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Pharmacology. 11. Adrenergic Agonists and Antagonists. > Introduction. > Flashcards

Introduction. Flashcards

1
Q

What is an agonist?

A

A substance that binds to a receptor and activates it.

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2
Q

What is an antagonist?

A

A substance that binds to a receptor and either blocks it from functioning or it reduces the effects of that receptor.

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3
Q

Adrenergic agonists will stimulate what kind of receptors?

A

Adrenergic receptors.

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4
Q

What physiological responses are produced when an adrenergic agonist binds to an adrenergic receptor?

A

Physiological responses that are similar to those of catecholamines.

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5
Q

What are the 2 classes of actions that adrenergic agonists can have?

A

Direct effects.

Indirect effects.

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6
Q

What are the effects of direct adrenergic agonists?

A

They bind to and stimulate adrenergic receptors.

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7
Q

What are the effects of indirect adrenergic agonists?

A

They lead to the release of catecholamines from adrenergic neurons.

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8
Q

What is the major neurotransmitter of adrenergic neurotransmission?

A

Norepinephrine.

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9
Q

Where is norepinephrine synthesised and stored?

A

At the terminal end of the pre-synaptic neuron.

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10
Q

What is the first step of norepinephrine synthesis in the pre-synaptic neuron?

A

Tyrosine is taken from the extracellular environment and converted to DOPA within the cell.

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11
Q

What is the rate limiting step in tyrosine formation?

A

The conversion of tyrosine to DOPA.

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12
Q

What enzyme converts tyrosine to DOPA?

A

Tyrosine hydroxylase.

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13
Q

What is the 2nd step of norepinephrine formation after DOPA has been formed?

A

DOPA is converted by DOPA decarboxylase to dopamine.

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14
Q

What is the 3rd step of norepinephrine formation after dopamine has been formed?

A

Dopamine is converted to norepinephrine by dopamine beta-hydroxylase.

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15
Q

What steps of norepinephrine formation are carried out in the cytoplasm?

A

All of the steps that lead to the formation of dopamine.

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16
Q

What steps of norepinephrine formation are carried out in the synaptic vesicle?

A

The conversion of dopamine to norepinephrine takes place in the synaptic vesicle.

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17
Q

When will the vesicles containing norepinephrine be released?

A

Following an action potential.

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18
Q

What happens after norepinephrine has been released into the synaptic cleft?

A

It travels to the post synaptic neuron and binds to adrenergic receptors on the cell membrane.

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19
Q

What happens once norepinephrine has bound to to adrenergic receptors on the post-synaptic cell membrane?

A

It causes an action potential to be generated in the post-synaptic neuron and this leads to cellular effects.

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20
Q

What happens to norepinephrine in the synaptic cleft after it has induced cellular responses in the post-synaptic neuron?

A

It is either taken back into the pre-synaptic neuron or it is metabolised by certain enzymes.

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21
Q

What name is given to the process where norepinephrine is taken back into the pre-synaptic neuron?

A

Re-uptake 1

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22
Q

What is the function of the pre-junctional receptor on the pre-synaptic cell of adrenergic neurons?

A

It detects norepinephrine in the synaptic cleft and provides negative feedback to stop the release of norepinephrine.

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23
Q

What are the 2 classes of adrenergic receptors?

A

Alpha receptors.

Beta receptors.

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24
Q

What are the 2 types of alpha receptors?

A

Alpha-1 receptors.

Alpha-2 receptors.

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25
Q

What are the 2 types of beta receptors?

A

Beta-1 receptors.

Beta-2 receptors.

Beta-3 receptors.

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26
Q

What kind of adrenergic receptors are of no medical significance?

A

Beta-3 receptors.

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27
Q

Where are alpha-1 receptors located?

A

On the post synaptic membrane of the effector organ.

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28
Q

Where are alpha-2 receptors located?

A

On pre-synaptic nerve endings.

On post synaptic neurons of the beta cells of the pancreas and on blood vessels.

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29
Q

What happens when alpha-1 receptors are activated in blood vessels?

A

Vasoconstriction.

