Adrenergic Antagonists Flashcards
(80 cards)
1
Q
Review: What are the adrenergic receptor types?
A
- a1 & a2
- b1 & b2
- D
2
Q
Review: Where are adrenergic receptors present?
A
- PNS
- CNS
3
Q
Review: What do adrenergic receptors bind?
A
- E
- NE
- DA
- other sympathomimetics
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
5
Q
Review: What are the adrenergic actions on the respiratory system?
A
- a1 decongestion
- b2 bronchodilation
6
Q
Review: What are the adrenergic actions on the eyes?
A
- a1 mydriasis, decrease redness
- a2 decrease IOP
7
Q
Review: What are the adrenergic actions on the GU tract?
A
- b2 delays fetal delivery
8
Q
Review: What are the adrenergic actions on the secretory glands?
A
- b increase apocrine sweat glands and salivary glands
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
10
Q
Review: What are the adrenergic actions on the CNS?
A
- feelings such as wakefulness, nervousness, anorexia, & euphoria
11
Q
What are the two types of alpha antagonists?
A
- reversible
- irreversible
12
Q
What is the half life of a reversible alpha antagonist?
A
- short
13
Q
Describe the binding of reversible alpha antagonists?
A
- compete with agonists and endogenous catecholamines
- easily bumped off when [high] agonist
14
Q
What is a reversible alpha antagonists duration of action dependent on?
A
- receptor affinity
- half life
15
Q
What is the half life of an irreversible alpha antagonist?
A
- long
16
Q
Describe the binding of irreversible alpha antagoinists
A
- form covalent bonds with receptor to permanently block it
17
Q
What is an irreversible alpha antagonists duration of action dependent on?
A
- synthesis of new receptors
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
19
Q
What are the side effects of a-antagonists in the CV system?
A
- orthostatic HTN
- tachycardia
20
Q
What is the effect of a-antagonists on the eyes?
A
- block mydriasis –> miosis
21
Q
What is the effect of a-antagonists on nose?
A
- block nasal vasoconstriction –> sinus congestion
22
Q
What is the effect of a-antagonists on GU tract?
A
- block a-mediated urinary retention –> facilitates urination
23
Q
What are examples of general a-antagonists?
A
- phenoxybenzamine (Dibenzyline)
- phentolamine (OraVerse)
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
25
What can general a-antagonist be used to treat?
- excessive catecholamine release (pheochromocytoma)
26
What are the effects of phentolamine, a general a-antagonist?
- reversible blockade of a1 and presynaptic a2
| - a1 blocking effects include decrease peripheral vascular resistance
27
What are the general classes of a1 antagonists?
- suffix: -osin
28
What class is tamsulosin and how does it work?
- a1 antagonist
| - relaxes arterial and venous smooth muscle and smooth muscle in prostate
29
What is a treatment for BPH?
- tamsulosin
30
What is a side effect of a1 antagonists?
HTN
31
How do b-receptor antagonists bind?
- reversibly
32
What is a "beta blocker"?
- b-antagonist in the CV system
33
What are beta blockers used for?
- controlling high BP
| - angina, CHF, MI
34
How do beta blockers work?
- reduce cardiac workload by blocking peripheral b2 receptors to cause vasodilation
35
How do beta blockers help angina patients?
- improve the balance between O2 supply and depand
36
Beta blockers block the _________ effects that would occur under _________ conditions.
- adrenergic
| - sympathetic
37
What are contraindicated in patients with asthma and COPD and why?
- beta blockers
| - no pure b1 blockers available therefor condition could be worsened by 'dirty' actions of beta blockers
38
What clinical use do beta blockers have on the eye?
- tx open angle glaucoma
| - decreases production of aqueous humor which reduces IOP
39
What are examples of beta blockers used for glaucoma?
- betaxolol (Betoptic)
- timolol (Timoptic)
- carteolol (Ocupress)
40
What are some unexpected effects of beta blockers?
- 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
What is a metabolic effect of beta blockers?
- block glucose mobilization
42
What are the effects of beta blockers on cholesterol?
