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Pharm > Autonomic > Flashcards

Autonomic Flashcards

1
Q

Are preganglionic sympathetic nerve fibers short or long?

A

short

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2
Q

Are the postganglionic PANS nerve fibers short or long?

A

long

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3
Q

What three neurotransmitters are released from the adrenal medulla?

A

epinephrine

norepinephrine

dopamine

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4
Q

Which six organs only receive sympathetic outflow?

A 
blood vessels
hair follicles 
sweat glands 
adrenal glands 
liver
kidney
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5
Q

In what body part do the PANS and SANS produce similar, rather than opposing, effects?

A

salivary glands

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6
Q

What is the effect of dopamine in the kidney?

A

vasodilatory

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7
Q

Is NPY released during high or low stimulation frequencies?

A

high

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8
Q

What transporter do hemicholiniums block? What two substances can then no longer diffuse into the cell?

A

Choline transporter

choline and sodium

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9
Q

What drug blocks acetylcholine entering a pre-synaptic vesicle?

A

Vesamicol

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10
Q

What is the MOA of neostigmine?

A

transient ACH-ase inhibitor

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11
Q

What is also stored in the presynaptic vesicle with acetylcholine?

A

ATP and proteoglycan

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12
Q

What protein does calcium interact with in the presynaptic terminal?

A

synaptotagmin

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13
Q

What are the subunits of NAchR?

A

two alpha, one beta, one gamma, one delta

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14
Q

What subunit of the NAchR does acetylcholine bind?

A

alpha

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15
Q

What muscarinic receptor subtype is present in the eye?

A

M3

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16
Q

Does muscarinic activation of the eye open or close the canal of Schlemm?

A

open

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17
Q

What cholinergic receptor is present in the lung? What two effects does activation of this receptor procude?

A

M3

bronchospasm AND secretion

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18
Q

What two effects does muscarinic activation do in the GI tract?

A

contraction

secretion

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19
Q

What does M3 activation of the detrusor do?

A

contraction

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20
Q

What does M3 activation of the trigone do?

A

relax

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21
Q

What does M3 activation do to most sphincters? What is the excpetion? What happens?

A

relax

lower esophageal , contracts

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22
Q

What type of muscarinic receptor is present on parietal cells? What is the effect of this receptors activation?

A

M3

acid secretion

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23
Q

What type of muscarinic receptor is on ECL cells? What is released?

A

M1 = ECL

histamine

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24
Q

What is the MOA of cimetidine?

A

H2R antagonist

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25
Q

What is the MOA of rinatidine?

A

H2R antagonist

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26
Q

What structure of the eye secretes aqueous humor?

A

ciliary body

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27
Q

What three receptors are present on the ciliary epithelium?

A

β2, β1, α2

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28
Q

What two receptors are on the ciliary muscle?

A

M3 and β2

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29
Q

What receptor is on the radial muscle?

A

α1

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30
Q

What receptor is on the sphincter muscle?

A

M3

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31
Q

What does ciliary muscle activation do to the canal of Schlemm?

A

opens it

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32
Q

What does βadrenergic blockade do to aqueous humor production?

A

decreases it

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33
Q

What does cGMP do in VSMCs?

A

inhibits Ca2+ influx

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34
Q

What are the four choline ester muscarinic agonist?

A

Acetylcholine
Methacholine
Carbachol
Bethanecol

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35
Q

What are the two alkaloid muscarinic agonists?

A

Muscarine and pilocarpine

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36
Q

Which two choline ester possess methyl groups? What property does this give the groups?

A

Methanacol and Bethanecol

Longer half life

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37
Q

Which two choline esters are resistant to acetylcholinesterase?

A

carbachol and bethanacol

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38
Q

What are the effects of low dose acetylcholine?

A

vasodilation

decreased peripheral resistance

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39
Q

What are the effects of high dose acetylcholine?

A

bradycardia

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40
Q

What are the two function of Methacholine?

A

to diagnose bronchial hypersensitivity

to Dx bella donna alkaloid poisoning

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41
Q

Which choline ester can equally effect nicotinic and muscarinic receptors?

A

carbachol

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42
Q

What is carbachol used for? Why?

A

to decrease intraocular pressure

openn canal of schlemm

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43
Q

Does bethanechol has muscarinic or nicotinic effects?

