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Pathology > Pharmacology Class 2020 :Cholinergics > Flashcards

Pharmacology Class 2020 :Cholinergics Flashcards

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
Q

What is the location and function of M3?

A

Location:
Exocrine glands, vessels, CNS neurons

Function: Increase intracellular calcium

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26
Q

What is the location and function of M4?

A

Location:
CNS neurons

Functions:
opening of potassium channels
Inhibition of adenyl cyclase

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27
Q

What is the location and function of M5?

A

Location:
Vascular endothelium

Function:
Increased intracellular calcium

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28
Q

What effects does cholinergics have upon the eyes?

A

Miosis or contraction of the pupil for accomodation

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29
Q

What is the affect of a cholinergic on the heart?

A

Decrease HR and BP

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30
Q

What is the affect of a cholinergic on respiratory?

A

Bronchial constrictions

Increased secretions

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31
Q

What is the affect of a cholinergic upon the GI?

A

Increased motility
Relax sphincters
Stimulates secretions

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32
Q

What is the affect of cholinergics on GU?

A

Relaxes sphincters

Bladder wall contraction

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33
Q

What is the affect of cholinergics on sweat glands?

A

Increase secretions such as tears, sweats, salivary

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34
Q

What are the two types of cholinergic drugs?

A

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

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35
Q

What are the two types of direct cholinergic agonist?

A

Esters and Alkaloids

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36
Q

What are the ester form agonist?

A

Bethanechol
Carbechol
Methacholine

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37
Q

What are the alkaloid form of agonist?

A

Pilocarpine

Muscarine

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38
Q

What are the indirect and reversible cholinergic agonist?

A 
Edrophonium
Neostigmine
Pyridostigmine
Physostigmine
Galantamine
Donepezil
Rivastigmine
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39
Q

What are the indirect and irreversible cholinergic agonist?

A

Malathion
Parathion
Sarin
Saron

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40
Q

The reversible indirect agonist are lipid soluble

True or False

A

False

Water Soluble

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41
Q

The irreversible indirect agonist are water soluble

True or False

A

False

Lipid Soluble

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42
Q

What are the characteristics of the reversible cholinergic indirect agonist?

A

Alcohols and carbamates
Shorter duration of action
minutes to hours

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43
Q

What are the characteristics of the irreversible cholinergic agonist?

A

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

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44
Q

What are the reversible agents of indirect irreversible cholenergic?

A

Atropine which blocks ACH binding to the receptor

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45
Q

What cholinergic agents are used to treat open angle acute glaucoma?

A

Pilocarpine by causing contraction of the iris and ciliay muscle which leads to aqueous humor outflow and decreases intraocular pressure

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46
Q

What can be used in the place of pilocarpine if the cholinergic is not effective in treating glaucoma?

A

Carbachol

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47
Q

What is the effect of cholinergics on the cardiovascular system?

A

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

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48
Q

What affects do cholinergic have on respiratory?

A

contraction of the bronchial smooth muscle and stimulates secretion

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49
Q

What agent is used to help diagnose asthma?

A

Methacholine

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50
Q

Cholinergics should be avoided when treating asthma

True or False

A

True

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51
Q

What affect does cholinergics have on GI?

A

Increased motility, secretion and relaxes sphincters

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52
Q

What cholinergic drugs treat postoperative ileus?

A

Neostigmine and bethanecol

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53
Q

What cholinergic drugs treat dry mouth?

A

Pilocarpine

Cevimeline

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54
Q

What cholinergic drugs treat genitourinary?

A

Neostigmine by releasing post operative bladder retention through bladder contraction

Bethanechol which relieves urinary retention and neurogenic bladder by making bladder lose its tone

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55
Q

What is the medical condition myasthenia gravis?

A

Edrophonium is used as a diagnostic agent but not available in the US

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56
Q

What is the agent used to treat myasthenia gravis?

A

Pyridostigmine and neostigmine

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57
Q

What cholinergic drugs are used in the reversal of NMB?

