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Drilldown: Medicines

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Medicines > fda max : 20 mg/d or 40 mg/d or 80 mg/d

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mechanism:
None (6) · Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1) · Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (1) · Selective alpha-1 adrenergic receptor antagonist. Lowers peripheral vascular resistance via vasodilation; in the CNS, blunts noradrenergic hyperarousal thought to drive trauma-related nightmares. (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) · The d-enantiomer is a highly β1-selective antagonist; the l-enantiomer triggers endothelial nitric-oxide–mediated vasodilation. Unique among beta blockers for this NO mechanism. (1) · TrkB/BDNF'"`UNIQ--ref-00000040-QINU`"' '"`UNIQ--vote-00000041-QINU`"' (1) · '"`UNIQ--vote-00000053-QINU`"' Also raises bradykinin, contributing to vasodilation and the characteristic dry cough. Renally cleared, unmetabolized; dose-adjust by eGFR'"`UNIQ--ref-00000054-QINU`"'. (1) · '"`UNIQ--vote-000003D1-QINU`"' SLCO1B1 polymorphism affects exposure but is most clinically actionable for simvastatin'"`UNIQ--ref-000003D2-QINU`"'. (1) · '"`UNIQ--vote-00000A1D-QINU`"' Like other ACE inhibitors, it raises bradykinin (driving the dry cough and rare angioedema). Renally cleared; dose-adjust in renal impairment'"`UNIQ--ref-00000A1E-QINU`"'. (1) · '"`UNIQ--vote-00000AEA-QINU`"' The 24-hour half-life supports once-daily dosing with consistent overnight BP control. Largely hepatically cleared (~98% biliary); no significant renal clearance dependence'"`UNIQ--ref-00000AEB-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)
uses:
Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1) · Major depressive disorder in adults (FDA-approved 2011) (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-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"' (1) · '"`UNIQ--vote-00000042-QINU`"', '"`UNIQ--vote-00000043-QINU`"', '"`UNIQ--vote-00000044-QINU`"' (1) · '"`UNIQ--vote-00000055-QINU`"', '"`UNIQ--vote-00000056-QINU`"', '"`UNIQ--vote-00000057-QINU`"', '"`UNIQ--vote-00000058-QINU`"' (1) · '"`UNIQ--vote-000003D3-QINU`"', '"`UNIQ--vote-000003D4-QINU`"' (1) · '"`UNIQ--vote-0000056B-QINU`"' (1) · '"`UNIQ--vote-0000059D-QINU`"' (1) · '"`UNIQ--vote-000005D0-QINU`"', '"`UNIQ--vote-000005D1-QINU`"', '"`UNIQ--vote-000005D2-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1) · '"`UNIQ--vote-00000669-QINU`"' (1) · '"`UNIQ--vote-00000A1F-QINU`"', '"`UNIQ--vote-00000A20-QINU`"', '"`UNIQ--vote-00000A21-QINU`"' (1) · '"`UNIQ--vote-00000AEC-QINU`"', '"`UNIQ--vote-00000AED-QINU`"' (1) · '"`UNIQ--vote-00000B81-QINU`"', '"`UNIQ--vote-00000B82-QINU`"', '"`UNIQ--vote-00000B83-QINU`"' (1) · '"`UNIQ--vote-00000EF4-QINU`"', '"`UNIQ--vote-00000EF5-QINU`"', '"`UNIQ--vote-00000EF6-QINU`"', '"`UNIQ--vote-00000EF7-QINU`"', '"`UNIQ--vote-00000EF8-QINU`"' (1) · '"`UNIQ--vote-0000111D-QINU`"', '"`UNIQ--vote-0000111E-QINU`"' (1)
fda max: (Click arrow to add another value)
pregnancy:
'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-0000056E-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000AF0-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension. Stop on detection'"`UNIQ--ref-0000005B-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension. Stop on detection'"`UNIQ--ref-00000A24-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension. Stop on detection'"`UNIQ--ref-00000B86-QINU`"' (1) · Category B (1) · Category C (3) · Category C'"`UNIQ--ref-00000045-QINU`"' (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; avoid (1) · Limited data; weigh benefits/risks (2) · Previously Category X; FDA removed the blanket statin contraindication in pregnancy in 2021. Use individualized; lactation generally avoided.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Previously Category X; FDA removed the blanket statin contraindication in pregnancy in 2021.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Widely used for hyperemesis gravidarum; reassuring data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

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