PHRD6925 MedChem Lecture 6 - Diuretics

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  1. 4 ways diuretics are classified
    • 1) chemical class
    • 2) MOA
    • 3) site of action
    • 4) effects on urine contents
  2. diuretics that are low molecular weight compounds that are freely filtered through the Bowman's capsule into the renal tubules
    osmotic diuretics
  3. therapeutic use for isosorbide
    reduce IOP in glaucoma
  4. identify:
    • osmotic diuretics
    • (mannitol, sorbitol, isosorbide)
  5. induces diuresis by inhibiting the formation for carbonic acid w/in proximal & distal tubular cells to limit the number of H+ available to promote sodium reabsorbtion
    carbonic anhydrase inhibitors
  6. most common therapeutic use for carbonic anhydrase inhibitors
    glaucoma - reduce rate of aqueous humour formation & reduce IOP
  7. identify:
    acetazolamide (carbonic anhydrase inhibitor)
  8. primary use for acetazolamide
    reduce rate of aqueous humour production -> reduce IOP in glaucoma
  9. inhibits the Na+/Cl- symporter in the distal convoluted tubule
    benzothiadizine/thiazide diuretics
  10. removal of which group would render the thiazide inactive?
  11. saturation at which location increases thiazide activity?
  12. how would you increase diuretic potency in a thiazide?
    substitution with a lipophilic group at position 3
  13. what is necessary for diuretic activity?
    electron-withdrawing group (Cl or Br) at C-6
  14. therapeutic uses for thiazide diuretics
    • hypertension
    • edema caused by cardiac decompensation
    • hepatic/renal disease
  15. inhibit Na+/K+/2Cl- symporter on the thick ascending limb of the loop of Henle
    loop/high-ceiling diuretics
  16. loop/high-ceiling diuretics have a ____ onset and ____ duration of action
    quick; short
  17. identify:
    • loop diuretics
    • (furosemide -> furan & sulfonamide)
  18. identify:
    torsemide - loop diuretic w/ sulfonylurea (& no furan ring)
  19. identify:
    triamterene - potassium sparing diuretic
  20. interferes with the process of cationic exchange by blocking luminal sodium channels in the late distal convoluted tubule & collecting duct
    potassium sparing drugs
  21. identify:
    • amiloride - potassium sparing diuretic
    • (open chain version of triamterene)
  22. most serious SE associated w/ potassium sparing drugs

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PHRD6925 MedChem Lecture 6 - Diuretics
2015-03-05 07:53:44

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