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Eprosartan Mesylate

Pronunciation: EP-roe-SAR-tan MES-i-late
Class: Angiotensin II receptor antagonist

Trade Names

Teveten
- Tablets, oral 400 mg
- Tablets, oral 600 mg

Pharmacology

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.

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Pharmacokinetics

Absorption

Bioavailability is approximately 13%. T max is 1 to 2 h.

Distribution

Approximately 98% is protein bound. Vd is 308 L (at steady state).

Metabolism

Metabolized to inactive metabolites.

Elimination

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.

Onset

1 to 2 h.

Peak

2 to 3 wk.

Special Populations

Renal 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.

Contraindications

None well documented.

Dosage and Administration

Adults

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.

General Advice

  • 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.

Storage/Stability

Store between 68° and 77°F.

Drug Interactions

ACE 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.

Adverse Reactions

CNS

Fatigue (2%); depression (1%).

GI

Abdominal pain (2%).

Genitourinary

UTI (1%).

Metabolic

Hypertriglyceridemia (1%).

Respiratory

Upper respiratory tract infection (8%); coughing, pharyngitis, rhinitis (4%).

Miscellaneous

Arthralgia, viral infection (2%).

Precautions

Warnings

Fetal toxicity

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

Monitor BP at regular intervals.


Pregnancy

Category D .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

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.

Renal effects

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.

Overdosage

Symptoms

No data reported.

Patient Information

  • 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.

Copyright © 2009 Wolters Kluwer Health.

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