1. Epi does what to receptors specifically on vessels
    • Stimulates all Alpha and Beta receptors
    • Stimulates Alpha (vasocostriction) and Beta (vasodilation) = (there are less B2 than A, but B2 are more sensitive to Epi. (small amt=B2) (large bolus=A) (medium=pressor than depressor)
  2. Epi on heart
    Stimulate B1 to increase HR and contractility
  3. Epi on metabolism
    Stimulate Betas to increase glucose in blood in all possible ways (Gluconeo, gycogen break down and none formed, fats to fatty acids)
  4. Epinephrine (duration and administration and for what?)
    • Start duration, not given orally, given by inhalation or parenterally
    • Treats asthma and bronchiospasms of anaphylactic shock
    • Stimulate Betas to increase glucose in blood in all possible ways (Gluconeo, gycogen break down and none formed, fats to fatty acids)
  5. is a chemical classification of amine molecules containing a benzene ring with OH substitutions at the 3 and 4 positions.
  6. 2 catecholamines that act as neurotransmitters in the CNS
    Dopamine and Epinephrine
  7. Tyrosine -->
    _____ -->
    Dopamine --->
    • DOPA
    • Norepinephrine
  8. rate limiting step in conversion of tyrosine to Norepinephrine
    Tyrosine to DOPA
  9. reason catecholamines aren't effective when given orally
    enzymes MAO and COMT readily break them down in liver
  10. mechanism for the termination of NE action where NE is taken back into the presynaptic terminal
    uptake I (most important 60-90% of the time)
  11. Some NE enters the post synaptic cell where it is enzymatically inactivated by the extra-neuronal enzyme, catechol-O-methyltransferase (COMT).
    uptake II
  12. is found in nerve terminal (mitochondrial membrane) and is in very high concentration in the liver.
  13. is found in the effector cells and in high concentration in the cytosol of the liver cells.
  14. mimic sympathetic function. They can do this either by directly stimulating the adrenergic receptors, or indirectly, by allowing more norepinephrine to be present in the synaptic cleft. Indirect acting _____ either cause release of the transmitter (NE) or prevent the normal termination of action (reuptake).
    Sympathomimetic drugs
  15. Endogenous sympathetic substances not effective when given orally
  16. Norepinephrine (3)
    • Acts on all As and Bs
    • Increases BP by stimulating As on Blood vessels (vasoconstriction and increased CO)
    • Not clinically useful b/c short duration, not orally effective
  17. Isoproterenol
    • Beta stimulatn only
    • produces bronchodilation (B2)
  18. Dopamine
    • metabolic precursor of Epi and NE
    • Used for Parkinson's (L-Dopa), is used as neurotransmitter in CNS
    • Treat compromised renal blood flow
    • High dose=stimulate A and B receptors --> increases BP and HR
  19. non-catecholamine Alpha Agonists (6)
    • Tyramine
    • Amphetamine
    • Methylphenidale (Ritalin)
    • Ephidrine
    • Phenylephrine
    • Methaxomine
    • (you can't TAME shelly in the PM, these also excite most thing so that works)
  20. non-catecholamine Alpha Agonists that are nasal decongestants
    • Ephidrine
    • Phenylephrine
    • Methaxomine
  21. Cause massive release of NE ---> Increases BP
    Inactivated by MAO
    Needs NE in neuron for results (false transmitter)
    Alpha Agonist
  22. Indirect actions
    orally effective
    enter CNS
    Toxic can be lethal
    Cerbral hemorrhage due to vasoconstriction
    can readily diffuse into the nerve terminal to cause NE release
    Use in hyperkinetic kids and narcoleptics
    Alpha Agonist
    Amphetamine and Methamphetamine
  23. Indirect action
    use for ADHD
    oral use
    CNS escilation
    Methylphenidale (Ritalin
  24. direct and indirect actions
    Acts on all A and Bs directly
    Causes bronchodilation (decongestion)
    short lasting mydriasis (dilation)
  25. Direct action
    produce mydriasis
    only orally effective in huge doses
    rebound effect in nasal congestant
  26. Direct action
    causes mydriasis
    atrial tachycardia treatment
    nasal decongestant
  27. Beta agonists (6)
    • Salmeterol
    • Metaproterenol
    • Albuterol
    • Rifrodine
    • Terbutaline
    • Dobutamine
    • (SMART D, that's me I'm also B+ blood type so it works)
  28. Direct-Beta2 selectivity
    Bronchial asthma
    cardiac side effects
  29. Direct Beta 2 selection
    long duration than metaproterenol
    prevent premature labor
  30. Direct Beta 2
  31. Direct Beta 2
  32. Direct Beta 2
    relax uterus
    delay premature labor FDA approved
  33. Direct Beta 2
    Increase Cardiac Output w/ out vasoconstriction
    Cardiac insufficiency, CHF
    cardiac surgery
    rapidly metabolized by liver
    does not stimulate dopamine receptors
  34. Reuptake blockers
    • Cocaine
    • Tricyclic Anti-depressants
    • (CT scan?)
