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Biomed 2 > Pharma - Autonomic Nervous System > Flashcards

Pharma - Autonomic Nervous System Flashcards

1
Q

define autonomic nervous system

A

all the neural pathways that leave the brain that do not innervate voluntary muscle

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2
Q

what fall under the peripheral nervous system

A

autonomic nervous system
somatic nervous system

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3
Q

what fall under ANS

A

sympathetic
parasympathetic

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4
Q

what are the roles of the ANS

A

pupillary dilation
dilation/constriction of blood vessels
force/rate of heart beat
movements of GI tract
secretion of most glands
energy motabolism

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5
Q

where does the point of contact between the first and second efferent neuron occur

A

ganglion

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6
Q

what is a ganglion

A

a group of nerve cell bodies that lie outside the CNS

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7
Q

are parasympathetic or sympathetic neurones longer

A

parasympathetic

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8
Q

what is a receptor agonist

A

a drug that mimics a neurotransmitter

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9
Q

what is a drug that blocks a neurotransmitter called

A

receptor antagonist

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10
Q

where are sympathetic preganglionic neurones located

A

midbrain
medulla
lateral horn of the spinal cord

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11
Q

in the sympathetic NS what do ganglia form

A

the sympathetic chain

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12
Q

where are parasympathetic preganglionic neurones located

A

medulla
sacral segment of spinal cord

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13
Q

where are ganglia located in the parasympathetic NS

A

in the target tissue

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14
Q

what do sympathetic postganglionic neurons to the smooth muscle of the renal vascular bed release

A

dopamine

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15
Q

at the adrenal gland, where do sympathetic preganglionic neurones not synapse and where do they

A

don’t - paravertebral sympathetic ganglion
do - directly onto the adrenal gland

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16
Q

what do preganglionic neurones release on the adrenal gland

A

acetylcholine
activate nicotinic receptors

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17
Q

function of adrenal glands

A

release epinephrine into systemic circulation

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18
Q

what does all excitatory transmission of all the autonomic ganglia involve

A

acetylcholine acting on nicotinic acetylcholine receptors

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19
Q

what does transmission of the postganglionic sympathetic synapse usually involve

A

noradrenaline acting of a-adrenoceptors or b-adrenoceptors

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20
Q

what does transmission at the postganglionic parasympathetic synapse usually involve

A

acetylcholine acting on muscarinic receptors

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21
Q

where does noradrenaline not act

A

sweat glands
resistance blood vessels in skeletal muscle

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22
Q

what drug classification does noradrenaline belong to and why

A

catecholamine
carries a catechol group

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23
Q

name all the metabolites in the synthetic pathway of adrenaline in order

A

tyrosine
L-DOPA
dopamine
adrenaline
noradrenaline

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24
Q

what converts tyrosine into L-DOPA and what does it do

A

tyrosine hydroxylase
adds an OH group to the benzene

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25
Q

what converts L-DOPA into dopamine and what does it do

A

dopadecarboxylase
removes the carboxylic acid from the α-carbon

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26
Q

what converts dopamine into noradrenaline and what does it do

A

dopaminebetahydroxylase
adds an OH group to the β-carbon

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27
Q

what converts noradrenaline into adrenaline and what does it do

A

PNMT
adds a methyl group to the amine
(NH-CH3)

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28
Q

what are the false transmitters metabolites

A

tyramine
octopamine
synephrine

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29
Q

what converts tyrosine into tyramine

A

DDC

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30
Q

what converts tyramine into octopamine

A

DBH

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31
Q

what converts octopamine into synephrine

A

PNMT

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32
Q

what is a competitive inhibitor of tyrosine hydroxylase

A

α-methyltyrosine

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33
Q

what is α-methyltyrosine used to treat

A

phaeochromocytoma

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34
Q

what is α-methyl-DOPA used for

A

interferes with NAdr transmission
leads to synthesis of false transmitter - α-methyl-NAdr

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35
Q

function of carbidopa

A

inhibits dopa-decarboxylase (DCC)

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36
Q

outline the treatment for Parkinson’s disease

A

co-administer carbidopa with L-DOPA
L-DOPA - to increase the amount of precursor for dopamine in the brain
carbidopa - inhibits DCC from converting L-DOPA to dopamine in the bloodstream, which cannot cross the BBB

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37
Q

how is NADR stored

A

stored in vesicles
transport is driven by a proton gradient
stored with ATP and chromogranin

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38
Q

what are drugs that interfere with NADR storgae

A

reserpine
guanethidine

39
Q

features of resperine

A

anti-hypertensive
side effect - depression

40
Q

features of guanethidine

A

anti-hypertensive
side-effect - orthostatic hypotension

41
Q

in terms of NAdr inactivation following release what are the features of uptake 1

A

NAT - noradrenaline transporter
high affinity, low capacity
present on nerve terminals
requires Na+ gradient and ATP
substrate specificity

42
Q

in terms of NAdr inactivation following release what are the features of uptake 2

