Autonomic Drugs - Unit 3 Flashcards
1
Q
post-ganglionic parasympathetic fibers release _____
A
Acetylcholine
2
Q
post-ganglionic sympathetic fibers release ____
A
Norepinephrine
3
Q
Chromaffin cells release ________
A
catecholamines: Epi+Norepi
(~80% Epinephrine ~20% Norepinephrine)
4
Q
Chromaffin cells are stimulated by the (sympathetic/parasympathetic) nervous system
A
sympathetic
5
Q
Classically, Preganglionic sympathetics release ________, and post ganglionic sympathetics release _______
A
Preganglionic symps: Acetylcholine
Postganglionic symps: Norepinephrine
6
Q
Classically, Preganglionic parasympathetics release ________, and postganglionic parasympathetics release _______
A
Preganglionic parasympathetics: Acetylcholine
postganglionic parasympathetics: Acetylcholine
7
Q
Sympathetic output is generally (discrete/diffuse) while parasympathetic output is (discrete/diffuse)
A
sympathetic: diffuse
parasympathetic: discrete
8
Q
Exceptions: for renal vessels, Pregang symps release ________, and postgang symps release _______
A
Preganglionic symps: Acetylcholine
Postganglionic symps: Dopamine!
9
Q
Which is degraded rapidly once released from a nerve terminal? (NE/ACh)
A
ACh
10
Q
Name 2 drugs that inhibit NE re-uptake:
A
- Cocaine
2. Tricyclic antidepressants, TCAs
11
Q
How does botulinum toxin work?
A
Blocks ACh release
12
Q
Why is an Nn receptor a bad target for ANS drugs?
A
It is in both the Symp and Parasymp systems!
13
Q
M1, M3, M5 are all (Gq/Gi/Gs) coupled
A
Gq, (increase IP3, Ca2+, DAG)
14
Q
M2, M4 are (Gq/Gi/Gs) coupled
A
Gi (decrease cAMP)
15
Q
Gs, stimulatory proteins (increase/decrease) cAMP
A
increase cAMP
16
Q
Gi, inhibitory proteins (increase/decrease) cAMP
A
decrease cAMP
17
Q
Which Muscarinic receptor is predominant in slowing heart rate?
A
M2
18
Q
Which Muscarinic receptor is common in the exocrine glands, blood vessels and smooth muscle?
A
M3
19
Q
Which Muscarinic receptor is predominant in creating myosis of the eye?
A
M3
20
Q
muscarinic receptors respond to release of (Epi/Norepi/ACh)
A
ACh
21
Q
Which Muscarinic receptor is predominant in bronchoconstriction?
A
M3
22
Q
What enzyme is inhibited by INDIRECT acting cholinomimetics?
A
acetylcholine esterase
23
Q
Drug: Direct-acting muscarinic cholinomimetic for Post-operative and neurogenic ileus and urinary retention
A
Bethanechol
24
Q
What makes Inocybe genus and Clitocybe genus of mushrooms toxic?
A
too much muscarine
25
Drug: Direct-acting muscarinic cholinomimetic for Glaucoma (ACh activates sphincter and ciliary muscles of eye
Pilocarpine
26
Drug: Direct-acting muscarinic cholinomimetic for Dry mouth Esp. Sjogren's (and post- radiation therapy) increased salivation
Cevimeline
27
Drug: ACh esterase inhibitor, a volatile nerve gas
Sarin
28
Drug: ACh esterase inhibitor, an insecticide
Parathion
29
Drug: ACh Esterase inhibitor, covalently carbamylates AChE, for myasthenia gravis and Post-op and neurogenic ileus; urinary retention
Neostigmine
30
If you are exposed to Sarin gas what you like be be given quickly before irreversible aging?
Pralidoxime
31
In myasthenia gravis, muscle weakness is caused by ________ that block acetylcholine receptors
auto-immune antibodies
32
What are the SLUDGE side effects that result from too much cholinergic stimulation?
```
Salivation
Lacrimation
Urination
Defication
GI distress
Emesis
```
33
Which 2 drug classes have the SLUDGE effects?
1. Muscarinic cholinomimetics
| 2. AChE inhibitors
34
Drug: AChE inhibitor for Alzheimer's (amplifies endogenous ACh in brain)
Donepezil
35
2 drugs: indirect acting AChE inhibitor for Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
1. Physostigmine (short acting)
| 2. Echothiophate (long acting)
36
Too much neostigmine can lead to flooding the ACh and paralysis. What do you use to check the effect of the neostigmine?
