Drilldown: Medicines
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generic:
brand:
classes:
Beta Blocker (1) ·
Cardioselective (β1) (1) ·
Dual orexin receptor antagonist (DORA) (2) ·
Multimodal antidepressant: SERT inhibitor + 5HT1A agonist + 5HT1B partial agonist + 5HT3/5HT7 antagonist (1) ·
Multimodal serotonergic; HSDD treatment (1) ·
PDE5 Inhibitor (1) ·
the first approved (1) ·
[[:Category:Alpha-1_blockers|Alpha-1 adrenergic blocker (non-selective)]] (1) ·
[[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (1) ·
[[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (1) ·
[[:Category:Antihypertensives|Antihypertensive]] (2) ·
[[:Category:Beta-3_agonists|β3 adrenergic agonist]] (1) ·
[[:Category:BPH_treatments|Benign prostatic hyperplasia treatment]] (1) ·
[[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (1) ·
[[:Category:Incretin_modulators|Incretin pathway modulator]] (1) ·
[[:Category:Overactive_bladder_medications|Overactive bladder medication]] (1)
mechanism:
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. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (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-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)
uses:
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 sleep maintenance) in adults (FDA-approved Jan 2022) (1) ·
Major depressive disorder in adults (FDA-approved 2013). Notable for evidence of cognitive benefit (processing speed) that distinguishes it from other antidepressants. (1) ·
'"`UNIQ--vote-000000B8-QINU`"', '"`UNIQ--vote-000000B9-QINU`"', '"`UNIQ--vote-000000BA-QINU`"', '"`UNIQ--vote-000000BB-QINU`"' (1) ·
'"`UNIQ--vote-000002C1-QINU`"' (1) ·
'"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1) ·
'"`UNIQ--vote-00000669-QINU`"' (1) ·
'"`UNIQ--vote-00000764-QINU`"' (1) ·
'"`UNIQ--vote-00000C4C-QINU`"', '"`UNIQ--vote-00000C4D-QINU`"' (1) ·
'"`UNIQ--vote-0000111D-QINU`"', '"`UNIQ--vote-0000111E-QINU`"' (1)
starting dose:
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; 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 daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) ·
25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) ·
25 mg PO once daily; titrate to 50 mg after 4-8 weeks if needed (1) ·
50 mg PO daily (25 mg in volume depletion or hepatic impairment) (1)
preparations:
1, 2, 5, 10 mg capsules and tablets (1) ·
100 mg tabs (1) ·
2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn) (1) ·
25 mg, 50 mg tablets (1) ·
25 mg, 50 mg, 100 mg tablets (1) ·
25, 50 mg ER tablets; 8 mg/mL granules for oral suspension (Myrbetriq Granules, pediatric) (1) ·
25, 50, 100 mg tablets; combination tablets with metformin (1) ·
5 mg, 10 mg, 15 mg, 20 mg tablets (1) ·
5 mg, 10 mg, 20 mg tablets (1) ·
5, 10 mg tabs (1)
fda max: (Click arrow to add another value)
routes:
onset:
1–2 h (1) ·
BP and symptomatic LUTS improvement within 1-2 weeks (1) ·
BP effect 1-2 weeks; antihypertensive peak 3-6 weeks (1) ·
Effects accumulate over weeks; assess at 8 weeks (1) ·
Postprandial glucose effect within days; HbA1c by 12 weeks (1) ·
Symptom improvement within weeks (1) ·
Typical antidepressant 4-6 week onset (1) ·
~30 min (3)
duration:
halflife:
2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-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) ·
~50 hours'"`UNIQ--ref-00000C4E-QINU`"' (1) ·
~66 hours (1) ·
~8 hours (shorter than suvorexant and lemborexant) (1)
bioavailability:
25 mg: ~29%; 50 mg: ~35%; food reduces absorption'"`UNIQ--ref-00000C4F-QINU`"' (1) ·
>90% (oral; not significantly affected by food)'"`UNIQ--ref-00001120-QINU`"' (1) ·
~15% (extensive hepatic first-pass) (1) ·
~33% (1) ·
~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"' (1) ·
~62% (1) ·
~75% (1) ·
~82% (1) ·
~87% (oral)'"`UNIQ--ref-00000766-QINU`"' (1) ·
~90% (low first-pass) (1)
pregnancy:
'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000000BE-QINU`"' (1) ·
Category B (1) ·
Category C (1) ·
Limited data.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (2) ·
Limited data; avoid (2) ·
Limited data; switch to insulin where feasible.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Limited data; weigh benefits/risks (1) ·
Not indicated; pregnancy effects unknown (1)
Showing below up to 10 results in range #1 to #10.