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 (2 each for eye, CNS, Bronchi, G; 1 for GU )
```
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 eye's ciliary muscles (and thus lens) is called _______
cycloplegia
39
Parasympathetic innervation drives pupillary (constriction/dilation)
constriction
hint: Mio*sis
40
Sympathetic innervation drives pupillary (constriction/dilation)
dilation
hint: Mydria*sis
41
A muscarinic antagonist (promotes/ inhibits) sweating
inhibits! (receptors are muscarinic cholinergic)
hint: dry as a bone
42
Drug: Tertiary amine, anti-muscarinics
| Targets CNS For parkinson's, penetrates BBB
Benztropine
43
2 Drug: Tertiary amine, anti-muscarinics
| For Mydriasis and cycloplegia
1. Atropine
| 2. Tropicamide
44
Drug: Tertiary amine, anti-muscarinics
| Targets CNS for Prevention or reduction of motion sickness, penetrates BBB
Scopolamine
45
2 Drugs: Tertiary amine, anti-muscarinics
| Target G.I. tract to reduce transient hypermobility
1. Glycopyrrolate
| 2. Dicyclomine
46
Drug: Tertiary amine, anti-muscarinics
| For postoperative bladder spams, incontinence
Tolterodine
47
2 Drug: Tertiary amine, anti-muscarinics
| For bronchidilation in asthma, COPD
1. Ipratropium
| 2. Tiotropium
48
Two ganglion blockers that block Nn receptors and sympathetic tone are
1. Hexamethonium
| 2. Mecamylamine
49
What are 1. Hexamethonium and 2. Mecamylamine used for?
"Bloodless" field surgery, bc ganglionic blockers that ↓ blood pressure
50
Two neuromuscular drugs that are non-depolarizing blockers at Nm junctions are:
1. Tubocurarine
2. Mivacurium
hint: crurare
51
When succinylcholine is administered, it causes initial (paralysis/ fasciculations) followed by (paralysis/ fasciculations)
Produces initial fasciculations and then paralysis within 1 minute.
52
What do 1. Tubocurarine and 2. Mivacurium do? When can they be used?
Block Nm receptors, skeletal muscle relaxation during surgery or mechanical ventilation
53
Accommodation of the eye is purely under (sympathetic/parasympathetic) control
parasympathetic
54
Blurred vision is a mark of a (muscarinic/ adrenergic)
muscarinic
55
To look in someone's eye, dilate it with (Atropine/Tropicamide)
Tropicamide!
hint: dilates eye for less time than
Atropine
56
To treat parkinson's use (Benztropine/Scopolamine)
Benztropine
57
To reduce motion sickness use (Benztropine/Scopolamine)
Scopolamine
58
To treat cholinergic poisoning like muscarine from mushrooms use _______
Atropine
59
Cholinesterase inhibitors are used to reverse the effects of (depolarizing/ non-depolarizing) blockers
non-depolarizing (closed blocked)
60
Botulinum toxin as botox is used to (block/ cause) muscle tone
blocks muscle tone: relaxes via SNAP25
61
The synthesis of Norepiniphrine begins with (arginine/ /Dopamine/ tyrosine/ DOPA)
Tyrosine -> DOPA -> dopamine -> N.E.
62
The effects of N.E. at a neuron are stopped by the action of the (uptake 1/ uptake2) transporter
uptake 1
63
N.E. is destroyed in the cell by (acetylcholine esterase/ mono amine oxidase/ PNMT)
MAO on the mitochondria
64
which is a neurotransmitter (N.E./ Epi)
N.E.
65
Which is a neurohormone (N.E./ Epi)
Epi
66
Which adrenergic receptor causes sm. muscle contraction including vasoconstriction(α1/ α2/ β1/ β2/ β3/ D1)
α1
67
Which adrenergic receptor causes increased heart inotropy (α1/ α2/ β1/ β2/ β3/ D1)
β1
68
Which adrenergic receptor causes sm. muscle relaxation including arteriole dilation(α1/ α2/ β1/ β2/ β3/ D1)
β2
69
Which adrenergic receptor inhibits neurotransmitter N.E. release (α1/ α2/ β1/ β2/ β3/ D1)
α2
70
Which adrenergic receptor causes lipolysis (α1/ α2/ β1/ β2/ β3/ D1)
β3
71
Which adrenergic receptor causes bronchiole relaxation (α1/ α2/ β1/ β2/ β3/ D1)
β2
72
Which receptor causes renal, mesenteric and cerebral arteriole dilation? (α1/ α2/ β1/ β2/ β3/ D1)
D1, dopamine as neurotransmitter
73
Phenylephrine is an (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
α1 agonist
| treats nasal congestion, and postural hypotention
74
Prazosin + tamsulosin are (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1) used to treat?
