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Medicines > routes : rectal or transdermal

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brand:
Aricept (oral), Adlarity (transdermal patch) (1) · Asacol HD, Pentasa, Lialda, Apriso, Delzicol, Rowasa (rectal), Canasa (suppository) (1) · Bayer, Ecotrin, Bufferin, St. Joseph (low-dose 81 mg), Excedrin (with acetaminophen and caffeine) (1) · Colace (sodium), Surfak (calcium); many generics OTC (1) · Cortef (oral), Solu-Cortef (IV), many topical brands (Cortizone, OTC); Plenadren, Alkindi (modified-release for adrenal insufficiency) (1) · Ditropan, Ditropan XL, Oxytrol (transdermal), Gelnique (gel) (1) · Dulcolax, Correctol, Bisac-Evac (1) · Estrace, Vivelle-Dot, Climara, Divigel, Evamist, Estring, Estraderm, Premarin (CEE, not strictly estradiol) (1) · Indocin (oral, IV, suppository), Tivorbex (low-dose), Indo-Lemmon (1) · Kapvay (ER, ADHD), Catapres (IR, antihypertensive), Catapres-TTS (transdermal patch), Duraclon (epidural injection) (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) · Nitrostat, Nitrolingual, NitroMist, Nitro-Bid, Nitro-Dur, Minitran, Rectiv (1) · Phenergan, Promethegan (suppositories) (1) · Ritalin, Ritalin LA, Concerta, Metadate CD, Daytrana, Quillivant XR (1) · Tylenol, Panadol (international), Ofirmev (IV); huge OTC presence (1) · Valium (oral, IV/IM, rectal), Diastat (rectal gel for breakthrough seizures), Valtoco (nasal spray for breakthrough seizures), Libervant (buccal film) (1) · Voltaren (IR oral, topical gel), Cataflam (potassium IR), Cambia (oral powder, migraine), Zorvolex (low-dose), Pennsaid (topical 2% solution), Flector (transdermal patch), Solaraze (3% gel for actinic keratosis) (1)
classes:
[[:Category:Analgesics|Analgesic]] (4) · [[:Category:Antipyretics|Antipyretic]] (2) · [[:Category:NSAIDs|Non-steroidal anti-inflammatory (NSAID)]] (2)
uses:
ADHD, narcolepsy (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-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`"' (3) · '"`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`"', '"`UNIQ--vote-00000026-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`"' (1) · '"`UNIQ--vote-000003B5-QINU`"', '"`UNIQ--vote-000003B6-QINU`"', '"`UNIQ--vote-000003B7-QINU`"', '"`UNIQ--vote-000003B8-QINU`"', '"`UNIQ--vote-000003B9-QINU`"' (1) · '"`UNIQ--vote-000006A2-QINU`"', '"`UNIQ--vote-000006A3-QINU`"', '"`UNIQ--vote-000006A4-QINU`"' (1) · '"`UNIQ--vote-000006DE-QINU`"', '"`UNIQ--vote-000006DF-QINU`"', '"`UNIQ--vote-000006E0-QINU`"' (1) · '"`UNIQ--vote-00000ACD-QINU`"', '"`UNIQ--vote-00000ACE-QINU`"', '"`UNIQ--vote-00000ACF-QINU`"', '"`UNIQ--vote-00000AD0-QINU`"' (1) · '"`UNIQ--vote-00000BBC-QINU`"', '"`UNIQ--vote-00000BBD-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-00001069-QINU`"', '"`UNIQ--vote-0000106A-QINU`"' (1) · '"`UNIQ--vote-00001341-QINU`"', '"`UNIQ--vote-00001342-QINU`"' (1)
starting dose:
None (1) · 100-200 mg PO once or twice daily; pediatric weight-based (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) · 5 mg PO once daily at bedtime; titrate to 10 mg/day after 4-6 weeks. Severe Alzheimer disease: may escalate to 23 mg/day. Adlarity patch: 5 or 10 mg/day applied weekly (1) · 5-15 mg PO once at bedtime; 10 mg PR for faster effect; bowel prep regimens use higher single doses (1) · Active UC: Lialda 2.4-4.8 g PO once daily, Apriso 1.5 g PO once daily; maintenance 1.2-2.4 g/d; rectal Rowasa enema 4 g HS for distal disease; Canasa 1 g suppository HS for proctitis (1) · Acute gout: 50 mg PO TID until symptom relief, then taper; maximum 200 mg/day for 3-5 days. Rheumatoid arthritis / osteoarthritis: 25-50 mg PO BID-TID. Patent ductus arteriosus: 0.2 mg/kg IV, then 0.1-0.2 mg/kg every 12-24 hours for 2 doses (1) · ADHD (Kapvay ER): 0.1 mg PO at bedtime, titrate weekly to 0.4 mg/day divided BID. HTN (IR): 0.1 mg PO BID, titrate by 0.1 mg increments (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) · Antiplatelet: 81 mg PO once