Pronunciation: EP-roe-SAR-tan MES-i-late
Class: Angiotensin II receptor antagonist
- Tablets, oral 400 mg
- Tablets, oral 600 mg
Antagonizes the effect of angiotensin II (vasoconstriction and aldosterone secretion) by blocking the angiotensin II receptor (AT 1 receptor) in vascular smooth muscle and the adrenal gland, producing decreased BP.
Bioavailability is approximately 13%. T max is 1 to 2 h.
Approximately 98% is protein bound. Vd is 308 L (at steady state).
Metabolized to inactive metabolites.
Terminal elimination half-life was 20 h. After oral dosing, approximately 90% is recovered in feces and approximately 7% in the urine (80% as unchanged drug). Cl is approximately 48.5 L/h.
1 to 2 h.
2 to 3 wk.
Special PopulationsRenal Function Impairment
AUC increased 70% to 90% and C max increased 30% to 50% in patients with moderate or severe renal impairment, respectively. No dosage adjustment needed.Hepatic Function Impairment
AUC increased approximately 40% in men with decreased hepatic function. No dosage adjustment needed.Elderly
AUC, C max , and T max increased approximately 2-fold. No dosage adjustment needed.Children
Pharmacokinetics have not been studied in patients younger than 18 y.Gender
There were no differences in the pharmacokinetics and plasma protein binding between men and women.Race
Oral clearance and steady-state volume of distribution were not influenced by race.
Indications and Usage
Treatment of hypertension.
None well documented.
Dosage and AdministrationAdults
PO 400 to 800 mg/day divided once or twice daily; usual starting dosage is 600 mg/day when used as monotherapy in patients who are not volume depleted.
- May administer with or without food.
- The antihypertensive effect is largely attained within 2 to 3 wk.
- If the antihypertensive effect is inadequate, a twice-daily regimen at the same total daily dose or an increase in dose may give a more satisfactory response.
- May administer with other antihypertensive agents.
Store between 68° and 77°F.
Drug InteractionsACE inhibitors (eg, ramipril)
The risk of hyperkalemia and renal dysfunction may be increased. Use with caution and closely monitor renal function and potassium levels.Aliskiren
The risk of hyperkalemia may be increased, particularly in diabetic patients. Coadministration is not recommended in diabetic patients. If coadministration cannot be avoided, closely monitor potassium concentrations and renal function.Lithium
Increased lithium concentrations and toxicity may occur during coadministration. Adjust the lithium dose as needed.NSAIDs (eg, celecoxib, ibuprofen)
The antihypertensive effect of eprosartan may be decreased. Coadministration of NSAIDs with eprosartan in patients who are elderly or volume-depleted (including those on diuretics), or have decreased renal function may result in deterioration of renal function.Potassium preparations
Eprosartan may decrease the renal excretion of potassium, increasing the risk of hyperkalemia and possibly resulting in cardiac arrhythmias or cardiac arrest. Adjust potassium preparation dose as needed.Potassium-sparing diuretics (eg, spironolactone)
The risk of hyperkalemia may be increased. Adjust treatment as needed.Trimethoprim
The risk of hyperkalemia, especially in elderly patients, may be increased. Adjust eprosartan dose as needed.
Fatigue (2%); depression (1%).
Abdominal pain (2%).
Upper respiratory tract infection (8%); coughing, pharyngitis, rhinitis (4%).
Arthralgia, viral infection (2%).
When pregnancy is detected, discontinue eprosartan mesylate as soon as possible. Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus.
Monitor BP at regular intervals.
Category D .
Safety and efficacy not established.
In patients with unilateral or bilateral renal artery stenosis, increases in serum creatinine or BUN may occur.
Hypotension in volume- and/or salt-depleted patients
Symptomatic hypotension may occur after eprosartan initiation in intravascularly volume- or salt-depleted patients (eg, those treated with high-dose diuretics). Correct these conditions prior to administration or use a lower starting dose.
Use with caution in patients whose renal function may depend on the activity of the renin-angiotensin-aldosterone system (eg, patients with severe CHF); use may be associated with oliguria, progressive azotemia, acute renal failure, and/or death.
No data reported.
- Advise women of childbearing age about the consequence of exposure to eprosartan during pregnancy. Ask these patients to report pregnancies to their health care provider as soon as possible.
- Advise patients to take eprosartan with or without food.
- If BP is not controlled with this medicine alone, inform patients that diuretics or other BP medicines may be prescribed.
- Inform patients that lifestyle changes (eg, stopping smoking, losing weight, exercising, limiting salt in diet) also help to lower BP.
- Instruct patients that achievement of maximum BP reduction will usually take about 2 to 3 wk.
- Instruct patients in methods of fall prevention, including rising slowly and sitting on the side of the bed before standing, especially early in therapy.
- Instruct patients to report symptoms of weakness, fatigue, dizziness, or light-headedness to their health care provider.
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