A

pyridostigmine and neostigmine

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58
Q

Physostigmine

A

Inhibits the enzyme acetylcholinesterase and has a tertiary amine that allows it to cross the BBB in the unionized form.

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59
Q

What is the antidote to reverse toxic effects caused by pure anticholinergics?

A 
Atropine
Benztropine
Scopolamine
Atropa
Belladonna
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60
Q

What is the adverse effects of physostigmine?

A

Seizures
Hallucinations
Arrythmia

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61
Q

What cholinergic agents treat alzheimer disease?

A

Donepezil
Galantamine
Rivastigmine

These drugs inhibit acetylcholinesterase which increases ACH in the CNS for synaptic transmission

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62
Q

What is alzheimers disease?

A

Characterized by the cholinergic deficiency in the cortex and basal forebrain

63
Q

What are the adverse effects and toxicity of the cholinergics?

A 
Nausea
Vomit
Salivation
Sweat
Bronchial constrict
decreased cardiac output
decreased inotropy
decreased chronotrophy
Muscle Weakness
Urinary urgency
64
Q

Do not use cholinergics if you have

A 
COPD
Asthma
Urinary tract obstruction
Acid peptic disease
hypotension
hyperthyroid
65
Q

Why are organophosphate cholinesterase inhibitors dangerous?

A

They allow too much ACH to accumulate

66
Q

What is a valuble decontamination method when poisoned by insecticide or organophosphate?

A

2 PAM which is used to knock of the organophosphate off the cholinesterase inhibitor which allow the break down of ACH

67
Q

What are the main muscarinic cholinergic receptor antagonist?

A

atropine
ipratropium
glycopyrrolate

68
Q

What are the anticholinergic effects of the eyes?

A

Mydriasis or

Cyclopegia which is blurred vision from dilated pupil paralysis

69
Q

What are the anticholinergic effects upon the skin?

A

dry skin and reduced sweating

70
Q

What are the affects of anticholinergics on the GI?

A

less motility

less gastric emptying

71
Q

What is the anticholinergic effect upon the heart?

A

increased heart rate

72
Q

what is the anticholinergic effect upon the respiratory?

A

bronchial dilation and decreased secretion

73
Q

What is the anticholinergic effects upon the genitourinary?

A

urinary retention

74
Q

What is the anticholinergic effect on the CNS?

A

Drowsiness
Hallucinations
Coma

75
Q

What are the muscarinic anatagonist?

A 
Atropine
Ipratropium
Scopolamine
Benztropine
Cyclopentolate
Darifenacin
Dicycloamine
Festoterodine
Glycopyrrolate
Oxybutynin
Pirenzepine
Propantheline
Solifenancin
Tolterodine
Trihexyphenidyl
Tropicamide
Trospium
76
Q

Where does atropine come from?

A

Belladonna plant and it is a competitive antagonist at the muscarinic receptors

77
Q

What are the therapeutic uses of atropine?

A

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
Q

What are the effects of atropine on the CNS?

A

Hallucination

Disorientation

Irritability

Restlessness

All of this at toxic dose because ACH is needed by the brain in a certain amount

79
Q

What receptor does atropine target within the heart?

A

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
Q

What is the effects of atropine on skin at toxic level?

A

Dry skin

Anihidrosis

81
Q

What effects does atropine have on the respiratory system?

A

promotes bronchodilation and decreases secretion

Inhibits bronchoconstriction caused by histamine , bradykinin

82
Q

What is the affect on the eye of atropine?

A

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
Q

What are the effects of atropine on GU?

A

Relaxes smooth muscle of the ureters and bladder wall to inhibit bladder contraction

84
Q

What are the effects of the atropine on GI?

A

Decreases motility by blocking the muscarinic receptors of the GI which cause a prolonged gastric emptying time and therefore vulnerabilty to ulcers

85
Q

Scopolamine

A

Prevention of motion sickness treatment

Treats postoperative vomit

86
Q

What is the MOA of scopolamine?

