Losartan
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Losartan
Cozaar
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Summary
Common uses
Hypertension0, Diabetic nephropathy0, Stroke prevention in LVH0, Heart failure (ACE-intolerant)0
Pharmacy
Starting dose
50 mg PO daily (25 mg in volume depletion or hepatic impairment)
Preparations
25 mg, 50 mg, 100 mg tablets
US FDA Max
100 mg/d
Pharmacology
Routes
Oral
Onset
BP effect 1-2 weeks; antihypertensive peak 3-6 weeks
Duration
24 hours
Half-life
2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174[1]
Bioavailability
~33% (extensive first-pass via CYP2C9 and CYP3A4)[1]
Pregnancy
Contraindicated in pregnancy (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection[1]
Legal status
Rx-only in US
Purported mechanism
Losartan is a selective AT1 angiotensin-II receptor antagonist; blocking AT1 produces vasodilation, decreased aldosterone, and reduced sodium retention without the bradykinin accumulation that drives ACE-inhibitor cough.0 Active metabolite EXP3174 is ~10-40-fold more potent than the parent and accounts for most of the antihypertensive effect; CYP2C9 polymorphism affects conversion[1].
References
edit- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Cozaar (losartan potassium), Merck, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020386s059lbl.pdf