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Pathology > Pharmacology Class 2020 :Cholinergics > Flashcards

Pharmacology Class 2020 :Cholinergics Flashcards

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1
Q

What are the two components of the Peripheral nervous system?

A

Central which includes brain and brainstem

Peripheral which includes Autonomic and Somatic

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2
Q

The autonomic nervous system is split into two parts

A

Sympathetic

Parasympathetic

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3
Q

Almost all efferent fibers leaving the CNS are cholinergic

True or False

A

True

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4
Q

What neurotransmitter do all preganglionic neurons release?

A

ACH

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5
Q

Which part of the nervous system has the most cholinergic fibers?

A

Parasympathetic

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6
Q

Where are nicotinic acetylcholine receptors located?

A

skeletal muscles or somatic

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7
Q

Where are muscarinic ACH receptors found?

A

Cardiac
Smooth muscle
Neuron endings
Sweat glands

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8
Q

What two neurons are required within the autonomic nervous system reach a target organ?

A

preganglionic

postganglionic

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9
Q

What do cholinergics drugs do?

A

Mimic or block the actions of chemical transmitters

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10
Q

Are parasympathetic nerve fibers long or short?

A

short

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11
Q

All receptors at the neuromuscular junction have what type of receptors?

A

nicotinic

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12
Q

All target organs of the parasympathetics have what type of receptor?

A

Muscarinic

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13
Q

All autonomic ganglia have nicotinic receptors

True or False

A

True

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14
Q

What major neurotransmitter is stored in vesicles?

A

ACH

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15
Q

What enzyme synthesizes ACH?

A

ACH is derived from Actyl coenzyme A by Choline or CHAT acetyltransferase preganglionic nerve terminal

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16
Q

What releases ACH?

A

Calcium dependent exocytosis

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17
Q

Where does ACH bind?

A

Nicotinic receptors on postganglionic cells

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18
Q

Which enzyme hydrolyzes ACH?

A

Acetylcholinesterase

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19
Q

Where is acetylcholinesterase found?

A

neuronal membranes

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20
Q

What blocks the calcium dependent exocytosis of ACH?

A

Botullinum toxin

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21
Q

Where is ACH degraded?

A

By acetylcholinesterase in the post synaptic cell

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22
Q

What are cholinergic receptors?

A

ACH receptors

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23
Q

What is the location and function of the M1 receptor?

A

Location:
CNS neurons, sympathetic
postganglionic neurons

Function:
Increased intracellular Ca

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24
Q

What is the location and function of M2 receptor?

