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Cardiovascular, Renal and Peripheral Pharmacology > Peripheral Nervous System, Adrenoreceptors and Ocular Pharmacology > Flashcards

Peripheral Nervous System, Adrenoreceptors and Ocular Pharmacology Flashcards

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
Q

How do β2 adrenoreceptors work?

A

Activate adenylyl cyclase via Gs, increasing cAMP, increasing kinase activity, increasing cell response - when activated in the lungs, causes relaxation/dilation of the bronchioles.

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26
Q

How do β3 adrenoreceptors work?

A

Activate adenylyl cyclase via Gs, increasing cAMP, increasing kinase activity, increasing cell response

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27
Q

How do α2 adrenoreceptors work?

A

INHIBIT adenylyl cyclase via Gi, decreasing cAMP, reduced kinase activity, reduced cell response = decreased release at adrenergic and cholinergic.

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28
Q

How do α1 adrenoreceptors work?

A

Activate PLC which increases IP3, increasing Ca release, increasing cell response also increases DAG.

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29
Q

What effect do active α1 have?

A

constrict/contract (except in the GI tract)

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30
Q

phenylephrine

A

α1 agonist (vasoconstrictor)

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31
Q

clonidine

A

α2 agonist (prevents NA release, decreasing the BP)

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32
Q

dobutamine

A

β1 agonist (increase cardiac contractility)

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33
Q

salbutamol

A

β2 agonist (bronchodilation)

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34
Q

prazosin

A

α1 antagonist (vasodilator)

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35
Q

yohimbine

A

α2 antagonist

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36
Q

phenoxybenzamine

A

non-selective α antagonist

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37
Q

phentolamine

A

non-selective α antagonist

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38
Q

labetalol

A

α/β antagonist

39
Q

carvediol

A

α/β antagonist

40
Q

propranolol

A

non-selective β antagonist

41
Q

atenolol

A

β1 antagonist

42
Q

timolol

A

β1 antagonist

43
Q

β blocker most important desired effect is where

A

heart/cardiovascular system

44
Q

unwanted effects of β blockers

A

bronchoconstriction, bradycardia, hypoglycaemia

45
Q

what type of receptors are muscarinic receptors?

A

GPCR

46
Q

which nervous system do muscarinic receptors work on?

A

parasympathetic

47
Q

M1, M3, M5 all work through which reaction

A

activated Gq, which activates IP3

48
Q

M2 works through

A

Gi, which decreases cAMP, reducing [Ca]

49
Q

when muscarinic receptors are activated, what is a side effect?

A

SLUDGE, lots of liquid released

50
Q

What is the main NT in the parasympathetic NS

A

ACh

51
Q

ACh is a…

A

cholinergic AGONIST

52
Q

Pilocarpine

A

cholinergic AGONIST

53
Q

Bethanachol

A

cholinergic AGONIST

54
Q

3 side effects of muscarinic antagonists

A

inhibit secretions, tachycardia, mydriasis

55
Q

atropine

A

non-selective muscarinic antagonist

56
Q

hyoscine

A

non-selective muscarinic antagonist

57
Q

pirenzepine

A

M1 selective antagonist (peptide ulcers)

58
Q

darifenacin

A

M3 selective antagonist

59
Q

side effects of non-selective muscarinic antagonists

A

urinary retention, dry mouth, blurred vision

60
Q

Nerve impulses are controlled by…

A

presynaptic M2 receptors

61
Q

which muscarinic receptors predominantly work in the airways

A

M3

62
Q

normal cholinergic signalling pathway in airways

A

nerve impulse –> ACh released –> M3 receptor –> Gq –> PLC –> Ca release –> contraction

63
Q

ipratropium

A

muscarinic antagonist

64
Q

how does ipratropium work?

A

relax SM in airways, dilating them and treating asthma/bronchitis

65
Q

problem with non-specific muscarinic receptors

A

block both M2 and M3, removing the negative feedback, so more ACh released, which could overcome the M3 block!

66
Q

M3 selective antagonist

A

tiotropium

67
Q

why is tiotropium good?

A

does not get inhibit the negative feedback loop at M2 presynaptically

68
Q

3 things muscarinic agonists help with

A

emptying bladder, glaucoma, slowing HR, secretion

69
Q

3 things muscarinic antagonists help with

A

prevent parasympathetic responses, inhibit secretion, tachycardia

70
Q

3 muscles in the eye

A

Radial, sphincter and ciliary muscles

71
Q

pupil dilation, contraction of radial SM, sympathetic innervation

A

mydriasis

72
Q

pupil gets smaller, contraction of sphincter SM, parasympathetic innervation

A

miosis

73
Q

NT and receptor for mydriasis

A

NA on α1

74
Q

NT and receptor for miosis

A

ACh on M3

75
Q

what would an α1 adrenoreceptor ANTAGONIST cause

A

miosis

76
Q

what would a M3 muscarinic receptor ANTAGONIST cause?

A

mydriasis

77
Q

pilocarpine

A

muscarinic agonist

78
Q

how would a muscarinic agonist act on the eye

A

miosis, contraction of constrictor, parasympathetic response, block constrictor muscle

79
Q

how would a muscarinic antagonist act on the eye

A

mydriasis, contraction of radial muscle, sympathetic response

80
Q

atropine

A

muscarinic antagonist

81
Q

dominant effect on the eye

A

PARA

82
Q

glaucoma is caused by

A

increase intra-ocular pressure

83
Q

what can cause open-angled glaucoma

A

obstruction in drainage through the TRABECULAR NETWORK and CANAL OF SCHLEMM

84
Q

what is the formation of aqueous humour stimulated by

A

β agonists

85
Q

what is the formation of aqueous humour inhibited by

A

α agonists (α1 agonists, vasoconstrictors decrease blood flow to ciliary body, β antagonists and α2 agonists decrease cAMP)

86
Q

β antagonist that would reduce AH formation

A

Timolol

87
Q

another drug group that could reduce AH formation

A

carbonic anhydrase inhibitors

88
Q

example of a carbonic anhydrase inhibitor

A

acetazolamide

89
Q

where is aqueous humour produced?

A

ciliary body

90
Q

what targets the trabecular meshwork?

A

Miotics

91
Q

example of a muscarinic agonist

A

pilocarpine

92
Q

2 ways the AH can flow out of the eye

A

trabecular meshwork (90%), uveoscleral pathway (10%)

93
Q

3 main drug targets for glaucoma and an example

A

trabecular meshwork outflow (PILOCARPINE), uveoscleral pathway (LATANOPROST), AH formation (β adrenoreceptor antagonist, TIMOLOL, α adrenoreceptor agonist, CLONIDINE, carbonic anhydrase inhibitor, ACETAZOLAMIDE).

94
Q

Wet Macular Degeneration drugs

A

VEGF inhibitors (VERTEPORFORIN)

Cardiovascular, Renal and Peripheral Pharmacology (13 decks)

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