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2013-02-10 16:10:53
Dr Dupre

543 exam 1
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  1. which drug is classified as an aryloxypropanolamine
  2. at higher doses metoprolol my bind to what receptor and effect what type of pts
    • B2 receptor
    • asthma pts
  3. metoprolol is metabolized by
    n-dealkylation and conjugation
  4. what percentage of metoprolol is excreted unchanged in the urine
  5. how is metoprolol excreted
    through liver and kidney
  6. which drug is classified as a benzothiadiazine sulfonamide diuretic
  7. HCTZ acid/base properties
    it is weakly acidic so you can make salts for IV administration
  8. metabolism of HCTZ
    cleared unchanged in urine
  9. enalapril undergoes what reaction to change to enalaprilat
    phase I hydrolysis
  10. being a large molecule allows enalapril to specifically target
    zn++ ion in ACE enyzme and not other enymes
  11. what is the enalaprilat at physiological pH
    zwitterionic at physiological pH and less soluble
  12. MOA of enalapril
    mimics TS of angiotensin I hydrolysis
  13. where is enalapril metabolized
    hydrolyzed to enaliprilat and cleared mostly in the urine (reduce dosage for renal impairment)
  14. which drug is classified as anthranilic acid sulfonamide (o-amino benzoic acid)
  15. MOA of furosemide
    NKCC transporter in the thick ascending loop of henle
  16. bile acid sequestrants acid/base properties
  17. what type of amine does cholestyramine contain
    quaternary amine
  18. what type of amine does colestipol contain
    secondary and tertiary amines
  19. colesevelam fragment A contains what type of amine
    primary amine
  20. colvesevelam fragment B contains what type of amine
    alkylated secondary and quaternary amine
  21. colesevelam fragment C contains what type of amine
    pair of secondary amines
  22. colesevelam fragment D contains
    alkylated secondary amine
  23. metabolism of BAS
    not metabolized but excreted fecally
  24. what is the prototype statin
  25. where did statins arise from
    isolated form two different peicillum fungi, thus a natural product
  26. what was the first statin and what yr was it approved
    lovastatin 1987
  27. which statin has the highest/lowest logP
  28. low logP in prevastatin important for
    hydrophilicity and decreased cell penetration in peripheral tissues, which leads to better selectivity for hepatic cells and reduced side effects
  29. name the inactive prodrug statins
    lovastatin and simvastatin
  30. what happens to atorvastatin which allows it to retain activity as an active metabolite
    ortho and para hydroxylation
  31. what happens to crestor which allows it to retain its activity as an active metabolite
    n-demethylation which produces a des-methyl analog
  32. which enyzmes are not metabolized by 3A4 enzymes
    crestor and prevachol
  33. acid base properties of fibrates
  34. which drug may cause cholelithiasis (gallstones)
  35. MOA of fibrates
    • accelerate removal of cholesterol
    • stimulate action of lipoprotein lipase
  36. metabolism of fenofibrate
    ester hydrolysis, glucoronidation
  37. metabolism of gemfibrozil
    oxidation of aromatic methyl groups to carboxylic acids, glucoronidation