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Designer benzodiazepine (1) · Research material (1) · Sedative-Hypnotic (1) · Triazolobenzodiazepine (1) · [[:Category:Aminoglycosides|Aminoglycoside antibiotic]] (1) · [[:Category:Analgesics|Analgesic (opioid-sparing parenteral)]] (1) · [[:Category:Antianginals|Antianginal]] (1) · [[:Category:Antibacterials|Antibacterial]] (3) · [[:Category:Antiglaucoma medicines|Antiglaucoma medicine]] (1) · [[:Category:Antihypertensives|Antihypertensive]] (1) · [[:Category:B-vitamins|B-vitamin]] (1) · [[:Category:Beta blockers|Beta blocker (non-selective)]] (1) · [[:Category:Calcineurin_inhibitors|Calcineurin inhibitor]] (1) · [[:Category:Chronobiotics|Chronobiotic (circadian phase regulator)]] (1) · [[:Category:Corticosteroids|Corticosteroid]] (1) · [[:Category:Crystalloid_IV_fluids|Crystalloid IV fluid]] (1) · [[:Category:Electrolyte_replacements|Electrolyte replacement]] (1) · [[:Category:Fluoroquinolones|Fluoroquinolone antibiotic]] (1) · [[:Category:Glucocorticoids|Glucocorticoid (intermediate-acting)]] (1) · [[:Category:Hematinics|Hematinic]] (1) · [[:Category:Immunosuppressants|Immunosuppressant]] (2) · [[:Category:Macrolide_antibiotics|Macrolide antibiotic]] (1) · [[:Category:Melatonin receptor agonists|Melatonin receptor agonist]] (1) · [[:Category:Migraine prophylactics|Migraine prophylactic]] (1) · [[:Category:Nitrates|Organic nitrate]] (1) · [[:Category:Non-benzodiazepine hypnotics|Non-benzodiazepine hypnotic]] (1) · [[:Category:NSAIDs|Non-steroidal anti-inflammatory (NSAID)]] (1) · [[:Category:Prokinetics|Prokinetic (off-label)]] (1) · [[:Category:Schedule IV controlled substances|Schedule IV controlled substance]] (1) · [[:Category:Sleep aids|Sleep aid]] (2) · [[:Category:Vasodilators|Vasodilator]] (1) · [[:Category:Vitamins|Vitamin]] (1) · [[GLP-1 receptor agonist]] · [[Antidiabetic medicines|Antidiabetic]] · Fc-fusion biologic (1) · [[GLP-1 receptor agonist]] · [[Antidiabetic medicines|Antidiabetic]] · First-in-class incretin mimetic (1) · [[GLP-1 receptor agonist]] · [[Antidiabetic medicines|Antidiabetic]] · [[Anti-obesity medicines|Anti-obesity]] · [[Cardiovascular risk reduction]] agent (2) · [[GLP-1 receptor agonist]] · [[GIP receptor agonist]] · [[Antidiabetic medicines|Antidiabetic]] · [[Anti-obesity medicines|Anti-obesity]] · "Twincretin" (1)
uses:
No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · [[Type 2 diabetes mellitus]] (adjunct, second-line) (1) · [[Type 2 diabetes mellitus]] (incl. pediatric ≥10 y) · [[Obesity]] (incl. pediatric ≥12 y) · [[Cardiovascular risk reduction]] in T2DM (1) · [[Type 2 diabetes mellitus]] · [[Cardiovascular risk reduction]] in T2DM (1) · [[Type 2 diabetes mellitus]] · [[Obesity]] · [[Cardiovascular risk reduction]] in obesity without diabetes · [[MASH]] with stage 2–3 fibrosis · [[Chronic kidney disease]] in T2DM (1) · [[Type 2 diabetes mellitus]] · [[Obesity]] · [[Obstructive sleep apnea]] in obesity (1) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"' (1) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"' (1) · '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (1) · '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"' (1) · '"`UNIQ--vote-00000039-QINU`"', '"`UNIQ--vote-0000003A-QINU`"', '"`UNIQ--vote-0000003B-QINU`"', '"`UNIQ--vote-0000003C-QINU`"', '"`UNIQ--vote-0000003D-QINU`"' (1) · '"`UNIQ--vote-00000607-QINU`"', '"`UNIQ--vote-00000608-QINU`"', '"`UNIQ--vote-00000609-QINU`"', '"`UNIQ--vote-0000060A-QINU`"' (1) · '"`UNIQ--vote-000008C0-QINU`"', '"`UNIQ--vote-000008C1-QINU`"', '"`UNIQ--vote-000008C2-QINU`"', '"`UNIQ--vote-000008C3-QINU`"' (1) · '"`UNIQ--vote-00000A8C-QINU`"', '"`UNIQ--vote-00000A8D-QINU`"', '"`UNIQ--vote-00000A8E-QINU`"', '"`UNIQ--vote-00000A8F-QINU`"', '"`UNIQ--vote-00000A90-QINU`"' (1) · '"`UNIQ--vote-00000C0A-QINU`"', '"`UNIQ--vote-00000C0B-QINU`"', '"`UNIQ--vote-00000C0C-QINU`"', '"`UNIQ--vote-00000C0D-QINU`"', '"`UNIQ--vote-00000C0E-QINU`"' (1) · '"`UNIQ--vote-00000D38-QINU`"', '"`UNIQ--vote-00000D39-QINU`"', '"`UNIQ--vote-00000D3A-QINU`"', '"`UNIQ--vote-00000D3B-QINU`"', '"`UNIQ--vote-00000D3C-QINU`"', '"`UNIQ--vote-00000D3D-QINU`"' (1) · '"`UNIQ--vote-000010AF-QINU`"', '"`UNIQ--vote-000010B0-QINU`"', '"`UNIQ--vote-000010B1-QINU`"', '"`UNIQ--vote-000010B2-QINU`"' (1) · '"`UNIQ--vote-000014BE-QINU`"', '"`UNIQ--vote-000014BF-QINU`"', '"`UNIQ--vote-000014C0-QINU`"', '"`UNIQ--vote-000014C1-QINU`"', '"`UNIQ--vote-000014C2-QINU`"' (1)
starting dose:
'''5 mg PO at bedtime for women, 5-10 mg for men''' (per FDA's 2013 sex-specific dose reduction for women due to slower clearance). Ambien CR 6.25 mg women / 6.25-12.5 mg men. Intermezzo SL 1.75 mg women / 3.5 mg men (1) · 0.5-3 mg PO 30-60 minutes before bedtime. Some patients respond to micro-doses (0.3 mg) without additional benefit at higher doses. For circadian phase shifting, timing relative to dim-light melatonin onset matters more than absolute dose (1) · 0.75 mg SC weekly'"`UNIQ--ref-00000053-QINU`"' (1) · 2.5 mg SC weekly × 4 wk (non-therapeutic ramp)'"`UNIQ--ref-000002FB-QINU`"' (1) · 250-500 mg PO QID; 7.5-12.5 mg/kg IV q6h; topical and ophthalmic per formulation (1) · Byetta: 5 µg SC twice daily, within 60 min before morning and evening meals'"`UNIQ--ref-000000E3-QINU`"' · Bydureon BCise: 2 mg SC once weekly'"`UNIQ--ref-000000E4-QINU`"' (1) · IM: 60 mg single dose or 30 mg every 6 hours. IV: 30 mg every 6 hours. Oral (continuation only): 10-20 mg every 4-6 hours. Sprix nasal: 31.5 mg every 6-8 hours. '''Maximum 5 days total combined use''' (1) · IV: traditional 1-1.7 mg/kg q8h or extended-interval 5-7 mg/kg q24h with target-trough monitoring; inhaled CF 300 mg BID × 28 days on / 28 days off; ophthalmic 1-2 drops in affected eye(s) q4h (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Ophthalmic: 1 drop 0.5% in affected eye(s) BID (or once daily for XE / Istalol). Oral hypertension: 10 mg PO BID, titrate to 60 mg/day. Migraine prophylaxis: 10 mg BID, titrate to 30 mg/day (1) · Oral 200-400 mg BID; ophthalmic 1-2 drops in affected eye(s) q2-4h initially, then taper; otic 5-10 drops in affected ear BID (1) · Ozempic: 0.25 mg SC weekly × 4 wk'"`UNIQ--ref-00000245-QINU`"' · Wegovy: 0.25 mg SC weekly × 4 wk'"`UNIQ--ref-00000246-QINU`"' · Rybelsus: 