Adrenergic Neurotransmission Flashcards

1
Q
A
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2
Q

Explain parasympathetic

A
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3
Q

Explain sympathetic

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4
Q
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5
Q

What does the adrenergic neurotransmission process include

A

Biosynthesis
Storage
Release
Interaction

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6
Q

Explain biosynthesis

A
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7
Q

Explain termination process

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8
Q

List the drug targets

A
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9
Q

What are the adrenergic chemical messengers

A

Noradrenaline (norepinephrine)
Adrenaline (epinephrine)

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10
Q

What is noradrenaline

A
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11
Q

What is adrenaline

A
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12
Q

Where are adrenergic receptors found

A

CNS and sympathetic nervous system

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13
Q

What are the two families of adrenergic receptors

A
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14
Q

Describe the alpha adrenergic receptors

A
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15
Q

Describe beta adrenergic receptors

A
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16
Q
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17
Q

How does Beta 1 increase heart rate

A

B1 is excitatory so it enhances influx of Ca2+ which leads to contractile proteins so more contraction which increase the heart rate

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18
Q

Explain the beta 1 adrenergic receptor as a therapeutic target

A
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19
Q

What are the physiologic consequences of beta 2 receptor activation

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20
Q

Explain beta 2 adrenergic receptors as a therapeutic target

A
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21
Q

What is the physiologic consequence of alpha 1 receptor

A

Vasoconstriction
Increase in blood pressure

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22
Q

What is the equation for BP

A
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23
Q

What does counteract the decreased mean arterial blood pressure

A
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24
Q

What are adrenergic agonists

A

Termed as sympathomimetic drugs

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25
Q

What are the three groups of sympathomimetic drugs

A
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26
Q

What are the adrenergic binding sites

A
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27
Q

Explain the structure activity relationship of catecholamine

A
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28
Q

Give the action and the place of alpha 1

A
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29
Q

Give the action and the place of alpha 2

A
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30
Q

Give the action and the place of beta 1

A
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31
Q

Give place and action of beta 2

A
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32
Q

How to make a drug more selective for b receptors

A

Adding larger alkyl substituent

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33
Q

What is isoprenaline

A
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34
Q

Which receptor has a larger lipophilic binding pocket

A

Beta receptors

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35
Q

What does it mean if a drug has small alkyl group

A

Not selective

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36
Q

What are the examples of non selective alpha adrenergic agonists

A

Epinephrine
Ephedrine
Pseudoephedrine

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37
Q

When is epinephrine used

A

Used in emergency situations such as anaphylactic shock and cardiac arrest

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38
Q

How is epinephrine given

A

Parenterally to avoid first pass effect and excessive metabolism

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39
Q

What is anaphylactic shock

A
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40
Q

In anaphylactic shock what happens if the patient can’t breath

A

Rapid damage of brain and organs

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41
Q

What does anaphylactic shock require

A

Immediate medical care for example administration of IM epinephrine

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42
Q

What should be done if the patient has previously been diagnosed with anaphylaxis

A

The patient may be carrying an EpiPen for immediate administration

43
Q

Repetitive administration of epinephrine can cause what

A

Tachycardia with heart rates potentially reaching 240 beats per minute which could be fatal

44
Q

The epinephrine will prevent what

A

Worsening of the airway constriction, stimulate the heart to continue beating, and may be life saving

45
Q

What is ephedrine

A

Natural product present in various plants, two asymmetric centers

46
Q

Ephedrine acts as what

A

Bronchodilator
Cardiac stimulant

47
Q

What the difference between epinephrine and ephedrine

A

Ephedrine doesn’t have phenolic groups so avoids metabolism and is more lipophilic so crosses the BBB

48
Q

What is ephedrine hydrochloride

A
49
Q

How is pseudoephedrine related to ephedrine

A

It is a diastereomer of ephedrine

50
Q

Describe the pseudoephedrine

A
51
Q

What is the principle mechanism of pseudoephedrine

A
52
Q

What is pseudoephedrine used for

A
53
Q

What are the examples for selective alpha 1 adrenergic agonists

A

Phenylephrine, metaraminol, methoxamine
2-Arylimidazoline family

54
Q

Describe the phenylephrine family

A
55
Q

What is the phenylephrine family used for

A
56
Q

Explain 2-Arylimidazoline family and their uses

A
57
Q

List the selective alpha 2 adrenergic agonists

A

Clonidine
Guanfacine
Methyldopa

58
Q

Explain clonidine

A
59
Q

Explain guanfacine

A
60
Q

Explain methyldopa

A
61
Q

List the beta 1 selective agonists

A

Dobutamine

62
Q

Explain dobutamine

A
63
Q

List the beta 2 selective adrenergic agonists

A

Isoprenaline
Soterenol and salbutamol
Salmeterol

64
Q

What are the selective beta 2 agonists used for

A
65
Q

Explain Isoprenaline

A
66
Q

How to increase the duration of action

A
67
Q

Explain soterenol and salbutamol

A
68
Q

Compare between salmeterol and albuterol (salbutamol)

A
69
Q

Salmeterol is prescribed for what

A
70
Q

Why Salmeterol longer duration than salbutamol

A

Because not substrate to MOA due to long chain

71
Q

Non selective antagonists are used as what

A

Antihypertensive

72
Q

Explain labetalol

A
73
Q

Explain carvedilol

A
74
Q

Explain phenoxybenzamine

A
75
Q

Explain with examples selective alpha 1 antagonists

A
76
Q

Explain alfuzosin

A
77
Q

Explain silldosin

A
78
Q

Compare between alfuzosin and silodosin

A

Alfuzosin has some effect on blood vessels and blood pressure while silodosin doesn’t

79
Q

Explain selective alpha 2 antagonists

A
80
Q

Give example of selective alpha 2 antagonist

A

Mirtazapine

81
Q

How to convert an agonist to a partial agonist

A
82
Q

Explain how propranolol was formed

A
83
Q

Propranolol is used as what

A

Used clinically as a racemate
S-enantiomer is the active enantiomer
Binds to beta 1 and 2 adrenoceptors

84
Q

What is the structure of propranolol

A

Aryloxyprooanolamine

85
Q

What was the first B blockers in clinical use for angina, supraventicular arrhythmia, and high blood pressure

A

Propranolol

86
Q

Explain the SAR of propranolol

A
87
Q

Propranolol represents what

A

First generation of B blockers

88
Q

Antihypertensive mechanism depends on what

A
89
Q

What are the side effects of propranolol

A
90
Q

Explain what the drug clearance depends on

A
91
Q

What is a rule for selective B1 antagonists

A
92
Q

Explain esmolol

A
93
Q

Esmolol is used for what ?

A

To control supraventricular tachycardia during surgery when short duration is desirable

94
Q

Compare between esmolol and metoprolol

A
95
Q

Explain selective vs non selective B1 antagonists

A
96
Q

What are the 1st and 2nd generation B blockers

A

N-Alkyl groups → isopropyl and tertiary butyl groups

97
Q

What is the third generation b blocker

A
98
Q

What are other drugs that affect adrenergic neurotransmission

A

Metyrosine
Alpha methyl dopa
Guanethidine (Ismelin)

99
Q

Explain the drugs that affect the biosynthesis of norepinephrine

A
100
Q

Explain methyldopa

A
101
Q

List the drugs that inhibit the release of norepinephrine

A
102
Q

Explain guanethidine

A
103
Q

Explain guanethidine use

A