Autonomic Drugs Flashcards

1
Q

Class of edrophonium

A

Ache i - short acting (reversible)

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2
Q

Class of pilocarpine

A

Muscarinic agonist

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3
Q

Class of bethanechol

A

Muscarinic agonist

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4
Q

Class of neostigmine

A

Ache i - intermediate acting (reversible)

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5
Q

Class of pyridostigmine, physostigmine, donepezil

A

Ache i (reversible)
Used for Alzheimers
Intermediate acting

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6
Q

class of echothiophate

A

Irreversible Ache i

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7
Q

What are organophosphate insecticides

A

Ache i - non therapeutic

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8
Q

Acetylcholinesterase inhibitors

MOA and uses

A

Increase ach, amplifies effects at cholinergic synapses, effects at nicotinic and muscarinic

Used to reverse NDMR blockade, MG, glaucoma, ileus, urinary retention, Alzheimer’s disease

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9
Q

What toxicity is expected with AChE i’s?

A

Increased ach, so increase PSNS, so bradycardia, increased salivation, increase muscle tone/hyperexcitability, Bronchoconstriction
CNS - excitation (possible convulsion) followed by depression (unconsciousness)

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10
Q

Ache i is not used to Reverse depolarizing blockade of succs, why?

A

Because sux is an agonist

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11
Q

Ache i drug effects

A

Increased secretions, increased GI motility, Bronchoconstriction, bradycardia, hypotension, miosis, large dose = depolarizing block, MG - improves transmission, NDMR reversal

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12
Q

what do we use edrophonium for?

A

Diagnosis of MG (to increase Ach, and increase transmission) - too short acting for therapeutic use

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13
Q

What do we use physostigmine for?

A

Treatment of glaucoma to decrease intraocular pressure by increasing PSNS and decreasing pressure

Works postganglionic PSNS

Cross BBB

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14
Q

What do we use pyridostigmine for?

A

Myasthenia Gravis to increase transmission at NMJ

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15
Q

Cholinergic crisis S&S

A

D - diarrhea, diaphoresis
U - urination
M - miosis
B - bradycardia

B - bronchoconstriction
E - excitation of skeletal muscle and CNS
L - lacrimation
S - salivation
S - sweating
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16
Q

What do you give as an antidote for cholinergic toxicity

A

Atropine = muscarinic blocker

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17
Q

What are the muscarinic agonist drugs?

A

Acetylcholine, carbachol, methacholine, bethanechol Muscarine, pilocarpine, oxotremorine, cevimeline

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18
Q

Muscarinic agonist drug effects

A

“Parasympathetomimetic”
CV = decrease HR, CO, and arterial blood pressure, vasodilation
GI = increased motility
Bladder = contracts
Lungs = bronchoconstriction
Increased secretions
Eye = miosis, accommodation for near vision, decreased intraocular pressure

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19
Q

How do muscarinic agonists cause vasodilation in vsmc

A

They bind to M3 receptors on endothelial cells which secrete NO and cause vasodilation

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20
Q

Where are the nicotinic acetylcholine receptors

A

NMJ, ganglia, CNS

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21
Q

NicotinicN receptors do what?

A

Stimulation of post-ganglionic neuronal activity and CNS stimulation

= increased autonomic outflow

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22
Q

NicotinicM receptors do what

A

Activation of skeletal muscle endplates leading to contraction

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23
Q

What is the class of atropine

A

Muscarinic antagonist

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24
Q

What is the class of glycopyrrolate

A

Muscarinic antagonist

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25
Q

What is the class of scopolomine

A

Muscarinic antagonist

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26
Q

What is the class of hexamethonium

A

NicotinicN ganglionic blocker

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27
Q

What is the class of atracurium, cisatricurium, vecuronium, roc, and panc

A

NicotinicM blocker

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28
Q

Atropine uses

A

Crosses BBB, useful for bradycardia and as an adjunct to blockade reversal

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29
Q

Scopolamine uses

A

Cross BBB +++

Used for motion sickness

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30
Q

Glycopyrrolate uses

A

Does not cross BBB
Blockade reversal adjunct to help wiht muscarinic activities of neostigmine (aka prevents bradycardia)
Short acting

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31
Q

Concerns with antimuscarinics

A

Hyperthermia, glaucoma, GU obstruction, prostatic hypertrophy, CV, GI ileus - further decreases motility

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32
Q

Medication classes with anticholinergic activities

A

Antihistamines, antispasmodics, antiparkinsonian, skeletal muscle relaxants, antipsychotics, antidepressants, antimuscarinics for urinary incontinence

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33
Q

NicotinicM antagonist effect

A

NDMRs

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34
Q

NicotinicN antagonist effects

A

Blocks ganglionic outflow

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35
Q

What is the class of norepinephrine?

A

Direct acting
Nonselective
Mixed alpha/beta agonist
Alpha 1 and Beta 1 (little beta2)

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36
Q

What is the class of phenylephrine

A

Direct acting selective alpha1 agonist

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37
Q

What is the class of dexmeditominide

A

Direct acting alpha 2 agonist

38
Q

What is the class of epinephrine

A

Direct acting mixed alpha/beta agonist, nonselective

39
Q

What is the class of isoproterenol

A

Direct acting non-selective beta agonist

40
Q

What is the class of dobutamine

A

Direct acting beta 1 agonist

41
Q

What ist he class of albuterol

A

Direct acting beta 2 agonist

42
Q

What is the class of ephedrine?

A

Indirect acting adrenergic agonist via NT release - can also act on receptors

“Mixed” acting

43
Q

How does cocaine work

A

NE Reuptake inhibition

44
Q

What is the class of tranylcypromine and selegiline

A

MAOi which stops breakdown of NE and dopamine

Tranylcypromine = nonselective
Selegiline = selective for MAO-b (dopamine)
45
Q

What is the class of prazosin

A

Selective alpha 1 antagonist

46
Q

What is the class of metoprolol and atenolol

A

Selective beta 1 antagonist

47
Q

What is the class of clonidine

A

Selective alpha 2 agonist

48
Q

What do amphetamines do

A

Displaces/releases stored catecholamine NT (NT releaser)

Inhibits catecholamine Reuptake

49
Q

How does tyramine work

A

NT releaser of catecholamines

Found in food, not a drug - this is the food-drug interactions of MAOis

50
Q

Dopamine receptor affinity

A

Low dose = dopa
Med dose = beta
High dose = alpha

51
Q

What does alpha 1 do?

A

Vasoconstriction (skin and splanchnic)
Mydriasis
Smooth muscle contracts (except GI)
GI/GU sphincter contract

52
Q

What does alpha 2 do

A

Decrease NE release presynaptically
CNS inhibit SNS outflow
Platelet aggregation
Pancreas = decrease insulin

53
Q

What does beta 1 do?

A

Increase heart rate and contractility
Renin release
Trophic effect = hypertrophy

54
Q

What does beta 2 do

A
Bronchodilator
Vasodilation (skeletal muscle beds)
Relaxes smooth muscle mostly
Skeletal muscle contracts = tremor
Relax GI/GU
Relax uterine smooth muscle
Glycogenolysis
55
Q

What class is phenoxybenxamine

A

Nonselective alpha blocker

56
Q

What class is phentolamine

A

Non selective alpha blocker

57
Q

what class is prazosin

A

Alpha 1 blocker

58
Q

What class is yohimbine

A

Alpha 2 blocker

59
Q

What class is propanolol

A

Nonselective beta blocker

60
Q

What class for metoprolol and esmolol

A

Beta 1 specific blocker

61
Q

Why wouldn’t you use selective beta 2 blockers

A

Risk for bronchoconstriction

62
Q

What type of innervation to the adrenal medulla, sweat glands, and blood vessels

A

SNS innervation only

63
Q

What is the dominant tone in cardiac, bronchial smooth muscle, GI tract, salivary glands?

A

PSNS

64
Q

What is the basal tone for sweat glands, arterioles, veins

A

SNS

65
Q

What does botulinum toxin do

A

Blocks release of Ach from presynaptic terminal

66
Q

What is acetylcholine synthesized from

A

Choline and acetyl-coA

67
Q

Name the M receptors and where they are

A
M1,4,5 = CNS
m2 = heart
M3 = smooth muscle, glands, endothelium, eye (circular)
68
Q

Norepinephrine synthesis

A

Tyrosine - dopa - dopamine - norepinephrine

69
Q

What does methylphenidate do

A

Stops Reuptake of norepinephrine (like cocaine)

70
Q

Alpha one and camp

A

Increases camp = smooth muscle contraction

71
Q

Alpha 2 and camp

A

Decreases camp - decreased NE release

72
Q

Betas and camp

A

Adenyl Cyclase = increased camp = increased kinase = activation to do the things it needs to do

73
Q

Sympathetic action on the heart

A

B1 - increase chronotropy and inotropy

74
Q

Parasympathetic action on the heart

A

M2 - decrease heart rate and inotropy

75
Q

SNS and PSNS actions on the lungs

A

Beta 2 - bronchodilation

M3,2 - bronchoconstriction

76
Q

SNS action on kidney

A

B1 - increase RASS

77
Q

SNS action on liver

A

b2 - increase gluconeogenesis

78
Q

SNS action on VSMC

A

Apha1 - constriction (skin and splanchnic)

Beta2 - dilation (sk muscle)

79
Q

SNS and PSNS action on GI walls

A

B2 - relax

M3 - contract

80
Q

What are the SNS and PSNS actions on GI sphincters

A

Alpha 1 - contract

M3 - relax

81
Q

What are the PSNS actions on GI secretions

A

M3 - increased secretions

82
Q

What are the SNS and PSNS effects on urinary bladder wall

A

Beta2 - relax

M3 - contracts

83
Q

SNS and PSNS effects on urinary bladder sphincter

A

Alpha1 - contract

M3 - relax

84
Q

SNS and PSNS effects on uterine smooth muscle

A
B2 = relax
M = contract
85
Q

SNS and PSNS on reproductive

A

Alpha 1 - ejaculate

M3 - erection

86
Q

SNS effect on adrenal medulla

A

NicotinicN - epi/norepinephrine release

87
Q

SNS and PSNS effect on eye

A

Alpha 1 - contract radial (SNS) - mydriasis

M3,2 - contract circular (PSNS) - miosis

88
Q

SNS effect on pilomotor smooth muscle

A

Contract alpha 1

89
Q

SNS effect on sweat glands - thermoregulatory

A

M - increased sweat

90
Q

SNS effect on sweat glands - aprocrine (stress)

A

Alpha 1 - sweat

91
Q

SNS effect on fat cells

A

B3 - lipolysis