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Medicines > duration : 4-6 hours or ~12 weeks

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classes:
[[:Category:Fixed-dose_combinations|Fixed-dose combination]] (5) · [[:Category:Antiemetics|Antiemetic]] (3) · [[:Category:Non-opioid_analgesics|Non-opioid analgesic (acetaminophen)]] (3) · [[:Category:Antihistamines|First-generation antihistamine]] (2) · [[:Category:Antipyretics|Antipyretic]] (2) · [[:Category:Barbiturates|Barbiturate (butalbital)]] (2) · [[:Category:Bronchodilators|Bronchodilator]] (2) · [[:Category:Methylxanthines|Methylxanthine (caffeine)]] (2) · [[:Category:NSAIDs|NSAID (aspirin)]] (2) · [[:Category:Opioid_analgesics|Opioid analgesic]] (2) · [[:Category:Schedule_III_controlled_substances|Schedule III controlled substance]] (2) · [[:Category:Schedule_II_controlled_substances|Schedule II controlled substance]] (2)
mechanism:
None (11) · Cleaves SNAP-25 protein in presynaptic motor and autonomic nerve terminals, blocking acetylcholine release; in chronic migraine, hypothesized to inhibit peripheral sensitization of trigeminovascular nociceptors (1) · Prodrug to [[Psilocin|psilocin]] (4-hydroxy-N,N-dimethyltryptamine), a partial agonist at the [[Receptor:5-HT2A|5-HT2A]] serotonin receptor; the action that defines the classical-psychedelic mechanism (1) · '"`UNIQ--vote-0000001D-QINU`"' '''QT prolongation''' risk at high doses prompted the FDA's 2015 caution against use in patients with prolonged QT or with concurrent QT-prolonging medicines'"`UNIQ--ref-0000001E-QINU`"'. (1) · '"`UNIQ--vote-0000001D-QINU`"' Major Beers-list concern in elderly patients for cognitive and fall risks. CYP2D6 substrate. At massive overdose, also produces sodium channel blockade with cardiac toxicity'"`UNIQ--ref-0000001E-QINU`"'. '"`UNIQ--effect-0000001F-QINU`"' (1) · '"`UNIQ--vote-00000054-QINU`"' The clinical efficacy endpoint is adequate visualization at colonoscopy, scored by the Boston Bowel Preparation Scale'"`UNIQ--ref-00000055-QINU`"'. (1) · '"`UNIQ--vote-00000093-QINU`"' At higher doses β2 selectivity is lost, producing β1 effects (tachycardia, tremor) and hypokalemia from intracellular potassium shift'"`UNIQ--ref-00000094-QINU`"'. (1) · '"`UNIQ--vote-000014DD-QINU`"' The combination is the most-prescribed opioid analgesic in the US for moderate-to-severe acute pain. CPIC PGx guidance addresses CYP2D6-driven exposure variation'"`UNIQ--ref-000014DE-QINU`"'. (1) · '"`UNIQ--vote-000014F7-QINU`"' Falling out of favor for acute pain due to aspirin's GI bleeding and antiplatelet effects compared with acetaminophen-opioid combinations; still used in selected indications'"`UNIQ--ref-000014F8-QINU`"'. (1) · '"`UNIQ--vote-00001513-QINU`"' The combination with acetaminophen provides additive non-opioid analgesia and lowers required codeine dose. CYP2D6 PGx is one of the most clinically actionable in current pharmacology; CPIC supports genotype-guided opioid selection'"`UNIQ--ref-00001514-QINU`"'. (1)
uses:
(investigational) '"`UNIQ--vote-000000EF-QINU`"', '"`UNIQ--vote-000000F0-QINU`"', '"`UNIQ--vote-000000F1-QINU`"', '"`UNIQ--vote-000000F2-QINU`"', '"`UNIQ--vote-000000F3-QINU`"' (1) · Chronic migraine (≥15 headache days/month), cervical dystonia, blepharospasm, hyperhidrosis, overactive bladder, urinary incontinence, strabismus, spasticity, cosmetic problems (1) · '"`UNIQ--vote-00000015-QINU`"', '"`UNIQ--vote-00000016-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-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"' (1) · '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"' (2) · '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"' (1) · '"`UNIQ--vote-00000056-QINU`"', '"`UNIQ--vote-00000057-QINU`"' (1) · '"`UNIQ--vote-00000095-QINU`"', '"`UNIQ--vote-00000096-QINU`"', '"`UNIQ--vote-00000097-QINU`"', '"`UNIQ--vote-00000098-QINU`"' (1) · '"`UNIQ--vote-000006A2-QINU`"', '"`UNIQ--vote-000006A3-QINU`"', '"`UNIQ--vote-000006A4-QINU`"' (1) · '"`UNIQ--vote-00000DDF-QINU`"', '"`UNIQ--vote-00000DE0-QINU`"', '"`UNIQ--vote-00000DE1-QINU`"', '"`UNIQ--vote-00000DE2-QINU`"' (1) · '"`UNIQ--vote-00000EF4-QINU`"', '"`UNIQ--vote-00000EF5-QINU`"', '"`UNIQ--vote-00000EF6-QINU`"', '"`UNIQ--vote-00000EF7-QINU`"', '"`UNIQ--vote-00000EF8-QINU`"' (1) · '"`UNIQ--vote-00000F78-QINU`"', '"`UNIQ--vote-00000F79-QINU`"', '"`UNIQ--vote-00000F7A-QINU`"' (1) · '"`UNIQ--vote-000014DF-QINU`"', '"`UNIQ--vote-000014E0-QINU`"', '"`UNIQ--vote-000014E1-QINU`"' (1) · '"`UNIQ--vote-000014F9-QINU`"' (1) · '"`UNIQ--vote-00001515-QINU`"', '"`UNIQ--vote-00001516-QINU`"' (1) · '"`UNIQ--vote-0000152F-QINU`"' (1) · '"`UNIQ--vote-0000159D-QINU`"', '"`UNIQ--vote-0000159E-QINU`"' (1) · '"`UNIQ--vote-000015B6-QINU`"' (1)
starting dose:
0.5-1 mg PO/IV once or twice daily; titrate to clinical response. Approximate equipotency: bumetanide 1 mg ≈ furosemide 40 mg ≈ torsemide 20 mg (1) · 1 tablet (4.8355 mg oxycodone / 325 mg aspirin) PO every 6 hours as needed (1) · 1-2 capsules (50 mg butalbital / 325 mg acetaminophen / 40 mg caffeine each) PO every 4 hours as needed; maximum 6 capsules/d (1) · 1-2 capsules (50 mg butalbital / 325 mg aspirin / 40 mg caffeine each) PO every 4 hours as needed; maximum 6 capsules/d (1) · 1-2 tablets (15-60 mg codeine, 300-600 mg acetaminophen) PO every 4-6 hours as needed (1) · 10 mg PO/IV/IM QID, '''not to exceed 12 weeks''' (tardive dyskinesia risk); intranasal Gimoti 15 mg BID (1) · 2 tablets (75 mg tramadol / 650 mg acetaminophen) PO every 4-6 hours as needed; maximum 8 tablets/day for ≤5 days (1) · 200-400 mg PO every 4-6 hours as needed. OTC max 1200 mg/day without provider direction; prescription max 3200 mg/day divided (1) · 325-1000 mg PO every 4-6 hours as needed; maximum 4 g/d in healthy adults, 3 g/d in regular users or hepatic risk; pediatric 10-15 mg/kg every 4-6 hours (1) · 4 L oral solution (GoLYTELY-class) split-dose: 2 L evening before, 2 L morning of procedure; low-volume products (MoviPrep, Plenvu) use 1-2 L with required clear-fluid intake (1) · 5 mg / 325 mg PO every 4-6 hours as needed; total acetaminophen <3 g/d (1) · Allergy: 25 mg PO BID-QID. Nausea/vomiting: 12.5-25 mg PO/IM/IV/PR every 4-6 hours. Motion sickness: 25 mg PO 30-60 minutes before travel. '''Pediatric <2 years: contraindicated''' (1) · Allergy: 25-50 mg PO every 4-6 hours. Insomnia: 25-50 mg PO at bedtime. IV (acute dystonia, severe allergic reaction): 25-50 mg slow IV push (1) · Anxiety: 25-50 mg PO QID. Pruritus: 25 mg PO TID-QID. Insomnia: 25-50 mg PO at bedtime. Pediatric: 50-100 mg/day divided (1) · Chronic migraine (PREEMPT protocol): 155 