A

Location:
Myocardium, smooth muscle, CNS
neurons

Function:
Opening of K channels, inhibition of
adenylyl cyclase

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25
What is the location and function of M3?
Location: Exocrine glands, vessels, CNS neurons Function: Increase intracellular calcium
26
What is the location and function of M4?
Location: CNS neurons Functions: opening of potassium channels Inhibition of adenyl cyclase
27
What is the location and function of M5?
Location: Vascular endothelium Function: Increased intracellular calcium
28
What effects does cholinergics have upon the eyes?
Miosis or contraction of the pupil for accomodation
29
What is the affect of a cholinergic on the heart?
Decrease HR and BP
30
What is the affect of a cholinergic on respiratory?
Bronchial constrictions | Increased secretions
31
What is the affect of a cholinergic upon the GI?
Increased motility Relax sphincters Stimulates secretions
32
What is the affect of cholinergics on GU?
Relaxes sphincters | Bladder wall contraction
33
What is the affect of cholinergics on sweat glands?
Increase secretions such as tears, sweats, salivary
34
What are the two types of cholinergic drugs?
Direct Acting which directly act on ACH receptors Indirect Acting which increases ACH through inhibition of acetylchoinesterase which allows more ACH to float around longer
35
What are the two types of direct cholinergic agonist?
Esters and Alkaloids
36
What are the ester form agonist?
Bethanechol Carbechol Methacholine
37
What are the alkaloid form of agonist?
Pilocarpine | Muscarine
38
What are the indirect and reversible cholinergic agonist?
``` Edrophonium Neostigmine Pyridostigmine Physostigmine Galantamine Donepezil Rivastigmine ```
39
What are the indirect and irreversible cholinergic agonist?
Malathion Parathion Sarin Saron
40
The reversible indirect agonist are lipid soluble True or False
False Water Soluble
41
The irreversible indirect agonist are water soluble True or False
False Lipid Soluble
42
What are the characteristics of the reversible cholinergic indirect agonist?
Alcohols and carbamates Shorter duration of action minutes to hours
43
What are the characteristics of the irreversible cholinergic agonist?
Nerve gases and insecticides Long duration of action due to covalent bonds between phosphorous enzyme complex Some compounds last more than 100 hours Cross BBB due to lipophilicity
44
What are the reversible agents of indirect irreversible cholenergic?
Atropine which blocks ACH binding to the receptor
45
What cholinergic agents are used to treat open angle acute glaucoma?
Pilocarpine by causing contraction of the iris and ciliay muscle which leads to aqueous humor outflow and decreases intraocular pressure
46
What can be used in the place of pilocarpine if the cholinergic is not effective in treating glaucoma?
Carbachol
47
What is the effect of cholinergics on the cardiovascular system?
Reduces peripheral vascular resistance and slows HR Cholinergic Agents are not usually used to treat heart problems due to adverse effects of decreased inotrophy, decreased chronotropy and decreased vascular resistance
48
What affects do cholinergic have on respiratory?
contraction of the bronchial smooth muscle and stimulates secretion
49
What agent is used to help diagnose asthma?
Methacholine
50
Cholinergics should be avoided when treating asthma True or False
True
51
What affect does cholinergics have on GI?
Increased motility, secretion and relaxes sphincters
52
What cholinergic drugs treat postoperative ileus?
Neostigmine and bethanecol
53
What cholinergic drugs treat dry mouth?
Pilocarpine | Cevimeline
54
What cholinergic drugs treat genitourinary?
Neostigmine by releasing post operative bladder retention through bladder contraction Bethanechol which relieves urinary retention and neurogenic bladder by making bladder lose its tone
55
What is the medical condition myasthenia gravis?
Edrophonium is used as a diagnostic agent but not available in the US
56
What is the agent used to treat myasthenia gravis?
Pyridostigmine and neostigmine
57
What cholinergic drugs are used in the reversal of NMB?
pyridostigmine and neostigmine
58
Physostigmine
Inhibits the enzyme acetylcholinesterase and has a tertiary amine that allows it to cross the BBB in the unionized form.
59
What is the antidote to reverse toxic effects caused by pure anticholinergics?
``` Atropine Benztropine Scopolamine Atropa Belladonna ```
60
What is the adverse effects of physostigmine?
Seizures Hallucinations Arrythmia
61
What cholinergic agents treat alzheimer disease?
Donepezil Galantamine Rivastigmine These drugs inhibit acetylcholinesterase which increases ACH in the CNS for synaptic transmission
62
What is alzheimers disease?
Characterized by the cholinergic deficiency in the cortex and basal forebrain
63
What are the adverse effects and toxicity of the cholinergics?
``` Nausea Vomit Salivation Sweat Bronchial constrict decreased cardiac output decreased inotropy decreased chronotrophy Muscle Weakness Urinary urgency ```
64
Do not use cholinergics if you have
``` COPD Asthma Urinary tract obstruction Acid peptic disease hypotension hyperthyroid ```
65
Why are organophosphate cholinesterase inhibitors dangerous?
