TEVETENCopy

• DRUGBANK - Eprosartan
• indication:

  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).

• pharmacology:

• mechanism:

  Eprosartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT<sub>1</sub> receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland). There is also an AT<sub>2</sub> 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 AT<sub>1</sub> receptor. Its affinity for the AT<sub>1</sub> receptor is 1,000 times greater than for the AT<sub>2</sub> receptor. In vitro binding studies indicate that eprosartan is a reversible, competitive inhibitor of the AT<sub>1</sub> receptor. Eprosartan has also been shown to bind to AT<sub>1</sub> receptors both presynaptically and synaptically. Its action on presynaptic AT<sub>1</sub> 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.

• absorprion:

  Absolute bioavailability following a single 300 mg oral dose of eprosartan is approximately 13%. Administering eprosartan with food delays absorption.

• halflife:

  The terminal elimination half-life of eprosartan following oral administration is typically 5 to 9 hours.

• roouteelimination:

• volumedistribution:

• clearance: