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USMLE Step 1 > Autonomic Pharmacology > Flashcards

Autonomic Pharmacology Flashcards

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USMLE® Step 1 flashcards
1
Q

Symptoms of excess parasympathetic activity?

A 
Diarrhea
Urinary retention
Miosis / ciliary muscle contraction
Bradycardia
BronchoSPASM
Excitation (muscles and CNS)
Lacrimation
Salivation
Sweating
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2
Q

Parasympathetic inhibition is aka ______ or ______ inhibition. Symptoms of parasympathetic inhibition?

A

Parasympathetic = muscarinic inhib, or anti-cholinergic. Sx =
Hot as a hare
Dry as a bone
Red as a beet
Blind as a bat (cycloplegia, mydriasis)
Mad as a hatter
Bloated as a toad (urinary retention & constipation)

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3
Q

Effect of anti-muscarinics on heart rate?

A

Inhibition of vagal tone = tachycardia

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4
Q

Three anti-muscarinic drugs used topically for pupillary dilation:

A

Homatropine
Tropicamide
Cyclopent.

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5
Q

Atropine is used mainly for (2):

A

Treatment of bradycardia
As an antidote to organophosphate poisoning (organophosphates inhibit AChE, too much ACh, need to switch parasympathetics off).

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6
Q

This drug is helpful in Parkinson’s and in tx of EPS from antipsychotic use:

A

Benztropine

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7
Q

Antimuscarinic used in tx of motion sickness:

A

Scopolamine

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8
Q

Antimuscarinic for COPD and asthma (2):

A

Ipratropium

Tiotropium

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9
Q

Antimuscarinics used to help increase urinary retention in urge incontinence (5):

A 
Oxybutynin
Tolterodine
Darifenacin
Solifenacin
Trospium
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10
Q

This antimuscarinic drug helps decrease oral secretions in intubated patients. What is its other main use?

A

Scopolamine

Also used for motion sickness

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11
Q

This drug helps decrease oral secretions when given parenterally:

A

Glycopyrrolate

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12
Q

Physostigmine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-cholinesterase

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13
Q

Pilocarpine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Direct cholinergic agonist

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14
Q

Oxybutynin: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-muscarinic

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15
Q

Atropine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Direct cholinergic agonist

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16
Q

Donepezil: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-cholinesterase

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17
Q

Pralidoxime: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Trick question!

Cholinesterase RE-GENERATOR.

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18
Q

Bethanecol: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Direct cholinergic agonist

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19
Q

Neostigmine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-cholinesterase

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20
Q

Darifenacin: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-muscarinic

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21
Q

Ipratropium: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-muscarinic

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22
Q

Tropicamide: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-muscarinic

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23
Q

Benztropine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-muscarinic

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24
Q

Scopolamine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-muscarinic

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25
Q

Edrophonium: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-cholinesterase

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26
Q

Tolterodine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-muscarinic

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27
Q

Trospium: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-muscarinic

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28
Q

Rivastigmine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-cholinesterase

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29
Q

Homatropine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-muscarinic

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30
Q

Pyridostigmine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Anti-cholinesterase

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31
Q

Carbachol: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?

A

Direct cholinergic agonist

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32
Q

Where does botulinum toxin act?

A

Botulinum toxin inhibits release of ACh from presynaptic nerve terminals causing paralysis.

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33
Q

The neurotransmitter of choice for all pre-ganglionic synapses:

A

ACh

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34
Q

Receptor type found in all autonomic ganglia:

A

Nicotinic

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35
Q

The adrenal medulla is innervated by what arm of the autonomic nervous system?

A

Sympathetic, but the fibers are cholinergic

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36
Q

Where are nicotinic receptors found? What kind of receptor are they?

A

All autonomic ganglia are nicotinic.

These are ligand-gated Na+ channels

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37
Q

What kind of receptor are muscarinic receptors?

A

G-protein coupled.

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38
Q

Where are muscarinic receptors found?

A

Parasympathetic post-ganglionic target organs

Sympathetic sweat glands

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39
Q

Direct cholinergic agonist used to treat post-operative ileus and urinary retention:

A

Bethanechol

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40
Q

Direct cholinergic agonist used in treatment of acute closure glaucoma:

A

Carbachol

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41
Q

This drug is a direct cholinergic agonist and is used to stimulate sweat / tears / saliva secretion.

A

Pilocarpine

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42
Q

Which direct cholinergic agent is resistant to AChE?

A

Pilocarpine

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43
Q

This anti-cholinesterase penetrates the BBB.

These do not:

A

Physostigmine Passes the BBB.

NeOstigmine (NO), Pyridostigmine = pyridNOstigmine do NOT cross the BBB

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44
Q

Drug used in treatment of atropine OD:

A

Physostigmine (“phyxes” it)

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45
Q

Drug used in diagnosis of myasthenia gravis (generic and brand names):

A

Echothiophate = Tensilon

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46
Q

Drug used in treatment of myasthenia gravis, has a long half life. T/F: This drug crosses the BBB.

A

Pyridostigmine, does not cross the BBB.

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47
Q

What kind of drug is echothiophate? What is it used for?

A

AChE inhibitor, used in glaucoma.

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48
Q

Mechanism of action of organophosphate poisoning? Antidote?

A

Organophosphates = irreversible AChE inhibitors. Give atropine to antagonize parasympathetics, give pralidoxime to regenerate AChE.

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49
Q

Anti-cholinesterases FDA approved for Alzheimer disease (3):

A

Donepezil
Rivastigmine
Galantamine

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50
Q

Three topical drugs used to induce mydriasis:

A

Homotropine
Tropicamide
Cyclopent

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51
Q

This drug is used to treat EPS and is helpful in Parkinson disease:

A

Benztropine

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52
Q

Name 3 huge medication classes with anti-cholinergic effects:

A

H1 blockers (diphenhydramine, doxylamine, chlorpheniramine)
Neuroleptics
TCAs
Amantadine

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53
Q

5 anti-muscarinics used to treat urge incontinence:

A

Oxybutynin
Tolteridine
Darifenacin / Solifenacin
Trospium

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54
Q

The synthesis of catecholamines starts with this molecule:

A

Phenylalanine

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55
Q

The enzyme that converts phenylalanine to tyrosine is:

Deficiency of this enzyme causes what disease?

A

Phenylalanine hydroxylase.

PKU = defective phenylalanine hydroxylase

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56
Q

Tyrosine is converted to dopa with this enzyme. Where did the tyrosine come from?

A

Tyrosine hydroxylase. Tyrosine was made from phenylalanine.

57
Q

Dopa is converted to dopamine by this enzyme. What drug inhibits this conversion?

A

Dopa decarboxylase is the enzyme,

Carbidopa inhibits the conversion

58
Q

In the synthesis of catecholamines, where is vitamin B6 required? What about vitamin C?

A

Vitamin B6 is needed for dopa -> dopamine.

Vitamin C is needed for dopamine -> NE.

59
Q

The conversion of NE to Epi requires this co-factor:

A

SAM

60
Q

The enzyme that converts NE to Epi? This hormone encourages this conversion. Co-factor required?

A

Phenylalanine N-methyltransferase. Cortisol helps NE -> Epi. SAM is needed.

61
Q

Where does melanin come from?

A

Dopa

62
Q

Which vitamin is needed to make dopamine?

A

B6

63
Q

Which vitamin is needed to make NE?

A

Vitamin C

64
Q

Sympathetic receptor for vascular smooth muscle contraction:

A

a1

65
Q

Sympathetic receptor responsible for decreased sympathetic outflow. This is coupled to which G protein?

