ANS Pharmacology Flashcards

1
Q

What endogenous ligand activates nicotinic receptors?

A

Acetylcholine

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2
Q

Where are nicotinic receptors located?

A

Centrally

Ganglia

Neuromuscular junctions

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3
Q

What endogenous ligand activates muscarinic receptors?

A

Acetylcholine

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4
Q

Where are muscarinic receptors located?

A

M1: centrally

M2: heart (inhibitory)

M3, M4: Smooth muscle and glands

M5: ??

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5
Q

What is the effect of a muscarinic agonist on the eye?

A

Pupillary constriction (miosis)

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6
Q

What is the effect of a muscarinic agonist on the bronchi?

A

Bronchoconstriction

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7
Q

What is the effect of a muscarinic agonist on the GIT?

A

Increased secretion and motility

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8
Q

What is the effect of a muscarinic agonist on the salivary glands?

A

Increased secretion

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9
Q

What is the effect of a muscarinic agonist on the heart?

A

Decreased HR

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10
Q

What is the effect of a muscarinic agonist on the bladder?

A

Urination

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11
Q

Does acetylcholine function in the sympathetic or parasympathetic system?

A

Parasympathetic

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12
Q

What family of drugs does pilocarpine belong to?

A

Muscarinic agonist

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13
Q

What are the uses of pilocarpine?

A

Myosis (pupil constriction)

Used in conjunction with mydriatics (dilators) to prevent adhesions in infection

Treatment of glaucoma?

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14
Q

What class of drugs does bethanechol belong to?

A

Muscarinic agonist

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15
Q

What disease might you use Bethanechol for?

A

FLUTD cats (stimulates detrusor muscle contraction and bladder emptying)

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16
Q

What are the side effects of bethanechol?

A

Stimulates GIT movement

Pupil constriction (myosis)

Increased bronchoconstriction and secretions

Reduced HR

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17
Q

Name four muscarinic agonists

A

Methacholine

Bethanechol

Pilocarpine

Carbachol

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18
Q

Which two muscarinic agonists have the strongest effects on GIT motility and bladder contraction?

A

Bethanechol

Carbachol

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19
Q

Which muscarinic agonist has the strongest effects on GIT and the pupil?

A

Pilocarpine

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20
Q

Which muscarinic agonist has the largest effect on heart rate?

A

Methacholine

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21
Q

Which class of drugs does atropine belong to?

A

Muscarinic antagonist (parasympatholytics)

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22
Q

Which class of drugs does scopolamine belong to?

A

Muscarinic antagonist (parasympatholytics)

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23
Q

Which class of drugs does glycopyrrolate belong to?

A

Muscarinic antagonist (parasympatholytic)

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24
Q

What drug class does propantheline belong to?

A

Muscarinic antagonist (parasympatholytics)

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25
Q

Which muscarinic antagonist does not cross the blood-brain barrier?

A

Propantheline

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26
Q

What are the actions of anti-muscarinics?

A

Increase HR

Dry up secretions (lacrimal, salivary, bronchial)

Dilate pupil

Urinary retention

Decrease bronchoconstriction

Reduce GIT motility

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27
Q

What are the indications of anti-muscarinics?

A

Premedicant to prevent bradycardia in anaesthesia

Minimise respiratory secretions

Antidote to cholinesterase inhibitor (organophosphates)

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28
Q

Name four competitive nicotinic antagonists

A

Curare

Pancuronium

Atracuronium

Vecuronium

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29
Q

Name a nicotinic agonist used as a depolarising agent

A

Suxamethonium

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30
Q

Name two agents that prevent release of Ach

A

Botulinum

Aminoglycoside antibiotics

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31
Q

What is the action and indication of a muscular antagonist (nicotinic)

A

paresis/paralysis

To assist with mechanical ventilation (e.g. anaesthesia)

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32
Q

Can vecuronium/pancuronium be reversed?

A

Yes, by cholinesterase inhibitors

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33
Q

What is suxamethonium used for?

A

e.g. intubation (paralysis of laryngeal muscles)

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34
Q

Describe the action of botulinum toxin

A

Prevents release of Ach from presynaptic membrane (irreversible)

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35
Q

Describe the pathogenesis of myasthenia gravis

A
  1. Genetic defect resulting in low numbers of nicotinic receptors
  2. Aquired autoimmune disease resulting in antibody destruction of nicotinic receptors
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36
Q

What drug class can be used in the treatment of myasthenia gravis?

A

Cholinesterase inhibitors

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37
Q

Name three cholinesterase inhibitors

A

Physostigmine

Neostigmine

Edrophonium

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38
Q

What drug class is physostigmine?

