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: 10 mg/d

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None (1) · Alprazolam (1) · Amlodipine (1) · Dapagliflozin (1) · Ezetimibe (1) · Flecainide (1) · Flibanserin (1) · Losartan (1) · Metoprolol (1) · Moxifloxacin (1) · Sitagliptin (1)

Addyi (1) · Avelox (oral/IV brand discontinued US); Vigamox, Moxeza (ophthalmic) (1) · Cozaar (1) · Dayvigo (1) · Farxiga (US), Forxiga (international) (1) · Januvia; with metformin Janumet/Janumet XR (1) · Lopressor (tartrate), Toprol XL (succinate) (1) · Norvasc, Katerzia (1) · Tambocor (US brand discontinued) (1) · Xanax (1) · Zetia (1)

Anxiolytic (1) · Benzodiazepine (1) · Beta Blocker (1) · Cardioselective (β1) (1) · Dual orexin receptor antagonist (DORA) (1) · Multimodal serotonergic; HSDD treatment (1) · Triazolobenzodiazepine (1) · [[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (1) · [[:Category:Antianginals|Antianginal]] (1) · [[:Category:Antiarrhythmics|Antiarrhythmic (Vaughan-Williams class IC)]] (1) · [[:Category:Antibacterials|Antibacterial]] (1) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (2) · [[:Category:Antihypertensives|Antihypertensive]] (2) · [[:Category:Calcium_channel_blockers|Calcium channel blocker]] (1) · [[:Category:Cholesterol_absorption_inhibitors|Cholesterol absorption inhibitor]] (1) · [[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (1) · [[:Category:Fluoroquinolones|Fluoroquinolone antibiotic]] (1) · [[:Category:Heart_failure_medications|Heart failure medication]] (1) · [[:Category:Incretin_modulators|Incretin pathway modulator]] (1) · [[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (1) · [[:Category:SGLT2_inhibitors|SGLT2 inhibitor]] (1)

None (2) · 5-HT1A agonist, 5-HT2A antagonist, with weaker activity at D4 and other receptors. Net effect involves enhanced prefrontal dopaminergic/noradrenergic tone with decreased serotonergic inhibition of sexual desire. (1) · Cardioselective β1-adrenergic antagonist. Selectivity is dose-dependent and partially lost at higher doses. (1) · Competitive antagonist at OX1R and OX2R. Faster receptor association/dissociation kinetics than suvorexant (~16 sec dissociation vs ~57 sec) hypothesized to support sleep onset, with sufficient duration for maintenance. (1) · GABA-A positive allosteric modulator'"`UNIQ--ref-00000067-QINU`"' '"`UNIQ--vote-00000068-QINU`"' (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-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-00000762-QINU`"' Largely renally cleared, hence the eGFR-tiered dosing. Rare but well-documented signals: acute pancreatitis (uncertain causal contribution), severe joint pain, and bullous pemphigoid (class effect, especially in older Asian patients)'"`UNIQ--ref-00000763-QINU`"'. (1) · '"`UNIQ--vote-00000D7A-QINU`"' Substantial QT-interval prolongation — the most QT-prolonging fluoroquinolone — limits use in patients on other QT-prolonging agents or with electrolyte abnormalities'"`UNIQ--ref-00000D7B-QINU`"'. (1) · '"`UNIQ--vote-0000113A-QINU`"' Concomitant β-blocker or CCB is required when used for AF to prevent 1:1 atrial flutter conduction (flecainide can slow atrial rate to a level where AV conduction allows dangerous ventricular rates). CYP2D6 substrate'"`UNIQ--ref-0000113B-QINU`"'. (1)

0.25 mg (1) · 10 mg PO once daily in the morning; 5 mg starting in heart failure (1) · 10 mg PO once daily, with or without food (1) · 100 mg at bedtime daily (1) · 100 mg PO once daily (50 mg if CrCl 30-44; 25 mg if <30 or dialysis) (1) · 2.5-5 mg PO once daily; titrate to 10 mg/d (1) · 25–50 mg BID (tartrate); 25–100 mg daily (succinate); 12.5 mg daily in HFrEF (1) · 400 mg PO/IV once daily (1) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · 50 mg PO BID; titrate to 100-200 mg BID; pill-in-pocket 200-300 mg PO single dose for AF conversion (1) · 50 mg PO daily (25 mg in volume depletion or hepatic impairment) (1)

