Eprosartan Mesylate
Pronouncation: (eh-pro-SAHR-tan MAL-ee-ate)Class: Angiotensin II receptor antagonist
Trade Names:
Teveten
- Tablets 400 mg
- Tablets 600 mg
Pharmacology
Feedback for Eprosartan Mesylate
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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 48.5ߙL/h.
Onset
1 to 2 h.
Peak
2 to 3 wk.
Special Populations
Renal Function ImpairmentAUC 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 ImpairmentAUC increased approximately 40%. No dosage adjustment needed.
ElderlyAUC, 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
AdultsPO 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
LithiumPlasma 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
WarningsPregnancyWhen 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 2ߙto 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.
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