A

muscarinic only

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44
Q

What choline ester is used to increase detrusor tone?

A

bethanechol

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45
Q

What choline ester is used to decrease internal sphincter tone?

A

Bethanechol

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46
Q

What choline ester can increase LES tone?

A

Bethanechol

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47
Q

Is muscarine destroyed by acetylcholinesterase activity?

A

no

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48
Q

What are the two muscarinic agonists?

A

muscarine and pilocarpine

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49
Q

What does pilocarpine do in the eye? What disease is pilocarpine used to treat?

A

miosis

glaucoma

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50
Q

What muscarinic agonist can open the canal of schlemm?

A

pilocarpine

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51
Q

What agonist can increase the tone of the trabecular meshwrok? What diease would this treat?

A

pilocarpine

wide-angle glaucoma

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52
Q

What does pilocarpine do to the ciliary muscle? What type of vision would this bring about?

A

contract

near

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53
Q

What are the two nicotinic agonists?

A

nicotine

succinylcholine

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54
Q

Does nicotine at the presynaptic autonomic ganglia produce sympathetic or parasympathetic effects on the heart? Why?

A

sympathetic

NN to adrenal medulla = ↑ E and NE

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55
Q

What will nicotine produce in the vasculature?

A

vasoconstriction

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56
Q

What will nicotine produce in the GI tract?

A

increased motility and secretion

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57
Q

What effect will nicotine produce at the carotid body baroreceptors? What will this lead to?

A

increased firing

increased respiratory rates

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58
Q

What will nicotine produce at the medullary emetic chemoreceptor?

A

nausea and vomiting

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59
Q

What disease is edrophonium used to Dx?

A

myasthenia gravis

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60
Q

What two drugs are used in the Tx of myasthenia gravis?

A

pyradostigmine and neostigmine

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61
Q

Do pyridostigmine and neostigmine produce CNS effects? Why or why not?

A

no

quaternary amines that don’t cross BBB

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62
Q

What drug is used to aid in paralytic ileus?

A

neostigmine

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63
Q

What drug is used to treat atony of urinary bladder?

A

neostigmine

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64
Q

When is the use of neostigmine contraindicated in the treatment of urinary or GI issues?

A

obstruction

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65
Q

What two Ach Inhibitors are used to treat Alzheimers? Why?

A

Tacrine and Dopenezil

Lipid soluble

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66
Q

What drug is used to treat Ach excess?

A

Atropine

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67
Q

What drug restores acetylcholinesterase activity? Why?

A

Pralidoxim

reverses phosphorylation

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68
Q

Which two acetylcholinesterase inhibitors do not phosphorylate AchE? Would pralidoxim reverse toxicity of these two drugs?

A

neostigmine and physostigmine

no

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69
Q

What are the three muscarinic antagonists?

A

Atropine

Ipratropium

Benztropine

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70
Q

What are the two NN and NM receptor antagonists?

A

hexamethonium

Mecamylamine

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71
Q

What is the non-depolarizing neuromuscular blocker?

A

D-tubocurarine

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72
Q

What is the depolarizing neuromuscular blocker?

A

succinylcholine

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73
Q

Does atropine possess selectivity for any muscarinic receptor subtype?

A

no

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74
Q

Does atropine effect blood pressure when given alone?

A

no

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75
Q

Does atropine cause hyper or hypo thermia?

A

hyperthermia

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76
Q

Does atropine cause urinary retention or excretion?

A

retention

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77
Q

Does atropine cause diarrhea or constipation?

A

constipation

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78
Q

What drug is used to prevent vagal reaction in pericardiocentesis?

A

atropine

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79
Q

What muscarinic antagonist is used to decrease bronchiolar secretions? What receptor primarily? What is another name for this drug?

A

Ipratropium

M3

Atrovent

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80
Q

What disease is Ipratropium primarily used to treat?

A

COPD

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81
Q

Does ipratropium cross the BBB?

A

no

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82
Q

What muscarinic antagonist can enter the CNS? Why? What disease is treated?

A

Benztropine

it is a tertiary amine

Parkinsons

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83
Q

What is the function of benztropine?

A

to re-establish the dopaminergic and cholinergic balance in the brain during parkinsons

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84
Q

What is a common side effect of all autonomic ganglion blockers?

