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.Pharmacology > Chapter 10: Adrenergic Agents > Flashcards

Chapter 10: Adrenergic Agents Flashcards

1
Q

modulation of the sympathetic nervous system can be done in 2 ways: ___ and ___

A

interacting with adrenergic receptors (direct); modulating amount of NE released into synapses (indirect)

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2
Q

t/f alpa ardrenergic receptors have multiple isoforms within each subtype

A

true

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3
Q

where are a1 receptors located?

A

vascular smooth muscle, prostate, heart

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4
Q

stimulation of a1 receptors has what physiologic response?

A

contraction

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5
Q

what is the mechanism of a1 receptors?

A

couple to gq protein, increase ca, increase contraction

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6
Q

what is the locatio of the a2 receptors?

A

cns

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7
Q

stimulation of a2 receptors has what physiologic response?

A

decreased NT release, indirect effect on decreasing heart contraction

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8
Q

what is the mechanism for A2 receptors?

A

couple to Gi protein, decrease cAMP levels

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9
Q

congestion in allergic rhinitis is caused by

A

swelling surrounding vascular tissue by immune cells infiltrating the area in response to histamine

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10
Q

stimulating a1 receptors activates the ____ coupled protein, increasing ___ and ___ which increaing intracelluar ___ leading to the smooth muscle contraction

A

Gq; Dag anf IP3; ca

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11
Q

what is the effect of A1 receptor activation on the sinuses?

A

constriction of blood vessels, reducing leakiness and infiltration of immune cellls to the area, resulting in congection

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12
Q

phenylephrine is a ____ commonly found in over the counter decongestants like tylenol sinus and is also found in combination products like cold and flu remedies

A

A1 receptor agonist

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13
Q

the actions of phenylephrine to reduce congestion may have adverse effects in patients with ____

A

hypertension

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14
Q

blocking the A1 receptor reduces ____ of the prostate and facilitates ____ of the bladder

A

smooth muscle contraction; voiding

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15
Q

A1A is found in the ___ smooth muscle

A

prostate

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16
Q

A1B is found in the ___ smooth muscle

A

vascular

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17
Q

list 2 examples of A1A receptor antagonists

A
  1. prazosin

2. tamsulosin

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18
Q

what receptors does prazosin act on?

A

A1A and A1b adrenergic receptors

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19
Q

what is an off target effect of prazosin?

A

lowering blood pressure

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20
Q

tamslulosin is more selective for what type of receptor?

A

A1A adrenergic receptor (no effect on BP)

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21
Q

excessive use of local phenylephrine in nasal spray can cause ___ of the A1 adrenergic receptors

A

downregulation

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22
Q

if congestion gets worse as a result of down regulation of the A1 adrenergic receptor, will adding more agonist (decongestant drug) help?

A

NO!

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23
Q

presynaptically in the CNS, stimulation of A2 receptors ___ the release of NT

A

reduces

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24
Q

A2 receptors are often called ____ receptors

A

auto

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25
Q

the function of autoreceptors is to reduce ___ by limiting the amount of ___ that can be released in the synapse

A

over-stimulation; NT

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26
Q

A2 receptors are expressed on the ___ neurons

A

presynaptic

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27
Q

stimulation of the autoreceptors reduces excitability of the ___ neuron

A

presynaptic

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28
Q

explain the inhibitory process that follows the activation of an A2 receptor

A

Gi coupled signalling cascade is activated, inhibiting adenyl cyclase and reducing cAMP and reduced opeining of Ca channels whcih prevents the release of NE vessicles

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29
Q

clonidine is an example of an A2 adrenergic receptor ___

A

agonist

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30
Q

what is the function of clonidine?

A

stimulates A2 receptors to reduce the amount of released of NE

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31
Q

what is the therapeutic use of clondidine? In what patients does it work best in?

A

lower bp ; those not responding to other antihypertensives

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32
Q

which of the beta receptors are more widespread in the body?

A

B2

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33
Q

B1 receptors are located in the ___

A

heart

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34
Q

both B receptors cause the increase in production of ___

A

cAMP

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35
Q

both B receptors are coupled to what G protein?

A

Gs

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36
Q

stimulation of B 1 receptors causes

A

increased heart rate and contractility

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37
Q

what the effect of lung B2 stimulation?

A

bronchodilation

38
Q

what is the effect of smooth muscle B2 stimulation?

A

relaxes

39
Q

what is the effect of liver b2 stimulation?

A

glycogenolysis

40
Q

NE, E and dobutamine are examples of B1 ____

A

agonists

41
Q

dobutamine is a ___ B1 agonist that can be used in emergency situations to increase ___

A

synthetic; cardiac output

42
Q

in cardiac cells, the increae in cAMP activates ___

A

PKA

43
Q

what is the effect of PKA on cardiac cells?

