Olmesartan
Olmesartan (medoxomil)
Benicar
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Summary
Pharmacy
Starting dose
20 mg PO once daily; titrate to 40 mg/d after 2 weeks if needed
Preparations
5, 20, 40 mg tablets
US FDA Max
40 mg/d
Pharmacology
Routes
Oral
Onset
BP effect 1-2 weeks; max at 2-3 weeks
Duration
24 hours
Half-life
~13 hours[1]
Bioavailability
~26% (oral; prodrug hydrolyzed by intestinal esterases to active olmesartan; not affected by food)[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
Olmesartan medoxomil is a prodrug hydrolyzed to the active 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 Sprue-like enteropathy with chronic diarrhea and villous atrophy is a well-described class-specific adverse effect first reported with olmesartan in 2013 (FDA safety advisory) and now recognized for the ARB class; reversible on discontinuation[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Benicar (olmesartan medoxomil), Daiichi Sankyo, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021286s044lbl.pdf