Olmesartan Medoxomil
Pronouncation: (ole-mih-SAR-tan meh-DOX-oh-mill)Class: Angiotensin II receptor antagonist
Trade Names:
Benicar
- Tablets 5 mg
- Tablets 20 mg
- Tablets 40 mg
Pharmacology
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Blocks vasoconstrictor effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT 1 receptor in vascular smooth muscle.
Pharmacokinetics
Absorption
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.
Distribution
The Vd is 17 L. 99% is protein bound.
Elimination
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.
Special Populations
Renal Function ImpairmentCcr is less than 20 mL/min. AUC is approximately tripled.
Hepatic Function ImpairmentAUC increased by approximately 60%. C max increased.
ElderlyAUC increased by 33%, and there is a 30% reduction in renal clearance.
GenderAUC increased 10% and C max increased by 15% in women. Minor differences.
Indications and Usage
Treatment of hypertension.
Contraindications
Standard considerations.
Dosage and Administration
AdultsPO Start with 20 mg once daily; after 2 wk, dosage may be increased to 40 mg/day if further reduction in BP is needed.
Storage/Stability
Store tablets at controlled room temperature (68° to 77°F).
Drug Interactions
None well documented.
Laboratory Test Interactions
LithiumPlasma concentrations may be increased by olmesartan, resulting in an increase in the pharmacologic and adverse effects of lithium.
Adverse Reactions
Cardiovascular
Tachycardia.
CNS
Dizziness; fatigue; vertigo; insomnia.
Dermatologic
Rash.
GI
Abdominal pain; dyspepsia; gastroenteritis; nausea.
Genitourinary
UTI.
Metabolic
Hypercholesterolemia; hyperlipemia; hyperuricemia.
Miscellaneous
Chest pain; pain; peripheral edema; arthritis; myalgia; skeletal pain.
Precautions
WarningsPregnancyWhen 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. |
Pregnancy
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.
Lactation
Undetermined.
Children
Safety and efficacy not established.
Renal Function
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.
Overdosage
Symptoms
Hypotension, tachycardia, bradycardia.
Patient Information
- Advise patient to take once daily as prescribed, without regard to meals, but to take with food if GI upset occurs.
- Advise patient to take each dose at about the same time each day.
- Inform patient that the drug controls, but not does cure, hypertension and to continue taking the drug as prescribed, even when BP is not elevated.
- Caution patient not to change the dose or stop taking unless advised by health care provider.
- Instruct patient to continue taking other BP medications as prescribed by health care provider.
- Instruct patient in BP and pulse measurement skills.
- Advise patient to monitor and record BP and pulse at home and to inform health care provider should abnormal measurements be noted. Advise patient to take record of BP and pulse to each follow-up visit.
- Instruct patient to lie or sit down if experiencing dizziness or lightheadedness when standing.
- Caution patient that inadequate fluid intake, excessive perspiration, diarrhea, or vomiting can lead to an excessive fall in BP resulting in lightheadedness or fainting.
- Emphasize to hypertensive patient the importance of the following other modalities on BP: weight control, regular exercise, smoking cessation, moderate intake of alcohol and salt.
- Instruct patient to stop taking drug and immediately report any of the following symptoms to health care provider: fainting; swelling of the face, lips, eyelids, or tongue.
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