Autonomic Pharmacology Flashcards
(138 cards)
1
Q
Symptoms of excess parasympathetic activity?
A
Diarrhea Urinary retention Miosis / ciliary muscle contraction Bradycardia BronchoSPASM Excitation (muscles and CNS) Lacrimation Salivation Sweating
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)
3
Q
Effect of anti-muscarinics on heart rate?
A
Inhibition of vagal tone = tachycardia
4
Q
Three anti-muscarinic drugs used topically for pupillary dilation:
A
Homatropine
Tropicamide
Cyclopent.
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).
6
Q
This drug is helpful in Parkinson’s and in tx of EPS from antipsychotic use:
A
Benztropine
7
Q
Antimuscarinic used in tx of motion sickness:
A
Scopolamine
8
Q
Antimuscarinic for COPD and asthma (2):
A
Ipratropium
Tiotropium
9
Q
Antimuscarinics used to help increase urinary retention in urge incontinence (5):
A
Oxybutynin Tolterodine Darifenacin Solifenacin Trospium
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
11
Q
This drug helps decrease oral secretions when given parenterally:
A
Glycopyrrolate
12
Q
Physostigmine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?
A
Anti-cholinesterase
13
Q
Pilocarpine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?
A
Direct cholinergic agonist
14
Q
Oxybutynin: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?
A
Anti-muscarinic
15
Q
Atropine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?
A
Direct cholinergic agonist
16
Q
Donepezil: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?
A
Anti-cholinesterase
17
Q
Pralidoxime: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?
A
Trick question!
Cholinesterase RE-GENERATOR.
18
Q
Bethanecol: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?
A
Direct cholinergic agonist
19
Q
Neostigmine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?
A
Anti-cholinesterase
20
Q
Darifenacin: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?
A
Anti-muscarinic
21
Q
Ipratropium: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?
A
Anti-muscarinic
22
Q
Tropicamide: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?
A
Anti-muscarinic
23
Q
Benztropine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?
A
Anti-muscarinic
24
Q
Scopolamine: Direct cholinergic agonist, anticholinesterase, or anti-muscarinic?
A
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