A

block baroreflex

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85
Q

What is the main tone in the arterioles? What do ganglionic blockers do in the arterioles?

A

vasodilation

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86
Q

What do ganglionic blockers do to venous return? What does this do to preload? What does this do to afterload?

A

decrease venous tone

decrease preload

decrease CO

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87
Q

What do ganglionic blockers do in the heart?

A

tachycardia

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88
Q

What do ganglionic blockers do to the iris/radial muscle?

A

mydriasis

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89
Q

What do ganglionic blockers do to the ciliary muscle?

A

cycloplegia

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90
Q

What do ganglionic blockers do in the GI tract?

A

constipation

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91
Q

What do ganglionic blockers do in the bladder?

A

urinary retention

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92
Q

What do ganglionic blockers do in the salivary glands?

A

xerostomia

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93
Q

What do ganglionic blockers do in the sweat glands?

A

anhidrosis

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94
Q

What is the MOA of non-depolarizing neuromuscular blockers?

A

prevent channel from opening

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95
Q

What is the MOA of depolarizing neuromuscular blockers?

A

prevent channel closing

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96
Q

Can NM blocking agents cross the CNS? Why?

A

no

highly ionized

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97
Q

What muscle responds last to neuromuscular blockers?

A

diaphragm

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98
Q

What is the main side effect of D-tubocurarine? Why?

A

hypotension

systemic histamine release

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99
Q

What is the main side effect of succinylcholine? Why?

A

hyperkalemia

cell is constantly trying to repolarize and is keeping potassium channels open

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100
Q

Why is succinylcholine contraindicated in patients with glaucoma?

A

sux can cause transiest increases in IO pressure

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101
Q

What does succinylcholine do to intraabdominal pressure?

A

increase

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102
Q

Can succinylcholine cause pain?

A

yes

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103
Q

What is the inhibitor of Tyrosine Hydroxylase?

A

Metyrosine

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104
Q

What enzyme works on tyramine? What molecule is created?

A

Dopamine β-hydroxylase

Octopamine

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105
Q

Regarding adrenergic synthesis, where can octopamine be shuttled into?

A

norepinephrine

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106
Q

What compound is tyramine synthesized from?

A

tyrosine

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107
Q

What compound is epinine synthesized from?

A

dopamine

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108
Q

What enzyme works on epinine? What is created?

A

Phenylamine β-hydroxylase

epinephrine

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109
Q

What is the Rate Limiting Enzyme of adrenergic synthesis?

A

Tyrosine Hydroxylase

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110
Q

What transporter carries catecholamines into the vesicle/ What drug inhibits this transporter?

A

VMAT

reserpine

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111
Q

What catecholamine is brought into the vesicle?

A

dopamine

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112
Q

What enzyme degrades catecholamines in the circulation?

A

Catech-O-methyl transferase

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113
Q

What two drugs inhibit adrenergic reuptake?

A

cocaine

ticyclic antidepressants

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114
Q

What is the re-uptake protein for dopamine?

A

DAT

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115
Q

What is the reuptake protein for serotonin?

A

SERT

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116
Q

What is the extraneuronal reuptake protein for catecholamines? What drug can inhibit this transpoter?

A

NET2

corticosteroids

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117
Q

Where is Monoamine Oxidase (MAO) located?

A

mitochondria

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118
Q

What is an MAO inhibitor?

A

Phenelzine

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119
Q

What does MAO-A degrade?

A

NE, 5-HT and Tyramine

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120
Q

What does MAO-B degrade?

A

dopamine

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121
Q

What is the main metabolite of norepinephrine found in the urine?

A

hydroxymethylmandelic acid

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122
Q

What does α1 activation in the kidney do?

A

decrease renin release

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123
Q

What does β2 in the pancreas do?

A

increase insulin secretion

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124
Q

What does D1 activation in the coronary vasculature do?

A

vasodilation

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125
Q

What does D1 activation in the kidney do?

A

↑ RBF, ↑ Na+ excretion, ↑ GFR

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126
Q

How does mydriasis differ from adrenergic agonists and cholinergic antagonists?

A

adrenergic = only mydriasis

muscarinic antagonists = mydriasis AND cycloplegia

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127
Q

Where do the ANS loop and hormonal loop meet?

A

mean arterial pressure

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128
Q

Phenylephrine is an agonist for what receptor?

A

α1 adrenergic

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129
Q

Terbutaline is an agonist for what receptor?

A

β2 adrenergic

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130
Q

How do indirect acting sympathomimetics function?

A

increasing availability of adrenergic hormones

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131
Q

What are the two MOAs of guanethidine?

A
  1. competes with NE for reuptake at NET1

2. blocks release of NE in response to action potential

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132
Q

What does reserpine do to the effects of indirect acting adrenergic agonists?

A

abolishes their effects

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133
Q

What are the two α1 adrenergic agonists?

A

phenylephrine

methoxamine

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134
Q

What are the two α2 adrenergic agonists?

A

clonidine

methylnorepinephrine

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135
Q

Which α-adrenergic receptor does norepinephrine activate more?

A

α1 = α2

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136
Q

Which β-adrenergic receptor does norepinephrine activate more?

A

β1 > β2

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137
Q

Which α-adrenergic receptor does epinephrine activate more?

A

α1 = α2

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138
Q

Which β-adrenergic receptor does epinephrine activate more?

A

β1 = β2

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139
Q

Which β-adrenergic receptor does dobutamine activate the most?

A

β1

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140
Q

What is the selectivity of dobutamine for β2 and α-adrenergic receptors?

A

β2 = α1

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141
Q

What is the selectivity for isoproterenol for β1 and β2 receptors?

A

β1 = β2

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142
Q

What four drugs selectivyt activate β2 receptors preferentially over β1 activation?

A

Albuterol, Terbutaline, Metaproterenol and Ritodrine

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143
Q

What is the selectivity of dopamine for the D1 and D2 receptor?

A

D1 = D2

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144
Q

What is the drug that is D2&raquo_space; D1 selective?

A

Fenoldopam

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145
Q

What is another name for clonidine?

A

catapres

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146
Q

What is the MOA of α-Methyldopa?

A

α2 agonist

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147
Q

What is another name for α-Methyldopa?

A

Aldomet

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148
Q

What is the clinical use of clonidine/catapres and α-Methyldopa/Aldomet ?

A

hypertension

149
Q

What are the two α2 agonists used for treat glaucoma?

A

Apraclonidine and Brimonidine

150
Q

What is another name for metaproterenol?

A

Metaprel

151
Q

Which β2 agonist is resistant to methylation by COMT?

A

Metaproterenol/Metapres

152
Q

What are the two uses of metaproterenol/Metaprel?

A

Tx of obstructive diseases

acute bronchospasm

153
Q

What β2 agonist is not a substrate for methylation by COMT?

A

terbutaline

154
Q

What are the three uses for terbutaline?

A

obstructive disease

acute bronchospasm

status asthmaticus

155
Q

What is another name for terbutaline?

A

Bricanyl

156
Q

What are two additional names for Albuterol?

A

Ventolin and Salbutamol

157
Q

What are the two uses of albuterol?

A

bronchospasm

delay labor

158
Q

What is another name for ritodrine?

A

Yutopar

159
Q

What is the use of ritodrine?

A

delay pregnancy

160
Q

What is the main side effect of β2 agonists? What increases the risk of this side effect?

A

tachycardia

MAO inhibitors

161
Q

How long should one wait between administering a β2 agonist after discontinuing MAOI use?

A

at least two weeks

162
Q

What three metabolites are increased during β2 agonist treatment?

A

glucose, lactate and free fatty acids

163
Q

What happens to levels of serum K+ during β2 agonist administration? In combination with other drugs is this an important effect to remember?

A

Hypokalemia

digoxin and diuretics

164
Q

Other than D1 > D2, what other adrenergic receptor can Fenoldopam activate?

A

α2 adrenergic

165
Q

What are the two clinical uses of Fenoldopam? What is the main side effect of Fenoldopam?

A

Hypertensive crisis and natriuresis

Hypotension

166
Q

What is another name for Fenoldopam?

A

Colorpam

167
Q

Does isoproterenol have any effect on α-receptors?

A

no

168
Q

What does isoproterenol do to peripheral resistance?

A

decrease

169
Q

What does isoproterenol do to heart rate?

A

increase

170
Q

What does isoproterenol do to cardiac contractility?

A

increase

171
Q

When is isoproterenol used regarding the heart? Why?

