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: Sedative-Hypnotic

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None (9) · (none, never marketed) (1) · Altoprev (ER), Mevacor (discontinued US); mostly generic (1) · Crestor, Ezallor (1) · Dalmane (1) · Doral (1) · Doriden (1) · Halcion (1) · Hetlioz (1) · Imovane (1) · Lipitor (1) · Lovaza, Omtryg (1) · Lunesta (1) · Mogadon (1) · Nembutal (1) · Niaspan (ER, Rx), Niacor (IR, Rx); huge OTC presence (1) · Placidyl (1) · Pravachol (1) · ProSom (1) · Quaalude (1) · Repatha (1) · Restoril (1) · Rohypnol (1) · Rozerem (1) · Seconal (1) · Sonata (1) · THIP (1) · Tricor, Lipofen, Antara, Fenoglide, Lofibra, Triglide, Trilipix (fenofibric acid) (1) · Vascepa (1) · Versed (1) · Xyrem (1) · Zetia (1) · Zocor (1)

None (9) · 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-0000004E-QINU`"' The EPA+DHA mix is biochemically and clinically distinct from icosapent ethyl'"`UNIQ--ref-0000004F-QINU`"'. (1) · '"`UNIQ--vote-000000F7-QINU`"' Minimal CYP3A4 dependence (CYP2C9 minor) reduces drug-drug interactions; transport in and out of hepatocytes is largely via OATP1B1, making SLCO1B1 PGx genotype the most clinically actionable marker for statin-associated myopathy'"`UNIQ--ref-000000F8-QINU`"'. (1) · '"`UNIQ--vote-000003D1-QINU`"' SLCO1B1 polymorphism affects exposure but is most clinically actionable for simvastatin'"`UNIQ--ref-000003D2-QINU`"'. (1) · '"`UNIQ--vote-000004A9-QINU`"' Modest HDL rise; LDL effects mixed. Renally cleared; combination with statin carries elevated myopathy risk (greater for gemfibrozil than fenofibrate, but caution still warranted)'"`UNIQ--ref-000004AA-QINU`"'. (1)

None (29) · 10 mg PO once daily, with or without food (1) · 10-20 mg PO once daily (1) · 10-20 mg PO once daily (5 mg in Asian ancestry, elderly, hypothyroidism, or strong CYP/SLCO1B1 interactions) (1) · 10-20 mg PO once daily in the evening (40 mg starting allowed for high CV risk) (1) · 140 mg SC every 2 weeks OR 420 mg SC monthly (3 consecutive injections 5 minutes apart due to volume) (1) · 2 g PO BID with meals (4 g/d total) (1) · 20 mg PO once daily with the evening meal; titrate to 40-80 mg/d (1) · 4 g PO daily (as 4 x 1 g capsules once daily, or 2 capsules BID) (1) · 40 mg PO once daily (10-20 mg in elderly, hepatic impairment, or strong drug interactions) (1) · Niaspan ER 500 mg PO at bedtime, titrate weekly to 1-2 g/d; flushing-protective aspirin 30-60 minutes before dose; pellagra replacement 100-500 mg/d (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Varies by salt form and brand; e.g., Tricor 145 mg PO daily; reduce to 48 mg in renal impairment (1)

None (29) · 0.5 g, 1 g capsules (1) · 1 g soft gelatin capsules containing ~465 mg EPA + ~375 mg DHA as ethyl esters (1) · 10 mg tablet; also as fixed-dose combinations with simvastatin (Vytorin) and atorvastatin (Liptruzet, withdrawn US 2015 but generics exist) (1) · 10 mg, 20 mg, 40 mg, 80 mg tablets (2) · 10, 20, 40 mg tablets; 20, 40, 60 mg ER tablets (1) · 140 mg/mL single-use prefilled syringe and SureClick autoinjector; Pushtronex 420 mg/3.5 mL on-body infusor (1) · 5, 10, 20, 40 mg tablets (1) · 5, 10, 20, 40, 80 mg tablets; 4 mg/mL oral suspension (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Multiple non-bioequivalent fenofibrate and fenofibric acid formulations: 48-200 mg (1) · OTC IR niacin 50-500 mg tablets; Niaspan ER 500, 750, 1000 mg tablets; "no-flush" niacin (inositol hexaniacinate, lacks evidence) (1)

