Lisinopril

Better Known as: Prinivil

• Marketed By: Merck & Co.
  
• Major Indication: Hypertension & Congestive Heart Failure
  
• Drug Class: ACE Inhibitor
• Date of FDA Approval (Patent Expiration): 1988 (2001)
  
• 1998 Sales: $690 Million
• Importance: It is the only Angiotensin-Converting Enzyme Inhibitor that is not a prodrug and is excreted unchanged in the urine. Was one of the best selling ACE inhibitors in history.
• 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. Lisinopril binds to the active site of , utilizing residues like as well as van der Waals interactions between the phenylpropyl group and Val 518. ^[2] Binding by Lisinopril actively inhibits ACE-1 binding and conversion of angiotensin 1 into angiotensin II.

For Pharmacokinetic Data References, See: References