Drilldown: Medicines
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brand:
classes:
mechanism:
None (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) ·
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-0000083E-QINU`"' CYP2C9 substrate; no clinically active metabolites. The IDNT trial established renoprotection in diabetic nephropathy independent of BP lowering, contributing to the ARB class indication in T2DM with proteinuria'"`UNIQ--ref-0000083F-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)
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) ·
Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022) (1) ·
'"`UNIQ--vote-00000669-QINU`"' (1) ·
'"`UNIQ--vote-00000840-QINU`"', '"`UNIQ--vote-00000841-QINU`"' (1) ·
'"`UNIQ--vote-00000AEC-QINU`"', '"`UNIQ--vote-00000AED-QINU`"' (1)
starting dose:
10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) ·
10 mg ~1 h before sexual activity (1) ·
150 mg PO once daily; titrate to 300 mg if needed (1) ·
25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) ·
40 mg PO once daily; titrate to 80 mg (1) ·
5 mg PO at bedtime; may increase to 10 mg if inadequate (1)
preparations:
fda max:
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duration:
halflife:
bioavailability:
pregnancy:
'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000844-QINU`"' (1) ·
'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000AF0-QINU`"' (1) ·
Category B (1) ·
Limited data; avoid (3)
Showing below up to 6 results in range #1 to #6.