Edrophonium
37
List the tertiary amine, anti-muscarinics (9) which generally block muscarinic function
```
Eye:
1. Atropine
2. Tropicamide
CNS:
3. Benztropine
4. Scopolamine
Bronchi:
5. Ipratropium
6. Tiotropium
GI:
7. Glycopyrrolate
8. Dicyclomine
GU:
9. Tolterodine
```
38
Paralysis of the ciliary muscles of the eye is called _______
cycloplegia
39
Parasympathetic innervation drives pupillary (constriction/dilation)
constriction
40
Sympathetic innervation drives pupillary (constriction/dilation)
dilation
41
Mydriasis is (constriction/dilation) of the pupil
dilation
42
A muscarinic antagonist (promotes/ inhibits) sweating
inhibits! (receptors are muscarinic cholinergic)
43
Drug: Tertiary amine, anti-muscarinics
| Targets CNS For parkinson's, penetrates BBB
Benztropine
44
2 Drug: Tertiary amine, anti-muscarinics
| For Mydriasis and cycloplegia
1. Atropine
| 2. Tropicamide
45
Drug: Tertiary amine, anti-muscarinics
| Targets CNS for Prevention or reduction of motion sickness, penetrates BBB
Scopolamine
46
2 Drugs: Tertiary amine, anti-muscarinics
| Target G.I. tract to reduce transient hypermobility
1. Glycopyrrolate
| 2. Dicyclomine
47
Drug: Tertiary amine, anti-muscarinics
| For postoperative bladder spams, incontinence
Tolterodine
48
2 Drug: Tertiary amine, anti-muscarinics
| For bronchidilation in asthma, COPD
1. Ipratropium
| 2. Tiotropium
49
Two ganglion blockers that block Nn receptors and sympathetic tone are
1. Hexamethonium
| 2. Mecamylamine
50
What are 1. Hexamethonium and 2. Mecamylamine used for?
"Bloodless" field surgery, the ganglionic blockers decrease blood pressure
51
Two neuromuscular drugs that are non-depolarizing blockers at Nm junctions are:
1. Tubocurarine
| 2. Mivacurium
52
When succinylcholine is administered, it causes initial (paralysis/ fasciculations) followed by (paralysis/ fasciculations)
Produces initial fasciculations and then paralysis within 1 minute.
53
What do 1. Tubocurarine and 2. Mivacurium do?
Block Nm receptors, skeletal muscle relaxation during surgery or mechanical ventilation
54
Accommodation of the eye is purely under (sympathetic/parasympathetic) control
parasympathetic
55
Blurred vision is a mark of a (muscarinic/ adrenergic)
muscarinic
56
To look in someone's eye, dilate it with (Atropine/Tropicamide)
Tropicamide, dialates eye for less time than
| Atropine
57
To treat parkinson's use (Benztropine/Scopolamine)
Benztropine
58
To reduce motion sickness use (Benztropine/Scopolamine)
Scopolamine
59
To treat cholinergic poisoning like muscarine from mushrooms use _______
Atropine
60
Cholinesterase inhibitors are used to reverse the effects of (depolarizing/ non-depolarizing) blockers
non-depolarizing
61
Botulinum toxin as botox is used to (block/ cause) muscle tone
blocks muscle tone: relaxes
62
The synthesis of Norepiniphrine begins with (arginine/ /Dopamine/ tyrosine/ DOPA)
Tyrosine -> DOPA -> dopamine -> N.E.
63
The effects of N.E. at a neuron are stopped by the action of the (uptake 1/ uptake2) transporter
uptake 1
64
N.E. is destroyed in the cell by (acetylcholine esterase/ mono amine oxidase/ PNMT)
MAO on the mitochondria
65
which is a neurotransmitter (N.E./ Epi)
N.E.
66
Which is a neurohormone (N.E./ Epi)
Epi
67
Which adrenergic receptor causes sm. muscle contraction including vasoconstriction(α1/ α2/ β1/ β2/ β3/ D1)
α1
68
Which adrenergic receptor causes increased heart inotropy (α1/ α2/ β1/ β2/ β3/ D1)
β1
69
Which adrenergic receptor causes sm. muscle relaxation including arteriole dilation(α1/ α2/ β1/ β2/ β3/ D1)
β2
70
Which adrenergic receptor inhibits neurotransmitter N.E. release (α1/ α2/ β1/ β2/ β3/ D1)
α2
71
Which adrenergic receptor causes lipolysis (α1/ α2/ β1/ β2/ β3/ D1)
β3
72
Which adrenergic receptor causes bronchiole relaxation (α1/ α2/ β1/ β2/ β3/ D1)
β2
73
Which receptor causes renal, mesenteric and cerebral arteriole dilation? (α1/ α2/ β1/ β2/ β3/ D1)
D1, dopamine as neurotransmitter
74
Phenylephrine is an (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
α1 agonist
| treats nasal congestion, and postural hypotention
75
Prazosin is an (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
α1 antagonist
| treats primary hypertension and BPH
76
Clonidine is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
α2 agonist in CNS
| treats Hypertension; shock; withdrawal from drug dependence
77
Fenoldopam is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
D1 agonist
| Increases blood flow at renal, mesenteric, and cerebral arteries
78
Dobutamine is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
β1, agonist
| treats Cardiac decompensation; shock; heart block
79
Atenolol and Metoprolol are both (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
β1 antagonists
| They treat HTN, Angina, Arrythmias, CHF
80
Albuterol and terbutaline are a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
β2 Agonist
Albuterol: bronchospasm; mild asthma; COPD
Terbutaline: above + prevents premature labor
81
Isoproterenol is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
β1 and β2 agonist, non-selective
| used to treat shock and heart block
82
Propranolol is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
β1 and β2 antagonist, non-selective
| use to treat Angina, Hypertension and Arrythmias
83
With low concentration of epinephrin at muscles, the (α1/β2) receptor trumps leading to (dilation/ contraction) of vascular smooth muscle
β2, dilation
with low epi
fight or flight
84
With high concentration of epinephrin at muscles, the (α1/β2) receptor trumps leading to (dilation/ contraction) of vascular smooth muscle
α1, contraction
| raises B.P.