A

bradycardia

TdP

172
Q

What can a high dose of isoproterenol do to the heart?

A

myocardial necrosis

173
Q

Why is isoproterenol used in CHF?

A

positive inotropic agent

174
Q

Does dobutamine affect norepinephrine release? Why?

A

no

dobutamine does not activate α2

175
Q

Does dobutamine affect TPR? Why?

A

no

β2 = α1

176
Q

At low doses, what adrenergic receptors does epinephrine primarily effect?

A

β1 and β2

177
Q

At moderate doses, other than β1 and β2, what receptor does epineprhine activate? What is the result?

A

α1

increases in TPR and BP

178
Q

At high doses, what adrenergic receptor does epinephrine primarily effect? What are the two main effects?

A

α1

increase in TPR and reflex bradycardia

179
Q

What is the function of SubQ epinephrine?

A

local vasoconstriction

180
Q

Regarding the vasculature, where are the two primary targets of epinephrine?

A

arterioles and precapillary sphincters

181
Q

Where is blood flow redistributed follow Epi administration?

A

skeletal msucle

182
Q

What does large dose epinephrine do to renal blood flow?

A

decrease

183
Q

What does large dose epinephrine do to filtration fraction?

A

increase

184
Q

What does large does epinephrine do to pulmonary arterial and venous circulation volume?

A

increase

185
Q

What does large dose epinephrine do to coronary circulation?

A

increase

186
Q

What is the MOA of phentolamine?

A

α1 = α2 antagonist

187
Q

What is the effect of epinephrine stimulation during Beta blockade?

A

massive increase in arterial pressure

188
Q

Does norepinephrine have higher affinity for β1 or α1 adrenergic receptors?

A

α1

189
Q

Does norepinephrine have higher affinity for β1 or β2 adrenergic receptors?

A

β1

190
Q

Are epinephrien and norepinephrine equipotent in stimulating β1 receptor?

A

yes

191
Q

What does norepinephrine do to coronary blood flow?

A

increase

192
Q

What does norepinephrine do to cardiac output?

A

mildly decrease

193
Q

What does norepinephrine do to renal blood flow?

A

decrease

194
Q

What does norepinephrine do to splanchnic and hepatic blood flow?

A

decrease

195
Q

What specific location can dopamine be synthesized in the kidney?

A

epithelial tissues of PCT

196
Q

Is dopamine metablozed by MAO, COMT or both?

A

MAO and COMT

197
Q

What does low dose dopamine do in the kidney?

A

diuretic

198
Q

What receptor does dopamine activate in the kidney? What effect does this produce?

A

D1

decreased Na+ reabsorption

199
Q

Why does dopamine produce vasodilation at low doses?

A

D2 presynaptic inhibition of norepinephrine release

200
Q

What is the effect of dopamine at moderate doses? What is an intermediate dose of dopamine?

A

tachycardia

2-5 µg/kg/hr

201
Q

What does moderate dose dopamine do to systolic pressure? DIastolic?

A

Systolic = increase

diastolic = no effect

202
Q

What is the effect of dopamine at high doses? What is a high dose of dopamine?

A

α1 activation

5-15 µg/kg/hr

203
Q

WHy does low dose dopamine produce a diuresis?

A

vasodilates PCT and leads to higher GFR

204
Q

What two drugs is the use of dopamine contraindicated in?

A

MAOI or tricyclic

205
Q

What is the main clinical use of dopamine?

A

to acutely improve cardiac and renal function

206
Q

Does the exchange of norepinephrine for amphetamine require Ca2+?

A

no

207
Q

What exogenous catecholamine can stimulate the medullary respiratory center?

A

amphetamine

208
Q

What two parts of the brain can amphetamine activate?

A

cortex and reticular activating center

209
Q

What adrenergic receptors can amphetamine activate?

A

α and β

210
Q

Do amphetamines increase systolic pressure? Diastolic?

A

increase systolic

increase diastolic

211
Q

Do amphetamines increase HR?

A

yes

212
Q

What is the main degradation route for tyramine?

A

MAO

213
Q

In what type of food is tyramine found?

A

fermented cheese

214
Q

What are the three α1 selective agonists?

A

Prazosin

Terazosin

Doxazosin

215
Q

What is the irreversible α1-antagonist?

