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Medicines > routes : Subcutaneous or Sublingual or intravenous

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brand:
(none, never marketed) (1) · Aimovig (1) · Ajovy (1) · Ambien (IR), Ambien CR (biphasic-release), Edluar (sublingual), Intermezzo (low-dose sublingual for middle-of-night awakening), Zolpimist (oral spray) (1) · Ativan (oral, injectable), Loreev XR (1) · Emgality (1) · Humalog, Admelog, Lyumjev (1) · Humira; biosimilars Amjevita, Cyltezo, Hadlima, Hulio, Hyrimoz, Idacio, Yusimry, Abrilada (1) · Imitrex (oral, injectable, nasal), Tosymra (nasal spray), Onzetra Xsail (nasal powder), Zembrace SymTouch (low-dose autoinjector), Sumavel DosePro (needle-free SC) (1) · Keppra (IR), Keppra XR, Spritam (3D-printed orally disintegrating), Roweepra (1) · Levemir, Levemir FlexTouch (US discontinuation announced 2024) (1) · Many OTC and Rx; Nascobal (intranasal); generic injection (1) · Mobic, Vivlodex (lower-dose capsules), Anjeso (IV) (1) · MS Contin (ER), Kadian (ER), Avinza (ER), Roxanol (IR oral solution), Duramorph (epidural / IT), Astramorph (IV), Infumorph (intrathecal pump), MorphaBond (IR abuse-deterrent) (1) · Multiple OTC dietary supplement formulations (1) · Nitrostat, Nitrolingual, NitroMist, Nitro-Bid, Nitro-Dur, Minitran, Rectiv (1) · NovoLog, Fiasp (ultra-rapid), Trurapi (1) · Repatha (1) · Robaxin (oral, injectable) (1) · Trandate, Normodyne (discontinued in US) (1) · Trexall, Otrexup, Rasuvo, Xatmep, Rheumatrex (discontinued) (1) · Xylocaine (injectable, oral solution, topical), Lidoderm (patch), ZTLido (patch), Glydo (jelly), EMLA (with prilocaine, topical) (1)
classes:
[[:Category:Analgesics|Analgesic]] (3) · [[:Category:Insulins|Insulin]] (3) · Anti-CGRP ligand monoclonal antibody (2) · [[:Category:Biologics|Biologic]] (2) · [[:Category:DMARDs|DMARD]] (2) · [[:Category:Immunosuppressants|Immunosuppressant]] (2) · [[:Category:Mealtime_insulins|Mealtime (bolus) insulin]] (2) · [[:Category:Rapid-acting_insulins|Rapid-acting insulin analog]] (2) · [[:Category:Schedule IV controlled substances|Schedule IV controlled substance]] (2) · [[:Category:Sleep aids|Sleep aid]] (2)
mechanism:
None (14) · Humanized IgG2 monoclonal antibody binding both isoforms of CGRP peptide (1) · Humanized IgG2 monoclonal antibody binding the CGRP receptor (not the peptide); blocks CGRP-mediated vasodilation and nociceptive signaling (1) · Humanized IgG4 monoclonal antibody binding CGRP peptide; prevents CGRP from activating its receptor (1) · Positive allosteric modulator of the GABA<sub>A</sub> receptor at the benzodiazepine binding site; increases frequency of Cl<sup>−</sup> channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1) · '"`UNIQ--vote-00000015-QINU`"' The favorable pregnancy safety profile and the dual mechanism support its first-line role in pregnancy-associated hypertension and in hypertensive emergencies where rapid, controllable BP reduction is needed'"`UNIQ--ref-00000016-QINU`"'. (1) · '"`UNIQ--vote-00000019-QINU`"' Once-daily dosing is a clinical advantage over short-half-life NSAIDs'"`UNIQ--ref-0000001A-QINU`"'. (1) · '"`UNIQ--vote-00000584-QINU`"' Binds the same insulin receptor as endogenous insulin with comparable mitogenic-to-metabolic ratio. Ultra-rapid formulations (Lyumjev) add treprostinil and citrate to accelerate absorption further'"`UNIQ--ref-00000585-QINU`"'. (1) · '"`UNIQ--vote-000010F8-QINU`"' Pre-treatment screening for latent TB (PPD or IGRA) and chronic hepatitis B is standard. Anti-drug antibody formation is a recognized cause of secondary loss of response'"`UNIQ--ref-000010F9-QINU`"'. (1)
uses:
None (1) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · Preventive treatment of migraine in adults (episodic and chronic) (2) · Preventive treatment of migraine in adults; episodic cluster headache (1) · '"`UNIQ--vote-00000013-QINU`"', '"`UNIQ--vote-00000014-QINU`"' (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-00000586-QINU`"', '"`UNIQ--vote-00000587-QINU`"', '"`UNIQ--vote-00000588-QINU`"' (1) · '"`UNIQ--vote-000005EF-QINU`"', '"`UNIQ--vote-000005F0-QINU`"', '"`UNIQ--vote-000005F1-QINU`"' (1) · '"`UNIQ--vote-00000607-QINU`"', '"`UNIQ--vote-00000608-QINU`"', '"`UNIQ--vote-00000609-QINU`"', '"`UNIQ--vote-0000060A-QINU`"' (1) · '"`UNIQ--vote-000007C1-QINU`"', '"`UNIQ--vote-000007C2-QINU`"', '"`UNIQ--vote-000007C3-QINU`"', '"`UNIQ--vote-000007C4-QINU`"', '"`UNIQ--vote-000007C5-QINU`"', '"`UNIQ--vote-000007C6-QINU`"', '"`UNIQ--vote-000007C7-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-00001372-QINU`"', '"`UNIQ--vote-00001373-QINU`"' (1) · '"`UNIQ--vote-0000147C-QINU`"', '"`UNIQ--vote-0000147D-QINU`"', '"`UNIQ--vote-0000147E-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) · 140 mg SC every 2 weeks OR 420 mg SC monthly (3 consecutive injections 5 minutes apart due to volume) (1) · 225 mg SC monthly, or 675 mg SC every 3 months (quarterly) (1) · 40 mg SC every