Drilldown: Medicines

None (3) · Methotrexate (1) · Vardenafil (1)

Belsomra (1) · Dayvigo (1) · Levitra, Staxyn (1) · Quviviq (1) · Trexall, Otrexup, Rasuvo, Xatmep, Rheumatrex (discontinued) (1)

Dual orexin receptor antagonist (DORA) (3) · PDE5 Inhibitor (1) · the first approved (1) · [[:Category:Antifolates|Antifolate]] (1) · [[:Category:Antineoplastics|Antineoplastic]] (1) · [[:Category:DMARDs|DMARD]] (1) · [[:Category:Immunosuppressants|Immunosuppressant]] (1)

None (2) · 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-00000669-QINU`"' (1) · '"`UNIQ--vote-000007C1-QINU`"', '"`UNIQ--vote-000007C2-QINU`"', '"`UNIQ--vote-000007C3-QINU`"', '"`UNIQ--vote-000007C4-QINU`"', '"`UNIQ--vote-000007C5-QINU`"', '"`UNIQ--vote-000007C6-QINU`"', '"`UNIQ--vote-000007C7-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) · Rheumatologic: 7.5-15 mg PO or SC '''once weekly''' (not daily — daily dosing is a recognized fatal error); folic acid 1 mg PO daily on non-MTX days; oncology dosing is far higher and indication-specific (1)

2.5 mg tablets; 10-50 mg/mL injection; pre-filled subcutaneous autoinjectors (Otrexup, Rasuvo); 2.5 mg/mL oral solution (Xatmep) (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)

10 mg/d (1) · 20 mg/d (2) · 50 mg/d (1) · Rheumatologic ~25 mg/week; oncology indication-specific (1)

intramuscular (1) · intrathecal (1) · IV (1) · Oral (5) · subcutaneous (1)

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) · Once-weekly dosing in rheumatology (1) · ~7-8 hours (3)

3-10 hours (low dose); 8-15 hours (high dose); much longer in third-space accumulation (pleural effusion, ascites)'"`UNIQ--ref-000007C8-QINU`"' (1) · 4–5 h (1) · ~12 hours (1) · ~17-19 hours (longer than daridorexant) (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

60-70% PO at low doses; saturable at high doses (parenteral routes preferred above 15-25 mg/week)'"`UNIQ--ref-000007C9-QINU`"' (1) · ~15% (extensive hepatic first-pass) (1) · ~44% (1) · ~62% (1) · ~82% (1)

'''Contraindicated in pregnancy''' (Category X); abortifacient and teratogenic. Discontinuation 3-6 months before conception is standard.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Category B (1) · Limited data; avoid (3)

Rx, Schedule IV (US) (3) · Rx-only in US (1) · [[USLegal:Prescription only|Rx-only]] in US (1)