3 mg PO daily × 30 d'"`UNIQ--ref-00000247-QINU`"' (1) · Pediatric 1-2 mg/kg/d (max 60 mg) PO for asthma exacerbation; adult dosing similar to prednisone milligram-for-milligram (~1:1 potency) (1) · Replacement: 1000 mcg IM daily for 1 week, then weekly for 4 weeks, then monthly; or 1000-2000 mcg PO daily (effective even in pernicious anemia via passive diffusion); intranasal 500 mcg weekly (1) · SL 0.3-0.6 mg every 5 minutes up to 3 doses for acute angina (call EMS if not resolved after the third); IV infusion 5-10 mcg/min titrated; transdermal patch 0.2-0.4 mg/hr for 12-14 hours daily (nitrate-free interval prevents tolerance) (1) · Transplant: 5-10 mg/kg/d divided BID, titrated to trough levels (typically 100-300 ng/mL depending on regimen and post-transplant interval); ophthalmic Restasis 0.05% one drop BID (1) · Victoza: 0.6 mg SC daily × 1 wk'"`UNIQ--ref-00000181-QINU`"' · Saxenda: 0.6 mg SC daily × 1 wk'"`UNIQ--ref-00000182-QINU`"' (1) · Volume and concentration titrated to clinical status; symptomatic hyponatremia: 3% NaCl 100-150 mL bolus, reassess (1)
preparations:
0.225%, 0.45%, 0.9%, 3%, 5% IV solutions; 0.9% nasal spray; 3% and 7% nebulizer solutions; oral tablets (1 g) (1) · 100, 250, 500, 1000, 5000 mcg tablets (OTC and Rx); 1000 mcg/mL injection; intranasal spray; sublingual (1) · 200, 300, 400 mg tablets (mostly generic now); 0.3% ophthalmic solution; 0.3% otic solution (1) · 250, 500 mg base or stearate tablets; ER tablets; ethyl succinate 200 mg/5 mL suspension; 500 mg, 1 g IV (lactobionate); 2% topical solution/gel; 0.5% ophthalmic ointment (1) · 5 mg tablets; 5 mg/5 mL, 10 mg/5 mL, 15 mg/5 mL oral solutions (sweetened pediatric); 5 mg/5 mL syrup; ophthalmic 0.12%, 1% suspensions and 1% solution (1) · Byetta pre-filled multi-dose pen: 5 µg / 10 µg per dose'"`UNIQ--ref-000000E5-QINU`"' · Bydureon BCise single-dose autoinjector: 2 mg extended-release microsphere suspension'"`UNIQ--ref-000000E6-QINU`"' (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · IR tablets 5, 10 mg; CR tablets 6.25, 12.5 mg; SL tablets 1.75, 3.5, 5, 10 mg; oral spray (1) · IV 10 mg/mL, 40 mg/mL; inhaled 300 mg/5 mL solution (Tobi, Bethkis); Podhaler dry powder; 0.3% ophthalmic solution and ointment (1) · OTC tablets, sublingual tablets, gummies, liquid, extended-release tablets and capsules; common strengths 0.5, 1, 3, 5, 10 mg (1) · Pre-filled multi-dose pen (0.25 / 0.5 / 1 / 2 mg, Ozempic;'"`UNIQ--ref-00000248-QINU`"' 0.25 / 0.5 / 1 / 1.7 / 2.4 mg, Wegovy'"`UNIQ--ref-00000249-QINU`"') · Oral tablet 3 / 7 / 14 mg co-formulated with SNAC absorption enhancer (Rybelsus)'"`UNIQ--ref-0000024A-QINU`"' (1) · Pre-filled multi-dose pen (3 mL): Victoza 6 mg/mL (0.6 / 1.2 / 1.8 mg per day);'"`UNIQ--ref-00000183-QINU`"' Saxenda 6 mg/mL (0.6 / 1.2 / 1.8 / 2.4 / 3.0 mg per day)'"`UNIQ--ref-00000184-QINU`"' (1) · Pre-filled single-dose pen and vial: 2.5 / 5 / 7.5 / 10 / 12.5 / 15 mg'"`UNIQ--ref-000002FC-QINU`"''"`UNIQ--ref-000002FD-QINU`"' (1) · Pre-filled single-dose pen: 0.75 / 1.5 / 3 / 4.5 mg'"`UNIQ--ref-00000054-QINU`"' (1) · Sandimmune 25, 100 mg capsules; Neoral 