Pharmacology of the Autonomic Nervous System (Jensen's video lecture) Flashcards

1
Q

Parasympathomimetics

A
  • Mimic the parasympathetic nervous system
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2
Q

Parasympatholytics

A
  • Inhibit the parasympathetic nervous system
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3
Q

Sympathomimetics

A
  • Mimic the sympathetic nervous system
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4
Q

Sympatholytics

A
  • Inhibit the sympathetic nervous system
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5
Q

Parasympathetic overview

A
  • Originate from cranial and sacral regions
  • Contain long preganglionic neurons
    > Cholinergic
  • Contain short postganglionic neurons
    > Cholinergic
  • Innervate visceral organs
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6
Q

Parasympathetic neurotransmitters and receptors

A
  • Release acetylcholine
  • Stimulate muscarinic receptors
  • Metabolized by cholinesterase
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7
Q

Sympathetic overview

A
  • Originate from thoracic and lumbar regions
  • Contain short (1-2cm) preganglionic neurons
    > Cholinergic
  • Contain long postganglionic neurons
    > Adrenergic
  • Innervate visceral organs
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8
Q

Sympathetic neurotransmitters and receptors

A
  • Release norepinephrine
  • Stimulate alpha and beta receptors
  • Metabolized by MAO (monoamine oxidase) and COMT (catechol-0-methyltransferase)
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9
Q

Benchmark parasympathetic responses

A
  • Miosis
  • Vasodilation
  • Negative inotropic and negative chronotropic responses
  • Bronchoconstriction
  • SLUD (salivation, lacrimation, urination, diarrhea)
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10
Q

Ways to mimic the parasympathetic nervous system

A
  • Stimulate muscarinic receptors

- Prevent the breakdown of Acetylcholine

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11
Q

Muscarinic receptor agonists

A
  • Acetylcholine
  • Bethanechol (Urecholine)
  • Pilocarpine
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12
Q

Acetylcholine - category

A
  • Parasympathomimetic
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13
Q

Acetylcholine - MOA

A
  • Muscarinic agonist

- Nicotinic agonist

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14
Q

Acetylcholine - distinguishing characteristics

A
  • Rapidly hydrolyzed by esterases
  • Acts on both muscarinic and nicotinic receptors
  • Quaternary ammonium group
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15
Q

Acetylcholine - predictable characterisitics

A
  • Short half life (seconds)
  • Diffuse activity
  • Limited distribution
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16
Q

Acetylcholine - predictable uses

A
  • Possible local ophthalmic use
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17
Q

Bethanechol - trade name

A
  • Urecholine
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18
Q

Bethanechol - category

A
  • Parasympathomimetic
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19
Q

Bethanechol - MOA

A
  • Muscarinic agonist
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20
Q

Bethanechol - distinguishing characteristics

A
  • Not metabolized by esterases
  • Quaternary ammonium group
  • Particular affinity for gut and bladder smooth muscle
  • Oral route preferred
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21
Q

Bethanechol - predictable characteristics

A
  • No CNS effects

- Longer 1/2 life allows distribution to areas of low blood flow

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22
Q

Bethanechol - predictable uses

A
  • Gastroparesis (postoperative)
  • Urinary retention
  • Xerostomia
  • Ocular diagnostics
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23
Q

Bethanechol - predictable side effects

A
  • Other parasympathomimetic effects, especially following parenteral Rx
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24
Q

Pilocarpine - category

A
  • Parasympathomimetic
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25
Q

Pilocarpine - MOA

A
  • Muscarinic receptor agonist
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26
Q

Pilocarpine - distinguishing characteristics

A
  • Plant origin (Pilocarpus jabarundi)
  • Tertiary ammonium group
  • Preferential activity on sweat glands
  • Resistant to esterases
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27
Q

Pilocarpine - predictable characteristics

A
  • Used as miotic and in treatment of glaucoma
  • Will cause accommodation
  • Used to treat xerostomia
  • May cause CNS effects at high plasma levels
  • Diaphoresis is common side effect
  • Duration of action up to 8 hours
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28
Q

