Trade Names:Benicar- Tablets 5 mg- Tablets 20 mg- Tablets 40 mg
Blocks vasoconstrictor effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT 1 receptor in vascular smooth muscle.
Rapidly and completely absorbed from the GI tract. The steady state is 3 to 5 days. The bioavailability is approximately 26% The T max is 1 to 2 h.
The Vd is 17 L. 99% is protein bound.
About 35% to 50% is eliminated through urine. The remainder is eliminated in feces via bile (50% to 65% recovered).
The total plasma clearance is 1.3 L/h. Renal clearance is 0.6 L/h. The t ½ is approximately 13 h.
Ccr is less than 20 mL/min. AUC is approximately tripled.Hepatic Function Impairment
AUC increased by approximately 60%. C max increased.Elderly
AUC increased by 33%, and there is a 30% reduction in renal clearance.Gender
AUC increased 10% and C max increased by 15% in women. Minor differences.
Treatment of hypertension.
PO Start with 20 mg once daily; after 2 wk, dosage may be increased to 40 mg/day if further reduction in BP is needed.
Store tablets at controlled room temperature (68° to 77°F).
None well documented.
Plasma concentrations may be increased by olmesartan, resulting in an increase in the pharmacologic and adverse effects of lithium.
Dizziness; fatigue; vertigo; insomnia.
Abdominal pain; dyspepsia; gastroenteritis; nausea.
Hypercholesterolemia; hyperlipemia; hyperuricemia.
Chest pain; pain; peripheral edema; arthritis; myalgia; skeletal pain.
When used in pregnancy during the second and third trimesters, drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. When pregnancy is detected, discontinue therapy as soon as possible.
Category C (first trimester); Category D (second and third trimester). Can cause injury or death to the fetus if used during second or third trimester.
Safety and efficacy not established.
In patients whose renal function may depend on activity of the renin-angiotensin-converting enzyme system (eg, patients with severe CHF), treatment with olmesartan may be associated with oliguria and progressive azotemia, rarely resulting in acute renal failure or death.
Hypotension, tachycardia, bradycardia.
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