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Medicines > onset : 1-2 hours or 30-60 minutes or ~1 hour

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classes:
None (1) · gut-restricted)]] (1) · selective COX-2)]] (1) · weak)]] (1) · [[:Category:Alpha-2 adrenergic agonists|Alpha-2 adrenergic agonist]] (1) · [[:Category:Analgesics|Analgesic]] (2) · [[:Category:Antidiarrheals|Antidiarrheal]] (1) · [[:Category:Antiemetics|Antiemetic]] (1) · [[:Category:Antihistamines|Antihistamine]] (3) · [[:Category:Antihistamines|First-generation antihistamine (piperazine)]] (1) · [[:Category:Antihistamines|First-generation antihistamine]] (1) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (1) · [[:Category:Antipyretics|Antipyretic]] (1) · [[:Category:Antispastics|Antispastic]] (1) · [[:Category:Antivertigo medicines|Antivertigo medicine]] (1) · [[:Category:Barbiturates|Barbiturate (butalbital)]] (2) · [[:Category:Basal_insulins|Basal insulin]] (3) · [[:Category:Decongestants|Decongestant]] (1) · [[:Category:Fixed-dose_combinations|Fixed-dose combination]] (3) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist (second-generation)]] (3) · [[:Category:Insulins|Insulin]] (3) · [[:Category:Insulin_secretagogues|Insulin secretagogue]] (1) · [[:Category:Long-acting_insulins|Long-acting insulin analog]] (2) · [[:Category:Methylxanthines|Methylxanthine (caffeine)]] (2) · [[:Category:Non-opioid_analgesics|Non-opioid analgesic (acetaminophen)]] (2) · [[:Category:NSAIDs|Non-steroidal anti-inflammatory (NSAID (1) · [[:Category:NSAIDs|Non-steroidal anti-inflammatory (NSAID)]] (1) · [[:Category:NSAIDs|NSAID (aspirin)]] (1) · [[:Category:Opioid_analgesics|Opioid analgesic (codeine (1) · [[:Category:Opioid_receptor_agonists|Peripheral opioid receptor agonist (μ-selective (1) · [[:Category:Orexigenics|Appetite-promoting medicine (orexigenic)]] (1) · [[:Category:Schedule_III_controlled_substances|Schedule III controlled substance]] (2) · [[:Category:Serotonin antagonists|Serotonin 5-HT2 antagonist]] (1) · [[:Category:Skeletal muscle relaxants|Skeletal muscle relaxant (centrally-acting)]] (2) · [[:Category:Sulfonylureas|Sulfonylurea (third-generation)]] (1) · [[:Category:Sympathomimetics|Sympathomimetic (indirect-acting)]] (1) · [[:Category:Tricyclic-related compounds|Tricyclic-related compound]] (1) · [[:Category:Ultra-long-acting_insulins|Ultra-long-acting insulin analog]] (1)
mechanism:
None (11) · '"`UNIQ--vote-00000013-QINU`"' Anticholinergic burden (dry mouth, blurred vision, urinary retention, cognitive effects) is the principal adverse-event concern and the basis for Beers-list cautions in elderly patients'"`UNIQ--ref-00000014-QINU`"'. (1) · '"`UNIQ--vote-00000017-QINU`"' Anticholinergic and sedating, with the standard first-generation antihistamine Beers-list concerns in elderly patients'"`UNIQ--ref-00000018-QINU`"'. (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-00000391-QINU`"' Minimal CYP metabolism; mostly renally cleared unchanged. Cetirizine is the active racemate; levocetirizine is the active R-enantiomer marketed separately'"`UNIQ--ref-00000392-QINU`"'. (1) · '"`UNIQ--vote-00000950-QINU`"' Mostly renally cleared unchanged; dose-reduce in renal impairment. Like cetirizine, retains slightly more sedation than fexofenadine in some users'"`UNIQ--ref-00000951-QINU`"'. (1) · '"`UNIQ--vote-00000CC9-QINU`"' Mostly excreted unchanged in feces and urine; P-glycoprotein substrate (the basis of the fruit-juice interaction). (1) · '"`UNIQ--vote-00001356-QINU`"' Binds the same insulin receptor as endogenous insulin with comparable mitogenic-to-metabolic ratio'"`UNIQ--ref-00001357-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:
'"`UNIQ--vote-00000015-QINU`"', '"`UNIQ--vote-00000016-QINU`"', '"`UNIQ--vote-00000017-QINU`"' (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-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"', '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"' (1) · '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"', '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"' (1) · '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"', '"`UNIQ--vote-00000026-QINU`"', '"`UNIQ--vote-00000027-QINU`"', '"`UNIQ--vote-00000028-QINU`"' (2) · '"`UNIQ--vote-00000239-QINU`"', '"`UNIQ--vote-0000023A-QINU`"' (1) · '"`UNIQ--vote-00000393-QINU`"', '"`UNIQ--vote-00000394-QINU`"', '"`UNIQ--vote-00000395-QINU`"' (1) · '"`UNIQ--vote-00000491-QINU`"' (1) · '"`UNIQ--vote-00000952-QINU`"', '"`UNIQ--vote-00000953-QINU`"' (1) · '"`UNIQ--vote-00000CCA-QINU`"', '"`UNIQ--vote-00000CCB-QINU`"' (1) · '"`UNIQ--vote-00000FCF-QINU`"', '"`UNIQ--vote-00000FD0-QINU`"', '"`UNIQ--vote-00000FD1-QINU`"' (1) · '"`UNIQ--vote-00001358-QINU`"', '"`UNIQ--vote-00001359-QINU`"' (1) · '"`UNIQ--vote-00001372-QINU`"', '"`UNIQ--vote-00001373-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:
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 mg PO once daily with breakfast; titrate by glycemic response (1) · 1-2 tablets (15-60 mg codeine, 300-600 mg acetaminophen) PO every 4-6 hours as needed (1) · 10 mg PO once daily (5 mg in older adults or if sedation occurs) (1) · 2 mg PO every 6-8 hours; titrate by 2-4 mg per dose every 1-4 days; maximum single dose 16 mg, maximum daily dose 36 mg (1) · 2 tablets (75 mg tramadol / 650 mg acetaminophen) PO every 4-6 hours as needed; maximum 8 tablets/day for ≤5 days (1) · 4 mg PO initially, then 2 mg after each loose stool, '''not to exceed 16 mg/d''' (8 mg OTC); chronic-use lower (1) · 5 mg PO once daily in the evening (1) · 60 mg PO BID or 180 mg PO once daily (1) · Allergy: 4 mg PO TID. Serotonin syndrome: 12 mg loading dose PO or by nasogastric tube, then 2 mg every 2 hours until clinical improvement. Appetite stimulation: 2-4 mg PO TID-QID (1) · IR 5 mg PO TID; titrate to 10 mg TID if needed. Amrix ER 15 mg PO once daily. Off-label insomnia / fibromyalgia: 5-10 mg PO at bedtime (1) · IR: 60 mg PO every 4-6 hours. 12-hour ER: 120 mg PO every 12 hours. 24-hour ER: 240 mg PO once daily. Pediatric: weight-based (1) · Motion sickness: 25-50 mg PO 1 hour before travel, repeat every 24 hours as needed. Vertigo: 25-100 mg/day divided (1) · Osteoarthritis: 200 mg PO once daily or 100 mg BID. Rheumatoid arthritis: 100-200 mg PO BID. Acute pain: 400 mg loading, then 200 mg every 12 hours (1) · OTC: 220 mg PO every 8-12 hours, max 660 mg/24h. Rx: 250-500 mg PO BID. Acute gout: 750 mg loading then 250 mg every 8 hours (1) · ~10 units SC at the same time daily, or 0.1-0.2 units/kg/d; titrate by fasting glucose (2) · ~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:
1 mg, 2 mg, 4 mg tablets (1) · 100 U/mL (FlexTouch pen) and 200 U/mL (FlexTouch pen, higher-dose convenience) (1) · 100 U/mL (Lantus, Basaglar, Semglee) vials and pens; 300 U/mL (Toujeo) pens (1) · 100 U/mL FlexTouch pen, vial (1) · 2 mg capsules and tablets; 1 mg/5 mL oral solution; combined with simethicone (Imodium Multi-Symptom) (1) · 30, 60, 180 mg tablets; 30 mg ODT; 6 mg/mL oral suspension; all OTC (1) · 5 mg tablets; 2.5 mg/5 mL oral solution; OTC (1) · 5 mg, 10 mg tablets; 5 mg, 10 mg chewables; 1 mg/mL oral syrup; OTC (1) · 50/325/40 mg capsules (1) · 50/325/40 mg capsules and tablets; oral solution (1) · Capsules 50, 100, 200, 400 mg; Elyxyb oral solution 25 mg/mL (1) · Codeine/acetaminophen 15/300 (#2 historical), 30/300 (#3), 60/300 (#4) mg tablets; 12/120 mg/5 mL elixir (1) · IR tablets 30, 60 mg; 12-hour ER tablets 120 mg; 24-hour ER tablets 240 mg; oral liquid; multiple combination products with antihistamines, NSAIDs, or expectorants (1) · IR tablets 5, 7.5, 10 mg; Amrix ER capsules 15, 30 mg (1) · OTC tablets 220 mg; Rx tablets 250, 375, 500 mg; ER tablets 375, 500, 750 mg (Naprelan); oral suspension 125 mg/5 mL; enteric-coated tablets (EC-Naprosyn) (1) · Tablets 12.5, 25 mg; chewable tablets 25 mg (1) · Tablets 2, 4 mg; capsules 2, 4, 6 mg ('''capsules and tablets are not bioequivalent''': capsules slower with food; tablets faster on empty stomach) (1) · Tablets 4 mg; oral syrup 2 mg/5 mL (1) · Tramadol/acetaminophen 37.5/325 mg tablets (1)
onset: (Click arrow to add another value)
halflife:
12-17 hours'"`UNIQ--ref-00000029-QINU`"' (1) · 18 hours (IR); 32-33 hours (ER)'"`UNIQ--ref-0000001A-QINU`"' (1) · 2.5 hours (short, requires TID-QID dosing)'"`UNIQ--ref-0000001D-QINU`"' (1) · 8-10 hours (longer in elderly and renal impairment)'"`UNIQ--ref-00000396-QINU`"' (1) · 8-16 hours'"`UNIQ--ref-0000001E-QINU`"' (1) · 9-16 hours (pH-dependent: acidic urine shortens, alkaline urine substantially extends)'"`UNIQ--ref-0000001B-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) · Tramadol ~5-7 hours (M1 metabolite ~9 hours); acetaminophen 1-3 hours'"`UNIQ--ref-00001530-QINU`"' (1) · ~11 hours'"`UNIQ--ref-00000029-QINU`"' (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) · ~25 hours apparent (functional duration well over 42 hours from multi-hexamer depot)'"`UNIQ--ref-0000135A-QINU`"' (1) · ~5-9 hours (parent and active metabolites combined)'"`UNIQ--ref-00000492-QINU`"' (1) · ~6 hours'"`UNIQ--ref-00000018-QINU`"' (1) · ~7 hours apparent'"`UNIQ--ref-00001374-QINU`"' (1) · ~8 hours (longer in elderly and renal impairment)'"`UNIQ--ref-00000954-QINU`"' (1) · ~9-14 hours'"`UNIQ--ref-00000FD2-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) · High (oral); not significantly affected by food'"`UNIQ--ref-00000397-QINU`"' (1) · Tramadol ~75% (oral); acetaminophen 85-98%'"`UNIQ--ref-00001531-QINU`"' (1) · ~0.3% (oral; extensive first-pass via CYP3A4 and P-glycoprotein-mediated efflux at the intestinal and blood-brain barriers limit systemic and CNS exposure at therapeutic doses)'"`UNIQ--ref-00000FD3-QINU`"' (1) · ~100% (oral; not significantly affected by food)'"`UNIQ--ref-00000493-QINU`"' (1) · ~100% from subcutaneous depot (1) · ~100% from subcutaneous depot (by definition of the route) (1) · ~25% (oral)'"`UNIQ--ref-00000019-QINU`"' (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) · ~33-55% (IR); reduced by food'"`UNIQ--ref-0000001B-QINU`"' (1) · ~40% (oral); food and formulation substantially alter the absorption profile'"`UNIQ--ref-0000001E-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) · ~85-90% (oral; not significantly affected by food)'"`UNIQ--ref-00000955-QINU`"' (1) · ~90% (oral, low first-pass)'"`UNIQ--ref-0000001C-QINU`"' (1) · ~95% (oral)'"`UNIQ--ref-0000001F-QINU`"' (1) · ~95% (oral)'"`UNIQ--ref-0000002A-QINU`"' (1) · ~99% (oral)'"`UNIQ--ref-0000002A-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-0000002B-QINU`"' (2) · 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) · 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) · 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) · 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) · 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) · 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) · Generally considered safe; widely used. Cetirizine and loratadine remain the more-studied alternatives.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe; widely used. Levocetirizine (the R-enantiomer) is an alternative with similar safety.<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; degludec has reassuring observational data.<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 human data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · Limited human data; older agent with substantial use experience.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Older agent with substantial use experience; observational signals reassuring for first-trimester exposure.<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) · Some controversial signal for first-trimester gastroschisis association in observational studies; limited use is generally considered acceptable after the first trimester.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (1) · '''[[USLegal:Behind-the-counter|Behind-the-counter]] in US''' under the Combat Methamphetamine Epidemic Act 2005: purchase restricted to ≤3.6 g/day and ≤9 g/30 days, with photo ID, logbook signature, and quantity logging required. Several states schedule higher than federal (1) · OTC in US (4) · [[USLegal:Over-the-counter|OTC]] as Bonine and Dramamine Less Drowsy; [[USLegal:Prescription only|Rx-only]] as Antivert (1) · [[USLegal:Over-the-counter|OTC]] in US at ≤220 mg/tablet and ≤660 mg/day; [[USLegal:Prescription only|Rx-only]] at higher strengths (1) · [[USLegal:Prescription only|Rx-only]] in US (6) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, distinguishing it from carisoprodol among muscle-spasm options'"`UNIQ--ref-0000001F-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, distinguishing it from the carisoprodol alternative for muscle spasm'"`UNIQ--ref-0000001C-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 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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