units divided across 31 sites in 7 head/neck muscle groups every 12 weeks (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) · MDI 90 mcg/puff, 2 puffs q4-6h prn; nebulized 2.5 mg in 3 mL saline q4-6h (1) · Modern clinical-trial standard: 25 mg synthesized psilocybin, single oral dose with psychological support (1) · Nebulized 500 mcg q6-8h (or with albuterol as DuoNeb); MDI 17 mcg/puff, 2 puffs QID; nasal 0.03% or 0.06% spray BID-TID (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)
preparations:
0.5, 1, 2 mg tablets; 0.25 mg/mL IV (1) · 325, 500, 650 mg tablets; 80, 160 mg chewables; 160 mg/5 mL pediatric liquid; 325 mg suppository; 1000 mg/100 mL IV (Ofirmev); fixed-dose combinations with opioids, decongestants, antihistamines (1) · 4.8355 mg oxycodone / 325 mg aspirin tablets (1) · 5, 10 mg tablets; 5 mg/5 mL solution; 5 mg/mL IV; 15 mg/spray intranasal (1) · 50, 100, or 200 unit vials of lyophilized powder for reconstitution (1) · 50/325/40 mg capsules (1) · 50/325/40 mg capsules and tablets; oral solution (1) · Atrovent HFA 17 mcg/actuation MDI; 500 mcg/2.5 mL nebulizer solution; 0.03% and 0.06% intranasal sprays; with albuterol as DuoNeb / Combivent Respimat (1) · Codeine/acetaminophen 15/300 (#2 historical), 30/300 (#3), 60/300 (#4) mg tablets; 12/120 mg/5 mL elixir (1) · MDI 90 mcg/puff; nebulizer solution 0.083% (2.5 mg/3 mL), 0.5%, 0.021%, 0.042%; syrup 2 mg/5 mL; 2 mg, 4 mg tablets; 4 mg, 8 mg ER (1) · Oxycodone/acetaminophen 2.5/325, 5/325, 7.5/325, 10/325 mg tablets; 5/325 mg/5 mL solution (1) · Powder for oral solution in 4 L jugs (PEG 3350 ~236 g + NaCl, NaHCO3, KCl, Na2SO4) and low-volume packets (1) · Synthesized psilocybin capsules (COMP360 and other investigational formulations); dried whole [[Psilocybe|Psilocybe]] mushrooms (variable potency, no legal supply chain in most jurisdictions); psilocybin truffles (Psilocybe sclerotia, legal in the Netherlands) (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 10, 25, 50 mg (HCl); capsules 25, 50, 100 mg (pamoate); oral suspension 25 mg/5 mL; injection 25, 50 mg/mL (IM only, never IV) (1) · Tablets 12.5, 25, 50 mg; oral syrup 6.25 mg/5 mL; suppositories 12.5, 25, 50 mg; injection 25 mg/mL and 50 mg/mL (1) · Tablets 200, 400, 600, 800 mg; capsules 200 mg; oral suspension 100 mg/5 mL; chewable tablets 100 mg; injection 100 mg/mL (Caldolor) (1) · Tablets 25, 50 mg; capsules; liquid; chewable; topical cream/gel; injection 50 mg/mL (1) · Tablets 500, 750 mg; injection 100 mg/mL (1) · Tramadol/acetaminophen 37.5/325 mg tablets (1)
duration: (Click arrow to add another value)
halflife:
1-1.5 hours'"`UNIQ--ref-00000DE3-QINU`"' (1) · 1-2 hours'"`UNIQ--ref-00000017-QINU`"' (1) · 1-3 hours (normal liver); markedly prolonged in overdose with glutathione depletion'"`UNIQ--ref-000006A5-QINU`"' (1) · 12-15 hours'"`UNIQ--ref-00000022-QINU`"' (1) · 14-25 hours (longer in elderly and hepatic impairment)'"`UNIQ--ref-00000026-QINU`"' (1) · 2-4 hours'"`UNIQ--ref-00000026-QINU`"' (1) · 4-6 hours (inhaled and PO)'"`UNIQ--ref-00000099-QINU`"' (1) · 4-8 hours (longer in elderly, 9-13 hours)'"`UNIQ--ref-00000026-QINU`"' (1) · 5-6 hours'"`UNIQ--ref-00000020-QINU`"' (1) · 5-6 hours'"`UNIQ--ref-00000EF9-QINU`"' (1) · Butalbital ~35 hours (long; cumulative effects with frequent use); acetaminophen 