Scribd Logo
Upload

Welcome to Scribd!

  • 372 views

    ACE Inhibitor

    Uploaded by

    Apurba Sarker Apu
    Angiotensin Converting Enzyme (ACE) catalyzes hydrolysis of dipeptide fragment Convert of angiotensin I (decapeptide) to angiotensin II (octapeptide) ACE inhibitors are competitive inhibitor

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPTX, PDF, TXT or read online from Scribd

    ACE Inhibitor

    Uploaded by

    Apurba Sarker Apu
    372 views19 pages
    Angiotensin Converting Enzyme (ACE) catalyzes hydrolysis of dipeptide fragment Convert of angiotensin I (decapeptide) to angiotensin II (octapeptide) ACE inhibitors are competitive inhibitor

    Copyright

    © Attribution Non-Commercial (BY-NC)

    Available Formats

    PPTX, PDF, TXT or read online from Scribd

    Did you find this document useful?

    Is this content inappropriate?

    Angiotensin Converting Enzyme (ACE) catalyzes hydrolysis of dipeptide fragment Convert of angiotensin I (decapeptide) to angiotensin II (octapeptide) ACE inhibitors are competitive inhibitor

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    372 views19 pages

    ACE Inhibitor

    Uploaded by

    Apurba Sarker Apu
    Angiotensin Converting Enzyme (ACE) catalyzes hydrolysis of dipeptide fragment Convert of angiotensin I (decapeptide) to angiotensin II (octapeptide) ACE inhibitors are competitive inhibitor

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    You are on page 1of 19

    ACE Inhibitors

    PHRM 304

    Schematic drawing shows the structure of ACE. There is a catalytic site on each extracellular lobe, each of which binds a zinc (Zn2+) atom.

    ACE
    Angiotensin Converting Enzyme (ACE) catalyzes hydrolysis of dipeptide fragment Convert of angiotensin I (decapeptide) to angiotensin II (octapeptide) ACE inhibitors are competitive inhibitor

    Competitive Inhibition

    Non-competitive Inhibition

    Angiotensins
    Angiotensin I Angiotensin II Decapeptide Octapeptide Aspartic acid Arginine ACE Aspartic acid Arginine Valine Tyrosine Valine Tyrosine Isoleucine Histidine Isoleucine Histidine Proline Phenyl alanine Proline Phenyl alanine - Histidine - Leucine

    Functions of ACE
    Angiotensinogen

    Angiotensin I
    +

    Bradykinin ACE
    +

    Prostaglandin Release

    Angiotensin II (Vasoconstrictor) Potent effect

    Inactive Bradykinin

    Vasodilatation

    Net result is vasoconstriction

    Functions of ACE

    ACE Side effects


    Dry cough in elderly (10-15% patient) Common among women Increase in bradykinin also increase prostaglandin release which causes dry cough

    ACE inhibitors
    11 approved inhibitors are available Based on chemical composition classified into three groups

    I. Sulfhydryl-containing ACE inhibitors

    Captopril

    Captopril was the first ACE inhibitor developed

    Not a prodrug

    II. Dicarboxylate-containing ACE inhibitors


    This is the largest group, including: Enalapril

    Ramipril
    Quinapril Perindopril Lisinopril Esters are act as prodrug
    Enalapril

    Lisinopril (orally active without being prodrug)

    III. Phosphonate-containing ACE inhibitors


    Fosinopril, the only member

    Active Sites in ACE


    To which angiotensin I or drug binds
    Zinc ion (Zn+2) Charged arginine unit (=NH2+) Hydrophobic pocket
    Arginine

    General structure of ACE inhibitors

    COOH

    Phosphonic acid Sulfhydryl Carboxylic acid

    Alanine Lysine

    You might also like