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Medicines > classes

: Sedative-Hypnotic

or [[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]]

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Bromazolam (1) · Clonazolam (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) · Irbesartan (1) · Lormetazepam (1) · Losartan (1) · Methaqualone (1) · Midazolam (1) · Nifoxipam (1) · Nitrazepam (1) · Olmesartan (medoxomil) (1) · Pentobarbital (1) · Quazepam (1) · Ramelteon (1) · Secobarbital (1) · Tasimelteon (1) · Telmisartan (1) · Temazepam (1) · Triazolam (1) · Valsartan (1) · Zaleplon (1) · Zopiclone (1)

None (9) · (none, never marketed) (1) · Avapro (1) · Benicar (1) · Cozaar (1) · Dalmane (1) · Diovan; Entresto (in fixed-dose combination with sacubitril) (1) · Doral (1) · Doriden (1) · Halcion (1) · Hetlioz (1) · Imovane (1) · Lunesta (1) · Micardis (1) · Mogadon (1) · Nembutal (1) · Placidyl (1) · ProSom (1) · Quaalude (1) · Restoril (1) · Rohypnol (1) · Rozerem (1) · Seconal (1) · Sonata (1) · THIP (1) · Versed (1) · Xyrem (1)

None (3) · 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 GABA<sub>A</sub> receptor at the benzodiazepine binding site; increases frequency of Cl<sup>−</sup> channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1) · Selective GABAA agonist (extrasynaptic delta subunit) (1) · '"`UNIQ--vote-000000B6-QINU`"' Active metabolite EXP3174 is ~10-40-fold more potent than the parent and accounts for most of the antihypertensive effect; CYP2C9 polymorphism affects conversion'"`UNIQ--ref-000000B7-QINU`"'. (1) · '"`UNIQ--vote-000004C8-QINU`"' Largely hepatically cleared (~80% biliary); no active metabolite. Sacubitril-valsartan (Entresto) combines an ARB with neprilysin inhibition for HFrEF and was a notable advance over the ARB-alone trial (PARADIGM-HF, 2014)'"`UNIQ--ref-000004C9-QINU`"'. (1) · '"`UNIQ--vote-0000083E-QINU`"' CYP2C9 substrate; no clinically active metabolites. The IDNT trial established renoprotection in diabetic nephropathy independent of BP lowering, contributing to the ARB class indication in T2DM with proteinuria'"`UNIQ--ref-0000083F-QINU`"'. (1) · '"`UNIQ--vote-00000AEA-QINU`"' The 24-hour half-life supports once-daily dosing with consistent overnight BP control. Largely hepatically cleared (~98% biliary); no significant renal clearance dependence'"`UNIQ--ref-00000AEB-QINU`"'. (1)

None (29) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-000000B8-QINU`"', '"`UNIQ--vote-000000B9-QINU`"', '"`UNIQ--vote-000000BA-QINU`"', '"`UNIQ--vote-000000BB-QINU`"' (1) · '"`UNIQ--vote-000004CA-QINU`"', '"`UNIQ--vote-000004CB-QINU`"', '"`UNIQ--vote-000004CC-QINU`"' (1) · '"`UNIQ--vote-0000056B-QINU`"' (1) · '"`UNIQ--vote-00000840-QINU`"', '"`UNIQ--vote-00000841-QINU`"' (1) · '"`UNIQ--vote-00000AEC-QINU`"', '"`UNIQ--vote-00000AED-QINU`"' (1)

None (29) · 150 mg PO once daily; titrate to 300 mg if needed (1) · 20 mg PO once daily; titrate to 40 mg/d after 2 weeks if needed (1) · 40 mg PO once daily; titrate to 80 mg (1) · 50 mg PO daily (25 mg in volume depletion or hepatic impairment) (1) · 80-160 mg PO once daily (40 mg BID in HFrEF, titrating up to 160 mg BID) (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

None (29) · 20, 40, 80 mg tablets (1) · 25 mg, 50 mg, 100 mg tablets (1) · 40, 80, 160, 320 mg tablets; oral suspension (1) · 5, 20, 40 mg tablets (1) · 75, 150, 300 mg tablets (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)

None (29) · 100 mg/d (1) · 300 mg/d (1) · 320 mg/d (hypertension); 320 mg/d (HF) (1) · 40 mg/d (1) · 80 mg/d (1) · N/A (never approved) (1)

None (29) · intranasal; rectal and IV reported. (1) · Oral (6) · sublingual (1)

None (29) · BP effect 1-2 weeks; antihypertensive peak 3-6 weeks (1) · BP effect 1-2 weeks; max at 2-3 weeks (1) · BP effect 2 hours; max at 4-6 weeks (1) · BP effect within 1-2 weeks (2) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (29) · 24 hours (5) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)

None (29) · 11-15 hours'"`UNIQ--ref-00000842-QINU`"' (1) · 2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~13 hours'"`UNIQ--ref-0000056C-QINU`"' (1) · ~24 hours (longest of the ARB class; suits patients with morning BP surge)'"`UNIQ--ref-00000AEE-QINU`"' (1) · ~6 hours'"`UNIQ--ref-000004CD-QINU`"' (1)

None (29) · 42-58% (oral; dose-dependent)'"`UNIQ--ref-00000AEF-QINU`"' (1) · 60-80% (oral; not significantly affected by food)'"`UNIQ--ref-00000843-QINU`"' (1) · Not formally characterized in humans. (1) · ~25% (oral; food reduces absorption ~40%)'"`UNIQ--ref-000004CE-QINU`"' (1) · ~26% (oral; prodrug hydrolyzed by intestinal esterases to active olmesartan; not affected by food)'"`UNIQ--ref-0000056D-QINU`"' (1) · ~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"' (1)

None (29) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000000BE-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000004CF-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-0000056E-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000844-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000AF0-QINU`"' (1) · 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)