Drilldown: Medicines

Azelastine (1) · Bimatoprost (1) · Brimonidine (1) · Bromazolam (1) · Ciprofloxacin (1) · Cyanocobalamin (vitamin B12) (1) · Dorzolamide (1) · Ketotifen (1) · Latanoprost (1) · Levofloxacin (1) · Melatonin (N-acetyl-5-methoxytryptamine) (1) · Moxifloxacin (1) · Nitroglycerin (glyceryl trinitrate, GTN) (1) · Olopatadine (1) · Tiotropium (1) · Zolpidem (tartrate) (1)

(none, never marketed) (1) · Alphagan P (ophthalmic glaucoma), Mirvaso (topical rosacea) (1) · Ambien (IR), Ambien CR (biphasic-release), Edluar (sublingual), Intermezzo (low-dose sublingual for middle-of-night awakening), Zolpimist (oral spray) (1) · Astelin, Astepro (intranasal); Optivar (ophthalmic); with fluticasone as Dymista (1) · Avelox (oral/IV brand discontinued US); Vigamox, Moxeza (ophthalmic) (1) · Cipro, Cipro XR, Ciloxan (ophthalmic) (1) · Levaquin (US brand discontinued); generic and ophthalmic Quixin/Iquix (1) · Lumigan (glaucoma), Latisse (eyelash growth) (1) · Many OTC and Rx; Nascobal (intranasal); generic injection (1) · Multiple OTC dietary supplement formulations (1) · Nitrostat, Nitrolingual, NitroMist, Nitro-Bid, Nitro-Dur, Minitran, Rectiv (1) · Patanol, Pataday (ophthalmic, now OTC), Patanase (intranasal) (1) · Spiriva, Spiriva Respimat (1) · Trusopt; with timolol as Cosopt (1) · Xalatan, Xelpros (1) · Zaditor, Alaway (ophthalmic, OTC); Zaditen (systemic, outside US) (1)

Designer benzodiazepine (1) · Research material (1) · Sedative-Hypnotic (1) · Triazolobenzodiazepine (1) · [[:Category:Alpha-2_agonists|Alpha-2 adrenergic agonist]] (1) · [[:Category:Antianginals|Antianginal]] (1) · [[:Category:Antibacterials|Antibacterial]] (3) · [[:Category:Antimuscarinics|Antimuscarinic]] (1) · [[:Category:B-vitamins|B-vitamin]] (1) · [[:Category:Bronchodilators|Bronchodilator]] (1) · [[:Category:Carbonic_anhydrase_inhibitors|Carbonic anhydrase inhibitor (topical)]] (1) · [[:Category:Chronobiotics|Chronobiotic (circadian phase regulator)]] (1) · [[:Category:Fluoroquinolones|Fluoroquinolone antibiotic]] (3) · [[:Category:Glaucoma_medications|Glaucoma medication]] (4) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist]] (3) · [[:Category:Hematinics|Hematinic]] (1) · [[:Category:Intranasal_antihistamines|Intranasal antihistamine]] (1) · [[:Category:Long-acting_muscarinic_antagonists|Long-acting muscarinic antagonist (LAMA)]] (1) · [[:Category:Mast_cell_stabilizers|Mast cell stabilizer]] (3) · [[:Category:Melatonin receptor agonists|Melatonin receptor agonist]] (1) · [[:Category:Nitrates|Organic nitrate]] (1) · [[:Category:Non-benzodiazepine hypnotics|Non-benzodiazepine hypnotic]] (1) · [[:Category:Ocular_hypotensive_agents|Ocular hypotensive agent]] (4) · [[:Category:Ophthalmic_antihistamines|Ophthalmic antihistamine]] (2) · [[:Category:Prostaglandin_analogs|Prostaglandin F2α analog]] (2) · [[:Category:Schedule IV controlled substances|Schedule IV controlled substance]] (1) · [[:Category:Sleep aids|Sleep aid]] (2) · [[:Category:Vasodilators|Vasodilator]] (1) · [[:Category:Vitamins|Vitamin]] (1)

None (11) · 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) · '"`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)

No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"' (1) · '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"' (1) · '"`UNIQ--vote-00000415-QINU`"', '"`UNIQ--vote-00000416-QINU`"' (1) · '"`UNIQ--vote-00000607-QINU`"', '"`UNIQ--vote-00000608-QINU`"', '"`UNIQ--vote-00000609-QINU`"', '"`UNIQ--vote-0000060A-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-000009BE-QINU`"', '"`UNIQ--vote-000009BF-QINU`"' (1) · '"`UNIQ--vote-00000B08-QINU`"', '"`UNIQ--vote-00000B09-QINU`"' (1) · '"`UNIQ--vote-00000C0A-QINU`"', '"`UNIQ--vote-00000C0B-QINU`"', '"`UNIQ--vote-00000C0C-QINU`"', '"`UNIQ--vote-00000C0D-QINU`"', '"`UNIQ--vote-00000C0E-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-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)

