Angiotensin II Antagonists

Treatment of hypertension; may be used alone or in combination with other antihypertensives

Hypersensitivity to eprosartan or any component; sensitivity to other A-II receptor antagonists; bilateral renal artery stenosis; primary hyperaldosteronism; pregnancy (2nd and 3rd trimester)

Avoid use or use a smaller dose in patients who are volume depleted; correct depletion first. Deterioration in renal function can occur with initiation. Use with caution in unilateral renal artery stenosis and pre-existing renal insufficiency; significant aortic/mitral stenosis. Safety and efficacy not established in pediatric patients.

1% to 10%:

Central nervous system: Fatigue (2%), depression (1%)

Endocrine & metabolic: Hypertriglyceridemia (1%)

Gastrointestinal: Abdominal pain (2%)

Genitourinary: Urinary tract infection (1%)

Respiratory: Upper respiratory tract infection (8%), rhinitis (4%), pharyngitis (4%), cough (4%)

Miscellaneous: Viral infection (2%), injury (2%)

<1% (Limited to important or life-threatening symptoms): Alcohol intolerance, weakness, substernal chest pain, facial edema, peripheral edema, fatigue, fever, hot flushes, influenza-like symptoms, malaise, rigors, pain, angina pectoris, bradycardia, abnormal EKG, extrasystoles, atrial fibrillation, hypotension, tachycardia, palpitations, anorexia, constipation, dry mouth, esophagitis, flatulence, gastritis, gastroenteritis, gingivitis, nausea, periodontitis, toothache, vomiting, anemia, purpura, increased transaminases, increased creatine phosphokinase, diabetes mellitus, glycosuria, gout, hypercholesterolemia, hyperglycemia, hyperkalemia, hypokalemia, hyponatremia, arthritis, aggravated arthritis, arthrosis, skeletal pain, tendonitis, back pain, anxiety, ataxia, insomnia, migraine, neuritis, nervousness, paresthesia, somnolence, tremor, vertigo, herpes simplex, otitis externa, otitis media, asthma, epistaxis, eczema, furunculosis, pruritus, rash, maculopapular rash, increased sweating, conjunctivitis, abnormal vision, xerophthalmia, tinnitus, albuminuria, cystitis, hematuria, micturition frequency, polyuria, renal calculus, urinary incontinence, leg cramps, peripheral ischemia, increases in BUN or creatinine, leukopenia, neutropenia, thrombocytopenia

Lithium: Risk of toxicity may be increased by eprosartan; monitor lithium levels.

Potassium-sparing diuretics (amiloride, potassium, spironolactone, triamterene): Increased risk of hyperkalemia.

Potassium supplements may increase the risk of hyperkalemia.

Trimethoprim (high dose) may increase the risk of hyperkalemia.

Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Eprosartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is therefore independent of the pathways for angiotensin II synthesis. Blockade of the renin-angiotensin system with ACE inhibitors, which inhibit the biosynthesis of angiotensin II from angiotensin I, is widely used in the treatment of hypertension. ACE inhibitors also inhibit the degradation of bradykinin, a reaction also catalyzed by ACE. Because eprosartan does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Whether this difference has clinical relevance is not yet known. Eprosartan does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.

Half-life: 5-7 hours

Time to peak serum concentration: 1-3 hours; clearance: 7.9 L/hour

Adults: Oral: Dosage must be individualized; can administer once or twice daily with total daily doses of 400-800 mg. Usual starting dose is 600 mg once daily as monotherapy in patients who are euvolemic. Limited clinical experience with doses >800 mg.

Dosage adjustment in hepatic impairment: No starting dosage adjustment is necessary; however, carefully monitor the patient

Elderly: No starting dosage adjustment is necessary; however, carefully monitor the patient

The angiotensin II receptor antagonists appear to have similar indications as the ACE inhibitors. While these drugs have been shown to be effective in treating hypertension, their efficacy in heart failure is being vigorously evaluated. The angiotensin II antagonists are especially useful in providing an alternative therapy in those patients who have intractable cough in response to ACE-inhibitor therapy. Similar to ACE inhibitors, pre-existing volume depletion caused by diuretic therapy may potentiate hypotension in response to angiotensin II antagonists.

No information available to require special precautions

No effects or complications reported

Tablet: 400 mg (scored), 600 mg