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Pharmacology > Lecture 5 - Sympathetic (Adrenergic) Pharmacology > Flashcards

Lecture 5 - Sympathetic (Adrenergic) Pharmacology Flashcards

1
Q

Two types of cholinergic receptors?

A

nicotinic

muscarinic

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2
Q

______: ligand-gated ion channel, membrane depolarization

A

nicotinic

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3
Q

What do M1, M3, and M5 do?

A

activates PLC
increases Ca2+
activates PKC

*causes excitation
gastric release, smooth muscle, gladder, etc.

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4
Q

What do M2, and M4 do?

A 
inhibits AC (adenylate cyclase)
activates K+ channels
inhibits PKA

*inhibition of cardiac and smooth muscle

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5
Q

What do alpha 1 adrenergic receptors do?

A

activates PLC
increases Ca2+

causes smooth muscle contraction (vasoconstriction, sphincter, mydriasis)

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6
Q

What do alpha 2 receptors do?

A

INHIBITS THE SYSTEM THAT RELEASES IT

  • inhibits AD
  • increases K+
  • hyperpolarization

this inhibits NE release
this inhibits insulin release
-presynaptic neuron pancreatic B cells ???

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7
Q

What do B receptors do?

A

activates AC
increase PKA activation

heart, lung, and energy regulation

Increases:

  • heart rate
  • contractility
  • bronchodilation
  • vasodilation
  • glyconeogenesis
  • lipolysis
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8
Q

Parasympathetic:

constrict pupils

A

M3

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9
Q

Parasympathetic:

stimulate salivation

A

M3

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10
Q

Parasympathetic:

slow heart rate

A

M2

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11
Q

Parasympathetic:

constrict airways

A

M3

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12
Q

Parasympathetic:

stimulate activity of stomach

A

M3

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13
Q

Parasympathetic:

  • inhibit release of glucose
  • stimulate gall bladder
A

I assume it’s M3

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14
Q

Parasympathetic:

stimulate activity of intestine

A

M3

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15
Q

M odd = ?

A

stimulatory

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16
Q

M even = ?

A

relaxation

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17
Q

Parasympathetic:

contract bladder

A

M3

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18
Q

Sympathetic:

dilate pupils

A

alpha 1

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19
Q

Sympathetic:

inhibit salivation

A

beta

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20
Q

Sympathetic:

increase HR

A

B1

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21
Q

Sympathetic:

relax airways

A

B2

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22
Q

Sympathetic:

inhibit activity of stomach

A

B2

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23
Q

Sympathetic:

stimulate release of glucose and inhibit gallbladder

A

B2

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24
Q

Sympathetic:

inhibit activity of intestine

A

B2

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25
Q

Sympathetic:

secrete epinephrine and NE

A

nicotinic

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26
Q

Sympathetic:

relax bladder

A

B2

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27
Q

Sympathetic:

promote ejaculation and vaginal contraction

A

alpha 1

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28
Q

For pupil opening:

-sympathetic acts on what muscle ?

A

radial muscle of iris

contraction (alpha 1)

mydriasis (pupil dilating)

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29
Q

For pupil opening:

-parasympathetic acts on what muscle ?

A

circular muscle of iris

contraction (M3)

miosis

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30
Q

For lens focusing:

-parasympathetic acts on what muscle?

A

ciliary muscle

contraction (M3)

near vision

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31
Q

Sympathetic effect on glands

gastrointestinal glands, salivary glands, lacrimal glands, nasal glands

A

effect from B adrenergic stimulation
-secretion of protein: enzyme and mucus

effect from alpha adrenergic stimulation

  • vasoconstriction - decrease water
  • decrease and concentrate secretions

Symp:
= fewer secretions
= more concentrated secretions

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32
Q

Parasympathetic effect on glands

gastrointestinal glands, salivary glands, lacrimal glands, nasal glands

A

effect from M3 muscarinic stimulation
-water secretory product

Parasymp:
= more sections
= less concentrated secretions (more watery)

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33
Q

Sympathetic effect on systemic blood vessels

A
  • contraction of skin and splanchnic vessels (alpha 1)

- relaxation of vessels in skeletal muscle (muscarinic)

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34
Q

Parasympathetic effect on systemic blood vessels

A

endothelial cells release EDRF (M3) - causes vessels to relax

EDRF = endothelial derived relaxing factor (causes vessels to relax)

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35
Q

NE mainly stimulates ??

