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Description: Irbesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.
Drug Type: Small Molecule; Approved; Investigational
Pharmacology: Irbesartan is a specific competitive antagonist of AT1 receptors with a much greater affinity (more than 8500-fold) for the AT1 receptor than for the AT2 receptor and no agonist activity.
Mechanism of Action: Irbesartan is a nonpeptide angiotensin II antagonist that selectively blocks the binding of angiotensin II to the AT1 receptor. In the renin-angiotensin system, angiotensin I is converted by angiotensin-converting enzyme (ACE) to form angiotensin II. Angiotensin II stimulates the adrenal cortex to synthesize and secrete aldosterone, which decreases the excretion of sodium and increases the excretion of potassium. Angiotensin II also acts as a vasoconstrictor in vascular smooth muscle. Irbesartan, by blocking the binding of angiotensin II to the AT1 receptor, promotes vasodilation and decreases the effects of aldosterone. The negative feedback regulation of angiotensin II on renin secretion also is inhibited, but the resulting rise in plasma renin concentrations and consequent rise in angiotensin II plasma concentrations do not counteract the blood pressure–lowering effect that occurs.
Indication: For the treatment of hypertension, and for the treatment of diabetic nephropathy with an elevated serum creatinine and proteinuria (>300 mg/day) in patients with type 2 diabetes and hypertension.
Half Life: 11-15 hours
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Thought leaders and organizations working on research involving irbesartan.

  • Hans-Henrik Parving
  • M Pfeffer
  • S Hohnloser
  • Thomas Kahan
  • Peter Hovind
  • Sanofi-Aventis
  • Bristol-Myers Squibb
  • Steno Diabetes Center
  • Novartis
  • Dresden University of Technology
  • Steno Diabetes Center
  • University of Udine
  • University of Alberta
  • CORE-Center for Outcomes Research
  • Karolinska Institutet Danderyd Hospital

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