0.25 mg, 0.5 mg, 1 mg, 2 mg tablets (immediate-release and orally disintegrating); 0.5 mg, 1 mg, 2 mg, 3 mg extended-release tablets; 1 mg/mL oral concentrate (1) · 10 mg tablet; also as fixed-dose combinations with simvastatin (Vytorin) and atorvastatin (Liptruzet, withdrawn US 2015 but generics exist) (1) · 100 mg tabs (1) · 2.5, 5, 10 mg tablets; 1 mg/mL oral suspension (1) · 25 mg, 50 mg, 100 mg tablets (1) · 25, 50, 100 mg tablets; combination tablets with metformin (1) · 400 mg tablets; 400 mg/250 mL IV; 0.5% ophthalmic solution (1) · 5 mg, 10 mg tablets (2) · 50, 100, 150 mg tablets (1) · Tartrate: 25, 50, 100 mg tabs; 1 mg/mL IV. Succinate ER: 25, 50, 100, 200 mg. (1)

IV (2) · Oral (11) · topical ophthalmic (1)

1–2 h (PO); immediate (IV) (1) · 30-60 min (immediate-release); 1-2 h (extended-release) (1) · AF conversion within hours of single PO dose (1) · BP effect 1-2 weeks; antihypertensive peak 3-6 weeks (1) · BP effect within 24 hours; full effect at 1-2 weeks (long half-life) (1) · Effects accumulate over weeks; assess at 8 weeks (1) · Glycosuria within hours; HbA1c effect at 12 weeks; CV/renal benefits over months (1) · Hours (1) · LDL lowering within 2 weeks (1) · Postprandial glucose effect within days; HbA1c by 12 weeks (1) · ~30 min (1)

12 hours (1) · 24 hours (6) · 6 h (immediate-release); ~11 h (extended-release) (1) · 6–12 h (tartrate); 24 h (succinate) (1) · Continuous daily dosing (1) · ~7-8 hours (1)

11-13 h (immediate-release); 11-16 h (extended-release) (1) · 2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-QINU`"' (1) · 30-50 hours'"`UNIQ--ref-00000078-QINU`"' (1) · 3–7 h (1) · ~11 h (1) · ~12 hours'"`UNIQ--ref-00000D82-QINU`"' (1) · ~12.4 hours'"`UNIQ--ref-00000765-QINU`"' (1) · ~12.9 hours'"`UNIQ--ref-00000552-QINU`"' (1) · ~14 hours (adults); longer in elderly and renal impairment'"`UNIQ--ref-0000113F-QINU`"' (1) · ~17-19 hours (longer than daridorexant) (1) · ~22 hours (parent + active glucuronide)'"`UNIQ--ref-00000450-QINU`"' (1)

64-90% (oral; not affected by food)'"`UNIQ--ref-00000079-QINU`"' (1) · 80-90% oral (1) · Variable (oral; rapidly conjugated to active glucuronide; food does not affect)'"`UNIQ--ref-00000451-QINU`"' (1) · ~33% (1) · ~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"' (1) · ~44% (1) · ~50% (1) · ~78% (oral; high-fat meal modestly reduces but is not clinically significant)'"`UNIQ--ref-00000553-QINU`"' (1) · ~87% (oral)'"`UNIQ--ref-00000766-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00001140-QINU`"' (1) · ~90% (oral; not affected by food but reduced by divalent cations)'"`UNIQ--ref-00000D83-QINU`"' (1)

'''Avoid in pregnancy where alternatives exist''' (animal cartilage toxicity).[[[Pharmacopedia:Citation needed|citation needed]]] (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000000BE-QINU`"' (1) · Avoid in second and third trimesters; fetal SGLT2 inhibition disrupts kidney development.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Category C (1) · Category D'"`UNIQ--ref-0000006C-QINU`"' (1) · Limited data; avoid (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; generally avoided particularly in combination with statin.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Limited data; switch to insulin where feasible.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Not indicated; pregnancy effects unknown (1) · Use in fetal SVT (transplacental antiarrhythmic therapy) is established; otherwise weigh against alternatives.[[[Pharmacopedia:Citation needed|citation needed]]] (1)

Rx, Schedule IV (US) (1) · Rx-only in US (1) · Rx-only in US (REMS program) (1) · Schedule IV (US) (1) · [[USLegal:Prescription only|Rx-only]] in US (5) · [[USLegal:Prescription only|Rx-only]] in US. '''Contraindicated in structural heart disease''' — CAST trial (1989) showed increased mortality from class IC agents in patients with prior MI; modern use is limited to structurally normal hearts'"`UNIQ--ref-00001141-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the same fluoroquinolone-class '''Boxed Warnings''' as ciprofloxacin/levofloxacin'"`UNIQ--ref-00000D84-QINU`"' (1)