A

alpha 1 receptors (in vessels)

-increases BP markedly

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36
Q

E has a higher affinity for ??

A

B receptor (in cardiac muscle)

  • increases heart rate and contractility
  • less effect on mean arterial pressure
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37
Q

NE and E do the same thing in high enough quantities, but in correct quantities: ??

A 
NE = alpha 1
E = beta
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38
Q

Sympathetic effect on GI smooth muscle

A

GI smooth muscle is relaxed by B2

GI spinchter is contracted by alpha 1

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39
Q

Parasympathetic effect on GI smooth muscle

A

GI smooth muscle is contracted by M3

GI sphincter is relaxed by M2 or M4

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40
Q

Describe the baroreceptor reflex

A

1) heart failure, hypovolemia, hemorrhage, postural changes, etc
2) drop in BP
3) carotid sinus/aortic arch is decreased in firing rate of afferents
4) cardiovascular centre

5) -increase in Symp nerve activity
- decrease in parasymp nerve activity

6) -increase HR
- increase in stroke volume
- arteriolar constriction

7) BP goes back to normal

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41
Q

4 types of adrenergic receptors ?

A

alpha 1
alpha 2
beta 1
beta 2

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42
Q

What organs do adrenergic receptors effect?

A

cardiac muscle
smooth muscle
glands

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43
Q

cardiac muscle
smooth muscle
glands

All respond to ??

A

NE and E

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44
Q

___: alpha > beta

A

NE

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45
Q

___: beta > alpha

A

E

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46
Q

Functions of alpha 1 adrenergic receptors

A
  • vasoconstriction
  • pupil dilation
  • inhibits uterine contractions in pregnancy
  • ejaculation
  • contraction of bladder neck and prostate
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47
Q

What medical purpose does vasoconstriction have?

A
  • nasal decongestant

- increase BP in trauma/shock pts

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48
Q

What medical purpose does pupil dilation have?

A

eye exams

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49
Q

What medical purpose does inhibiting uterine contractions have?

A

delay birth

*usually a negative side effect of certain medications

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50
Q

What medical purpose does ejaculation have?

A

none yet - but drugs are in development

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51
Q

What medical purpose does contraction of bladder neck and prostate have?

A

it is simply a negative side effect

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52
Q

Functions of alpha 2 adrenergic receptors

A
  • inhibits neurotransmitter release thus inhibiting sympathetic (adrenergic) activation
  • inhibits it’s own neutron from firing
  • inhibitor of adrenergic system
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53
Q

Where are alpha 2 adrenergic receptors located?

A

-presynaptic junction

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54
Q

alpha 2 receptors are not perfectly opposite of alpha 1

other examples of it’s functions are: ?

A
  • cardiac (and other) vasoconstriction
  • decreased NE release in brain (a good thing?)
  • inhibition of lipolysis and insulin release
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55
Q

Primary medical importance of alpha 2 receptors is ??

A

CNs (neuronal)

hypertension

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56
Q

Functions of Beta 1 receptors

A

Kidney:
-renin release causes vasoconstriction

Heart:
-increases HR, contractility, velocity of conduction in AV node

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57
Q

Functions of beta 2 receptors

A
  • bronchial dilation
  • relaxation of uterine muscle
  • vasodilation
  • glycogenolysis (increase production of glucose)
  • glucagon release
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58
Q

What is dopamine’s function?

A

dilates renal blood vessels

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59
Q

_____ = increases vasoconstriction, pupil dilation, relaxes uterine contraction, contraction of bladder, and prostate neck, ejaculation

A

alpha 1

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60
Q

____ = cardiac vasoconstriction, inhibits NE brain release, inhibits insulin release

A

alpha 2

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61
Q

___ = increase HR and contraction, renin release

A

beta 1

62
Q

____ = lung bronchi dilation, relaxation of uterus, vasodilation, glucose release

A

beta 2

63
Q

Pseudophedrine is ??

A

agonist of alpha 1

64
Q

What does pseudophedrine do?

A

dry nose up

increase BP

65
Q

Prazosin is ??

A

antagonist of alpha 1

66
Q

What does prazosin do?

A

allows nose to drip

lowers BP

67
Q

Clonidine is ??

A

agonist of alpha 2

68
Q

What does clonidine do?

A

drop BP

relax prostate

69
Q

Isoproterenol Dobutamine is ??

A

agonist of beta 1

70
Q

What does isoproterenol dobutamine do?

A

increases HR

71
Q

Propranolol is a ??

