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54 Cards in this Set

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1. For alpha receptors, what activates it more, Epi or NE?
a. E>or equal to NE
2. For B1 receptors, which activates more, E or NE?
a. EQUAL!
3. For B2 receptors, what activates more epi or NE?
a. E>>>>>NE
4. What 2 things inactivate Epi and NE?
a. MAO and COMT
What is Depivefrin
a. Prodrug converted into epinephrine
b. Topical, ophthalmic agent
c. Direct acting adrenomimetic
6. What are the 5 alpha 1 selective agonists and method of delivery
a. Phenylephrine (Neo-Synephrine, Sudafed PE)
b. Metaraminol (Aramine): Paraenteral
c. Xylometazoline (Chlorohist-LA, Inspire, Neo-Synephrine II Long Acting, Otrivin):nasal
d. Oxymetazoline (Afrin, Neo-Synephrine 12 Hours, etc.) – also activate a2 :Nasal
e. Midodrine (ProAmatine): oral
7. What are the 2 alpha 2 selective agonists? How are they given?
a. Brimonidine (Alphagan)
b. Apraclonidine (lopidine)
c. Both topical for the eye
8. What is isoprotenernol and how is it administered?
a. Non-selective B agonis
b. Parenteral
9. What is dobutamine and how is it administered?
a. (+) isomer – b1 agonist, a1 antagonist
b. (-) isomer – a1 agonist
c. Pareneteral
11. What are the direct acting adrenomimetics for B2 selective agonists? 4
a. Albuterol (Proventil, Ventolin, etc.)
b. Metaproterenol (Alupent)
c. Pirbuterol (Maxair)
d. Terbutaline (Brethine, etc.)
12. What are the 3 drugs used as nasal decongestants?
a. Phenylephrine
b. Xylometazoline
c. Oxymetazoline
13. How are the 3 nasal decongestant drugs applied?
a. Topically
14. How does phenyephrine work on the body for nasal congestion?
a. Phenylephrine
i. Activate alpha 1 receptors
1. Vasoconstriction
a. End result: shrink swollen mucosa
15. What is the difference in duration between the 3 decongestant drugs?
a. Phenylephrine: short duration of action
b. Xylometazoline and Oxymetazoline: long duration of action
16. What is the problem with chronic use of the nasal decongestants?
a. Chronic use will cause rebound nasal congestion
b. Can occur within a week of using the drug
c. Chronic use causes down regulation of the alpha 1 receptor
i. But you still are using the drug so you still get an open nasal passage
1. Yet the second you take it away, the receptors are down regulated so you get rebound nasal congestion!
17. Chronic use of alpha agnosists summary
a. Chronic activation of the a1 receptor on the nasal mucosa causes down regulation of the receptor
b. When the drug is stopped, there is insufficient endogenous NE to activate the few receptors that remain
c. This causes rebound nasal congestion
18. When you have anaphylaxis, what is the Mast cell response?
a. Release histamine, bradykinin, leuktrienes
19. When you have anaphylaxis, it is possible to get angioedema, how does epi act on this?
a. a1 – constrict capillary beds. This counteracts the dilation & increased vascular permeability of capillaries
20. when you have anaphylaxis, you can have bronchoconstriction, what does epi do to treat?
a. b2 – bronchodilation
21. when you have anaphylaxis, you can have pruritus or urticaria, what does Epi do to treat it?
a. b – suppress release of mediators from mast cells
22. when you have anaphylaxis, you can have hypotension, how does epi treat this?
a. a1, b1 – raise BP
23. Why is NE not the drug of choice for anaphylaxis?
a. NE doesn’t bind to B2 receptors, so it doesn’t treat bronchoconstriction
24. What are 2 drugs that are used in hypotension, how do they work?
a. NE and PE
i. Activate alpha 1 receptors
1. Vasoconstriction
a. Increase BP
25. What are 3 drugs that can be used to treat shock?
a. Dopamine
b. Dobutamine (gets heart squeezing, use for Cardiogenic Shock)
c. NE (used for Hypovolemic shock)
26. What is the difference between hypotension and shock?
a. Shock is extreme hypotension, and you are not perfusing organs
27. Where is the major location of dopamine receptors? What effect does this have
a. Renal vasculature
b. Causes vasodilation to increase renal blood flow (to help preserve kidneys)
