Pharmacology Exam I part 3

  1. Substances that affect drug metabolism
    grapefruit juice -CYP 3A4 inhibitor, St John's wort, other herbal products, isosafrole, safrole: CYPA1, CYPA2 INHIBITOR (found in perfrume and root beer)
  2. Phase II metabolism
    considered anabolic, phase I metabolism is combined with another component to make it inactive, generally more water soluble and predictable than phase I reactions
  3. Phase II turns lipid soluble drugs into
    water soluble drugs
  4. Blood-brain barrier and placenta
    only very lipid soluble drugs can pass
  5. What age group metabolize poorly?
    old people and very young people
  6. Another word for elimination?
  7. Drug targets:
    receptors, enzymes, transporters, ion channels
  8. 3 types of receptors
    ligand-gated ion channels, g-protein coupled receptors, and nuclear receptors
  9. ligand-gated ion channels
    time scale is in milliseconds (takes effect very fast) occurs in membrane bound (doesn't cross)
  10. G-protein coupled receptors
    occur in seconds (found in heart)
  11. Nuclear receptors
    ligand has to cross cell membrane (ex. in oestregen receptors); causes gene transcription because the ligand changes DNA (ex. birth control takes a while to work)
  12. Why does it take G-protein receptors a bit longer?
    G-protein membranes have seven membrane-spanning a-helices
  13. Monamine transporters are important in the
    central nervous system
  14. Peripheral nervous system 2 divisions
    somatic (involuntary movement) and visceral
  15. 2 subdivisions of visceral
    parasympathetic and sympathetic
  16. Neurotransmitters for parasympathetic system
    acetylcholine (AcH)
  17. Neurotransmitters for sympathetic system
    Norepinephrine and epinephrine
  18. Increasing Norepinephrine does what to heart rate?
    increase heart rate
  19. Decreasing Norepinephrine does what to heart rate?
    decreases heart rate
  20. Muscarinic receptors:
    G-protein linked receptors; 5 subtypes (depend on location) m1=neuronal,m2=cardiac,m3=glandular smooth muscle, m4/m5=CNS;Agonist=AcH; Antagonist=atropine and scopolamine
  21. AcH in the heart does what to heart rate and force of contration
    decreases both heart rate and force of contraction
  22. norepinephrine is not used in muscarinic receptors
    becuase the half life is short and would be broken down before a physological response appears
  23. Muscarinic agonists
    "pilocarpine: used for glaucoma, increases intraocular pressure which activates constrictor muscle to promote fluid drainage.
  24. Muscarinic antagonists
    • 1)inhibit secretions (salivary, lacrimal bronchial)
    • 2) increase heart rate (tacliycardio)
    • 3) dilate pupil
    • 4) increase GI motility
    • 5) relax smooth muscle
    • 6) increase GI activity
  25. Nicotinic receptors
    skeletal muscle (only place where these receptors are used), nicotinic antagonists, skeletal muscle relaxants, non-depolarizing blockers (bind to receptor and prevent AcH from binding)
  26. There is no depolarization in nicotinic antagonists, true or false?
    true. (ex. atracurium and tubocurarine)
  27. Depolarizing blockers
    bind and depolarize membrane (produce effects) and can't repolarize, these compounds stay bound to receptor for a long time, nothing you can do to reverse effects of these. (ex. succinylcholine)
  28. Acetylcholinesterarse (in depolarizing blockers)
    breaks down AcH and then the choline is taken back up
  29. Acetaylcholinesterase inhibtors:
    block AcHesterase and increase AcH at receptors
  30. Reversible AcHesterase (inhibit)
    • have short duration¬†
    • Example 1
    • neostigmine for the condition of myastehnia graris (autoimmune disease that breaks down muscle and causes fatigue) increases AcH levels at skeletal muscle receptors)
    • Example 2
    • aricept (donepezil) reversible AcHesterase inhibitor used for alzheimers
  31. Irreversible inhibitors provide how many hours of AcH?
    about 20-24 hours
  32. Atropine
    mAcH (muscarinic), smooth, when used as antidote the effects of AcH inhibitors will be reversed
Card Set
Pharmacology Exam I part 3
omg long exam review