Drilldown: Medicines

None (1) · Fexofenadine (1) · Glimepiride (1) · Insulin detemir (1) · Insulin glargine (1) · Irbesartan (1) · Telmisartan (1)

Allegra, Allegra Allergy 24 Hour, Mucinex Allergy (combo) — all now OTC in US (1) · Amaryl (1) · Avapro (1) · Lantus, Basaglar, Semglee, Toujeo (U-300) (1) · Levemir, Levemir FlexTouch (US discontinuation announced 2024) (1) · Micardis (1) · Rexulti (1)

5HT1A activity than aripiprazole (1) · 5HT2A (1) · Atypical antipsychotic (1) · D2/5HT1A partial agonist with stronger α1A (1) · [[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (2) · [[:Category:Antihistamines|Antihistamine]] (1) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (1) · [[:Category:Antihypertensives|Antihypertensive]] (2) · [[:Category:Basal_insulins|Basal insulin]] (2) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist (second-generation)]] (1) · [[:Category:Insulins|Insulin]] (2) · [[:Category:Insulin_secretagogues|Insulin secretagogue]] (1) · [[:Category:Long-acting_insulins|Long-acting insulin analog]] (2) · [[:Category:Sulfonylureas|Sulfonylurea (third-generation)]] (1)

None (2) · 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) · '"`UNIQ--vote-00000237-QINU`"' Binds the same insulin receptor as endogenous insulin with comparable mitogenic-to-metabolic ratio; provides basal hepatic glucose suppression and peripheral glucose uptake without prandial peaks'"`UNIQ--ref-00000238-QINU`"'. (1) · '"`UNIQ--vote-0000083E-QINU`"' CYP2C9 substrate; no clinically active metabolites. The IDNT trial established renoprotection in diabetic nephropathy independent of BP lowering, contributing to the ARB class indication in T2DM with proteinuria'"`UNIQ--ref-0000083F-QINU`"'. (1) · '"`UNIQ--vote-00000AEA-QINU`"' The 24-hour half-life supports once-daily dosing with consistent overnight BP control. Largely hepatically cleared (~98% biliary); no significant renal clearance dependence'"`UNIQ--ref-00000AEB-QINU`"'. (1) · '"`UNIQ--vote-00000CC9-QINU`"' Mostly excreted unchanged in feces and urine; P-glycoprotein substrate (the basis of the fruit-juice interaction). (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-00000239-QINU`"', '"`UNIQ--vote-0000023A-QINU`"' (1) · '"`UNIQ--vote-00000491-QINU`"' (1) · '"`UNIQ--vote-00000840-QINU`"', '"`UNIQ--vote-00000841-QINU`"' (1) · '"`UNIQ--vote-00000AEC-QINU`"', '"`UNIQ--vote-00000AED-QINU`"' (1) · '"`UNIQ--vote-00000CCA-QINU`"', '"`UNIQ--vote-00000CCB-QINU`"' (1) · '"`UNIQ--vote-00001372-QINU`"', '"`UNIQ--vote-00001373-QINU`"' (1)

1-2 mg PO once daily with breakfast; titrate by glycemic response (1) · 150 mg PO once daily; titrate to 300 mg if needed (1) · 40 mg PO once daily; titrate to 80 mg (1) · 60 mg PO BID or 180 mg PO once daily (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) · ~10 units SC at the same time daily, or 0.1-0.2 units/kg/d; titrate by fasting glucose. Frequently dosed BID at moderate-to-high doses (1)

0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets (1) · 1 mg, 2 mg, 4 mg tablets (1) · 100 U/mL (Lantus, Basaglar, Semglee) vials and pens; 300 U/mL (Toujeo) pens (1) · 100 U/mL FlexTouch pen, vial (1) · 20, 40, 80 mg tablets (1) · 30, 60, 180 mg tablets; 30 mg ODT; 6 mg/mL oral suspension; all OTC (1) · 75, 150, 300 mg tablets (1)

180 mg/d (adults) (1) · 300 mg/d (1) · 4 mg/d (schizophrenia); 3 mg/d (AD agitation); 3 mg/d (MDD adjunct) (1) · 8 mg/d (1) · 80 mg/d (1) · Titrated to glucose (1) · Titrated to glucose; no fixed ceiling (1)

Oral (5) · Subcutaneous (1) · 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 (1) · 24 hours (3) · Daily dosing (1) · ~12-24 hours (dose-dependent; BID dosing often needed at higher doses) (1) · ~24 hours per dose (peakless profile by design) (1)

11-15 hours'"`UNIQ--ref-00000842-QINU`"' (1) · ~12 hours apparent (functional duration ~24 hours due to depot release kinetics)'"`UNIQ--ref-0000023B-QINU`"' (1) · ~14 hours'"`UNIQ--ref-00000CCC-QINU`"' (1) · ~24 hours (longest of the ARB class; suits patients with morning BP surge)'"`UNIQ--ref-00000AEE-QINU`"' (1) · ~5-9 hours (parent and active metabolites combined)'"`UNIQ--ref-00000492-QINU`"' (1) · ~7 hours apparent'"`UNIQ--ref-00001374-QINU`"' (1) · ~91 hours (1)

42-58% (oral; dose-dependent)'"`UNIQ--ref-00000AEF-QINU`"' (1) · 60-80% (oral; not significantly affected by food)'"`UNIQ--ref-00000843-QINU`"' (1) · ~100% (oral; not significantly affected by food)'"`UNIQ--ref-00000493-QINU`"' (1) · ~100% from subcutaneous depot (by definition of the route) (1) · ~33% (oral; fruit juices including grapefruit, orange, and apple reduce absorption substantially via OATP1A2 inhibition — distinctive interaction not seen with most other H1s)'"`UNIQ--ref-00000CCD-QINU`"' (1) · ~60% from subcutaneous depot (reduced by reversible albumin binding via the myristic acid side chain that also extends duration)'"`UNIQ--ref-00001375-QINU`"' (1) · ~95% (1)

'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000844-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000AF0-QINU`"' (1) · Avoid; switch to insulin. Neonatal hypoglycemia reported.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe; loratadine and cetirizine have more pregnancy data and are typically preferred.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Insulin is the preferred glucose-lowering therapy in pregnancy; glargine has reassuring observational data, though NPH and detemir remain the traditional choices.<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) · One of the better-studied basal insulin analogs in pregnancy; reassuring data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

OTC in US (1) · Rx (1) · [[USLegal:Prescription only|Rx-only]] in US (5)