Cholinesterase inhibitors

A
  • Neostigmine

- Malathione

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29
Q

Neostigmine - category

A
  • Parasympathomimetic
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30
Q

Neostigmine - MOA

A
  • Reversible cholinesterase inhibitor
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31
Q

Neostigmine - distinguishing characteristics

A
  • Quaternary ammonium group
  • Contains ester group (slowly hydrolyzed: 1-2 hour 1/2 life)
  • Poorly absorbed following oral Rx
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32
Q

Neostigmine - predictable activities

A
  • Elevates Ach levels
  • Causes both muscarinic and nicotinic stimulation
  • Numerous peripheral side effects
  • No CNS effects
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33
Q

Neostigmine - predictable uses

A
  • Miosis and Rx glaucoma (local administration)
  • Rx myasthenia gravis
  • Antidote to some drugs (Atropine)
  • Atonic gut and bladder
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34
Q

Malathione - category

A
  • Parasympathomimetic
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35
Q

Malathione - MOA

A
  • Irreversible cholinesterase inhibitor
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36
Q

Malathione - distinguishing characteristics

A
  • Tertiary ammonium group
  • Binds covalently to esterases
  • Not hydrolyzed by esterases
  • Rapidly absorbed through multiple routes
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37
Q

Malathione - predictable characteristics

A
  • Causes SLUD and other ANS activities
  • Causes CNS disturbances
  • No therapeutic use
  • Used as insecticide
  • Similar agents used as chemical weapons
  • Atropine is the antidote, plus supportive therapy
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38
Q

Ways to inhibit the parasympathetic nervous system

A
  • Antagonize the muscarinic receptors
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39
Q

Muscarinic receptor antagonists

A
  • Atropine
  • Ipratropium
  • Scopolamine
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40
Q

Atropine - category

A
  • Parasympatholytic
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41
Q

Atropine - MOA

A
  • Muscarinic receptor antagonist
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42
Q

Atropine - distinguishing characteristic

A
  • From plant origin (Atropa belladonna)
  • Tertiary ammonium group
  • Ester group required for activity
  • Resistant to hydrolysis by esterases
  • Metabolized in liver with a 1/2 life of about 4 hours
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43
Q

Atropine - predictable activities

A
  • CNS toxicity, especially in children, even after ophthalmic Rx
  • Inhibit SLUD and other parasympathetic activities
  • Used in ophthalmology - mydriasis and cycloplegia
  • Used as antidote to parasympathomimetics
  • Used to treat diarrhea
  • Once used to treat asthma
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44
Q

Ipratropium - trade name

A
  • Atrovent
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45
Q

Ipratropium - category

A
  • Parasympatholytic
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46
Q

Ipratropium - MOA

A
  • Muscarinic antagonist
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47
Q

Ipratropium - distinguishing characteristics

A
  • Quaternary ammonium group

- Minimal inhibition of mucociliary clearance

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48
Q

Ipratropium - predictable actions

A
  • No CNS effects
  • Bronchodilation
  • Limited mucous accumulation
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49
Q

Scopolamine - category

A
  • Parasympatholytic
50
Q

Scopolamine - MOA

A
  • Muscarinic receptor antagonist
51
Q

Scopolamine - distinguishing characterisitcs

A
  • From plant origin (Hyocyamus niger)

- Greater CNS distribution than atropine

52
Q

Scopolamine - predictable actions

A
  • Greater CNS side effects and abuse potential than atropine
  • Used less frequently than atropine
  • Used to treat motion sickness
53
Q

Benchmark sympathetic responses

A

Beta 1
- Positive inotropic and positive chronotropic responses

Beta 2

  • Bronchodilation
  • Relaxation of mymetrium
  • Insulin release

Alpha 1

  • Vasoconstriction
  • Mydriasis

Alpha 2
- Norepinephrine release

54
Q

Ways to mimic the sympathetic nervous system

A
  • Stimulate adrenergic receptors
  • Promote release of norepinephrine
  • Prevent elimination of norepinephrine
55
Q

