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Medicines (732)

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: Sedative-Hypnotic

or [[:Category:Antianginals|Antianginal]]

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Amlodipine (1) · Bromazolam (1) · Clonazolam (1) · Deschloroetizolam (1) · Diclazepam (1) · Diltiazem (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) · Isosorbide (dinitrate, mononitrate) (1) · Lormetazepam (1) · Methaqualone (1) · Midazolam (1) · Nifedipine (1) · Nifoxipam (1) · Nitrazepam (1) · Nitroglycerin (glyceryl trinitrate, GTN) (1) · Pentobarbital (1) · Quazepam (1) · Ramelteon (1) · Secobarbital (1) · Tasimelteon (1) · Temazepam (1) · Triazolam (1) · Verapamil (1) · Zaleplon (1) · Zopiclone (1)

None (9) · (none, never marketed) (1) · Calan, Calan SR, Verelan, Verelan PM, Isoptin SR (1) · Cardizem, Tiazac, Cartia XT, Dilacor XR, Taztia XT, Matzim LA (1) · Dalmane (1) · Doral (1) · Doriden (1) · Halcion (1) · Hetlioz (1) · Imdur (mononitrate ER), Isordil (dinitrate); generics; with hydralazine as BiDil for HFrEF in self-identified Black patients (1) · Imovane (1) · Lunesta (1) · Mogadon (1) · Nembutal (1) · Nitrostat, Nitrolingual, NitroMist, Nitro-Bid, Nitro-Dur, Minitran, Rectiv (1) · Norvasc, Katerzia (1) · Placidyl (1) · Procardia, Procardia XL, Adalat CC, Afeditab CR (1) · ProSom (1) · Quaalude (1) · Restoril (1) · Rohypnol (1) · Rozerem (1) · Seconal (1) · Sonata (1) · THIP (1) · Versed (1) · Xyrem (1)

None (6) · 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-00000073-QINU`"' The long half-life gives smooth, once-daily BP control with low rebound. CYP3A4 substrate; pedal edema is the characteristic, dose-related, non-fluid-overload side effect'"`UNIQ--ref-00000074-QINU`"'. (1) · '"`UNIQ--vote-0000063C-QINU`"' Avoid in HFrEF (negative inotropy). CYP3A4 substrate AND moderate inhibitor — interacts substantially with statins (especially simvastatin), tacrolimus, cyclosporine, and many other CYP3A4 substrates'"`UNIQ--ref-0000063D-QINU`"'. (1)

None (29) · 2.5-5 mg PO once daily; titrate to 10 mg/d (1) · ER 180-240 mg PO once daily; IR 30 mg PO QID; IV 0.25 mg/kg over 2 min for acute rate control, then 5-15 mg/h infusion (1) · ER 30-60 mg PO once daily; immediate-release 10 mg PO TID (now rarely used for hypertension due to reflex tachycardia) (1) · IR 80-120 mg PO TID; ER 180-240 mg PO daily; IV 2.5-5 mg over 2 min for SVT termination (under monitoring); cluster prophylaxis up to 480-960 mg/d in divided doses (1) · Isosorbide mononitrate ER: 30-60 mg PO once daily in the morning, titrate to 120-240 mg/d; isosorbide dinitrate IR: 5-20 mg PO TID with a 12-14 hour nitrate-free interval to prevent tolerance (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (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)

None (29) · 10, 20 mg IR capsules; 30, 60, 90 mg ER tablets (1) · 2.5, 5, 10 mg tablets; 1 mg/mL oral suspension (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · IR 30, 60, 90, 120 mg tablets; multiple ER capsules and tablets 60-420 mg; IV 5 mg/mL (1) · IR 40, 80, 120 mg tablets; SR/ER 100-360 mg; IV 2.5 mg/mL (1) · Mononitrate 10, 20 mg IR; 30, 60, 120 mg ER; dinitrate 5, 10, 20, 30, 40 mg IR and ER (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)

