Drilldown: Medicines

None (4) · Fexofenadine (1) · Glimepiride (1) · Insulin detemir (1) · Insulin glargine (1) · Vardenafil (1)

Allegra, Allegra Allergy 24 Hour, Mucinex Allergy (combo) — all now OTC in US (1) · Amaryl (1) · Belsomra (1) · Dayvigo (1) · Lantus, Basaglar, Semglee, Toujeo (U-300) (1) · Levemir, Levemir FlexTouch (US discontinuation announced 2024) (1) · Levitra, Staxyn (1) · Nuplazid (1) · Quviviq (1)

Dual orexin receptor antagonist (DORA) (3) · PDE5 Inhibitor (1) · Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism) (1) · the first approved (1) · [[:Category:Antihistamines|Antihistamine]] (1) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (1) · [[: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 (3) · 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) · Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (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) · Selective inverse agonist at 5HT2A receptors with weaker activity at 5HT2C. Has no significant dopamine D2 affinity, unique among approved antipsychotics. Inverse agonism (rather than antagonism) reduces constitutive 5HT2A receptor activity below baseline. (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-00000CC9-QINU`"' Mostly excreted unchanged in feces and urine; P-glycoprotein substrate (the basis of the fruit-juice interaction). (1)

Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (1) · 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 maintenance) in adults (FDA-approved Dec 2019) (1) · Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022) (1) · '"`UNIQ--vote-00000239-QINU`"', '"`UNIQ--vote-0000023A-QINU`"' (1) · '"`UNIQ--vote-00000491-QINU`"' (1) · '"`UNIQ--vote-00000669-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) · 10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 10 mg ~1 h before sexual activity (1) · 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) · 34 mg PO once daily (1) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · 60 mg PO BID or 180 mg PO once 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)

1 mg, 2 mg, 4 mg tablets (1) · 10 mg, 34 mg capsules/tablets (1) · 100 U/mL (Lantus, Basaglar, Semglee) vials and pens; 300 U/mL (Toujeo) pens (1) · 100 U/mL FlexTouch pen, vial (1) · 2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn) (1) · 25 mg, 50 mg tablets (1) · 30, 60, 180 mg tablets; 30 mg ODT; 6 mg/mL oral suspension; all OTC (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1)

10 mg/d (1) · 180 mg/d (adults) (1) · 20 mg/d (2) · 34 mg/d (1) · 50 mg/d (1) · 8 mg/d (1) · Titrated to glucose (1) · Titrated to glucose; no fixed ceiling (1)

Oral (7) · 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:

Search

12-24 hours (1) · 24 hours (1) · 4–5 h (1) · 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) · ~7-8 hours (3)

4–5 h (1) · ~12 hours (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) · ~17-19 hours (longer than daridorexant) (1) · ~5-9 hours (parent and active metabolites combined)'"`UNIQ--ref-00000492-QINU`"' (1) · ~57 hours (parent), ~200 h (active metabolite) (1) · ~7 hours apparent'"`UNIQ--ref-00001374-QINU`"' (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

Not characterized; oral dosing once daily (1) · ~100% (oral; not significantly affected by food)'"`UNIQ--ref-00000493-QINU`"' (1) · ~100% from subcutaneous depot (by definition of the route) (1) · ~15% (extensive hepatic first-pass) (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) · ~44% (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) · ~62% (1) · ~82% (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) · Category B (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; avoid (4) · 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, Schedule IV (US) (3) · Rx-only in US (1) · Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) (1) · [[USLegal:Prescription only|Rx-only]] in US (3)