Chem Basis ACEIs and ARBs 1

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  1. Angiotensin Converting Enzyme (ACE) catalyzes the conversion of _____________ to ____________ by cleaving 2 amino acids.
    Angiotensin-I to angiotensin-II
  2. Ag-II is responsible for maintaining blood pressure homeostasis by what actions?
    Vasoconstriction by acting on AT-1 receptors, ↑ aldosterone release, ↑ sympathetic tone and ↑ BP
  3. Why might ACEIs cause hyperkalemia?
    They reduce aldosterone levels
  4. (True/False) ACE-I also inhibits degradation of bradykinin.
  5. What symptoms are commonly associated with ACEIs ability to inhibit the degradation of bradykinin?
    Angioedema and dry cough
  6. What proportion of patients on ACEIs develop a dry cough?
    About 10%
  7. Angiotensin II is generated by two pathways, what are they?
    Renin angiotensin system, and Chymases
  8. Do ACEIs block all Ag-II from being produced?
    No, they only block one pathway
  9. What type of drug would block both the renin-angiotensin and Chymases pathway of Ag-II production?
    Angiotensin Receptor Blockers (ARBs)
  10. The main effect of ARBs is at what angiotensin receptor?
  11. Do ARBs have an effect on AT2 receptors?
  12. What are the effects of AT2 receptor agonism?
    Vasodilation, tissue repair and inhibition of growth hormone
  13. Wince AT2 agonism causes vasodilation and promotes tissue repair, why are drugs with balanced antagonism of AT1 and AT2 desired?
    Concern that unopposed AT2 stimulation may have side effects
  14. What are the two important active sites of ACE that enable binding to Angiotensin I?
    Zinc and cationic binding site
  15. What are the therapeutic indications for ACEIs?
    Hypertension and Heart Failure
  16. Why are ACEIs not very effective in African Americans?
    African American have low Renin
  17. Can ACEIs be used in African Americans?
    Yes, especially in those at risk of renal dysfunction
  18. (True/False) ACEIs are effective as monotherapy in decreasing mild-severe hypertension and can be used as a first line therapy.
  19. The efficacy of ACEIs is higher as a monotherapy or in combination?
    In combination with thiazide diuretics or CCBs
  20. How can you prevent acute hypotension episodes with ACEI use?
    Start at low doses and titrate up
  21. (True/False) ACEIs are a good choice for patients with hypertension and complicating factors such as nephropathy, HF, myocardial infarction or diabetes.
  22. Intravenous enalaprilat is used for what situation?
    Short management of relatively stable patients who cannot take oral medication
  23. Patients with CHF and symptomatic HF should be on either _____________ or ______________.
    ACE-I or hydralazine/nitrate combination
  24. What are the major side effects of ARBs?
    CNS: headache and dizziness
  25. Do ARBs cause a dry cough?
  26. ARBs are used to treat what type of Hypertension?
    mild to moderate
  27. ARBs can be given as a monotherapy or in combination?
  28. What drugs are ARBs commonly given in combination with?
    Thiazide diuretics
  29. Can ARBs be used for HF?
  30. When are ARBs usually used?
    When a patient cannot tolerate dry cough or angioedema of ACEIs
  31. What are the three classes of marketed ACEIs?
    Catopril analogs, enalapril analogs, phosphorus containing analogs
  32. What feature do all classes of ACEIs share?
    Features that allow them to bind to the cationic and zinc binding site
  33. What type of interaction binds ACEIs to the cationic and zinc binding sites?
  34. What is the Pharmacophore for Captopril Analogs?
  35. 2D-methyl, 3-mercapto propanoyl-L-prolineImage Upload 1
  36. The carboxylic terminal of the proline of Captopril Analogs is essential for what?
    Binding to the cationic site
  37. The mercapto group of Captopril Analogs is essential for binding to what binding site?
    Zinc binding site
Card Set
Chem Basis ACEIs and ARBs 1
Chem Basis ACEIs and ARBs 1
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