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
uses for atropine
antidote to anticholinesterase poisoning sinus brady AV block
26
adverse effects of atropine
``` 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
27
scopolamine
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
28
ipratropium Bromide (atrovent)
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)
29
Dicyclomine (Bentyl, Bentylol)
anticholinergic drug used for Irritable bowel syndrome, also for functional bowel disorders such as diarrhea and hypermotility
30
Overactive bladder is AKA
urgency incontinence
31
Overactive bladder has 4 major symptoms
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
32
what causes urge incontinence
involuntary contractions of the bladder detrusor
33
what type of drugs are used for overactive bladder
anticholinergic agents
34
M1 location
salivary glands | CNS
35
M1 response to activation
salivation | enhanced cognition
36
M1 response to blockade
dry mouth | confusion, hallucinations
37
M2 location
heart
38
M2 response to activation
bradycardia
39
M2 response to blockade
tachycardia
40
M3 location
``` salivary glands bladder: detrusor GI smooth muscle eyes: iris sphincter ciliary muscle lacrimal gland ```
41
M3 response to activation
``` salivation bladder detrusor contraction increased GI tone and motility miosis ciliary muscle contraction (accomodation) lacrimal gland tearing ```
42
M3 response to blockade
``` dry mouth Detrusor relaxation GI decreased tone and motility mydriasis (pupil dilation) blurred vision dry eyes ```
43
for overactive bladder you want to target which muscarinic subtype for receptor
M3
44
anticholinergic drug that acts primarily at M3 and is used for overactive bladder
Oxybutynin (Ditropan XL, Gelnique, Oxytrol) | Tolterodine (Detrol, Detrol LA)
45
common side effects for oxybutynin
``` dry mouth constipation tachycardia urinary hesitancy urinary retention mydriasis burred vision dry eyes ```
46
Darifenacin (Enablex) - selectivity
displays the greatest degree of M3 selectivity
47
side effects of Darifenacin (enablex)
``` dry mouth constipation dyspepsia gastritis headache ```
48
what patient population should avoid Darifenacin
someone with severe liver impariment
49
Solifenacin (VESIcare)
similar to Darifenacin but not quite as selective to M3
50
Most common side effects of Solifenacin (VESIcare)
dry mouth constipation blurred vision others -dyspepsia urinary retention headache nasal dryness
51
rare adverse effect of Solifenacin (VESIcare)
angioedema | prolong QT interval
52
what patient population should avoid solifenacin
severe hepatic impairment
53
Tolterodine (Detrol, Detrol LA)
anticholinergic side effects are less with this med
54
serious adverse effect of Tolterodine
prolong QT interval, dosage should not exceed 4mg/day
55
Fesoterodine (Toviaz)
nonselective muscarinic antagonist used only for OAB | does not cause dysrythmias
56
Trospium (Sanctura XR, Trosec)
nonselective muscarinic blocker indicated only for OAB - low bioavailability, lack of CNS effects, lack of metabolism related interactions with other drugs
57
how to relieve dry mouth with muscarinic antagonists
sip on fluids chew sugar free gum alcohol free mouthwash
58
other pt education with muscarinic antagonists
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
antimuscarinic (anticholinergic) toxicity symptoms
``` 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
treatment for anticholinergic toxicity
minimize intestinal absorption of the antimuscarinic agent administer antidote - physostigmine
61
patient education for xerostomia adverse effect of Atropine
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
Pt education on vision changes for atropine
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
Atropine contraindications
Glaucoma - atropine raises IOP and glaucoma is characterized by IOP Intestinal atony due to constipation risk
64
antimuscarinic med pt education due to urinary retention
