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PHAR 341 - Pharmacology > Cholinergic Pharmacology > Flashcards

Cholinergic Pharmacology Flashcards

1
Q

Effect of a direct-acting Cholinergic agonist in the CNS

A
  • doesn’t cross the blood brain barrier
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2
Q

Effect of a direct-acting Cholinergic Agonist on the Cardiovascular system

A
  • vasodilation

- decrease intropy and chronotropy

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3
Q

Effects of a direct-acting Cholinergic Agonist on the Respiratory System

A
  • bronchoconstriction

- increased secretion

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4
Q

Effects of direct-acting Cholinergic Agonist on the GI System

A
  • increased motility and secretion
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5
Q

Effects of direct-acting Cholinergic Agonists on the Urinary system

A
  • potential increase in voiding pressure
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6
Q

Effects of direct-acting Cholinergic Agonist on the Glands

A
  • sweating

- salivation

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7
Q

Carbachol (drug type)

A
  • activates both nicotinic and muscarinic receptors
  • ACh analogue that is resistant to cholinesterases - have a longer half life
  • direct-acting cholinergic drug
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8
Q

Carbachol uses

A
  • open angle glaucoma
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9
Q

Muscarinic Receptor Selective Direct Acting Cholergic Agonist

A
  • Bethanechol
  • Pilocarpine
  • Cevimeline
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10
Q

Bethanechol Pharmacology

A
  • resistant to cholineresterases -> longer action
  • acts predominantly at muscarinic receptors
  • primarily affects GI and urinary tracts (orally)
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11
Q

Bethanechol Uses

A
  • urinary retention

- gastroesophageal Reflux

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12
Q

Pilocarpine Pharmacology

A
  • naturally occuring alkaloid
  • longer acting than ACh
  • predominantly muscarinic action
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13
Q

Pilocarpine Uses

A
  • open angle glaucoma

- Xerostomia (dry mouth)

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14
Q

Muscarinic Receptor Subtypes

A

M1, M2, M3, M4, M5

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15
Q

Stimulatory Muscarinic Receptor Subtypes

A
  • M1, M3, M5

- post-synaptic

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16
Q

Inhibitory Muscarinic Receptor Subtypes

A
  • M2, M4

- pre-synaptic

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17
Q

M1 is located in:

A
  • Parasympathetic ganglia
  • Salivary Gland
  • Stomach
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18
Q

Activation of M1 in the Parasympathetic ganglia causes:

A
  • increased parasympathetic tone
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19
Q

Activation of M1 in the Salivary gland causes:

A
  • increased saliva
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20
Q

Activation of M1 in the Stomach causes:

A
  • acid release
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21
Q

M2 is located in:

A
  • Heart
  • GI smooth muscle
  • Bladder smooth muscle
  • CNS
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22
Q

Activation of M2 in the heart causes:

A
  • decrease heart rate

- decrease force of contraction

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23
Q

Activation of M2 in the GI smooth muscle causes:

A
  • opposes sympathetically-mediated relaxation
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24
Q

Activation of M2 in the Bladder smooth muscle causes:

A
  • opposes sympathetically- mediated relaxation
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25
Activation of M2 in the CNS causes:
- analgesia - maybe
26
M3 is located in:
- Bladder Smooth muscle - Airway smooth muscle - GI smooth muscle - Eye - Glands - Blood vessels
27
Activation of M3 in the Bladder smooth muscle causes:
- contraction of the bladder for micturation
28
Activation of M3 in the Airway smooth muscle causes:
- bronchoconstriction
29
Activation of M3 in the GI smooth muscle causes:
- contraction
30
Activation of M3 in the Eye causes:
- constriction of pupil - contraction of ciliary muscle - contraction of trabecular meshwork
31
Activation of M3 in the Glands causes:
- salivation
32
Activation of M3 in the Blood Vessels causes:
- dilation (through the endothelium release of NO)
33
M4 is located in:
- prejunctional nerve endings | - CNS
34
Activation of M4 in the prejunctional nerve endings caues:
- inhibition of ANS transmittion
35
Activation of M4 in the CNS causes:
- Schizoprenia or Analgesia - maybe?
36
M5 is found in:
CNS
37
Activation of M5 in the CNS causes:
- facilitates dopamine releases | - regulates cerebral vascular tone by causing vascular dilation
38
Cevimeline Pharmacology
- activates M1 and M3 receptors - prevalent in salivary glands - 40 fold relative affinity for M3 than M2 for the cardiac receptor compared to pilocarpine
39
Cevimeline Uses
- Sjorgen's Syndrome
40
Nicotine Pharmacology
- natural alkaloid - activates both neuronal (ganglion and CNS) and skeletal muscle nicotinic receptors - greater affinity for neuronal receptors - activates both parasympathetic and sympathetic ganglian
41
Nicotine Effects on the CNS
- marked stimulation - realses glutamate, dopamine etc.. - high doses cause tremor and can lead to convulsions - stimulates the chemoreceptors trigger zone (nausea)
42
Nicotine effects on the Cardiovascular System
- hypertension - tachycardia (stimulates sympathetic ganglion)
43
Nicotien effects on the Respiratory System
- bronchoconstriction | - increased secretions
44
Nicotine effects on the GI system:
- Nausea - Vomitting - increased bowel motility (diarrhea)
45
Nicotine effects on the Urinary System
- potential increase in voiding pressure (usually not observed)
46
Nicotine effects on the Glands:
- initial salivary and bronchial secretion | - then inhibition
47
Nicotine effects on the Peripheral Nervous System
- transient stimulation followed by a more prolonged desensitization of the autonomic ganglia and skeletal muscles
48
Nicotine Uses
- smoking cessation
49
Nicotinic Receptor Agonists
- nicotine | - Varenicline
50
Varenicline Pharmacology
- partial agnosit/antagonist highly selective for alpha4beta2 nicotinic ACh receptor - inhibits nicotine-induced dopaminergic reward pathway activation - decreases the reinforming effect of smoking bymaking it less rewarding
51
Varenicline Uses
- smoking cessation
52
Varenicline Adverse Effects
- mild to moderate nausea reported - insomnia and abnormal dreams - neuropsychiatric adverse events
53
Indirect-Acting Cholinergic Agonists MOA:
- cholinesterase inhibitors which block the break down of ACh at 1. Neuromuscular synapse 2. Autonomic ganglion synapses 3. parasympathetic effector synapses
54
Edrophonium Pharmacology
- reverses paralysis of non-depolarizing neuromuscluar blockers - Cholinesterase inhibitor (aka indirect-acting cholinergic agonist)
55
Edrophonium Uses
- myasthenia gravis diagnostic event
56
Neostigmine Pharmacology
- cholinesterase inhibitor (aka indirect-acting cholinergic agonist)
57
Neostigmine Uses
- postoperative ileus | - postoperative urinary retention
58
Pyridastigmine Pharmacology
- cholinesterase inhibitor (aka indirect-acting cholinergic agonist)
59
Pyridastigmine Uses
- myasthenia gravis (DOC)
60
Indirect-acting cholinergic agonists that do not cross the blood brain barrier
- edrophonium - neostigmine - pyridostigmine
61
Indirect-acting cholinergic agonists that cross the blood brain barrier
