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Pharm 2 Exam > ch 14 > Flashcards

ch 14 Flashcards

1
Q

muscarinic antagonists are aka

A

anticholinergic drugs
parasympatholytic drugs
antimuscarinic drugs

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2
Q

anticholinergic means that it produces

A

selective muscarinic blockade

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3
Q

anticholinergic drugs

children

A

have a role in the management of resp conditions in childhood

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4
Q

anticholinergic drugs

pregnant women

A

Oxybutynin is relatively safe

others- no

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5
Q

anticholinergic drugs

breastfeeding

A

can inhibit lactation

full risk is unknown

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6
Q

anticholinergic drugs

older adults

A

not appropriate

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7
Q

muscarinic receptor locations

A

sweat glands
blood vessels
all organs regulated by the parasympathetic ns

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8
Q

effects of muscarinic receptor activation

A

decreased HR
Increased gland secretion
smooth muscle contraction

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9
Q

Muscarinic receptor antagonist

A

atropine

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10
Q

NicotinicN receptor location

A

all ganglia of the autonomic ns

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11
Q

NicotinicN effects of receptor activation

A

promotes ganglionic transmission

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12
Q

NicotinicN receptor antagonist

A

Mecamylamine

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13
Q

NicotinicM receptor location

A

neuromuscular junctions

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14
Q

NicotinicM effects of receptor activation

A

skeletal muscle contraction

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15
Q

NicotinicM receptor antagonist

A

Alpha Tubocurarine

Succinylcholine

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16
Q

Atropine Pharm effects on the

Heart

A

Increases HR

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17
Q

Atropine Pharm effects on the

Exocrine glands

A

decreases secretion from salivary glands
bronchial glands, sweat glands
and the acid-secreting cells of the stomach

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18
Q

Atropine Pharm effects on the

smooth muscle

A

relaxation of the bronchi
decreased tone of the urinary bladder detrusor (urinary retention)
decreased tone and motility of GI tract (constipation)

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19
Q

Atropine Pharm effects on the

eyes

A

mydriasis (dilation of the pupil)

cycloplegia (relaxation of the ciliary muscle) - focuses for far vision

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20
Q

Atropine Pharm effects on the

CNS

A

mild CNS excitation at therapeutic doses
At toxic doses - hallucinations and delirium which can resemble pyschosis
Extremely high doses- coma, resp arrest, death

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21
Q

How can atropine be given

A

topically to eyes
IM
IV
subq

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22
Q

Peak for atropine

A

30 min to one hour

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23
Q

Atropine half life

A

3 hours and as long as 10-17 hours

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24
Q

Atropine elimination

A

hepatic metabolism

urinary excretion

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25
Q

uses for atropine

A

antidote to anticholinesterase poisoning
sinus brady
AV block

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26
Q

adverse effects of atropine

A 
xerostomia (dry mouth)
Blurred vision
photophobia
elevation of IOP
Urinary retention
constipation
anhidrosis (absence of sweat)
Tachycardia

in patients with asthma, antimuscarinic drugs can cause thicker secretions leading to bronchial plugging

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27
Q

scopolamine

A

muscarinic antagonist
therapeutic doses of atropine produce mild cns excitation, this drug produces sedation
It will also suppress emesis and motion sickness where atropine will not, production of cycloplegia and mydriasis for ophthalmic procedures, production of preanesthetic sedation and obstetric amnesia

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28
Q

ipratropium Bromide (atrovent)

A

anticholinergic drug used to treat asthma, COPD, rhinitis caused by allergies or common cold.
Inhalation for asthma and COPD
nasal spray for rhinitis from allergies or common cold
Not associated with antimuscarinic side effects (minimal systemic effects)

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29
Q

Dicyclomine (Bentyl, Bentylol)

A

anticholinergic drug used for Irritable bowel syndrome, also for functional bowel disorders such as diarrhea and hypermotility

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30
Q

Overactive bladder is AKA

A

urgency incontinence

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31
Q

Overactive bladder has 4 major symptoms

A

1) urinary urgency
2) urinary frequency - 8 or more times in 24 hrs
3) nocturia - waking 2 or more times to void
4) urge incontinence

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32
Q

what causes urge incontinence

A

involuntary contractions of the bladder detrusor

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33
Q

what type of drugs are used for overactive bladder

A

anticholinergic agents

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34
Q

M1 location

A

salivary glands

CNS

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35
Q

M1 response to activation

A

salivation

enhanced cognition

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36
Q

M1 response to blockade

A

dry mouth

confusion, hallucinations

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37
Q

M2 location

A

heart

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38
Q

M2 response to activation

A

bradycardia

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39
Q

M2 response to blockade

A

tachycardia

40
Q

M3 location

A 
salivary glands
bladder: detrusor
GI smooth muscle
eyes: iris sphincter
          ciliary muscle
           lacrimal gland
41
Q

