Autonomic Pharmacology Flashcards

1
Q

What are the two main neurotransmitters for the efferent neurons?

A

Acetylcholine Norepinephrine

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2
Q

What is the origin of the sympathetic nervous system?

A

Thoracolumbar (T1-L3) in the sympathetic chain ganglion

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3
Q

What are the fiber lengths of the pre and post ganglionic neurons of the SNS?

A

Short pre-ganglionic Long post ganglionic

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4
Q

What is the origin of the parasympathetic nervous system?

A

Cranial Sacral (originate via cranial nerves)

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5
Q

Where are the ganglia located in the SNS?

A

Paravertebrial chain

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6
Q

How are is the SNS distributed throughout the body?

A

Widely distributed, post-ganglionic neurons may innervate more than one organ

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7
Q

What are the fiber lengths of the pre and post ganglionic neurons of the PSNS?

A

Long pre-ganglionicShort post ganglionic

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8
Q

Where are the ganglia located in the PSNS?

A

Near the effector tissue

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9
Q

What is the typical response of the SNS?

A

Flight of fight

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10
Q

How is the PSNS distributed throughout the body?

A

Discrete, post-ganglionic neurons are not branched and are directed to a specific organ

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11
Q

What is the primary response of the PSNS?

A

Rest and digest

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12
Q

What are the two types of nicotinic receptors?

A

Nicotinic neural (Nn)Nicotinic muscular (Nm)

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13
Q

How does the SNS and the PSNS react to each other?

A

Opposing, antagonistic effects

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14
Q

What type of receptors and neurotransmitter are at all preganglionic junctions?

A

Nn receptors agonized by Ach

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15
Q

What type of receptor and neurotransmitter are at the sweat glands?

A

Muscarinic receptors agonized by Ach (sweat glands are innervated by the SNS)

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16
Q

What type of receptors and neurotransmitters are at adrenergic tissues?

A

Alpha and beta receptors are agonized by Norepinephrine

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17
Q

The term adrenergic is used to describe which type of drugs?

A

Epinephrine
Norepinephrine
Dopamine

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18
Q

What dopamine receptor is predominately peripheral?

A

D1 (D2 more important for the brain)

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19
Q

What are nonadrenergic/noncholinergic neurotransmitters?

A

Neurotransmitters and or co-transmitters that function in the PNS, unsure of exact role currently

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20
Q

What are the criteria for a neurotransmitter?

A
  1. Synthesis2. Storage3. Release 4. Action at receptor5. Termination
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21
Q

What two components make up an acetylcholine molecule?

A

Acetyl CoACholine

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22
Q

What enzyme breaks down acetylcholine?

A

Acetylcholinesterase, choline is recycled by transporter

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23
Q

What is unique about the choline transporter?

A

It is rate limiting

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24
Q

How many subtypes are there of muscarinic acetylcholine receptors?

A

M1-M5

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25
Q

What distinguishes the two subgroups of muscarinic Ach receptors?

A

The two subgroups are stimulatory and inhibitory, the difference is the second messenger

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26
Q

What type of receptor is the muscarinic Ach receptor?

A

G-protein coupled receptor

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27
Q

What type of receptor is the nicotinic Ach receptor?

A

Ligand-gated Na and K depolarizing channel

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28
Q

Where are muscarinic Ach receptors located?

A

Parasympathetic effector tissues (heart, endothelium, smooth muscle and glands)

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29
Q

Where are nicotinic Ach receptors located?

A

Autonomic ganglia-NnCNS-NnSkeletal muscle innervated by somatic nerves-Nm

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30
Q

How are blood vessels affected by the PSNS?

A

Blood vessels are only innervated by the SNS, but M2 receptors on endothelium can cause vasodilation

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31
Q

How is norepinephrine synthesized?

A

Tyrosine –> DOPA –> Dopamine –> NE

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32
Q

What two enzymes break down Norepinephrine?

A

MAOCOMT

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33
Q

How is the action of Norepinephrine terminated?

A

Re-uptake

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34
Q

What type of receptors are alpha and beta?

A

G-protein coupled receptors

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35
Q

What is the difference between the two alpha receptors?

A

A1 is excitatory (increased Ca)A2 is inhibitory (decreased cAMP)

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36
Q

What are the ligands for the alpha and beta receptors?

A

Epinephrine
Norepinephrine
Dopamine (at high doses)

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37
Q

Which adrenergic receptor is most susceptible to change?

A

Betas are susceptible to adaptive changes (up or down regulate)

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38
Q

What are the autonomic effector tissues?

A

Hear, Kidney, Liver, Smooth muscle, Somatic motor, and Fat cells

39
Q

What adrenergic receptor causes the release of renin?

A

Beta1

40
Q

What effects does the beta2 receptor have on the liver?

A

Glycogenolysis and gluconeogenesis

41
Q

Why might a beta2 agonist be given to a patient in preterm labor?

A

It causes uterine relaxation

42
Q

How does the SNS effect the eye?

A

Contracts radial muscle –> pupil dilationEye Ciliary –> increased secretion of aqueous humor

43
Q

What muscarinic receptor is agonized for the GI/GU and eyes?

A

M3

44
Q

What receptors are on the sweat glands?

