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Pharmacology II - CP > Autonomic Drugs Overview > Flashcards

Autonomic Drugs Overview Flashcards

1
Q

Direct acting cholinergic drugs are either ____ or ____

A

muscarinic agonist or nicotinic agonist

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2
Q

muscarinic agonists include

A

acetylcholine, muscarine, pilocarpine, bethanechol

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3
Q

nicotinic agonists include

A

acetylcholine, nicotine, succinylcholine, varenicline

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4
Q

indirect acting cholinergic drugs are either ____ or ____

A

AChE Inhibitors that are reversible or irreversible

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5
Q

reversible AChE inhibitors include

A

edrophonium, neostigmine, pyridostigmine, physostigmine, donepezil

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6
Q

irreversible AChE inhibitors include

A

echothiophate
organophosphate insecticides
Sarin nerve gases

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7
Q

is edrophonium long, intermediate, or short acting?

A

short

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8
Q

is neostigmine long, intermediate, or short acting?

A

intermediate

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9
Q

Acetylcholine

A

quaternary ammonium
short duration
has nicotinic and muscarinic activity

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10
Q

MOA AChE inhibitors (indirect)

A

bind to active site and inhibit AChE

prevents ACh from binding so increases the ACh concentration, t 1/2, and activity

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11
Q

is edrophonium an alcohol or carbamate?

A

alcohol

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12
Q

is neostigmine an alcohol or carbamate?

A

carbamate

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13
Q

Clinical uses for AChE inhibitors

A

reverseal of NM blockade by nondepolarizing drugs, myasthenia gravis diagnosis and treatment, glaucoma, ileus, postop urinary retention, Alzheimer’s

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14
Q

AChE inhibitors effects

A

autonomic nervous system = increased secretions, increased GI motility, bronchoconstriction, bradycardia, hypotension, miosis

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15
Q

AChE inhibitors adverse effects

A

if given in large doses = depolarizing block

toxicity = excitation (convulsion) then depression (unconscious)

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16
Q

which reversible AChE inhibitors are quarternary amines and what is the significance of that?

A

edrophonium and neostigmine

polar = don’t cross BBB

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17
Q

which reversible AChE inhibitors are tertiary amines and what is the significance of that?

A

physostigmine

nonpolar = crosses BBB

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18
Q

onset and DOA for edrophonium

A

onset: 30-60 seconds
DOA: 10 minutes

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19
Q

onset and DOA for neostigmine

A

onset: 10 -30 minutes
DOA: 2- 4 hours

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20
Q

onset and DOA for physostigmine

A

onset: 3- 8 minutes
DOA: 1 hour

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21
Q

Cholinergic crisis toxicity mnemonic

A 
DUMBBELLS
D - diarrhea, diaphoresis
U- urination
M - miosis
B - bradycardia
B- bronchoconstriction
E - excitation, emesis
L - lacrimation
S - salivation, sweating
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22
Q

What is the antidote for muscarinic toxicity?

A

atropine

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23
Q

What is the antidote for AChE Inhibitor toxicity?

A

atropine or pralidoxime (have to give early)

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24
Q

which muscarinic agonist is typically used for treatment of bladder and GI hypotonia?

A

betanechol (stimulates motility)

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25
Q

what do muscarine, pilocarpine, oxotremorine, and cevimeline have in common?

A

muscarinic receptor specificity

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26
Q

muscarinic agonist effects (parasympathomimetic)

A 
decrease HR, CO, and arterial pressure
vasodilation via nitric oxide
increase GI motility
contracts bladder
bronchoconstriction
increase secretions
miosis, decrease intraocular pressure
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27
Q

clinical uses for muscarinic agonists

A

glaucoma, ileus, urinary retention, xerostomia (Dry mouth)

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28
Q

mnemonic for muscarinic agonist GI/GU effects

A 
SLUDGE
s- salivation
l - lacrimation
u - urination
d - diarrhea
g - GI upset
e - emesis
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29
Q

nicotinic nerve agonists effects

A

stimulation of post ganglionic neuronal activity, CNS stimulation

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30
Q

nicotinic nerve agonists clinical use

A

smoking cessation

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31
Q

nicotinic nerve agonists adverse effects

A

CNS stimulation, skeletal muscle depolarization/blockade, HTN, increase HR, N/V/D

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32
Q

nicotinic muscle agonist effects

A

activation of NM endplates, contraction

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33
Q

nicotinic muscle agonist clinical uses

A

depolarizing skeletal muscle paralysis

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34
Q

anticholinergics are either ____ or _____

A

muscarinic antagonist or nicotinic antagonist

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35
Q

nonselective muscarinic antagonist examples

A

atropine, glycopyrrolate, scopolamine

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36
Q

nicotinic nerve ganglionic blocker example

A

hexamethonium (historical)

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37
Q

nicotinic muscle NM blocker examples

A

atracurium, cisatracurium, vecuronium, rocuronium, pancuronium

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38
Q

muscarinic antagonist effects

A

increase HR, bronchodilation, decreased GI/GU, decrease glands/secretions, decrease sweating, mydriasis, sedation

39
Q

would you expect effects at the blood vessels with muscarinic antaognists?

A

no

40
Q

would you expect effects at the skeletal muscle with muscarinic antagonists?