Sympathomimetics

A
  • Epinephrine
  • Phenylephrine (Neosynephrine)
  • Clonidine (Catapres)
  • Isoproterenol (Isuprel)
  • Albuterol (Ventolin)
  • Amphetamine
  • Cocaine
  • Tyramine
  • Reserpine
  • Ephedrine
  • Pseudoephedrine
  • Methamphetamine
  • Phenelzine (Nardil)
56
Q

Epinephrine - category

A
  • Sympathomimetic
57
Q

Epinephrine - MOA

A
  • Stimulate alpha and beta receptors
58
Q

Epinephrine - distinguishing characteristics

A
  • Metabolized in gut, blood, and multiple tissues

- More beta and less alpha activity than norepinephrine

59
Q

Epinephrine - predictable characteristics

A
  • Ineffective orally

- Very short half life (minutes)

60
Q

Epinephrine - predictable uses

A
  • Cardiac emergencies
  • Bronchospasm
  • Adjunct to local anesthesia
61
Q

Epinephrine - predictable side effects

A
  • Tachycardia and increased force of contraction

- Blood pressure disturbance (usually hypertension)

62
Q

Phenylephrine - trade name

A
  • Neosynephrine
63
Q

Phenylephrine - category

A
  • Sympathomimetic
64
Q

Phenylephrine - MOA

A
  • Alpha 1 receptor agonist
65
Q

Phenylephrine - distinguishing characteristics

A
  • Effective orally

- Limited access to CNS

66
Q

Phenylephrine - predictable uses

A
  • Nasal decongestant

- Mydriatic

67
Q

Phenylephrine - predictable side effects

A
  • Rebound congestion
  • Increased peripheral resistance
  • Reflex bradycardia
68
Q

Clonidine - trade name

A
  • Catapres
69
Q

Clonidine - category

A
  • Sympathomimetic

- Dubious classification because it’s a selective alpha 2 agonist

70
Q

Clonidine - MOA

A
  • Alpha 2 receptor agonist
71
Q

Clonidine - distinguishing characteristics

A
  • Effective orally
  • Crosses blood-brain barrier
  • Prefers alpha receptors in brainstem
  • Long half-life
  • Long duration of action
  • Diminish discharge from medular vasomotor center
72
Q

Clonidine - predictable uses

A
  • Antihypertensive

- ADHD

73
Q

Clonidine - predictable side effects

A
  • Dry mouth
  • Sedation
  • Sexual dysfunction
74
Q

Isoproteronol - trade name

A
  • Isuprel
75
Q

Isoproteronol - category

A
  • Sympathomimetic
76
Q

Isoproteronol - MOA

A
  • Beta receptor agonist (both 1 and 2)
77
Q

Isoproteronol - distinguishing characteristics

A
  • Metabolized by COMT
  • Short duration of action
  • Both beta 1 and beta 2
78
Q

Isoproteronol - predictable actions

A
  • Tachycardia
  • Bronchodilation
  • Replaced often by more selective beta agonists
79
Q

Isoproteronol - predictable uses

A
  • Cardiac arrest
80
Q

Albuterol - trade name

A
  • Ventolin
81
Q

Albuterol - category

A
  • Sympathomimetic
82
Q

Albuterol - MOA

A
  • Beta 2 receptor agonist
83
Q

Albuterol - distinguishing characteristics

A
  • Effective orally or by inhalation
  • Limited cardiovascular effects
  • Duration of action of several hours
84
Q

