Usage
- Eprosartan is primarily prescribed for the treatment of essential hypertension (high blood pressure). It can be used as monotherapy or in combination with other antihypertensive medications like thiazide diuretics (e.g., hydrochlorothiazide) or calcium channel blockers (e.g., nifedipine). It has also been used for diabetic nephropathy and congestive heart failure (CHF).
- Pharmacological Classification: Angiotensin II Receptor Blocker (ARB)
- Mechanism of Action: Eprosartan blocks the action of angiotensin II, a hormone that causes blood vessels to constrict (narrow). By blocking angiotensin II receptors, eprosartan causes vasodilation (widening of blood vessels), which lowers blood pressure.
Alternate Names
- International Nonproprietary Name (INN): Eprosartan
- Brand Names: Teveten, Teveten HCT (combined with hydrochlorothiazide)
How It Works
- Pharmacodynamics: Eprosartan selectively binds to the angiotensin II type 1 (AT1) receptor, blocking the vasoconstrictor and aldosterone-secreting effects of angiotensin II. This results in decreased peripheral resistance and blood pressure. It does not affect bradykinin levels, which may contribute to a lower incidence of cough compared to ACE inhibitors.
- Pharmacokinetics: Eprosartan is well-absorbed orally. It is highly protein-bound and undergoes minimal metabolism in the liver. It is primarily excreted unchanged in the bile and to a lesser extent in the urine. The elimination half-life is approximately 5-9 hours.
- Mode of Action: Eprosartan acts as a competitive antagonist at the AT1 receptor, preventing angiotensin II from binding and exerting its effects.
- Receptor Binding/Enzyme Inhibition: Binds to AT1 receptors. Does not inhibit CYP450 enzymes.
- Elimination Pathways: Primarily biliary excretion, some renal excretion.
Dosage
Standard Dosage
Adults:
- Initial: 600 mg orally once daily, in patients without intravascular volume depletion.
- Maintenance: 400-800 mg orally per day, taken once daily or in two divided doses. Twice-daily dosing may enhance the antihypertensive effect.
Children:
- Safety and efficacy not established. Not recommended for use in children and adolescents under 18 years of age.
Special Cases:
- Elderly Patients: No initial dosage adjustment is usually needed.
- Patients with Renal Impairment: No initial dosage adjustment is typically needed for mild to moderate impairment. For moderate or severe renal impairment (creatinine clearance <60 mL/min), the maximum dose is 600 mg daily.
- Patients with Hepatic Dysfunction: No initial dosage adjustment is typically needed for mild to moderate impairment. Contraindicated in severe hepatic impairment.
- Patients with Comorbid Conditions: Patients with diabetes should not use eprosartan with aliskiren. Caution should be used in patients with heart failure, aortic or mitral valve stenosis, and those on a low-salt diet.
Clinical Use Cases
Eprosartan’s primary use is in managing hypertension, and it is not typically administered in situations like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Other medications are generally preferred in these settings for rapid blood pressure control or specific hemodynamic goals.
Dosage Adjustments
Dose adjustments may be necessary based on blood pressure response and renal or hepatic function. If once-daily dosing does not adequately control blood pressure, twice-daily dosing at the same total daily dose or an increase in the total daily dose may be considered.
Side Effects
Common Side Effects:
- Dizziness
- Lightheadedness
- Headache
- Fatigue
- Runny or stuffy nose
- Cough
- Upper respiratory tract infection
Rare but Serious Side Effects:
- Angioedema (swelling of face, lips, tongue, throat, or extremities)
- Hypotension (low blood pressure)
- Renal impairment
- Hyperkalemia (high potassium levels)
Long-Term Effects:
Potential long-term effects are primarily related to uncontrolled hypertension if the medication is not effective or is not taken as prescribed.
Adverse Drug Reactions (ADR):
Angioedema and acute renal failure are serious ADRs requiring prompt medical attention.
