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Medicines (732)

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: Sedative-Hypnotic

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Aripiprazole (1) · Bromazolam (1) · Clonazolam (1) · Clozapine (1) · Deschloroetizolam (1) · Diclazepam (1) · Estazolam (1) · Eszopiclone (1) · Ethchlorvynol (1) · Flualprazolam (1) · Flubromazepam (1) · Flubromazolam (1) · Flunitrazepam (1) · Flunitrazolam (1) · Flurazepam (1) · Gaboxadol (1) · GHB (1) · Glutethimide (1) · Lormetazepam (1) · Methaqualone (1) · Midazolam (1) · Nifoxipam (1) · Nitrazepam (1) · Olanzapine (1) · Pentobarbital (1) · Quazepam (1) · Quetiapine (1) · Ramelteon (1) · Risperidone (1) · Secobarbital (1) · Tasimelteon (1) · Temazepam (1) · Triazolam (1) · Zaleplon (1) · Zopiclone (1)

None (9) · (none, never marketed) (1) · Abilify (oral), Abilify Maintena (monthly IM LAI), Aristada (aripiprazole lauroxil IM LAI), Abilify Asimtufii (bi-monthly IM LAI), Abilify MyCite (digital ingestion sensor) (1) · Clozaril (Novartis, original brand; 25 mg and 100 mg tablets); FazaClo (orally disintegrating tablets, 12.5/25/100/150/200 mg); Versacloz (oral suspension 50 mg/mL); multiple generics. All clozapine products are subject to the same REMS monitoring requirements. (1) · Dalmane (1) · Doral (1) · Doriden (1) · Halcion (1) · Hetlioz (1) · Imovane (1) · Lunesta (1) · Mogadon (1) · Nembutal (1) · Placidyl (1) · ProSom (1) · Quaalude (1) · Restoril (1) · Risperdal (oral), Risperdal M-Tab (ODT), Risperdal Consta (biweekly IM LAI), Perseris (monthly SC LAI), Uzedy (monthly/bimonthly SC LAI), Rykindo (biweekly IM LAI) (1) · Rohypnol (1) · Rozerem (1) · Seconal (1) · Seroquel (1) · Sonata (1) · THIP (1) · Versed (1) · Xyrem (1) · Zyprexa (oral, IM acute), Zyprexa Zydis (ODT), Zyprexa Relprevv (LAI), Lybalvi (with samidorphan) (1)

None (5) · Dopamine D2 and serotonin 5-HT2A receptor antagonist'"`UNIQ--ref-0000008D-QINU`"' '"`UNIQ--vote-0000008E-QINU`"' (1) · Extremely potent GABAA positive allosteric modulator (1) · GABAA positive allosteric modulator (15) · GABAA positive allosteric modulator (non-benzodiazepine) (3) · GABAA positive allosteric modulator; very long half-life (1) · GABAA potentiator (1) · GABAA potentiator and direct activator (2) · GABAB agonist; GHB receptor agonist (1) · Melatonin receptor agonist (2) · Positive allosteric modulator of the GABAA receptor at the benzodiazepine binding site; increases frequency of Cl− channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1) · Selective GABAA agonist (extrasynaptic delta subunit) (1) · '"`UNIQ--vote-00000049-QINU`"' (1)

None (29) · 12.5 mg PO once or twice daily. Titrate gradually: 25-50 mg/day increments every 1-2 days as tolerated. Target dose 300-450 mg/day in divided doses (BID or TID). Most patients stabilize between 200-600 mg/day. Therapeutic plasma level guide: target trough clozapine ≥350 ng/mL. (1) · 25 mg (schizophrenia, immediate-release); 50 mg (bipolar mania, immediate-release); 50 mg (Seroquel XR, schizophrenia or bipolar) (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (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 / mania: 1 mg PO BID, titrate to 4-8 mg/day. Pediatric autism irritability: 0.25-0.5 mg/day, weight-titrated. Consta LAI: 25 mg IM every 2 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)

None (29) · 25 mg, 50 mg, 100 mg, 200 mg, 300 mg, 400 mg immediate-release tablets; 50 mg, 150 mg, 200 mg, 300 mg, 400 mg extended-release tablets (Seroquel XR) (1) · Clozaril 25 mg and 100 mg tablets; FazaClo orally disintegrating tablets (12.5/25/100/150/200 mg); Versacloz oral suspension 50 mg/mL. All brands subject to identical REMS ANC monitoring requirements. Generic tablets widely available. (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Tablets 0.25, 0.5, 1, 2, 3, 4 mg; M-Tab ODT 0.5, 1, 2, 3, 4 mg; oral solution 1 mg/mL; Consta LAI 12.5, 25, 37.5, 50 mg; Perseris SC LAI 90, 120 mg monthly (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)

