Pharmacology of the Sympathetic Nervous System Flashcards

1
Q

give a description of a sympathetic nerve

A

short preganglionic axons whose cell body located within the spinal cord in the intermediolateral column (IML) and long postganglionic axons

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2
Q

what is the main neurotransmitter released at sympathetic neuroeffector junctions

A

noradrenaline (along with ATP). there are also cotransmitters that are released such as NPY

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3
Q

what does sympathetic innervation of sweat glands release

A

acetylcholine (acts on muscarinic receptors)

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4
Q

what are the major agonists in the sympathetic system?

A
the catecholamines:
noradrenaline 
adrenaline 
dopamine 
isoprenaline
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5
Q

describe beta-2 receptors

A

beta 2 receptors are not innervated and are inhibitory

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6
Q

decribe beta-1 receptors

A

beta 1 receptors are excitatory and innervated

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7
Q

what feature do all adrenoreceptors share?

A

they are all G-protein coupled receptor type receptors containing 7 transmembrane spanning domains

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8
Q

which effector mechanism is linked to alpha1 adrenoreceptors?

A

the alpha1 adrenoreceptors are primarily coupled to phospholipase C with an increase in IP3 and Diacylglycerol (DAG)

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9
Q

Which effector mechanism is linked to alpha2 adrenoreceptors?

A

negatively coupled to adenyl cyclase

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10
Q

Which effector mechanism are linked to beta adrenoreceptors?

A

increase in cyclic AMP and protein phosphorylation via protein kinase A

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11
Q

Where is noradrenaline primarily released from

A

sympathetic nerve terminals

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12
Q

where is adrenaline primarily released from

A

adrenal medulla

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13
Q

describe potency of noradrenaline

A

noradrenaline is more potent on alpha than beta

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14
Q

describe potency of adrenaline

A

adrenaline is more potent on beta than alpha

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15
Q

what is potency of isoprenaline

A

very selective for beta- adrenoreceptors

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16
Q

what are general alpha adrenoreceptor agonists and what are they primarily used for?

A

adrenaline and noradrenaline

primarily used for anaphylactic shock, cardiac arrest and to prolong anaesthesia

17
Q

name an alpha1 agonist and what is it mainly used for?

A

phenylephrine

primarily used as a nasal decongestant

18
Q

name an alpha2 agonist and what is it mainly used for?

A

clonidine

anti-hypertensive

19
Q

name some other alpha2 agonists and what they are used for?

A

dipivefrine - adrenaline prodrug
bromindine

used to treat open angle glaucoma - reduces the rate of production of aqueous humour

20
Q

what is the role of beta 2 selective agonists?

A

salbutamol and salmeterol

  • used in asthma for bronchodilation and to relax the uterus in premature labour
21
Q

what do indirect acting sympathomimetic drugs do?

A

release noradrenaline in the absence of nerve stimulation

22
Q

name some indirectly acting sympathomimetics

A

tyramine
ephedrine
amphetamine

23
Q

the effects of adrenaline on the heart are a combination of the actions of which two drugs?

A

noradrenalin and isoprenaline

24
Q

beta1 agonists and what are they used for?

A

dobutamine and bisoprolol

used for congestive heart failure

25
what were the first alpha- adrenoreceptors to be described?
the ergot alkaloids
26
what is ergotamine used for?
to treat migraine
27
what is ergometrine used for?
to treat heamorrhage
28
which drugs inhibit noradrenaline synthesis?
carbidopa alpha methyl dopa metirosine disulfiram
29
what does metirosine do?
inhibits tyrosine hydroxylase (rate limiting step)
30
what does carbidopa do?
inhibits dopa-decarboxylase
31
what does alpha methyl dopa do?
converted by dopamine beta hydroxylase to alpha methyl dopamine then converted to alpha methyl noradrenaline and becomes false transmitter and resistant to degredation by MAO
32
what does disulfiram do?
blocks dopamine-beta hydroxylase
33
what does reserpine do?
depletion of noradrenaline by preventing the passage of catecholamines into the storage vesicles and are then inactivated by MAO
34
what does guanethidine do?
inhibits release of noradrenaline
35
what do cocaine and TCA-desmethylimipramine do?
block uptake of the noradrenaline
36
what is phenelzine?
non-selective MAO inhibitor - can cause tyramine cheese reaction and greatly increased sympathetic response and sub-arachnoid haemorrhage
37
what is selegeline?
MAO-B selective inhibitor