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Pharmacology - Exam 2 > Adrenergic Antagonists > Flashcards

Adrenergic Antagonists Flashcards

1
Q

Review: What are the adrenergic receptor types?

A
  • a1 & a2
  • b1 & b2
  • D
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2
Q

Review: Where are adrenergic receptors present?

A
  • PNS

- CNS

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3
Q

Review: What do adrenergic receptors bind?

A
  • E
  • NE
  • DA
  • other sympathomimetics
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4
Q

Review: What are the adrenergic actions on the CV system?

A
  • a1 vasoconstriction, increase BP
  • b1 increase HR and CO
  • b2 vasodilation, decrease BP
  • central a2 vasodilation
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5
Q

Review: What are the adrenergic actions on the respiratory system?

A
  • a1 decongestion

- b2 bronchodilation

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6
Q

Review: What are the adrenergic actions on the eyes?

A
  • a1 mydriasis, decrease redness

- a2 decrease IOP

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7
Q

Review: What are the adrenergic actions on the GU tract?

A
  • b2 delays fetal delivery
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8
Q

Review: What are the adrenergic actions on the secretory glands?

A
  • b increase apocrine sweat glands and salivary glands
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9
Q

Review: What are the adrenergic actions on metabolism?

A
  • overall increase energy (breakdown stores)
  • b increase glycogenolysis and lypolysis
  • a2 decrease lipolysis
  • b2 increase insulin release
  • a2 decrase insulin release
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10
Q

Review: What are the adrenergic actions on the CNS?

A
  • feelings such as wakefulness, nervousness, anorexia, & euphoria
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11
Q

What are the two types of alpha antagonists?

A
  • reversible

- irreversible

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12
Q

What is the half life of a reversible alpha antagonist?

A
  • short
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13
Q

Describe the binding of reversible alpha antagonists?

A
  • compete with agonists and endogenous catecholamines

- easily bumped off when [high] agonist

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14
Q

What is a reversible alpha antagonists duration of action dependent on?

A
  • receptor affinity

- half life

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15
Q

What is the half life of an irreversible alpha antagonist?

A
  • long
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16
Q

Describe the binding of irreversible alpha antagoinists

A
  • form covalent bonds with receptor to permanently block it
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17
Q

What is an irreversible alpha antagonists duration of action dependent on?

A
  • synthesis of new receptors
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18
Q

What is the effect of a-antagonists in the CV system?

A
  • block a1 mediated vasoconstriction

- leads to decreased peripheral vascular resistance and decreased BP

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19
Q

What are the side effects of a-antagonists in the CV system?

A
  • orthostatic HTN

- tachycardia

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20
Q

What is the effect of a-antagonists on the eyes?

A
  • block mydriasis –> miosis
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21
Q

What is the effect of a-antagonists on nose?

A
  • block nasal vasoconstriction –> sinus congestion
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22
Q

What is the effect of a-antagonists on GU tract?

A
  • block a-mediated urinary retention –> facilitates urination
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23
Q

What are examples of general a-antagonists?

A
  • phenoxybenzamine (Dibenzyline)

- phentolamine (OraVerse)

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24
Q

What are the effects of phenoxybenzamine, a general a-antagonist?

A
  • irreversible blockage of a1>a2
  • blockade of vasoconstriction leading to vasodilation
  • blocks presynaptic a2 receptors
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25
Q

What can general a-antagonist be used to treat?

A
  • excessive catecholamine release (pheochromocytoma)
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26
Q

What are the effects of phentolamine, a general a-antagonist?

A
  • reversible blockade of a1 and presynaptic a2

- a1 blocking effects include decrease peripheral vascular resistance

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27
Q

What are the general classes of a1 antagonists?

A
  • suffix: -osin
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28
Q

What class is tamsulosin and how does it work?

A
  • a1 antagonist

- relaxes arterial and venous smooth muscle and smooth muscle in prostate

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29
Q

What is a treatment for BPH?

A
  • tamsulosin
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30
Q

What is a side effect of a1 antagonists?

A

HTN

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31
Q

How do b-receptor antagonists bind?

A
  • reversibly
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32
Q

What is a “beta blocker”?

A
  • b-antagonist in the CV system
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33
Q

What are beta blockers used for?

A
  • controlling high BP

- angina, CHF, MI

34
Q

How do beta blockers work?

A
  • reduce cardiac workload by blocking peripheral b2 receptors to cause vasodilation
35
Q

How do beta blockers help angina patients?

A
  • improve the balance between O2 supply and depand
36
Q

Beta blockers block the _________ effects that would occur under _________ conditions.

A
  • adrenergic

- sympathetic

37
Q

What are contraindicated in patients with asthma and COPD and why?

A
  • beta blockers

- no pure b1 blockers available therefor condition could be worsened by ‘dirty’ actions of beta blockers

38
Q

What clinical use do beta blockers have on the eye?

A
  • tx open angle glaucoma

- decreases production of aqueous humor which reduces IOP

39
Q

What are examples of beta blockers used for glaucoma?

A
  • betaxolol (Betoptic)
  • timolol (Timoptic)
  • carteolol (Ocupress)
40
Q

What are some unexpected effects of beta blockers?

