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
Q

what were the first alpha- adrenoreceptors to be described?

A

the ergot alkaloids

26
Q

what is ergotamine used for?

A

to treat migraine

27
Q

what is ergometrine used for?

A

to treat heamorrhage

28
Q

which drugs inhibit noradrenaline synthesis?

A

carbidopa
alpha methyl dopa
metirosine
disulfiram

29
Q

what does metirosine do?

A

inhibits tyrosine hydroxylase (rate limiting step)

30
Q

what does carbidopa do?

A

inhibits dopa-decarboxylase

31
Q

what does alpha methyl dopa do?

A

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
Q

what does disulfiram do?

A

blocks dopamine-beta hydroxylase

33
Q

what does reserpine do?

A

depletion of noradrenaline by preventing the passage of catecholamines into the storage vesicles and are then inactivated by MAO

34
Q

what does guanethidine do?

A

inhibits release of noradrenaline

35
Q

what do cocaine and TCA-desmethylimipramine do?

A

block uptake of the noradrenaline

36
Q

what is phenelzine?

A

non-selective MAO inhibitor - can cause tyramine cheese reaction and greatly increased sympathetic response and sub-arachnoid haemorrhage

37
Q

what is selegeline?

A

MAO-B selective inhibitor