Drilldown: Medicines

None (3) · Bupropion (1) · 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) · Quviviq (1) · Wellbutrin (IR, SR, XL), Zyban (smoking cessation), Aplenzin (hydrobromide salt), Forfivo XL (1)

Dual orexin receptor antagonist (DORA) (3) · PDE5 Inhibitor (1) · the first approved (1) · [[:Category:Antidepressants|Antidepressant]] (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:NDRIs|Norepinephrine-dopamine reuptake inhibitor (NDRI)]] (1) · [[:Category:Smoking cessation medicines|Smoking cessation medicine]] (1) · [[:Category:Sulfonylureas|Sulfonylurea (third-generation)]] (1)

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) · 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) · '"`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)

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-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"' (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) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · 60 mg PO BID or 180 mg PO once daily (1) · SR 150 mg PO once daily for 3 days, then 150 mg BID. XL 150 mg PO once daily for 4 days, then 300 mg once daily. Zyban (smoking cessation) 150 mg daily for 3 days, then 150 mg BID (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) · 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) · SR tablets 100, 150, 200 mg; XL tablets 150, 300 mg; IR tablets 75, 100 mg (less common); Aplenzin (bupropion hydrobromide) 174, 348, 522 mg (1)

10 mg/d (1) · 180 mg/d (adults) (1) · 20 mg/d (2) · 450 mg/day; doses above this raise seizure risk steeply (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) · SR ~12 hours; XL 24 hours (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) · Bupropion ~21 hours; hydroxybupropion (active metabolite) ~20-37 hours'"`UNIQ--ref-00000023-QINU`"' (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) · ~7 hours apparent'"`UNIQ--ref-00001374-QINU`"' (1) · ~8 hours (shorter than suvorexant and lemborexant) (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) · ~5-20% (extensive first-pass), highly variable between individuals'"`UNIQ--ref-00000024-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) · ~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 (3) · Limited human data; some animal cardiac signal not clearly replicated in human cohort studies; observational signals inconclusive.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (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, Schedule IV (US) (3) · Rx-only in US (1) · [[USLegal:Prescription only|Rx-only]] in US (3) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults. Not controlled'"`UNIQ--ref-00000025-QINU`"' (1)