Drilldown: Medicines
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generic:
brand:
classes:
Dual orexin receptor antagonist (DORA) (3) ·
the first approved (1) ·
[[:Category:Acetylcholinesterase inhibitors|Acetylcholinesterase inhibitor]] (1) ·
[[:Category:Anti-dementia medicines|Anti-dementia medicine]] (1) ·
[[:Category:Antidepressants|Antidepressant]] (3) ·
[[:Category:Anxiolytics|Anxiolytic]] (2) ·
[[:Category:SSRIs|Selective serotonin reuptake inhibitor (SSRI)]] (3)
mechanism:
None (3) ·
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) ·
'"`UNIQ--vote-0000001D-QINU`"' CYP2C19 + CYP3A4 metabolism, with CPIC PGx guidance: poor CYP2C19 metabolizers have ~3-fold higher exposure and benefit from a lower starting dose; ultrarapid metabolizers may have inadequate response'"`UNIQ--ref-0000001E-QINU`"'. (2)
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-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"' (1) ·
'"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"' (2) ·
'"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"', '"`UNIQ--vote-00000026-QINU`"', '"`UNIQ--vote-00000027-QINU`"', '"`UNIQ--vote-00000028-QINU`"', '"`UNIQ--vote-00000029-QINU`"', '"`UNIQ--vote-0000002A-QINU`"' (1)
starting dose:
10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) ·
10 mg PO once daily; titrate to 20 mg/day after 1-2 weeks if needed (1) ·
20 mg PO once daily; titrate to 40 mg/day after 1 week if tolerated. Elderly (>60) and hepatic impairment: 20 mg/day ceiling (1) ·
25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) ·
5 mg PO at bedtime; may increase to 10 mg if inadequate (1) ·
5 mg PO once daily at bedtime; titrate to 10 mg/day after 4-6 weeks. Severe Alzheimer disease: may escalate to 23 mg/day. Adlarity patch: 5 or 10 mg/day applied weekly (1) ·
MDD/GAD: 20 mg PO once daily. Panic disorder: 10 mg titrating to 40 mg. OCD: 20 mg titrating to 40-60 mg. CR: 25 mg/day. Brisdelle: 7.5 mg at bedtime for hot flashes (1)
preparations:
25 mg, 50 mg tablets (1) ·
5 mg, 10 mg tablets (1) ·
5 mg, 10 mg, 15 mg, 20 mg tablets (1) ·
IR tablets 10, 20, 30, 40 mg; CR tablets 12.5, 25, 37.5 mg; oral suspension 10 mg/5 mL; Brisdelle capsules 7.5 mg (1) ·
Oral tablets 5, 10, 23 mg; ODT 5, 10 mg; Adlarity transdermal patch 5, 10 mg/day (weekly application) (1) ·
Tablets 10, 20, 40 mg; oral solution 10 mg/5 mL (1) ·
Tablets 5, 10, 20 mg; oral solution 1 mg/mL (1)
fda max:
routes: (Click arrow to add another value)
onset:
Antidepressant effect emerges over 1-2 weeks (1) ·
Antidepressant effect emerges over 1-2 weeks; full clinical effect 4-6 weeks (1) ·
Antidepressant effect over 1-2 weeks; full clinical effect 4-6 weeks (1) ·
Cognitive effect emerges gradually over weeks to months; ceiling effect at the therapeutic dose (1) ·
~30 min (3)
duration: (Click arrow to add another value)
halflife:
27-32 hours'"`UNIQ--ref-00000026-QINU`"' (1) ·
~12 hours (1) ·
~17-19 hours (longer than daridorexant) (1) ·
~21 hours (with nonlinear pharmacokinetics from CYP2D6 autoinhibition)'"`UNIQ--ref-0000002B-QINU`"' (1) ·
~35 hours'"`UNIQ--ref-00000026-QINU`"' (1) ·
~70 hours (long, supports once-daily dosing without peak-trough variation)'"`UNIQ--ref-0000001B-QINU`"' (1) ·
~8 hours (shorter than suvorexant and lemborexant) (1)
bioavailability:
pregnancy:
None (1) ·
'''Among the least preferred SSRIs in pregnancy.''' Observational signal for cardiac malformations (atrial and ventricular septal defects) with first-trimester exposure, and the most severe neonatal adaptation syndrome of any SSRI with third-trimester exposure'"`UNIQ--ref-0000002D-QINU`"' (1) ·
Limited data; avoid (3) ·
Limited human data; rarely indicated in pregnancy given the patient population.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Observational signal for persistent pulmonary hypertension of the newborn (small absolute risk) and neonatal adaptation syndrome with third-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1)
legal:
Rx, Schedule IV (US) (3) ·
[[USLegal:Prescription only|Rx-only]] in US (1) ·
[[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000028-QINU`"' (2) ·
[[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-0000002E-QINU`"' (1)
Showing below up to 7 results in range #1 to #7.