Captopril

From Proteopedia

Revision as of 17:26, 28 November 2010 by David Canner (Talk | contribs)
Jump to: navigation, search

Captopril, also known as Capoten

Drag the structure with the mouse to rotate

Contents

Better Known as: Capoten

  • Marketed By: Bristol-Myers Squibb
  • Major Indication: Hypertension & Congestive Heart Failure
  • Drug Class: ACE Inhibitor
  • Date of FDA Approval (Patent Expiration): 1981 (1996)
  • 2009 Sales: N/A
  • Why You Should Care: It was the first Angiotensin-Converting Enzyme Inhibitor. Was one of the earliest successes of Structure-Based drug design.
  • The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information

Mechanism of Action

Extensive research has validated a pathological role for Angiotensin II 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 primary degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure. Captopril binds to the ACE-1 binding site of , preventing ACE-1 from binding angiotensin. Captopril,, forming electrostatic interactions with His 353, Glu 384, Lys 511, His 513 and Tyr 520, along with zinc cation. [2]

Pharmacokinetics

ACE-Inhibitor Pharmacokinetics Comparison at Equivalent Dosages
Parameter Captopril Lisinopril Ramipril Enalapril Benazepril Perindopril Trandolapril
Tmax (hr)
Cmax (ng/ml)
Bioavailability (%)
Protein Binding (%) 96.7
T1/2 (hr)
AUC (ng/ml/hr)
IC50 (nM)
Equivalent Dosage (mg)
Metabolism

References

  1. ↑ Ferrario CM. Role of angiotensin II in cardiovascular disease therapeutic implications of more than a century of research. J Renin Angiotensin Aldosterone Syst. 2006 Mar;7(1):3-14. PMID:17083068
  2. ↑ Natesh R, Schwager SL, Evans HR, Sturrock ED, Acharya KR. Structural details on the binding of antihypertensive drugs captopril and enalaprilat to human testicular angiotensin I-converting enzyme. Biochemistry. 2004 Jul 13;43(27):8718-24. PMID:15236580 doi:10.1021/bi049480n

Proteopedia Page Contributors and Editors (what is this?)

David Canner, Alexander Berchansky

Retrieved from "http://52.214.119.220/wiki/index.php/Captopril"
Personal tools