Autonomic Pharmacology Flashcards Preview

USMLE Step 1 > Autonomic Pharmacology > Flashcards

Flashcards in Autonomic Pharmacology Deck (138)
1

Symptoms of excess parasympathetic activity?

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

2

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

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)

3

Effect of anti-muscarinics on heart rate?

Inhibition of vagal tone = tachycardia

4

Three anti-muscarinic drugs used topically for pupillary dilation:

Homatropine
Tropicamide
Cyclopent.

5

Atropine is used mainly for (2):

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

6

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

Benztropine

7

Antimuscarinic used in tx of motion sickness:

Scopolamine

8

Antimuscarinic for COPD and asthma (2):

Ipratropium
Tiotropium

9

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

Oxybutynin
Tolterodine
Darifenacin
Solifenacin
Trospium

10

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

Scopolamine
Also used for motion sickness

11

This drug helps decrease oral secretions when given parenterally:

Glycopyrrolate

12

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

Anti-cholinesterase

13

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

Direct cholinergic agonist

14

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

Anti-muscarinic

15

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

Direct cholinergic agonist

16

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

Anti-cholinesterase

17

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

Trick question!
Cholinesterase RE-GENERATOR.

18

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

Direct cholinergic agonist

19

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

Anti-cholinesterase

20

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

Anti-muscarinic

21

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

Anti-muscarinic

22

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

Anti-muscarinic

23

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

Anti-muscarinic

24

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

Anti-muscarinic

25

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

Anti-cholinesterase

26

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

Anti-muscarinic

27

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

Anti-muscarinic

28

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

Anti-cholinesterase

29

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

Anti-muscarinic

30

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

Anti-cholinesterase

31

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

Direct cholinergic agonist

32

Where does botulinum toxin act?

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

33

The neurotransmitter of choice for all pre-ganglionic synapses:

ACh

34

Receptor type found in all autonomic ganglia:

Nicotinic

35

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

Sympathetic, but the fibers are cholinergic

36

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

All autonomic ganglia are nicotinic.
These are ligand-gated Na+ channels

37

What kind of receptor are muscarinic receptors?

G-protein coupled.

38

Where are muscarinic receptors found?

Parasympathetic post-ganglionic target organs
Sympathetic sweat glands

39

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

Bethanechol

40

Direct cholinergic agonist used in treatment of acute closure glaucoma:

Carbachol

41

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

Pilocarpine

42

Which direct cholinergic agent is resistant to AChE?

Pilocarpine

43

This anti-cholinesterase penetrates the BBB.
These do not:

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

44

Drug used in treatment of atropine OD:

Physostigmine ("phyxes" it)

45

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

Echothiophate = Tensilon

46

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

Pyridostigmine, does not cross the BBB.

47

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

AChE inhibitor, used in glaucoma.

48

Mechanism of action of organophosphate poisoning? Antidote?

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

49

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

Donepezil
Rivastigmine
Galantamine

50

Three topical drugs used to induce mydriasis:

Homotropine
Tropicamide
Cyclopent

51

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

Benztropine

52

Name 3 huge medication classes with anti-cholinergic effects:

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

53

5 anti-muscarinics used to treat urge incontinence:

Oxybutynin
Tolteridine
Darifenacin / Solifenacin
Trospium

54

The synthesis of catecholamines starts with this molecule:

Phenylalanine

55

The enzyme that converts phenylalanine to tyrosine is:
Deficiency of this enzyme causes what disease?

Phenylalanine hydroxylase.
PKU = defective phenylalanine hydroxylase

56

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

Tyrosine hydroxylase. Tyrosine was made from phenylalanine.

57

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

Dopa decarboxylase is the enzyme,
Carbidopa inhibits the conversion

58

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

Vitamin B6 is needed for dopa -> dopamine.
Vitamin C is needed for dopamine -> NE.

59

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

SAM

60

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

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

61

Where does melanin come from?

Dopa

62

Which vitamin is needed to make dopamine?

B6

63

Which vitamin is needed to make NE?

Vitamin C

64

Sympathetic receptor for vascular smooth muscle contraction:

a1

65

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

a2, Gi coupled

66

Sympathetic receptor that modulates heart rate and contractility:

b1

67

Sympathetic receptor that bronchodilates and vasodilates:

b2

68

Gq coupled receptors include:

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

69

Gi coupled receptors include:

MAD 2's
M2, a2, D2

70

The second messenger for Gq coupled receptor:
Which protein kinase is associated with the Gq cascade?

Phospholipase C -> PIP2 -> DAG / IP3
Protein kinase C

71

Gs and Gi are coupled to this molecule:

Adenylyl cyclase

72

Protein kinase for Gs and Gi?
Protein kinase for Gq?

Gs and Gi are protein kinase A,
Gq is protein kinase C

73

M1 parasympathetic receptors are found mostly in this organ system:

Gut

74

M2 parasympathetic receptors are found mainly in the:

Heart

75

Parasympathetic receptor whose activation causes everything to leak:

M3

76

Receptor activation relaxes renal vascular smooth muscle:

D1

77

Three autoreceptors on noradrenergic terminals:

a2, m2, AT2

78

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

Guanethidine
Bretylium

79

Three drugs that encourage NE release:

Amphetamines
Tyramine
Ephedrine

80

Two drugs that block NE reuptake

Cocaine
TCAs

81

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

Hemicholinium

82

Drug that keeps ACh from being packaged into vesicles:

Vesamicol

83

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

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

84

Botox causes what kind of paralysis, what mechanism?

Flaccid, it prevents ACh from being released.

85

Main effect of a1 adrenergic receptor stimulation:

Vascular smooth muscle contraction.

86

Main effect of a2 receptor stimulation is:

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

87

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

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

88

b2 receptors have two huge effects when activated:

Bronchodilation, vasodilation.

89

Stimulation of this receptor relaxes renal vascular smooth muscle:

D1

90

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

a2 decreases insulin, b2 increases insulin release.

91

Sympathetic receptor that mediates mydriasis:

a1

92

Sympathetic receptor that blocks NE release:

a2

93

Sympathetic receptor that mediates bronchodilation:

b2

94

Sympathetic receptor that causes increase in cardiac contractility:

b1

95

Sympathetic receptor that mediates bladder muscle contraction:

a1

96

Sympathetic receptor that increases renin:

b1

97

Sympathetic receptor that decreases uterine tone:

b2

98

Sympathetic receptors (2) that increase lipolysis:

b1, b2

99

Sympathetic receptor that vasodilates:

b2

100

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

a1, b2.

101

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

Epi

102

Drug of choice for anaphylactic shock:

Epi

103

Drug of choice for cardiogenic shock:
Why?

Dobutamine
Has b1 activity mostly, is an inotrope and chronotrope.

104

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

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

105

Drug with a1 and a2 specificity:

NE

106

Drug with b1 and b2 specificity:

Isoproterenol

107

Drug that acts at a1 > a2 receptors:

Phenylephrine

108

Drugs with mainly b2 > b1 activity:

Albuterol, salmetrol, terbutaline

109

Drug that works almost purely at b2 receptors:

Ritodrine

110

Receptors stimulated by phenylephrine:

a1, a2

111

Receptors stimulated by NE

a1, a2, some b1

112

Receptors stimulated by isoproterenol:

b1, b2

113

Dobutamine stimulates:

b1 mostly

114

This drug causes short QT and can make bradyarrhythmias worse:

Isoproterenol

115

This drug is used in cardiac stress testing:

Dobutamine

116

This drug reduces premature uterine contractions:

Ritodrine

117

Name 3 indirect sympathomimetics:
Which is also a reuptake inhibitor?

Amphetamines
Ephedrine
Cocaine *

118

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

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

119

Name 2 non-selective a-blockers:
Which is irreversible?

Phenoxybenzamine *
Phentolamine

120

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

Phenoxybenzamine

121

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

a1

122

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

HTN and urinary retention

123

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

a1

124

Mirtazapine blocks what sympathetic receptor?

a2

125

Name 3 non-selective b-blockers:

Propranolol, timolol, nadolol

126

Two drugs that block both a1 and b1:
These drugs overall have what effect on the heart?

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

127

4 b1-selective blockers:

Metoprolol
Atenolol
Esmolol
Nebivolol

128

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

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

Receptor stimulated by this sympathomimetic:
Clonidine

a2

130

Receptor stimulated by this sympathomimetic:
Dopamine

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

131

Receptor stimulated by this sympathomimetic:
Phenylephrine

a1 > a2

132

Receptor stimulated by this sympathomimetic:
Albuterol

b2 (some b1)

133

Receptor stimulated by this sympathomimetic:
NE

a1, a2, b1

134

Receptor stimulated by this sympathomimetic:
Isoproterenol

b1, b2

135

Receptor stimulated by this sympathomimetic:
Epi

a1, a2, b1, b2

136

Receptor stimulated by this sympathomimetic:
Dobutamine

b1

137

Receptor stimulated by this sympathomimetic:
Terbutaline

b2 (some b1)

138

This drug is used to halt premature labor:

Terbutaline