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Principles Of Pharmacology > Week 7 > Flashcards

Week 7 Flashcards

1
Q

Which branch of the nervous system is the ‘Parasympathetic’ nervous system part of?

A

Autonomic

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2
Q

What is the overall purpose of the parasympathetic nervous system?

A

‘Rest and Digest’

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3
Q

Describe the ganglion structure in the parasympathetic branch of the autonomic nervous system

A

Short pre-ganglionic neurone.

Long post-ganglionic neurone.

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4
Q

Describe the difference between the proximity of the ganglia to the effectors in the parasympathetic and sympathetic branches of the autonomic nervous system

A

Parasympathetic - ganglia much closer to effectors

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5
Q

What is meant by organs being ‘antagonistic’?

A

They have both parasympathetic and sympathetic innervation working against each other.

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6
Q

What is the neurotransmitter used by the parasympathetic nervous system?

A

Acetyl choline

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7
Q

What receptors are used in the parasympathetic branch of the autonomic nervous system?

A

Nicotinic

Muscarinic

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8
Q

What was the first known neurotransmitter?

A

Acetyl Choline

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9
Q

Who discovered Acetyl Choline and in what year?

A

1921 - Otto Lowei

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10
Q

What animal did Otto Lowei experiment on to discover the uses of Acetyl Choline as a neurotransmitter ?

A

Frogs

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11
Q

What nerve stimulates the heart?

A

Vagus nerve

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12
Q

What effect does the parasympathetic nervous system have on heart rate?

A

Slows

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13
Q

What branch of the autonomic nervous system does muscarine act on?

A

Selectively stimulates receptors of the parasympathetic branch.

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14
Q

Why does Muscarine often act on the same receptors as Acetyl Choline?

A

Muscarine is structurally similar to Acetyl choline

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15
Q

What type of receptors are Muscarinic receptors?

A

G-protein coupled

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16
Q

What model do muscarinic receptors use to produce a response?

A

Second messenger models

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17
Q

What are M1 muscarinic receptors used for and where are the found?

A

Neural effects in the brain and stomach.

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18
Q

Where are M2 muscarinic receptors found and what are they used for?

A

To control the cardiac muscle - found in the heart.

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19
Q

Where are M3 muscarinic receptors found and what are they used for?

A

To control smooth muscle - found in the eyes, GI tract, bladder and lungs.

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20
Q

What type of muscarinic receptors are found in the heart?

A

M2

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21
Q

What type of muscarinic receptors are found in the brain?

A

M1

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22
Q

Outline the main subtypes of muscarinic receptors

A

M1, M2, M3

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23
Q

What causes the different subtypes of muscarinic receptors?

A

Their different connections with different G proteins.

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24
Q

What are alkaloids?

A

Naturally occurring nitrogen containing compounds which have important physiological effects on humans and other animals.

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25
Q

What effects does Arecoine have?

A

Has no therapeutic effects but can have muscarinic and nicotinic actions and some changes to the CNS.

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26
Q

What are the muscarinic effects of agonist in the parasympathetic nervous system?

A 
Pupil constriction
Decreased heart rate
Increase GI motility
Salivation
Bronchoconstriction
Bladder contraction
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27
Q

Why can’t ACh be used alone to control the parasympathetic nervous system? (Why must muscarine be used as-well)?

A

ACh has both muscaric and nicotinic effects so will stimulate all sub-types of receptor and therefore isn’t as selective as muscarine.

ACh also has short-lived effects where as muscarine has longer lasting effects.

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28
Q

Describe the time period for which ACh and muscarine have effects ?

A

ACh - short

Muscarine - longer

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29
Q

What are the benefits of using muscarine over Acetylcholine to control the parasympathetic nervous system?

A

It stimulates muscarinic receptors but has little or no effect on nicotinic receptors so is more specific than ACh.

Prolonged widespread action (longer than ACh).

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30
Q

Why is the use of muscarine limited by side effects?

A

Muscarine is not highly specific to sub types of muscarinic receptors.

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31
Q

What types of receptors does ACh act on in the parasympathetic nervous branch ?

A

Nicotinic and muscarinic

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32
Q

What type of receptors does muscarine act on in the parasympathetic nervous branch ?

A

Muscarinic

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33
Q

What are the positive effects of muscarinic agonist?

A

Increases GI peristalsis
Increases bladder constriction
Reduces intraocular pressure

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34
Q

What are the adverse effects of muscarinic agonists?

A

Colic
Diarrhoea
Cardiovascular depression
Bronchoconstriction

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35
Q

What are the issues related with cardiovascular depression?

A

Causes low blood pressure

36
Q

What is intraocular pressure?

A

Raised pressure in the eyes

37
Q

What is colic?

A

Spasms in the GI tract

38
Q

What is Pilocarpine used to treat?

A

Glaucoma

39
Q

What property of Pilocarpine allows it to be able to treat Glaucoma?

A

Lipid soluble so can penetrate the cornea.

40
Q

What causes Glaucoma?

A

If the iris of the eye folds during dilation, there can be used drainage of aqueous humour from the eye. This means Aqueous humour builds u and causes increased intraocular pressure in the eye.

This can damage the optic nerve and reduce vision.

