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Pharm 2 Exam > Ch 13 > Flashcards

Ch 13 Flashcards

1
Q

cholinesterase inhibitors do what?

A

activate cholinergic receptors indirectly by preventing the breakdown of acetylcholine

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2
Q 
These 6 categories are what type of drugs?
muscarinic agonists
muscarinic antagonists
cholinesterase inhibitors
ganglionic stimulating agents
ganglionic blocking agents
neuromuscular blocking agents
A

cholinergic drugs

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3
Q

muscarinic agonists selectively mimic the effects of _______ at the muscarinic receptors.

A

muscarinic agonists selectively mimic the effects of acetylcholine at the muscarinic receptors.

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4
Q

The ________ ________ prevent the breakdown of acetylcholine by _______________. As a result, more ___________ remains available to activate cholinergic receptors.

A

The cholinesterase inhibitors prevent the breakdown of acetylcholine by acetylcholinesterase. As a result, more acetylcholine remains available to activate cholinergic receptors.

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5
Q

______________selectively mimic the effects of acetylcholine at nicotinicN (neuronal) receptors of autonomic ganglia.

What is its common use

A

Ganglionic stimulating agents

Nicotine in smoking cessation programs

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6
Q

______________, represented by mecamylamine, selectively block ganglionic nicotinicN receptors.

A

Ganglionic blocking agents

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7
Q

_____________, represented by d-tubocurarine and succinylcholine, selectively block the effects of acetylcholine at nicotinicM (muscle) receptors at the neuromuscular junction.

A

Neuromuscular blocking agents

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8
Q

muscarinic agonists are also known as

A

parasympathetic agents

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9
Q

other names for Bethanechol

A

Urecholine

Duvoid

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10
Q

MOA for Bethanechol

A

direct acting muscarinic agonist
Binds reversibly to muscarinic cholinergic receptors to cause activation
Acts selectively at muscarinic receptors, having little or no effect on nicotinic receptors, either in ganglia or in skeletal muscle

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11
Q

pharm affects of Bethanechol

A

muscarinic receptor activation
heart - decreases heart rate
exocrine glands - increases sweating, salivation, bronchial secretions and secretion of gastric acid
smooth muscles - of lungs and GI tract - promotes contraction of bronchi and increased tone and motility of GI smooth muscle
bladder - contraction of the detrusor muscle and relaxation of the trigone and sphincter - results in bladder emptying
vascular - relaxation - hypotension
eyes - pupillary constriction (miosis) accommodation for near vision

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12
Q

Bethanechol is given how?

A

oral administration

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13
Q

Therapeutic uses Bethanechol

A

Approved only for urinary retention
muscarinic activation relaxes the trigone and sphincter muscles and increases voiding pressure by contracting the detrusor muscle which composes the bladder wall.

approved to treat urinary retention in postoperative and postpartum patients and to treat retention secondary to neurogenic atony of the bladder

