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Eprosartan

Eprosartan: A Selective ARB for Hypertension and Cardiovascular Protection

Introduction

Hypertension, commonly referred to as high blood pressure, affects over a billion people worldwide and is a major risk factor for cardiovascular disease, stroke, renal failure, and premature death. Managing hypertension requires a multi-faceted approach, including lifestyle interventions and pharmacological agents. Among these agents, angiotensin II receptor blockers (ARBs) have carved out a significant therapeutic niche due to their efficacy and favorable safety profile.

Eprosartan is one such ARB, approved for the treatment of hypertension and showing promise in the reduction of cardiovascular events. Though less commonly prescribed compared to other ARBs like losartan or telmisartan, eprosartan offers unique pharmacological features that warrant attention.

Eprosartan

  • Generic Name: Eprosartan

  • Drug Class: Angiotensin II Receptor Blocker (ARB)

  • Brand Names: Teveten®, Teveten HCT® (with hydrochlorothiazide)

  • Molecular Formula: C23H24N2O4S

  • Route of Administration: Oral

  • FDA Approval: 1997

Eprosartan selectively inhibits the angiotensin II type 1 (AT1) receptor, preventing angiotensin II from exerting its vasoconstrictive, sodium-retentive, and pro-inflammatory effects. The result is vasodilation, reduced blood pressure, and decreased cardiovascular strain.

Mechanism of Action

Eprosartan works by blocking the AT1 receptor, the primary site where angiotensin II exerts its physiological effects, such as:

  • Vasoconstriction

  • Aldosterone secretion (leading to sodium and water retention)

  • Sympathetic nervous system activation

  • Vascular smooth muscle hypertrophy

  • Renal sodium reabsorption

By antagonizing AT1 receptors, Eprosartan:

  • Lowers systemic vascular resistance.

  • Reduces preload and afterload.

  • Improves arterial compliance.

  • Inhibits the progression of left ventricular hypertrophy (LVH) and renal disease.

Unlike ACE inhibitors, ARBs like eprosartan do not interfere with bradykinin metabolism, resulting in a lower incidence of cough and angioedema.

Pharmacokinetics and Pharmacodynamics

  • Absorption: ~13% oral bioavailability

  • Time to Peak Plasma Concentration: 1–3 hours

  • Half-life: ~5–9 hours

  • Protein Binding: ~98%

  • Metabolism: Not significantly metabolized; excreted unchanged

  • Excretion: Feces (61%), urine (37%)

Eprosartan is distinct from many ARBs in that it is not a prodrug and does not undergo hepatic metabolism, reducing the likelihood of drug-drug interactions and making it suitable for patients with liver dysfunction.

Clinical Indications

1. Essential Hypertension

Eprosartan is approved as monotherapy or in combination with other antihypertensives for the management of high blood pressure. It effectively reduces systolic and diastolic pressure and has been shown to be effective across a broad range of patients, including:

  • Elderly individuals

  • Diabetics

  • Those with metabolic syndrome

2. Hypertension with High Cardiovascular Risk

Eprosartan has demonstrated benefits in patients with elevated risk for cardiovascular events, particularly through blood pressure control and vascular remodeling.

3. Renal Protection

Like other ARBs, eprosartan may slow the progression of nephropathy in hypertensive patients with proteinuria or diabetes, though direct evidence is more extensive for drugs like losartan or irbesartan.

4. Combination Therapy

Available as Eprosartan + Hydrochlorothiazide (Teveten HCT), the combination offers additive antihypertensive effects through volume reduction and vasodilation.

Dosing Guidelines

  • Initial Dose: 600 mg once daily

  • Maximum Dose: 800 mg/day (either as a single dose or in two divided doses)

Dose adjustments are not typically required for elderly patients or those with mild-to-moderate renal impairment. In patients with hepatic impairment, cautious use is advised even though the drug is not extensively metabolized.

Clinical Trials and Efficacy

MOSES Trial (Morbidity and Mortality After Stroke, Eprosartan Compared with Nitrendipine for Secondary Prevention)

  • Compared eprosartan to nitrendipine in patients with a history of stroke or transient ischemic attack (TIA).

  • Eprosartan showed significant reduction in recurrent cerebrovascular and cardiovascular events, despite similar blood pressure control.