M3 response to activation

A 
salivation
bladder detrusor contraction
increased GI tone and motility
miosis 
ciliary muscle contraction (accomodation)
lacrimal gland tearing
42
Q

M3 response to blockade

A 
dry mouth
Detrusor relaxation
GI decreased tone and motility
mydriasis (pupil dilation)
blurred vision
dry eyes
43
Q

for overactive bladder you want to target which muscarinic subtype for receptor

A

M3

44
Q

anticholinergic drug that acts primarily at M3 and is used for overactive bladder

A

Oxybutynin (Ditropan XL, Gelnique, Oxytrol)

Tolterodine (Detrol, Detrol LA)

45
Q

common side effects for oxybutynin

A 
dry mouth
constipation
tachycardia
urinary hesitancy
urinary retention
mydriasis
burred vision
dry eyes
46
Q

Darifenacin (Enablex) - selectivity

A

displays the greatest degree of M3 selectivity

47
Q

side effects of Darifenacin (enablex)

A 
dry mouth
constipation
dyspepsia
gastritis
headache
48
Q

what patient population should avoid Darifenacin

A

someone with severe liver impariment

49
Q

Solifenacin (VESIcare)

A

similar to Darifenacin but not quite as selective to M3

50
Q

Most common side effects of Solifenacin (VESIcare)

A

dry mouth
constipation
blurred vision

others -dyspepsia
urinary retention
headache
nasal dryness

51
Q

rare adverse effect of Solifenacin (VESIcare)

A

angioedema

prolong QT interval

52
Q

what patient population should avoid solifenacin

A

severe hepatic impairment

53
Q

Tolterodine (Detrol, Detrol LA)

A

anticholinergic side effects are less with this med

54
Q

serious adverse effect of Tolterodine

A

prolong QT interval, dosage should not exceed 4mg/day

55
Q

Fesoterodine (Toviaz)

A

nonselective muscarinic antagonist used only for OAB

does not cause dysrythmias

56
Q

Trospium (Sanctura XR, Trosec)

A

nonselective muscarinic blocker indicated only for OAB - low bioavailability, lack of CNS effects, lack of metabolism related interactions with other drugs

57
Q

how to relieve dry mouth with muscarinic antagonists

A

sip on fluids
chew sugar free gum
alcohol free mouthwash

58
Q

other pt education with muscarinic antagonists

A

avoid hazardous activities if vision is impaired
avoid sugared gum, hard candy and cough drops due to increased risk of tooth decay
urinary retention can be minimized by voiding before taking the med
constipation can be reduced by increasing dietary fiber and fluids
avoid vigorous exercise in warm environments to prevent hyperthermia

59
Q

antimuscarinic (anticholinergic) toxicity symptoms

A 
HOT as a hare (hyperthermia)
DRY as a bone (dry eyes, dry mouth, dry skin)
RED as a beet (flushed face)
BLIND as a bat (mydriasis)
MAD as a hatter (delirium)
60
Q

treatment for anticholinergic toxicity

A

minimize intestinal absorption of the antimuscarinic agent

administer antidote - physostigmine

61
Q

patient education for xerostomia adverse effect of Atropine

A

dry mouth can promote tooth decay, gum problems and oral infections. Dryness can be alleviated by sipping fluids, chewing sugar-free gum, using salivary stimulants (citrus-flavored or tart sugarless candies, maltose lozenges) oral moisturizers (saliva substitutes, XyliMelts are available over-the-counter. Avoid sugary gum and hard candy.

use alcohol free mouth wash

62
Q

Pt education on vision changes for atropine

A

can focus on far and blurr near vision
do not drive if vision is impaired

the eye may be rendered unable to adapt to bright light. Wear dark glasses if photophobia is a problem

63
Q

Atropine contraindications

A

Glaucoma - atropine raises IOP and glaucoma is characterized by IOP

Intestinal atony due to constipation risk

64
Q

antimuscarinic med pt education due to urinary retention

A

void prior to taking med

65
Q

antimuscarinic med pt education due to anhidrosis

A

avoid activities that could lead to overheating. No sweat hinders ability to cool down

66
Q

antimuscarinic med cautions (Atropine

A

Asthma pt - bronchial plugging
pre-existing tachycardia
Pt with BPH - worsen urinary retention

