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Pharm 2018-2019 > Autonomic Drugs - Unit 3 > Flashcards

Autonomic Drugs - Unit 3 Flashcards

1
Q

post-ganglionic parasympathetic fibers release _____

A

Acetylcholine

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2
Q

post-ganglionic sympathetic fibers release ____

A

Norepinephrine

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3
Q

Chromaffin cells release ________

A

catecholamines: Epi+Norepi

(~80% Epinephrine ~20% Norepinephrine)

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4
Q

Chromaffin cells are stimulated by the (sympathetic/parasympathetic) nervous system

A

sympathetic

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5
Q

Classically, Preganglionic sympathetics release ________, and post ganglionic sympathetics release _______

A

Preganglionic symps: Acetylcholine

Postganglionic symps: Norepinephrine

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6
Q

Classically, Preganglionic parasympathetics release ________, and postganglionic parasympathetics release _______

A

Preganglionic parasympathetics: Acetylcholine

postganglionic parasympathetics: Acetylcholine

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7
Q

Sympathetic output is generally (discrete/diffuse) while parasympathetic output is (discrete/diffuse)

A

sympathetic: diffuse
parasympathetic: discrete

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8
Q

Exceptions: for renal vessels, Pregang symps release ________, and postgang symps release _______

A

Preganglionic symps: Acetylcholine

Postganglionic symps: Dopamine!

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9
Q

Which is degraded rapidly once released from a nerve terminal? (NE/ACh)

A

ACh

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10
Q

Name 2 drugs that inhibit NE re-uptake:

A
  1. Cocaine

2. Tricyclic antidepressants, TCAs

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11
Q

How does botulinum toxin work?

A

Blocks ACh release

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12
Q

Why is an Nn receptor a bad target for ANS drugs?

A

It is in both the Symp and Parasymp systems!

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13
Q

M1, M3, M5 are all (Gq/Gi/Gs) coupled

A

Gq, (increase IP3, Ca2+, DAG)

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14
Q

M2, M4 are (Gq/Gi/Gs) coupled

A

Gi (decrease cAMP)

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15
Q

Gs, stimulatory proteins (increase/decrease) cAMP

A

increase cAMP

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16
Q

Gi, inhibitory proteins (increase/decrease) cAMP

A

decrease cAMP

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17
Q

Which Muscarinic receptor is predominant in slowing heart rate?

A

M2

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18
Q

Which Muscarinic receptor is common in the exocrine glands, blood vessels and smooth muscle?

A

M3

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19
Q

Which Muscarinic receptor is predominant in creating myosis of the eye?

A

M3

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20
Q

muscarinic receptors respond to release of (Epi/Norepi/ACh)

A

ACh

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21
Q

Which Muscarinic receptor is predominant in bronchoconstriction?

A

M3

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22
Q

What enzyme is inhibited by INDIRECT acting cholinomimetics?

A

acetylcholine esterase

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23
Q

Drug: Direct-acting muscarinic cholinomimetic for Post-operative and neurogenic ileus and urinary retention

A

Bethanechol

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24
Q

What makes Inocybe genus and Clitocybe genus of mushrooms toxic?

A

too much muscarine

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25
Q

Drug: Direct-acting muscarinic cholinomimetic for Glaucoma (ACh activates sphincter and ciliary muscles of eye

A

Pilocarpine

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26
Q

Drug: Direct-acting muscarinic cholinomimetic for Dry mouth Esp. Sjogren’s (and post- radiation therapy) increased salivation

A

Cevimeline

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27
Q

Drug: ACh esterase inhibitor, a volatile nerve gas

A

Sarin

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28
Q

Drug: ACh esterase inhibitor, an insecticide

A

Parathion

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29
Q

Drug: ACh Esterase inhibitor, covalently carbamylates AChE, for myasthenia gravis and Post-op and neurogenic ileus; urinary retention

A

Neostigmine

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30
Q

If you are exposed to Sarin gas what you like be be given quickly before irreversible aging?

A

Pralidoxime

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31
Q

In myasthenia gravis, muscle weakness is caused by ________ that block acetylcholine receptors

A

auto-immune antibodies

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32
Q

What are the SLUDGE side effects that result from too much cholinergic stimulation?

