Olmesartan

Benicar is indicated for the treatment of hypertension in adults and children six years of age and older, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes including the class to which this drug principally belongs. There are no controlled trials demonstrating risk reduction with Benicar. Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise, and limited sodium intake. Many patients will require more than one drug to achieve blood pressure goals.

Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation and renal reabsorption of sodium. Olmesartan blocks the vasoconstrictor effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT 1 receptor in vascular smooth muscle. Its action is, therefore, independent of the pathways for angiotensin II synthesis. An AT 2 receptor is found also in many tissues, but this receptor is not known to be associated with cardiovascular homeostasis. Olmesartan has more than a 12,500-fold greater affinity for the AT 1 receptor than for the AT 2 receptor.

Indication Starting Dose Dose Range Adult Hypertension 20 mg once daily 20 - 40 mg once daily Pediatric Hypertension (6 years of age and older) 20 to <35 kg 20 to <35 kg 10 mg once daily 10 - 20 mg once daily ≥ 35 kg ≥ 35 kg 20 mg once daily 20 - 40 mg once daily

Do not co-administer aliskiren with Benicar in patients with diabetes.

Boxed warning (fetal toxicity): When pregnancy is detected, discontinue Benicar as soon as possible. Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. Avoid fetal (in utero) exposure. Use of Benicar in children <1 year of age is not recommended. Observe for signs and symptoms of hypotension in volume- or salt-depleted patients with treatment initiation. Monitor for worsening renal function in patients with renal impairment. Sprue-like enteropathy has been reported. Consider alternative antihypertensive therapy in cases where no other etiology is found.

The most common adverse reaction in adults was dizziness (3%).

Agents increasing potassium levels may lead to increase in serum potassium. NSAID use may lead to increased risk of renal impairment and loss of antihypertensive effect. Dual inhibition of the renin-angiotensin system: Increased risk of renal impairment, hypotension, and hyperkalemia. Lithium: Increases in serum lithium concentrations and lithium toxicity. Colesevelam hydrochloride: Consider administering olmesartan at least 4 hours before colesevelam hydrochloride dose.

Store at 20-25°C (68-77°F).