do not use in obstruction

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14
Q

muscarinic receptor locations

A

sweat glands
blood vessels
all organs regulated by the parasympathetic NS

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15
Q

Muscarinic effects of receptor activation

A

many including
decreased HR
Increased gland secretion
smooth muscle contraction

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16
Q

Muscarinic Receptor agonists

A

Bethanechol

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17
Q

receptor location for NicotinicN

A

All ganglia of the autonomic NS

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18
Q

effects of receptor activation for NicotinicN

A

Promotes ganglionic transmission

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19
Q

Receptor agonists for NicotinicN

A

Nicotine

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20
Q

Receptor location for NicotinicM

A

Neuromuscular junctions

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21
Q

Effects of Receptor Activation for NicotinicM

A

Skeletal muscle contraction

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22
Q

Receptor agonists for NicotinicM

A

Nicotine

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23
Q

Pilocarpine (Isopto Carpine, Diocarpine, Pilopine HS, Salagen) metabolism

A

hepatic

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24
Q

Pilocarpine (Isopto Carpine, Diocarpine, Pilopine HS, Salagen) half life

A

1-1.5 hrs

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25
Q

Pilocarpine (Isopto Carpine, Diocarpine, Pilopine HS, Salagen) elimination

A

urine

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26
Q

Cevimeline (Evoxac) metabolism

A

hepatic

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27
Q

Cevimeline (Evoxac) elimination

A

urine - 84%

feces

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28
Q

Muscarinic agonists

children

A

safety and effectiveness unknown for bethanechol and cevimeline

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29
Q

Muscarinic agonists

pregnant women

A

Unknown

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30
Q

Muscarinic agonists

Breastfeeding women

A

Unknown if excreted in breastmilk

recommended nursing be discontinued while taking these drugs

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31
Q

Muscarinic agonists

Older adults

A

because older patients may have decreased cardiac, hepatic or renal function, care must be taken to evaluate risks on an individual basis

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32
Q

adverse affects bethanechol

cardiac

A

hypotension (secondary to vasodilation)

Bradycardia

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33
Q

adverse affects bethanechol

GI

A

excessive salivation
increased gastric acid
abd cramps
diarrhea

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34
Q

adverse affects bethanechol

Urinary

A

increase pressure in the urinary tract - can be hazardous to someone with obstruction or weakness of the bladder wall

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35
Q

adverse affects bethanechol

resp

A

exacerbation of asthma

can cause bronchoconstriction

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36
Q

adverse affects bethanechol

in patients with hypothyroidism

A

dysrhythmias - can increase heart rate to the point of a dysrhythmia for patients with hypothyroidism due to their heart being exquisitely sensitive to the effects of norepinephrine.

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37
Q

baseline data for bethanechol

A 
vital signs
urinary trends (times and amounts)
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38
Q

Monitoring for bethanechol

A

intake and output
observe for signs of excessive muscarinic response - abnormal salivation, sweating, urinary urgency, bradycardia, hypotension

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39
Q

Bethanechol is contraindicated for patients with

A 
peptic ulcer disease
urinary tract obstruction
intestinal obstruction
coronary insufficiency
hypotension
asthma
hyperthyroidism
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40
Q

How to minimize adverse effects for bethanechol

A

take on an empty stomach to reduce n/v

treat excessive muscarinic stimulation with atropine and supportive measures

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41
Q

Xerostomia

A

dry mouth resulting from reduced or absent saliva flow
if untreated, it can lead to peridontal disease, dental caries, altered taste, oral ulcers, candidiasis, difficulty eating and speaking

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42
Q

Cevimeline also known as

A

Evoxac

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43
Q

what type of agonist is Cevimeline (Evoxac)

A

Muscarinic

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44
Q

what is Cevimeline (Evoxac) used for?

A

relief of xerostomia in patients with Sjogren syndrome (autoimmune disorder)

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45
Q

How does Cevimeline (Evoxac) work?

A

activates muscarinic receptors on residual healthy tissue in salivary glands - promoting salivation

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46
Q

What other things is Cevimeline used for but not approved for

A

keratoconjunctivitis sicca (inflammation of the cornea and conjunctiva) and dry eye

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47
Q

most common adverse effects of Cevimeline (Evoxac)

A

excessive sweating, nausea, rhinitis, diarrhea

increased risk of UTI

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48
Q

Education for Cevimeline (Evoxac)

A

increased water intake

this medicine promotes miosis (constriction of pupil)
and may cause blurred vision - can make driving at night dangerous

49
Q

Cevimeline (Evoxac) is contraindicated in what patient populations and why?

