Drilldown: Medicines
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generic:
brand:
classes:
Anxiolytic (1) ·
Benzodiazepine (1) ·
Beta Blocker (1) ·
Cardioselective (β1) (1) ·
Dual orexin receptor antagonist (DORA) (1) ·
Triazolobenzodiazepine (1) ·
[[:Category:Anti-influenza_agents|Anti-influenza agent]] (1) ·
[[:Category:Antianginals|Antianginal]] (1) ·
[[:Category:Antiarrhythmics|Antiarrhythmic (Vaughan-Williams class IC)]] (1) ·
[[:Category:Antibacterials|Antibacterial]] (1) ·
[[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (1) ·
[[:Category:Antihypertensives|Antihypertensive]] (1) ·
[[:Category:Antivirals|Antiviral]] (1) ·
[[:Category:Calcium_channel_blockers|Calcium channel blocker]] (1) ·
[[:Category:Cholesterol_absorption_inhibitors|Cholesterol absorption inhibitor]] (1) ·
[[:Category:Fluoroquinolones|Fluoroquinolone antibiotic]] (1) ·
[[:Category:Heart_failure_medications|Heart failure medication]] (1) ·
[[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (1) ·
[[:Category:Neuraminidase_inhibitors|Neuraminidase inhibitor]] (1) ·
[[:Category:SGLT2_inhibitors|SGLT2 inhibitor]] (1)
mechanism:
None (3) ·
Cardioselective β1-adrenergic antagonist. Selectivity is dose-dependent and partially lost at higher doses. (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) ·
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) ·
'"`UNIQ--vote-00000D7A-QINU`"' Substantial QT-interval prolongation — the most QT-prolonging fluoroquinolone — limits use in patients on other QT-prolonging agents or with electrolyte abnormalities'"`UNIQ--ref-00000D7B-QINU`"'. (1) ·
'"`UNIQ--vote-0000113A-QINU`"' Concomitant β-blocker or CCB is required when used for AF to prevent 1:1 atrial flutter conduction (flecainide can slow atrial rate to a level where AV conduction allows dangerous ventricular rates). CYP2D6 substrate'"`UNIQ--ref-0000113B-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-000004F5-QINU`"', '"`UNIQ--vote-000004F6-QINU`"', '"`UNIQ--vote-000004F7-QINU`"', '"`UNIQ--vote-000004F8-QINU`"', '"`UNIQ--vote-000004F9-QINU`"' (1) ·
'"`UNIQ--vote-0000054E-QINU`"', '"`UNIQ--vote-0000054F-QINU`"', '"`UNIQ--vote-00000550-QINU`"', '"`UNIQ--vote-00000551-QINU`"' (1) ·
'"`UNIQ--vote-00000D7C-QINU`"', '"`UNIQ--vote-00000D7D-QINU`"', '"`UNIQ--vote-00000D7E-QINU`"', '"`UNIQ--vote-00000D7F-QINU`"', '"`UNIQ--vote-00000D80-QINU`"', '"`UNIQ--vote-00000D81-QINU`"' (1) ·
'"`UNIQ--vote-00000E91-QINU`"', '"`UNIQ--vote-00000E92-QINU`"', '"`UNIQ--vote-00000E93-QINU`"' (1) ·
'"`UNIQ--vote-0000113C-QINU`"', '"`UNIQ--vote-0000113D-QINU`"', '"`UNIQ--vote-0000113E-QINU`"' (1)
starting dose:
0.25 mg (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) ·
25–50 mg BID (tartrate); 25–100 mg daily (succinate); 12.5 mg daily in HFrEF (1) ·
400 mg PO/IV once daily (1) ·
5 mg PO at bedtime; may increase to 10 mg if inadequate (1) ·
50 mg PO BID; titrate to 100-200 mg BID; pill-in-pocket 200-300 mg PO single dose for AF conversion (1) ·
Treatment: 75 mg PO BID × 5 days (adult); pediatric weight-based; prophylaxis: 75 mg PO once daily × 7-10 days (1)
preparations:
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) ·
2.5, 5, 10 mg tablets; 1 mg/mL oral suspension (1) ·
30, 45, 75 mg capsules; 6 mg/mL oral suspension (1) ·
400 mg tablets; 400 mg/250 mL IV; 0.5% ophthalmic solution (1) ·
5 mg, 10 mg tablets (2) ·
50, 100, 150 mg tablets (1) ·
Tartrate: 25, 50, 100 mg tabs; 1 mg/mL IV. Succinate ER: 25, 50, 100, 200 mg. (1)
fda max: (Click arrow to add another value)
routes:
onset:
1–2 h (PO); immediate (IV) (1) ·
30-60 min (immediate-release); 1-2 h (extended-release) (1) ·
AF conversion within hours of single PO dose (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) ·
Hours (1) ·
LDL lowering within 2 weeks (1) ·
Symptom shortening detectable within 24-48 hours of starting (small absolute benefit; ~1 day reduction in symptom duration) (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) ·
3–7 h (1) ·
~12 hours'"`UNIQ--ref-00000D82-QINU`"' (1) ·
~12.9 hours'"`UNIQ--ref-00000552-QINU`"' (1) ·
~14 hours (adults); longer in elderly and renal impairment'"`UNIQ--ref-0000113F-QINU`"' (1) ·
~17-19 hours (longer than daridorexant) (1) ·
~22 hours (parent + active glucuronide)'"`UNIQ--ref-00000450-QINU`"' (1) ·
~6-10 hours (oseltamivir carboxylate, the active metabolite)'"`UNIQ--ref-00000E94-QINU`"' (1)
bioavailability:
64-90% (oral; not affected by food)'"`UNIQ--ref-00000079-QINU`"' (1) ·
80-90% oral (1) ·
Variable (oral; rapidly conjugated to active glucuronide; food does not affect)'"`UNIQ--ref-00000451-QINU`"' (1) ·
~44% (1) ·
~50% (1) ·
~75% (oral, as the active carboxylate after hepatic esterase activation)'"`UNIQ--ref-00000E95-QINU`"' (1) ·
~78% (oral; high-fat meal modestly reduces but is not clinically significant)'"`UNIQ--ref-00000553-QINU`"' (1) ·
~90% (oral)'"`UNIQ--ref-00001140-QINU`"' (1) ·
~90% (oral; not affected by food but reduced by divalent cations)'"`UNIQ--ref-00000D83-QINU`"' (1)
pregnancy:
'''Avoid in pregnancy where alternatives exist''' (animal cartilage toxicity).<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
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 C (1) ·
Category D'"`UNIQ--ref-0000006C-QINU`"' (1) ·
Generally used when influenza treatment is indicated; pregnancy is a recognized risk factor for severe influenza.<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) ·
Use in fetal SVT (transplacental antiarrhythmic therapy) is established; otherwise weigh against alternatives.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1)
legal:
Rx, Schedule IV (US) (1) ·
Rx-only in US (1) ·
Schedule IV (US) (1) ·
[[USLegal:Prescription only|Rx-only]] in US (4) ·
[[USLegal:Prescription only|Rx-only]] in US. '''Contraindicated in structural heart disease''' — CAST trial (1989) showed increased mortality from class IC agents in patients with prior MI; modern use is limited to structurally normal hearts'"`UNIQ--ref-00001141-QINU`"' (1) ·
[[USLegal:Prescription only|Rx-only]] in US. Carries the same fluoroquinolone-class '''Boxed Warnings''' as ciprofloxacin/levofloxacin'"`UNIQ--ref-00000D84-QINU`"' (1)
Showing below up to 9 results in range #1 to #9.