41
Q

Which division of the autonomic nervous system causes pupil contraction?

A

Parasympathetic

42
Q

Which division of the autonomic nervous system causes pupil dilation?

A

Sympathetic

43
Q

What muscles of the eye does the parasympathetic nervous system act on to cause pupil constriction?

A

Circular muscles

44
Q

What muscles of the eye does the sympathetic nervous system act on to cause pupil dilation?

A

Radial muscles

45
Q

What is Bradycardia?

A

Slow heart rate

46
Q

When does Bradycardia often occur

A

After myocardial infarction

47
Q

What can be used to treat Bradycardia?

A

Muscarinic Antagonists

48
Q

What are Muscarinic antagonists often used to treat?

A

Block vagal nerve slowing of the heart.

To treat bradycardia.

Preoperative agents

49
Q

How do Muscarinic agents act as Preoperative agents?

A

They reduce bodily secretions before surgery

50
Q

What are some of the side effects of muscarinic receptors?

A 
Dry mouth
Constipation
Urinary Retention
Tachycardia
Sedation
51
Q

What is Tachycardia?

A

When the heart beats more than 100 times per minute.

52
Q

What is Pirenzepine used to treat and how?

A

Selectively blocks M1 receptors in gastric acid secretion.

Used to reduce stomach ulcers.

53
Q

What muscarinic receptors does Pirenzepine act on?

A

M1

54
Q

What muscarinic receptors does Darifenacin act on?

A

M3

55
Q

What is Darifenacin used to treat and how?

A

Urinary incontinence

Inhibits parasympathetic contraction of the bladder

56
Q

What are cholinesterase’s ?

A

Breakdown Actetyl choline and terminate its action.

57
Q

What are Pseudocholinesterases ?

A

They break down Ach and similar substances to terminate their action.

58
Q

What are Psudocholinesterases present?

A

In the blood plasma

59
Q

Where are cholinesterases present?

A

The parasympathetic nervous system, somatic nervous system, ganglia and CNS.

60
Q

At what substrate concentrations do pseudocholinesterase work best?

A

Low

61
Q

At what substrate concentration do Cholinesterase’s work best?

A

High

62
Q

Describe the duration time of reversible acetylcholinesterases

A

Short (2-10 mins)

63
Q

Describe the binding of reversible acetylcholinesterase to enzymes

A

Loosely bound by electrostatic forces. No covalent bonding

64
Q

What are the clinical uses of reversible acetylcholinesterase?

A

Diagnosing Myaesthenia gravis

65
Q

What test is used to confirm Myasthenia Gravis?

A

Edrophonium test

66
Q

Describe how the Edrophonium test works

A

Facial weakness is provoked by repeated facial movements. Edrophonium is then given by slow I.V. infections. In Myasthenia Gravis, facial weakness is removed by this test.

67
Q

If a person has Myasthenia Gravis, how will they respond to the Edrophonium test?

A

Their facial weakness will be removed

68
Q

Do irreversible Acetylcholinesterase use covalent bonding?

A

No

69
Q

Describe the duration that reversible acetylcholinesterase act for.

A

MEdium (3-8 hours)

70
Q

Describe the bonding of Reversible acetylcholinesterases with substrates.

A

Covalent bonding with substrate

71
Q

Compare the hydrolysis time of ACh using reversible or irreversible acetylcholinesterases

A

Longer with reversible

72
Q

How do acetycholineusterases affect neuromuscular transmission at skeletal muscular junctions?

A

Enhance it

73
Q

What type of neuromuscular junctions do acetylcholinesterases increase transmission at?

A

Skeletal muscle junctions

74
Q

What are the uses of reversible Acetylcholinesterases?

A

Enhance motility and secretions of the gut.

Treatment of urinary retention.

Treatment of Glaucoma.

Treatment of Myasthenia Gravis.

Reverses Tubocurarine effects.

75
Q

Describe the action time of Irreversible Anticholinesterases

A

Long - hundreds of hours

76
Q

What type of compounds are irreversible anticholinesterases?

A

Organophosphorus compounds

77
Q

Describe the bonding of irreversible anticholinesterases with substrates.

A

Form very stable phosphorus-enzyme bonds.

78
Q

Describe the hydrolysis time of irreversible anticholinesterases

A

Very slow; Weeks/ days

79
Q

Describe the uses of irreversible anticholinesterases

A

In chemical weapons

As insecticides

80
Q

Describe the toxicity of irreversible acetylcholinesterases

A

Highly toxic

81
Q

What are the toxic effects of anticholinesterases?

A

Excessive muscarinic stimulation

Nicotinic stimulation

CNS effects

82
Q

What are the negative effects of excessive muscarinic stimulation?

A

Stimulation, vomiting, diarrhoea, bronchoconstriction, bronchosecretion, pupil constriction.

83
Q

What are the negative effects Acetylcholinesterase on the CNS?

A

Convulsions

Coma

84
Q

What is the purpose of Atropine?

A

Blocks muscarinic receptors

85
Q

What are the effects of Pralidoxine?

A

Splits the phosphorus-enzyme bonds caused by anticholinesterases and allows the enzyme to reform

Principles Of Pharmacology (11 decks)

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