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30
Q

Alpha-1 receptors are mostly affected by what 3 hormones and in what level of potency?

A

Epinephrine.

Norepinephrine.

Isoproterenol.

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31
Q

What kind of receptors are alpha-1 receptors?

A

GCPR’s.

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32
Q

What protein are the GCPR’s of alpha-1 receptors connected to?

A

A GQ protein.

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33
Q

What happens to the GQ receptor when alpha-1 receptors are activated?

A

It is activated and the activates phospholipase C which cleaves PIP-3 to form IP-3 and DAG to act as 2nd messengers.

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34
Q

What is the function of IP-3 and DAG in alpha-1 receptors?

A

AG activates a protein kinase.

IP-3 releases calcium which activates smooth muscle.

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35
Q

Alpha-2 receptors are linked to what protein?

A

A GI protein.

36
Q

What is the function of the GI protein that is bound to alpha-2 receptors?

A

It prevents calcium ions being released into the pre-synaptic neuron so no neurotransmitter can be released.

It inhibits adenylyl cyclase and this leads to smooth muscle contraction.

37
Q

What protein are beta-1 and beta-2 receptors linked to?

A

The stimulatory G protein which is GS.

38
Q

What is the function of the GS protein that is bound to beta-1 and beta-2 receptors?

A

It activates adenylyl cyclase which converts ATP to cyclic AMP.

39
Q

What are the effects on the body once the GS protein that is bound to beta-1 and beta-2 receptors has been activated?

A

It stimulates heart muscle contraction.

It stimulates smooth muscle relaxation.

It stimulates glycogenolysis.

40
Q

Where are beta-1 receptors located?

A

In the heart.

In the juxta-glomerular apparatus of the kidney.

In fat cells.

41
Q

Will beta-1 receptors have a higher affinity for epinephrine or norepinephrine?

A

It has equal affinity for both.

42
Q

Increases in heart rate will always be due to what kind of receptors?

A

Beta-1 receptors.

43
Q

Where are beta-2 receptors located?

A

In the blood vessels of skeletal muscle.

In the liver.

In the smooth muscles of the bronchus.

In the GI tract.

In the uterus.

44
Q

Will beta-2 receptors have a higher affinity for epinephrine or norepinephrine?

A

Epinephrine.

45
Q

Epinephrine binding to the beta-1 receptors of the heart will have what 3 effects on the heart?

A

Increased heart rate.

Increased contractility of the heart.

Increased cardiac output.

46
Q

Norepinephrine binding to the beta-1 receptors of the heart will have what 2 effects on the heart?

A

Initial increase in heart rate before it is reduced by vagal stimulation.

Increased contractility of the heart.

47
Q

Epinephrine binding to the beta-1 receptors of the heart will have what 2 effects on blood pressure?

A

Increase in systolic pressure.

Decrease in diastolic pressure.

48
Q

Norepinephrine binding to the beta-1 receptors of the heart will have what 2 effects on blood pressure?

A

Increase in systolic pressure.

Increase in diastolic pressure.

49
Q

What receptors are found in the blood vessels of the skin, the mucosa and the kidneys?

A

Alpha-1 receptors.

Alpha-2 receptors.

50
Q

Epinephrine binding to the alpha-1 receptors and alpha-2 receptors of the blood vessels will have what effects on blood vessel size?

A

Vasoconstriction.

51
Q

Norepinephrine binding to the alpha-1 receptors and alpha-2 receptors of the blood vessels will have what effects on blood vessel size?

A

Vasoconstriction.

52
Q

What receptors are found in the blood vessels of the splanchnic organs and heart?

A

Alpha receptors.

Beta-2 receptors.

53
Q

Epinephrine binding to the alpha receptors and beta-2 receptors of the blood vessels will have what effects on blood vessel size?

A

Vasodilation.

54
Q

Are the compensatory changes to the heart rate following the release of epinephrine?

A

No, the heart will continue to beat at a high rate.

55
Q

What adrenergic receptors are found in the bronchial muscle?

A

Beta-2 receptors.

