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Cardio/Pulm Final > Lecture 10 (DSA): Intro to ANS Pharm > Flashcards

Lecture 10 (DSA): Intro to ANS Pharm Flashcards

1
Q

How do agonists activate a receptor?

A

Activate the receptor to signal as a direct result of binding to it.

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2
Q

Agonists can activate a receptor to produce effects in what 2 ways?

A

1) All of the receptors biologic functions

2) Selectively promote one function more than another

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3
Q

Antagonists do what to the signaling of receptor?

A

Block the generation of a signal by binding to the receptor

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4
Q

What are cholinomimetic agents?

A

Drugs that mimic ACh:

  • AChR agonists
  • Acetylcholinesterase inhibitors
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5
Q

What are cholinoceptor-blocking drugs?

A

AChR antagonists

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6
Q

What are sympathomimetic agents?

A

Drugs that mimic or enhance α- and β- receptor (agonists)

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7
Q

What are 2 ways sympathomimetic agents act as an agonist?

A

1) Enhance catecholamine release

2) Block re-uptake of catecholamines

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8
Q

What are adrenoceptor-blocking drugs?

A

α- and β- receptor antagonists

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9
Q

How does sympathetic innervation of the SA node affect heart rate?

A

Increases heart rate

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10
Q

What is the receptor on the SA node for sympathetic innervation?

A

β1 adrenergic receptor

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11
Q

How does parasympathetic innervation of the SA node affect heart rate?

A

Decrease in heart rate

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12
Q

What is the receptor on the SA node for parasympathetic innervation?

A

M2 (muscarinic)

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13
Q

What does sympathetic innervation of the atria cause?

A

Increase in contractility and conduction velocity?

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14
Q

What is the receptor in the atria for sympathetic innervation?

A

β1 adrenergic receptor

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15
Q

What does parasympathetic innervation of the atria cause?

A

Decrease in contractility

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16
Q

What is the receptor in the atria for parasympathetic innervation?

A

M2 (muscarinic)

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17
Q

What does sympathetic innervation of the tracheal and bronchial smooth muscle cause?

A

Relaxation

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18
Q

What is the primary receptor for sympathetic innervation of the bronchial and tracheal smooth muscle?

A

β2 adrenergic receptor

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19
Q

What does parasympathetic innervation of the tracheal and bronchial smooth muscle cause?

A

Contraction

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20
Q

What is the primary receptor for parasympathetic innervation of the bronchial and tracheal smooth muscle?

A

M2=M3 (muscarinic)

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21
Q

What does sympathetic innervation of the bronchial glands cause?

A

Decreased secretion or increased secretion

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22
Q

What are the α1 receptors of bronchial glands responsible for?

A

Decreased secretion

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23
Q

What are the β2 receptors of bronchial glands responsible for?

A

Increased secretion

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24
Q

What does parasympathetic innervation of the bronchial glands cause?

A

Contraction

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25
Q

What receptors are found on bronchial glands for parasympathetic innervation?

A

M2, M3 (muscarinic)

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26
Q

What are the neurotransmitters and receptors for parasympathetic nervous system?

A

NT: ACh

Receptors: nAChR and mAChR

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27
Q

What are the neurotransmitters and receptors for sympathetic nervous system?

A

NE > Epi; ACh

Receptors: α, β, nAChR, and mAChR

28
Q

Sympathetic nervous system uses what NT to activate which receptor in the adrenal medulla to release what NT?

A

ACh activates nicotinic ACh receptors to release epinephrine

29
Q

Sweat glands contain what receptor on them and are innervated by what part of the autonomic NS?

A

Muscarininc choline receptos (mAChR) activated by ACh from the sympathetic nervous system

30
Q

Synthesis of epinephrine primarily occurs where; from what?

A

Adrenal medualla from NE—->Epi

31
Q

Dopamine is the precursor to what?

A

NE and epinephrine

32
Q

Which muscarinic receptors are coupled to Gq/11 and their activation results in?

A

M1, M3, M5

  • Activation of PLC; IP3, DAG cascade (smooth muscle contraction)
33
Q

When IP3 levels go up what occurs?

A

Contraction of smooth muscle

34
Q

Which muscarinic receptors are coupled to Gi/o and their activation results in?

