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

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

(121 cards)

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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
Pilocarpine - MOA
- Muscarinic receptor agonist
26
Pilocarpine - distinguishing characteristics
- Plant origin (Pilocarpus jabarundi) - Tertiary ammonium group - Preferential activity on sweat glands - Resistant to esterases
27
Pilocarpine - predictable characteristics
- 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
28
Cholinesterase inhibitors
- Neostigmine | - Malathione
29
Neostigmine - category
- Parasympathomimetic
30
Neostigmine - MOA
- Reversible cholinesterase inhibitor
31
Neostigmine - distinguishing characteristics
- Quaternary ammonium group - Contains ester group (slowly hydrolyzed: 1-2 hour 1/2 life) - Poorly absorbed following oral Rx
32
Neostigmine - predictable activities
- Elevates Ach levels - Causes both muscarinic and nicotinic stimulation - Numerous peripheral side effects - No CNS effects
33
Neostigmine - predictable uses
- Miosis and Rx glaucoma (local administration) - Rx myasthenia gravis - Antidote to some drugs (Atropine) - Atonic gut and bladder
34
Malathione - category
- Parasympathomimetic
35
Malathione - MOA
- Irreversible cholinesterase inhibitor
36
Malathione - distinguishing characteristics
- Tertiary ammonium group - Binds covalently to esterases - Not hydrolyzed by esterases - Rapidly absorbed through multiple routes
37
Malathione - predictable characteristics
- 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
38
Ways to inhibit the parasympathetic nervous system
- Antagonize the muscarinic receptors
39
Muscarinic receptor antagonists
- Atropine - Ipratropium - Scopolamine
40
Atropine - category
- Parasympatholytic
41
Atropine - MOA
- Muscarinic receptor antagonist
42
Atropine - distinguishing characteristic
- 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
43
Atropine - predictable activities
- 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
44
Ipratropium - trade name
- Atrovent
45
Ipratropium - category
- Parasympatholytic
46
Ipratropium - MOA
- Muscarinic antagonist
47
Ipratropium - distinguishing characteristics
- Quaternary ammonium group | - Minimal inhibition of mucociliary clearance
48
Ipratropium - predictable actions
- No CNS effects - Bronchodilation - Limited mucous accumulation
49
Scopolamine - category
- Parasympatholytic
50
Scopolamine - MOA
- Muscarinic receptor antagonist
51
Scopolamine - distinguishing characterisitcs
- From plant origin (Hyocyamus niger) | - Greater CNS distribution than atropine
52
Scopolamine - predictable actions
- Greater CNS side effects and abuse potential than atropine - Used less frequently than atropine - Used to treat motion sickness
53
Benchmark sympathetic responses
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
Ways to mimic the sympathetic nervous system
- Stimulate adrenergic receptors - Promote release of norepinephrine - Prevent elimination of norepinephrine
55
Sympathomimetics
- Epinephrine - Phenylephrine (Neosynephrine) - Clonidine (Catapres) - Isoproterenol (Isuprel) - Albuterol (Ventolin) - Amphetamine - Cocaine - Tyramine - Reserpine - Ephedrine - Pseudoephedrine - Methamphetamine - Phenelzine (Nardil)
56
Epinephrine - category
- Sympathomimetic
57
Epinephrine - MOA
- Stimulate alpha and beta receptors
58
Epinephrine - distinguishing characteristics
- Metabolized in gut, blood, and multiple tissues | - More beta and less alpha activity than norepinephrine
59
Epinephrine - predictable characteristics
- Ineffective orally | - Very short half life (minutes)
60
Epinephrine - predictable uses
- Cardiac emergencies - Bronchospasm - Adjunct to local anesthesia
61
Epinephrine - predictable side effects
- Tachycardia and increased force of contraction | - Blood pressure disturbance (usually hypertension)
62
Phenylephrine - trade name
- Neosynephrine
63
Phenylephrine - category
- Sympathomimetic
64
Phenylephrine - MOA
- Alpha 1 receptor agonist
65
Phenylephrine - distinguishing characteristics
- Effective orally | - Limited access to CNS
66
Phenylephrine - predictable uses
- Nasal decongestant | - Mydriatic
67
Phenylephrine - predictable side effects
