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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
Q

Activation of M2 in the CNS causes:

A
  • analgesia - maybe
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26
Q

M3 is located in:

A
  • Bladder Smooth muscle
  • Airway smooth muscle
  • GI smooth muscle
  • Eye
  • Glands
  • Blood vessels
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27
Q

Activation of M3 in the Bladder smooth muscle causes:

A
  • contraction of the bladder for micturation
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28
Q

Activation of M3 in the Airway smooth muscle causes:

A
  • bronchoconstriction
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29
Q

Activation of M3 in the GI smooth muscle causes:

A
  • contraction
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30
Q

Activation of M3 in the Eye causes:

A
  • constriction of pupil
  • contraction of ciliary muscle
  • contraction of trabecular meshwork
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31
Q

Activation of M3 in the Glands causes:

A
  • salivation
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32
Q

Activation of M3 in the Blood Vessels causes:

A
  • dilation (through the endothelium release of NO)
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33
Q

M4 is located in:

A
  • prejunctional nerve endings

- CNS

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34
Q

Activation of M4 in the prejunctional nerve endings caues:

A
  • inhibition of ANS transmittion
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35
Q

Activation of M4 in the CNS causes:

A
  • Schizoprenia or Analgesia - maybe?
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36
Q

M5 is found in:

A

CNS

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37
Q

Activation of M5 in the CNS causes:

A
  • facilitates dopamine releases

- regulates cerebral vascular tone by causing vascular dilation

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38
Q

Cevimeline Pharmacology

A
  • activates M1 and M3 receptors - prevalent in salivary glands
  • 40 fold relative affinity for M3 than M2 for the cardiac receptor compared to pilocarpine
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39
Q

Cevimeline Uses

A
  • Sjorgen’s Syndrome
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40
Q

Nicotine Pharmacology

A
  • natural alkaloid
  • activates both neuronal (ganglion and CNS) and skeletal muscle nicotinic receptors - greater affinity for neuronal receptors
  • activates both parasympathetic and sympathetic ganglian
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41
Q

Nicotine Effects on the CNS

A
  • marked stimulation - realses glutamate, dopamine etc..
  • high doses cause tremor and can lead to convulsions
  • stimulates the chemoreceptors trigger zone (nausea)
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42
Q

Nicotine effects on the Cardiovascular System

A
  • hypertension
  • tachycardia
    (stimulates sympathetic ganglion)
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43
Q

Nicotien effects on the Respiratory System

A
  • bronchoconstriction

- increased secretions

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44
Q

Nicotine effects on the GI system:

A
  • Nausea
  • Vomitting
  • increased bowel motility (diarrhea)
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45
Q

Nicotine effects on the Urinary System

A
  • potential increase in voiding pressure (usually not observed)
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46
Q

Nicotine effects on the Glands:

A
  • initial salivary and bronchial secretion

- then inhibition

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47
Q

Nicotine effects on the Peripheral Nervous System

A
  • transient stimulation followed by a more prolonged desensitization of the autonomic ganglia and skeletal muscles
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48
Q

Nicotine Uses

A
  • smoking cessation
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49
Q

Nicotinic Receptor Agonists

A
  • nicotine

- Varenicline

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50
Q

Varenicline Pharmacology

A
  • 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
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51
Q

Varenicline Uses

A
  • smoking cessation
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52
Q

Varenicline Adverse Effects

A
  • mild to moderate nausea reported
  • insomnia and abnormal dreams
  • neuropsychiatric adverse events
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53
Q

Indirect-Acting Cholinergic Agonists MOA:

A
  • cholinesterase inhibitors which block the break down of ACh at
    1. Neuromuscular synapse
    2. Autonomic ganglion synapses
    3. parasympathetic effector synapses
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54
Q

Edrophonium Pharmacology

A
  • reverses paralysis of non-depolarizing neuromuscluar blockers
  • Cholinesterase inhibitor (aka indirect-acting cholinergic agonist)
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55
Q

Edrophonium Uses

A
  • myasthenia gravis diagnostic event
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56
Q

Neostigmine Pharmacology

A
  • cholinesterase inhibitor (aka indirect-acting cholinergic agonist)
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57
Q

Neostigmine Uses

A
  • postoperative ileus

- postoperative urinary retention

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58
Q

Pyridastigmine Pharmacology

A
  • cholinesterase inhibitor (aka indirect-acting cholinergic agonist)
59
Q

Pyridastigmine Uses

A
  • myasthenia gravis (DOC)
60
Q

Indirect-acting cholinergic agonists that do not cross the blood brain barrier

A
  • edrophonium
  • neostigmine
  • pyridostigmine
61
Q

Indirect-acting cholinergic agonists that cross the blood brain barrier

A
  • donepezil
  • rivastigmine
  • galantamine
62
Q

Donepezil Pharmacology

A
  • selective Acetylcholinesterase

- non-competitive

63
Q

Rivastigmine Pharmacology

A
  • Acetylcholinesterase and butyrylcholinesterase

- non-competitive

64
Q

Galantamine Pharmacology

A
  • Acetycholinesterase and butyrylcholinesterase
  • competative
  • nicotinic receptor modulation
65
Q

