Drilldown: Medicines

None (1) · Ketotifen (1) · Methimazole (thiamazole) (1) · Solifenacin (1)

Tapazole; outside US Mercazole (1) · Vesicare (1) · Vraylar (1) · Zaditor, Alaway (ophthalmic, OTC); Zaditen (systemic, outside US) (1)

Atypical antipsychotic (1) · D2/D3/5HT1A partial agonist (1) · [[:Category:Antimuscarinics|Antimuscarinic (M3-selective)]] (1) · [[:Category:Antithyroid_agents|Antithyroid agent]] (1) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist]] (1) · [[:Category:Mast_cell_stabilizers|Mast cell stabilizer]] (1) · [[:Category:Ophthalmic_antihistamines|Ophthalmic antihistamine]] (1) · [[:Category:Overactive_bladder_medications|Overactive bladder medication]] (1) · [[:Category:Thionamides|Thionamide]] (1)

None (1) · '"`UNIQ--vote-00000DFA-QINU`"' CYP3A4 substrate; QT-interval prolongation has been reported at higher doses. Like other antimuscarinics, contributes to cumulative anticholinergic burden in older adults'"`UNIQ--ref-00000DFB-QINU`"'. (1) · '"`UNIQ--vote-00000ECD-QINU`"' Agranulocytosis is the most-feared adverse effect (~0.3%, usually first 90 days of treatment; warn patients to seek urgent CBC for fever or severe sore throat). Hepatotoxicity is class-recognized but more often associated with PTU'"`UNIQ--ref-00000ECE-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)

Schizophrenia (FDA-approved 2015). Acute manic or mixed episodes of bipolar I disorder. Bipolar I depression (FDA-approved 2019). Adjunctive treatment of major depressive disorder (FDA-approved Dec 2022). (1) · '"`UNIQ--vote-00000DFC-QINU`"', '"`UNIQ--vote-00000DFD-QINU`"' (1) · '"`UNIQ--vote-00000ECF-QINU`"', '"`UNIQ--vote-00000ED0-QINU`"', '"`UNIQ--vote-00000ED1-QINU`"', '"`UNIQ--vote-00000ED2-QINU`"' (1) · '"`UNIQ--vote-00001286-QINU`"' (1)

10-40 mg PO daily depending on hyperthyroidism severity; titrate by clinical and biochemical response (target TSH/free T4) (1) · 5 mg PO once daily; titrate to 10 mg after 2 weeks if needed (1) · Ophthalmic 1 drop in each eye every 8-12 hours (1) · Schizophrenia: 1.5 mg PO daily, increase to 1.5-6 mg as tolerated. Bipolar mania: 1.5 mg, may increase to 3-6 mg. Bipolar depression: 1.5 mg daily for 14 days, then 3 mg. MDD adjunct: 1.5 mg, may increase to 3 mg. (1)

None · 10 mg, 20 mg, 40 mg, 80 mg tablets · 2.5, 5, 10, 20 mg tabs · 5 mg, 10 mg tablets · 5, 10 mg tablets · 5, 10, 20, 40 mg tablets · 0.005% ophthalmic solution (50 mcg/mL); typical 2.5 mL bottle · 0.01%, 0.03% ophthalmic solution · 0.025%, 0.035% ophthalmic solutions · 0.1% (Patanol), 0.2% (Pataday once-daily original), 0.7% (Pataday 24-hour) ophthalmic solutions; 0.6% nasal spray · 0.1%, 0.15% intranasal spray; 0.05% ophthalmic solution; combination Dymista (azelastine 0.137 mg + fluticasone 50 mcg/spray) · 0.1%, 0.15%, 0.2% ophthalmic solutions; 0.33% topical gel; combinations with timolol (Combigan) and brinzolamide (Simbrinza) · 0.225%, 0.45%, 0.9%, 3%, 5% IV solutions; 0.9% nasal spray; 3% and 7% nebulizer solutions; oral tablets (1 g) · 0.25 mg, 0.5 mg, 1 mg, 2 mg tablets (immediate-release and orally disintegrating); 0.5 mg, 1 mg, 2 mg, 3 mg extended-release tablets; 1 mg/mL oral concentrate · 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets · 0.25, 0.5 mcg oral capsules; 1 mcg/mL oral solution; 1 mcg/mL IV; 3 mcg/g topical ointment · 0.35 mg POP tablets; 5 mg tablets (Aygestin); component of COCs and combination HRT · 0.4 mg capsules · 0.4, 0.8, 1 mg OTC; 1 mg Rx; 5 mg/mL injection · 0.5 g, 1 g capsules

Other values:

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1 drop per eye q8-12h (1) · 10 mg/d (5 mg if severe renal or moderate hepatic impairment, or strong CYP3A4 inhibitors) (1) · 6 mg/d (psychosis/mania); 3 mg/d (depression adjunct) (1) · 60 mg/d typical (1)

Oral (3) · Topical ophthalmic (1)

Biochemical improvement within 2-4 weeks; full euthyroid state 6-12 weeks (1) · Symptom improvement within 1-2 weeks (1) · Weeks for psychosis/mood efficacy (1) · Within minutes (1)

24 hours (2) · 8-12 hours (1) · Daily dosing; active metabolites with very long half-lives (up to 1-3 weeks) (1)

Cariprazine ~2-4 d; major active metabolites desmethyl-cariprazine (DCAR) ~1-3 weeks → 'oral depot' effect with delayed steady-state and reduced effect of missed doses (1) · Not meaningfully described for ophthalmic use'"`UNIQ--ref-00001287-QINU`"' (1) · ~4-6 hours (plasma); intrathyroidal accumulation gives a much longer functional duration'"`UNIQ--ref-00000ED3-QINU`"' (1) · ~45-68 hours'"`UNIQ--ref-00000DFE-QINU`"' (1)

Adequate oral bioavailability (1) · Topical with minimal systemic absorption'"`UNIQ--ref-00001288-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00000DFF-QINU`"' (1) · ~93% (oral)'"`UNIQ--ref-00000ED4-QINU`"' (1)

None (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 (1) · Limited data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

OTC in US (1) · Rx (1) · [[USLegal:Prescription only|Rx-only]] in US (2)