'''5 mg PO at bedtime for women, 5-10 mg for men''' (per FDA's 2013 sex-specific dose reduction for women due to slower clearance). Ambien CR 6.25 mg women / 6.25-12.5 mg men. Intermezzo SL 1.75 mg women / 3.5 mg men (1) · 0.5-3 mg PO 30-60 minutes before bedtime. Some patients respond to micro-doses (0.3 mg) without additional benefit at higher doses. For circadian phase shifting, timing relative to dim-light melatonin onset matters more than absolute dose (1) · 1 drop in affected eye(s) TID (monotherapy); BID with timolol (Cosopt) (1) · 1 drop in the affected eye(s) once daily in the evening (1) · 1 drop in the affected eye(s) once daily in the evening (Lumigan); Latisse applied to upper lash line at bedtime (1) · 18 mcg DPI once daily (HandiHaler); 2.5 mcg per actuation × 2 inhalations once daily (Respimat) (1) · 400 mg PO/IV once daily (1) · 500-750 mg PO BID; 400 mg IV q8-12h (1) · 500-750 mg PO/IV once daily (1) · Intranasal 0.1% or 0.15%: 1-2 sprays/nostril BID; ophthalmic 0.05%: 1 drop in each eye BID (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) · Ophthalmic 1 drop in each eye every 8-12 hours (1) · Ophthalmic Pataday 0.7%: 1 drop in each eye once daily (24-hour formulation); Patanol 0.1% BID; intranasal Patanase 2 sprays/nostril BID (1) · Replacement: 1000 mcg IM daily for 1 week, then weekly for 4 weeks, then monthly; or 1000-2000 mcg PO daily (effective even in pernicious anemia via passive diffusion); intranasal 500 mcg weekly (1) · SL 0.3-0.6 mg every 5 minutes up to 3 doses for acute angina (call EMS if not resolved after the third); IV infusion 5-10 mcg/min titrated; transdermal patch 0.2-0.4 mg/hr for 12-14 hours daily (nitrate-free interval prevents tolerance) (1)

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) · 100, 250, 500, 1000, 5000 mcg tablets (OTC and Rx); 1000 mcg/mL injection; intranasal spray; sublingual (1) · 18 mcg HandiHaler capsules; 2.5 mcg/actuation Respimat solution inhaler (1.25 mcg/actuation for asthma indication) (1) · 2% ophthalmic solution (Trusopt); 2%/0.5% fixed combination with timolol (Cosopt, Cosopt PF) (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) · IR tablets 5, 10 mg; CR tablets 6.25, 12.5 mg; SL tablets 1.75, 3.5, 5, 10 mg; oral spray (1) · OTC tablets, sublingual tablets, gummies, liquid, extended-release tablets and capsules; common strengths 0.5, 1, 3, 5, 10 mg (1) · SL 0.3, 0.4, 0.6 mg tablets; lingual spray 0.4 mg/spray; ER 2.5-9 mg capsules; transdermal patch 0.1-0.8 mg/hr; 2% ointment; 0.4% rectal ointment; 5 mg/mL IV (1)

1 drop per eye q8-12h (1) · 1 drop/eye/day (more frequent dosing reduces efficacy) (1) · 10 mg/day (IR); 12.5 mg/day (CR) (1) · 2 sprays/nostril BID (1) · 400 mg/d (1) · 750 mg/d (1) · Indication-specific; titrated to effect (1) · N/A (never approved) (1) · No strict ceiling; water-soluble vitamin, low toxicity (1) · Not formally established (dietary supplement); doses above ~3-5 mg show no additional efficacy but increase next-day sedation risk (1) · Once daily (Pataday 0.7%); BID (other ophthalmic) (1) · One dose per day (1) · One drop per eye per day (1) · TID per eye (2) · ~1500 mg/d (oral); 1200 mg/d (IV) (1)

None · Oral · IV · topical · IM · intranasal · rectal · subcutaneous · topical ophthalmic · ophthalmic · intramuscular · intravenous · transdermal · vaginal · Subcutaneous (abdomen · sublingual · thigh · inhaled · SC · intra-articular

Other values:

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15 minutes (1) · 15-30 minutes (1) · 30-60 minutes (immediate-release oral) (1) · Bronchodilation 30 minutes; steady-state at 1-2 weeks (1) · Hours (3) · 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) · Reticulocyte response at 3-5 days; neurologic recovery weeks to months (and may be incomplete if longstanding) (1) · SL/spray: 1-3 minutes; IV: minutes; patch: 30-60 minutes (1) · Symptom relief within 30-60 minutes (1) · Within minutes (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