A

Cholinesterase inhibitor

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39
Q

What drug class does neostigmine belong to?

A

Cholinesterase inhibitor

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40
Q

What drug class does Edrophonium belong to?

A

Cholinesterase inhibitor

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41
Q

What drug class does curare belong to?

A

Competitive nicotinic antagonist

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42
Q

Describe the mechinism of action of pancuronium

A

competitive nicotinic antagonist

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43
Q

Describe the mechanism of action of atracuronium

A

competitive nicotinc antagonist

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44
Q

Describe the mechanism of action of vecuronium

A

competitive nicotinic antagonist

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45
Q

Describe the mechanism of action of suxamethonium

A

Nicotinic agonist (depolarising agent)

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46
Q

Describe the mechanism of action of aminoglycosides

A

Prevents release of acetylcholine

47
Q

Name other compounds that inhibit cholinesterase

A

Organophosphates

Some pesticides

Some herbicides

Nerve gases

Some anthelminthics

48
Q

What does SLUDGE refer to?

A

Symptoms of AChE inhibitor poisoning

Salivation
Lacrimation
Urination
Defecation
Gastrointestinal problems
Emesis

49
Q

What is the antidote for OP poisoning?

A

Atropine

50
Q

Describe the location and action of alpha 1 adrenoreceptors

A

Mainly smooth muscle

Release of intracellular Ca++: muscle contraction

51
Q

Describe the location and action of alpha 2 adrenoreceptors

A

Located presynaptically

Pre-synaptic inhibition of NA release

52
Q

Describe the location and action of beta 1 adrenoreceptors

A

Primarily in cardiac muscle

Increased Ca++ conductance: Increased HR and contractility

53
Q

Describe the location and action of Beta 2 adrenoreceptors

A

Located on smooth muscle

Phosphorylation of intracellular proteins: muscle relaxation

54
Q

Describe the location and action of Beta 3 adrenoreceptors

A

Mainly on adipose tissue

Lipolysis and thermogenesis

55
Q

What are the primary sympathetic receptor type(s) and effects in cardiac muscle

A

Beta 1 adrenoreceptors

Increased HR and force

56
Q

What are the primary sympathetic receptor types and effects on blood vessels?

A

(Skin, viscera) alpha 1 adrenoreceptors -> constriction

(Skeletal muscle) Beta 2 adrenoreceptors -> dilation

57
Q

What are the primary sympathetic receptor types and effects on bronchi?

A

Beta 2 adrenoreceptors: bronchodilation

58
Q

What are the primary sympathetic receptor types and effects in the GIT?

A

(Smooth muscle): alpha 1, alpha 2, beta 2: decreased motility

(Sphincters): alpha 2, beta 2: constriction

59
Q

What are the primary sympathetic receptor types and effects in the bladder?

A

(Smooth muscle) Beta 2: relaxation

(Sphincter) Alpha 1: contraction

60
Q

What are the primary sympathetic receptor types and effects in the eye?

A

(Pupil) alpha 1: contraction of radial muscles -> dilation of pupil

(Ciliary muscle) beta 2: relaxation (far vision)

61
Q

What are the primary receptor types and effects in sweat glands

A

M3 (muscarinic)

Secretion

62
Q

What are the primary sympathetic receptor types and effects in the liver

A

alpha 1, beta 2

glycogenolysis, gluconeogenesis

63
Q

Adrenaline has affinity for which receptors?

A

+++ Beta 1, Beta 2

++ Alpha 1, Alpha 2

64
Q

Noradrenaline has affinity for which receptors?

A

+++ Alpha 1, Alpha 2

++ Beta 1, Beta 2

65
Q

Dopamine has affinity for which receptors?

A

++ Alpha 1, Alpha 2, Beta 1, Beta 2,
Dopamine

66
Q

Salbutamol has affinity for which receptors?

A

+++ Beta 2

+ Beta 1

(no action at alpha receptors)

67
Q

Phenylephrine has affinity for which receptors?

A

++ alpha 1, alpha 2

(no action at beta receptors)

68
Q

Xylazine has affinity for which receptors

A

++ alpha 2

(selective)

69
Q

What are the main uses for adrenaline?

A

Increase HR, bronchodilation

70
Q

What are the main (peripheral) uses for dopamine?

A

Increased HR and BP

71
Q

What are the main uses for salbutamol?

A

Bronchodilation

72
Q

What are the main uses for phenylephrine?

A

Increase BP, constriction of vessels in nose (decrease secretions), local control of bleeding

73
Q

What is the main use of xylazine?