void prior to taking med
65
antimuscarinic med pt education due to anhidrosis
avoid activities that could lead to overheating. No sweat hinders ability to cool down
66
antimuscarinic med cautions (Atropine
Asthma pt - bronchial plugging pre-existing tachycardia Pt with BPH - worsen urinary retention
67
Atropine/muscarinic antagonists dug interactions
antihistamines phenothiazine antipsychotics tricyclic antidepressants
68
Baseline data prior to atropine
HR BP ECG
69
Monitoring for Atropine
HR BP recheck ECG for pt reports of palpitations or Chest pain
70
first line treatment for OAB
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
Second line treatment for OAB
Anticholinergic agents Darifenacin (Enablex) - Highly M3 selective Oxybutynin - Primarily M3 selective Tolterodine - Nonselective
72
What side effects will you see when using who is a M3 selective agent
``` constipation blurred vision photophobia dry eyes dry mouth ```
73
for a pt who can not take anticholinergics, what would be an alternative med for OAB as a treatment option
Mirabegron (Myrbetriq) - B3 agonist
74
Different additional side effect for Oxybutynin
``` 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
CYP3A4 and oxybutynin
Be aware drugs that inhibit or induce CYP3A4 may alter oxybutynin blood levels to increase tox (inhibitors) or reduce effectiveness (inducers)
76
which drug for OAB is most selective for M3
Darifenacin (Enablex)
77
Adverse Effects of Darifenacin (Enablex)
``` dry mouth constipation dyspepsia gastritis headache ```
78
Drug interactions for Oxybutynin, Darifenacin (Enablex) and Solifenacin (Vesicare) and Tolterodine (Detrol, Detrol LA) and Fesoterodine (Toviaz)- CYP3A4 inhibitors
Azole antifungal drugs (Ketoconazole, itraconazole) Protease inhibitors for HIV/AIDS (ritonavir, nelfinavir) Clarithromycin (macrolide Anibiotic)
79
what pt population should avoid Darifenacin (Enablex) and Solifenacin (Vesicare)
Severe liver impairment
80
Solifenacin (Vesicare) adverse effects
``` dry mouth constipation blurred vision dyspepsia urinary retention headache nasal dryness ```
81
Dangerous adverse effects of Solifenacin (Vesicare)
Angioedema of face, lips, tongue, larynx At high doses (10-30mg/day) can prolong QT interval
82
How should a pt take Solifenacin (Vesicare)
should be swallowed intact with liquid with or without food
83
For pt taking Solifenacin (Vesicare) with moderate hepatic or severe renal impairment and for those taking a powerful CYP3A4 inhibitor dosage should not exceed
5mg/day
84
which anticholinergic drug used for OAB has the longest half life?
Solifenacin (Vesicare) at 45-68 hrs
85
what is the selectivity for Tolterodine (Detrol, Detrol LA)
non-selective
86
Side effect differences in Tolterodine (Detrol, Detrol LA)
anticholinergic side effects affect fewer pt compared with other anticholinergics prescribed for OAB
87
most common side effects Tolterodine (Detrol, Detrol LA) at 2mg twice daily
dry mouth constipation dry eyes cns effects occur infrequently somnolence vertigo dizziness less than 1% tachycardia urinary retention
88
Anticholinergics for OAB with QT risk
Tolterodine (Detrol, Detrol LA) | Solifenacin (VESIcare)
89
Fesoterodine (Toviaz) adverse effects
dry mouth, constipation less common dizziness fatigue blurred vision non-selective
90
What kind of selectivity does Trospium (Sanctura XR) offer
nonselective | only indicated for OAB
91
What is notable about Trospium (Sanctura XR)
low bioavailability lack of CNS effects (doesnt cross BBB) No CYP interactions
92
side effects of Trospium (Sanctura XR)
dry mouth constipation rarely dry eyes urinary retention
93
potential drug interactions for Trospium (Sanctura XR)
Vancomycin metformin digoxin procainamide
94
muscarinic antagonists (anticholinergics) pt ed for constipation
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
Which med for OAB has the lowest bioavailability
Trospium
96
Which med for OAB do you not have to worry about CYP
Trospium