Toxicity of Cholinergic agonist drugs in the CNS

A
  • anxiety
  • headache
  • tremors
  • confusion
  • coma
66
Q

Toxicity of Cholinergic agonist drugs in the eye

A
  • lacrimation
  • miosis
  • blurred vision
67
Q

Toxicity of Cholinergic agonist drugs on the cardiovascular system

A
  • Bradycardia

- hyper or hypo tension

68
Q

Toxicity of Cholinergic agonist drugs on the respiratory system

A
  • bronchial constrictions

- increased secretions

69
Q

Toxicity of Cholinergic agonist drugs on the GIT

A
  • nausea
  • vomitting
  • diarrhea
  • abominal cramps
70
Q

Toxicity of Cholinergic agonist drugs on the Bladder

A
  • increased uriniary urgency

- involunatry micturation

71
Q

Toxicity of Cholinergic agonist drugs on the glands

A
  • increased salivation

- increased sweating

72
Q

Toxicity of Cholinergic agonist drugs on the skeletal muscles

A
  • inital spasms leading to muscle weakness and respiratory paralysis
73
Q

Diarrhea cause

A
  • parasympathetic

- muscarinic

74
Q

Urination cause:

A
  • parasympathetic

- muscarinic

75
Q

Miosis cause:

A
  • parasympathetic

- muscarinic

76
Q

Muscles weakness cause:

A
  • not para or sympathetic

- nicotinic

77
Q

Bronchospasm cause:

A
  • parasympathetic

- muscarinic

78
Q

Excitation cause:

A
  • not para or sympathetic

- nicotinic

79
Q

Lacrimation cause:

A
  • parasympathetic

- muscarinic

80
Q

Seizures cause:

A
  • not para or sympathetic

- nicotinic

81
Q

Sweating cause:

A
  • sympathetic

- muscarinic

82
Q

Salivation cause:

A
  • Both para and sympathetic

- muscarinic and andegeric

83
Q

Pralidoxime Pharmacology

A
  • cleaves the dialkylphosphate group from the active site of acetylcholinesterase
  • reactivation of the enzyme
  • only works acutely
  • onset within 1 hour
84
Q

Atropine Pharmacology

A
  • competitive antagonist at all muscarinic receptor subtypes
85
Q

Atropine Effects on the CNS

A
  • slight drowsiness

- hallucinations

86
Q

Atropine Effects on Cardiovascular

A
  • increased heart rate

- faster conduction

87
Q

Atropine Effects on Respiratory

A
  • bronchodilation

- decreased secretions

88
Q

Atropine Effects on GI

A
  • decreased motility

- decreased secretion

89
Q

Atropine Effects on Urinary

A
  • urinary rentention
90
Q

Atropine Effects on Glands

A
  • decreased salivation

- decreased sweating (hyperthermia)

91
Q

Atropine Effects on Ocular

A
  • mydriasis
  • blurred vision
  • paralysis of accommodation
92
Q

Atropine Uses

A
  • acute myocardial infarction/cardiopulmonary resuscitation
  • treatment of pesticide over dose
  • preoperative
  • eye exams
93
Q

Atropine used to treat acute MI/cardiopulmonary resuscitation

A
  • reverses sustained bradycardia
  • reduces ventricular arrythmias (PVCs)
  • treats nausea from administering morphine (common for pain with MI)
94
Q

Atropine use to treat pesticide overdose

A
  • counteracts the effect of increased ACh at muscarinic receptors
  • given with Pralidoxime
95
Q

Atropine used preoperatively

A
  • given before surgery

- counteracts general anesthesia-induced bradycardia, salivation and increased brochial secretions

96
Q

Atropine used for eye exams

A
  • produced mydriasis (pupil dilation)
  • cycloplegia (inability to accommodate)
  • very long duration (up to 10 days)
97
Q

Anti-musarinic drugs - natural alkaloids

A
  • Atropine

- Scopolamine

98
Q

Scopolamine Pharmacology

A
  • competitive antagonist at all muscarinic receptors
99
Q

Scopolamine Adverse Effects

A
  • drowsiness and fatigue b/c it penetrates the blood brain barrier
100
Q

Scopolamine Uses

A
  • motion sickness
101
Q

Scopolamine for treatment of Motion Sickness

A
  • decreases salivary secretions
  • decreases GI motility
  • acts on CNS to decrease nausea
102
Q