α1 antagonist (tamsulosin = 𝛂1A)
Prazosin = peripheral vasospasm
Tamsulosin/Flomax) = BPH
hint: treats primary hypertension and BPH; a2 antags useless in periphery
75
Clonidine is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
α2 agonist in CNS
| treats Hypertension; shock; withdrawal from drug dependence
76
Fenoldopam is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
D1 agonist
| Increases blood flow at renal, mesenteric, and cerebral arteries
77
Dobutamine is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
β1, agonist
| treats Cardiac decompensation; shock; heart block
78
Atenolol and Metoprolol are both (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
β1 antagonists
| They treat HTN, Angina, Arrythmias, CHF
79
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
80
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
81
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
82
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
83
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.
84
Increases release of cytoplasmic N.E. (cocaine/ tyramine)
tyramine
| similar to amphetamine
85
Prevents N.E. re-uptake (cocaine/ tyramine/ amphetamine)
cocaine
86
short term tolerance is called ________
tachyphylaxis
87
increased blood flow at renal, mesenteric and cerebral vasculature (low dose/ medium dose/ high dose) Dopamine
low dose dopamine
88
has direct heart β1 inotropy effects and indirect release of N.E. (low dose/ medium dose/ high dose) Dopamine
medium dose dopamine
89
has direct α1 vascular effect and indirect N.E. release causing vasoconstriction (low dose/ medium dose/ high dose) Dopamine
high dose dopamine
90
acts at the D1 receptor only, increases renal blood flow (Dopamine/ Fenoldopam)
Fenoldopam
91
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
92
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
93
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
94
epi pens are used for anaphylaxis for their action on (α1/ α2/ β1/ β2/ β3/ D1) receptors
B2, for bronchodilation
95
For control of post-partum bleeding, and alpha agonist (Ergonovine/ Ergotamine/ Bromocriptine)
Ergonovine
96
For control of acute migraines, both and alpha agonsit and a 5HT agonist (Ergonovine/ Ergotamine/ Bromocriptine)
Ergotamine
97
For control of parkinsons and hyperprolactenemia (Ergonovine/ Ergotamine/ Bromocriptine)
Bromocriptine, a dopamine agonist
98
Which CNS α2 agonist is a pro-drug? (clonidine/ α-methyl dopa)
α-methyl dopa
| crosses BBB
99
Both treat hypertension, which treats drug dependance (clonidine/ α-methyl dopa)
clonidine
100
Which β2 agonist is better for asthma? (terbutaline/ albuterol)
albuterol
101
Which β2 agonist relaxes the uterus to prevent pre-mature labor? (terbutaline/ albuterol)
terbutaline
102
β2 agonist terbutaline and albuterol will cause (vasoconstriction/ vasodilation)
vasodilation
103
Non-selective β1+β2 blocker, first generation
| Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol
Propranolol and Timolol
104
β1 selective blocker, second generation (Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol)
Metoprolol + Atenolol + Bisproprolol
105
Non-selective β1+β2 blocker, also blocks α1, third generation
(Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol)
Labetalol and Carvedilol
106
β1 selective blocker, plus Ca2+ channel blocker, third generation
(Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol)
Betaxolol
107
Why use 2nd or 3rd gen beta blockers in pts. with heart failure?
protect against sympathetic drive
108
Beta blockers are partial "contraceptives" due to their side effect of _______ ______
sexual dysfunction
109
Phentolamine and Phenoxybenzamine are an (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
α1 and α2 antagonist
hint: --> vasoD + ↓BP --> reflex tachy: use for Pheochromocytoma, Raynaud's and frostbite
110
Which is better treated with an alpha blocker? (athlosclerotic dz./ vasospastic dz)
vasospastic, such as Raynaud's
111
postural hypotension is associated with (α blockers/ β blockers)
α blockers
112
Which nerve ending blocker prevents synthesis of N.E.
| α-methyltyrosine/ reserpine/ guanethidine
α-methyltyrosine
113
Which nerve ending blocker prevents the packaging of N.E.
| α-methyltyrosine/ reserpine/ guanethidine
reserpine and guanethidine
114
Which nerve ending blocker can be used for hypertension
| (α-methyltyrosine/ reserpine/ guanethidine
reserpine and guanethidine
115
Which nerve ending blocker stops the vesicular transporter of N.E. leading to empty vesicles
(α-methyltyrosine/ reserpine/ guanethidine)
reserpine
116
Which nerve ending blocker is preferentially packaged into vesicles, blocking N.E. transport
(α-methyltyrosine/ reserpine/ guanethidine)
guanethidine
117
M1, M3, M5 are all (Gq/Gi/Gs) coupled
Gq, (increase IP3, Ca2+, DAG)
118
non selective 𝛂 antagonists are clinically used for _____
pheochromcytoma
119
what adrenergic drug class can be used to tx htn, heart dz, and glaucoma
β antagonists
120
all 𝛂 receptors antagonists are reversible EXCEPT
phenoxybenzamine (this or metyrosine can tx pheochromocytoma)
hint: covalently changes 𝛂 rcp
121
what happens when epi is added after phentolamine? epi after propanolol
drastic ↓BP (bc epi stimulates β2 rcps (vasoD));
| no change in/blocks ↑contractile F + HR (only ↑BP dt 𝛂1 rcp vasoC)
122
to treat htn from pheocrymocytoma or clonidine withdrawal, use
prazosin/labetalol; SE = ortho hytpotn