- Rebound congestion - Increased peripheral resistance - Reflex bradycardia
68
Clonidine - trade name
- Catapres
69
Clonidine - category
- Sympathomimetic | - Dubious classification because it's a selective alpha 2 agonist
70
Clonidine - MOA
- Alpha 2 receptor agonist
71
Clonidine - distinguishing characteristics
- 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
Clonidine - predictable uses
- Antihypertensive | - ADHD
73
Clonidine - predictable side effects
- Dry mouth - Sedation - Sexual dysfunction
74
Isoproteronol - trade name
- Isuprel
75
Isoproteronol - category
- Sympathomimetic
76
Isoproteronol - MOA
- Beta receptor agonist (both 1 and 2)
77
Isoproteronol - distinguishing characteristics
- Metabolized by COMT - Short duration of action - Both beta 1 and beta 2
78
Isoproteronol - predictable actions
- Tachycardia - Bronchodilation - Replaced often by more selective beta agonists
79
Isoproteronol - predictable uses
- Cardiac arrest
80
Albuterol - trade name
- Ventolin
81
Albuterol - category
- Sympathomimetic
82
Albuterol - MOA
- Beta 2 receptor agonist
83
Albuterol - distinguishing characteristics
- Effective orally or by inhalation - Limited cardiovascular effects - Duration of action of several hours
84
Albuterol - predictable uses
- Bronchodilator
85
Albuterol - predictable side effects
- Weak and occasional tachycardia | - Vasodilation
86
Amphetamine - category
- Sympathomimetic
87
Amphetamine - MOA
- Stimulate release of norepinephrine and dopamine
88
Amphetamine - distinguishing characteristics
- Enters CNS | - Inhibits MAO
89
Amphetamine - predictable actions
``` - 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
Additional substances that increase norepinephrine release
- Cocaine - Tyramine - Reserpine - Ephedrine - Pseudoephedrine - Methamphetamine
91
Phenelzine - trade name
- Nardil
92
Phenelzine - category
- Sympathomimetic
93
Phenelzine - MOA
- Monoamine oxidase inhibitor
94
Phenelzine - distinguishing characteristics
- Readily absorbed - Crosses blood-brain barrier - Increases synaptic catecholamine levels
95
Phenelzine - predictable uses
- Antidepressant
96
Phenelzine - predictable side effects
- Sympathomimetic actions
97
Ways to inhibit the sympathetic nervous system
- Block the adrenergic receptors | - Deplete the stores of norepinephrine
98
Sympatholytics
- Prazocin (Minipress) - Propranolol (Inderal) - Metoprolol (Lopressor) - Reserpine
99
Prazocin - trade name
- Minipress
100
Prazocin - category
- Sympatholytic
101
Prazocin - MOA
- Alpha 1 receptor antagonist
102
Prazocin - distinguishing characteristics
- Effective orally | - Highly protein bound (5% free)
103
Prazocin - predictable uses
- Hypertension
104
Prazocin - predictable side effects
- Hypotension - Syncope - Reflex tachycardia
105
Propranolol - trade name
- Inderal
106
Propranolol - category
- Sympatholytic
107
Propranolol - MOA
- Beta 1 and 2 receptor antagonist
108
Propranolol - distinguishing characteristics
- Very lipid soluble - Significant 1st pass metabolism - Highly variable plasma levels
109
Propranolol - uses
- Antihypertensive - Antiangina - Antiarrhythmic
110
Propranolol - side effects
- Plasma asthma patients at risk | - Place diabetics at risk
111
Metoprolol - trade name
- Lopressor
112
Metoprolol - category
- Sympatholytic
113
Metoprolol - MOA
- Beta 1 receptor antagonist
114
Metoprolol - distinguishing characteristics
- Similar to propranolol - Very lipid soluble - Significant 1st pass metabolism - Highly variable plasma levels
115
Metoprolol - uses
- Antihypertensive (without risk to asthmatics and diabetics)
116
Metoprolol - similar drugs
- Atenolol (Tenormin) | - Others that are less commonly prescribed
117
Reserpine - category
- Sympatholytic
118
Reserpine - MOA
- Promotes release of norepinephrine and reduces reuptake, resulting in depletion of norepinephrine stores
119
Reserpine - distinguishing characteristics
- Derived from plant origin - Transitory sympathomimetic followed by prolonged sympatholytic effect - Antiquated for therapeutic use - Extensive research use
120
Reserpine - predictable use
- Antihypertensive
121
Reserpine - predictable side effects
- Prolonged paralysis of sympathetic nervous system

Pharmacology I (4 decks)

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