A
  • block glucose mobilization, consistent with a1
  • worsen high cholesterol, not usually an issue since they are usually on a 2nd rx to lower cholesterol
  • intrinsic sympathomimetic activity
  • local anesthetic activty
41
Q

What is a metabolic effect of beta blockers?

A
  • block glucose mobilization
42
Q

What are the effects of beta blockers on cholesterol?

A
  • increase VLDL

- decrease HDL (not good)

43
Q

Define intrinsic sympathomimetic activity (ISA)

A
  • partial agonist of a beta blocker
44
Q

What are the effects of ISA?

A
  • decrease likelihood of negative features of beta blockers (i.e. bronchoconstriction and bradycardia)
  • reduce therapeutic effects of beta blockers with ISA activity
45
Q

What are drugs with ISA activity?

A
  • labetalol
  • pindolol
  • acebutolol
46
Q

How do beat blockers achieve local anesthetic qualities?

A
  • block Na+ channels in nerve axons, prevents depolarization and transfer of information
47
Q

What are the clinical indications for beta blocker use?

A
  • HTN
  • ischemic heart dz
  • arrhthmias
  • heart failure
  • glaucoma
  • migraine H/A
  • performance anxiety
48
Q

What determines if a patient should be using beta blockers for HTN as their 1st line option?

A
  • “compelling indications”

- i.e. heart failure, post-MI, angina, diabetes and more

49
Q

What are the #1 and #2 beta blockers for HTN?

A
  • metoprolol (Lopressor, Toprol)

- atenolol (Tenormin)

50
Q

How do beta blockers treat ischemic heart disease?

A
  • b1 blockers decrease cardiac workload via decreased HR and strength of squeeze
  • results in less O2 demand making the available O2 enough
51
Q

What are beta blockers that are used to treat ischemic heart disease?

A
  • propranolol (Inderal)

- metoprolol (Loressor)

52
Q

Define arrhytmia

A
  • abnormal electrical rhythms in cardiac m.
53
Q

How do beta blockers treat arrhythmias?

A
  • suppress supraventricular and ventricular arrhythmias
  • extend resting period of AV node
  • slows ventricular response
54
Q

What are examples of beta blockers that treat arrhythmias?

A
  • metoprolol (Lopressor)

- sotalol (Betapace)

55
Q

What is the general effect of beta blockers on the heart?

A
  • decrease HR
56
Q

T/F: Beta blockers are useful in patients with acute heart failure.

A
  • False, chronic
57
Q

What is the effect of beta blockers on the eye?

A
  • decrease aqueous humor to decrease IOP
58
Q

How are beta blockers useful to treat hyperthyroidism?

A
  • decrease symptoms by blocking adrenergic receptors

- decrease the conversion of T4 to T3

59
Q

How are beta blockers helpful in treating migraine H/As?

A
  • reduce frequency and/or intensity
60
Q

How are beta blockers helpful in treating performance anxiety?

A
  • slows HR

- reduces palmar sweating

61
Q

How are beta blockers helpful in treating hepatic disease?

A
  • reduce elevated BP, specifically in portal vein
62
Q

What are the major unwanted side effects of beta blockers?

A
  • bradycardia
  • worsening of asthma
  • worsening of CO in patients with heart failure
  • exacerbation of hypoglycemia in diabetics
63
Q

What are the minor unwanted side effects of beta blockers?

A
  • mild sedation
  • vivid dreams
  • depression
64
Q

What drug typically gives minor unwanted side effects?

A
  • propranolol
65
Q

T/F: Beta blockers cannot be stopped abruptly.

A
  • True
66
Q

What is a risk of abruptly stopping a beta blocker?

A
  • rebound HTN
67
Q

How do you choose a beta blocker?

A
  • *clinical studies**
  • safety issues
  • partial agonist activity
  • differences in metabolism
  • differences in elimination half-life
68
Q

What metabolizes ACh?

A
  • AChE
69
Q

What metabolize NE, E, and DA?

A
  • MAO

- COMT

70
Q

What does NET do?

A
  • decreases NE

- reuptakes NE

71
Q

What occurs with a1 receptors are stimulated inthe CV system?

A
  • vasoconstriction
72
Q

What occurs with a2 receptors are stimulated in the CV system?

A
  • peripheral: vasoconstriction

- central: vasodilation to lower BP

73
Q

What occurs with b1 receptors are stimulated in the CV system?

A
  • increase HR

- increase contractility

74
Q

Where are b1 receptors mostly located in the CV?

A
  • heart
75
Q

What occurs with b2 receptors in CV system?

A
  • vasodilation to decrease BP
76
Q

Where are b2 receptors found in the CV system?

A
  • peripherally
77
Q

What is the effect of an adrenergic antagonist (a1 antagonist) on the CV system?

A
  • vasodilation
78
Q

What is the effect of an adrenergic antagonist (b1) on the CV system?

A
  • decrease HR

- decrease contractility

79
Q

What is the effect of an adrenergic antagonist on the lungs?

A
  • bronchoconstriction
80
Q

What is the effect of an adrenergic antagonist on glucose in blood?

A
  • blocks mobility
  • blocks lipolysis
  • blocks availability of glucose

Pharmacology - Exam 2 (4 decks)

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