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Drilldown: Medicines

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Medicines > fda max: 20 mg/d & onset : HbA1c effect at 12-16 weeks (slower than other classes) or ~30 min

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generic:
None (1) · Vardenafil (1)
brand:
Belsomra (1) · Levitra, Staxyn (1)
classes:
Dual orexin receptor antagonist (DORA) (1) · PDE5 Inhibitor (1) · the first approved (1)
mechanism:
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)
uses:
Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1) · '"`UNIQ--vote-00000669-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)
preparations:
2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn) (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1)
fda max: (Click arrow to add another value)
routes:
Oral (2)
onset: (Click arrow to add another value)
duration:
4–5 h (1) · ~7-8 hours (1)
halflife:
4–5 h (1) · ~12 hours (1)
bioavailability:
~15% (extensive hepatic first-pass) (1) · ~82% (1)
pregnancy:
Category B (1) · Limited data; avoid (1)
legal:
Rx, Schedule IV (US) (1) · Rx-only in US (1)
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