Ipratroprium and Tiotropium Pharmacology

A
  • given as inhaler or nebulizer

- very low systemic side effects b/c little drug is absorbed

103
Q

Ipratroprium and Tiotropium Uses

A
  • topical bronchodilator for adjunctive treatment of asthma
104
Q

Benzotropine Uses

A
  • treatment of functional tremor in young patients with parkinson’s disease
  • reduces drooling associated with Parkinson’s
105
Q

Anti-muscarinic - synthetic/semisynthetic non-selective drugs

A
  • Ipratroprium
  • Tiotropium
  • Benzotropine
106
Q

Muscarinic Selective Receptor Subtype drugs

A
  • Pirenzapine
  • Oxybutnin
  • Darifenacin
107
Q

Pirenzapine Pharmacology

A
  • relatively selective M1 receptor antagonist
  • low incidence of dry mouth
  • decreases gastric acid secretion
108
Q

Pirenzapine uses

A
  • once used for peptic ulcers
109
Q

Oxybutnin Pharmacology

A
  • 10x greater selectivity for M1 and M3 receptors than M2
  • decreases frequency of detrusor (bladder) muscle contractions
  • delays desire to void
110
Q

Oxybutnin Uses

A
  • urinary incontinence due to detrusor muscle hyperractivity
111
Q

Oxybutnin Adverse Effects

A
  • dry mouth, drowsiness, constipation, and blurred vision during discontinuation of therapy
112
Q

Darifenacin Pharmacology

A
  • M3 selective antagonist

- inhibits bladder muscle tone at doses that do not effect salvation

113
Q

Treatment for Overactive Bladder

A
  • Oxybutnin
  • Darifenacin
  • Botulinum neurotoxin
114
Q

Effects of ganglion blockade on CNS

A
  • if the drug crosses the BBB it alters cognitive processing
115
Q

Effects of ganglion blockade on the Eye

A
  • Pupil dilation

- failure to accommodate

116
Q

Effects of ganglion blockade on the CVS

A
  • decrease in blood pressure

- orthostatic hypotension due to blockade of normal sympathetic relexes

117
Q

Effects of ganglion blockade on Arterioles

A
  • vasodilation

- increased peripheral flow -> hypotension

118
Q

Effects of ganglion blockade on Veins

A
  • dilation
  • pooling of blood
  • decreased venous return
119
Q

Effects of ganglion blockade on Heart

A
  • tachycardia
120
Q

Effects of ganglion blockade on the GIT

A
  • reduced tone and motility

- constipation

121
Q

Effects of ganglion blockade on the Urinary bladder

A
  • urinary retention
122
Q

Effects of ganglion blockade on the salivary glands

A
  • dry mouth
123
Q

Effects of ganglion bloackade on sweat glands

A
  • dry, hot skin
124
Q

Normal tone of the Eye

A
  • Parasympathetic
125
Q

Normal tone of the Arterioles

A
  • Sympathetic
126
Q

Normal tone of the Veins

A
  • Sympathetic
127
Q

Normal tone of the Heart

A
  • Parasympathetic
128
Q

Normal tone of the GIT

A
  • Parasympathetic
129
Q

Normal tone of the Urinary bladder

A
  • Parasympathetic
130
Q

Normal tone of the Salivary Glands

A
  • Parasympathetic
131
Q

Normal tone of the Sweat Glands

A
  • Sympathetic
132
Q

Competitive ganglion blockers

A
  • Trimethaphan

- Tubocurarine

133
Q

Trimethaphan Pharmacology

A
  • competitive antagonist at the neuronal nicotinic (NN) ACh receptor subtype
  • prevents depolarization of the parasympathetic effector neuron by ACh
  • direct peripheral vasodilator action
134
Q

Tubocurarine Pharmacology

A
  • not very selective
  • also blocks the NM (muscle nicotinic) receptor
  • relaxes skeletal muscles
135
Q

Non-competitive ganglion blockers

A
  • Mecamylamine

- Hemicholinium

136
Q

Mecamylamine Pharmacology

A
  • open channel block of nicotinic receptor

- can cross the BBB

137
Q

Hemicholinium Pharmacology

A
  • 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
Q

Trimethaphan Uses

A
  • hypertension emergencies (sudden increase in BP)
  • malignant hypertension
  • postoperative hypertension
  • competative
139
Q

Mecamylamine Uses

A
  • essential hypertension

- non-competative

140
Q

Ganglion Blockers Adverse Effects in CVS

A
  • orthostatic hypotension (blocks baroreceptor reflex)
141
Q

Ganglion Blockers Adverse Effects in the Eyes

A
  • blurred vision

- dilated pupils

142
Q

Ganglion Blockers Adverse Effects in the GIT

A
  • constipation, vomiting, nausea, anorexia, dry mouth
143
Q

Ganglion Blockers Adverse Effects in the Urinary tract

A
  • uriniary retention

- sexual dysfunction

PHAR 341 - Pharmacology (7 decks)

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