Ramipril

Better Known as: Altace or Ramipro

• Marketed By: King Pharmaceuticals (Now part of Pfizer Inc.)
  
• Major Indication: Hypertension & Congestive Heart Failure
  
• Drug Class: ACE Inhibitor
• Date of FDA Approval (Patent Expiration): 1991 (2007)
  
• 2006 Sales: $650 Million
• Importance: One of the best selling Angiotensin-Converting Enzyme Inhibitors of all time. Long acting ACE Inhibitor.
• See Pharmaceutical Drugs for more information about other drugs and diseases

Mechanism of Action

Angiotensin II has been implicated in cardiac, renal and vascular diseases. ^[1] Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since ACE-1 is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure. Ramipril is quickly metabolized into Ramiprilat, the most active metabolite of Ramipril. Ramiprilat binds to the active site of , actively inhibiting ACE-1 from binding and converting Angiotensin I into Angiotensin II. ACE-1 using residues Glu 395, His 497, Lys 495, Gln 265, Tyr 504, Tyr 496 and Tyr 507, tightly affixing the inhibitor to the active site of ACE-1.

For Pharmacokinetic Data References, See: References