhythmic.<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.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; some observational signals reassuring relative to other antidepressants.<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; observational signals not clearly causal.<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) · TCA class signal; limited human data specific to nortriptyline.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Use in fetal SVT (transplacental antiarrhythmic therapy) is established; otherwise weigh against alternatives.<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 in US (2) · [[USLegal:Prescription only|Rx-only]] in US (7) · [[USLegal:Prescription only|Rx-only]] in US. '''Contraindicated in structural heart disease''' — CAST trial (1989) showed increased mortality from class IC agents in patients with prior MI; modern use is limited to structurally normal hearts'"`UNIQ--ref-00001141-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries a '''Boxed Warning''' for bleeding risk and against aspirin maintenance doses above 100 mg/d (reduces ticagrelor efficacy, per PLATO subgroup analysis)'"`UNIQ--ref-00000C94-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`"' (2) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000025-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000028-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the same fluoroquinolone-class '''Boxed Warnings''' as ciprofloxacin/levofloxacin'"`UNIQ--ref-000014C5-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Caution with QT-prolonging medicines (quinidine itself is class IA antiarrhythmic, and the dose here, though sub-antiarrhythmic, still contributes to QT)'"`UNIQ--ref-00001585-QINU`"' (1)

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