A 
Salivation 
Lacrimation
Urination
Defication
GI distress
Emesis
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33
Q

Which 2 drug classes have the SLUDGE effects?

A
  1. Muscarinic cholinomimetics

2. AChE inhibitors

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34
Q

Drug: AChE inhibitor for Alzheimer’s (amplifies endogenous ACh in brain)

A

Donepezil

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35
Q

2 drugs: indirect acting AChE inhibitor for Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)

A
  1. Physostigmine (short acting)

2. Echothiophate (long acting)

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36
Q

Too much neostigmine can lead to flooding the ACh and paralysis. What do you use to check the effect of the neostigmine?

A

Edrophonium

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37
Q

List the tertiary amine, anti-muscarinics (9) which generally block muscarinic function

A 
Eye: 
1. Atropine
2. Tropicamide 
CNS:
 3. Benztropine
 4. Scopolamine
Bronchi: 
5. Ipratropium
6. Tiotropium
GI:
7. Glycopyrrolate
8. Dicyclomine
GU:
9. Tolterodine
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38
Q

Paralysis of the ciliary muscles of the eye is called _______

A

cycloplegia

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39
Q

Parasympathetic innervation drives pupillary (constriction/dilation)

A

constriction

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40
Q

Sympathetic innervation drives pupillary (constriction/dilation)

A

dilation

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41
Q

Mydriasis is (constriction/dilation) of the pupil

A

dilation

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42
Q

A muscarinic antagonist (promotes/ inhibits) sweating

A

inhibits! (receptors are muscarinic cholinergic)

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43
Q

Drug: Tertiary amine, anti-muscarinics

Targets CNS For parkinson’s, penetrates BBB

A

Benztropine

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44
Q

2 Drug: Tertiary amine, anti-muscarinics

For Mydriasis and cycloplegia

A
  1. Atropine

2. Tropicamide

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45
Q

Drug: Tertiary amine, anti-muscarinics

Targets CNS for Prevention or reduction of motion sickness, penetrates BBB

A

Scopolamine

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46
Q

2 Drugs: Tertiary amine, anti-muscarinics

Target G.I. tract to reduce transient hypermobility

A
  1. Glycopyrrolate

2. Dicyclomine

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47
Q

Drug: Tertiary amine, anti-muscarinics

For postoperative bladder spams, incontinence

A

Tolterodine

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48
Q

2 Drug: Tertiary amine, anti-muscarinics

For bronchidilation in asthma, COPD

A
  1. Ipratropium

2. Tiotropium

49
Q

Two ganglion blockers that block Nn receptors and sympathetic tone are

A
  1. Hexamethonium

2. Mecamylamine

50
Q

What are 1. Hexamethonium and 2. Mecamylamine used for?

A

“Bloodless” field surgery, the ganglionic blockers decrease blood pressure

51
Q

Two neuromuscular drugs that are non-depolarizing blockers at Nm junctions are:

A
  1. Tubocurarine

2. Mivacurium

52
Q

When succinylcholine is administered, it causes initial (paralysis/ fasciculations) followed by (paralysis/ fasciculations)

A

Produces initial fasciculations and then paralysis within 1 minute.

53
Q

What do 1. Tubocurarine and 2. Mivacurium do?

A

Block Nm receptors, skeletal muscle relaxation during surgery or mechanical ventilation

54
Q

Accommodation of the eye is purely under (sympathetic/parasympathetic) control

A

parasympathetic

55
Q

Blurred vision is a mark of a (muscarinic/ adrenergic)

A

muscarinic

56
Q

To look in someone’s eye, dilate it with (Atropine/Tropicamide)

A

Tropicamide, dialates eye for less time than

Atropine

57
Q

To treat parkinson’s use (Benztropine/Scopolamine)

A

Benztropine

58
Q

To reduce motion sickness use (Benztropine/Scopolamine)

A

Scopolamine

59
Q

To treat cholinergic poisoning like muscarine from mushrooms use _______

A

Atropine

60
Q

Cholinesterase inhibitors are used to reverse the effects of (depolarizing/ non-depolarizing) blockers

A

non-depolarizing

61
Q

Botulinum toxin as botox is used to (block/ cause) muscle tone

A

blocks muscle tone: relaxes

62
Q

The synthesis of Norepiniphrine begins with (arginine/ /Dopamine/ tyrosine/ DOPA)

A

Tyrosine -> DOPA -> dopamine -> N.E.