A

use with caution with heart disease
-can reduce heart rate and slow cardiac conduction

contraindicated in uncontrolled asthma patients
increases airway resistance
use in caution for controlled asthma patients, chronic bronchitis or chronic COPD

50
Q

drug interactions for Cevimeline (Evoxac)

A

Can intensify cardiac depression caused by beta blockers bc both drugs decrease heart rate and cardiac conduction.

beneficial effects of cevimeline can be antagonized by drugs that block muscarinic receptors such as atropine, tricyclic antidepressants, antihistamines and phenothiazine antipsychotics

51
Q

What type of agonist is Pilocarpine (Salagen)

A

Muscarinic

52
Q

What is Pilocarpine (Salagen) mainly used for

A

topical therapy of glaucoma (ophthalmic disorder characterized by elevated intraocular pressure (IOP) with subsequent injury to the ophthalmic nerve

Treatment for dry mouth from Sjogren syndrome or for salivary gland damage from radiation therapy of the head and neck cancer. (oral version is under Salagen)

53
Q

At lower doses the principal adverse effect for Pilocarpine (Salagen) is

A

sweating. If dosage is excessive, it can produce the full spectrum of muscarinic effects

54
Q

Muscarinic poisoning can result from overdose with 2 kinds of medicine and ingestion of what?

A

1) Direct acting muscarinic agonists (bethanechol, pilocarpine)
2) indirect-acting cholinomimetics (cholinesterase inhibitors)
3) ingestion of certain mushrooms (Inocybe, Clitocybe spp. )

55
Q

Muscarinic Toxicity symptoms

A 
DUMBELS
Diaphoresis/Diarrhea
Urination
Miosis
Bradycardia/Bronchospasm/Bronchorrhea
Emesis
Lacrimation
Salivation
56
Q

Treatment for muscarinic toxicity

A

Administer atropine (a selective muscarinic blocking agent) and provide supportive therapy

57
Q

pt education for muscarinic agonists and cholinesterase inhibitors

A

Take drug 1 hour before meals or 2 hrs after meals to decrease risk of n/v

Inform patients about muscarinic toxicity and when to seek help

58
Q

Cholinesterase inhibitors are drugs that prevent ____________________________

A

the degradation of acetylcholine by acetylcholinesterase (cholinesterase) - by doing this they increase the amount of ACh available to activate receptors, thus enhancing cholinergic action.

59
Q

cholinesterase inhibitors are aka

A

anticholinesterase drugs

60
Q

Because of their lack of sensitivity, cholinesterase inhibitors are limited to only a few therapeutic applications such as

A 
treatment of:
Myasthenia gravis
glaucoma
Alzheimer disease
Parkinson disease dementia
Poisoning by muscarinic antagonists
61
Q

2 categories of cholinesterase inhibitors

A

reversible inhibitors - moderate duration

irreversible inhibitors - long duration

62
Q

trade name for pyridostigmine

A

Mestinon

Regonol

63
Q

What type of inhibitor is Pyridostigmine (Mestinon, Regonol)

A

reversible cholinesterase inhibitors

64
Q

what is the drug of choice for management of MG (myathenia gravis) and also approved for what

A

Pyridostigmine (Mestinon, Regonol)

approved for reversal of nondepolarizing muscle relaxants

65
Q

Pyridostigmine (Mestinon, Regonol) and crossing membranes/absorption

A

cannot readily cross membranes including those of the GI tract, blood brain barrier, and placenta

poorly absorbed after oral administration and has minimal effects on the brain and fetus

66
Q

pharm effects of pyridostigmine

A

by decreasing the breakdown of aceytlcholine, pyridostigmine and other cholinesterase inhibitors make more ACh available which can intensify transmission at virtually all junctions where ACh is the transmitter.

(Pyridostigmine is the busy bone for cholinesterase)

67
Q

muscarinic responses for pyridostigmine

A

identical to those of the direct-acting muscarinic agonists

by preventing breakdown of ACh, - indirectly cause bradycardia, bronchial constriction, urinary urgency, increased glandular secretions, increased tone and motility of GI muscle, miosis, focusing of the lens for near vision

68
Q

neuromuscular effects of cholinesterase inhibitors

A

effects on skeletal muscle are dose dependent
at therapeutic doses they increase force of contraction

toxic doses reduce force of contraction

69
Q

CNS effects of cholinesterase inhibitors

A

therapeutic levels can produce mild stimulation

toxic levels depress the CNS - including respirations

70
Q

Physostigmine metabolism

A

hydrolysis by cholinesterases

71
Q

Physostigmine elimination

A

urine

72
Q

Contraindications for cholinesterase inhibitors

A 
Obstruction of gi tract
Obstruction in urinary tract
Poetic ulcer disease
Asthma
Coronary insufficiency
Hyperthyroidism
73
Q

