Adrenergic effects Flashcards

1
Q

What are sympathomimetics?

A

Drug that recreates the stimulation of a sympathetic nerve

Either they’re directly acting or they act indirectly by boosting the level of noradrenaline

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2
Q

What is isoprenaline?

A

• Isoprenaline is a synthetic chemical which was developed for research purposes

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3
Q

Potency in alpha and beta adrenergic receptors

A
  • In Alpha, noradrenaline more potent than adrenaline which is more potent than isoprenaline
  • In Beta, isoprenaline more potent than adrenaline which is more potent than noradrenaline
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4
Q

What are all adrenoreceptors examples of?

A

All adrenoreceptors are examples of GPCR

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5
Q

REFER TO NOTES FOR RECEPTORS AND THERE EFFECTS

A

1

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6
Q

What do alpha 1 adrenoreceptor contract?

A

• Contract vascular smooth muscle

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7
Q

What do alpha 1 adrenoreceptor increase?

A

Increase total peripheral resistance

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8
Q

What do alpha 1 adrenoreceptors look like?

A

Looks like beads on strings-Varicosities

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9
Q

What do varicosities spray out?

A

Varicosities spray out transmitter

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10
Q

Pathway of alpha 1 adrenoreceptor?

A
  • IP3 binds to its own receptor which is a Ca2+ channel thus causing the release of Ca2+ from the internal calcium stores
  • DAG tends to stay in the lipid phase and can activate ion channels itself or activate PKC
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11
Q

What other tissues are alpha 1 adrenoreceptors found in?

A

• Are found in other tissue:
○ Leading to contraction of the seminal vesicles
○ Contraction of Iris muscle which results in diluted pupils
Contraction of pilomotor muscle which controls hair

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12
Q

Main role of alpha 2 adrenoreceptor?

A

Main role is the inhibition of neurotransmitter release

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13
Q

Mechanism of adrenoreceptor 2

A

• Negative feedback mechanism which tends to be a receptor located on the nerve terminals or the varicosities
○ Decreased likely hood of the Ca2+ ion channel being opened and it becomes less sensitive to voltage
○ Adenylate cyclase becomes inhibited so the cAMP goes down and PKA goes down
○ The beta subunits stimulate some potassium channels so a cell becomes calmer. Potassium leaves a cell and the membrane potential becomes more negative
This is where the neurone can be hyperpolarised, reducing the activity of the Ca2+ channels

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14
Q

Beta 1 adrenoreceptors

A

• Sympathetic innervation is throughout the heart
• Innervation of the SAN, AVN, atria and ventricles
An increase in heart rate

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15
Q

What happens when sympathetic nerve stimulated?

A

○ When the sympathetic nerve is stimulated, it depolarised the action potential and it becomes briefer
Results in a larger but shorter contraction which is more powerful

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16
Q

Beta 1 adrenoreceptor mechanism

A

• There is an increase in cAMP which interacts with a pacemaker channel in the SAN
More calcium released but also more calcium uptake

17
Q

Beta 1/2 adrenoreceptor

A

• Increases cardiac muscle function
• Beta 2 adrenoreceptor relaxes vascular smooth muscle:
○ Especially airways
○ Skeletal muscle vasculature
○ Coronary and cerebral blood vessels
• PKA inhibits the go mechanism in smooth muscles

18
Q

What do beta 1 blocker do

A

• Reduce arrhythmia

Less renin production in kidneys

19
Q

What are the main uses of adrenoreceptor blockers

A
• Eye drops
• Heart 
• Kidneys
• Urination
  Adrenal gland tumour