Anticholinergics Flashcards

(79 cards)

1
Q

brand name of atropine

A

atropine

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2
Q

how is atropine supplied

A
  1. 4 mg/mL (vial)

0. 1 mg/mL (1mg ER injector)

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3
Q

classification of atropine

A

tertiary amine

alkaloid of belladonna plant

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4
Q

MOA of atropine

A

Competitive antagonist
Combines reversibly with muscarinic cholinergic receptors to block the action of Ach at parasympathetic postganglionic sites.

*crosses BBB easilty
*combines to receptor without leading to the cell membrane permeability, inhibition of adenylate cyclase and alteration in calcium response that would normally lead to a cholinergic response in the presence of Ach.
Little effect at nicotinic cholinergic receptos
Weak analgesic action

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5
Q

M1 receptor function

A

M1- CNS stomach

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6
Q

M2 receptor function

A

M2- airway smooth muscle and the heart

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7
Q

M3 receptor function

A

M3- CNS, airway smooth muscle, glandular tissues and vascular endothelial cells.

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8
Q

M4 receptor function

A

M4- CNS

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9
Q

M5 receptor function

A

M5- CNS

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10
Q

uses of atropine

A

preopmedication to inhibit salivation and secretions

treatment of symptomatic sinus bradycardia

AV block

antidote for anticholinesterase poisoning, organophosphate insecticides

decrease side effects of anticholinesterases (edrophonium and neostigmine)

ophthalmic- mydrasis and cycloplegia for examination

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11
Q

dose of atropine for neuromuscular blockage reversal

A

IV 25-30 mcg/kg 30-60 seconds before neostigmine or 7-10 mcg/kg 30-60 seconds before edrophonium

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12
Q

is atropine effective with heart transplant patients for increasing the HR

A

NO- bradycardia may unresponsive

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13
Q

dose of atropine for treating bradycardia

A

IV 0.5 mg q 3-5 minutes

not to exceed a total of 3 mg

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14
Q

max dose of atropine for bradycardia

A

3 mg or 0.4 mg/kg

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15
Q

dose of atropine for salivation inhibition preanesthesia

A

IM IV Subq
0.4-0.6 mg 30-60 minutes preop
q4-6 hours

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16
Q

what effect can doses of less than 0.5 mg of atropine have on the bradycardic patient

A

paradoxical bradycardia

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17
Q

what is given along with atropine during organophosphate poisoning to decrease secretions

A

pralidoxime

cholinesterase reactivator

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18
Q

what actions does atropine reverse?

A

muscarinic but NOT nicotinic effects of organophosphate poisoning

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19
Q

onset of atropine

A

about 1 minute

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20
Q

peak of atropine

A

?

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21
Q

duration of atropine

A

30-60 minutes IV

2-4 hours IM

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22
Q

metabolism of atropine

A

hepatic via enzymatic hydrolysis to inactive metabolites

effects may be prolonged with severe hepatic impairment

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23
Q

half life of atropine

A

2-3 hours

much longer in children

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24
Q

elimination of atropine

A

renal (30-50%)

