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Journal of Human Hypertension (2002) 16 (Suppl 2), S13S16
2002 Nature Publishing Group All rights reserved 0950-9240/02 $25.00www.nature.com/jhhThe new oral angiotensin II antagonist
olmesartan medoxomil: a concise
overviewHR BrunnerDivision of Hypertension and Vascular Medicine, Centre Hospitalier Universitaire Vaudois, Lausanne,
SwitzerlandThe new orally active angiotensin II (A II) type-1 receptor
antagonist olmesartan medoxomil is a prodrug, which
is rapidly converted in vivo to the active metabolite,
olmesartan. The pharmacology, antihypertensive efficacy and safety of olmesartan medoxomil and/or the
pharmacologically active metabolite, olmesartan, have
been evaluated in both non-clinical and clinical models.
Orally administered olmesartan medoxomil is rapidly
absorbed from the gastrointestinal tract and converted
during absorption to olmesartan, which is subsequently
excreted without further metabolism. Peak plasma concentrations of olmesartan occur 13 h after administration, after which concentrations decrease with an
elimination half-life of 1015 h. The absolute bioavailability of olmesartan from olmesartan medoxomil tablets is 28.6%. In a single-dose crossover study in 16
patients with mild-to-moderate hypertension receiving a
sodium-restricted diet, statistically significant loweringKeywords: olmesartan medoxomil; pharmacokinetics; efficacy; safety; tolerabilityof mean 24-h blood pressure was seen at doses of 10
80 mg. Evaluation of 14 phase II/III studies has confirmed the antihypertensive efficacy of olmesartan
medoxomil in over 3500 patients who received the drug
for up to 2 years. Frequencies of adverse events during
treatment with olmesartan medoxomil and placebo are
similar, with no evidence of a dose response. There are
no clinically significant effects on laboratory parameters, and the drug-interaction potential of olmesartan
medoxomil is low. Current indications are that olmesartan medoxomil is a true once-daily, orally active A II
antagonist with good antihypertensive efficacy and a
favourable adverse-event profile. Clinical pharmacodynamic and efficacy studies support a usual dose of
20 mg once daily, increasing to 40 mg if needed.
Journal of Human Hypertension (2002) 16 (Suppl 2), S13
S16. DOI: 10.1038/sj/jhh/1001391IntroductionPharmacologyThe potentially harmful pressor effect of angiotensin
II (A II) has long been recognized, and A II blockade,
first using angiotensin-converting enzyme (ACE)
inhibitors and more recently with A II type-1 receptor (AT1 receptor) antagonists, has been an exciting
development that has completely changed the management of clinical hypertension and congestive
heart failure.1 Orally active olmesartan medoxomil
is among the latest A II antagonists to be developed.
Olmesartan medoxomil is a prodrug that...