Adrenergic Agonists II And Antgagonists Flashcards

1
Q

Affects of alpha 2 agonists on the vascular system

A

When give orally they accumulate int he CNS and reduce sympathetic outflow and blood pressure
Reflex tachycardia

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2
Q

B2 agonists effect on the vascular system

A

Vasodilate, decrease blood pressure

Reflex tachycardia

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3
Q

Effects of low doses of dopamine on the vascular system

A

Vasodilation of renal vessels
D1
W

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4
Q

What is considered the renal dose of dopamine

A

Low dose

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5
Q

Medium doses of dopamine on the vascular system

A

Works on B1 receptors

Stimulates HR and force

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6
Q

What is considered the cardiac dose of dopamine

A

Medium dose

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7
Q

High dose of dopamine on the vascular system

A

Acts on alpha 1

Increases BP

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8
Q

What are the direct acting adrenergic agonists

A
NE
Epi
Isoproterenol
Phenylephrine 
Albuterol 
Mirabegron
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9
Q

What receptors do NE target

A

A1, a2, b1 agonist

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10
Q

Main action of NE

A

Increases TPR and BP, initial tachycardia followed by long term bradycardia (reflex)

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11
Q

What receptors do epi work on

A

A1,a2,b1,b2 agonist

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12
Q

Low dose of epi

A

Activate beta receptors

-lowers BP and increases HR

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13
Q

High doses of epi

A

Activate alpha receptors

-increases BP, initial tachycardia followed by lone term bradycardia

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14
Q

Between epi and NE, which one can increases blood pressure?

A

Both

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15
Q

Between NE and epi, which one can decrease blood pressure

A

Epi in low doses

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16
Q

What is the difference between NE and epi

A

epi can stimulate B2 receptors
-B2 receptors are not innervated, so NE cannot get to them, but since Epi is in the blood, it can stimulate them that way.

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17
Q

What receptors get targeted in low dose NE

A

All receptors

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18
Q

At what dose does epi look like NE

A

High doses

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19
Q

How do NE and epi both increases BP

A

Alpha one receptors

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20
Q

Adrenergic receptor sensitivity

A

B>a at low doses

A effects dominant at high doses

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21
Q

Dopamine receptor sensitivity

A

D1>B1>a1

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22
Q

What kind of agonist is isoproterenol

A

B1B2

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23
Q

What does isoproterenol do

A

Lower BP and increases HR

  • looks like low dose epi
  • not used clinically bc it causes arrhymias
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24
Q

What kind of agonist is phenylephirine

A

A1

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25
Q

What does pehnylephrine do

A

Increased BP but causes reflex bradycardia; mydriasis

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26
Q

What kind of agonist is albuteral

A

B2 agonist

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27
Q

What kind of agonist is mirabegron

A

B3 agonist for unirnary incontinence, some B1 effects that may increases BP
-relaxes detrusor muscle

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28
Q

What are the indirect acting adrenergic agonists

A

Amphetamine
Tyramine
Cocaine

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29
Q

These dont act on alpha or beta receptors but rather are taken up into the presynaptic neuron where they enhance the release of NE from synaptic vesicles

A

Indirect acting adrenergic agonists

-kinda do the same work as achase inhibitors but on different NT

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30
Q

Amphetamine

A
  • indirect acting adrenergic agonist
  • enhances NE release from adrenergic nerve terminals
  • stimulates the CNS
  • stimulant
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31
Q

Tyramine

A
  • indirect-acting adrenergic agonist
  • not a drug
  • found in wine, ripe cheese, and soy sauce
  • oxidized by MAO, normally has no effect on person
  • if pt taking MAOIs, then these could result in hypertensive crisis
  • stimulant
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32
Q

If someone is on an MOAI antidepressant, why should they avoid red wine, ripe cheese, and soy sauce?

