Peripheral Nervous System, Adrenoreceptors and Ocular Pharmacology Flashcards

(94 cards)

1
Q

2 regions of the Peripheral Nervous System

A

Somatic and Autonomic

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2
Q

3 regions of the Autonomic Nervous System

A

Enteric, Parasympathetic and Sympathetic

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3
Q

3 places nicotinic receptors can be found

A

Muscle, neuronal (CNS) and neuronal (autonomic ganglia)

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4
Q

what are nicotinic receptors in the autonomic ganglia regulated by?

A

Muscarinic receptors

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5
Q

Effect of M1 receptor

A

Slow EPSP

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6
Q

Effect of M2 receptor

A

Slow IPSP

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7
Q

Effect of M3 receptor

A

late/slow EPSP

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8
Q

Most postsynaptic SYMPATHETIC fibres release…

A

NA

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9
Q

Most postsynaptic PARASYMPATHETIC fibres release…

A

ACh

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10
Q

What NT acts on Muscarinic Receptors?

A

ACh

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11
Q

2 exceptions for NA release in the sympathetic nervous system

A

Sweat glands and Renal vessels (dopamine)

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12
Q

3 types of pre-synaptic modulation

A

homo/heterotropic inhibition, tissue/plasma derived substances and co-trasnporters

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13
Q

name 3 examples of tissue/plasma derived substances that help modulate pre-synaptically

A

prostaglandins, histamine, adenosine and bradykinin

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14
Q

name 3 examples of cotransporters that help modulate pre-synaptically

A

ATP, neuropeptides and NO

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15
Q

What NT is associated with the Sympathetic NS

A

Noradrenaline

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16
Q

What amino acid does NA derive from

A

Tyrosine

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17
Q

Pathway from Tyrosine –> Adrenaline

A

Tyrosine –> DOPA –> Dopamine –> NA –> A

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18
Q

α-methyl-p-tyrosine

A

tyrosine hydroxylase inhibitor (reduce amount of NA)

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19
Q

carbidopa

A

DOPA decarboxylase inhibitor (reduce amount of NA)

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20
Q

methyldopa

A

α2 agonist (reduce amount of NA, via negative feedback)

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21
Q

guanethidine

A

substrate for NET and VMAT, blocking the effect of adrenergic receptors

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22
Q

reserpine

A

inhibits VMAT, blocking the effect of adrenergic receptors

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23
Q

What effects would the drugs decreasing the amount of NA have?

A

anti-sympathetic: hypotension, bradycardia, sexual dysfunction

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24
Q

How do β1 adrenoreceptors work?

A

Activate adenylyl cyclase via Gs, increasing cAMP, increasing kinase activity, increasing cell response - found predominantly in the heart, when activated increase the HR