- donepezil - rivastigmine - galantamine
62
Donepezil Pharmacology
- selective Acetylcholinesterase | - non-competitive
63
Rivastigmine Pharmacology
- Acetylcholinesterase and butyrylcholinesterase | - non-competitive
64
Galantamine Pharmacology
- Acetycholinesterase and butyrylcholinesterase - competative - nicotinic receptor modulation
65
Toxicity of Cholinergic agonist drugs in the CNS
- anxiety - headache - tremors - confusion - coma
66
Toxicity of Cholinergic agonist drugs in the eye
- lacrimation - miosis - blurred vision
67
Toxicity of Cholinergic agonist drugs on the cardiovascular system
- Bradycardia | - hyper or hypo tension
68
Toxicity of Cholinergic agonist drugs on the respiratory system
- bronchial constrictions | - increased secretions
69
Toxicity of Cholinergic agonist drugs on the GIT
- nausea - vomitting - diarrhea - abominal cramps
70
Toxicity of Cholinergic agonist drugs on the Bladder
- increased uriniary urgency | - involunatry micturation
71
Toxicity of Cholinergic agonist drugs on the glands
- increased salivation | - increased sweating
72
Toxicity of Cholinergic agonist drugs on the skeletal muscles
- inital spasms leading to muscle weakness and respiratory paralysis
73
Diarrhea cause
- parasympathetic | - muscarinic
74
Urination cause:
- parasympathetic | - muscarinic
75
Miosis cause:
- parasympathetic | - muscarinic
76
Muscles weakness cause:
- not para or sympathetic | - nicotinic
77
Bronchospasm cause:
- parasympathetic | - muscarinic
78
Excitation cause:
- not para or sympathetic | - nicotinic
79
Lacrimation cause:
- parasympathetic | - muscarinic
80
Seizures cause:
- not para or sympathetic | - nicotinic
81
Sweating cause:
- sympathetic | - muscarinic
82
Salivation cause:
- Both para and sympathetic | - muscarinic and andegeric
83
Pralidoxime Pharmacology
- cleaves the dialkylphosphate group from the active site of acetylcholinesterase - reactivation of the enzyme - only works acutely - onset within 1 hour
84
Atropine Pharmacology
- competitive antagonist at all muscarinic receptor subtypes
85
Atropine Effects on the CNS
- slight drowsiness | - hallucinations
86
Atropine Effects on Cardiovascular
- increased heart rate | - faster conduction
87
Atropine Effects on Respiratory
- bronchodilation | - decreased secretions
88
Atropine Effects on GI
- decreased motility | - decreased secretion
89
Atropine Effects on Urinary
- urinary rentention
90
Atropine Effects on Glands
- decreased salivation | - decreased sweating (hyperthermia)
91
Atropine Effects on Ocular
- mydriasis - blurred vision - paralysis of accommodation
92
Atropine Uses
- acute myocardial infarction/cardiopulmonary resuscitation - treatment of pesticide over dose - preoperative - eye exams
93
Atropine used to treat acute MI/cardiopulmonary resuscitation
- reverses sustained bradycardia - reduces ventricular arrythmias (PVCs) - treats nausea from administering morphine (common for pain with MI)
94
Atropine use to treat pesticide overdose
- counteracts the effect of increased ACh at muscarinic receptors - given with Pralidoxime
95
Atropine used preoperatively
- given before surgery | - counteracts general anesthesia-induced bradycardia, salivation and increased brochial secretions
96
Atropine used for eye exams
- produced mydriasis (pupil dilation) - cycloplegia (inability to accommodate) - very long duration (up to 10 days)
97
Anti-musarinic drugs - natural alkaloids
- Atropine | - Scopolamine
98
Scopolamine Pharmacology
- competitive antagonist at all muscarinic receptors
99
Scopolamine Adverse Effects
- drowsiness and fatigue b/c it penetrates the blood brain barrier
100
Scopolamine Uses
- motion sickness
101
Scopolamine for treatment of Motion Sickness
- decreases salivary secretions - decreases GI motility - acts on CNS to decrease nausea
102
Ipratroprium and Tiotropium Pharmacology
- given as inhaler or nebulizer | - very low systemic side effects b/c little drug is absorbed
103
Ipratroprium and Tiotropium Uses