A

phosphorylate voltage-gated ca channels, which increases the amount of Ca that enters the cells during membrane depolarization, therefore greater cardiac output

44
Q

epinephrine causes an increase in the mean ____ bp

A

arterial

45
Q

blocking B1 with propranolol prevents the actions on epinephrine in the ___ but not in the ___

A

cardiac muscle; blood vessels

46
Q

competitive antagonists of B adrenergic receptors are typically called ___

A

beta blockers

47
Q

the clinical use of propranolol has declined and selective b blockers like ___ are on the rise

A

metroprolol

48
Q

metoprolol and other selective B blockers are preferred because they …

A

act in cardiac tissue and have fewer unintended effects

49
Q

propranolol is a ___ beta blocker

A

non-selective

50
Q

metoprolol is a ___ B blocker

A

selective

51
Q

____ was one of the first clinically available B blockers for hypertension

A

propranolol

52
Q

propranolol is very ____ , has a high ___ and can enter the ___

A

lipophillic, Vd; CNS

53
Q

metoprolol has ___ agonist activity

A

inverse

54
Q

topical b blockers in the form of eyedrops are used for treatment of ___ . Is this a common course of treatment for this condition?

A

glaucoma ; no but it used to be very popular

55
Q

what are the 2 effects of using topical b blockers in glaucoma?

A
  1. decreases aq humour production

2. decreases IOP

56
Q

give an example of topical beta blocker used in the treatment of glaucome

A

timolol

57
Q

which beta receptor is suggested to be the path to lowering IOP in the use of timolol?

A

B2

58
Q

timolol is a ___ B blocker

A

non-selective

59
Q

in the lungs, modulation of B2 receptors is important to treating conditions such as ___ and ___

A

asthma and COPD

60
Q

B2 are expressed extensively in the ____

A

lungs

61
Q

endogenously, ___ has a higher affinity for B2 receptors than ___

A

E; NE

62
Q

when the symapthetic system is activated, much of the response in the lungs is due to what NT?

A

epinephrine

63
Q

____ is used to treat bronchoconstriction in anaphylactic shock

A

epinephrine

64
Q

epinephrine has actions at A1 and B1 receptors, so to decrease bronchocondtriction, there are also significant cardiovascular effecst, why is this not too big of an issue?

A

half life of epinephrine is short, so effects are not prolonged

65
Q

what is salbutamol?

A

synthetic B2 receptor agonist that is inhaled to cause bronchodilation

66
Q

where does salbutamol act?

A

locally in the lungs

67
Q

the action of salbutamol occurs ____

A

rapidly

68
Q

when is salbutamol administered?

A

at onset of symptoms in patients with asthma

69
Q

B2 agonists such as salbutamol are typically called ____ medications for the treatment of asthma

A

rescue

70
Q

pseudophedrine is an example of a ___ adrenergic receptor agonist

A

mixed

71
Q

pseudoephedrine can be found in some OTC ____ products, but has been controllled due to it being a starting material for making ___

A

cold and decongestant; methamphetamine (crystal meth_

72
Q

the primary therapeutic target of pseudoephedrine is ___ receptors to cause ___

A

A1; vasoconstriction

73
Q

pseudoephedrine also targets ___ receptors, which increases cardiac output

A

beta

74
Q

the effect of pseudoephedrine on B receptors can be problematic for patients with ___

A

hypertension

75
Q

t/f blocking both A and B receptors reduces BP more than if only one was activated alone

A

true

76
Q

Carvediol is an ____ of B1, B2 and a1 receptrs

A

antagonist

77
Q

what is the primary action of carvediol?

A

lower bp

78
Q

carvediol binds reversibly or irreversibly?

A

reversibly

79
Q

what is the order of receptor affinity from highest to lowest in carvediol ?

A

B1, A1, B2

80
Q

blocking B2 may worsen they symptoms of __ and ___

A

asthma and COPD

81
Q

blocking A1 may worsen the symptoms of ___

A

orthostatic hypotension

82
Q

what patients should not take carvediol?

A

patients with asthma, COPD and hypotension

83
Q

___-like drugs are structurally similar to catecholamines, thus are good substrates for catecholamine transporters

A

amphetamine

84
Q

what is the action of amphetamine/

A

enters presynaptic cell ny NET, taken into the NE vessicles by VMAT and then displaces NE from the vessicle and accumulate in the cytoplasm until it is passively released into the synapse

85
Q

are action potentials required for amphetamine to cause release of NE?

A

no

86
Q

adderall is the amphetamine available as an RX for patients with

A

ADHD

87
Q

speed is an example of an ___

A

amphetamine

88
Q

when acting on the CNS, amphetamine in most people casues a ___

A

rush or a high

89
Q

___ and ____ block the NET transporter, preventing NE reuptake into presynaptic neuron

A

cocaine and atomoxetine

90
Q

therapeutically, atomoxetine is another Rx option for

A

ADHD

.Pharmacology (55 decks)

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