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classes:
Beta blocker (3) · Atypical antipsychotic (2) · Barbiturate (2) · Sedative-hypnotic (2) · [[:Category:Fixed-dose_combinations|Fixed-dose combination]] (2) · [[:Category:Mood stabilizers|Mood stabilizer]] (2) · [[:Category:Neuroleptics|Neuroleptic]] (2)
mechanism: (Click arrow to add another value)
uses:
None (13) · Major depressive disorder in adults (FDA-approved 2011) (1) · Major depressive disorder in adults (FDA-approved 2013). Notable for evidence of cognitive benefit (processing speed) that distinguishes it from other antidepressants. (1) · Major depressive disorder in adults (FDA-approved August 2022) (1) · Schizophrenia (FDA-approved 2015). Acute manic or mixed episodes of bipolar I disorder. Bipolar I depression (FDA-approved 2019). Adjunctive treatment of major depressive disorder (FDA-approved Dec 2022). (1) · Schizophrenia (FDA-approved Dec 2019). Bipolar depression as monotherapy or adjunct to lithium/valproate (FDA-approved Dec 2021). (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`"' (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-0000004B-QINU`"', '"`UNIQ--vote-0000004C-QINU`"', '"`UNIQ--vote-0000004D-QINU`"', '"`UNIQ--vote-0000004E-QINU`"' (1) · '"`UNIQ--vote-0000004C-QINU`"', '"`UNIQ--vote-0000004D-QINU`"', '"`UNIQ--vote-0000004E-QINU`"' (1) · '"`UNIQ--vote-00000932-QINU`"', '"`UNIQ--vote-00000933-QINU`"', '"`UNIQ--vote-00000934-QINU`"', '"`UNIQ--vote-00000935-QINU`"', '"`UNIQ--vote-00000936-QINU`"', '"`UNIQ--vote-00000937-QINU`"' (1) · '"`UNIQ--vote-0000129E-QINU`"' (1) · '"`UNIQ--vote-00001567-QINU`"' (1) · '"`UNIQ--vote-0000159D-QINU`"', '"`UNIQ--vote-0000159E-QINU`"' (1)
starting dose:
None (15) · 1 tablet (dextromethorphan 45 mg / bupropion 105 mg) PO daily × 3 days, then increase to 1 tablet BID (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) · 10 mg PO once daily × 7 days, then 20 mg × 7 days, then 40 mg as target dose (take with food) (1) · 10 mg PO once daily; may increase to 20 mg as tolerated, or decrease to 5 mg if needed (1) · 15-37.5 mg PO once daily before breakfast or 1-2 hours after; Lomaira 8 mg TID (1) · 300 mg PO at bedtime night 1, 300 mg BID day 2, 300 mg TID day 3; titrate to clinical effect, commonly 1800-3600 mg/day divided TID (1) · 42 mg PO once daily with food (no titration) (1) · 500-750 mg PO BID; 400 mg IV q8-12h (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) · Schizophrenia / acute mania: 5-10 mg PO once daily, target 10-15 mg/day. Acute agitation IM: 10 mg, may repeat in 2 hours. Relprevv LAI: 150-300 mg every 4 weeks after oral overlap (1) · Schizophrenia/bipolar mania: 10-15 mg PO once daily, target 15-30 mg. MDD adjunct: 2-5 mg/day, target 5-15 mg. Pediatric autism irritability: 2 mg, titrate to 5-15 mg. Maintena LAI: 400 mg IM every 4 weeks after oral overlap (1) · Schizophrenia: 1.5 mg PO daily, increase to 1.5-6 mg as tolerated. Bipolar mania: 1.5 mg, may increase to 3-6 mg. Bipolar depression: 1.5 mg daily for 14 days, then 3 mg. MDD adjunct: 1.5 mg, may increase to 3 mg. (1) · Week 1: 1 tablet (8/90 mg) PO morning; week 2: 1 tablet AM + 1 PM; week 3: 2 AM + 1 PM; week 4 onward: 2 AM + 2 PM (32 mg naltrexone / 360 mg bupropion/d) (1)
preparations:
None (12) · 1.5 mg, 3 mg, 4.5 mg, 6 mg capsules (1) · 10 mg, 20 mg, 40 mg tablets (1) · 15, 30, 37.5 mg capsules/tablets; 8 mg Lomaira (1) · 250, 500, 750 mg IR tablets; 500, 1000 mg ER tablets (XR); 250, 500 mg/5 mL oral suspension; 200, 400 mg IV; 0.3% ophthalmic solution and ointment; 0.2% otic (1) · 42 mg capsules (1) · 5 mg, 10 mg, 20 mg tablets (1) · 50/325/40 mg capsules and tablets; oral solution (1) · 8 mg naltrexone / 90 mg bupropion ER tablets (titration-pack design) (1) · Capsules 100, 300, 400 mg; tablets 600, 800 mg; oral solution 250 mg/5 mL; Gralise ER tablets 300, 600 mg (once-daily); Horizant ER tablets 300, 600 mg (gabapentin enacarbil, an inactive parent compound metabolized to gabapentin in vivo) (1) · Dextromethorphan 45 mg + bupropion 105 mg ER tablets (1) · Oral tablets 50 mg (ReVia, Depade, generics); Vivitrol extended-release IM suspension 380 mg single-dose vial; Contrave (naltrexone 8 mg + bupropion 90 mg ER tablets); compounded 1, 2, 3, 4.5 mg tablets/capsules for LDN (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, 15, 20, 30 mg; ODT 10, 15 mg; oral solution 1 mg/mL; acute IM injection 9.75 mg/1.3 mL; Maintena LAI 300, 400 mg monthly; Aristada LAI 441, 662, 882, 1064 mg (4-8 week dosing); Asimtufii bi-monthly (1) · Tablets 2.5, 5, 7.5, 10, 15, 20 mg; ODT (Zydis) 5, 10, 15, 20 mg; acute IM injection 10 mg/vial; Relprevv LAI 210, 300, 405 mg vials (1) · Tablets 5, 10, 40 mg (40 mg dispersible restricted to OTPs); oral concentrate 10 mg/mL; oral solution 1, 2, 10 mg/mL; injection 10 mg/mL (1) · Tablets: 100 mg, 200 mg (scored). [[Armodafinil]] (Nuvigil), the R-enantiomer of modafinil, is available separately as 50 mg, 150 mg, 200 mg, and 250 mg tablets. (1)
onset:
None (11) · 1-2 weeks for neuropathic pain and anxiolytic effect; anticonvulsant effect at therapeutic plasma level (1) · 20 minutes (oral); 5 minutes (IV) (1) · 30-60 minutes (1) · 4-6 weeks for full antidepressant effect (claimed earlier onset for some patients due to 5HT1A partial agonism) (1) · Antipsychotic effect over weeks (1) · Appetite suppression within hours; weight loss over weeks-months (1) · Hours (1) · Modest appetite suppression within weeks; weight loss over months (1) · Neuroleptic effect emerges over days to weeks; activation symptoms (akathisia, insomnia) often within days (1) · Oral analgesic effect 30-60 minutes; opioid-withdrawal suppression 30 minutes (oral); IV ~10 minutes (1) · Oral peak plasma 1 hour; therapeutic opioid blockade within hours of first dose. IM Vivitrol: peak plasma 2-3 days; therapeutic blockade through the dosing interval. (1) · Peak plasma concentration in 2-4 hours after oral administration. Clinically perceptible wakefulness-promoting effects typically begin within 1-2 hours of dosing.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Sedation from first dose; neuroleptic effect emerges over days to weeks (1) · Significant antidepressant response by week 1 in trials (faster than monoaminergic antidepressants which take 4-6 weeks) (1) · Sublingual analgesic effect 30-60 minutes; MOUD craving suppression within hours; Butrans patch steady-state in 3 days. (1) · Typical antidepressant 4-6 week onset (1) · Weeks for psychosis/mood efficacy (1)
bioavailability:
None (11) · '''Saturable''' via the LAT-1 amino-acid transporter, producing nonlinear pharmacokinetics: ~60% at 300 mg single dose, falling to ~35% at 1200 mg single dose'"`UNIQ--ref-0000002A-QINU`"' (1) · Adequate oral bioavailability (1) · Butalbital well-absorbed; caffeine ~100%; acetaminophen 85-98%'"`UNIQ--ref-000015A0-QINU`"' (1) · High (oral)'"`UNIQ--ref-000012A0-QINU`"' (1) · Limited but adequate; take with food (1) · Naltrexone ~5% (oral, extensive first-pass to 6β-naltrexol); bupropion ER ~87%'"`UNIQ--ref-00001569-QINU`"' (1) · Not formally characterized for the combination (1) · Oral bioavailability is not precisely established in the label but absorption is rapid and essentially complete. Food delays peak plasma concentration by approximately one hour but does not reduce the extent of absorption.'"`UNIQ--ref-0000006F-QINU`"' (1) · ~25% (oral, with extensive first-pass)'"`UNIQ--ref-00000023-QINU`"' (1) · ~30% (sublingual; the primary therapeutic route); ~10-20% (oral swallowed, low due to first-pass); ~50% (buccal Belbuca); transdermal Butrans bypasses first-pass.'"`UNIQ--ref-00000050-QINU`"' (1) · ~5-40% (oral, highly variable due to extensive first-pass metabolism; mean ~5-10% for parent naltrexone with the majority of pharmacologic effect coming from 6-beta-naltrexol). IM Vivitrol bypasses first-pass entirely.'"`UNIQ--ref-00000050-QINU`"' (1) · ~60% (oral); ~100% (IM)'"`UNIQ--ref-00000027-QINU`"' (1) · ~70% (oral; reduced by divalent cations — antacids, iron, calcium, dairy)'"`UNIQ--ref-00000939-QINU`"' (1) · ~70-85% (oral, high relative to other opioids) (1) · ~72% (with food); much lower fasting (~36%) (1) · ~75% (1) · ~87% (oral)'"`UNIQ--ref-00000026-QINU`"' (1)
pregnancy:
None (15) · '''Avoid in pregnancy where alternatives exist''' (animal cartilage toxicity; class-wide concern); use only when benefit clearly outweighs.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Contraindicated in pregnancy (FDA label).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Contraindicated in pregnancy.<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) · Limited data (1) · Limited data; avoid (1) · Limited data; National Pregnancy Registry for Atypical Antipsychotics (1) · Limited data; weigh benefits/risks (2) · Limited human data; signal for neonatal extrapyramidal symptoms 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) · Limited human data; some signal for cardiac malformations and developmental delay but confounded by maternal disease and polytherapy.<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) · Signal for gestational diabetes and metabolic syndrome with maternal exposure; the metabolic load can be substantial during pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
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