A

M2 and M4

  • Inhibition of AC; decreased cAMP production, activation of K+ channels
35
Q

A decrease in cAMP production controlled by the M2 receptors of cardiac muscle have what affect?

A

Decrease in strength and force of contraction in cardiac tissue, decreases rate.

36
Q

Why is having M3 receptors important in the gut?

A

When stimulated by the parasympathetic nervous system will causes contraction allowing for digestion to resume

37
Q

Explain the basic mechanism of tyrosine to NE?

A

Tyrosine enters the nerve and is converted to dopa, then to dopamine (in the cytoplasm). Dopamine is shuttled into vesicle where it is converted to NE.

38
Q

After the NE or epi has performed its function on the α- or β-receptors what occurs?

A

Will undergo reuptake by a transporter and be stored until needed again.

39
Q

What is the vesicular monoamine transporter (VMAT-2)?

A
  • Transports NE, Epi, DA, and serotonin into vesicles for storage
  • Inhibited by Reserpine
40
Q

What does cocaine inhibit?

A

Blocks the transporter of NE, causes NE accumulation

41
Q

What are the 2 main enzymes for the metabolism of catecholamines?

A

1) Monoamine oxidase (MAO)

2) Catechol-O-methyltransferase (COMT)

42
Q

Are there degradative enzyme for catecholamines during signaling?

A

No, they differ from cholinergic signaling, and instead undergo reuptake into the nerve.

43
Q

Where are the Alpha-1 receptors found?

A

Vascular, GU smooth muscle, intestinal smooth muscle, Heart

44
Q

What is the Alpha-1 response in the vascular and GU smooth muscle?

A

Contraction = Vasoconstriction

45
Q

What is the Alpha-1 response in the heart?

A

Increased contractile force, arrhythmia’s

46
Q

Where are the Alpha-2 receptors found?

A

Vascular smooth muscle, pancreatic islet (B cells), Platelets, and nerve terminals

47
Q

Function of Alpha-2 receptors in nerve terminals and vascular smooth muscle?

A

Nerve terminals - Decreased release of NE

Vascular - Contraction

48
Q

Function of Alpha-2 receptors on platelets?

A

Aggregation

49
Q

Where are the Beta-1 receptors found?

A

Heart and Juxtaglomerular cells

50
Q

Function of the Beta-1 cells in the heart?

A

Increased force and rate of contraction and AV nodal conduction velocity

51
Q

Where are the Beta-2 receptors found?

A

Smooth muscle (vascular, bronchial, GI, GU), Skeletal muscle

52
Q

Function of Beta-2 receptors

A
  • Relaxation of smooth muscle

- Glycogenolysis; uptake of K+

53
Q

Epinephrine has a stronger affect on which adrenergic receptor?

A

Beta-2

54
Q

In the heart which receptor produces the greatest sympathetic effects?

A

Beta-1

55
Q

In the blood vessels which receptor predominates for the sympathetic nervous system?

A

Alpha-1

56
Q

In the heart which receptor predominates for parasympathetic innervation?

A

Muscarinic (M2)

57
Q

In the blood vessels which receptor predominates for parasympathetic innervation?

A

Muscarinic (M3)

58
Q

ACh & muscarinic agonists given IV cause what, due to?

A

Vasodilation due to release of nitric oxide (NO)

59
Q

Smooth muscle of blood vessels are NOT innervated by?

A

Parasympathetic neurons

60
Q

Activation of mAChRs on endothelial cells causes production and release of?

A

Endothelium-derived relaxing factor (EDRF), also known as nitric oxide (NO)

61
Q

Where are chromaffin cells located and what kind of receptor do they contain?

A

Found within the Adrenal Medulla and contain NAChR’s

62
Q

What are the effects of Reserpine?

A

Blockade of NE storage and depletion by MAO

63
Q

Botulinum toxin effects?

A

Anticholinergic; inhibition of NT release

64
Q

Nicotine and pilocarpine are?

A

nAChR and mAChR agonists (Cholinomimetic)

65
Q

Tubocurarine and atropine are?

A

nAChR and mAChR antagonists (Anticholinergic)

66
Q

Alpha blockers (phentolamine) and beta blockers (propranolol) are?

A

Antiadrenergic

67
Q

Alpha agonists (nepinephrine) and beta agonists (albuterol) are?

A

Adrenomimetic

Cardio/Pulm Final (18 decks)

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