They allow too much ACH to accumulate
66
What is a valuble decontamination method when poisoned by insecticide or organophosphate?
2 PAM which is used to knock of the organophosphate off the cholinesterase inhibitor which allow the break down of ACH
67
What are the main muscarinic cholinergic receptor antagonist?
atropine ipratropium glycopyrrolate
68
What are the anticholinergic effects of the eyes?
Mydriasis or | Cyclopegia which is blurred vision from dilated pupil paralysis
69
What are the anticholinergic effects upon the skin?
dry skin and reduced sweating
70
What are the affects of anticholinergics on the GI?
less motility | less gastric emptying
71
What is the anticholinergic effect upon the heart?
increased heart rate
72
what is the anticholinergic effect upon the respiratory?
bronchial dilation and decreased secretion
73
What is the anticholinergic effects upon the genitourinary?
urinary retention
74
What is the anticholinergic effect on the CNS?
Drowsiness Hallucinations Coma
75
What are the muscarinic anatagonist?
``` Atropine Ipratropium Scopolamine Benztropine Cyclopentolate Darifenacin Dicycloamine Festoterodine Glycopyrrolate Oxybutynin Pirenzepine Propantheline Solifenancin Tolterodine Trihexyphenidyl Tropicamide Trospium ```
76
Where does atropine come from?
Belladonna plant and it is a competitive antagonist at the muscarinic receptors
77
What are the therapeutic uses of atropine?
To treat bradycardia by blocking cholinergics which reduce HR Decrease salivation/ secretions Dilate pupil in opthamology for exam Treat muscarinic mushroom poison Organophosphate poison
78
What are the effects of atropine on the CNS?
Hallucination Disorientation Irritability Restlessness All of this at toxic dose because ACH is needed by the brain in a certain amount
79
What receptor does atropine target within the heart?
It blocks the M2 receptors on the SA nodal pacemaker to antagonize the parasympathetic tone of the heart which can lead to tachycardia if atropine is at toxic level
80
What is the effects of atropine on skin at toxic level?
Dry skin | Anihidrosis
81
What effects does atropine have on the respiratory system?
promotes bronchodilation and decreases secretion Inhibits bronchoconstriction caused by histamine , bradykinin
82
What is the affect on the eye of atropine?
Cause unopposed sympathetic dilator activity and mydriasis by blocking the cholinergic responss on the pupillary sphincter muscle of the iris which leads to cycloplegia and photophobia
83
What are the effects of atropine on GU?
Relaxes smooth muscle of the ureters and bladder wall to inhibit bladder contraction
84
What are the effects of the atropine on GI?
Decreases motility by blocking the muscarinic receptors of the GI which cause a prolonged gastric emptying time and therefore vulnerabilty to ulcers
85
Scopolamine
Prevention of motion sickness treatment Treats postoperative vomit
86
What is the MOA of scopolamine?
Blocks neural pathways from vestibular apparatus in the inner ear to the emetic center in the brainstem
87
Why does scopolamine have a more significant effect on CNS than atropine?
It can pass BBB easily because of its lipophillic nature and therefore at toxic levels cause drowsiness, amnesia, fatigue and dreamless sleep
88
Which anticholinergics treat overactive bladder?
``` Oxybutynin Trospium Solifenancin Darifenancin Tolterodine Festoerodine ```
89
What is the MOA of anticholinergics used to treat overactive bladder?
Target M3 receptors in the bladder to relieve spasm
90
Anticholinergics used to treat an overactive bladder has 1/5 the anticholinergic activity of atropine , but 4 to 10 times the antispasmodic activity True or False
True
91
What MOA does atropine use to treat bradycardia?
Block M2 receptors on the SA nodal pacemaker cells
92
Which anticholinergics treat parkinson?
Benztropine and Trihexyphenidyl by antagonizing ACH
93
What treats IBS?
Dicyclomine and Hyoscyamine by reducing the spasmotic effects on the smooth muscle GI tract
94
What are the anticholinergics that treat drooling?
Glycopyrrolate and Atropine by inhibiting salivation and secretion as well as causing bronchodilation
95
Ipratropium is a treatment for what medical condition?
COPD by blocking ACH in the bronchial smooth muscle to cause bronchodilation
96
Xerostomia
Dry mouth
97
What are the adverse effects of ipratropium?
xerostomia cough blurred vision
98
What are the effects of anticholinergics on ophthalmology?
Mydriasis and cyclopegia
99
What are the specific names of the anticholinergics used in opthamology exams?
Homatropine Atropine Tropicamide
100
Anticholinergic adverse effects of eyes
increased angle closure pressure
101
Anticholinergic adverse effects of the GI
slow motility which allows gastric ulcers | Peptic Ulcer disease
102
Anticholinergic adverse effects of the GU
Prevents contraction
103
Anticholinergic effects on Myasthenia Gravis
Worse symptoms
104
Glycopyrrolate is used to treat which medical condition?
Duodenal ulcer | Sialorrhea
105
Benzotropine is used to treat which medical condition?
Extrapyramidal symptoms and Parksonism
106
Homatropine is used to treat which medical condition?
Opthamological examination | Myhidrasis and cycloplegia induction