A

Thermoregulatory-MuscarinicApocrine (stress)-Alpha

45
Q

What effect does the B3 receptor exhibit?

A

Lipolysis

46
Q

Why don’t we use ganglionic blocking drugs?

A

Blocks ALL autonomic output

47
Q

What is the chemical composition of Acetylcholine?

A

Quaternary ammonium that works on both Nn and Nm ach receptors

48
Q

Why aren’t other cholinergic agents able to be broken down by AchE?

A

Other cholinergic agents do not have an ester like Ach and cannot be broken down by AchE

49
Q

How does AchE break down Ach?

A

AchE hydrolyzes Ach

50
Q

What type of AchE inhibitor is Neostigmine?

A

Carbamate, it is reversible

51
Q

What type of AchE inhibitor is Edrophonium?

A

Alcohol, it is reversible

52
Q

What is the only type of irreversible AchE inhibitors?

A

Organophosphates

53
Q

What is the prototype muscarinic antagonist?

A

Atropine

54
Q

What were ganglionic blockers used for?

A

Hypertensive emergency

55
Q

Why don’t catecholamines cross the BBB?

A

They are Quaternary Amines, charged particles

56
Q

What adrenergic receptors does Epinephrine agonize?

A

A1 A2 B1 B2 B3

57
Q

Why do we used Epinephrine with local anesthetics?

A

It constricts the blood vessels and keeps the LA in the area for a longer period of time

58
Q

What adrenergic receptors does Norepinephrine agonize?

A

A1 A2 B1 (little effect on B2) more alpha effects

59
Q

What type of drug is isoproterenol?

A

Non-selective beta agonist (B1 & B2)

60
Q

What adrenergic receptor does Dobutamine agonize?

A

B1

61
Q

What adrenergic agent has the highest affinity for Alpha receptors?

A

Epinephrine > Norepinephrine > Isoproterenol

62
Q

What adrenergic agent has the highest affinity for Beta receptors?

A

Isoproterenol > Epinephrine > Norepinephrine

63
Q

What are some side effects of an Alpha1 specific antagonist?

A

Nasal congestionOrthostatic HoTNTachycardia

64
Q

Why isn’t there a Beta2 specific antagonist?

A

We do not want to cause bronchoconstriction

65
Q

What is the chemical structure of catecholamines?

A

Benzene ring with two HO

66
Q

What is the function of COMT?

A

An enzyme that deactivates the catecholamine dopa, dopamine, epinephrine and norepinephrine

67
Q

What is the function of MAO?

A

An enzyme that catalyzes the oxidation of amines

68
Q

What cholinergic antagonist treats profound bradycardia most effectively?

A

Atropine > Glycopyrolate > Scopolamine

69
Q

What are additional benefits of using anti-muscarinic agents?

A

Prevents salivationPost-op N/VSedation

70
Q

What is the only anti-muscarinic agent that doesn’t cross the BBB?

A

Glycopyrolate

71
Q

What is the concentration of Atropine?

A

0.4mg/mL

72
Q

What is the does of Atropine?

A

15-70mcg/kg

73
Q

What is the onset, peak and duration of Atropine?

A

Onset: 15-30sPeak: 2minDuration: 1-2hrs

74
Q

What is the concentration of Glycopyrolate?

A

0.2mg/mL

75
Q

What is the dose of Glycopyrolate?

A

10-20mgc/kg

76
Q

What is the onset, peak and duration of Glycopyrolate?

A

Onset: 1minPeak: 5minDuration: 2-4hrs

77
Q

What is the concentration of Edrophonium?

A

10mg/mL

78
Q

What is the dose of Edrophonium?

A

0.5-1mg/kg

79
Q

What is the onset, peak and duration of Edrophonium?

A

Onset:30-60 secsPeak: 1-5minDuration: 5-20min

80
Q

What is the concentration of neostigmine?

A

0.5-1mg/mL

81
Q

What is the dose of Neostigmine?

A

0.04-0.08mg/kg

82
Q

What is the onset peak and duration of Neostigmine?

A

Onset: 1-3minsPeak: 5-7minsDuration: 40-60mins

83
Q

What are the three types of indirect acting adrenergic agonists?

A

NT releaseRe-uptake inhibitorsMAOI

84
Q

What is the prototype beta2 agonist?

A

Albuterol

85
Q

What is the prototype alpha1 antagonist?

A

Prazosin

86
Q

What are the three mechanisms of neurotransmitter termination?

A

ReuptakeEnzyme degradationDiffusion

87
Q

How does the botulinum toxin affect neurotransmission?

A

Prevents the release of Ach from the vesicle

88
Q

What are the muscarinic receptor ligands?

A

AchMuscarine

89
Q

What are the nicotinic receptor ligands?

A

AchNicotineSucs

90
Q

What enzyme breaks down cGMP?

A

PDE5, phosphodiesterase 5

91
Q

What enzyme makes NO for L-arginine in the muscarinic receptor mediated vasodilation?

A

Nitric oxide synthase

92
Q

What types of drugs are indirect acting cholinergic agonists?

A

AchE inhibitors

93
Q

What mechanism causes vasoconstriction with alpha1 agonists?

A

Once agonized there is an increase in Ca causing calmodulin activation and increases actin myosin interaction