12 hours (1) · 24 hours (4) · 24 hours (0.7% formulation); 8-12 hours (lower-strength) (1) · 24 hours (long receptor dissociation half-life from M3) (1) · 3-4 hours (1) · 6-8 hours (IR); 8 hours (CR via biphasic release) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · 8-12 hours (3) · 8-12 hours (TID dosing needed) (1) · N/A (replacement) (1) · SL: 30 minutes; patch: 12-14 hours; IV continuous (1)

1-3 minutes (very short)'"`UNIQ--ref-00000C0F-QINU`"' (1) · 30-50 minutes (short)'"`UNIQ--ref-00000021-QINU`"' (1) · 4 hours'"`UNIQ--ref-00000938-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Not meaningfully described for ophthalmic use'"`UNIQ--ref-00001287-QINU`"' (1) · ~12 hours'"`UNIQ--ref-00000D82-QINU`"' (1) · ~17 minutes (free acid, the active form, in aqueous humor)'"`UNIQ--ref-00000417-QINU`"' (1) · ~2.5 hours'"`UNIQ--ref-0000001A-QINU`"' (1) · ~22 hours; longer 54 hours (desmethylazelastine, active metabolite)'"`UNIQ--ref-000013B6-QINU`"' (1) · ~25-44 hours plasma; receptor kinetics drive the once-daily duration'"`UNIQ--ref-000009C0-QINU`"' (1) · ~3 hours (systemic, when measurable; topical action dominates)'"`UNIQ--ref-000011D9-QINU`"' (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) · ~45 minutes (free acid in aqueous humor)'"`UNIQ--ref-00000DA1-QINU`"' (1) · ~6 days (plasma); hepatic stores last 3-5 years (1) · ~6-8 hours'"`UNIQ--ref-00000CF5-QINU`"' (1)

Highly route-dependent: SL bypasses first-pass; oral has extensive first-pass (used only for chronic ER preparations); transdermal predictable'"`UNIQ--ref-00000C10-QINU`"' (1) · Inhaled lung deposition ~20%; systemic absorption from lung ~33%; oral component negligible'"`UNIQ--ref-000009C1-QINU`"' (1) · Intranasal ~40% systemic; ophthalmic minimal'"`UNIQ--ref-000013B7-QINU`"' (1) · Not formally characterized in humans. (1) · Oral ~1-3% via passive diffusion at high doses (independent of intrinsic factor); IM/SC ~100% (1) · Topical with measurable systemic absorption (small CA inhibition observed clinically with chronic use)'"`UNIQ--ref-00000B0B-QINU`"' (1) · Topical with minimal systemic absorption'"`UNIQ--ref-000011DA-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) · Topical; minimal systemic absorption'"`UNIQ--ref-00000418-QINU`"' (1) · Topical; minimal systemic absorption'"`UNIQ--ref-00000DA2-QINU`"' (1) · ~15% (oral; highly variable due to extensive and variable first-pass metabolism)'"`UNIQ--ref-00000022-QINU`"' (1) · ~70% (oral)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~70% (oral; reduced by divalent cations — antacids, iron, calcium, dairy)'"`UNIQ--ref-00000939-QINU`"' (1) · ~90% (oral; not affected by food but reduced by divalent cations)'"`UNIQ--ref-00000D83-QINU`"' (1) · ~99% (oral; matched 1:1 IV-to-PO conversion)'"`UNIQ--ref-00000CF6-QINU`"' (1)

'''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; LABA/LAMA strategies in pregnancy generally favor agents with the most reassuring 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) · Limited human data; case reports of neonatal sedation with late-pregnancy exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; endogenous hormone, but supplemental pharmacological doses are not well characterized in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Routinely supplemented in vegan pregnancies and pernicious anemia.<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)

None (2) · OTC (Astepro 0.15%) and [[USLegal:Prescription only|Rx-only]] (other intranasal, ophthalmic, Dymista) in US (1) · OTC (low/mid-dose oral) and [[USLegal:Prescription only|Rx-only]] (injection, intranasal) in US (1) · OTC (Pataday ophthalmic) and [[USLegal:Prescription only|Rx-only]] (Patanase intranasal) in US (1) · OTC in US (1) · [[USLegal:Over-the-counter|OTC]] dietary supplement in the US ('''not FDA-regulated as a medicine'''; multiple studies show OTC products contain 50-470% of labeled melatonin content); [[USLegal:Prescription only|Rx-only]] in the EU and UK (1) · [[USLegal:Prescription only|Rx-only]] in US (6) · [[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 IV|Schedule IV controlled substance]] in US. Carries the FDA '''Boxed Warning''' for '''complex sleep behaviors''' (sleep-driving, sleep-walking, sleep-eating, other parasomnias) added in 2019'"`UNIQ--ref-0000001C-QINU`"' (1)