Actions and Spectrum: 

eprosartan is a medication that belongs to the class of drugs,angiotensin II receptor blockers (ARBs).

Its main action is to block the binding of angiotensin II to its receptors, which causes blood vessels to narrow and the release of hormones that increase blood pressure. By blocking this action, eprosartan helps to widen blood vessels, lower blood pressure, and improve blood flow. 

In terms of its spectrum of activity, eprosartan is primarily used for treatment, hypertension (high blood pressure) in adults. It may also be used to help prevent complications related to high blood pressure, such as heart attack and stroke. 

DRUG INTERACTION

Contraindicated  

Serious Use Alternative  

Monitor Closely  

Minor  

Frequency defined 

1-10% 

• Fatigue (2%) 
• Abdominal pain (2%) 
• Cough (4%) 
• Upper respiratory infection (8%) 

Frequency not defined 

• Myalgia 
• Back pain 
• Dizziness 
• Headache 
• Neutropenia 
• Facial edema 

Black Box Warning: 

eprosartan does not have a black box warning. However, like other medications in its class (ARBs), eprosartan may increase the risk of fetal injury or death if taken during pregnancy.

Therefore, it is important for women of childbearing age to use effective contraception while taking eprosartan and to discuss their options with their healthcare provider. 

Contraindication/Caution: 

Contraindication 

• Hypersensitivity: Patients who have a known hypersensitivity to eprosartan or any of its components should not take this medication. 
• Pregnancy: eprosartan may cause fetal injury or death if taken during pregnancy. Therefore, it is contraindicated in pregnant women or women who may become pregnant while taking the medication. 
• Breastfeeding: eprosartan may be present in breast milk and can harm a nursing baby. It is contraindicated in breastfeeding women. 
• Severe liver disease: eprosartan is primarily metabolized by the liver. Patients with severe liver disease may not be able to metabolize eprosartan properly, leading to increased levels of the drug in the bloodstream. 
• Bilateral renal artery stenosis: eprosartan may cause further decreases in kidney function in patients with bilateral renal artery stenosis. 

Caution 

• Renal impairment: eprosartan is eliminated from the body primarily through the kidneys. Patients with mild- moderate renal impairment may need a lower dosage of eprosartan to avoid further damage to their kidneys. 
• Hepatic impairment: eprosartan is metabolized in the liver. Patients with mild to moderate hepatic impairment may need a lower dosage of eprosartan to avoid toxicity. 
• Heart failure: eprosartan may cause further decreases in blood pressure in patients with heart failure. Patients with heart failure should have their blood pressure monitored closely while taking eprosartan. 
• Volume depletion: eprosartan may cause a decrease in blood pressure, especially in patients with low blood volume or dehydration. Patients should maintain adequate hydration while taking eprosartan. 
• Hyperkalemia: eprosartan may cause an increase in potassium levels in the blood. Patients with hyperkalemia or those taking other medications that increase potassium levels should be monitored closely while taking eprosartan. 
• Diabetes: eprosartan may affect blood sugar levels in patients with diabetes. Patients with diabetes should monitor their blood sugar levels closely while taking eprosartan. 

Pregnancy consideration: 

Pregnancy Category: 

C -1st trimester 

D -2nd and 3rd trimesters. 

During the 2nd and 3rd trimesters of the pregnancy period, these drugs have been linked with fetal injury that involves anuria, hypotension,reversible or irreversible renal failure, neonatal skull hypoplasia and death 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.      
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women      
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.     
• Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.      
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.      
• Category N: There is no data available for the drug under this category 

Pharmacology: 

eprosartan is an angiotensin II receptor blocker (ARB) medication that works by selectively blocking the binding of AT-II to AT-I receptor, which is found on many cells in the body, including those in blood vessels, heart, kidneys, and adrenal gland. 

By blocking the AT1 receptor, eprosartan prevents the vasoconstrictive and aldosterone-secreting effects of angiotensin II, leading to vasodilation and a reduction in blood pressure. This action also leads to a decrease in sodium and water reabsorption by the kidneys, which can further contribute to a reduction in blood pressure. 

Pharmacodynamics: 

Mechanism of Action: 

eprosartan is Angiotensin II blocker that works by displacing angiotensin II from the AT1 receptor. This process may lower blood pressure by counteracting AT1-induced vasoconstriction, aldosterone release, catecholamine release, arginine vasopressin release,

water absorption, and hypertrophic responses. It may lead to a more comprehensive inhibition of the renin-angiotensin system compared to ACE inhibitors, and it does not affect the response to bradykinin. Additionally, it inhibits the pressor effects of an angiotensin II infusion in a dose-dependent manner. 

Pharmacokinetics: 

Absorption 

The half-life of this medication is between 5 to 9 hours. It takes approximately 4 hours for the medication to take effect, and the peak plasma concentration is also reached around 4 hours after administration. The bioavailability of the medication is 13%, which can be increased by consuming food or with age. 

Distribution 

eprosartan is highly protein-bound, with approximately 98% of the drug bound to protein molecules. The volume of distribution (Vd) of the medication is 3.8 L 

Metabolism 

eprosartan undergoes partial conjugation with glucuronic acid in the liver during metabolism. The primary metabolite produced as a result is an acyl glucuronide metabolite, which is inactive. 

Elimination and Excretion 

eprosartan is primarily eliminated through feces, with approximately 90% of the drug being excreted in this manner. A small amount of the medication (around 7%) is eliminated through urine. 

The total body clearance of the medication is 48.5 L/hr, indicating that the drug is cleared relatively quickly from the body. The renal clearance of the medication is between 39 to 45 mL/min 

Administration: 

Oral administration 

eprosartan is typically administered orally in the form of tablets. The recommended dosage can be changed depending on condition being treated, age and other factors. It is generally recommended to take eprosartan with or without food once daily, at around the same time each day. 

It is essential to follow the prescribing healthcare provider’s instructions carefully when taking this medication. Do not stop taking the medication abruptly without consulting a healthcare provider, as this could cause a sudden increase in blood pressure. 

If a dose is missed, it is recommended to take it as soon as possible, unless it is almost time for the next scheduled dose, in which case it is advisable to skip the missed dose and resume with the regular dosing schedule. 

Patient information leaflet 

Generic Name: eprosartan 

Pronounced: [ ep-roe-SAR-tan ] 

Why do we use eprosartan? 

eprosartan is an angiotensin II receptor blocker (ARB) medication that is primarily used for the treatment of hypertension (high blood pressure) in adults. It works by blocking the action of AT- II, a hormone that can cause blood vessels to narrow, which can lead to high blood pressure. 

In addition to hypertension, eprosartan may also be used in the management of other cardiovascular conditions, such as heart failure and diabetic nephropathy (kidney disease due to diabetes). However, the use of eprosartan in these conditions may vary depending on the patient’s specific situation and other medications they are taking.