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25
How do β2 adrenoreceptors work?
Activate adenylyl cyclase via Gs, increasing cAMP, increasing kinase activity, increasing cell response - when activated in the lungs, causes relaxation/dilation of the bronchioles.
26
How do β3 adrenoreceptors work?
Activate adenylyl cyclase via Gs, increasing cAMP, increasing kinase activity, increasing cell response
27
How do α2 adrenoreceptors work?
INHIBIT adenylyl cyclase via Gi, decreasing cAMP, reduced kinase activity, reduced cell response = decreased release at adrenergic and cholinergic.
28
How do α1 adrenoreceptors work?
Activate PLC which increases IP3, increasing Ca release, increasing cell response also increases DAG.
29
What effect do active α1 have?
constrict/contract (except in the GI tract)
30
phenylephrine
α1 agonist (vasoconstrictor)
31
clonidine
α2 agonist (prevents NA release, decreasing the BP)
32
dobutamine
β1 agonist (increase cardiac contractility)
33
salbutamol
β2 agonist (bronchodilation)
34
prazosin
α1 antagonist (vasodilator)
35
yohimbine
α2 antagonist
36
phenoxybenzamine
non-selective α antagonist
37
phentolamine
non-selective α antagonist
38
labetalol
α/β antagonist
39
carvediol
α/β antagonist
40
propranolol
non-selective β antagonist
41
atenolol
β1 antagonist
42
timolol
β1 antagonist
43
β blocker most important desired effect is where
heart/cardiovascular system
44
unwanted effects of β blockers
bronchoconstriction, bradycardia, hypoglycaemia
45
what type of receptors are muscarinic receptors?
GPCR
46
which nervous system do muscarinic receptors work on?
parasympathetic
47
M1, M3, M5 all work through which reaction
activated Gq, which activates IP3
48
M2 works through
Gi, which decreases cAMP, reducing [Ca]
49
when muscarinic receptors are activated, what is a side effect?
SLUDGE, lots of liquid released
50
What is the main NT in the parasympathetic NS
ACh
51
ACh is a...
cholinergic AGONIST
52
Pilocarpine
cholinergic AGONIST
53
Bethanachol
cholinergic AGONIST
54
3 side effects of muscarinic antagonists
inhibit secretions, tachycardia, mydriasis
55
atropine
non-selective muscarinic antagonist
56
hyoscine
non-selective muscarinic antagonist
57
pirenzepine
M1 selective antagonist (peptide ulcers)
58
darifenacin
M3 selective antagonist
59
side effects of non-selective muscarinic antagonists
urinary retention, dry mouth, blurred vision
60
Nerve impulses are controlled by...
presynaptic M2 receptors
61
which muscarinic receptors predominantly work in the airways
M3
62
normal cholinergic signalling pathway in airways
nerve impulse --> ACh released --> M3 receptor --> Gq --> PLC --> Ca release --> contraction
63
ipratropium
muscarinic antagonist
64
how does ipratropium work?
relax SM in airways, dilating them and treating asthma/bronchitis
65
problem with non-specific muscarinic receptors
block both M2 and M3, removing the negative feedback, so more ACh released, which could overcome the M3 block!
66
M3 selective antagonist
tiotropium
67
why is tiotropium good?
does not get inhibit the negative feedback loop at M2 presynaptically
68
3 things muscarinic agonists help with
emptying bladder, glaucoma, slowing HR, secretion
69
3 things muscarinic antagonists help with
prevent parasympathetic responses, inhibit secretion, tachycardia
70
3 muscles in the eye
Radial, sphincter and ciliary muscles
71
pupil dilation, contraction of radial SM, sympathetic innervation
mydriasis
72
pupil gets smaller, contraction of sphincter SM, parasympathetic innervation
miosis
73
NT and receptor for mydriasis
NA on α1
74
NT and receptor for miosis
ACh on M3
75
what would an α1 adrenoreceptor ANTAGONIST cause
miosis
76
what would a M3 muscarinic receptor ANTAGONIST cause?
mydriasis
77
pilocarpine
muscarinic agonist
78
how would a muscarinic agonist act on the eye
miosis, contraction of constrictor, parasympathetic response, block constrictor muscle
79
how would a muscarinic antagonist act on the eye
mydriasis, contraction of radial muscle, sympathetic response
80
atropine
muscarinic antagonist
81
dominant effect on the eye
PARA
82
glaucoma is caused by
increase intra-ocular pressure
83
what can cause open-angled glaucoma
obstruction in drainage through the TRABECULAR NETWORK and CANAL OF SCHLEMM
84
what is the formation of aqueous humour stimulated by
β agonists
85
what is the formation of aqueous humour inhibited by
α agonists (α1 agonists, vasoconstrictors decrease blood flow to ciliary body, β antagonists and α2 agonists decrease cAMP)
86
β antagonist that would reduce AH formation
Timolol
87
another drug group that could reduce AH formation
carbonic anhydrase inhibitors
88
example of a carbonic anhydrase inhibitor
acetazolamide
89
where is aqueous humour produced?
ciliary body
90
what targets the trabecular meshwork?
Miotics
91
example of a muscarinic agonist
pilocarpine
92
2 ways the AH can flow out of the eye
trabecular meshwork (90%), uveoscleral pathway (10%)
93
3 main drug targets for glaucoma and an example
trabecular meshwork outflow (PILOCARPINE), uveoscleral pathway (LATANOPROST), AH formation (β adrenoreceptor antagonist, TIMOLOL, α adrenoreceptor agonist, CLONIDINE, carbonic anhydrase inhibitor, ACETAZOLAMIDE).
94
Wet Macular Degeneration drugs
VEGF inhibitors (VERTEPORFORIN)