107
What is the clinical use of ipratropium?
Reduces or prevents bronchospasm
108
What are the oxybutynin used for?
Reduces detrusor smooth muscle tone
109
What is the clinical use of 2 PAM?
Regenerates active ACHE and can relieve skeletal muscle end plate block
110
Histamine function
Neurotransmitter and Neuromodulator Mediates allergic and inflammatory reaction with some role in anaphylatic reaction Vasodilation Release C reactive proteins
111
Which cells release histamine?
Mast Cells | Basophils
112
Where are the most abundant stores of histamine?
In mast cells of the nose, mouth, feet, blood vessels, internal body surfaces or places prone to injury
113
Non mast cell histamine
Neuroendocrine control, cardiovascular regurgitation , thermal and body weight regulation, sleep and arousal
114
Fundal Cells of the Stomach
Histamine release stimulates acid production
115
When is histamine released ?
Allergic Type 1 hypersensitivity
116
What are the four receptors that histamine binds to within the body?
H1 = smooth muscle, endothelium and brain H2=Gastric Mucosa, cardiac muscle, mast cells and brain H3=Presynaptic brain, Myenteric plexus H4= Eosinophils, Neutrophils, CD4 t cells for immune response
117
Which histamine receptor lowers BP?
H1
118
Which histamine receptor reduces HR?
H2
119
Which histamine receptor cause flushing?
H1
120
Which histamine receptor gives a sense of warmth?
H1
121
Which histamine receptor gives a headache?
H1
122
Which histamine receptor causes edema?
H1
123
What is the effect of histamine binding to H1 in the GI?
Contraction of intestinal smooth muscle
124
Which histamine receptor stimulation results in acid secretion?
H2 causes secretion of acid from parietal cells
125
What is the effect of H1 stimulation within the respiratory ?
Bronchoconstriction
126
What affect does H1 stimulation have in CNS?
pain and itching
127
What affect does histamine have on skin?
Wheal and flare
128
What can happen GU from histamine?
Histamine induced contractions lead to abortion
129
Which histamine receptor causes arousal in the circadian sleep/wake cyle?
H1
130
What affects do Histamine have in CNS?
Memory and learning Suppression of feeding Body Temperature control
131
What is the triple response?
1. Red spot 2. Flare Response 3. Edema All from an intradermal injection of histamine that causes a triple response
132
What are the histamine antagonist?
Epi cause opposite effect on smooth muscle and anaphylaxis treatment. The release inhibition of mast cells by Cromolyn and Nedocromil which stabilize mast cells
133
What condition is a histamine anatgonist good to treat?
asthma
134
What condition is a histamine antagonist good to treat?
asthma
135
What are H1 antagonist?
``` Allergy and cold medicine Sleep aids motion sickness antientic 1st and 2nd generation H1 antagonist ```
136
What are H2 antagonist?
``` Pepti ulcer disease GERD Ulcer prophylaxis Heartburn Famotidine Cimetidine Rantidine ```
137
H3 antagonism can help with what condition?
weight loss
138
What are the effects of H4 antagonism?
Decrease pain and improve cognitive impairment
139
What are the first generation antihistamines?
Diphenhydramine which is benadryl ``` Hydroxyzine Meclizine Promethazine Cyproheptadine Bromopheniramine Chlorpheniramine ```
140
What are the second generation antihistamines?
``` Fexofenadine Loratadine Cetrizine Desloratadine Levicetirizine ```
141
What are the effects of first generation antihistamines?
``` More sedation More lipophillic Well absorbed Shorter acting 4-6 hours per dose More side effects Sedating More Anti ACH effects ```
142
What are effects of 2nd generation antihistamines?
``` Much less sedation Less lipophilic Well absorbed Longer Acting 12-24 hours Less side effects Little/no sedation Much less anti ACH effects ```
143
What does diphenhydramine treat?
anaphylaxis | allergic rhinitis, hay fever
144
Hyroxyzine treats which condition?
Pruritus
145
Why are second generation agents preferred to treat seasonal allergies?
Less drowsy Antagonizes histamine effects on smooth muscle, blood vessels, immune cells Also block muscarinic receptors
146
Which drugs treat motion sickness and vestibular disturbances?
Diphenhydramine Dimenhydrinate Promethazine Meclizine
147
What are MOA of the antagonist that treat motion sickness?
Antimuscarinic effects by suppressing vestibular end organ receptors and inhibits activation of central cholinergic pathways.
148
Which drug is used to treat nausea and vomiting in pregnant woman?
Doxylamine combined with B6
149
What is a drug to treat generalized anxiety?
Hyroxyzine
150
What are a drugs that are sleep aids?
Doxylamine | Diphenhyramine
151
Cypropheptadine
Unique antihistamine because it has antiseronergic activity that is no longer used to treat allergies
152
What are some antihistamine cough and cold products?
Chloropheniramine | Bromopheniramine
153
What are the adverse anticholinergic affects and toxcity
``` Sedation Dry mouth blurred vision urine retention GI upset nausea ``` Excitation and convulsions in children Postural hypotension
154
Which two second generation antihistamines are isomers?
Loratadine and Desloratidine

Pathology (10 decks)

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