Conclusion: Eprosartan may have protective vascular effects beyond blood pressure lowering.

Comparative Effectiveness

While all ARBs function via similar mechanisms, Eprosartan differs in structure and pharmacokinetics. Compared to losartan:

  • Not a prodrug

  • No active metabolites

  • Less hepatic metabolism

  • Greater affinity for AT1 receptor

These differences may influence individual response, tolerability, and interaction profiles.

Adverse Effects

Eprosartan is generally well-tolerated, with a side effect profile similar to placebo in many trials.

Common Side Effects

  • Headache

  • Dizziness

  • Fatigue

  • Nausea

  • Cough (rare)

Serious but Rare Reactions

  • Angioedema (very rare with ARBs compared to ACE inhibitors)

  • Hyperkalemia

  • Renal function impairment in susceptible individuals (e.g., those with bilateral renal artery stenosis)

  • Hypotension, especially in volume-depleted individuals

Contraindications and Cautions

  • Pregnancy: Contraindicated due to risk of fetal toxicity (especially in 2nd and 3rd trimesters)

  • Severe hepatic impairment

  • Bilateral renal artery stenosis

  • Known hypersensitivity to eprosartan or other ARBs

Monitoring is essential in patients with comorbid kidney disease or those on potassium-sparing diuretics to prevent hyperkalemia.

Drug Interactions

Eprosartan has fewer interactions compared to drugs metabolized by the CYP450 system, but caution is advised with:

  • Potassium supplements or K-sparing diuretics (risk of hyperkalemia)

  • NSAIDs (may impair renal function and reduce antihypertensive effect)

  • Lithium (can increase lithium toxicity)

  • Diuretics (can cause excessive BP reduction if patient is volume-depleted)

Use in Special Populations

Elderly

  • Well-tolerated, no dose adjustment required

  • Effective even in patients with isolated systolic hypertension

Renal Impairment

  • Dose adjustment typically not required

  • Monitor serum creatinine and potassium

Hepatic Impairment

  • Use with caution; limited data on severe impairment

Pediatrics

  • Not approved for use in children or adolescents

Eprosartan vs. Other ARBs

Property Eprosartan Losartan Valsartan Telmisartan
Prodrug No Yes No No
Hepatic metabolism Minimal CYP2C9 Low Low
Half-life (h) 5–9 2 6 24
Cardiovascular Outcomes Evidence Moderate (MOSES) Extensive (LIFE) Moderate Strong (ONTARGET)

Though not as extensively studied as telmisartan or losartan, eprosartan remains a viable option, especially in patients needing minimal hepatic drug processing.

Patient Counseling Points

  • Take at the same time each day, with or without food.

  • Do not use during pregnancy. Discuss contraception if of childbearing age.

  • Report symptoms of dizziness, swelling, or rapid weight gain.

  • Avoid salt substitutes containing potassium.

  • Regular monitoring of blood pressure, kidney function, and potassium is important.

  • Inform all healthcare providers of its use, especially before surgery or new medications.

Eprosartan in the Context of Global Guidelines

While not mentioned as often as other ARBs, Eprosartan is endorsed by several international guidelines (e.g., JNC-8, ESC/ESH, NICE) under the ARB category for:

  • First-line therapy in patients intolerant to ACE inhibitors.

  • Use in comorbid diabetes, heart failure, or chronic kidney disease.

Future Perspectives

While newer ARBs and novel antihypertensives continue to emerge, eprosartan remains a relevant option, particularly for:

  • Patients requiring non-hepatic metabolism

  • Those who are ACE inhibitor-intolerant

  • Potential use in stroke prevention, based on evidence from MOSES

Research may yet further elucidate non-hemodynamic benefits, such as anti-inflammatory effects, endothelial protection, and organ-specific advantages.

Conclusion

Eprosartan stands as a selective, well-tolerated ARB with proven efficacy in lowering blood pressure and potential benefits in cardiovascular protection. Though less widely used than some of its counterparts, it remains a clinically valuable option, especially in specific patient populations needing tailored therapy. Its favorable safety profile, minimal drug interactions, and evidence in stroke prevention make it a strong contender for inclusion in the therapeutic arsenal against hypertension.