56
Q

What effect will epinephrine have on the beta-2 receptors of the bronchial muscle?

A

Relaxation of the muscle.

57
Q

What adrenergic receptors are found in the smooth muscle of the GIT?

A

Alpha-1 receptors.

Alpha-2 receptors.

Beta-2 receptors.

58
Q

What effect will epinephrine have on the receptors that control the smooth muscle of the GIT?

A

Relaxation of the muscles.

59
Q

What effect will norepinephrine have on the receptors that control the smooth muscle of the GIT?

A

Relaxation of the muscles.

60
Q

What receptors are found on the detrusor muscle of the bladder?

A

Beta-2 receptors.

61
Q

What receptors are found on the sphincter muscle of the bladder?

A

Alpha-1 receptor.

62
Q

What effect will epinephrine have when it binds to the detrusor muscle of the bladder?

A

Relaxation.

63
Q

What effect will epinephrine have when it binds to the sphincter of the bladder?

A

Contraction.

64
Q

What effect will norepinephrine have when it binds to the sphincter of the bladder?

A

Contraction.

65
Q

What adrenergic receptors are found on the uterus?

A

Alpha-1 receptors.

Alpha-2 receptors.

Beta-2 receptors.

66
Q

What effect will epinephrine have when it binds to the adrenergic receptors of the uterus?

A

Relaxation/contraction of the uterus.

67
Q

What adrenergic receptors are found on the vas deferens of the male?

A

Alpha-1 receptors.

68
Q

What effect will epinephrine have when it binds to the adrenergic receptors of the vas deferens of the male?

A

Ejaculation.

69
Q

What effect will norepinephrine have when it binds to the adrenergic receptors of the vas deferens of the male?

A

Ejaculation.

70
Q

What adrenergic receptors are found on the pilomotor muscles of the skin?

A

Alpha-1 receptors.

71
Q

What effects will norepinephrine have on the adrenergic receptors of the pilomotor muscles of the skin?

A

Contraction.

72
Q

What effects will epinephrine have on the adrenergic receptors of the pilomotor muscles of the skin?

A

Contraction.

73
Q

What adrenergic receptors are found on the radial muscle of the iris?

A

Alpha-1 receptors.

74
Q

What effects will norepinephrine have on the adrenergic receptors of the radial muscle of the iris?

A

Contraction/pupil dilation.

75
Q

What effects will epinephrine have on the adrenergic receptors of the radial muscle of the iris?

A

Contraction/pupil dilation.

76
Q

What adrenergic receptors are found on the ciliary muscles of the eye?

A

Beta-2 receptors.

77
Q

What effects will epinephrine have on the adrenergic receptors of the ciliary muscles of the eye?

A

Relaxation.

78
Q

What effects will norepinephrine/epinephrine have when it binds to beta-2 and alpha-1 receptors of the liver?

A

Glycogenolysis.

79
Q

What effects will norepinephrine/epinephrine have when it binds to alpha-2 and beta-2 receptors on the beta cells of the pancreas?

A

Alpha-2 receptors lead to decreased secretion.

Beta-2 receptors lead to increased secretion.

80
Q

What are the major functions of alpha-1 receptors?

A

Vasoconstriction of blood vessels.

Increasing the muscle tone in sphincter muscles.

81
Q

What is the major function of alpha-2 receptors?

A

Vasoconstriction of blood vessels.

82
Q

What is the major function of beta-1 receptors?

A

An increase in cardiac output.

Vasodilation within skeletal muscle.

83
Q

What is the major function of beta-2 receptors?

A

Relaxation of smooth muscle in certain areas of the body.

Glycogenolysis.

84
Q

Are catecholamines well absorbed via the oral route?

A

No.

85
Q

Are catecholamines well absorbed via the subcutanous route?

A

Yes, but they are absorbed very slowly.

86
Q

What enzymes will metabolise catecholamines?

A

Mono-amine oxidase.

Catechol-O-methyltransferase.

87
Q

How are catecholamines excreted?

A

In urine.

Pharmacology. 11. Adrenergic Agonists and Antagonists. (7 decks)

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