Pharmacology #2 (local anesthetics)

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  1. Prototype drugs: Local Anesthetics (5)
    • Procaine
    • Benzocaine
    • Tertacaine
    • Lidocaine
    • Bupivicaine
  2. Most LA's are weak _____, with pKa of _____
    bases, 8-9
  3. What are the two types linking bonds that determine the disposition of an LA?
    ester and amide
  4. Esters are hydrolyzed by ______________ in the _____ AND _____
    butyrcholinesterase, plasma and liver
  5. Amides are resistant to ________; they are ________ in the _________
    hydrolysis, N-alkylated in the liver
  6. which type of LA  is up to 95% protein bound, and which protein is it bound to?
    amides, a1-acid glycoprotein
  7. What is the mechanism of action for LA's?
    reversible block of nerve impulse conduction by binding and blocking voltage dependent Na channels.
  8. what is the order of blockage of LA's (neuro types)
    pain, sensory, motor
  9. Is the major site of action INSIDE the cell membrane?
  10. What factors influence nerve blocks?
    • Size of nerve fiber
    • Position of nerve
    • pKa
    • Inflammation
    • Blood flow
    • Firing rate
  11. Why is inflamed tissure resistant to LA's?
    inflammation causes a reduction in pH.  This reductions causes the LA, which is a weak base, to be in the ionized form which is less available to pass into the cell.
  12. how does firing rate effect LA's?
    LA's work more rapidly on nerves that fire more rapidly.  Example is Sympathetic nerves
  13. Which type of LA has a higher tendency to cause systemic toxicity?
    AMIDES (Bc longer half life in blood)
  14. Which type of LA is more likely to cause an allergic rxn?
  15. Procaine is a _____-acting ______, used mainly for infiltration due to ______ potency and _____ T1/2.
    short, ESTER, LOW, short
  16. Benzocaine is _____-acting Ester, used mostly _______.
    short, topically
  17. tetracaine is _______-acting _______, used for _______ anesthesia.
    Long, ESTER, spinal
  18. Does tetracaine have a high toxicity?
  19. Which LA Esters has the slowest hydrolysis?
  20. Lidocaine is an _______, with longer duration that procaine, used for ________, and for people with allergy to Esters
    AMIDE, anti-arrythmia
  21. Bupivicaine is an _______, with ______-acting action, and has ______ toxicity than lidocaine.
    AMIDE, Long, Higher
  22. Proparacaine has replaced ______ for anesthesia of the ________.  Why?
    cocaine, cornea.  Less irritating
  23. What is the advantage of admin epi with local anesthetics?
    increases duration of action by causing vasoconstriction and slower clearance time
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Pharmacology #2 (local anesthetics)
2013-02-19 16:12:42
AA Eory anesthesia

drugs and info for pharm exam 2- local anesthetics
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