Drilldown: Medicines

None (1) · Bisoprolol (1) · Cyclobenzaprine (1) · Insulin degludec (1) · Meclizine (1) · Nebivolol (1)

Antivert (Rx), Bonine (OTC), Dramamine Less Drowsy (OTC) (1) · Bystolic (1) · Flexeril (IR; brand discontinued in US, generic widely available), Amrix (ER) (1) · Rexulti (1) · Tresiba (1) · Zebeta (1)

5HT1A activity than aripiprazole (1) · 5HT2A (1) · Atypical antipsychotic (1) · Beta Blocker (2) · Cardioselective (β1) (1) · Cardioselective (β1) + vasodilator (1) · D2/5HT1A partial agonist with stronger α1A (1) · [[:Category:Antiemetics|Antiemetic]] (1) · [[:Category:Antihistamines|First-generation antihistamine (piperazine)]] (1) · [[:Category:Antivertigo medicines|Antivertigo medicine]] (1) · [[:Category:Basal_insulins|Basal insulin]] (1) · [[:Category:Insulins|Insulin]] (1) · [[:Category:Skeletal muscle relaxants|Skeletal muscle relaxant (centrally-acting)]] (1) · [[:Category:Tricyclic-related compounds|Tricyclic-related compound]] (1) · [[:Category:Ultra-long-acting_insulins|Ultra-long-acting insulin analog]] (1)

None (1) · Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (1) · Partial agonist at D2 and 5HT1A. Antagonist at 5HT2A, α1A, α1B, α2C. More potent 5HT2A antagonism, 5HT1A partial agonism, and α1 antagonism (relative to D2 partial agonism) than aripiprazole, proposed to reduce akathisia and enhance affective/cognitive effects. (1) · The d-enantiomer is a highly β1-selective antagonist; the l-enantiomer triggers endothelial nitric-oxide–mediated vasodilation. Unique among beta blockers for this NO mechanism. (1) · '"`UNIQ--vote-00000013-QINU`"' Anticholinergic burden (dry mouth, blurred vision, urinary retention, cognitive effects) is the principal adverse-event concern and the basis for Beers-list cautions in elderly patients'"`UNIQ--ref-00000014-QINU`"'. (1) · '"`UNIQ--vote-00001356-QINU`"' Binds the same insulin receptor as endogenous insulin with comparable mitogenic-to-metabolic ratio'"`UNIQ--ref-00001357-QINU`"'. (1)

Schizophrenia (FDA-approved 2015). Adjunctive treatment of major depressive disorder (2015). '''Agitation associated with dementia due to Alzheimer disease''' (FDA-approved May 2023, first agent specifically approved for this problem). Investigational for PTSD (combined with sertraline). (1) · '"`UNIQ--vote-00000015-QINU`"', '"`UNIQ--vote-00000016-QINU`"', '"`UNIQ--vote-00000017-QINU`"' (1) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"' (1) · '"`UNIQ--vote-0000059D-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1) · '"`UNIQ--vote-00001358-QINU`"', '"`UNIQ--vote-00001359-QINU`"' (1)

2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) · 5 mg daily (1) · IR 5 mg PO TID; titrate to 10 mg TID if needed. Amrix ER 15 mg PO once daily. Off-label insomnia / fibromyalgia: 5-10 mg PO at bedtime (1) · Motion sickness: 25-50 mg PO 1 hour before travel, repeat every 24 hours as needed. Vertigo: 25-100 mg/day divided (1) · Schizophrenia: 1 mg PO daily × 4 days, then 2 mg daily × 3 days, then 4 mg daily. MDD adjunct: 0.5-1 mg daily, increase to 2 mg max. AD agitation: 0.5 mg daily, titrate to 2-3 mg daily. (1) · ~10 units SC at the same time daily, or 0.1-0.2 units/kg/d; titrate by fasting glucose (1)

0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets (1) · 100 U/mL (FlexTouch pen) and 200 U/mL (FlexTouch pen, higher-dose convenience) (1) · 2.5, 5, 10, 20 mg tabs (1) · 5, 10 mg tabs (1) · IR tablets 5, 7.5, 10 mg; Amrix ER capsules 15, 30 mg (1) · Tablets 12.5, 25 mg; chewable tablets 25 mg (1)

100 mg/day (vertigo) (1) · 20 mg/d (1) · 30 mg/day (IR or ER) (1) · 4 mg/d (schizophrenia); 3 mg/d (AD agitation); 3 mg/d (MDD adjunct) (1) · 40 mg/d (1) · Titrated to glucose; no fixed ceiling (1)

Oral (5) · Subcutaneous (never IV; not for use in insulin pumps) (1)

None · Hours · 30-60 minutes · 1-2 hours · ~30 min · LDL lowering at 2 weeks, max by 4 weeks · ~1 hour · 15-30 minutes · 15–30 min · 1–2 h · 30–60 min · Antidepressant effect emerges over 1-2 weeks · BP and symptomatic LUTS improvement within 1-2 weeks · BP effect within 1-2 weeks · Clinical improvement within 24-72 hours · Days · Motor improvement over days at therapeutic dose · Over weeks · Postprandial glucose effect within days; HbA1c by 12 weeks · Sleep effect from first dose; antidepressant effect over 1-4 weeks

Other values:

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12-24 hours (IR); 24 hours (Amrix ER) (1) · 12-24 hours (long for an antihistamine) (1) · 24 h (2) · >42 hours per dose (effectively flat once at steady state) (1) · Daily dosing (1)

18 hours (IR); 32-33 hours (ER)'"`UNIQ--ref-0000001A-QINU`"' (1) · 9–12 h (1) · ~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers) (1) · ~25 hours apparent (functional duration well over 42 hours from multi-hexamer depot)'"`UNIQ--ref-0000135A-QINU`"' (1) · ~6 hours'"`UNIQ--ref-00000018-QINU`"' (1) · ~91 hours (1)

~100% from subcutaneous depot (1) · ~12% (extensive metabolizers); ~96% (poor metabolizers) (1) · ~25% (oral)'"`UNIQ--ref-00000019-QINU`"' (1) · ~33-55% (IR); reduced by food'"`UNIQ--ref-0000001B-QINU`"' (1) · ~90% (low first-pass) (1) · ~95% (1)

Category C (2) · Insulin is the preferred glucose-lowering therapy in pregnancy; degludec has reassuring observational data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; National Pregnancy Registry available (1) · Limited human data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Older agent with substantial use experience; observational signals reassuring for first-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

Rx (1) · Rx-only in US (2) · [[USLegal:Over-the-counter|OTC]] as Bonine and Dramamine Less Drowsy; [[USLegal:Prescription only|Rx-only]] as Antivert (1) · [[USLegal:Prescription only|Rx-only]] in US (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, distinguishing it from the carisoprodol alternative for muscle spasm'"`UNIQ--ref-0000001C-QINU`"' (1)