85
Increases release of cytoplasmic N.E. (cocaine/ tyramine)
tyramine
| similar to amphetamine
86
Prevents N.E. re-uptake (cocaine/ tyramine/ amphetamine)
cocaine
87
short term tolerance is called ________
tachyphylaxis
88
increased blood flow at renal, mesenteric and cerebral vasculature (low dose/ medium dose/ high dose) Dopamine
low dose dopamine
89
has direct heart β1 inotropy effects and indirect release of N.E. (low dose/ medium dose/ high dose) Dopamine
medium dose dopamine
90
has direct α1 vascular effect and indirect N.E. release causing vasoconstriction (low dose/ medium dose/ high dose) Dopamine
high dose dopamine
91
acts at the D1 receptor only, increases renal blood flow (Dopamine/ Fenoldopam)
Fenoldopam
92
With bolus N.E.
H.R. (increases/decreases)
B.P. (increases/decreases)
TPR (increases/decreases)
H.R. decreases due to vagal feedback
B.P. increases α1 constriction
TPR increases α1 constriction
93
With bolus epinephrine
H.R. (increases/decreases)
B.P. (increases/decreases)
TPR (increases/decreases)
H.R. increases β1 increases inotropy
B.P. increases β1 increases inotropy
TPR decreases β2 sm. muscle dilation
94
With bolus isoproterenol
H.R. (increases/decreases)
B.P. (increases/decreases)
TPR (increases/decreases)
H.R. increases due to β1 + feedback
B.P. decreases β2 sm. muscle dilation
TPR decreases β2 sm. muscle dilation
95
epi pens are used for anaphylaxis for their action on (α1/ α2/ β1/ β2/ β3/ D1) receptors
B2, for bronchodilation
96
For control of post-partum bleeding, and alpha agonist (Ergonovine/ Ergotamine/ Bromocriptine)
Ergonovine
97
For control of acute migraines, both and alpha agonsit and a 5HT agonist (Ergonovine/ Ergotamine/ Bromocriptine)
Ergotamine
98
For control of parkinsons and hyperprolactenemia (Ergonovine/ Ergotamine/ Bromocriptine)
Bromocriptine, a dopamine agonist
99
Which CNS α2 agonist is a pro-drug? (clonidine/ α-methyl dopa)
α-methyl dopa
| crosses BBB
100
Both treat hypertension, which treats drug dependance (clonidine/ α-methyl dopa)
clonidine
101
Which β2 agonist is better for asthma? (terbutaline/ albuterol)
albuterol
102
Which β2 agonist relaxes the uterus to prevent pre-mature labor? (terbutaline/ albuterol)
terbutaline
103
β2 agonist terbutaline and albuterol will cause (vasoconstriction/ vasodilation)
vasodilation
104
Non-selective β1+β2 blocker, first generation
| Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol
Propranolol and Timolol
105
β1 selective blocker, second generation (Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol)
Metoprolol + Atenolol + Bisproprolol
106
Non-selective β1+β2 blocker, also blocks α1, third generation
(Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol)
Labetalol and Carvedilol
107
β1 selective blocker, plus Ca2+ channel blocker, third generation
(Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol)
Betaxolol
108
Why use 2nd or 3rd gen beta blockers in pts. with heart failure?
protect against sympathetic drive
109
Beta blockers are partial "contraceptives" due to their side effect of _______ ______
sexual dysfunction
110
Phentolamine and Phentoxybenzamine are an (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
α1 and α2 antagonist
| for Pheochromocytoma, Raynaud's and frostbite
111
Which is better treated with an alpha blocker? (athlosclerotic dz./ vasospastic dz)
vasospastic, such as Raynaud's
112
postural hypotension is associated with (α blockers/ β blockers)
α blockers
113
Which nerve ending blocker prevents synthesis of N.E.
| α-methyltyrosine/ reserpine/ guanethidine
α-methyltyrosine
114
Which nerve ending blocker prevents the packaging of N.E.
| α-methyltyrosine/ reserpine/ guanethidine
reserpine and guanethidine
115
Which nerve ending blocker can be used for hypertension
| (α-methyltyrosine/ reserpine/ guanethidine
reserpine and guanethidine
116
Which nerve ending blocker stops the vesicular transporter of N.E. leading to empty vesicles
(α-methyltyrosine/ reserpine/ guanethidine)
reserpine
117
Which nerve ending blocker is preferentially packaged into vesicles, blocking N.E. transport
(α-methyltyrosine/ reserpine/ guanethidine)
guanethidine
118
M1, M3, M5 are all (Gq/Gi/Gs) coupled
Gq, (increase IP3, Ca2+, DAG)
