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Principles Pharmacology > Autonomic Pharmacology > Flashcards

Autonomic Pharmacology Flashcards

1
Q

What does the somatic afferent include?

A

Nerves supplying skin, joints, muscle

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2
Q

What does the somatic efferent include?

A

Neurons leaving spinal cord and enervating muscle (voluntary contraction)

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3
Q

What nervous system are the myenteric plexus and submucosal plexus part of?

A

ENS

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4
Q

What is a ganglion?

A

a collection of nerve cell bodies that lie outside of the CNS

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5
Q

Which system, parasympathetic or sympathetic uses ACh neurotransmitter for the preganglionic neurone and noradrenaline in the postganglionic neurone?

A

Sympathetic

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6
Q

In which are the axons shorter, pre or post ganglionic neurones?

A

Pre ganglionic neurones

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7
Q

What neurotransmitter does the parasympathetic system use for both preganglionic and postganglionic neurones?

A

ACh

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8
Q

State the 5 steps of neurochemical transmission.

A

-Uptake of transmitting precursor
-Synthesis of transmitter
-Storage of transmitter
-Depolarization by Action Potential
-Calcium ion influx through voltage activated calcium ion channels
-Calcium induced release of transmitter (exocytosis)
-Receptor activation
-Enzyme-mediated inactivation
OR
-Reuptake of transmitter

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9
Q

In sympathetic division of ANS, what does ACh open in the postganglion neurone and what does this cause?

A

Ligand-gated ion channels, causing depolarization and generation of action potentials

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10
Q

What does noradenaline activate in the sympathetic division?

A

G-protein coupled adrenoceptors

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11
Q

What does ACh activate in the parasympathetic division?

A

G-protein coupled muscarinic acetylcholine receptors

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12
Q

Where is muscarine found?

A

poisonous mushrooms

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13
Q

How many glycoprotein subunits do ligand-gated ion channels contain and what do these form?

A

5, and central ion conducting channel (each spans the cell membrane)

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14
Q

What do ligand-gated channels allow?

A

rapid changes in permeability of membrane to certain ions, alters membrane potential

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15
Q

How many binding sites are there normally for ACh receptors?

A

2

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16
Q

When the transmitter binds to the binding site on to the ion channel, does a conformational change occur immediately?

A

No, short delay

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17
Q

How many glyoprotein subunits are in an ACh receptor?

A

5

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18
Q

What are the steps of cholinergic transmission?

A
  • Uptake of choline via transporter
  • Synthesis of ACh via CAT
  • Storage of ACh via transporter
  • Depolarization by action potential
  • Ca2+ influx
  • Calcium ion induced release of ACh (exocytosis)
  • Activation of ACh receptor subtypes (M1-M3)
  • Degradation of ACh to choline and acetate by AChE, terminating transmission
  • Reuptake and reuse of choline
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19
Q

What opens when 2 ACh molecules bind to receptor?

A

Sodium channel, creating graded depolarisation that can vary in amplitude

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20
Q

What is the name given to this graded depolarisation?

A

EPSP

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21
Q

What happens if depolarisation reaches threshold?

A

voltage-gated sodium ion channels open and nerve transmission occurs

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22
Q

Which is the only drug that affects cholinergic transmission at ganglia with any clinical significance?

A

Nicotine

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23
Q

What does nicotine mimic the effect of?

A

ACh

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24
Q

What does hexamethonium do and how?

A

Selectively blocks ganglionic transmission by open channel block (a form of non-competitive antagonism)

25
Q

What are the most popular type of receptor in the body involved in chemical transmission?

A

G-protein coupled receptors

26
Q

Which of these are G-proteins involved in: Rods and cones of retinas to allow sight; transduction of odors from curry to electrical signals

A

Both!

27
Q

Are the receptor, G-protein and effector separate or combined proteins?

A

Separate

28
Q

Is signalling via G-proteins fast or slow in comparison to transmitter-gated ion channels?

A

Slow

29
Q

What type of membrane protein is the receptor?

A

Integral

30
Q

What type of membrane protein is the G-protein?

A

Peripheral

31
Q

What does the receptor protein consist of?

A

Single polypeptide with extracellular NH2 and intracellular COOH termini

32
Q

How many transmembrane spans does the receptor contain and what are they joined by?

A

7, 3 extracellular and 3 intracellular connecting loops

33
Q

What is it that allows the receptor to interact with the G-protein?

A

large intracellular loop and COOH tail

34
Q

G-proteins consist of how many polypeptide subunits?

A

3

35
Q

Which of the G-protein’s subunits can disassociate from the other two?

A

alpha

36
Q

Where is the guanine nucleotide binding site in the G-protein and what can it hold?

A

alpha subunit, GTP or GDP

37
Q

When G-proteins couple with receptors to cause a conformational change, the affinity of the binding site for what is reduced and what occurs?

A

GDP, so this dissociates from and GTP binds to the alpha subunit

38
Q

What does the G-protein lose its affinity for after GTP binding?

A

Beta-gamma subunit, so alpha protein dissociates

39
Q

What does the alpha subunit combine with to turn on or off action?

A

effector

40
Q

What acts as an enzyme and what does it hydrolyse in G-protein function to turn off the signal?

A

the alpha subunit, hydrolyses GTP to GDP and Pi, to turn off signal

41
Q

What are muscarinic receptors examples of?

A

G-protein coupled receptors

42
Q

How many clinically important muscarinic receptors are there?

A

3 (M1,2,3)

43
Q

Which receptors cause acid secretion in the stomach?

A

M1

44
Q

Which receptors are present on the SAN?

A

M2

45
Q

What do presynaptic autoreceptors mediate?

A

Inhibition of transmitter release (negative feedback)

46
Q

If NA or ACh are released, what happens to amounts of Ca coming in?

A

Limited, decreased release of NA and ACh (negative feedback)

47
Q

What does cocaine structurally resemble?

A

Noradrenaline

48
Q

What transporter is noradrenaline recognised by?

A

U1

49
Q

What do both amphetamine and cocaine cause?

A

vasoconstriction (alpha 1 stimulation) and cardiac arrythmias (B1 stimulation)

50
Q

What does amphetamine structurally resemble?

A

Noradrenaline

51
Q

What does Amphetamine inhibit?

A

MAO enzyme

52
Q

What does amphetamine cause increased stimulation of?

A

Adrenoceptor

53
Q

What does prazosin block?

A

alpha 1 (selective, competitive antagonist)

54
Q

What is prazosin used for?

A

Anti-hypertensive agent. Vasodilates.

55
Q

What does atenolol block?

A

B1

56
Q

What is atenolol used for?

A

anti-anginal, anti-hypertensive

57
Q

What does salbutomol do?

A

Selective agonist of B2. Used as bronchodilator in asthma

58
Q

What is atropine used for?

A

To reverse bradycardia following MI and in anticholinesterase poisoning

59
Q

What does atropine block?

A

Competitive antagonist of muscarinic ACh receptors (M1, M2 and M3 with equal affinity)

Principles Pharmacology (6 decks)

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