Contraindications
- Hypersensitivity to eprosartan or any of its components
- Second and third trimesters of pregnancy
- Severe hepatic impairment
- Bilateral renal artery stenosis
- Concomitant use of aliskiren in patients with diabetes or renal impairment (GFR <60 mL/min/1.73 m²)
Drug Interactions
- Aliskiren: Increased risk of hypotension, hyperkalemia, and renal impairment. Contraindicated in patients with diabetes or renal impairment.
- Lithium: Increased lithium levels. Monitor lithium levels closely.
- Potassium-sparing diuretics (e.g., spironolactone, amiloride): Increased risk of hyperkalemia.
- Potassium supplements: Increased risk of hyperkalemia.
- NSAIDs: May reduce the antihypertensive effect of eprosartan and increase the risk of renal impairment.
- Other antihypertensives: Additive hypotensive effects.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: D (first trimester); X (second and third trimesters) - contraindicated
- Fetal Risks: May cause fetal injury or death, especially during the second and third trimesters.
- Breastfeeding: Not recommended. Eprosartan may pass into breast milk.
Drug Profile Summary
- Mechanism of Action: Angiotensin II receptor blocker (ARB)
- Side Effects: Dizziness, lightheadedness, headache, fatigue, cough, angioedema (rare), hypotension (rare), renal impairment (rare), hyperkalemia (rare)
- Contraindications: Hypersensitivity, pregnancy (2nd and 3rd trimesters), severe hepatic impairment, bilateral renal artery stenosis, concomitant use of aliskiren in patients with diabetes or renal impairment.
- Drug Interactions: Aliskiren, lithium, potassium-sparing diuretics, potassium supplements, NSAIDs.
- Pregnancy & Breastfeeding: Contraindicated in pregnancy (2nd and 3rd trimesters). Not recommended during breastfeeding.
- Dosage: Adults: 400-800 mg daily. Special adjustments may be necessary for renal impairment.
- Monitoring Parameters: Blood pressure, renal function (serum creatinine, BUN), potassium levels.
Popular Combinations
- Eprosartan + Hydrochlorothiazide (Teveten HCT): Combines the ARB with a thiazide diuretic for additive antihypertensive effects.
Precautions
- Monitor renal function, especially in patients with renal impairment or heart failure.
- Monitor potassium levels, especially in patients taking potassium supplements or potassium-sparing diuretics.
- Use with caution in patients with hepatic impairment.
- Avoid concomitant use of aliskiren in patients with diabetes or renal impairment.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Eprosartan?
A: Initial dose is 600 mg once daily in patients without volume depletion. The maintenance dose is 400-800 mg daily, taken once or twice daily.
Q2: How does Eprosartan differ from an ACE inhibitor?
A: While both lower blood pressure by affecting the renin-angiotensin-aldosterone system, ARBs like eprosartan tend to have a lower incidence of cough compared to ACE inhibitors.
Q3: Can Eprosartan be used in pregnancy?
A: No. Eprosartan is contraindicated during the second and third trimesters of pregnancy due to the risk of fetal harm.
Q4: What are the most serious side effects of Eprosartan?
A: Angioedema, acute renal failure, and hypotension are rare but serious potential side effects.
Q5: Does Eprosartan interact with other medications?
A: Yes. Clinically significant interactions can occur with medications such as aliskiren, lithium, potassium-sparing diuretics, potassium supplements, and NSAIDs.
Q6: What should be monitored in patients taking Eprosartan?
A: Blood pressure, renal function (serum creatinine and BUN), and potassium levels should be monitored periodically.
Q7: Can Eprosartan be used with other antihypertensive medications?
A: Yes. Eprosartan is often used in combination with other antihypertensives, such as thiazide diuretics or calcium channel blockers, to achieve better blood pressure control.
Q8: How long does it take for Eprosartan to work?
A: The maximum blood pressure-lowering effect may take 2-3 weeks to be achieved.
Q9: Can Eprosartan be crushed or chewed?
A: While some sources indicate the tablets can be crushed, it’s best to consult the specific product information or check with a pharmacist before altering the tablet form, as this can affect the drug’s release and absorption. It’s generally recommended to swallow tablets whole.