What is important to know about Neostigmine (Bloxiverz, prostigmin)

A

Oral absorption is poor, oral has been discontinued in US but still available in some countries

74
Q

Physostigmine use

A

Can cross blood brain barrier

Drug of choice for poisoning by atropine and other drugs that cause muscarinic blockade

75
Q

Pyridostigmine treats

A

MG

76
Q

Pyridostigmine baseline data

A

HR
BP
ECG
Assess muscle strength, fatigue, ptosis, ability to swallow to determine the extent of neuromuscular dysfunction

77
Q

Pyridostigmine monitoring

A 
HR
BP
Recheck ECG if pt has Bradycardia, palpitations, chest pain, shortness of breath
Titrate dose based on
1) times of drug administration 
2) time fatigue occurs
3) state of muscle strength
4) signs of excessive muscarinic stimulation

Monitor for signs of myasthenic crisis

78
Q

Signs of myasthenic crisis

A

Extreme muscle weakness
Paralysis of resp muscles

Manage Wirh resp support and increase dose)

Make sure it is not cholinergic crisis

79
Q

Difference in myasthenic crisis and cholinergic crisis

A

Signs of excessive muscarinic stimulation - this will accompany cholinergic crisis but not myasthenic crisis

80
Q

Pyridostigmine evaluating therapeutic effects

A

Assess for increased strength and muscle control

81
Q

What are the 3 cholinesterase inhibitors that are approved for management of Alzheimer disease

A

Donepezil (Aricept)
Galantamine (Razadyne)
Rivastigmine (Exelon)

82
Q

The irreversible cholinesterase inhibitors have only one indication

A

Glaucoma

83
Q

What is the drug name of the one irreversible cholinesterase approved for glaucoma

A

Echothiophate

84
Q

What is the concern with irreversible cholinesterase inhibitors

A

That these agent might be employed as weapons of terrorism

Highly lipid soluble

Readily absorbed from all routes of administration even through skin

85
Q

Irreversible cholinesterase inhibitors are aka

A

Organophosphate cholinesterase inhibitors

86
Q

Pharm effects or reversible cholinesterase inhibitors

A

Essentially the same as the reversible but the irreversible last a long time. Responsive to reversible inhibitors are brief

87
Q

Organophosphate cholinesterase inhibitors are employed primarily as

A

Insecticides

88
Q

Toxic doses of irreversible cholinesterase inhibitors produce excessive what

What type of crisis is this?

A

Excessive muscarinic, nicotine and CNS effects.

Cholinergic crisis

89
Q

Overstimulation of muscarinic causes

A 
Profuse secretions from salivary
Bronchiole
Involuntary urination and defication 
Laryngospasm
Bronchoconstriction
90
Q

Prominent nicotinic effects cause

A

Muscle weakness
Cramps
Twitching

91
Q

Neuromuscular blockade can result in

A

Paralysis of resp muscles

Death from apnea

92
Q

What Meds to treat cholinesterase inhibitor poisoning

A

Atropine for muscarinic stinkin
Pralidoxime for reverse inhibition of cholinesterase
Benzodiazepines to suppress convulsions

Resp depression from cholinesterase inhibitors cannot be managed with drugs

Treatment consists of mechanical ventilation with oxygen

93
Q

what is MG

A

neuromuscular disorder characterized by fluctuating muscle weakness and a predisposition to rapid fatigue

symptoms result from an autoimmune process where their immune system attacks nicotinicM receptors on skeletal muscle

94
Q

common symptoms of MG

A

ptosis (drooping eyelids)
difficulty swallowing
weakness of skeletal muscles

95
Q

In MG what are the signs of undermedication?

