Drilldown: Medicines
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generic:
brand:
classes:
Anxiolytic (1) ·
Benzodiazepine (1) ·
Dual orexin receptor antagonist (DORA) (1) ·
Triazolobenzodiazepine (1) ·
[[:Category:Alpha-2_agonists|Alpha-2 adrenergic agonist]] (1) ·
[[:Category:Antianginals|Antianginal]] (1) ·
[[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (1) ·
[[:Category:Antihypertensives|Antihypertensive]] (1) ·
[[:Category:Calcium_channel_blockers|Calcium channel blocker]] (1) ·
[[:Category:Carbonic_anhydrase_inhibitors|Carbonic anhydrase inhibitor (topical)]] (1) ·
[[:Category:Cholesterol_absorption_inhibitors|Cholesterol absorption inhibitor]] (1) ·
[[:Category:Glaucoma_medications|Glaucoma medication]] (2) ·
[[:Category:Heart_failure_medications|Heart failure medication]] (1) ·
[[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (1) ·
[[:Category:Ocular_hypotensive_agents|Ocular hypotensive agent]] (2) ·
[[:Category:SGLT2_inhibitors|SGLT2 inhibitor]] (1)
mechanism:
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) ·
GABA-A positive allosteric modulator'"`UNIQ--ref-00000067-QINU`"' '"`UNIQ--vote-00000068-QINU`"' (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)
uses:
Insomnia (sleep onset and/or maintenance) in adults (FDA-approved Dec 2019) (1) ·
'"`UNIQ--vote-00000069-QINU`"', '"`UNIQ--vote-0000006A-QINU`"', '"`UNIQ--vote-0000006B-QINU`"' (1) ·
'"`UNIQ--vote-00000075-QINU`"', '"`UNIQ--vote-00000076-QINU`"', '"`UNIQ--vote-00000077-QINU`"' (1) ·
'"`UNIQ--vote-0000044C-QINU`"', '"`UNIQ--vote-0000044D-QINU`"', '"`UNIQ--vote-0000044E-QINU`"', '"`UNIQ--vote-0000044F-QINU`"' (1) ·
'"`UNIQ--vote-0000054E-QINU`"', '"`UNIQ--vote-0000054F-QINU`"', '"`UNIQ--vote-00000550-QINU`"', '"`UNIQ--vote-00000551-QINU`"' (1) ·
'"`UNIQ--vote-00000B08-QINU`"', '"`UNIQ--vote-00000B09-QINU`"' (1) ·
'"`UNIQ--vote-000010CE-QINU`"', '"`UNIQ--vote-000010CF-QINU`"', '"`UNIQ--vote-000010D0-QINU`"' (1)
starting dose:
0.25 mg (1) ·
1 drop in affected eye(s) TID (monotherapy); BID with timolol (Cosopt) (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) ·
2.5-5 mg PO once daily; titrate to 10 mg/d (1) ·
5 mg PO at bedtime; may increase to 10 mg if inadequate (1) ·
Ophthalmic 1 drop in affected eye(s) TID; topical Mirvaso 0.33% gel applied to face daily (1)
preparations:
0.1%, 0.15%, 0.2% ophthalmic solutions; 0.33% topical gel; combinations with timolol (Combigan) and brinzolamide (Simbrinza) (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) ·
10 mg tablet; also as fixed-dose combinations with simvastatin (Vytorin) and atorvastatin (Liptruzet, withdrawn US 2015 but generics exist) (1) ·
2% ophthalmic solution (Trusopt); 2%/0.5% fixed combination with timolol (Cosopt, Cosopt PF) (1) ·
2.5, 5, 10 mg tablets; 1 mg/mL oral suspension (1) ·
5 mg, 10 mg tablets (2)
fda max: (Click arrow to add another value)
routes:
onset:
30-60 min (immediate-release); 1-2 h (extended-release) (1) ·
BP effect within 24 hours; full effect at 1-2 weeks (long half-life) (1) ·
Glycosuria within hours; HbA1c effect at 12 weeks; CV/renal benefits over months (1) ·
IOP lowering at 1 hour; max at 2-3 hours (1) ·
IOP lowering at 2 hours; max at 4 hours (1) ·
LDL lowering within 2 weeks (1) ·
~30 min (1)
duration:
halflife:
11-13 h (immediate-release); 11-16 h (extended-release) (1) ·
30-50 hours'"`UNIQ--ref-00000078-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) ·
~3 hours'"`UNIQ--ref-000010D1-QINU`"' (1) ·
~4 months in erythrocytes (carbonic anhydrase binding in red cells; not relevant to topical IOP duration)'"`UNIQ--ref-00000B0A-QINU`"' (1)
bioavailability:
64-90% (oral; not affected by food)'"`UNIQ--ref-00000079-QINU`"' (1) ·
80-90% oral (1) ·
Topical with measurable systemic absorption (small CA inhibition observed clinically with chronic use)'"`UNIQ--ref-00000B0B-QINU`"' (1) ·
Topical; clinically meaningful systemic absorption can produce systemic α2 effects (somnolence, hypotension), especially in children'"`UNIQ--ref-000010D2-QINU`"' (1) ·
Variable (oral; rapidly conjugated to active glucuronide; food does not affect)'"`UNIQ--ref-00000451-QINU`"' (1) ·
~44% (1) ·
~78% (oral; high-fat meal modestly reduces but is not clinically significant)'"`UNIQ--ref-00000553-QINU`"' (1)
pregnancy:
Avoid in second and third trimesters; fetal SGLT2 inhibition disrupts kidney development.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Category D'"`UNIQ--ref-0000006C-QINU`"' (1) ·
Limited data.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Limited data; avoid (1) ·
Limited data; case series and registries suggest no major teratogenicity but other antihypertensives (labetalol, nifedipine) are typically preferred.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Limited data; generally avoided particularly in combination with statin.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Limited data; weigh against alternatives.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1)
Showing below up to 7 results in range #1 to #7.