- topical bronchodilator for adjunctive treatment of asthma
104
Benzotropine Uses
- treatment of functional tremor in young patients with parkinson's disease - reduces drooling associated with Parkinson's
105
Anti-muscarinic - synthetic/semisynthetic non-selective drugs
- Ipratroprium - Tiotropium - Benzotropine
106
Muscarinic Selective Receptor Subtype drugs
- Pirenzapine - Oxybutnin - Darifenacin
107
Pirenzapine Pharmacology
- relatively selective M1 receptor antagonist - low incidence of dry mouth - decreases gastric acid secretion
108
Pirenzapine uses
- once used for peptic ulcers
109
Oxybutnin Pharmacology
- 10x greater selectivity for M1 and M3 receptors than M2 - decreases frequency of detrusor (bladder) muscle contractions - delays desire to void
110
Oxybutnin Uses
- urinary incontinence due to detrusor muscle hyperractivity
111
Oxybutnin Adverse Effects
- dry mouth, drowsiness, constipation, and blurred vision during discontinuation of therapy
112
Darifenacin Pharmacology
- M3 selective antagonist | - inhibits bladder muscle tone at doses that do not effect salvation
113
Treatment for Overactive Bladder
- Oxybutnin - Darifenacin - Botulinum neurotoxin
114
Effects of ganglion blockade on CNS
- if the drug crosses the BBB it alters cognitive processing
115
Effects of ganglion blockade on the Eye
- Pupil dilation | - failure to accommodate
116
Effects of ganglion blockade on the CVS
- decrease in blood pressure | - orthostatic hypotension due to blockade of normal sympathetic relexes
117
Effects of ganglion blockade on Arterioles
- vasodilation | - increased peripheral flow -> hypotension
118
Effects of ganglion blockade on Veins
- dilation - pooling of blood - decreased venous return
119
Effects of ganglion blockade on Heart
- tachycardia
120
Effects of ganglion blockade on the GIT
- reduced tone and motility | - constipation
121
Effects of ganglion blockade on the Urinary bladder
- urinary retention
122
Effects of ganglion blockade on the salivary glands
- dry mouth
123
Effects of ganglion bloackade on sweat glands
- dry, hot skin
124
Normal tone of the Eye
- Parasympathetic
125
Normal tone of the Arterioles
- Sympathetic
126
Normal tone of the Veins
- Sympathetic
127
Normal tone of the Heart
- Parasympathetic
128
Normal tone of the GIT
- Parasympathetic
129
Normal tone of the Urinary bladder
- Parasympathetic
130
Normal tone of the Salivary Glands
- Parasympathetic
131
Normal tone of the Sweat Glands
- Sympathetic
132
Competitive ganglion blockers
- Trimethaphan | - Tubocurarine
133
Trimethaphan Pharmacology
- competitive antagonist at the neuronal nicotinic (NN) ACh receptor subtype - prevents depolarization of the parasympathetic effector neuron by ACh - direct peripheral vasodilator action
134
Tubocurarine Pharmacology
- not very selective - also blocks the NM (muscle nicotinic) receptor - relaxes skeletal muscles
135
Non-competitive ganglion blockers
- Mecamylamine | - Hemicholinium
136
Mecamylamine Pharmacology
- open channel block of nicotinic receptor | - can cross the BBB
137
Hemicholinium Pharmacology
- open channel block of the nicotinic receptor - blocks the uptake of choline into the presynaptic terminal - causes decrease synthesis of ACh - decrease efficacy of synaptic transmission in the ganglion
138
Trimethaphan Uses
- hypertension emergencies (sudden increase in BP) - malignant hypertension - postoperative hypertension - competative
139
Mecamylamine Uses
- essential hypertension | - non-competative
140
Ganglion Blockers Adverse Effects in CVS
- orthostatic hypotension (blocks baroreceptor reflex)
141
Ganglion Blockers Adverse Effects in the Eyes
- blurred vision | - dilated pupils
142
Ganglion Blockers Adverse Effects in the GIT
- constipation, vomiting, nausea, anorexia, dry mouth
143
Ganglion Blockers Adverse Effects in the Urinary tract
- uriniary retention | - sexual dysfunction

PHAR 341 - Pharmacology (7 decks)

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