Drilldown: Medicines

None (4) · Desvenlafaxine (succinate) (1) · Paroxetine (HCl; mesylate as Pexeva) (1) · Vardenafil (1)

Belsomra (1) · Dayvigo (1) · Levitra, Staxyn (1) · Nuplazid (1) · Paxil (IR), Paxil CR (controlled-release), Brisdelle (low-dose for menopausal vasomotor symptoms), Pexeva (paroxetine mesylate) (1) · Pristiq (1) · Quviviq (1)

Dual orexin receptor antagonist (DORA) (3) · PDE5 Inhibitor (1) · Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism) (1) · the first approved (1) · [[:Category:Antidepressants|Antidepressant]] (2) · [[:Category:Anxiolytics|Anxiolytic]] (1) · [[:Category:SNRIs|Serotonin-norepinephrine reuptake inhibitor (SNRI)]] (1) · [[:Category:SSRIs|Selective serotonin reuptake inhibitor (SSRI)]] (1)

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) · 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) · Selective inverse agonist at 5HT2A receptors with weaker activity at 5HT2C. Has no significant dopamine D2 affinity, unique among approved antipsychotics. Inverse agonism (rather than antagonism) reduces constitutive 5HT2A receptor activity below baseline. (1)

Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (1) · 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`"' (1) · '"`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) · '"`UNIQ--vote-00000669-QINU`"' (1)

10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 10 mg ~1 h before sexual activity (1) · 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) · 34 mg PO once daily (1) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · 50 mg PO once daily ('''no titration required''', distinguishing it favorably from venlafaxine) (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)

10 mg, 34 mg capsules/tablets (1) · 2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn) (1) · 25 mg, 50 mg tablets (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1) · ER tablets 25, 50, 100 mg (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)

10 mg/d (1) · 20 mg/d (2) · 34 mg/d (1) · 50 mg/d (1) · 50 mg/day (IR); 62.5 mg/day (CR); 60 mg/day (OCD) (1) · 50 mg/day (no efficacy benefit shown for higher doses despite the 100 mg strength being available) (1)

Oral (7)

None · Hours · 30-60 minutes · 1-2 hours · ~30 min · LDL lowering at 2 weeks, max by 4 weeks · ~1 hour · 15-30 minutes · 15–30 min · 1–2 h · 30–60 min · Antidepressant effect emerges over 1-2 weeks · BP and symptomatic LUTS improvement within 1-2 weeks · BP effect within 1-2 weeks · Clinical improvement within 24-72 hours · Days · Motor improvement over days at therapeutic dose · Over weeks · Postprandial glucose effect within days; HbA1c by 12 weeks · Sleep effect from first dose; antidepressant effect over 1-4 weeks

Other values:

Search

24 hours (1) · 24 hours (once-daily dosing) (1) · 4–5 h (1) · Daily dosing (1) · ~7-8 hours (3)

4–5 h (1) · ~11 hours'"`UNIQ--ref-0000001A-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) · ~57 hours (parent), ~200 h (active metabolite) (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

Highly variable due to saturable first-pass metabolism'"`UNIQ--ref-0000002C-QINU`"' (1) · Not characterized; oral dosing once daily (1) · ~15% (extensive hepatic first-pass) (1) · ~44% (1) · ~62% (1) · ~80% (oral)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~82% (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) · Category B (1) · Limited data; avoid (4) · Observational signal for neonatal adaptation syndrome with late-pregnancy exposure (SNRI class effect).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

Rx, Schedule IV (US) (3) · Rx-only in US (1) · Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-0000001C-QINU`"' (1) · [[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)