Chem Basis Diuretics 2

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Chem Basis Diuretics 2
2013-12-01 13:25:45
Chem Basis Diuretics
Chem Basis Diuretics 2
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  1. What is the Pharmacophore for Thiazide diuretics?
    • Sulfamylbenzothiadiazine 1,1 dioxide
  2. What is a Sulfamylbenzothiadiazine 1,1 dioxide?
    • Benzene ring attached to a six membered ring that contains a Sulfur and 2 N's
  3. In a Sulfamylbenzothiadiazine 1,1 dioxide, what atom is number “1”, “2” and “4”?
    • 1: S, 2 and 4: Nitorgens
  4. Is the sulfonamide group at position 7 on Thiazide diuretics essential?
  5. Yes
  6. Spirolactone has what Pharmacophore?
    • Yes
  7. Spirolactone has a similar structure to what endogenous molecules?
    • Steroid –like similar to Aldosterone
  8. Since spirolactone has a very similar structure to Aldosterone, why does it not have agonist action?
    • Lacks an essential aldehyde group at position C13 and C17–ketol
    • and the C11–formyl groups
  9. (True/False) Spirolactone is metabolized to several sulfur and non-sulfur containing inactive metabolites.
    False, it is metabolized to Active metabolites
  10. What is Canrenone?
    A non-sulfur active metabolite of Spirolactone that is primarily responsible for its therapeutic effects
  11. (True/False) Pteridine Analogs are used as monotherapy in the treatment of hypertension.
    False, never used as a Monotherapy
  12. When are Pteridine Analogs usually used?
    In combination with other diuretics to counter the hypokalemic effect (e.g. with thiazides)
  13. What part of nephron do Pteridine Analogs act on?
    distal renal tubules
  14. What is the MOA of Pteridine Analogs?
    Act directly on distal tubules to block the reabsorption of Na and secretion of K
  15. Do Pteridine Analogs effect Aldosterone?
  16. Do Pteridine Analogs have K sparing effects?
  17. Thiazide diuretics are commonly used in combination with ARBs, ACEIs or BBs for treatment of hypertension?
  18. Why are thiazide diuretics particularly useful in African American patients?
    African American patients often have low Renin levels
  19. Loop diuretics of Thiazide diuretics inhibit more Na reabsorption, why?
    Loop diuretics as they work in the thick ascending limb of the loop of Henle
  20. Is Furosemide used in patients with normal kidney function?
  21. Why is Furosemide not used for hypertension in patients with normal kidney function?
    Poor ability to modify arteriolar tone (less than thiazides)