Drilldown: Medicines

None (3) · Lorazepam (1) · Pramipexole (1) · Ropinirole (1) · Vardenafil (1)

Ativan (oral, injectable), Loreev XR (1) · Belsomra (1) · Dayvigo (1) · Levitra, Staxyn (1) · Mirapex (IR), Mirapex ER (1) · Quviviq (1) · Requip (IR), Requip XL (extended-release) (1)

Dual orexin receptor antagonist (DORA) (3) · PDE5 Inhibitor (1) · the first approved (1) · [[:Category:Antiparkinsonians|Antiparkinsonian]] (2) · [[:Category:Anxiolytics|Anxiolytic]] (1) · [[:Category:Benzodiazepines|Benzodiazepine]] (1) · [[:Category:Dopamine agonists|Dopamine D2/D3 receptor agonist (non-ergot)]] (2) · [[:Category:Schedule IV controlled substances|Schedule IV controlled substance]] (1)

None (4) · 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)

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-00000013-QINU`"', '"`UNIQ--vote-00000014-QINU`"' (1) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-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`"' (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) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · Anxiety: 0.5-1 mg PO BID-TID. Insomnia: 1-2 mg PO at bedtime. Status epilepticus: 4 mg IV (adult), repeat after 5-10 minutes if needed. Acute agitation: 1-2 mg IM (1) · Parkinson disease: 0.125 mg PO TID, titrate weekly to maintenance ~1.5 mg TID. Restless legs syndrome: 0.125 mg PO 2-3 hours before bedtime, titrate to 0.5 mg/day if needed (1) · Parkinson disease: 0.25 mg PO TID, titrate weekly. Restless legs syndrome: 0.25 mg PO 1-3 hours before bedtime, titrate to 4 mg/day if needed (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) · IR tablets 0.125, 0.25, 0.5, 0.75, 1, 1.5 mg; ER tablets 0.375, 0.75, 1.5, 2.25, 3, 3.75, 4.5 mg (1) · IR tablets 0.25, 0.5, 1, 2, 3, 4, 5 mg; XL tablets 2, 4, 6, 8, 12 mg (1) · Tablets 0.5, 1, 2 mg; oral concentrate 2 mg/mL; injection 2 mg/mL and 4 mg/mL; Loreev XR capsules 1, 2, 3 mg (1)

10 mg/d (1) · 10 mg/day (anxiety, oral) (1) · 20 mg/d (2) · 24 mg/day (Parkinson disease); 4 mg/day (restless legs syndrome) (1) · 4.5 mg/day (Parkinson disease); 0.5 mg/day (restless legs syndrome) (1) · 50 mg/d (1)

intramuscular (1) · intravenous (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:

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4–5 h (1) · 6-8 hours (1) · TID dosing (IR); once-daily (ER) (1) · TID dosing (IR); once-daily (XL) (1) · ~7-8 hours (3)

12-15 hours (intermediate); '''no active metabolites''' (key clinical feature)'"`UNIQ--ref-00000029-QINU`"' (1) · 4–5 h (1) · 8-12 hours (longer in elderly and renal impairment)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~12 hours (1) · ~17-19 hours (longer than daridorexant) (1) · ~6 hours'"`UNIQ--ref-00000015-QINU`"' (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

>90% (oral)'"`UNIQ--ref-0000001C-QINU`"' (1) · ~15% (extensive hepatic first-pass) (1) · ~44% (1) · ~55% (oral)'"`UNIQ--ref-00000016-QINU`"' (1) · ~62% (1) · ~82% (1) · ~90% (oral)'"`UNIQ--ref-0000002A-QINU`"' (1)

Category B (1) · Limited data; avoid (3) · Limited human data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; rarely indicated in pregnancy given the typical patient population.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Some signal for cleft lip/palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.<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) · [[USLegal:Prescription only|Rx-only]] in US (2) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the benzodiazepine class '''Boxed Warning''' for risk of fatal respiratory depression, coma, and death when combined with opioids'"`UNIQ--ref-0000002B-QINU`"' (1)