For the treatment of hypertension.
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<sub>1</sub> receptor in vascular smooth muscle. Its action is, therefore, independent of the pathways for angiotensin II synthesis. Olmesartan has more than a 12,500-fold greater affinity for the AT<sub>1</sub> receptor than for the AT<sub>2</sub> receptor.
Symptoms of overdose include dehydration (dry mouth, excessive thirst, muscle pain or cramps, nausea and vomiting, weakness), dizziness, low blood pressure, and slow or irregular heartbeat.
Bioavailability is about 26%. Food does not affect the bioavailability of olmesartan.
Approximately 13 hours
* 17 L
* Total plasma cl=1.3 L/h * Renal cl=0.6 L/h