28. What are 2 other locations dopamine acts (other than renal) and what is the effect?
a. Middle dose of dopamine effects B1 receptors
i. Leads to increase CO and BP
b. High dose of dopamine effects a1 receptor
i. Increase PVR and BP
29. Why does standing on your head cardiovert SVT (supraventricular tachycardia)
a. Blood flows to baroreceptor want to decrease the heart flow
i. So you INCREASE VAGAL outflow (PNS)
30. If you have AV block what do you want to give to treat? (2)
a. Want to activate B1 receptors
b. Give Epi or isoproterenol
31. What are the 4 short acting Asthma/COPD drugs?
a. albuterol
b. metaproterenol
c. pirbuterol
d. terbutaline
32. What are the 3 long acting Asthma/COPD drugs
a. salmeterol
b. formoterol
c. arformoterol
33. How does albuterol help treat asthma?
a. Activate B2 receptor, bronchodilation, open airways
34. What is the advantage of giving albuterol vs. epinephrine/isoproterenol to treat asthma?
a. Less B1 side effects
35. What drug do you give to prevent premature labor? How does it work
a. Terbutaline
b. Activation of B2 receptors to cause uterine smooth muscle relaxation
c. End result: stop uterine contractions
36. What drug can be used to dilate the pupil? What is the mechanism?
a. PE (phenyephrine)
b. Will activate alpha 1 receptor to contract iris radial smooth muscle
c. End result: Pupil dilation without cycloplegia
37. What in the F is cycloplegia?
a. Paralysis of the ciliary muscle
38. What is the adverse effect from alpha adrenergic activation (blood vessels)
a. Reduce peripheral blood flow
b. Marked elevation of BP, increased Cardiac work and precipitate cardiac ischemia, MI and failure
i. Due to increasing afterload
39. What is the adverse effect from alpha adrenergic activation at the infusion site?
a. Can have excessive contraction of blood vessels at infusion site
b. Causing ischemia and necrosis
40. What is the adverse effect from beta adrenergic activation?
a. Increased heart rate
i. Causing: Palpitations, tachycardia,
cardiac arrhythmias
ii. Increase force of contraction
1. Leading to increased workload
a. Causing angina
41. What adverse effect of B activation can be seen in the liver?
a. B2 receptor activation on liver stimulates glycogenolysis
42. What adverse effect can B activation have on skeletal muscle (negative)
a. Tremor
43. What are the contraindicaitons for direct acting adrenomimetics? 3
a. Cardiovascular disease
b. Hyperthyroidism
c. Diabetes
44. What is tyramine? Is it a drug? How does it work?
a. Indirect acting adrenomimetics
b. Not a drug
c. Promotes the release of NE from the sympathetic nerve terminal
45. What metabolizes tyramine?
a. MAO
46. If tyramine is not metabolized in the liver, what can happen?
a. It gets into the blood stream
b. Finds a NE transporter
c. Gets into sympathetic nerve terminal and displaces NE from the terminal
d. This ends up activating a1 and B receptors!
47. What may happen if a person is taking a drug that inhibits the activity of MAO (i.e., MAO inhibitor) and eats a lot of cheese and drinks a lot of beer?
a. Hypertensive crisis!
48. What are the mixed acting adrenomimetics?
a. Ephedrine (generic)
b. Pseudoephedrine (Sudafed, generic, etc.)
49. How does Ephedrine work? What kind of adrenomimetic is it?
a. Mixed acting adrenomimetic
i. Releases NE from nerve terminals
ii. Activates a and b receptors
b. Crosses the blood brain barrier
i. Mild stimulant
50. What are the approved uses of Ephedrine? 3
a. Asthma, COPD
b. Nasal congestion
51. How would ephedrine be useful for treating nasal congestion?
a. Want to activate alpha 1
i. Ephedrine causes increase release of NE
1. This activates the a1 receptors in blood vessels of the nasal mucosa (note that the ephedrine itself also activates these a1 receptors)
a. Leads to decreased nasal congestion
52. How would ephedrine be useful for treating asthma?
a. Ephedrine
i. Activates B2 receptors on bronchiole smooth muscle
1. Bronchodilation
53. Ephedrine is seldom used to treat asthma. Why?
a. Side effects
54. What are the side effects of ephedrine? 2 areas, multiple effects
a. Cardiovascular
i. Excessive stimulation of the heart (b1)
ii. Use of ephedra or ephedrine alkaloids has been temporally linked to stroke, MI, and sudden death
b. CNS
i. Insomnia
ii. Nervousness
iii. Anxiety
55. How does pseudoephedrine work? How is it different than ephedrine? What is its use? Delivery method?
a. Directly activates a, and to a lesser extent, b receptors
b. Releases NE from the nerve terminal
c. Has less CNS effects than ephedrine
d. Used as a nasal decongestant
i. Oral