Pharmacology Exam #2 (CNS depressants I & II)

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  1. CNS depressants categories:
    • benzodiazepines
    • non-benzodiazepines receptor agonists
    • anxioselective drugs
    • alcohols
  2. what are the prototype benzo's?
    • diazepam
    • triazepam
  3. what are the prototype NBRA's?
    • zolpidem (ambien)
    • eszopiclone (lunesta)
  4. what are the prototype anxioselective drugs?
  5. do benzo's have a higher margin of safety than barbs?
  6. Benzo mech of action:
    potentiation of action of inhibitory NT λ-aminobutiric acid (GABA) at GABA-A receptor, on a site separate from GABA binding site. 

    *GABA increases Cl- conductance, and benzo only increases frequency of channel opening if GABA is present
  7. diazepam is a GABA ______ and _________ GABA-mediated ____ conductance.
    agonist, enhances, Cl-
  8. Flumazenil is a GABA-A ________, binding the __________ receptor and competitively blocking benzo fx.  no fx alone
    antagonist, benzo
  9. B-carb carb ester is an ____________, binds to the ________ receptor and _______ GABA-mediated Cl- conductance.  what fx does this cause?
    inverse-agonist, benzo, reduces.

    Leads to anxiety, muscle spasm, proconvulsive state
  10. what are the two classes of benzo's? uses?
    • Short acting- tx of sleep disorder w/o anxiety
    • Long acting- antianxiety fx, with steady sate concentration.  TX of anxiety and sleep disorders.
  11. what prototype drug is classified as a SHORT_ACTING benzo?
  12. what prototype drug is classified as a LONG_ACTING benzo?
  13. How are Benzo's metabolized?
    liver- microsomal oxidase system
  14. triazolam metabolism chain
    triazolam(T1/2 3hr)-->a-hydroxydiazepam (T1/2 1-2 hr) -->  glucuronidation --> excretion
  15. diazepam metabolism chain:
    diazepam(T1/2 30hr)-->desmethyldiazepam (T1/2 50 hr) --> oxazepam (T1/2 7hrs) --> glucuronidation --> excretion
  16. does tolerance and dependence occur with benzo's?
    YES w/ chronic use
  17. Therapeutic uses of Benzo's:
    • anxiety tx
    • muscles spasm tx
    • anticonvulsant
    • sleep disorders
    • anesthesia
    • fixing circadian rhythm
  18. What is Flumazenil used for?
    • TX of benzo and NBRA overdose
    • hasten recovery of sedation from benzo use
  19. what drugs react with benzo's?
    potentiate all sedative-hypnotic drugs.  Cross tolerance btw benzo's and other sedative hypnotic drugs can be observed.
  20. NBRA's bind to the same receptor as Benzo's but cause less_________   and ________.
    muscle relaxation and anticonvulsant fx
  21. Zolpidem is selective what type of benzo receptor>? is it rapidly absorbed?
    • type 1
    • yes
  22. does Zolpidem produce a morning hangover feeling?
  23. Buspirone is an ____________ drug.  it has anti-anxiety fx sim to _______.
    anxioselective, diazepam
  24. how long does it take to get the fx of buspirone?
    days or weeks
  25. buspirone used in the treatment of?
    chronic anxiety disorder
  26. buspirone is not a what?
  27. buspirone mechanism of action?
    partial agonist of 5ht1a serotonin receptors. inhibits firing of serotonergic neurons in the brain stem.
  28. Busprirone is not a sedative-hypnotic drug:
    does not act on GABA-A, no sedation, no potentiation or cross tolerance
  29. What drugs are used to treat alcoholism?
    • naltrexone
    • acamprosate
Card Set:
Pharmacology Exam #2 (CNS depressants I & II)

Info and drugs for pharm exam 2 (CNS depressants I & II)
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