other week (most adult indications); IBD induction 160 mg week 0, 80 mg week 2, then 40 mg every other week (1) · 7.5 mg PO once daily; titrate to 15 mg daily if needed. Vivlodex 5 mg PO once daily, max 10 mg (1) · 70 mg SC monthly; may increase to 140 mg monthly (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) · 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) · Migraine: 240 mg SC loading dose, then 120 mg SC monthly. Cluster: 300 mg SC at onset of cluster period, then monthly during cluster. (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) · Oral: 50-100 mg at migraine onset, may repeat in 2 hours if needed. SC: 6 mg, may repeat in 1 hour. Nasal: 5-20 mg per nostril, may repeat in 2 hours (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) · Rheumatologic: 7.5-15 mg PO or SC '''once weekly''' (not daily — daily dosing is a recognized fatal error); folic acid 1 mg PO daily on non-MTX days; oncology dosing is far higher and indication-specific (1) · SC 4-6 units (or 1 unit per 10-15 g carbs) at meals; titrate to postprandial glucose (1) · SC 4-6 units (or 1 unit per 10-15 g carbs) at meals; titrate to postprandial glucose. Typical total daily dose 0.5-1 U/kg/d split between basal and prandial coverage in T1DM (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) · ~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)
preparations:
100 U/mL (Humalog, Admelog, Lyumjev) vials, pens, cartridges; 200 U/mL Humalog KwikPen (1) · 100 U/mL (NovoLog, Fiasp) vials, pens, cartridges (1) · 100 U/mL FlexTouch pen, vial (1) · 100, 250, 500, 1000, 5000 mcg tablets (OTC and Rx); 1000 mcg/mL injection; intranasal spray; sublingual (1) · 120 mg/mL prefilled syringe or autoinjector (1) · 140 mg/mL single-use prefilled syringe and SureClick autoinjector; Pushtronex 420 mg/3.5 mL on-body infusor (1) · 2.5 mg tablets; 10-50 mg/mL injection; pre-filled subcutaneous autoinjectors (Otrexup, Rasuvo); 2.5 mg/mL oral solution (Xatmep) (1) · 225 mg/1.5 mL prefilled syringe or autoinjector (1) · 40 mg/0.4 mL or 40 mg/0.8 mL prefilled syringe and autoinjector pen; 10, 20, 80 mg pediatric/induction strengths (1) · 70 mg/mL or 140 mg/mL prefilled autoinjector (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) · Oral tablets 25, 50, 100 mg; SC injection 4, 6 mg autoinjector; needle-free SC 6 mg (Sumavel); nasal spray 5, 20 mg; nasal powder 22 mg (Onzetra Xsail); low-dose autoinjector 3 mg (Zembrace SymTouch) (1) · OTC tablets, sublingual tablets, gummies, liquid, extended-release tablets and capsules; common strengths 0.5, 1, 3, 5, 10 mg (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:
60-70% PO at low doses; saturable at high doses (parenteral routes preferred above 15-25 mg/week)'"`UNIQ--ref-000007C9-QINU`"' (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) · Not formally characterized in humans. (1) · Not formally established (1) · Not formally established (high SC) (1) · Oral ~1-3% via passive diffusion at high doses (independent of intrinsic factor); IM/SC ~100% (1) · ~100% (oral)'"`UNIQ--ref-00000020-QINU`"' (1) · ~100% (oral; near-complete absorption)'"`UNIQ--ref-00000018-QINU`"' (1) · ~100% from subcutaneous depot (2) · ~14% (oral; substantial first-pass); ~97% (subcutaneous); ~17% (nasal)'"`UNIQ--ref-00000016-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) · ~60% from subcutaneous depot (reduced by reversible albumin binding via the myristic acid side chain that also extends duration)'"`UNIQ--ref-00001375-QINU`"' (1) · ~64% from SC depot'"`UNIQ--ref-00001104-QINU`"' (1) · ~70% (oral)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~72% from SC depot'"`UNIQ--ref-00001480-QINU`"' (1) · ~82% SC (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) · '''Contraindicated in pregnancy''' (Category X); abortifacient and teratogenic. Discontinuation 3-6 months before conception is standard.<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 (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) · 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) · Insulin is the preferred glucose-lowering therapy in pregnancy; aspart is widely used.<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; lispro is widely used.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data.<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.<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; pregnancy registry data have been broadly reassuring relative to baseline malformation rates.<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) · 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 (2) · OTC (low/mid-dose oral) and [[USLegal:Prescription only|Rx-only]] (injection, intranasal) in US (1) · Rx (3) · [[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 (8) · [[USLegal:Prescription only|Rx-only]] in US (some OTC formulations exist) (1) · [[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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