DrugindexOnline^{2nd edition}

Pronouncation: (eh-pro-SAHR-tan MAL-ee-ate)
Class: Angiotensin II receptor antagonist

Trade Names:
Teveten
- Tablets 400 mg
- Tablets 600 mg

Mechanism of Action

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.

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

½ is 5 to 9 h. Approximately 90% recovered in the urine 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 approximately two-fold, and C _max increased 50% and 30% in those with moderate or severe renal function impairment, respectively. Unbound fraction increased by 35% and 59%. No dosage adjustment needed.

Hepatic Function Impairment

AUC increased approximately 40%. No dosage adjustment needed.

Elderly

AUC, C _max , and T _max increased approximately two-fold. No dosage adjustment needed.

Indications and Usage

Treatment of hypertension.

Contraindications

Standard considerations.

Dosage and Administration

Adults

PO 400 to 800 mg/day; usual starting dose 600 mg/day.

Storage/Stability

Store at room temperature in a tightly closed container.

Drug Interactions

None well documented.

Laboratory Test Interactions

Lithium

Plasma concentrations may be increased by eprosartan, resulting in an increase in the pharmacologic and adverse effects of lithium.

Adverse Reactions

Cardiovascular

Abnormal ECG; extrasystoles; atrial fibrillation.

CNS

Fatigue; depression.

GI

Abdominal pain.

Genitourinary

UTI.

Metabolic

Hypertriglyceridemia; hyperkalemia; hypokalemia.

Respiratory

Upper respiratory tract infection; rhinitis; pharyngitis; coughing.

Miscellaneous

Arthralgia.

Precautions

Warnings Pregnancy 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.

Pregnancy

Category C (first trimester); Category D (second and third trimesters).

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

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 death.

Patient Information

• Instruct patient to take the medication as prescribed at the same time each day.
• Inform patient that eprosartan controls but does not cure hypertension.
• Caution patient to take the dose exactly as prescribed and not to stop taking the medication even if feeling better.
• Instruct patient not to increase or decrease the dosage.
• Instruct patient that achievement of maximum BP reduction will usually take about 2 to 3 wk.
• Instruct family and patient in BP and pulse measurement skills.
• Caution patient to call primary health care provider should abnormal measurements occur.
• Instruct patient in methods of fall prevention including rising slowly and sitting on the side of the bed before standing, especially early in therapy.
• Inform patient of the importance of adjunct therapies such as dietary planning, regular exercise program, weight reduction, low sodium diet, alcohol reduction, smoking cessation, and stress management.
• Instruct patient to report symptoms of weakness, fatigue, dizziness, or lightheadedness to health care provider.
• Caution patient to notify health care provider or dentist of eprosartan use prior to surgery or treatment.