A

a2, Gi coupled

66
Q

Sympathetic receptor that modulates heart rate and contractility:

A

b1

67
Q

Sympathetic receptor that bronchodilates and vasodilates:

A

b2

68
Q

Gq coupled receptors include:

A

q-C HAV 1M&M:
H1, a1, V1
M1, M3

69
Q

Gi coupled receptors include:

A

MAD 2’s

M2, a2, D2

70
Q

The second messenger for Gq coupled receptor:

Which protein kinase is associated with the Gq cascade?

A

Phospholipase C -> PIP2 -> DAG / IP3

Protein kinase C

71
Q

Gs and Gi are coupled to this molecule:

A

Adenylyl cyclase

72
Q

Protein kinase for Gs and Gi?

Protein kinase for Gq?

A

Gs and Gi are protein kinase A,

Gq is protein kinase C

73
Q

M1 parasympathetic receptors are found mostly in this organ system:

A

Gut

74
Q

M2 parasympathetic receptors are found mainly in the:

A

Heart

75
Q

Parasympathetic receptor whose activation causes everything to leak:

A

M3

76
Q

Receptor activation relaxes renal vascular smooth muscle:

A

D1

77
Q

Three autoreceptors on noradrenergic terminals:

A

a2, m2, AT2

78
Q

Two drugs that block the release of NE from nerve terminals:

A

Guanethidine

Bretylium

79
Q

Three drugs that encourage NE release:

A

Amphetamines
Tyramine
Ephedrine

80
Q

Two drugs that block NE reuptake

A

Cocaine

TCAs

81
Q

Drug that blocks the uptake of choline into a nerve terminal:

A

Hemicholinium

82
Q

Drug that keeps ACh from being packaged into vesicles:

A

Vesamicol

83
Q

What is the mechanism of action of black widow toxin? What kind of paralysis does this cause?

A

Black widow toxin encourages release of all ACh from nerve terminals, causes spastic paralysis.

84
Q

Botox causes what kind of paralysis, what mechanism?

A

Flaccid, it prevents ACh from being released.

85
Q

Main effect of a1 adrenergic receptor stimulation:

A

Vascular smooth muscle contraction.

86
Q

Main effect of a2 receptor stimulation is:

A

Modulatory. Most a2 receptors are autoreceptors, main outcome of stimulation is to turn down sympathetic tone.

87
Q

b1 receptors are found mainly in this organ. What is the overall effect of activating them?

A

b1 are in the heart mostly, get an increase in myocardial contractility, heart rate, and conduction through the AV node.

88
Q

b2 receptors have two huge effects when activated:

A

Bronchodilation, vasodilation.

89
Q

Stimulation of this receptor relaxes renal vascular smooth muscle:

A

D1

90
Q

Activation of this sympathetic receptor decreases insulin release. A different one increases insulin release, what is it?

A

a2 decreases insulin, b2 increases insulin release.

91
Q

Sympathetic receptor that mediates mydriasis:

A

a1

92
Q

Sympathetic receptor that blocks NE release:

A

a2

93
Q

Sympathetic receptor that mediates bronchodilation:

A

b2

94
Q

Sympathetic receptor that causes increase in cardiac contractility:

A

b1

95
Q

Sympathetic receptor that mediates bladder muscle contraction:

A

a1

96
Q

Sympathetic receptor that increases renin:

A

b1

97
Q

Sympathetic receptor that decreases uterine tone:

A

b2

98
Q

Sympathetic receptors (2) that increase lipolysis:

A

b1, b2

99
Q

Sympathetic receptor that vasodilates:

A

b2

100
Q

Activation of this sympathetic receptor causes an increase in peripheral resistance. Another causes a decrease in PR.

A

a1, b2.

101
Q

Drug that has a1, a2, b1, and b2 activity.

A

Epi

102
Q

Drug of choice for anaphylactic shock:

A

Epi

103
Q

Drug of choice for cardiogenic shock:

Why?

A

Dobutamine

Has b1 activity mostly, is an inotrope and chronotrope.

104
Q

Drug of choice in septic shock:
Receptors:
What is the big risk of using this drug in someone with shock?

A

NE
a1 and a2 activity w/o much b2.
Decreases renal perfusion.

105
Q

Drug with a1 and a2 specificity:

A

NE

106
Q

Drug with b1 and b2 specificity:

A

Isoproterenol

107
Q

Drug that acts at a1 > a2 receptors:

A

Phenylephrine

108
Q

Drugs with mainly b2 > b1 activity:

A

Albuterol, salmetrol, terbutaline

109
Q

Drug that works almost purely at b2 receptors:

A

Ritodrine

110
Q

Receptors stimulated by phenylephrine:

A

a1, a2

111
Q

Receptors stimulated by NE

A

a1, a2, some b1

112
Q

Receptors stimulated by isoproterenol:

A

b1, b2

113
Q

Dobutamine stimulates:

A

b1 mostly

114
Q

This drug causes short QT and can make bradyarrhythmias worse:

A

Isoproterenol

115
Q

This drug is used in cardiac stress testing:

A

Dobutamine

116
Q

This drug reduces premature uterine contractions:

A

Ritodrine

117
Q

Name 3 indirect sympathomimetics:

Which is also a reuptake inhibitor?

A

Amphetamines
Ephedrine
Cocaine *

118
Q

What is a sympathoplegic? Can you name 2? What are these drugs used for?

A

An a2 adrenergic agonist. Clonidine, a-methyldopa. Used in malignant HTN.

119
Q

Name 2 non-selective a-blockers:

Which is irreversible?

A

Phenoxybenzamine *

Phentolamine

120
Q

You give this drug to people with a pheo before you try to remove their tumor:

A

Phenoxybenzamine

121
Q

Sympathetic blockers ending in -osin tend to block this receptor:

A

a1

122
Q

Prazosin, terazosin, doxazosin, and tamulosin are used to treat…

A

HTN and urinary retention

123
Q

Prazosin, terazosin, doxazosin, and tamulosin act to block this receptor:

A

a1

124
Q

Mirtazapine blocks what sympathetic receptor?

A

a2

125
Q

Name 3 non-selective b-blockers:

A

Propranolol, timolol, nadolol

126
Q

Two drugs that block both a1 and b1:

These drugs overall have what effect on the heart?

A

Carvedilol, labetalol.

Decrease work of the heart – a1 stimulation tends to drop PR, b1 stimulation drops HR and contractility.

127
Q

4 b1-selective blockers:

A

Metoprolol
Atenolol
Esmolol
Nebivolol

128
Q

Two drugs that are weak b1 / b2 agonists and therefore act as b-blockers:
These drugs are particularly useful in what scenario?

A

Acebutolol, pindolol
Useful in people w/ HTN and bradycardia: b1 stimulation helps maintain HR at the same time as b2 stimulation drops the BP

129
Q

Receptor stimulated by this sympathomimetic:

Clonidine

A

a2

130
Q

Receptor stimulated by this sympathomimetic:

Dopamine

A

d1&2, b2, b1, a2, a1 as dose increases progressively

131
Q

Receptor stimulated by this sympathomimetic:

Phenylephrine

A

a1 > a2

132
Q

Receptor stimulated by this sympathomimetic:

Albuterol

A

b2 (some b1)

133
Q

Receptor stimulated by this sympathomimetic:

NE

A

a1, a2, b1

134
Q

Receptor stimulated by this sympathomimetic:

Isoproterenol

A

b1, b2

135
Q

Receptor stimulated by this sympathomimetic:

Epi

A

a1, a2, b1, b2

136
Q

Receptor stimulated by this sympathomimetic:

Dobutamine

A

b1

137
Q

Receptor stimulated by this sympathomimetic:

Terbutaline

A

b2 (some b1)

138
Q

This drug is used to halt premature labor:

A

Terbutaline

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