A

no

41
Q

clinical uses of muscarinic antagonists

A

motion sickness, parkinson’s, COPD, asthma, excessive secretions, GI hypermotility, urinary urgency, bradycardia

42
Q

which muscarinic antagonists are tertiary amines and what is the significance of that?

A

atropine and scopolamine

crosses BBB

43
Q

half life of atropine

A

about 4 hours
in elderly - 10 hours
eye effects may last days

44
Q

half life, onset, DOA of scopolamine

A

1-4 hours (IV), onset 10 minutes, DOA 2 hours (IV)

45
Q

glycopyrrolate half life, onset, DOA

A

1 hour, onset 1 minute, DOA 7 hours

46
Q

memory aid for anticholinergic effects

A

Dry as a bone, hot as a pistol, red as a beet, blind as a bat, mad as a hatter

47
Q

medication classes with anticholinergic activity

A

antihistamines, antispasmodics, antiparkinson drugs, skeletal muscle relaxants, antipsychotics, antidepressants, antimuscarinics for urinary incontinence

48
Q

which patient population is especially susceptible to anticholinergic toxicity

A

elderly

49
Q

nicotinic muscle antagonists effects and clinical uses

A

effects: competitive antagonism at skeletal muscle, non depolarizing
uses: skeletal muscle relaxation for surgical, intubation, and ventilation control

50
Q

nicotonic nerve antagonist effects and uses

A

effects: blocks ganglionic output
uses: historical, hypertensive emergency

51
Q

direct acting adrenergic agonists include

A

alpha agonists, beta agonists, mixed alpha and beta agonists

52
Q

indirect acting adrenergic agonists include

A

NT releasers, NE reuptake inhibitors, MAO inhibitors

53
Q

nonselective alpha agonist

A

norepinephrine

54
Q

alpha 1 agonist

A

phenylephrine

55
Q

alpha 2 agonist

A

clonidine, dexmedetomidine

56
Q

nonselective beta agonist

A

isoproterenol

57
Q

beta 1 agonist

A

dobutamine

58
Q

beta 2 agonist

A

albuterol

59
Q

mixed alpha/beta agonist

A

epinephrine, norepinephrine

60
Q

epinephrine receptors

A

alpha 1 and 2, beta 1 and 2

61
Q

norepinephrine receptors

A

alpha 1 and 2 and beta 1

62
Q

neurotransmitter releasers

A

amphetamine and ephedrine

63
Q

norepi reuptake inhibitors

A

cocaine, SNRI

64
Q

MAO inhibitors

A

tranylcypromine, selegiline

65
Q

dopamine receptors

A

alpha 1, beta 1, dopamine 1 and 2

66
Q

endogenous catecholamines

A

dopamine, epi, norepi

67
Q

why don’t we give catecholamines PO?

A

they are polar, poor CNS penetration

68
Q

ephedrine, pseudoephedrine

A

displaces/releases stored catecholamine NT

some agonist activity

69
Q

amphetamine

A

displaces/releases stored catecholamine NT, inhibits catecholamine reuptake

70
Q

cocaine

A

blocks NE reuptake, blocks sodium channels

71
Q

tyramine

A

displaces/releases stored catecholamines

in fermented foods and interact with MAOIs (HTN crisis)

72
Q

alpha 1 agonist effects

A

vasoconstriction
smooth muscle contracts expect in GI
GI/GU sphincters contract
mydriasis

73
Q

alpha 2 agonist effects

A

decreases NE release, inhibit sympathetic outflow

platelet aggregation, decrease insulin

74
Q

beta 1 agonist effects

A

increase HR and contractility
increase renin release
trophic effect

75
Q

beta 2 agonist effects

A

bronchodilation, vasodilation, most smooth muscle relaxes, tremors, GI/GU relax, glycogenolysis

76
Q

low dose epinephrine

A

beta effects

77
Q

high dose epinephrine

A

alpha effects

78
Q

epinephrine effects with local anesthetics

A

causes vasoconstriction to keep LA in the desired area and prevent systemic effects

79
Q

low dose dopamine

A

Dopamine 1 in renal, mesenteric, coronary vascular beds

80
Q

medium dose dopamine

A

Beta 1

81
Q

high dose dopamine

A

alpha 1

82
Q

which drug has the highest affinity for alpha receptors?

A

epinephrine

83
Q

which drug has the highest affinity for beta receptors?

A

isoproterenol

84
Q

nonselective alpha adrenergic blocker

A

phenoxybenzamine

phentolamine

85
Q

alpha 1 adrenergic blocker

A

prazosin

86
Q

alpha 2 adrenergic blocker

A

yohimbine

87
Q

nonselective beta blocker

A

propranolol

88
Q

beta 1 blocker

A

metoprolol

esmolol

89
Q

why don’t we have beta 2 blockers?

A

would cause bronchoconstriction (no real good reason to do that)

90
Q

a beta 2 receptor agonist would NOT

A

stimulate renin release

beta 1

91
Q

the effects of isoproterenol could be blocked by a

A

nonselective beta adrenergic receptor antagonist

92
Q

what would be expected upon administration of a muscarinic agonist drug, but NOT with parasympathetic nerve stimulation?

A

vasodilation

93
Q

cholinergic receptors would be found at all of the following sites except

A

juxtaglomerular cells

Pharmacology II - CP (12 decks)

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