A

Phenoxybenzamine

216
Q

What is the non-selective alpha anagonist?

A

Phentolamine

217
Q

What are the three selective α2 antagonists?

A

Yohimbine

Rauwoscine

Torazoline

218
Q

What drug is used to treat a pheochromocytoma?

A

phenoxybenzamine

219
Q

What is the main drug used in the Tx of BPH? Why?

A

Tamsulosin

relaxes prostate to keep urine flowing

220
Q

What are the four non-selective β-blockers?

A

Propranalol

Nadolol

Timolol

Pindolol

221
Q

Which non-selective β-blocker possesses intrinsic sympathomimetic activity?

A

Pindolol

222
Q

What are the five selective β-blockers?

A 
Atenolol
Metoprolol
Esmalol
Beliprolol
Acebutolol
223
Q

What adrenergic blocking pattern do carvedilol and labetolol display?

A

β1 = β2/ α1 > α2

224
Q

Do β-blockers increase or decrease lipolysis?

A

decrease

225
Q

Do β-blockers increase or decrease VLDL?

A

increase

226
Q

Do β-blockers increase or decrease HDL?

A

decrease

227
Q

Which of the five cardioselective β-blockers possesses ISA?

A

acebutolol

228
Q

β-blockers with ISA have the ability to cause what?

A

undesirable bradycardia

229
Q

What are the two lipid soluble β-blockers?

A

Propranalol and Metoprolol

230
Q

Do hydrophilic or hydrophobic β-blockers enter the brain?

A

hydrophilic

231
Q

Which type of β-blocker, hydrophilic or hydrophobic, are excreted virtually unchanged by the kidney?

A

hydrophilic

232
Q

Where are hydrophobic β-blockers metabolized?

A

liver

233
Q

What is the most common symptom of β-blockers? Why?

A

fatigue

decreased cardiac output

234
Q

Why can β-blockers increase the risk of diabetes?

A

decreased insulin sensitivity

235
Q

What is the only symptom of hypoglycemia that patients on a β-blocker may experience?

A

sweating

236
Q

Where does the M1 receptor predominate?

A

glands

237
Q

Is muscarine destroyed by AchE?

A

no

238
Q

Does the PANS or SANS usually dominate in the heart?

A

PANS

239
Q

What three cardiovascular drugs have anti-muscarinic properties?

A

quinidine

procainamide

Tricyclics

240
Q

What is the MOA of Physostigmine? What two conditions are Physostigmine used to treat?

A

AchE Inhibitor

glaucoma and Atropine overdose

241
Q

What does the D of DUMBBELSS stand for?

A

diarrhea

242
Q

What does the U of DUMBBELSS stand for?

A

urination

243
Q

What does the M of DUMBBELSS stand for?

A

miosis

244
Q

What do the B’s of DUMBBELSS stand for?

A

bradycardia

bronchoconstriction

245
Q

What does the E of DUMBBELSS stand for?

A

Excitement

246
Q

What does the L of DUMBBELSS stand for?

A

lacrimation

247
Q

What do the S’s of DUMBBELSS stand for?

A

salivation

sweating

248
Q

What is the main adverse side effect of tubocurarine?

A

systemic histamine release

249
Q

Treatment with tubucurarine is usually preceeded by treatmeant with what type of drug?

A

Antihistamine

250
Q

Where does the conversion of epinephrine to norepinephrine occur?

A

vesicle

251
Q

What drug functions similar to bretylium?

A

Guanethidine

252
Q

What does α2 activation of the platelets do?

A

aggregation

253
Q

What does α2 activation of the pancreas do?

A

inhibit insulin secretion

254
Q

What is the MOA of paragyline?

A

MAOI

255
Q

What is the MOA of entacapone?

A

COMT inhibitor

256
Q

At a low dose of epinephrine, what is the predominant response between β2 and α1?

A

β2 = low dose wins

257
Q

At a high dose of epinephrine, what is the predominant response between β2 and α1?

A

α1 = high dose wins

258
Q

β2 agonists can decrease the release of what two inflammatory cytokines in the lungs?

A

leukotrienes and histamine

259
Q

β2 agonists can decrease the release of what inflammatory enzyme?

A

PLA2

260
Q

What should always be corrected before dopamine use?