A

ptosis

difficulty swallowing

96
Q

In MG what are the signs of overmedication?

A

excessive salivation and other muscarinic response

97
Q

When might a MG patient need to anticipate increased dosage needs?

A

30 - 60 minutes before activities such as eating or shopping

98
Q

_______ can be used to overcome excessive muscarinic blockade by atropine

A

Cholinesterase inhibitors

99
Q

______ can be used to reduce excessive muscarinic stimulation caused by cholinesterase inhibitors

A

Atropine - but cant be used routinely bc it can mask early signs (excessive salivation) of overdose with anticholinesterase agents

100
Q

drug of choice for treating poisoning by atropine and other drugs that cause muscarinic blockade including antihistamines and phenothiazine antipsychotics but not tricyclic antidepressants owing to a risk for causing seizures.

A

Physostigmine

101
Q

what medication is used for diagnosis for MG, not treatment

A

Edrophonium (Enlon)

102
Q

drugs approved for Alzheimer disease

A

Donepezil (Aricept)
Galantamine (Razadyne)
Rivastigmine (Exelon)

103
Q

what cholinesterase inhibitor is approved for Alzheimer and dementia of Parkinson Disease

A

Rivastigmine (Exelon)

104
Q

irreversible cholinesterase inhibitors have only one indication

A

treatment of glaucoma

105
Q

which med category were produced for possible use as nerve agents but never deployed

A

irreversible cholinesterase inhibitors

106
Q

to break the bond and reverse the inhibition of cholinesterase for organophosphate cholinesterase inhibitors, we must administer

A

pralidoxime -cholinesterase reactivator

107
Q

cholinesterase inhibitors are commonly employed primarily as

A

insecticides

can be absorbed through skin

108
Q

toxic doses of irreversible cholinesterase inhibitors produce

organophosphate cholinesterase poisoning

A

excessive muscarinic stimulation and depolarizing neuromuscular blockade

overstim of muscarinic
profuse secretions from salivary and bronchial gland
involuntary urination and defecation
laryngospasm
bronchoconstriction
prominent nicotinic effects
muscle weakness
fasciculations - muscle twitch
cramps
twitching

neuromuscular blockade effects
paralysis
death from apnea

CNS effects
anxiety
confusion to delirium
convulsions

109
Q

treatment of organophosphate cholinesterase poisoning

A

atropine to reduce muscarinic stim

pralidoxime to reverse inhibition of cholinesterase

benzodiazepine (diazepam) to suppress convulsions

resp depression from cholinesterase inhibitors cannot be managed with drugs ->mechanical ventilation

110
Q

MG pt who are inadequately medicated may experience _____ which is a state characterized by extreme muscle weakness caused by ______

A

myasthenic crisis

insufficient ACh at the NMJ

111
Q

left untreated myasthenic crisis can lead to

A

death from paralysis of muscles of resp

112
Q

what med is given in myasthenic crisis

A

cholinesterase inhibitor (ie: neostigmine)

113
Q

overdose with a cholinesterase inhibitor can produce

A

cholinergic crisis

114
Q

symptoms of cholinergic crisis

A

extreme muscle weakness or
paryalysis
excessive muscarinic stimulation
Dumbels

Diaphoresis/Diarrhea
Urination
Miosis
Bradycardia/Bronchospasm/Bronchorrhea
Emesis
Lacrimation
Salivation
115
Q

treatment of cholinergic crisis

A

resp support
atropine
hold the offending cholinesterase inhibitor until muscle strength returned

116
Q

how to distinguish myasthenic crisis from cholinergic crisis

A

1) look at history of med use and look for signs of excessive muscarinic stim
2) if this info is inadequate for your diff, use edrophonium

alleviates symptoms -> myasthenic
worsens symptoms -> cholinergic

117
Q

MG pt in crisis edrophonium alleviates symptoms

A

Myasthenic crisis

118
Q

MG pt in crisis edrophonium worsens symptoms

A

Cholinergic Crisis

Pharm 2 Exam (18 decks)

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