None (29) · 10 mg/d (1) · 120 mg/d (ER); IR not for chronic hypertension (1) · 240 mg/d (mononitrate ER); 160 mg/d (dinitrate) (1) · Indication-specific; titrated to effect (1) · N/A (never approved) (1) · ~480 mg/d (oral) for cardiovascular indications; higher off-label for cluster (1) · ~480 mg/d (oral); IV per protocol (1)

None (29) · intranasal; rectal and IV reported. (1) · IV (3) · lingual spray (1) · MI reports) (1) · multiple ER formulations) (1) · Oral (3) · Oral (IR (1) · Oral (IR and multiple ER) (1) · oral ER (1) · Oral; sublingual IR is discouraged (uncontrolled BP drops (1) · rectal (1) · Sublingual (2) · sublingual (dinitrate) (1) · topical (1) · transdermal (1)

None (29) · BP effect within 24 hours; full effect at 1-2 weeks (long half-life) (1) · IR 20 minutes; ER ~6 hours (1) · IV: 1-3 minutes (SVT termination); PO IR: 30-60 minutes; ER: hours (1) · IV: 3-7 minutes (rate control); PO IR: 30-60 minutes; ER: hours (1) · SL/spray: 1-3 minutes; IV: minutes; patch: 30-60 minutes (1) · SL: 2-5 minutes; PO mononitrate: 30-60 minutes (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (29) · 24 hours (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · IR 4-8 hours; ER 24 hours (1) · IR: 4-8 hours; ER: 24 hours (1) · IR: 6-8 hours; ER: 24 hours (1) · Mononitrate ER: 12-24 hours; dinitrate IR: 4-6 hours (1) · SL: 30 minutes; patch: 12-14 hours; IV continuous (1)

None (29) · 1-3 minutes (very short)'"`UNIQ--ref-00000C0F-QINU`"' (1) · 2-5 hours (IR); ER formulations extend functional duration via osmotic/matrix release'"`UNIQ--ref-0000074D-QINU`"' (1) · 3-4.5 hours (IR); 5-7 hours (ER; effective duration 24 hours via formulation)'"`UNIQ--ref-00000642-QINU`"' (1) · 3-7 hours (IR); functional 24 hours (ER)'"`UNIQ--ref-00000A6B-QINU`"' (1) · 30-50 hours'"`UNIQ--ref-00000078-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Mononitrate ~5 hours; dinitrate ~1 hour'"`UNIQ--ref-00001461-QINU`"' (1)

None (29) · 64-90% (oral; not affected by food)'"`UNIQ--ref-00000079-QINU`"' (1) · 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) · Mononitrate ~100% (no first-pass; the principal advantage over dinitrate); dinitrate ~20%'"`UNIQ--ref-00001462-QINU`"' (1) · Not formally characterized in humans. (1) · ~20-35% (oral; extensive first-pass via CYP3A4 with R/S enantiomer differences)'"`UNIQ--ref-00000A6C-QINU`"' (1) · ~40% (oral; extensive first-pass via CYP3A4)'"`UNIQ--ref-00000643-QINU`"' (1) · ~50% IR (extensive first-pass via CYP3A4); ER products release-rate-limited'"`UNIQ--ref-0000074E-QINU`"' (1)

None (29) · 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 data.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Limited data; alternative antihypertensives generally preferred. Crosses placenta.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Limited data; case series and registries suggest no major teratogenicity but other antihypertensives (labetalol, nifedipine) are typically preferred.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Limited data; labetalol/nifedipine generally preferred. Crosses placenta.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Oral nifedipine is one of the preferred agents for severe hypertension in pregnancy and for tocolysis in preterm labor.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Used in obstetric emergencies (uterine relaxation, severe hypertension) when needed; otherwise limited routine use.[[[Pharmacopedia:Citation needed|citation needed]]] (1)