Anticholinergics Flashcards

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
Q

adverse CV effects of atropine

A

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.

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26
Q

adverse CNS effects of atropine

A
ataxia, 
coma, 
delirium, 
disorientation, 
dizziness, 
drowseiness, 
excitement,
 hallucination, 
HA, 
insomnia, 
nervousness (treat with physostigmeine)
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27
Q

adverse derm effects of atropine

A

anhydrosis, scarlatiniform rash, skin rash, urticarial,

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28
Q

adverse GI effects of atropine

A

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

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29
Q

adverse GU effects of atropine

A

urinary hesitancy

urinary retention

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30
Q

NMS adverse effects of atropine

A

laryngospasm

weakness

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31
Q

adverse respiratory effects of atropine

A

decreased volume of secretions from the nose, mouth, pharynx, and bronchi, decreases airway resistance via relaxation of bronchi and bronchiolar smooth muscle.

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32
Q

contraindications of atropine

A

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
Q

Expected with atropinization:

A

flushing, mydriasis, tachycardia, dyness of mouth/nose

34
Q

brand name of glycopyrolate

A

Robinul

35
Q

how is glycopyrolate supplied

A

0.2 mg/mL

36
Q

classification of glycopyrolate

A

quaternary ammonium compound

37
Q

does glycopyrolate cross the BBB

A

no

more potent than atropine but lacks CNS activity because of poor penetration of the BBB

38
Q

MOA of glycopyrolate

A

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
Q

uses of glycopyrolate

A

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
Q

dose of glycopyrolate for NBM reversal

A
  1. 05-0.15 mg/kg

0. 2 mg for each 1 mg of neostigmine or 5 mg of pyridostigmine

41
Q

dose of glycopyrolate for reduction of secretions

A

preoperatively IM 4 mcg/kg

intra-op IV 0.1 mg repeated as needed 2-3 minutes intervals

42
Q

when do you give glycopyrolate for reduction of secretions preoperatively

A

30-60 minutes before procedure

43
Q

onset of glycopyrolate

A

2-3 minutes

44
Q

peak of glycopyrolate

A

5 min

45
Q

half-life of glycopyrolate

A

1.25 hours

variable with kids

46
Q

metabolism of glycopyrolate

A

hepatic minimal renal 80%

47
Q

elimination of glycopyrolate

A

85% renal- unchanged drug

48
Q

adverse effects of glycopyrolate

A

Cholinergic side effects
same as atropine
except LOW CNS SE d/t poor penetration of BBB

49
Q

typical dose for glycopyrolate

A

0.2 mg intraoperatively for bradycardia

50
Q

what is glycopyrolate incompatible with

A

LR

51
Q

is glycopyrolate safe with glaucoma patients?

A

least mydriatic

dose for bradycardia does not cause adverse effects with these patients.

52
Q

brand name of scopalamine

A

transderm-Scop

53
Q

how is scopolamine supplied

A

1.5 mg in 72 hour patch

54
Q

classification of scopalamine

A

tertiary amine

alkaloid of belladonna plant

55
Q

properties of scopolamine on BBB

A

easily penetrates BBB

lipophilic

56
Q

MOA of scopalamine

A

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
Q

uses of scopolamine transdermal

A

N/V

motion sickness and recovery from ages and surgery

58
Q

uses of scopolamine injection

A

preoperative medication to produce amnesia, sedation, tranquilization, antiemetic effects, decrease salivary and respiratory secretion

59
Q

dose of scopolamine transdermal patch

A

5mcg/hr for 72 hours

1 patch hairless location

4 hours before surgery/night before

1 hour before cesarean section

60
Q

dose of scopalopmine subq

A

antiemetic

0.6- 1 mg

61
Q

dose of scopolamine IM IV subQ

A

0.6 mg 3-4 x daily

62
Q

onset of scopolamine oral,

A

Oral IM 0.5-1 hour

63
Q

transdermal

A

Transdermal 6-8 hours

64
Q

peak of scopalomine

A

20-60 minutes

65
Q

half life of scopalamine

A

2-3 hours

66
Q

metabolism of scopalomine

A

primarily hepatic

67
Q

elimination of scopolamine

A

1 % unchanged in urine

68
Q

adverse effects of scopolamine CV

A
Cardiac arrhythmias, 
flushing,
 orthostatic hypotension, 
palpitations, 
tachycardia.
69
Q

AE of scopolamine CNS

A

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
Q

derm AE or scopalamine

A

: skin eruptions, dry skin, dyshidrosis, erythema, pruritus, rash, urticarial,

71
Q

endocrine AE of scopalomine

A

thirst

72
Q

can scopolamine be given to a pregnant woman

A
class C
crosses placenta
may cause respiratory depression
neonatal hemorrhange
1 hour before c-section to reduce risk
73
Q

scopolamine is the most effective…

A

antisalagogue
at preventing motion sickness
most sedative also

74
Q

scopolamine has the least affect on…

A

heart rate of the 3 anticholinergics

75
Q

contraindications with scopalamine

A

Avoid with obstructive uropathy

Prostatic hypertrophy

Narrow angle glaucoma

Pyloric stenosis

76
Q

GU,GI AE with scopolamine

A

GU: constipation, diarrhea, dry throat, dysphagia, n/v xerostomia,

GI dysuria, urinary retention

77
Q

ocular AE with scopalomine

A

Ocular: impair accommodation, blurred vision, conjunctival infection ,cycloplegia, dryness, glaucoma,

78
Q

respiratory AE with scopolamine

A

Resp: dry nose, dyspnea

79
Q

other AE with scopolamine

A

Misc, anaphylaxis, shock, angio-edema, diaphoresis, hypersensitivity, heat intolerance