Eprosartan
Eprosartan Uses, Dosage, Side Effects, Food Interaction and all others data.
Eprosartan is an angiotensin II receptor antagonist used to treat hypertension. It performs 2 actions on the renin angiotensin system. By preventing the binding of angiotensin II to AT1, vascular smooth muscle relaxes and vasodilation occurs. By inhibiting norepinephrine production, blood pressure is further reduced.
Angiotensin II, the principal pressor agent of the renin-angiotensin system, is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme [kininase II]. It is responsible for effects such as vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Eprosartan selectively blocks the binding of angiotensin II to the AT1 receptor, which in turn leads to multiple effects including vasodilation, a reduction in the secretion of vasopressin, and reduction in the production and secretion of aldosterone. The resulting effect is a decrease in blood pressure.
| Trade Name | Eprosartan |
| Availability | Prescription only |
| Generic | Eprosartan |
| Eprosartan Other Names | Éprosartan, Eprosartan, Eprosartanum |
| Related Drugs | amlodipine, lisinopril, metoprolol, losartan, furosemide, hydrochlorothiazide |
| Weight | 400mg, 600mg |
| Type | Oral tablet |
| Formula | C23H24N2O4S |
| Weight | Average: 424.513 Monoisotopic: 424.145677956 |
| Protein binding | Plasma protein binding of eprosartan is high (approximately 98%) and constant over the concentration range achieved with therapeutic doses. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Eprosartan is an ARB used to treat hypertension, diabetic nephropathy, and congestive heart failure.
For the management of hypertension alone or in combination with other classes of antihypertensive agents. Also used as a first-line agent in the treatment of diabetic nephropathy, as well as a second-line agent in the treatment of congestive heart failure (only in those intolerant of ACE inhibitors).
Eprosartan is also used to associated treatment for these conditions: Congestive Heart Failure (CHF), Diabetic Nephropathy, High Blood Pressure (Hypertension)
How Eprosartan works
Eprosartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland). There is also an AT2 receptor found in many tissues but it is not known to be associated with cardiovascular homeostasis. Eprosartan does not exhibit any partial agonist activity at the AT1 receptor. Its affinity for the AT1 receptor is 1,000 times greater than for the AT2 receptor. In vitro binding studies indicate that eprosartan is a reversible, competitive inhibitor of the AT1 receptor. Eprosartan has also been shown to bind to AT1 receptors both presynaptically and synaptically. Its action on presynaptic AT1 receptors results in the inhibition of sympathetically stimulated noradrenaline release. Unlike ACE inhibitors, eprosartan and other ARBs do not interfere with response to bradykinins and substance P, which allows for the absence of adverse effects that are present in ACE inhibitors (eg. dry cough).
Toxicity
There was no mortality in rats and mice receiving oral doses of up to 3000 mg eprosartan/kg and in dogs receiving oral doses of up to 1000 mg eprosartan/kg.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
[Moderate] GENERALLY AVOID: Moderate-to-high dietary intake of potassium, especially salt substitutes, may increase the risk of hyperkalemia in some patients who are using angiotensin II receptor blockers (ARBs).
ARBs can promote hyperkalemia through inhibition of angiotensin II-induced aldosterone secretion.
Patients with diabetes, heart failure, dehydration, or renal insufficiency have a greater risk of developing hyperkalemia.
MANAGEMENT: Patients should receive dietary counseling and be advised to not use potassium-containing salt substitutes or over-the-counter potassium supplements without consulting their physician.
If salt substitutes are used concurrently, regular monitoring of serum potassium levels is recommended.
Patients should also be advised to seek medical attention if they experience symptoms of hyperkalemia such as weakness, irregular heartbeat, confusion, tingling of the extremities, or feelings of heaviness in the legs.
Eprosartan Drug Interaction
Moderate: sildenafil, sildenafilMinor: tadalafil, tadalafilUnknown: ethanol, ethanol, arginine, arginine, metoprolol, metoprolol, phenytoin, phenytoin, clopidogrel, clopidogrel, tramadol, tramadol, thiamine, thiamine, cyanocobalamin, cyanocobalamin
Eprosartan Disease Interaction
Major: diabetes, angioedema, hypotensionModerate: CHF, hyperkalemia, renal artery stenosis, renal impairment, renal/liver disease
Elimination Route
Absolute bioavailability following a single 300 mg oral dose of eprosartan is approximately 13%. Administering eprosartan with food delays absorption.
Half Life
The terminal elimination half-life of eprosartan following oral administration is typically 5 to 9 hours.
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