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Medicines > routes : transdermal or None

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generic:
 
brand:
None (237)
classes:
Research material (131) · Classic Psychedelic (69) · Stimulant (43) · Opioid (31) · Sedative-hypnotic (29) · Tryptamine (26) · Phenethylamine (25) · Botanical (23) · Benzodiazepine (22) · Anticonvulsant (19) · Dissociative (19) · Analgesic (17) · Antidepressant (17) · Antipsychotic (17) · Antiparkinsonian (16) · Empathogen (16) · Neuroleptic (16) · Cathinone (14) · Nootropic (13) · Lysergamide (12)
mechanism:
5-HT2A agonist (27) · GABAA positive allosteric modulator (22) · None (17) · Monoamine releasing agent (11) · CB1/CB2 agonist (7) · Potent mu-opioid receptor agonist (6) · Sodium channel blocker (6) · Dopamine/norepinephrine reuptake inhibitor (5) · GABAA potentiator; NMDA antagonist (5) · Phenothiazine D2 antagonist (5) · Potent 5-HT2A agonist (5) · 5-HT1B/1D agonist (4) · LSD analogue; 5-HT2A agonist (4) · Mu-opioid receptor agonist (4) · Muscarinic receptor antagonist (4) · Prodrug of LSD; 5-HT2A agonist (4) · Selective norepinephrine reuptake inhibitor (4)
uses:
None (396) · ADHD, narcolepsy (1) · Antimanic, Antidepressive, Antisuicide (1) · Pain, cough, disquiet (1) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-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`"' (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-000006DE-QINU`"', '"`UNIQ--vote-000006DF-QINU`"', '"`UNIQ--vote-000006E0-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:
None (399) · 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) · 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) · 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) · 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) · 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 (399) · 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) · 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 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) · 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)
fda max:
None (399) · 150 mg/day (oral); use lowest effective dose for shortest duration per FDA NSAID class guidance (1) · 2.4 mg/day (HTN, IR); 0.4 mg/day (ADHD, Kapvay) (1) · 23 mg/day (1) · 30 mg/d (XL) typical (1) · Indication-specific; lowest effective dose for shortest duration is the WHI-era standard (1) · Indication-specific; titrated to effect (1)
routes: (Click arrow to add another value)
onset:
None (398) · 20–60 min (oral) (1) · 30-60 min (IR oral); 2-3 days to steady state (transdermal patch) (1) · 30-60 minutes (oral); slower for topical (1) · 30-60 minutes (PO) (1) · Cognitive effect emerges gradually over weeks to months; ceiling effect at the therapeutic dose (1) · SL/spray: 1-3 minutes; IV: minutes; patch: 30-60 minutes (1) · Vasomotor relief 2-4 weeks; bone density gains over months (1)
duration:
None (397) · 24 hours (once-daily dosing) (1) · 6-8 hours (IR oral); 12-24 hours (ER) (1) · 8-12 hours (IR); ~7 days (transdermal patch) (1) · About 20 minutes (1) · IR 3–5 h; LA/SR 6–8 h; Concerta 10–12 h; Daytrana ~9 h wear time (1) · IR: 6-10 hours; ER: 24 hours (1) · Route- and formulation-dependent (1) · SL: 30 minutes; patch: 12-14 hours; IV continuous (1)
halflife:
None (397) · 1-2 hours (parent compound)'"`UNIQ--ref-00000029-QINU`"' (1) · 1-3 minutes (very short)'"`UNIQ--ref-00000C0F-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) · 9–12 minutes (intravenous) (1) · ~13-20 hours (oral); transdermal pharmacokinetics buffer the peaks/troughs of oral dosing'"`UNIQ--ref-000003BA-QINU`"' (1) · ~70 hours (long, supports once-daily dosing without peak-trough variation)'"`UNIQ--ref-0000001B-QINU`"' (1)
bioavailability:
None (398) · 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) · 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) · ~30% (high first-pass) (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)
pregnancy:
None (398) · 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) · 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) · 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) · 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) · 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) · 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 (397) · OTC (transdermal patch in women) and [[USLegal:Prescription only|Rx-only]] (other forms) in US (1) · Schedule II (1) · [[USLegal:DEA Schedule I|Schedule I]] (United States) (1) · [[USLegal:Prescription only|Rx-only]] for oral and most topical formulations in US; Voltaren Arthritis Pain 1% gel switched to [[USLegal:Over-the-counter|OTC]] in 2020 (1) · [[USLegal:Prescription only|Rx-only]] in US (3) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, like guanfacine and unlike the psychostimulant alternatives for ADHD'"`UNIQ--ref-00000028-QINU`"' (1)

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