  35. Blocks reuptake 1
    NE reuptake
  36. Catecholamine reuptake
    Tricyclic Anti-depressants
  37. Blockers of Adrenergic Nerves
    • Clonidine
    • Alpha-Methyl Dopa
    • Alpha-Methyl-Paratyrosine
    • (BAN CAMP AMD)
  38. Blockers of Adrenergic Nerves MAOs (7)
    • a) depression of CNS sympathetic tone
    • b) inhibition of NE synthesis
    • c) false transmitter production
    • d) deplation of catecholamine storage
    • e) prevention of action potential effectiveness
    • f) destruction of adrenergic nerve terminals
    • g) ganglionic and receptor blockade
  39. Drugs that are taken up by pump that takes in NE shouldn't be administered with what drugs for what reason.
    reuptake inhibitors b/c they will prevent their action b/c they aren't being transported
  40. Antihypertensive
    Alpha 2 stimulant in CNS -->decreases sympathetic tone to blood vessels and heart
    EtOH and opiod addiction helper
    Synergestic effect w/opiods
  41. Decrease BP Decrease sympathetic tone
    Alpha 2 agonists
    Not metabolized by MAO
    Alpha-Methyl Dopa
  42. Drugs that stimulate Alpha 2 produce what in BP.
    • vasoconstriction in periphery but hypotensive action in CNS for hours.
    • This is called CNS acting sympatho-inhibitory agents
  43. Decreases NE in postganglion b/c it is a substrate for tyrosine hydroxylase which is the rate-limiting step in NE formation
    Alpha-methyl-para tyrosine
  44. Agents that are taken up by adrenergic neurons, metabolized to an active amine, stored with NE in vesicles and released with NE by an action potential are called false transmitter precursors.
    false transmitter precursor
  45. Several drugs act to deplete catecholamines from sympathetic nerve endings and thus reduce sympathetic reactivity.
    Catecholamine depletion
  46. Catecholamine depletion
    • Reserpine
    • Guanethidine
    • 6-OH Dopa
    • (RG-6 on a CD)
  47. interrupts storage of NE, Epi, Dopa in vesicles
    decreases BP redirectly
    Enters CNS
  48. Deplete NE - blocks AP
    Potent antihypertensive drug
    no pass BBB
  49. destroys nerve terminals
    6-OH Dopa
  50. Alpha Blockers
    • Phentolamine
    • Phenoxybenzamine
    • Prazosin
    • Terazosin/Doxazosin
    • Yohimbine
    • Clonidine and Alpha-Methyldopa
    • (I got nothing to help)
  51. Alpha 1 preference
    short action
  52. Alpha 1 preference
    Long duration
    Can become irreversible (competitive --> non-comp inhibition)
  53. Alpha 1 selection
    No large tachycardia reflex
    decrease BP
  54. Like Prazosin
    Treat benign hypertrophic prostates
  55. select Alpha 2
    prevents effects of hypotensive dopamine
  56. Experimental studies in pts w/spinal cord damage show Alpha blockage in these drugs (2)
    Clonidine and methyldopa
  57. Beta Blockers
    • Piadolol
    • Propranolol
    • Alenolol
    • Metaprolol
    • Betarolol
    • Esmolol
    • Nadolol
    • Timolol
    • (PPAM BENT)
  58. Beta 1 & 2 blockage
    Decrease BP
  59. Beta 1 selective
    Decrease Plasma Renin
  60. Beta 1 selective
    less CNS side effects than Metaprolol
    Excrete by kidneys
  61. Nonselective
    Intrinsic Sympothemimetic Activity --> stimulate Beta 1 (tolerated better during exercise)
  62. Potent Beta 1 & 2 Blocker
    Treat open angle glaucoma
    Prevent reinfections to myocardium
    Decrease intraoccular pressure
  63. Non-selective
    long duration
  64. Beta 1 selection
    Liver metabolism
    Long 1/2 life
  65. Beta 1 selection
    short 1/2 life
    Control ventricular HR for emergency or critically ill
  66. Alpha and Beta Blockers
    • Labetalol
    • Carvedilol
    • (LC blocked heidi and spencer)
  67. Beta 1&2 and alpha blocker
    blockage toward Alpha 2
    Some Beta 2 - stimulation
    lower plasma Renin
    lower BP
    small reflex effect on HR or CO
  68. Similar actions to labetalol
    "Free Radical Scavenger"
    Protects heart cells from damage
    Approved for pts w/congestive heart failure
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