A

low affinity, high capacity
present on extra-neuronal tissue

43
Q

what was used to demonstrate the uptake mechanism of NAdr

A

iversen

44
Q

what blocks uptake mechanism 2

A

cortisol

45
Q

what blocks uptake mechanism 1 and what are they most clinically used as

A

cocaine
imipramine
desipramine
amitryptaline

46
Q

what weakly blocks uptake mechanism 1

A

guanethidine

47
Q

structure of imipramine

A

tricyclic antidepressant
first one

48
Q

what are drugs that stimulate NAdr release

A

indirect sympathominetics:
tyramine
ephedrine
amphetamine

49
Q

what are the 2 important enzymes and metabolites in NAdr metabolism

A

monoamine oxidase (MAO)
catechol-O-methyltransferase (COMT)
VMA
MHPG

50
Q

what does COMT convert norepinephrine into

A

normetanephrine

51
Q

what does MAO convert normetanephrine into

A

mopegal

52
Q

what converts mopegal into VMA

A

AD

53
Q

what does MAO convert norepinephrine into

A

dopegal

54
Q

what does AR convert norepinephrine into

A

DHPG

55
Q

in NAdr metabolism what happens to DHPG

A

COMT converts it into MHPG

56
Q

what converts MHPG into mopegal and what can reverse this process

A

ADH
AR

57
Q

what are drugs that interfere with NAdr metabolism

A

monoamine oxidase inhibitors (MAOI’s)
iproniazid

58
Q

what are the adrenoceptor subtypes

A

α- isoforms 1/2
β - 1/2/3

59
Q

function of autoreceptors

A

mediates feedback inhibition of neurotransmitter release at the synapse
α1 - predominantly postsynaptic
α2 - predominantly presynaptic

60
Q

what are all β adenoceptors

A

are all GPCR’s and stimulate cAMP formation

61
Q

what do β1 adrenoceptors stimulate

A

cardiac acceleration lipolysis
decrease gut motility and secretion
renin release

62
Q

what do β2 adrenoceptors release

A

bronchodilation
vasodilation of blood vessels to skeletal muscle
glycogen breakdown

63
Q

why would clonidine (α2) have an antihypertensive action

A

clonidine will agonise α2 receptors which are located at the presynaptic membrane
causes a block to noradrenaline release

64
Q

what occurs if you antagonise an α1 adrenocepor

A

anti-hypertensive effect

65
Q

what is isoprenaline

A

a β1 adrenoceptor agonist
used in treatment for asthma
associated with high incidences of heart failure

66
Q

what is salbutamol

A

a β2 adrenoceptor agonist
effective bronchodilator by inhalation

67
Q

what is dobutamine

A

a β1 agonist
used as a cardiac stimulant

68
Q

what is propanolol

A

β adrenoceptor antagonist
non-selective beta blocker
anti-hypertensive
has local anaesthetic action
can cause bronchoconstriction

69
Q

what is atenolol

A

β1 adrenoceptor antagonist
cardio-selective

70
Q

what do atenolol and propanolol both have in their structure

A

oxymethylene bridge

71
Q

what are the signalling properties of α1 adrenoceptors

A

increase in IP3
increase in DAG
mostly excitatory

72
Q

what are the signalling properties of α2 adrenoceptors

A

decrease in cAMP
decrease in CA2+ channels
increase in K+ conductance

73
Q

what are the signalling properties of β1,2,3 adrenoceptors

A

increase in cAMP
mostly excitatory

74
Q

what enzyme makes acetylcholine and from what

A

acetyl CoA and choline
choline acetyltransferase (CAT)

75
Q

what is the rate limiting step for ACh synthesis

A

choline being taken into the nerve transmitter by choline transporter

76
Q

how is ACh taken into presynaptic vesicles and what blocks it

A

via active transport
vesamicol

77
Q

what is ACh released in response to

A

calcium entry into the presynaptic terminal

78
Q

the synaptic cleft is rich in which enzyme and what is its function

A

acetylcholinesterase
breaks down ACh into choline and acetic acid

79
Q

what blocks choline transporter

A

hemicholinium

80
Q

how do different doses of acetylcholine receptors affect blood pressure

A

low doses (2-50μg) causes a drop in blood pressure
higher doses of 5mg cause a rise in blood pressure

81
Q

what blocks muscarinic and nicotinic action

A

muscarinic - atropine
nicotinic - excess of nicotine

82
Q

which drugs have muscarinic and nicotinic action

A

acetylcholine
carbachol

83
Q

what drugs are selective for muscarinic action

A

bethanechol
muscarine
pilocarpine
oxotremorine

84
Q

muscarinic receptors effect of agonists on cardiovascular system

A

decreased HR
decreased cardiac output
decreased vasodilation

85
Q

muscarinic receptors effect of agonists on GI system

A

increased activity

86
Q

muscarinic receptors effect of agonists on gland secretion

A

increased sweating
increased lacrimation
increased salivation

87
Q

features of muscarinic 1 receptors

A

type - neural
location - CNS
cellular action:
increase in IP3 and DAG
function - increase gut motility
increase gastric acid secretion

88
Q

features of muscarinic 2 receptors

A

type - cardiac
location - atria/presynaptic terminals
cellular action - decrease in cAMP
function - cardiac and neural inhibition

89
Q

features of muscarinic 3 receptors

A

type - glandular
location - exocrine glands, smooth muscle, vascular endothelium
cellular action - increase in IP3 and DAG
function - secretion, smooth muscle contraction, vasodilation (via NO)

90
Q

name 2 muscarinic receptor antagonists

A

atropine
pirenzepine

91
Q

what are the effects of nicotine and DMPP

A

stimulation of autonomic ganglia

92
Q

what does hexamethonium block

A

ganglionic nicotinic receptors

93
Q

what can hexamethonium be used to treat

A

hypertension - lowers blood pressure

94
Q

what are the potential side effects of hexamethonium

A

dry mouth
reduced gastric acid secretion
constipation
urinary retention
blurred vision
postural hypotension
sexual dysfunction

Biomed 2 (18 decks)

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