A

antagonist of Beta 1 and beta 1

72
Q

What does propranolol do?

A

decrease HR

73
Q

Isoproterenol Terbutaline is ??

A

agonist of Beta 2

74
Q

see slide 19

A

okay man

75
Q

distribution of alpha 1

A

blood vessels

GI sphincter

76
Q

distribution of alpha 2

A

presynaptic terminal

77
Q

distribution of beta 1

A

heart

78
Q

distribution of beta 2

A

airway, GI, urogenital

79
Q

alpha 1 and beta 2 are antagonistic in some ____ ______

A

blood vessels

alpha 1 causes constriction
beta 2 causes dilation

*generally B2 dominates where both are found

80
Q

stimulators (sympathomimetic) mimic action of ???

A

norepinephrine, dopamine, and epinephrine

81
Q

List some uses of adrenergic agonists

A
  • hemodynamic compromise (shock, depressed cardiac rhythm)
  • bronchospasms (asthma)
  • nasal and sinus congestion
82
Q

Epinephrine stimulates ??

A

both alpha and beta receptors

83
Q

E is also called ?

A

adrenaline

84
Q

Epinephrine is mainly given in ______

A

emergencies:

-asthma, cardiac arrest, anaphylaxis

85
Q

Why do you give E parenterally or intramuscularly?

A

GI tract enzymes destroy the drug so it cannot be given orally

86
Q

Why would epinephrine be given with an anesthetic?

A

it causes vasoconstriction - which allows anesthetic to stay in body longer

87
Q

E = works ____, but ___-acting

A

works fast

short-acting

88
Q

What are some negative side effects of epinephrine?

A
  • stimulant effects on brain
  • hypertension-induced hemorrhage
  • cardiac arrhythmia
  • hyperglycemia in a diabetic
89
Q

NE is used primarily for?

A

-treating shock

increasing BP

90
Q

Pseudoephedrine is used for?

A

nasal decongestant

91
Q

NE and dopamine are critical for ?

A 
mood control
motor control
depression
anxiety
parkinson's disease
92
Q

What does cocaine do?

A
  • inhibits reuptake of serotonin, norepinephrine, and dopamine
  • it’s inhibiting the reuptake - so it is staying in your body longer and making you happier
  • non-selective for receptor subtype and organ
  • peripheral activation causes side effects (HR increase, sweating, hypertension, etc)
93
Q

How do amphetamines work?

A

inhibits uptake and increases neurotransmitter release (including serotonin and NE)

-very potent in the CNS and periphery

94
Q

List some types of amphetamines

A

crystal meth
ritalin
MDMA (ecstasy)

95
Q

Selegiline is a ??

A

MAOi

monoamine oxidase inhibitor

96
Q

Selegiline is used in ??

A

anti-parkinson’s disease

97
Q

Selegiline is used with ??

A

levadopa

98
Q

side effects of seligiline ?

A

dry mouth
constipation
tachycardia

99
Q

Phenelzine is ??

A

Monoamine oxidase inhibitor

100
Q

Phenelzine is used as?

A

anti-depressant

101
Q

side effects of Phenelzine

A 
dry mouth
constipation
urinary retention
mydriasis
hyperthermia
sweating
hypertension
102
Q

all anti-depressants activate ___

A

SNS

103
Q

Amitriptyline is a _____

A

TCA (tricyclic antidepressant)

104
Q

Contraindications of amitriptyline

A
  • urinary retention
  • pregnancy
  • myocardial infarction
  • congestive heart failure
105
Q

is alpha 2 sympathomimetic?

A

NO

-because they inhibit sympathetic response

106
Q

Example of an alpha 1 agonist

A

phenylephrine

107
Q

What do stimulants affect?

A

adrenergic

108
Q

Examples of stimulants

A

cocaine, nicotine, caffeine, meth

109
Q

Side effects of stimulants

A

sweats, manic behaviour, anxiety, paranoia

110
Q

Dobutamine is a

A

beta 1 agonist

111
Q

how is dobutamine used?

A
  • used in congestive heart failure

- increases cardiac output (because it is a beta 1 agonist)

112
Q

albuterol (salbutamol, ventolin) is a ??

A

beta 2 agonist

113
Q

albuterol (salbutamol, ventolin) is used for?

A

asthma, COPD

this is a short-acting inhaler
lasts 2 hrs

114
Q

salmeterol is a ??

A

beta 2 agonist

115
Q

salmeterol is used for?