25, 100 mg modified soft gel; 100 mg/mL oral solution; 50 mg/mL IV; Restasis 0.05% ophthalmic emulsion (1) · SL 0.3, 0.4, 0.6 mg tablets; lingual spray 0.4 mg/spray; ER 2.5-9 mg capsules; transdermal patch 0.1-0.8 mg/hr; 2% ointment; 0.4% rectal ointment; 5 mg/mL IV (1) · Tablets 10 mg; injection 15 mg/mL and 30 mg/mL; nasal spray 15.75 mg/spray (Sprix); ophthalmic solution 0.4%, 0.45%, 0.5% (1) · Tablets 5, 10, 20 mg; ophthalmic solution 0.25%, 0.5%; ophthalmic gel-forming solution 0.25%, 0.5% (Timoptic-XE) (1)
routes: (Click arrow to add another value)
bioavailability:
100% (IV); essentially complete (oral) (1) · Highly route-dependent: SL bypasses first-pass; oral has extensive first-pass (used only for chronic ER preparations); transdermal predictable'"`UNIQ--ref-00000C10-QINU`"' (1) · IV/IM ~100%; inhaled: minimal systemic; oral: negligible (not used orally for systemic infection)'"`UNIQ--ref-000010B4-QINU`"' (1) · Not formally characterized in humans. (1) · Oral ~1-3% via passive diffusion at high doses (independent of intrinsic factor); IM/SC ~100% (1) · Sandimmune: highly variable (~30%); Neoral microemulsion: ~50%, less variable; '''Sandimmune and Neoral are NOT bioequivalent and not interchangeable''''"`UNIQ--ref-00000A92-QINU`"' (1) · SC ~47%–65%'"`UNIQ--ref-0000005A-QINU`"' (1) · SC ~55%'"`UNIQ--ref-0000018B-QINU`"' (1) · SC ~65%–75%<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · SC ~80%<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · SC ~89%<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> · Oral ~0.4–1% (SNAC-enhanced)'"`UNIQ--ref-00000254-QINU`"' (1) · ~100% (oral, but oral use is limited to continuation from parenteral)'"`UNIQ--ref-00000021-QINU`"' (1) · ~15% (oral; highly variable due to extensive and variable first-pass metabolism)'"`UNIQ--ref-00000022-QINU`"' (1) · ~30-65% (oral; acid-labile, hence enteric-coated formulations; food affects absorption variably)'"`UNIQ--ref-00000D3F-QINU`"' (1) · ~50% (oral); systemic absorption from ophthalmic application is clinically meaningful via nasolacrimal drainage'"`UNIQ--ref-0000001C-QINU`"' (1) · ~70% (oral)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~70% (oral)'"`UNIQ--ref-000008C5-QINU`"' (1) · ~95% (oral)'"`UNIQ--ref-000014C4-QINU`"' (1)
pregnancy:
None (1) · '''Avoid in pregnancy where alternatives exist''' (animal cartilage toxicity; class-wide concern).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Aminoglycoside-class ototoxicity in fetal cochlea is documented; use only when alternatives have failed.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Avoid from 20 weeks gestation onward per FDA's 2020 expanded NSAID warning; contraindicated from 30 weeks. Specifically contraindicated in labor and delivery due to inhibition of uterine contractions'"`UNIQ--ref-00000022-QINU`"' (1) · Avoid. Benzodiazepines are associated with neonatal sedation, floppy-infant syndrome, and withdrawal; teratogenic signal weak but non-zero. Designer benzo with no safety data, assume worst-case. (1) · Avoid. Discontinue at least 1 month before planned pregnancy. Animal data show embryofetal harm.'"