A

Blocks neural pathways from vestibular apparatus in the inner ear to the emetic center in the brainstem

87
Q

Why does scopolamine have a more significant effect on CNS than atropine?

A

It can pass BBB easily because of its lipophillic nature and therefore at toxic levels cause drowsiness, amnesia, fatigue and dreamless sleep

88
Q

Which anticholinergics treat overactive bladder?

A 
Oxybutynin
Trospium
Solifenancin
Darifenancin
Tolterodine
Festoerodine
89
Q

What is the MOA of anticholinergics used to treat overactive bladder?

A

Target M3 receptors in the bladder to relieve spasm

90
Q

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

91
Q

What MOA does atropine use to treat bradycardia?

A

Block M2 receptors on the SA nodal pacemaker cells

92
Q

Which anticholinergics treat parkinson?

A

Benztropine and Trihexyphenidyl by antagonizing ACH

93
Q

What treats IBS?

A

Dicyclomine and Hyoscyamine by reducing the spasmotic effects on the smooth muscle GI tract

94
Q

What are the anticholinergics that treat drooling?

A

Glycopyrrolate and Atropine by inhibiting salivation and secretion as well as causing bronchodilation

95
Q

Ipratropium is a treatment for what medical condition?

A

COPD by blocking ACH in the bronchial smooth muscle to cause bronchodilation

96
Q

Xerostomia

97
Q

What are the adverse effects of ipratropium?

A

xerostomia
cough
blurred vision

98
Q

What are the effects of anticholinergics on ophthalmology?

A

Mydriasis and cyclopegia

99
Q

What are the specific names of the anticholinergics used in opthamology exams?

A

Homatropine
Atropine
Tropicamide

100
Q

Anticholinergic adverse effects of eyes

A

increased angle closure pressure

101
Q

Anticholinergic adverse effects of the GI

A

slow motility which allows gastric ulcers

Peptic Ulcer disease

102
Q

Anticholinergic adverse effects of the GU

A

Prevents contraction

103
Q

Anticholinergic effects on Myasthenia Gravis

A

Worse symptoms

104
Q

Glycopyrrolate is used to treat which medical condition?

A

Duodenal ulcer

Sialorrhea

105
Q

Benzotropine is used to treat which medical condition?

A

Extrapyramidal symptoms and Parksonism

106
Q

Homatropine is used to treat which medical condition?

A

Opthamological examination

Myhidrasis and cycloplegia induction

107
Q

What is the clinical use of ipratropium?

A

Reduces or prevents bronchospasm

108
Q

What are the oxybutynin used for?

A

Reduces detrusor smooth muscle tone

109
Q

What is the clinical use of 2 PAM?

A

Regenerates active ACHE and can relieve skeletal muscle end plate block

110
Q

Histamine function

A

Neurotransmitter and Neuromodulator

Mediates allergic and inflammatory reaction with some role in anaphylatic reaction

Vasodilation
Release C reactive proteins

111
Q

Which cells release histamine?

A

Mast Cells

Basophils

112
Q

Where are the most abundant stores of histamine?

A

In mast cells of the nose, mouth, feet, blood vessels, internal body surfaces or places prone to injury

113
Q

Non mast cell histamine

A

Neuroendocrine control, cardiovascular regurgitation , thermal and body weight regulation, sleep and arousal

114
Q

Fundal Cells of the Stomach

A

Histamine release stimulates acid production

115
Q

When is histamine released ?

A

Allergic Type 1 hypersensitivity

116
Q

What are the four receptors that histamine binds to within the body?

A

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
Q

Which histamine receptor lowers BP?

118
Q

Which histamine receptor reduces HR?

119
Q

Which histamine receptor cause flushing?

120
Q

Which histamine receptor gives a sense of warmth?

121
Q

Which histamine receptor gives a headache?

122
Q

Which histamine receptor causes edema?