unchanged drug and metabolites

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25
adverse CV effects of atropine
Cardiac arrhythmias, flushing, hypotension, palpitations, tachycardia. (not for 2degree type 2 or 3degree AV block). Caution with HF, CAD, tachyarrhythmias, → MI low doses can cause transit decrease in HR mediated through an unkown mech Larger doses increase HR by blocking bagal effects on M2 receptors on the SA node. High doses of atropine cause skin vasodilation.
26
adverse CNS effects of atropine
``` ataxia, coma, delirium, disorientation, dizziness, drowseiness, excitement, hallucination, HA, insomnia, nervousness (treat with physostigmeine) ```
27
adverse derm effects of atropine
anhydrosis, scarlatiniform rash, skin rash, urticarial,
28
adverse GI effects of atropine
decreased motility from esophagus to colon, Ageusia loss of taste, bloating constipation, delayed gastric emptying, nausea, paralytic ileus, vomiting, zerostomia, LES sphincter relaxation, decreased barrier pressure and an increased in incidence of reflux from stomach to esophagus
29
adverse GU effects of atropine
urinary hesitancy | urinary retention
30
NMS adverse effects of atropine
laryngospasm | weakness
31
adverse respiratory effects of atropine
decreased volume of secretions from the nose, mouth, pharynx, and bronchi, decreases airway resistance via relaxation of bronchi and bronchiolar smooth muscle.
32
contraindications of atropine
Pts with obstructive uropathy Contraindicated in patients with prostatic hypertrophy Pts with pyloric stenosis Avoid: hiatal hernia, paralytic ileus, intestinal atony of elderly patient, severe ulcerative colitis, toxic megacolon
33
Expected with atropinization:
flushing, mydriasis, tachycardia, dyness of mouth/nose
34
brand name of glycopyrolate
Robinul
35
how is glycopyrolate supplied
0.2 mg/mL
36
classification of glycopyrolate
quaternary ammonium compound
37
does glycopyrolate cross the BBB
no | more potent than atropine but lacks CNS activity because of poor penetration of the BBB
38
MOA of glycopyrolate
competitive antagonist combines reversibly with muscarinic cholinergic receptors to block the action of Ach at parasympathetic postganglionic sites combines to receptor without leading to the cell membrane permeability inhibits adenylate cyclase alters calcium response that normally leads to a cholinergic response in the presence of Ach little to no effects at nicotinic cholincergic receptors
39
uses of glycopyrolate
Adjunct with acetylcholinesterase inhibitors = ANTAGONIZE effect of Ach at muscarinic receptors Inhibit salivation and excessive secretions intraopperatively to counteract drug induced BRADYARRHTHMIAS COPD/ chronic bronchitis and emphysema maintenance
40
dose of glycopyrolate for NBM reversal
0. 05-0.15 mg/kg | 0. 2 mg for each 1 mg of neostigmine or 5 mg of pyridostigmine
41
dose of glycopyrolate for reduction of secretions
preoperatively IM 4 mcg/kg intra-op IV 0.1 mg repeated as needed 2-3 minutes intervals
42
when do you give glycopyrolate for reduction of secretions preoperatively
30-60 minutes before procedure
43
onset of glycopyrolate
2-3 minutes
44
peak of glycopyrolate
5 min
45
half-life of glycopyrolate
1.25 hours variable with kids
46
metabolism of glycopyrolate
hepatic minimal renal 80%
47
elimination of glycopyrolate
85% renal- unchanged drug
48
adverse effects of glycopyrolate
Cholinergic side effects same as atropine except LOW CNS SE d/t poor penetration of BBB
49
typical dose for glycopyrolate
0.2 mg intraoperatively for bradycardia
50
what is glycopyrolate incompatible with
LR
51
is glycopyrolate safe with glaucoma patients?
least mydriatic | dose for bradycardia does not cause adverse effects with these patients.
52
brand name of scopalamine
transderm-Scop
53
how is scopolamine supplied
1.5 mg in 72 hour patch
54
classification of scopalamine
tertiary amine | alkaloid of belladonna plant
55
properties of scopolamine on BBB
easily penetrates BBB | lipophilic
56
MOA of scopalamine
Competitive antagonist blocking action of acetylcholine at parasynaptic sites at cholinergic (postganglionic) muscarinic receptors in smooth muscle (GI, GI, Heart), secretory glands (salivation), and CNS Increases CO Dries secretions No nicotinic effects
57
uses of scopolamine transdermal
N/V | motion sickness and recovery from ages and surgery
58
uses of scopolamine injection
preoperative medication to produce amnesia, sedation, tranquilization, antiemetic effects, decrease salivary and respiratory secretion
59
dose of scopolamine transdermal patch
5mcg/hr for 72 hours 1 patch hairless location 4 hours before surgery/night before 1 hour before cesarean section
60
dose of scopalopmine subq
antiemetic | 0.6- 1 mg
61
dose of scopolamine IM IV subQ
0.6 mg 3-4 x daily
62
onset of scopolamine oral,
Oral IM 0.5-1 hour
63
transdermal
Transdermal 6-8 hours
64
peak of scopalomine
20-60 minutes
65
half life of scopalamine
2-3 hours
66
metabolism of scopalomine
primarily hepatic
67
elimination of scopolamine
1 % unchanged in urine
68
adverse effects of scopolamine CV
``` Cardiac arrhythmias, flushing, orthostatic hypotension, palpitations, tachycardia. ```
69
AE of scopolamine CNS
Acute toxic psychosis (rare), agitation (rare), ataxia, confusion ,delusion (rare), disorientation, dizziness (rare), drowsiness, fatigue, hallucinations, HA, irritability, loss of memory, paranoid, restless Sedation: 100 X more potent than atropine at inhibiting the RAS- enhances sedative s/e of opiods or BZDs signinficantly less sedation with patch vs IV
70
derm AE or scopalamine
: skin eruptions, dry skin, dyshidrosis, erythema, pruritus, rash, urticarial,
71
endocrine AE of scopalomine
thirst
72
can scopolamine be given to a pregnant woman
``` class C crosses placenta may cause respiratory depression neonatal hemorrhange 1 hour before c-section to reduce risk ```
73
scopolamine is the most effective…
antisalagogue at preventing motion sickness most sedative also
74
scopolamine has the least affect on…
heart rate of the 3 anticholinergics
75
contraindications with scopalamine
Avoid with obstructive uropathy Prostatic hypertrophy Narrow angle glaucoma Pyloric stenosis
76
GU,GI AE with scopolamine
GU: constipation, diarrhea, dry throat, dysphagia, n/v xerostomia, GI dysuria, urinary retention
77
ocular AE with scopalomine
Ocular: impair accommodation, blurred vision, conjunctival infection ,cycloplegia, dryness, glaucoma,
78
respiratory AE with scopolamine
Resp: dry nose, dyspnea
79
other AE with scopolamine
Misc, anaphylaxis, shock, angio-edema, diaphoresis, hypersensitivity, heat intolerance