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Medicines > routes : Sublingual or intravenous or thigh

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classes:
Designer benzodiazepine (1) · preferential COX-2)]] (1) · Research material (1) · Sedative-Hypnotic (1) · Triazolobenzodiazepine (1) · [[:Category:Analgesics|Analgesic]] (2) · [[:Category:Anesthetics|Anesthetic]] (1) · [[:Category:Antianginals|Antianginal]] (1) · [[:Category:Antiarrhythmics|Antiarrhythmic (Vaughan Williams Class IB)]] (1) · [[:Category:Anticonvulsants|Anticonvulsant]] (1) · [[:Category:Antihypertensives|Antihypertensive]] (1) · [[:Category:Anxiolytics|Anxiolytic]] (1) · [[:Category:B-vitamins|B-vitamin]] (1) · [[:Category:Benzodiazepines|Benzodiazepine]] (1) · [[:Category:Beta blockers|Combined alpha-1 and non-selective beta blocker]] (1) · [[:Category:Chronobiotics|Chronobiotic (circadian phase regulator)]] (1) · [[:Category:Hematinics|Hematinic]] (1) · [[:Category:Local anesthetics|Local anesthetic (amide class)]] (1) · [[:Category:Melatonin receptor agonists|Melatonin receptor agonist]] (1) · [[:Category:Nitrates|Organic nitrate]] (1) · [[:Category:Non-benzodiazepine hypnotics|Non-benzodiazepine hypnotic]] (1) · [[:Category:NSAIDs|Non-steroidal anti-inflammatory (NSAID (1) · [[:Category:Opioid analgesics|Opioid analgesic (natural phenanthrene from opium poppy)]] (1) · [[:Category:Schedule II controlled substances|Schedule II controlled substance]] (1) · [[:Category:Schedule IV controlled substances|Schedule IV controlled substance]] (2) · [[:Category:Skeletal muscle relaxants|Skeletal muscle relaxant (centrally-acting)]] (1) · [[:Category:Sleep aids|Sleep aid]] (2) · [[:Category:SV2A ligands|Synaptic vesicle protein 2A (SV2A) ligand]] (1) · [[: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-00000015-QINU`"', '"`UNIQ--vote-00000016-QINU`"' (1) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"' (2) · '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"' (1) · '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (3) · '"`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-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-00000607-QINU`"', '"`UNIQ--vote-00000608-QINU`"', '"`UNIQ--vote-00000609-QINU`"', '"`UNIQ--vote-0000060A-QINU`"' (1) · '"`UNIQ--vote-00000C0A-QINU`"', '"`UNIQ--vote-00000C0B-QINU`"', '"`UNIQ--vote-00000C0C-QINU`"', '"`UNIQ--vote-00000C0D-QINU`"', '"`UNIQ--vote-00000C0E-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) · 7.5 mg PO once daily; titrate to 15 mg daily if needed. Vivlodex 5 mg PO once daily, max 10 mg (1) · Adult: 500 mg PO BID, titrate by 1000 mg/day every 2 weeks. Pediatric: 10-20 mg/kg/day divided BID, weight-titrated (1) · Anxiety: 0.5-1 mg PO BID-TID. Insomnia: 1-2 mg PO at bedtime. Status epilepticus: 4 mg IV (adult), repeat after 5-10 minutes if needed. Acute agitation: 1-2 mg IM (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) · Infiltration: 1-2% solution; '''4.5 mg/kg ceiling without epinephrine, 7 mg/kg with epinephrine'''. IV antiarrhythmic: 1-1.5 mg/kg bolus then infusion 1-4 mg/minute. Lidoderm patch: up to 3 patches per 12 hours (1) · IR oral: 15-30 mg every 4 hours as needed. ER opioid-naive: 15-30 mg every 12 hours. IV/IM/SC: 2-10 mg every 3-4 hours. Epidural / intrathecal: see surgical or palliative-care protocols (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Oral: 100 mg PO BID, titrate to 400 mg BID. IV: 20 mg over 2 minutes, repeat 40-80 mg every 10 minutes as needed (maximum cumulative 300 mg); continuous infusion 2 mg/minute (1) · Oral: 1500 mg PO QID for 2-3 days (load), then 750-1500 mg QID maintenance. IV/IM: 1000 mg every 8 hours for acute spasm (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) · 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) · 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)
preparations:
100, 250, 500, 1000, 5000 mcg tablets (OTC and Rx); 1000 mcg/mL injection; intranasal spray; sublingual (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) · Injection 0.5-4% solutions (with and without epinephrine); topical cream 4-5%; transdermal patch 5% (Lidoderm), 1.8% (ZTLido); oral 2% viscous solution; jelly 2%; ophthalmic (1) · IR tablets 15, 30 mg; oral solution 10 mg/5 mL, 20 mg/mL, 100 mg/5 mL (concentrated); suppositories; ER tablets and capsules in multiple strengths; injectable 0.5-50 mg/mL (1) · IR tablets 250, 500, 750, 1000 mg; XR tablets 500, 750 mg; oral solution 100 mg/mL; injection 100 mg/mL; Spritam ODT 250, 500, 750, 1000 mg (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) · 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) · 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 0.5, 1, 2 mg; oral concentrate 2 mg/mL; injection 2 mg/mL and 4 mg/mL; Loreev XR capsules 1, 2, 3 mg (1) · Tablets 100, 200, 300 mg; injection 5 mg/mL (1) · Tablets 500, 750 mg; injection 100 mg/mL (1) · Tablets 7.5, 15 mg (Mobic); capsules 5, 10 mg (Vivlodex); oral suspension 7.5 mg/5 mL; injection 30 mg/mL (Anjeso) (1)
routes: (Click arrow to add another value)
bioavailability:
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) · Not formally characterized in humans. (1) · Oral ~1-3% via passive diffusion at high doses (independent of intrinsic factor); IM/SC ~100% (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)'"`UNIQ--ref-00000020-QINU`"' (1) · ~100% (oral; near-complete absorption)'"`UNIQ--ref-00000018-QINU`"' (1) · ~15% (oral; highly variable due to extensive and variable first-pass metabolism)'"`UNIQ--ref-00000022-QINU`"' (1) · ~25% (oral; extensive first-pass)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~25-40% (oral; extensive first-pass)'"`UNIQ--ref-00000021-QINU`"' (1) · ~35% (oral, extensive first-pass; not used orally for systemic effect); ~100% (IV)'"`UNIQ--ref-00000021-QINU`"' (1) · ~70% (oral)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~89% (oral)'"`UNIQ--ref-00000021-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00000024-QINU`"' (1)
pregnancy:
None (1) · '''Among the safest antihypertensives in pregnancy''', recommended for chronic hypertension during pregnancy and first-line for severe hypertension in preeclampsia and eclampsia'"`UNIQ--ref-0000001C-QINU`"' (1) · '''Considered one of the safest anticonvulsants in pregnancy''', with reassuring monotherapy registry data comparable to lamotrigine and in sharp contrast to valproate, topiramate, and carbamazepine'"`UNIQ--ref-00000021-QINU`"' (1) · Avoid from 20 weeks gestation onward per FDA's 2020 expanded NSAID warning (fetal renal dysfunction, oligohydramnios); contraindicated from 30 weeks (risk of premature ductus arteriosus closure)'"`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) · Chronic third-trimester exposure produces neonatal opioid withdrawal syndrome and respiratory depression at delivery.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Extensive use experience in obstetric anesthesia; broadly considered safe'"`UNIQ--ref-00000022-QINU`"' (1) · Limited human data.<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) · 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) · Some signal for cleft lip/palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.<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)
legal:
None (1) · OTC (low/mid-dose oral) and [[USLegal:Prescription only|Rx-only]] (injection, intranasal) 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 most formulations; some low-concentration topical formulations are [[USLegal:Over-the-counter|OTC]] (4% cream) (1) · [[USLegal:Prescription only|Rx-only]] in US (3) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, distinguishing it from carisoprodol which is Schedule IV'"`UNIQ--ref-00000019-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance'"`UNIQ--ref-00000022-QINU`"' (1) · [[USLegal:Schedule II|Schedule II controlled substance]] in US; WHO essential medicine'"`UNIQ--ref-00000022-QINU`"' (1) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the benzodiazepine class '''Boxed Warning''' for risk of fatal respiratory depression, coma, and death when combined with opioids'"`UNIQ--ref-00000025-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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