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: 10 mg/d

or 100 mg/d

or 20 mg/d

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None (3) · Alprazolam (1) · Amlodipine (1) · Bisoprolol (1) · Dapagliflozin (1) · Ezetimibe (1) · Flibanserin (1) · Losartan (1) · Sitagliptin (1) · Terazosin (1) · Vardenafil (1)

Addyi (1) · Belsomra (1) · Cozaar (1) · Dayvigo (1) · Farxiga (US), Forxiga (international) (1) · Hytrin (US brand discontinued); mostly generic (1) · Januvia; with metformin Janumet/Janumet XR (1) · Levitra, Staxyn (1) · Norvasc, Katerzia (1) · Trintellix (US), Brintellix (formerly) (1) · Xanax (1) · Zebeta (1) · Zetia (1)

None (3) · 5-HT1A agonist, 5-HT2A antagonist, with weaker activity at D4 and other receptors. Net effect involves enhanced prefrontal dopaminergic/noradrenergic tone with decreased serotonergic inhibition of sexual desire. (1) · 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) · GABA-A positive allosteric modulator'"`UNIQ--ref-00000067-QINU`"' '"`UNIQ--vote-00000068-QINU`"' (1) · Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (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) · '"`UNIQ--vote-00000073-QINU`"' The long half-life gives smooth, once-daily BP control with low rebound. CYP3A4 substrate; pedal edema is the characteristic, dose-related, non-fluid-overload side effect'"`UNIQ--ref-00000074-QINU`"'. (1) · '"`UNIQ--vote-000000B6-QINU`"' Active metabolite EXP3174 is ~10-40-fold more potent than the parent and accounts for most of the antihypertensive effect; CYP2C9 polymorphism affects conversion'"`UNIQ--ref-000000B7-QINU`"'. (1) · '"`UNIQ--vote-00000762-QINU`"' Largely renally cleared, hence the eGFR-tiered dosing. Rare but well-documented signals: acute pancreatitis (uncertain causal contribution), severe joint pain, and bullous pemphigoid (class effect, especially in older Asian patients)'"`UNIQ--ref-00000763-QINU`"'. (1) · '"`UNIQ--vote-0000111B-QINU`"' Intraoperative floppy iris syndrome is a recognized class effect. Recently emerging evidence (observational) suggests possible Parkinson's disease risk reduction via PGK1 binding — investigational and not a clinical indication'"`UNIQ--ref-0000111C-QINU`"'. (1)

0.25 mg (1) · 1 mg PO at bedtime to limit first-dose syncope; titrate weekly to 5-10 mg (1) · 10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 10 mg PO once daily in the morning; 5 mg starting in heart failure (1) · 10 mg PO once daily, with or without food (1) · 10 mg PO once daily; may increase to 20 mg as tolerated, or decrease to 5 mg if needed (1) · 10 mg ~1 h before sexual activity (1) · 100 mg at bedtime daily (1) · 100 mg PO once daily (50 mg if CrCl 30-44; 25 mg if <30 or dialysis) (1) · 2.5-5 mg PO once daily; titrate to 10 mg/d (1) · 2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · 50 mg PO daily (25 mg in volume depletion or hepatic impairment) (1)

0.25 mg, 0.5 mg, 1 mg, 2 mg tablets (immediate-release and orally disintegrating); 0.5 mg, 1 mg, 2 mg, 3 mg extended-release tablets; 1 mg/mL oral concentrate (1) · 1, 2, 5, 10 mg capsules and tablets (1) · 10 mg tablet; also as fixed-dose combinations with simvastatin (Vytorin) and atorvastatin (Liptruzet, withdrawn US 2015 but generics exist) (1) · 100 mg tabs (1) · 2.5, 5, 10 mg tablets; 1 mg/mL oral suspension (1) · 2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn) (1) · 25 mg, 50 mg, 100 mg tablets (1) · 25, 50, 100 mg tablets; combination tablets with metformin (1) · 5 mg, 10 mg tablets (2) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1) · 5 mg, 10 mg, 20 mg tablets (1) · 5, 10 mg tabs (1)

Oral (13)

1–2 h (1) · 30-60 min (immediate-release); 1-2 h (extended-release) (1) · BP and symptomatic LUTS improvement within 1-2 weeks (1) · BP effect 1-2 weeks; antihypertensive peak 3-6 weeks (1) · BP effect within 24 hours; full effect at 1-2 weeks (long half-life) (1) · Effects accumulate over weeks; assess at 8 weeks (1) · Glycosuria within hours; HbA1c effect at 12 weeks; CV/renal benefits over months (1) · LDL lowering within 2 weeks (1) · Postprandial glucose effect within days; HbA1c by 12 weeks (1) · Typical antidepressant 4-6 week onset (1) · ~30 min (3)

24 h (1) · 24 hours (6) · 4–5 h (1) · 6 h (immediate-release); ~11 h (extended-release) (1) · Continuous daily dosing (1) · Daily dosing (1) · ~7-8 hours (2)

11-13 h (immediate-release); 11-16 h (extended-release) (1) · 2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-QINU`"' (1) · 30-50 hours'"`UNIQ--ref-00000078-QINU`"' (1) · 4–5 h (1) · 9–12 h (1) · ~11 h (1) · ~12 hours (1) · ~12 hours'"`UNIQ--ref-0000111F-QINU`"' (1) · ~12.4 hours'"`UNIQ--ref-00000765-QINU`"' (1) · ~12.9 hours'"`UNIQ--ref-00000552-QINU`"' (1) · ~17-19 hours (longer than daridorexant) (1) · ~22 hours (parent + active glucuronide)'"`UNIQ--ref-00000450-QINU`"' (1) · ~66 hours (1)

64-90% (oral; not affected by food)'"`UNIQ--ref-00000079-QINU`"' (1) · 80-90% oral (1) · >90% (oral; not significantly affected by food)'"`UNIQ--ref-00001120-QINU`"' (1) · Variable (oral; rapidly conjugated to active glucuronide; food does not affect)'"`UNIQ--ref-00000451-QINU`"' (1) · ~15% (extensive hepatic first-pass) (1) · ~33% (1) · ~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"' (1) · ~44% (1) · ~75% (1) · ~78% (oral; high-fat meal modestly reduces but is not clinically significant)'"`UNIQ--ref-00000553-QINU`"' (1) · ~82% (1) · ~87% (oral)'"`UNIQ--ref-00000766-QINU`"' (1) · ~90% (low first-pass) (1)

'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000000BE-QINU`"' (1) · Avoid in second and third trimesters; fetal SGLT2 inhibition disrupts kidney development.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Category B (1) · Category C (1) · Category D'"`UNIQ--ref-0000006C-QINU`"' (1) · Limited data.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Limited data; avoid (2) · Limited data; case series and registries suggest no major teratogenicity but other antihypertensives (labetalol, nifedipine) are typically preferred.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Limited data; generally avoided particularly in combination with statin.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Limited data; switch to insulin where feasible.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Limited data; weigh benefits/risks (1) · Not indicated; pregnancy effects unknown (1)

Rx (1) · Rx, Schedule IV (US) (2) · Rx-only in US (2) · Rx-only in US (REMS program) (1) · Schedule IV (US) (1) · [[USLegal:Prescription only|Rx-only]] in US (6)