A

These foods contain tyramine which is metabolized by MAO. If you inhibit the MAO, you wont metabolize tyramines and you will get a NE agonist effect that could cause a hypertensive crisis
-rare but fatal

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33
Q

Cocaine

A
  • indirect acting adrenergic agonist
  • blocks the reuptake of NE
  • increased NE at synapse causes stimulant effect
  • a1 and B1 agonist specifically
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34
Q

Why is there nasal ischemia in someone who snorts cocaine

A

Tons of alpha1 being stimulated by NE, causing vasoncsontriction

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35
Q

What is the mixed action adrenergic agonist

A

Ephedrine

36
Q

Ephedrine

A
  • mixed-action adrenergic agonist
  • enhances release of NE from nerve terminals
  • can also directly stimulate the a and B receptors
  • acts like amphetamine AND epi
37
Q

Characterized by being able to enhance the release of NE and stimulate the a and b receptors

A

Mixed action adrenergic agonists like ephedrine

38
Q

Why was pseudoephredrine replaced with phenylephrine

A

Because people were making meth with it

39
Q

What do we use for anaphylaxis

A

Adrenergic agonist

Epinephrine is the drug of choice

40
Q

Adrenergic agonist on the eye

A

Alpha1 agonists like phenylephrine used topically to produce mydriasis for eye exams

41
Q

Adrenergic agonist and the bronchi

A

B2 agonists are the drug of choice for acute asthmatic bronchoconsriction (allbuterol)

42
Q

Adrenergic agonist and nasal decongestion

A

A1 agonists cause vasoconstriction and decrease nasal secretions (phenylephrine)
-used to be ephedrine

43
Q

Using epinephrine for an anaphylactic reaction has what kind of binding?

A

Physiologic binding with histamine. They both bind different receptors

44
Q

What are the two categories of adrenergic antagonists

A

B blockers

A blockers

45
Q

Phenoxybenzamine

A

Alpha adrenergic blocker
Irreversible, long acting
Long half life bc irreversible
Non selective

46
Q

Why does phenoxybenzamine have a long half life

A

Because it is irreversible

47
Q

Which alpha adrenergic blocker as a covalent bond with a1 and a2 receptors

A

Phenoxybenzamine

48
Q

What are the reversible, shorter acting, alpha adrenergic agonists that are selective for a1?

A
ZOSINS!
Prazosin
Doxazosin
Terazosin
Alfuzosin
49
Q

What is ther reversible, shorter acting, nonselective adrenergic agonist?

A

Phentolamine

50
Q

What is the reversible, shorter acting adrenergic antagonist that is selective for a2?

A

Mirtazapine

51
Q

What happens when you block alpha 2 receptors

A

Can be done with mirtazapine

Increases NE, blocking negative feedback

52
Q

Effects of alpha 1 blockers

A
ZOSINs
Vasodilate
Decrease BP
Reflex tachycardia
-this is limited because the negative feedback from the alpha2 receptors is still working
53
Q

Effects of an alpha adrenergic blocker such as phentolamine

A

Blocks a1 and a2
Decrease BP
Reflex tachycardia
-increased tachycardia because the negative feedback from a2 is knocked out

54
Q

Which will have a more severe tachycardia, phentolamine or prazosin?

A

Phenylalanine

55
Q

A catecholamine secreting tumor of cells from the adrenal medulla

A

Pheochromocytoma

56
Q

What does pheochromocytoma do to epi and NE

A

Increases both, which increases BP

57
Q

Treatment for pheochromocytoma

A

Phenoxybezamine is useful as treatment prior to surgery or for maintenance therapy if surgery is not desired

  • want to give them thsis drug because it blocks a1 (and a2 but that does not matter here).
  • a zosin could be used, but we just dont do it
58
Q

Primary benefit of using phenoxybenzamine for pheochromocytoma

A

Block of peripheral alpha 1 receptors (even though this drug also blocks a2 receptors)

59
Q

How do you remember that phenoxybexamine is a treatment for pheochomocytoma?