63
Q

The effects of N.E. at a neuron are stopped by the action of the (uptake 1/ uptake2) transporter

A

uptake 1

64
Q

N.E. is destroyed in the cell by (acetylcholine esterase/ mono amine oxidase/ PNMT)

A

MAO on the mitochondria

65
Q

which is a neurotransmitter (N.E./ Epi)

A

N.E.

66
Q

Which is a neurohormone (N.E./ Epi)

A

Epi

67
Q

Which adrenergic receptor causes sm. muscle contraction including vasoconstriction(α1/ α2/ β1/ β2/ β3/ D1)

A

α1

68
Q

Which adrenergic receptor causes increased heart inotropy (α1/ α2/ β1/ β2/ β3/ D1)

A

β1

69
Q

Which adrenergic receptor causes sm. muscle relaxation including arteriole dilation(α1/ α2/ β1/ β2/ β3/ D1)

A

β2

70
Q

Which adrenergic receptor inhibits neurotransmitter N.E. release (α1/ α2/ β1/ β2/ β3/ D1)

A

α2

71
Q

Which adrenergic receptor causes lipolysis (α1/ α2/ β1/ β2/ β3/ D1)

A

β3

72
Q

Which adrenergic receptor causes bronchiole relaxation (α1/ α2/ β1/ β2/ β3/ D1)

A

β2

73
Q

Which receptor causes renal, mesenteric and cerebral arteriole dilation? (α1/ α2/ β1/ β2/ β3/ D1)

A

D1, dopamine as neurotransmitter

74
Q

Phenylephrine is an (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)

A

α1 agonist

treats nasal congestion, and postural hypotention

75
Q

Prazosin is an (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)

A

α1 antagonist

treats primary hypertension and BPH

76
Q

Clonidine is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)

A

α2 agonist in CNS

treats Hypertension; shock; withdrawal from drug dependence

77
Q

Fenoldopam is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)

A

D1 agonist

Increases blood flow at renal, mesenteric, and cerebral arteries

78
Q

Dobutamine is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)

A

β1, agonist

treats Cardiac decompensation; shock; heart block

79
Q

Atenolol and Metoprolol are both (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)

A

β1 antagonists

They treat HTN, Angina, Arrythmias, CHF

80
Q

Albuterol and terbutaline are a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)

A

β2 Agonist
Albuterol: bronchospasm; mild asthma; COPD
Terbutaline: above + prevents premature labor

81
Q

Isoproterenol is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)

A

β1 and β2 agonist, non-selective

used to treat shock and heart block

82
Q

Propranolol is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)

A

β1 and β2 antagonist, non-selective

use to treat Angina, Hypertension and Arrythmias

83
Q

With low concentration of epinephrin at muscles, the (α1/β2) receptor trumps leading to (dilation/ contraction) of vascular smooth muscle

A

β2, dilation
with low epi
fight or flight

84
Q

With high concentration of epinephrin at muscles, the (α1/β2) receptor trumps leading to (dilation/ contraction) of vascular smooth muscle

A

α1, contraction

raises B.P.

85
Q

Increases release of cytoplasmic N.E. (cocaine/ tyramine)

A

tyramine

similar to amphetamine

86
Q

Prevents N.E. re-uptake (cocaine/ tyramine/ amphetamine)

A

cocaine

87
Q

short term tolerance is called ________

A

tachyphylaxis

88
Q

increased blood flow at renal, mesenteric and cerebral vasculature (low dose/ medium dose/ high dose) Dopamine

A

low dose dopamine

89
Q

has direct heart β1 inotropy effects and indirect release of N.E. (low dose/ medium dose/ high dose) Dopamine

A

medium dose dopamine

90
Q

has direct α1 vascular effect and indirect N.E. release causing vasoconstriction (low dose/ medium dose/ high dose) Dopamine

A

high dose dopamine

91
Q

acts at the D1 receptor only, increases renal blood flow (Dopamine/ Fenoldopam)