Albuterol - predictable uses

A
  • Bronchodilator
85
Q

Albuterol - predictable side effects

A
  • Weak and occasional tachycardia

- Vasodilation

86
Q

Amphetamine - category

A
  • Sympathomimetic
87
Q

Amphetamine - MOA

A
  • Stimulate release of norepinephrine and dopamine
88
Q

Amphetamine - distinguishing characteristics

A
  • Enters CNS

- Inhibits MAO

89
Q

Amphetamine - predictable actions

A
- Alpha and beta stimulation by norepinephrine
     > Vasoconstriction
     > Cardiac stimulation
     > Increased blood pressure
     > Mydriasis
- CNS stimulation
     > Euphoria
     > Insomnia
     > Anxiety
     > Loss of appetite
     > Hyperthermia
- Used to treat narcolepsy, obesity, and ADHD
- High abuse potential makes it a scheduled substance
90
Q

Additional substances that increase norepinephrine release

A
  • Cocaine
  • Tyramine
  • Reserpine
  • Ephedrine
  • Pseudoephedrine
  • Methamphetamine
91
Q

Phenelzine - trade name

A
  • Nardil
92
Q

Phenelzine - category

A
  • Sympathomimetic
93
Q

Phenelzine - MOA

A
  • Monoamine oxidase inhibitor
94
Q

Phenelzine - distinguishing characteristics

A
  • Readily absorbed
  • Crosses blood-brain barrier
  • Increases synaptic catecholamine levels
95
Q

Phenelzine - predictable uses

A
  • Antidepressant
96
Q

Phenelzine - predictable side effects

A
  • Sympathomimetic actions
97
Q

Ways to inhibit the sympathetic nervous system

A
  • Block the adrenergic receptors

- Deplete the stores of norepinephrine

98
Q

Sympatholytics

A
  • Prazocin (Minipress)
  • Propranolol (Inderal)
  • Metoprolol (Lopressor)
  • Reserpine
99
Q

Prazocin - trade name

A
  • Minipress
100
Q

Prazocin - category

A
  • Sympatholytic
101
Q

Prazocin - MOA

A
  • Alpha 1 receptor antagonist
102
Q

Prazocin - distinguishing characteristics

A
  • Effective orally

- Highly protein bound (5% free)

103
Q

Prazocin - predictable uses

A
  • Hypertension
104
Q

Prazocin - predictable side effects

A
  • Hypotension
  • Syncope
  • Reflex tachycardia
105
Q

Propranolol - trade name

A
  • Inderal
106
Q

Propranolol - category

A
  • Sympatholytic
107
Q

Propranolol - MOA

A
  • Beta 1 and 2 receptor antagonist
108
Q

Propranolol - distinguishing characteristics

A
  • Very lipid soluble
  • Significant 1st pass metabolism
  • Highly variable plasma levels
109
Q

Propranolol - uses

A
  • Antihypertensive
  • Antiangina
  • Antiarrhythmic
110
Q

Propranolol - side effects

A
  • Plasma asthma patients at risk

- Place diabetics at risk

111
Q

Metoprolol - trade name

A
  • Lopressor
112
Q

Metoprolol - category

A
  • Sympatholytic
113
Q

Metoprolol - MOA

A
  • Beta 1 receptor antagonist
114
Q

Metoprolol - distinguishing characteristics

A
  • Similar to propranolol
  • Very lipid soluble
  • Significant 1st pass metabolism
  • Highly variable plasma levels
115
Q

Metoprolol - uses

A
  • Antihypertensive (without risk to asthmatics and diabetics)
116
Q

Metoprolol - similar drugs

A
  • Atenolol (Tenormin)

- Others that are less commonly prescribed

117
Q

Reserpine - category

A
  • Sympatholytic
118
Q

Reserpine - MOA

A
  • Promotes release of norepinephrine and reduces reuptake, resulting in depletion of norepinephrine stores
119
Q

Reserpine - distinguishing characteristics

A
  • Derived from plant origin
  • Transitory sympathomimetic followed by prolonged sympatholytic effect
  • Antiquated for therapeutic use
  • Extensive research use
120
Q

Reserpine - predictable use

A
  • Antihypertensive
121
Q

Reserpine - predictable side effects

A
  • Prolonged paralysis of sympathetic nervous system