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Principles Of Pharmacology > Week 7 > Flashcards

Week 7 Flashcards

(85 cards)

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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
What effects does Arecoine have?
Has no therapeutic effects but can have muscarinic and nicotinic actions and some changes to the CNS.
26
What are the muscarinic effects of agonist in the parasympathetic nervous system?
``` Pupil constriction Decreased heart rate Increase GI motility Salivation Bronchoconstriction Bladder contraction ```
27
Why can't ACh be used alone to control the parasympathetic nervous system? (Why must muscarine be used as-well)?
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.
28
Describe the time period for which ACh and muscarine have effects ?
ACh - short | Muscarine - longer
29
What are the benefits of using muscarine over Acetylcholine to control the parasympathetic nervous system?
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).
30
Why is the use of muscarine limited by side effects?
Muscarine is not highly specific to sub types of muscarinic receptors.
31
What types of receptors does ACh act on in the parasympathetic nervous branch ?
Nicotinic and muscarinic
32
What type of receptors does muscarine act on in the parasympathetic nervous branch ?
Muscarinic
33
What are the positive effects of muscarinic agonist?
Increases GI peristalsis Increases bladder constriction Reduces intraocular pressure
34
What are the adverse effects of muscarinic agonists?
Colic Diarrhoea Cardiovascular depression Bronchoconstriction
35
What are the issues related with cardiovascular depression?
Causes low blood pressure
36
What is intraocular pressure?
Raised pressure in the eyes
37
What is colic?
Spasms in the GI tract
38
What is Pilocarpine used to treat?
Glaucoma
39
What property of Pilocarpine allows it to be able to treat Glaucoma?
Lipid soluble so can penetrate the cornea.
40
What causes Glaucoma?
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
Which division of the autonomic nervous system causes pupil contraction?
Parasympathetic
42
Which division of the autonomic nervous system causes pupil dilation?
Sympathetic
43
What muscles of the eye does the parasympathetic nervous system act on to cause pupil constriction?
Circular muscles
44
What muscles of the eye does the sympathetic nervous system act on to cause pupil dilation?
Radial muscles
45
What is Bradycardia?
Slow heart rate
46
When does Bradycardia often occur
After myocardial infarction
47
What can be used to treat Bradycardia?
Muscarinic Antagonists
48
What are Muscarinic antagonists often used to treat?
Block vagal nerve slowing of the heart. To treat bradycardia. Preoperative agents
49
How do Muscarinic agents act as Preoperative agents?
They reduce bodily secretions before surgery
50
What are some of the side effects of muscarinic receptors?
``` Dry mouth Constipation Urinary Retention Tachycardia Sedation ```
51
What is Tachycardia?
When the heart beats more than 100 times per minute.
52
What is Pirenzepine used to treat and how?
Selectively blocks M1 receptors in gastric acid secretion. | Used to reduce stomach ulcers.
53
What muscarinic receptors does Pirenzepine act on?
M1
54
What muscarinic receptors does Darifenacin act on?
M3
55
What is Darifenacin used to treat and how?
Urinary incontinence | Inhibits parasympathetic contraction of the bladder
56
What are cholinesterase's ?
Breakdown Actetyl choline and terminate its action.
57
What are Pseudocholinesterases ?
They break down Ach and similar substances to terminate their action.
58
What are Psudocholinesterases present?
In the blood plasma
59
Where are cholinesterases present?
The parasympathetic nervous system, somatic nervous system, ganglia and CNS.
60
At what substrate concentrations do pseudocholinesterase work best?
Low
61
At what substrate concentration do Cholinesterase's work best?
High
62
Describe the duration time of reversible acetylcholinesterases
Short (2-10 mins)
63
Describe the binding of reversible acetylcholinesterase to enzymes
Loosely bound by electrostatic forces. No covalent bonding
64
What are the clinical uses of reversible acetylcholinesterase?
Diagnosing Myaesthenia gravis
65
What test is used to confirm Myasthenia Gravis?
Edrophonium test
66
Describe how the Edrophonium test works
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
If a person has Myasthenia Gravis, how will they respond to the Edrophonium test?
Their facial weakness will be removed
68
Do irreversible Acetylcholinesterase use covalent bonding?
No
69
Describe the duration that reversible acetylcholinesterase act for.
MEdium (3-8 hours)
70
Describe the bonding of Reversible acetylcholinesterases with substrates.
Covalent bonding with substrate
71
Compare the hydrolysis time of ACh using reversible or irreversible acetylcholinesterases
Longer with reversible
72
How do acetycholineusterases affect neuromuscular transmission at skeletal muscular junctions?
Enhance it
73
What type of neuromuscular junctions do acetylcholinesterases increase transmission at?
Skeletal muscle junctions
74
What are the uses of reversible Acetylcholinesterases?
Enhance motility and secretions of the gut. Treatment of urinary retention. Treatment of Glaucoma. Treatment of Myasthenia Gravis. Reverses Tubocurarine effects.
75
Describe the action time of Irreversible Anticholinesterases
Long - hundreds of hours
76
What type of compounds are irreversible anticholinesterases?
Organophosphorus compounds
77
Describe the bonding of irreversible anticholinesterases with substrates.
Form very stable phosphorus-enzyme bonds.
78
Describe the hydrolysis time of irreversible anticholinesterases
Very slow; Weeks/ days
79
Describe the uses of irreversible anticholinesterases
In chemical weapons | As insecticides
80
Describe the toxicity of irreversible acetylcholinesterases
Highly toxic
81
What are the toxic effects of anticholinesterases?
Excessive muscarinic stimulation Nicotinic stimulation CNS effects
82
What are the negative effects of excessive muscarinic stimulation?
Stimulation, vomiting, diarrhoea, bronchoconstriction, bronchosecretion, pupil constriction.
83
What are the negative effects Acetylcholinesterase on the CNS?
Convulsions | Coma
84
What is the purpose of Atropine?
Blocks muscarinic receptors
85
What are the effects of Pralidoxine?
Splits the phosphorus-enzyme bonds caused by anticholinesterases and allows the enzyme to reform

Principles Of Pharmacology (11 decks)

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