daily. Acute MI/stroke: 162-325 mg chewed. Analgesic: 325-650 mg PO every 4-6 hours as needed (1) · Anxiety: 2-10 mg PO 2-4 times daily. Alcohol withdrawal: 10-20 mg PO/IV every 4-6 hours, symptom-triggered. Status epilepticus: 5-10 mg IV. Breakthrough seizures: Diastat rectal 0.2-0.5 mg/kg or Valtoco intranasal 5-20 mg (1) · IR 5 mg PO BID-TID; ER 5-10 mg PO daily, titrate; transdermal patch 3.9 mg/d twice weekly (OTC) (1) · IR oral 50 mg PO TID or 75 mg BID. Voltaren 1% gel: apply 2-4 g to affected area QID. Pennsaid 2%: 40 drops to knee BID. Flector patch: every 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) · Oral 1-2 mg daily; transdermal patch 0.025-0.05 mg/d twice weekly; transdermal gel 0.5-1 g/d; vaginal 10 mcg tablet twice weekly for GSM. Always combine with a progestogen in patients with an intact uterus. (1) · Physiologic replacement 15-25 mg/d divided (e.g., 10 mg AM, 5 mg noon, 5 mg afternoon); stress dose 50-100 mg IV q6-8h; adrenal crisis 100 mg IV then 50-100 mg q6h; topical 0.5-2.5% applied 2-4×/d (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)
preparations:
None (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) · 5 mg enteric-coated tablets; 10 mg rectal suppositories; OTC and Rx (1) · 5 mg IR tablets; 5, 10, 15 mg ER tablets; 5 mg/5 mL syrup; 3.9 mg/24 h transdermal patch (Oxytrol); 10% topical gel (1) · 5, 10, 20 mg oral tablets; 100, 250, 500, 1000 mg IV (Solu-Cortef); 0.5%, 1%, 2.5% topical creams/ointments; rectal foam and enemas (1) · 50, 100, 250 mg capsules; 50 mg/5 mL syrup; OTC (1) · Capsules 25, 50 mg; ER capsules 75 mg; oral suspension 25 mg/5 mL; suppositories 50 mg; injection 1 mg/vial (PDA closure) (1) · IR tablets 0.1, 0.2, 0.3 mg; ER tablets 0.1, 0.2 mg (Kapvay); transdermal patches 0.1, 0.2, 0.3 mg/24h (TTS-1/2/3, weekly); epidural injection (Duraclon) (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 25, 50 mg; ER tablets 100 mg; Cataflam IR 50 mg; Zorvolex 18, 35 mg; Voltaren gel 1%; Pennsaid 2% topical solution; Flector transdermal patch; Solaraze 3% gel; Cambia oral powder 50 mg (1) · Multiple non-bioequivalent oral formulations (pH-, time-, and moisture-dependent release); rectal enema 4 g/60 mL; 1 g rectal suppository (1) · Oral 0.5, 1, 2 mg tablets; transdermal patches (twice-weekly and once-weekly); 0.06% gel; 1.53 mg/spray topical; vaginal ring (Estring); vaginal tablet (Vagifem/Yuvafem); vaginal cream (1) · Oral tablets 5, 10, 23 mg; ODT 5, 10 mg; Adlarity transdermal patch 5, 10 mg/day (weekly application) (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 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 2, 5, 10 mg; oral solution 1, 5 mg/mL; injection 5 mg/mL; Diastat rectal gel 2.5, 5, 10, 20 mg; Valtoco nasal spray 5, 7.5, 10 mg/dose; Libervant buccal film (1) · Tablets 81 (low-dose), 325, 500, 650 mg; chewable 81 mg; enteric-coated tablets; effervescent tablets; suppositories (1)
routes: (Click arrow to add another value)
halflife:
1-2 hours (parent compound)'"`UNIQ--ref-00000029-QINU`"' (1) · 1-3 hours (normal liver); markedly prolonged in overdose with glutathione depletion'"`UNIQ--ref-000006A5-QINU`"' (1) · 1-3 minutes (very short)'"`UNIQ--ref-00000C0F-QINU`"' (1) · 12-15 hours'"`UNIQ--ref-00000022-QINU`"' (1) · 12-16 hours'"`UNIQ--ref-00000026-QINU`"' (1) · 2-3 hours (parent and active N-desethyl metabolite)'"`UNIQ--ref-000006E1-QINU`"' (1) · 2–3 h (parent compound) (1) · 4-5 hours'"`UNIQ--ref-00000026-QINU`"' (1) · Aspirin 15-30 minutes; salicylate metabolite 2-3 hours (concentration-dependent, saturable at high doses)'"`UNIQ--ref-00000027-QINU`"' (1) · Diazepam 20-50 hours; '''N-desmethyldiazepam (nordazepam) 30-200 hours''' is the major active metabolite and accumulates substantially with chronic dosing'"`UNIQ--ref-00000026-QINU`"' (1) · Morphine 2-4 hours; morphine-6-glucuronide active metabolite 2-4 hours (longer with renal impairment)'"`UNIQ--ref-00000020-QINU`"' (1) · Not meaningfully described (1) · Plasma ~1-2 hours; biologic ~8-12 hours'"`UNIQ--ref-00000AD1-QINU`"' (1) · Variable; effect dependent on local intestinal action rather than systemic kinetics'"`UNIQ--ref-0000106B-QINU`"' (1) · ~13-20 hours (oral); transdermal pharmacokinetics buffer the peaks/troughs of oral dosing'"`UNIQ--ref-000003BA-QINU`"' (1) · ~5-10 hours (5-ASA)'"`UNIQ--ref-00000BBE-QINU`"' (1) · ~70 hours (long, supports once-daily dosing without peak-trough variation)'"`UNIQ--ref-0000001B-QINU`"' (1)