`UNIQ--ref-0000005B-QINU`"' (1) · Avoid. Discontinue before planned pregnancy.'"`UNIQ--ref-000000EF-QINU`"' (1) · Avoid. Discontinue before planned pregnancy.'"`UNIQ--ref-0000018C-QINU`"' (1) · Avoid. Discontinue ≥1 month pre-conception. May reduce oral contraceptive efficacy during titration.'"`UNIQ--ref-00000304-QINU`"' (1) · Generally considered safe; commonly used in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; case reports of neonatal sedation with late-pregnancy exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; endogenous hormone, but supplemental pharmacological doses are not well characterized in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; β-blocker class effects include fetal growth restriction and neonatal bradycardia/hypoglycemia.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Routinely supplemented in vegan pregnancies and pernicious anemia.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Standard fluid and electrolyte management (1) · Use when benefits outweigh; small association with oral clefts debated.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Used in obstetric emergencies (uterine relaxation, severe hypertension) when needed; otherwise limited routine use.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Used in transplant pregnancy when continued immunosuppression is required; reassuring data overall but careful monitoring needed.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (1) · OTC (low/mid-dose oral) and [[USLegal:Prescription only|Rx-only]] (injection, intranasal) in US (1) · OTC (ophthalmic ointment) and [[USLegal:Prescription only|Rx-only]] (other forms) in US (1) · Rx-only;'"`UNIQ--ref-0000005C-QINU`"' not a controlled substance (1) · Rx-only;'"`UNIQ--ref-000000F0-QINU`"' not a controlled substance (1) · Rx-only;'"`UNIQ--ref-0000018D-QINU`"' not a controlled substance (1) · Rx-only;'"`UNIQ--ref-00000256-QINU`"' not a controlled substance (1) · Rx-only;'"`UNIQ--ref-00000305-QINU`"' not a controlled substance (1) · [[USLegal:Over-the-counter|OTC]] dietary supplement in the US ('''not FDA-regulated as a medicine'''; multiple studies show OTC products contain 50-470% of labeled melatonin content); [[USLegal:Prescription only|Rx-only]] in the EU and UK (1) · [[USLegal:Prescription only|Rx-only]] for parenteral formulations; OTC for oral, nasal, and many nebulizer products (1) · [[USLegal:Prescription only|Rx-only]] in US (5) · [[USLegal:Prescription only|Rx-only]] in US. Carries '''Boxed Warning''' for risk of malignancy and serious infection; nephrotoxicity, hypertension, and immunosuppression-associated complications'"`UNIQ--ref-00000A93-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the same fluoroquinolone-class '''Boxed Warnings''' as ciprofloxacin/levofloxacin'"`UNIQ--ref-000014C5-QINU`"' (1) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the FDA '''Boxed Warning''' for '''complex sleep behaviors''' (sleep-driving, sleep-walking, sleep-eating, other parasomnias) added in 2019'"`UNIQ--ref-0000001C-QINU`"' (1)

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