PHRD6925 MedChem Lecture 8 - Central & peripheral sympatholytics & vasodilators

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daynuhmay
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297646
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PHRD6925 MedChem Lecture 8 - Central & peripheral sympatholytics & vasodilators
Updated:
2015-03-05 04:03:45
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medchem
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medchem
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  1. which would be metabolized by an esterase?
    bottom left (esmolol)
  2. which beta blockers are more cardioselective?
    2nd gen -> selective for 1-adrenoceptors
  3. identify:
    1-receptor blocker
  4. block effect of sympathetic nerves on BV's by stimulating G protein & activating SM contraction through the IP3 signal transduction pathway
    1-receptor blockers
  5. identify:
    methyldopa - centrally acting sympatholytic
  6. therapeutic use for methyldopa
    antihypertensive
  7. therapeutic use of hydralazine
    mod-severe HTN
  8. 2 direct-acting vasodilators that undergo glucuronidation to be excreted
    • 1) hydralazine
    • 2) minoxidil
  9. how is minoxidil activated?
    metabolized by hepatic sulfotransferase
  10. prolongs the opening of the K+ channels in VSM, sustaining greater vasodilation on arterioles than veins
    • potassium channel openers (direct-acting vasodilators) 
    • eg: minoxidil
  11. inhibits breakdown of cGMP, enhancing VSM relaxation & vasodilation
    PDE5 inhibitors
  12. identify:
    PDE3 inhibitors (inamrinone, milrinone)
  13. identify:
    sildenafil (PDE5 inhibitor)

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