1-3 hours; caffeine 3-7 hours'"`UNIQ--ref-0000159F-QINU`"' (1) · Butalbital ~35 hours; aspirin (acetyl group) ~15 minutes, salicylate 2-3 hours; caffeine 3-7 hours'"`UNIQ--ref-000015B7-QINU`"' (1) · Codeine 2.5-3.5 hours; acetaminophen 1-3 hours'"`UNIQ--ref-00001517-QINU`"' (1) · Not absorbed (1) · Oxycodone 3-5 hours; acetaminophen 1-3 hours'"`UNIQ--ref-000014E2-QINU`"' (1) · Oxycodone 3-5 hours; aspirin (acetyl group) 15-20 minutes, salicylate 2-3 hours at therapeutic doses'"`UNIQ--ref-000014FA-QINU`"' (1) · Psilocin: ~2-3 h; psilocybin itself is a prodrug, dephosphorylated within minutes of absorption (1) · Tissue half-life not formally measured; clinical effect ~12 weeks (1) · Tramadol ~5-7 hours (M1 metabolite ~9 hours); acetaminophen 1-3 hours'"`UNIQ--ref-00001530-QINU`"' (1) · ~2 hours (plasma; minimal relevance — local-action drug)'"`UNIQ--ref-00000F7B-QINU`"' (1)
bioavailability:
Butalbital well-absorbed; aspirin 50-75%; caffeine ~100%'"`UNIQ--ref-000015B8-QINU`"' (1) · Butalbital well-absorbed; caffeine ~100%; acetaminophen 85-98%'"`UNIQ--ref-000015A0-QINU`"' (1) · Codeine ~60% (oral); acetaminophen 85-98%'"`UNIQ--ref-00001518-QINU`"' (1) · Inhaled lung deposition with minimal systemic absorption (the basis of the favorable safety profile vs systemic antimuscarinics)'"`UNIQ--ref-00000F7C-QINU`"' (1) · Local (intramuscular) (1) · Negligible (not absorbed)'"`UNIQ--ref-00000058-QINU`"' (1) · Oral bioavailability of psilocin from administered psilocybin approximately 50% (1) · Oxycodone 60-87%; aspirin 50-75%'"`UNIQ--ref-000014FB-QINU`"' (1) · Tramadol ~75% (oral); acetaminophen 85-98%'"`UNIQ--ref-00001531-QINU`"' (1) · ~10% inhaled reaches systemic circulation; ~50% PO'"`UNIQ--ref-0000009A-QINU`"' (1) · ~100% (oral, but oral use is limited to continuation from parenteral)'"`UNIQ--ref-00000021-QINU`"' (1) · ~100% (oral; near-complete absorption)'"`UNIQ--ref-00000018-QINU`"' (1) · ~25% (oral, with extensive first-pass)'"`UNIQ--ref-00000023-QINU`"' (1) · ~40-60% (oral, with significant first-pass)'"`UNIQ--ref-00000027-QINU`"' (1) · ~60-87% oxycodone (high and predictable, less CYP-genotype-dependent than codeine or hydrocodone); 85-98% acetaminophen'"`UNIQ--ref-000014E3-QINU`"' (1) · ~80% (oral)'"`UNIQ--ref-00000027-QINU`"' (1) · ~80% (oral; reduced by significant first-pass)'"`UNIQ--ref-00000EFA-QINU`"' (1) · ~80-100% (oral)'"`UNIQ--ref-00000027-QINU`"' (1) · ~80-95% (oral; more reliable than furosemide, comparable to torsemide)'"`UNIQ--ref-00000DE4-QINU`"' (1) · ~85-98% (oral)'"`UNIQ--ref-000006A6-QINU`"' (1)
pregnancy:
None (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-00000028-QINU`"' (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 where possible; class concerns as for other loop diuretics.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Avoid; aspirin teratogenicity concerns plus opioid neonatal withdrawal.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Avoid; neonatal opioid withdrawal documented.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Avoided; barbiturate + aspirin teratogenicity and bleeding concerns.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Category C; limited data (1) · Generally avoided; barbiturate exposure in late pregnancy can produce neonatal withdrawal and respiratory depression.