None (29) · 16 mg/day (schizophrenia, adult); 6 mg/day (bipolar maintenance, autism irritability) (1) · 20 mg/day (oral) (1) · 30 mg/day (adult schizophrenia); 15 mg/day (MDD adjunct) (1) · 800 mg/day (1) · 900 mg/day (split into BID or TID dosing). Clinical practice rarely exceeds 600 mg/day; seizure risk increases substantially above 600 mg/day and requires consideration of prophylactic anticonvulsant.'"`UNIQ--ref-0000004A-QINU`"' (1) · N/A (never approved) (1)

None (29) · intramuscular (acute and long-acting) (2) · intramuscular (LAI) (1) · intranasal; rectal and IV reported. (1) · Oral (5) · Oral only. No parenteral formulation (a major limitation in acute agitation requiring rapid tranquilization). (1) · subcutaneous (LAI) (1) · sublingual (1)

None (29) · 30-60 min (sedation); days to weeks (neuroleptic effect) (1) · Neuroleptic effect emerges over days to weeks (1) · Neuroleptic effect emerges over days to weeks; activation symptoms (akathisia, insomnia) often within days (1) · Oral peak plasma 2.5 hours. Clinical antipsychotic response typically emerges over weeks with continued titration; full response assessment requires 3-6 months at adequate therapeutic levels. (1) · Sedation from first dose; neuroleptic effect emerges over days to weeks (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (29) · 24 hours (oral); 2-4 weeks (LAI formulations) (1) · 24 hours (oral); 2-4 weeks (LAI) (1) · 24 hours (oral); 4-8 weeks (LAI) (1) · 6-8 h (immediate-release); 24 h (extended-release) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Due to the half-life of 12 hours (wide range), dosing is BID or TID. Once-daily dosing produces higher peak/trough fluctuations and is generally not used except for a single end-of-day dose in stable patients. (1)

None (30) · 21-54 hours'"`UNIQ--ref-00000026-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Risperidone 3-20 hours; '''9-hydroxy-risperidone (paliperidone) ~20-24 hours''' is the major active metabolite and is separately marketed as a parent compound (Invega)'"`UNIQ--ref-00000021-QINU`"' (1) · ~6 h (parent compound, immediate-release); ~9-12 h (active metabolite N-desalkylquetiapine, also called norquetiapine) (1) · ~75 hours (long, accumulates over weeks)'"`UNIQ--ref-00000023-QINU`"' (1)

None (29) · Approximately 50-60% (oral; subject to first-pass metabolism); food does not significantly affect absorption.'"`UNIQ--ref-0000004C-QINU`"' (1) · Not formally characterized in humans. (1) · Tablet ~100% relative to oral solution; extensive first-pass metabolism (1) · ~60% (oral); ~100% (IM)'"`UNIQ--ref-00000027-QINU`"' (1) · ~70% (oral)'"`UNIQ--ref-00000022-QINU`"' (1) · ~87% (oral)'"`UNIQ--ref-00000024-QINU`"' (1)

None (30) · Avoid. Benzodiazepines are associated with neonatal sedation, floppy-infant syndrome, and withdrawal; teratogenic signal weak but non-zero. Designer benzo with no safety data, assume worst-case. (1) · Limited human data; signal for neonatal extrapyramidal symptoms and withdrawal with third-trimester exposure.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Pregnancy categories were retired by FDA in 2015. Quetiapine has reassuring active-comparator cohort data without consistent teratogenic signal; among the preferred neuroleptics when treatment is clinically necessary in pregnancy. See pregnancy_details for the full citation set. (1) · Signal for gestational diabetes and metabolic syndrome with maternal exposure; the metabolic load can be substantial during pregnancy.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Signal for neonatal extrapyramidal symptoms and withdrawal with third-trimester exposure.[[[Pharmacopedia:Citation needed|citation needed]]] (1)

None (33) · [[USLegal:Prescription only|Prescription only]]; not a controlled substance (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the atypical-neuroleptic '''Boxed Warning''' for increased mortality in elderly patients with dementia-related psychosis'"`UNIQ--ref-00000023-QINU`"' (1)