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Drilldown: Medicines

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Medicines > fda max : 10 mg/d or 20 mg/d or 400 mg/d

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mechanism:
None (3) · Cardioselective β1-adrenergic antagonist. Selectivity is dose-dependent and partially lost at higher doses. (1) · Competitive antagonist at OX1R and OX2R. Faster receptor association/dissociation kinetics than suvorexant (~16 sec dissociation vs ~57 sec) hypothesized to support sleep onset, with sufficient duration for maintenance. (1) · Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1) · GABA-A positive allosteric modulator'"`UNIQ--ref-00000067-QINU`"' '"`UNIQ--vote-00000068-QINU`"' (1) · Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (1) · Selective inhibitor of PDE5. Slightly higher PDE5/PDE6 selectivity vs sildenafil (less visual side effect) but more PDE1 cross-activity (occasional QT effects at high doses). (1) · '"`UNIQ--vote-00000073-QINU`"' The long half-life gives smooth, once-daily BP control with low rebound. CYP3A4 substrate; pedal edema is the characteristic, dose-related, non-fluid-overload side effect'"`UNIQ--ref-00000074-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-0000111B-QINU`"' Intraoperative floppy iris syndrome is a recognized class effect. Recently emerging evidence (observational) suggests possible Parkinson's disease risk reduction via PGK1 binding — investigational and not a clinical indication'"`UNIQ--ref-0000111C-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)
uses:
Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1) · Insomnia (sleep onset and/or maintenance) in adults (FDA-approved Dec 2019) (1) · Major depressive disorder in adults (FDA-approved 2013). Notable for evidence of cognitive benefit (processing speed) that distinguishes it from other antidepressants. (1) · '"`UNIQ--vote-00000069-QINU`"', '"`UNIQ--vote-0000006A-QINU`"', '"`UNIQ--vote-0000006B-QINU`"' (1) · '"`UNIQ--vote-00000075-QINU`"', '"`UNIQ--vote-00000076-QINU`"', '"`UNIQ--vote-00000077-QINU`"' (1) · '"`UNIQ--vote-0000044C-QINU`"', '"`UNIQ--vote-0000044D-QINU`"', '"`UNIQ--vote-0000044E-QINU`"', '"`UNIQ--vote-0000044F-QINU`"' (1) · '"`UNIQ--vote-000004F5-QINU`"', '"`UNIQ--vote-000004F6-QINU`"', '"`UNIQ--vote-000004F7-QINU`"', '"`UNIQ--vote-000004F8-QINU`"', '"`UNIQ--vote-000004F9-QINU`"' (1) · '"`UNIQ--vote-0000054E-QINU`"', '"`UNIQ--vote-0000054F-QINU`"', '"`UNIQ--vote-00000550-QINU`"', '"`UNIQ--vote-00000551-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1) · '"`UNIQ--vote-00000669-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-0000111D-QINU`"', '"`UNIQ--vote-0000111E-QINU`"' (1) · '"`UNIQ--vote-0000113C-QINU`"', '"`UNIQ--vote-0000113D-QINU`"', '"`UNIQ--vote-0000113E-QINU`"' (1)
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