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; generally considered acceptable when needed.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (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; older agent with substantial use experience; some signal for first-trimester exposure but not conclusive.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited use in pregnancy; chronic third-trimester opioid 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) · Long the preferred analgesic-antipyretic in pregnancy; recent observational studies have raised speculative neurodevelopmental signals that remain under investigation.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Not absorbed; generally considered acceptable when bowel prep is required<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Not studied in human pregnancy; no approved clinical use in any population (1) · Older agent with substantial use experience, including in hyperemesis gravidarum; broadly reassuring observational data'"`UNIQ--ref-00000024-QINU`"' (1) · Older agent with substantial use experience; broadly considered safe in pregnancy'"`UNIQ--ref-00000028-QINU`"' (1) · Preferred SABA in pregnancy; benefits of asthma control outweigh limited risks.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Widely used for hyperemesis gravidarum; reassuring data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (3) · OTC and [[USLegal:Prescription only|Rx-only]] (IV, combination products) in US (1) · Rx; black-box warning for distant spread of toxin effect (1) · [[USLegal:Over-the-counter|OTC]] for most oral and topical formulations; [[USLegal:Prescription only|Rx-only]] for injectable (1) · [[USLegal:Over-the-counter|OTC]] in the US at ≤200 mg per tablet / ≤1200 mg/day; [[USLegal:Prescription only|Rx-only]] at higher strengths and indications (1) · [[USLegal:Prescription only|Rx-only]] in US (4) · [[USLegal:Prescription only|Rx-only]] in US (most products; some low-volume packs OTC) (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries a '''Boxed Warning''' for '''tardive dyskinesia''' (irreversible movement disorder), driving the 12-week chronic-use limit'"`UNIQ--ref-00000EFB-QINU`"' (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, which is a meaningful clinical advantage over the benzodiazepine alternatives for short-term anxiety'"`UNIQ--ref-00000028-QINU`"' (1) · [[USLegal:Schedule III|Schedule III controlled substance]] in US (Fiorinal is scheduled federally; Fioricet with acetaminophen is unscheduled federally despite identical butalbital content, a regulatory quirk) (1) · [[USLegal:Schedule III|Schedule III controlled substance]] in US. '''Contraindicated in children <12''' for any indication and in any age post-tonsillectomy/adenoidectomy (FDA 2017 black-box advisory)'"`UNIQ--ref-00001519-QINU`"' (1) · [[USLegal:Schedule II|Schedule II controlled substance]] in US (1) · [[USLegal:Schedule II|Schedule II controlled substance]] in US. Acetaminophen content limited to ≤325 mg per dosage unit (FDA 2014) (1) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US (tramadol was reclassified from non-controlled to Schedule IV in 2014 after recognition of dependence risk) (1)

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