Better Known as: Altace or Ramipro
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 Angiotensin-Converting Enzyme, actively inhibiting ACE-1 from binding and converting Angiotensin I into Angiotensin II. ACE-1 binds Ramiprilat 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.
Pharmacokinetics
For Pharmacokinetic Data References, See: References
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References
- ↑ 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
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