None (29) · 10 mg/d (1) · 2 g/d (Niaspan); higher off-label use historical (1) · 4 g/d (2) · 40 mg/d (rarely needed; 40 mg restricted to patients not at goal on 20 mg) (1) · 40 mg/d standard; 80 mg/d restricted to patients tolerating 80 mg for ≥12 months without myopathy (post-SEARCH 2011 FDA restriction) (1) · 420 mg/month (1) · 80 mg/d (2) · 80 mg/d (40 mg/d if combined with diltiazem, verapamil, danazol; lower limits with various interactions) (1) · Formulation-specific (e.g., 145 mg/d Tricor, 200 mg/d Lipofen) (1) · N/A (never approved) (1)

None (29) · intranasal; rectal and IV reported. (1) · Oral (11) · Subcutaneous (1) · sublingual (1)

None (29) · LDL lowering at 1 week, max by 4 weeks (1) · LDL lowering at 2 weeks, max by 4 weeks (3) · LDL lowering at 2 weeks, max by 4 weeks; cardiovascular benefit months to years (1) · LDL lowering within 2 weeks (1) · LDL reduction ~50-60% from baseline at 1-2 weeks (1) · Lipid changes 4-8 weeks (1) · Triglyceride lowering at 2-4 weeks; max at 8 weeks (1) · Triglyceride lowering at 4-8 weeks (1) · Triglyceride lowering at 4-8 weeks; CV benefit emerges over months (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (29) · 12 hours (1) · 2-4 weeks per dose (1) · 24 hours (6) · 24 hours (evening dosing aligns with overnight HMG-CoA reductase peak) (1) · 24-48 hours per dose (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Daily dosing (1)

None (29) · 14 hours (parent); 20-30 hours including active ortho- and para-hydroxylated metabolites'"`UNIQ--ref-0000001B-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Not well characterized; tissue incorporation over weeks'"`UNIQ--ref-00000051-QINU`"' (1) · ~1 hour (IR niacin); ER formulations extend functional duration'"`UNIQ--ref-00001038-QINU`"' (1) · ~11-17 days'"`UNIQ--ref-0000147F-QINU`"' (1) · ~19 hours'"`UNIQ--ref-000000FC-QINU`"' (1) · ~2 hours (parent and active β-hydroxy acid metabolite); pharmacodynamic effect lasts 24 hours via target turnover'"`UNIQ--ref-0000017A-QINU`"' (1) · ~2-3 hours (parent); pharmacodynamic effect 24 hours via target turnover'"`UNIQ--ref-000003D5-QINU`"' (1) · ~2-4 hours (parent and active β-hydroxy acid metabolite); pharmacodynamic effect 24 hours via target turnover'"`UNIQ--ref-00000807-QINU`"' (1) · ~20 hours (fenofibric acid, the active metabolite)'"`UNIQ--ref-000004AD-QINU`"' (1) · ~22 hours (parent + active glucuronide)'"`UNIQ--ref-00000450-QINU`"' (1) · ~89 hours (EPA, the active metabolite)'"`UNIQ--ref-000013D1-QINU`"' (1)

None (29) · <5% (extensive hepatic first-pass; food enhances absorption of IR, hence the evening-meal dosing)'"`UNIQ--ref-00000808-QINU`"' (1) · <5% (extensive hepatic first-pass; statin pharmacology is hepatocellular, not systemic)'"`UNIQ--ref-0000017B-QINU`"' (1) · High (oral; food enhances)'"`UNIQ--ref-00001039-QINU`"' (1) · Improved with food'"`UNIQ--ref-00000052-QINU`"' (1) · Increased with food (varies by formulation; the micronized and nanocrystal forms are less food-dependent)'"`UNIQ--ref-000004AE-QINU`"' (1) · Not formally characterized in humans. (1) · Substantially improved with high-fat meal; take with food'"`UNIQ--ref-000013D2-QINU`"' (1) · Variable (oral; rapidly conjugated to active glucuronide; food does not affect)'"`UNIQ--ref-00000451-QINU`"' (1) · ~14% (extensive hepatic first-pass)'"`UNIQ--ref-0000001C-QINU`"' (1) · ~17% (oral; food slightly reduces absorption)'"`UNIQ--ref-000003D6-QINU`"' (1) · ~20% (oral; hydrophilic, minimal CYP metabolism, mostly excreted unchanged in bile)'"`UNIQ--ref-000000FD-QINU`"' (1) · ~72% from SC depot'"`UNIQ--ref-00001480-QINU`"' (1)

None (30) · OTC (low-dose, dietary supplement) and [[USLegal:Prescription only|Rx-only]] (Niaspan ER) in US (1) · [[USLegal:Prescription only|Rx-only]] in US (10)