bioavailability:
Highly formulation-dependent; the goal is colonic delivery with minimal systemic exposure'"`UNIQ--ref-00000BBF-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) · Local action; minimal systemic effect (1) · Low systemic absorption (enteric coating delivers drug to colon)'"`UNIQ--ref-0000106C-QINU`"' (1) · Oral ~5% (extensive first-pass to estrone and conjugates); transdermal bypasses first-pass, giving more physiologic estradiol:estrone ratio'"`UNIQ--ref-000003BB-QINU`"' (1) · ~100% (oral)'"`UNIQ--ref-0000001C-QINU`"' (1) · ~100% (oral)'"`UNIQ--ref-00000027-QINU`"' (1) · ~25% (oral, with extensive first-pass)'"`UNIQ--ref-00000023-QINU`"' (1) · ~25-40% (oral; extensive first-pass)'"`UNIQ--ref-00000021-QINU`"' (1) · ~30% (high first-pass) (1) · ~50% (oral; reduced by buffering and enteric coating but onset clinically similar)'"`UNIQ--ref-00000028-QINU`"' (1) · ~50-60% (oral; substantial first-pass metabolism)'"`UNIQ--ref-0000002A-QINU`"' (1) · ~6% IR oral (substantial first-pass to active N-desethyl metabolite, which contributes most of the antimuscarinic adverse effects); transdermal bypasses first-pass and is better tolerated'"`UNIQ--ref-000006E2-QINU`"' (1) · ~75-85% (oral); ~60% (transdermal at steady state)'"`UNIQ--ref-00000027-QINU`"' (1) · ~85-98% (oral)'"`UNIQ--ref-000006A6-QINU`"' (1) · ~93% (oral); ~90% (rectal)'"`UNIQ--ref-00000027-QINU`"' (1) · ~96% (oral)'"`UNIQ--ref-00000AD2-QINU`"' (1)
pregnancy:
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`"' (1) · Avoid from 20 weeks gestation onward per FDA's 2020 expanded NSAID warning; contraindicated from 30 weeks (risk of premature ductus arteriosus closure, which is paradoxically the basis of the neonatal PDA-closure indication)'"`UNIQ--ref-00000028-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) · Contraindicated in pregnancy (use is not appropriate during gestation; class label X). Lactation considerations vary by indication.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered acceptable for short-term use.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe at standard doses; benefits typically outweigh in active IBD.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe.<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 human data; rarely indicated in pregnancy given the patient population.<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) · Low-dose (81 mg) safe and indicated for preeclampsia prophylaxis after 12 weeks in high-risk patients per USPSTF; high-dose aspirin avoid third trimester due to premature ductus arteriosus closure and bleeding risk (1) · Older agent with substantial use experience but limited controlled data; case reports of neonatal sedation and transient hypertension with maternal use near term.<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, including in hyperemesis gravidarum; broadly reassuring observational data'"`UNIQ--ref-00000024-QINU`"' (1) · Pregnancy categories were retired by FDA in 2015. Limited reproductive data with small observational signal for cardiac malformations; risk-benefit decision, with many patients deferring ADHD treatment during pregnancy. See pregnancy_details for the full discussion. (1) · Some signal for cleft 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) · Use when benefits outweigh; widely used at physiologic doses for adrenal insufficiency.<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)

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