Drilldown: Medicines

Losartan (1) · Valsartan (1)

Cozaar (1) · Diovan; Entresto (in fixed-dose combination with sacubitril) (1)

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'"`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-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)

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)

25 mg, 50 mg, 100 mg tablets (1) · 40, 80, 160, 320 mg tablets; oral suspension (1)

None · Indication-specific · 40 mg/d · 10 mg/d · 20 mg/d · 80 mg/d · 10 mg/d (adults) · 100 mg/d · 4 g/d · 400 mg/d · 40 mg/d typical; up to 240 mg/d for Zollinger-Ellison · 5 mg/d · 50 mg/d · 600 mg/d · No fixed ceiling; titrate to clinical effect and tolerability with CDC opioid prescribing guidance constraints on morphine-milligram-equivalent (MME) totals · No fixed maximum; titrated to TSH target · TID per eye · Titrated to glucose; no fixed ceiling · Titrated to glucose; no fixed maximum · '''20 mg/day in adults >60 years''' per FDA's 2011-2012 QT-prolongation warning; 40 mg/day in adults ≤60

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Oral (2)

BP effect 1-2 weeks; antihypertensive peak 3-6 weeks (1) · BP effect 2 hours; max at 4-6 weeks (1)

24 hours (2)

2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-QINU`"' (1) · ~6 hours'"`UNIQ--ref-000004CD-QINU`"' (1)

~25% (oral; food reduces absorption ~40%)'"`UNIQ--ref-000004CE-QINU`"' (1) · ~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"' (1)

'''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)

[[USLegal:Prescription only|Rx-only]] in US (2)