A

asthma, COPD

this is long acting inhaler
lasts 12 hrs

116
Q

what do anti-adrenergic drugs do?

A

inhibit or block the effects of sympathetic nerve stimulation

117
Q

are anti-adrenergic drugs naturally occurring?

A

no - only exist as synthetic drugs

118
Q

most anti-adrenergic drugs block ??

A

alpha 1
beta 1
beta 2

119
Q

alpha 2 agonists are _____ ________

A

adrenergic antagonists

120
Q

alpha 2 agonists treat _________

A

hypertension

121
Q

clonidine is an ??

A

alpha 2 agonist

122
Q

prazosin and doxasin are ?

A

alpha 1 antagonists

123
Q

what do prazosin and doxasin treat?

A

they treat hypertension

-they are competitive blockers of alpha 1 therefore causing decreased blood pressure

124
Q

Tamsulosin is a ??

A

alpha 1 antagonist

125
Q

what does tamsulosin treat?

A

prostatic hypertrophy and vasospastic (urinary) problems

*tamsulosin is more selective for alpha 1 A receptors on prostate

126
Q

What is congestive heart failure?

A

causes decreased preload and after load by decreasing peripheral resistance (through vasodilation)
-this leads to increased cardiac output

127
Q

Explain how you can use two different drugs to treat congestive heart failure

A

-use a B1 agonist to activate the heart to increase CO
AND
-use an alpha 1 antagonist to inhibit the peripheral vessels to decrease peripheral resistance (makes it easier for the hear to pump to the periphery)

128
Q

What are some side effects of blocking alpha 1 receptors?

A
  • early on, causes massive orthostatic hypotension (fainting when standing) so need to start with low doses
  • vertigo
  • sexual dysfunction
  • reflex tachycardia
  • floppy iris syndrome (eye)
129
Q

What are beta blockers used for?

A

-used to treat rapid pulse arrhythmias, hypertension, MI, other heart problems

130
Q

beta blocker ____ contractility, CO, heart rate, and BP

A

decreases

131
Q

beta blockers ____ oxygen demand on the heart

A

decrease

132
Q

beta blocks ____ the conduction through the AV node, and slow down ventricular response

A

slows

133
Q

how many generations of beta blockers are there?

A

3

134
Q

___ gen beta blockers are non selective (they act on B1 and B2)

A

1st

135
Q

___ gen beta blockers are cardioselective (act only on B1)

A

2nd

136
Q

___ gen beta blockers are partially selective (with alpha 1 inhibition)

A

3rd

137
Q

What do non selective beta blockers do?

A

Block both beta 1 (heart) and beta 2 (lung) receptors

138
Q

Propranolol is a ?

A

non selective beta blocker

i.e. 1st gen beta blocker

139
Q

Nonselective beta blockers can cause ____

A

bronchospasms

140
Q

What would propranolol do then?

If it is a nonselective beta blocker (1st gen beta blocker)

A
  • decrease CO
  • peripheral vasoconstriction
  • slow decrease in hypertension
  • bronchoconstriction
  • decreased glycogenolysis and glucagon secretion - this amplifies the effect of insulin on hypoglycaemia
141
Q

Timolol is a ??

A

non-specific beta blocker

142
Q

What is timolol used for?

A

used for glaucoma by decreasing production of aqueous humour and intraocular pressure

143
Q

What were 2nd gen beta blockers (B1 specific blockers) developed for?

A

Developed specifically to avoid bronchoconstriction of B2 receptors

144
Q

What are 2nd gen (B1 specific blockers) used for?

A

used to treat hypertension

-reduced pulmonary, vascular, and blood glucose effects

145
Q

Atenolol is a ??

A

2nd gen (B1 specific) beta blocker

146
Q

How do 3rd gen (partial alpha receptor) beta blockers work?

A

they cause a reduction in a receptor which leads to reduced peripheral resistance and therefore causes less load on the heart

147
Q

Carvedilol is a ??

A

3rd generation beta blocker (partial alpha receptor blockage)

148
Q

How does carvedilol work?

A

It has a higher affinity for B1 and B2, so it reduces HR significantly and may exacerbate asthma

149
Q

Labetalol is a ??

A

3rd generation beta blocker (partial alpha receptor blockage)

150
Q

How does labetalol work?

A

it has a higher affinity for alpha 1 so it will reduce BP w/o a large effect on RESTING HR

Pharmacology (21 decks)

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