- increase VLDL
| - decrease HDL (not good)
43
Define intrinsic sympathomimetic activity (ISA)
- partial agonist of a beta blocker
44
What are the effects of ISA?
- decrease likelihood of negative features of beta blockers (i.e. bronchoconstriction and bradycardia)
- reduce therapeutic effects of beta blockers with ISA activity
45
What are drugs with ISA activity?
- labetalol
- pindolol
- acebutolol
46
How do beat blockers achieve local anesthetic qualities?
- block Na+ channels in nerve axons, prevents depolarization and transfer of information
47
What are the clinical indications for beta blocker use?
- HTN
- ischemic heart dz
- arrhthmias
- heart failure
- glaucoma
- migraine H/A
- performance anxiety
48
What determines if a patient should be using beta blockers for HTN as their 1st line option?
- "compelling indications"
| - i.e. heart failure, post-MI, angina, diabetes and more
49
What are the #1 and #2 beta blockers for HTN?
- metoprolol (Lopressor, Toprol)
| - atenolol (Tenormin)
50
How do beta blockers treat ischemic heart disease?
- b1 blockers decrease cardiac workload via decreased HR and strength of squeeze
- results in less O2 demand making the available O2 enough
51
What are beta blockers that are used to treat ischemic heart disease?
- propranolol (Inderal)
| - metoprolol (Loressor)
52
Define arrhytmia
- abnormal electrical rhythms in cardiac m.
53
How do beta blockers treat arrhythmias?
- suppress supraventricular and ventricular arrhythmias
- extend resting period of AV node
- slows ventricular response
54
What are examples of beta blockers that treat arrhythmias?
- metoprolol (Lopressor)
| - sotalol (Betapace)
55
What is the general effect of beta blockers on the heart?
- decrease HR
56
T/F: Beta blockers are useful in patients with acute heart failure.
- False, chronic
57
What is the effect of beta blockers on the eye?
- decrease aqueous humor to decrease IOP
58
How are beta blockers useful to treat hyperthyroidism?
- decrease symptoms by blocking adrenergic receptors
| - decrease the conversion of T4 to T3
59
How are beta blockers helpful in treating migraine H/As?
- reduce frequency and/or intensity
60
How are beta blockers helpful in treating performance anxiety?
- slows HR
| - reduces palmar sweating
61
How are beta blockers helpful in treating hepatic disease?
- reduce elevated BP, specifically in portal vein
62
What are the major unwanted side effects of beta blockers?
- bradycardia
- worsening of asthma
- worsening of CO in patients with heart failure
- exacerbation of hypoglycemia in diabetics
63
What are the minor unwanted side effects of beta blockers?
- mild sedation
- vivid dreams
- depression
64
What drug typically gives minor unwanted side effects?
- propranolol
65
T/F: Beta blockers cannot be stopped abruptly.
- True
66
What is a risk of abruptly stopping a beta blocker?
- rebound HTN
67
How do you choose a beta blocker?
* *clinical studies**
- safety issues
- partial agonist activity
- differences in metabolism
- differences in elimination half-life
68
What metabolizes ACh?
- AChE
69
What metabolize NE, E, and DA?
- MAO
| - COMT
70
What does NET do?
- decreases NE
| - reuptakes NE
71
What occurs with a1 receptors are stimulated inthe CV system?
- vasoconstriction
72
What occurs with a2 receptors are stimulated in the CV system?
- peripheral: vasoconstriction
| - central: vasodilation to lower BP
73
What occurs with b1 receptors are stimulated in the CV system?
- increase HR
| - increase contractility
74
Where are b1 receptors mostly located in the CV?
- heart
75
What occurs with b2 receptors in CV system?
- vasodilation to decrease BP
76
Where are b2 receptors found in the CV system?
- peripherally
77
What is the effect of an adrenergic antagonist (a1 antagonist) on the CV system?
- vasodilation
78
What is the effect of an adrenergic antagonist (b1) on the CV system?
- decrease HR
| - decrease contractility
79
What is the effect of an adrenergic antagonist on the lungs?
- bronchoconstriction
80
What is the effect of an adrenergic antagonist on glucose in blood?
- blocks mobility
- blocks lipolysis
- blocks availability of glucose