A

Fenoldopam

92
Q

With bolus N.E.
H.R. (increases/decreases)
B.P. (increases/decreases)
TPR (increases/decreases)

A

H.R. decreases due to vagal feedback
B.P. increases α1 constriction
TPR increases α1 constriction

93
Q

With bolus epinephrine
H.R. (increases/decreases)
B.P. (increases/decreases)
TPR (increases/decreases)

A

H.R. increases β1 increases inotropy
B.P. increases β1 increases inotropy
TPR decreases β2 sm. muscle dilation

94
Q

With bolus isoproterenol
H.R. (increases/decreases)
B.P. (increases/decreases)
TPR (increases/decreases)

A

H.R. increases due to β1 + feedback
B.P. decreases β2 sm. muscle dilation
TPR decreases β2 sm. muscle dilation

95
Q

epi pens are used for anaphylaxis for their action on (α1/ α2/ β1/ β2/ β3/ D1) receptors

A

B2, for bronchodilation

96
Q

For control of post-partum bleeding, and alpha agonist (Ergonovine/ Ergotamine/ Bromocriptine)

A

Ergonovine

97
Q

For control of acute migraines, both and alpha agonsit and a 5HT agonist (Ergonovine/ Ergotamine/ Bromocriptine)

A

Ergotamine

98
Q

For control of parkinsons and hyperprolactenemia (Ergonovine/ Ergotamine/ Bromocriptine)

A

Bromocriptine, a dopamine agonist

99
Q

Which CNS α2 agonist is a pro-drug? (clonidine/ α-methyl dopa)

A

α-methyl dopa

crosses BBB

100
Q

Both treat hypertension, which treats drug dependance (clonidine/ α-methyl dopa)

A

clonidine

101
Q

Which β2 agonist is better for asthma? (terbutaline/ albuterol)

A

albuterol

102
Q

Which β2 agonist relaxes the uterus to prevent pre-mature labor? (terbutaline/ albuterol)

A

terbutaline

103
Q

β2 agonist terbutaline and albuterol will cause (vasoconstriction/ vasodilation)

A

vasodilation

104
Q

Non-selective β1+β2 blocker, first generation

Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol

A

Propranolol and Timolol

105
Q

β1 selective blocker, second generation (Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol)

A

Metoprolol + Atenolol + Bisproprolol

106
Q

Non-selective β1+β2 blocker, also blocks α1, third generation
(Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol)

A

Labetalol and Carvedilol

107
Q

β1 selective blocker, plus Ca2+ channel blocker, third generation
(Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol)

A

Betaxolol

108
Q

Why use 2nd or 3rd gen beta blockers in pts. with heart failure?

A

protect against sympathetic drive

109
Q

Beta blockers are partial “contraceptives” due to their side effect of _______ ______

A

sexual dysfunction

110
Q

Phentolamine and Phentoxybenzamine are an (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)

A

α1 and α2 antagonist

for Pheochromocytoma, Raynaud’s and frostbite

111
Q

Which is better treated with an alpha blocker? (athlosclerotic dz./ vasospastic dz)

A

vasospastic, such as Raynaud’s

112
Q

postural hypotension is associated with (α blockers/ β blockers)

A

α blockers

113
Q

Which nerve ending blocker prevents synthesis of N.E.

α-methyltyrosine/ reserpine/ guanethidine

A

α-methyltyrosine

114
Q

Which nerve ending blocker prevents the packaging of N.E.

α-methyltyrosine/ reserpine/ guanethidine

A

reserpine and guanethidine

115
Q

Which nerve ending blocker can be used for hypertension

(α-methyltyrosine/ reserpine/ guanethidine

A

reserpine and guanethidine

116
Q

Which nerve ending blocker stops the vesicular transporter of N.E. leading to empty vesicles
(α-methyltyrosine/ reserpine/ guanethidine)

A

reserpine

117
Q

Which nerve ending blocker is preferentially packaged into vesicles, blocking N.E. transport
(α-methyltyrosine/ reserpine/ guanethidine)

A

guanethidine

118
Q

M1, M3, M5 are all (Gq/Gi/Gs) coupled

A

Gq, (increase IP3, Ca2+, DAG)

Pharm 2018-2019 (7 decks)

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