A

They both have the same amount of letters and they both start with PHE

60
Q

A condition caused by enlargement of the prostate gland; the urethra beceoms compressed and causes urinary obstruction

A

Benign prostatic hyperplasia

61
Q

What is benign prostatic hyperplasia treated with

A

Doxazosin, tamsulosin

62
Q

Why are doxazosin and tamsulosin good for treating benign prostatic hyperplasia?

A

Block a1 receptors in the lower urinary tract and prostate

63
Q

What is the BEST drug for benign prostatic hyperplasia and why?

A

Tamsulosin, it targets alpha1A receptors, the predominant subtype of alpha receptor found in the prostate

64
Q

What is the predominant alpha receptor in the prostate

A

Alpha1A

65
Q

What drugs should someone with benign prostatic hyperplasia avoid

A

Alpha1 agonists

66
Q

If someone has benign prostatic hyperplasia and hypertension, what is a good treatment plan for them

A

Normally we treat with tamsulosin because it targets the exact receptor we need it to (alpah1A), but if they have hypertension, and we give them any zosin, it will take care of both problems.

67
Q

What drugs do we use to react hypertension

A

Prazosin, doxazosin (alpha blockers)

Really any zosin

68
Q

What is the mechanism of zosins treating HTN

A

Block of peripheral a1 receptors vasodilate and lowers TPR and BP

69
Q

Toxicity of alpha blockers

A
  • ortho static (postural) hypotension

- reflex tachycardia

70
Q

Orthostatic hypotension from alpha blocker toxicity

A

The a1 selective blockers are associated with an exaggerated orthostatic hypotensive response to the first dose, therefore the first dose is usually small

71
Q

How do you avoid getting orthostatic hypotension with an alpha blocker

A

Take a smaller dose to begin with and work your way up

72
Q

Reflex tachycardia as a slide effect of alpha blockers

A

More with nonsense to explain alpha blockers, could cause an angina attack

73
Q

What do the names of all B blockers end in

A

Olol

74
Q

What are the exceptions of B blockers names not ending in olol

A

Labetalol

Carvedilol

75
Q

What are the nonspecific B blockers?

A
Propranolol 
Nadolol
Timolol
Pindolol
Penbutolol

ALL IN 2ND HALF OF ALPHABET (N-Z)
N=NONSPECIFIC
BLOCK B1 and B2

76
Q

What are the B1 specific blockers

A
Atenolol 
Betaxolol 
Bisoprolol
Esmolol
Acebutolol
Metoprolol

ALL IN THE FIRST HALF OF THE ALPHABET(A-M)

77
Q

Which drugs are alpha1 and B blockers?

A

Labetalol
Carvedilol

They are a1 and B blockers if ending in alol or ilol

78
Q

Beta blockers and local anesthetic

A

Certain B blockers can have a local anesthetic action, except in the eye, these drugs are never used topically in the eye where anesthesi of the cornea is highly undesirable

79
Q

Why do we never use topical beta blockers in the eye

A

Because they have local anesthetic effects, we do not want to anesthetize the cornea

80
Q

Cardiovascular effects of B blockers

A

Block of B1 receptors on the heart causing decreased HR

Block of B2 receptor prevents vasodilation

81
Q

Renal effects of B blockers

A

Block of B1 receptors inhibits the release of renin

82
Q

Bronchoconstircion with B blockers

A

Block of B2 receptors on the lungs causes bronchoconstriction (problems with asthma or COPD)

83
Q

Glucose metabolism and B blockers

A

Block of B2 receptors causes decreased glycogenolysis and lowers blood glucose

84
Q

Glaucoma and B blockers

A

Decreases IOP by decreases aqueous humor production by the ciliary body (beta-2 block)

85
Q

Adverse effects of B blockers

A
  • hypotension, bradycardia, fatigue, drowsiness
  • bronchoconstriction
  • CNS depression
  • increased lipids (unknown why)
86
Q

Chronic presence of B blocker

A

Will cause the up regulation of B1 receptors on the heart and abrupt discontinuation could cause angina, HTN or arrhythmia
-always taper