123
Q

What is the effect of histamine binding to H1 in the GI?

A

Contraction of intestinal smooth muscle

124
Q

Which histamine receptor stimulation results in acid secretion?

A

H2 causes secretion of acid from parietal cells

125
Q

What is the effect of H1 stimulation within the respiratory ?

A

Bronchoconstriction

126
Q

What affect does H1 stimulation have in CNS?

A

pain and itching

127
Q

What affect does histamine have on skin?

A

Wheal and flare

128
Q

What can happen GU from histamine?

A

Histamine induced contractions lead to abortion

129
Q

Which histamine receptor causes arousal in the circadian sleep/wake cyle?

130
Q

What affects do Histamine have in CNS?

A

Memory and learning
Suppression of feeding
Body Temperature control

131
Q

What is the triple response?

A
  1. Red spot
  2. Flare Response
  3. Edema

All from an intradermal injection of histamine that causes a triple response

132
Q

What are the histamine antagonist?

A

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
Q

What condition is a histamine anatgonist good to treat?

134
Q

What condition is a histamine antagonist good to treat?

135
Q

What are H1 antagonist?

A 
Allergy and cold medicine
Sleep aids
motion sickness
antientic
1st and 2nd generation H1 antagonist
136
Q

What are H2 antagonist?

A 
Pepti ulcer disease
GERD
Ulcer prophylaxis
Heartburn
Famotidine
Cimetidine
Rantidine
137
Q

H3 antagonism can help with what condition?

A

weight loss

138
Q

What are the effects of H4 antagonism?

A

Decrease pain and improve cognitive impairment

139
Q

What are the first generation antihistamines?

A

Diphenhydramine which is benadryl

Hydroxyzine 
Meclizine
Promethazine
Cyproheptadine
Bromopheniramine
Chlorpheniramine
140
Q

What are the second generation antihistamines?

A 
Fexofenadine
Loratadine
Cetrizine
Desloratadine
Levicetirizine
141
Q

What are the effects of first generation antihistamines?

A 
More sedation
More lipophillic
Well absorbed
Shorter acting 4-6 hours per dose
More side effects
Sedating
More Anti ACH effects
142
Q

What are effects of 2nd generation antihistamines?

A 
Much less sedation
Less lipophilic
Well absorbed
Longer Acting 12-24 hours
Less side effects
Little/no sedation
Much less anti ACH effects
143
Q

What does diphenhydramine treat?

A

anaphylaxis

allergic rhinitis, hay fever

144
Q

Hyroxyzine treats which condition?

145
Q

Why are second generation agents preferred to treat seasonal allergies?

A

Less drowsy
Antagonizes histamine effects on smooth muscle, blood vessels, immune cells
Also block muscarinic receptors

146
Q

Which drugs treat motion sickness and vestibular disturbances?

A

Diphenhydramine
Dimenhydrinate
Promethazine
Meclizine

147
Q

What are MOA of the antagonist that treat motion sickness?

A

Antimuscarinic effects by suppressing vestibular end organ receptors and inhibits activation of central cholinergic pathways.

148
Q

Which drug is used to treat nausea and vomiting in pregnant woman?

A

Doxylamine combined with B6

149
Q

What is a drug to treat generalized anxiety?

A

Hyroxyzine

150
Q

What are a drugs that are sleep aids?

A

Doxylamine

Diphenhyramine

151
Q

Cypropheptadine

A

Unique antihistamine because it has antiseronergic activity that is no longer used to treat allergies

152
Q

What are some antihistamine cough and cold products?

A

Chloropheniramine

Bromopheniramine

153
Q

What are the adverse anticholinergic affects and toxcity

A 
Sedation
Dry mouth
blurred vision
urine retention
GI upset
nausea

Excitation and convulsions in children
Postural hypotension

154
Q

Which two second generation antihistamines are isomers?

A

Loratadine and Desloratidine

Pathology (10 decks)

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