67
Q

Atropine/muscarinic antagonists dug interactions

A

antihistamines
phenothiazine antipsychotics
tricyclic antidepressants

68
Q

Baseline data prior to atropine

A

HR
BP
ECG

69
Q

Monitoring for Atropine

A

HR
BP
recheck ECG for pt reports of palpitations or Chest pain

70
Q

first line treatment for OAB

A

Behavioral Therapy - scheduled voiding
timing fluid intake
doing Kegel exercises to strengthen pelvic floor muscles
avoiding caffeine - a diuretic that may also increase detrusor activity

71
Q

Second line treatment for OAB

A

Anticholinergic agents
Darifenacin (Enablex) - Highly M3 selective
Oxybutynin - Primarily M3 selective
Tolterodine - Nonselective

72
Q

What side effects will you see when using who is a M3 selective agent

A 
constipation
blurred vision
photophobia
dry eyes
dry mouth
73
Q

for a pt who can not take anticholinergics, what would be an alternative med for OAB as a treatment option

A

Mirabegron (Myrbetriq) - B3 agonist

74
Q

Different additional side effect for Oxybutynin

A 
M3
urinary retention
urinary hesitancy
constipation
blurred vision
photophobia
dry eyes
dry mouth

specific
tachycardia

below is prominent in pediatric
confusion
hallucinations
agitation

below is prominent in older adult
hallucinations
confusion
sedation

75
Q

CYP3A4 and oxybutynin

A

Be aware drugs that inhibit or induce CYP3A4 may alter oxybutynin blood levels to increase tox (inhibitors) or reduce effectiveness (inducers)

76
Q

which drug for OAB is most selective for M3

A

Darifenacin (Enablex)

77
Q

Adverse Effects of Darifenacin (Enablex)

A 
dry mouth
constipation
dyspepsia
gastritis
headache
78
Q

Drug interactions for Oxybutynin, Darifenacin (Enablex) and Solifenacin (Vesicare) and Tolterodine (Detrol, Detrol LA) and Fesoterodine (Toviaz)- CYP3A4 inhibitors

A

Azole antifungal drugs (Ketoconazole, itraconazole)
Protease inhibitors for HIV/AIDS (ritonavir, nelfinavir)
Clarithromycin (macrolide Anibiotic)

79
Q

what pt population should avoid Darifenacin (Enablex) and Solifenacin (Vesicare)

A

Severe liver impairment

80
Q

Solifenacin (Vesicare) adverse effects

A 
dry mouth 
constipation
blurred vision
dyspepsia
urinary retention
headache
nasal dryness
81
Q

Dangerous adverse effects of Solifenacin (Vesicare)

A

Angioedema of face, lips, tongue, larynx

At high doses (10-30mg/day) can prolong QT interval

82
Q

How should a pt take Solifenacin (Vesicare)

A

should be swallowed intact with liquid with or without food

83
Q

For pt taking Solifenacin (Vesicare) with moderate hepatic or severe renal impairment and for those taking a powerful CYP3A4 inhibitor dosage should not exceed

A

5mg/day

84
Q

which anticholinergic drug used for OAB has the longest half life?

A

Solifenacin (Vesicare) at 45-68 hrs

85
Q

what is the selectivity for Tolterodine (Detrol, Detrol LA)

A

non-selective

86
Q

Side effect differences in Tolterodine (Detrol, Detrol LA)

A

anticholinergic side effects affect fewer pt compared with other anticholinergics prescribed for OAB

87
Q

most common side effects Tolterodine (Detrol, Detrol LA) at 2mg twice daily

A

dry mouth
constipation
dry eyes

cns effects occur infrequently
somnolence
vertigo
dizziness

less than 1%
tachycardia
urinary retention

88
Q

Anticholinergics for OAB with QT risk

A

Tolterodine (Detrol, Detrol LA)

Solifenacin (VESIcare)

89
Q

Fesoterodine (Toviaz) adverse effects

A

dry mouth, constipation

less common
dizziness
fatigue
blurred vision

non-selective

90
Q

What kind of selectivity does Trospium (Sanctura XR) offer

A

nonselective

only indicated for OAB

91
Q

What is notable about Trospium (Sanctura XR)

A

low bioavailability
lack of CNS effects (doesnt cross BBB)
No CYP interactions

92
Q

side effects of Trospium (Sanctura XR)

A

dry mouth
constipation

rarely
dry eyes
urinary retention

93
Q

potential drug interactions for Trospium (Sanctura XR)

A

Vancomycin
metformin
digoxin
procainamide

94
Q

muscarinic antagonists (anticholinergics) pt ed for constipation

A

can be reduced by increasing dietary fiber and fluids
laxative if severe
need for adequate fluids if fiber supplements are taken to avoid worsening the constipation

95
Q

Which med for OAB has the lowest bioavailability

A

Trospium

96
Q

Which med for OAB do you not have to worry about CYP

A

Trospium

Pharm 2 Exam (18 decks)

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