A

Anaesthesia/sedation

74
Q

Why would epinephrine be used with a local anaesthetic?

A

Reduce perfusion and prolong action

SHOULD NOT BE USED ON EXTREMITIES

75
Q

Name two selective alpha 1 agonists

A

Phenylpropranolamine (Propalin)

Pseudoephedrine

76
Q

Name a use for Phenylpropranolamine (Propalin) or Pseudoephedrine

A

Urinary incontinence

77
Q

List four alpha2 agonists

A

Xyalzine

Medetomidine

Demetomidine

Romifidine

78
Q

What is the mechanism of action of xylazine?

A

Alpha 2 agonist

79
Q

What is the mechanism of action of Medetomidine?

A

Alpha 2 agonist

80
Q

What is the mechanism of action of Demetomidine?

A

Alpha 2 agonist

81
Q

What is the mechanism of action of Romifidine?

A

Alpha 2 agonist

82
Q

Name two alpha 2 antagonists

A

Yohimbine

Atipamezole

83
Q

What is the mechanism of action of yohimbine?

A

Alpha 2 antagonist

84
Q

What is the mechanism of action of Atipamezole?

A

Alpha 2 antagonist

85
Q

Name a use for alpha 2 antagonists

A

Reversal of alpha 2 agonists (reversal of sedation)

86
Q

Describe how an alpha 2 agonist causes sedation

A

Agonist at alpha 2 receptors, which are located on presynaptic membrane

Reduces release of noradrenaline

Decreased action of noradrenaline at postsynaptic alpha receptors

87
Q

Name a selective beta 1 agonist

A

Dobutamine

(does have action at other receptors at high doses)

88
Q

What can dobutamine be used for

A

Post cardiac arrest (positive inotrope)

Maintain HR and BP in surgery

89
Q

Name three selective Beta 2 agonists

A

Salbutamol

Terbutaline

Clenbuterol

(Does have a small amount of activity at Beta 1 also_

90
Q

What is the mechanism of action of dobutamine

A

(Selective) Beta 1 agonist

91
Q

What is the mechanism of action of salbutamol?

A

(Selective) Beta 2 agonist

92
Q

What is the mechanism of action of salbutamol?

A

(Selective) Beta 2 agonist

93
Q

What is the mechanism of action of terbutaline?

A

(Selective) Beta 2 agonist

94
Q

What is the mechanism of action of clenbuterol?

A

(Selective) Beta 2 agonist

95
Q

What are the indications of Beta 2 agonists?

A

Feline asthma

Chronic obstructive pulmonary disease (horses)

96
Q

Name three non-selective Beta agonists

A

Adrenaline

Noradrenaline

Isoprenaline

97
Q

What is the mechanism of action of isoprenaline?

A

Non-selective beta agonist

98
Q

Name two non-selective alpha adrenoreceptor antagonists (sympatholytics)

A

Phenoxybenzamine

Phentolamine

99
Q

Name a non-selective beta adrenoreceptor antagonist

A

Propranolol

100
Q

What is the action of phenoxybenzamine?

A

alpha 1 and 2 antagonist

101
Q

What is the action of phentolamine?

A

alpha 1 & 2 antagonist

102
Q

What is the action of propranolol?

A

Beta 1 and 2 antagonist

103
Q

Name an alpha 1 antagonist

A

Prazosin

104
Q

What is the mechanism of action of prazosin?

A

Alpha 1 antagonist

105
Q

Name two Beta 1 antagonists

A

Atenolol

Metoprolol

106
Q

What is the mechanism of action of atenolol?

A

Beta 1 antagonist

107
Q

What is the mechanism of action of metoprolol

A

Beta 1 antagonist

108
Q

What are the uses for prazosin?

A

hypertension, congestive heart failure, relax urinary sphincter

109
Q

What are indications for beta antagonists?

A

tachycardia

atrial fibrillation

hypertrophic heart disease

110
Q

What are some possible side effects of non-selective beta blockers?

A

Increased bronchoconstriction (asthma?)

Decrease cardiac contraction (heart problems?)

Block glycogenolysis (hypoglycaemic/diabetic?)

111
Q

What is the function of monoamine oxidase (MAO)?

A

Catabolism of adrenaline, noradrenaline, dopamine

112
Q

What is an indication for adrenaline?

A

Anaphylactic shock

113
Q

Name four muscarinic antagonists

A

Atropine

Hyoscine (scopolamine)

Glycopyrrolate

Propantheline

114
Q

Are muscarinic antagonists competitive or non-competitive?

A

Competitive