A

hypovolemia

261
Q

Does methanechol stimulate nicotonic or muscarinic receptors more?

A

muscarinic

262
Q

What do choline esters do at low dose to the CV system?

A

vasodilation

263
Q

What do choline esters do at high dose to the CV system?

A

bradycardia

264
Q

What is another name for bethanechol? What receptors does bethanechol primarily function at?

A

Ureocholine

M3

265
Q

What three diseases is pilocarpine contraindicated? Why?

A

peptic ulcers –>M3 on parietal cells

GI disorders

Asthma

266
Q

What does nicotine do to heart rate? Why?

A

increase

release of epi and NE from adrenal medulla

267
Q

What is the drug used to treat Ach overdose?

A

atropine

268
Q

What is another name for benztropine?

A

Cogentin

269
Q

What two drugs discussed in this section are highly ionized?

A

Succinylcholine

D-tubocurarine

270
Q

What is the MOA of tubocurarine?

A

prevents NM opening

271
Q

What is another name for tubocurarine?

A

Anectine

272
Q

What is a common complaint after the use of neuromuscular blockers?

A

muscle pain

273
Q

What does α1 activation in the arteries produce?

A

increase afterload

274
Q

What does α1 activation in the veins produce?

A

increase preload

275
Q

What are the two MOAs of ephedrine?

A

indirectly releases norepinephrine

directly activates adrenoreceptors

276
Q

What are the two indirect acting adrenoceptor agonists?

A

amphetamine and tyramine

277
Q

What is the MOA of amphetamine and tyramine?

A

displace norepinephrine from granules

278
Q

What type of drug can strongly potentiate the effects of amphetamine and tyramine?

A

MAOI

279
Q

What is the difference between amphetamine and tyramine?

A

tyramine cant cross BBB

280
Q

What is destroyed by MAO, tyramine of amphetamine?

A

tyramine

281
Q

What can produce diuresis, amphetamine or tyramine?

A

tyramine

282
Q

Liver failure would cause increases in the levels of what two β-blockers?

A

Metoprolol and Propranalol

283
Q

What ion is exchanged for dopamine at the vesicular membrane?

A

H+

284
Q

What hormone activates ECL cells?

A

gastrin

285
Q

What are the four irreversible AchE Inhibitors?

A

Echothiophate
Malathion
Parathion
Sarin

286
Q

What two choline esters have a methyl group attached to them?

A

Methacholine

Carbachol

287
Q

Which choline ester has zero nicotinic effects?

A

Bethanachol

288
Q

Does acetylcholine usually activate NM receptors? Why?

A

no

can’t penetrate fat

289
Q

What are the two clinical uses of acetylcholine?

A

short lasting miosis

provocative test in coronary angiography

290
Q

What is another name for methacholine?

A

Provocholine

291
Q

What is the clinical use of carbachol?

A

glaucoma

292
Q

What muscarinic subtype does bethanechol work on primarily? What is another name for this drug?

A

M3

Ureocholine

293
Q

What are the three uses of bethanechol?

A

urinary retention

gastric atony

gastric abnormalities

294
Q

What are two other names for Pilocarpine?

A

Isopto Carpine

Salagen

295
Q

What does pilocarpine hypersensitivity indicate?

A

PANS dysfunction

296
Q

What drug (s) is/are used to treat myasthenia?

A

Neostigmine or Pyridostigmine

297
Q

What can echothiophosphate be used to treat?

A

glaucoma

298
Q

What cell type does ipratropium function on?

A

bronchiolar SMCs

299
Q

What do ganglionic blockers do in the heart?

A

tachycardia

300
Q

What do ganglionic blockers do in the iris?

A

mydriasis

301
Q

What do ganglionic blockers do in the ciliary muscle?

A

cycloplegia

302
Q

What is the MOA of bretylium? What protein is inhibited?

A

prevents adrenergic vesicle fusion

VAMP

303
Q

What organ is COMT contained in?

A

Liver

304
Q

Where is the highest density of α1 adrenergic receptors?

A

arterioles

305
Q

What agonist binds vanilloid receptors?

A

capsacin

306
Q

What is another name for phenylephrine?

A

neo-Synephrine

307
Q

What are the four α2 agonists?

A

Clonidine (Catapres)
α-Methyldopa (aldomet)
Apraclonidine
Brimonidine

308
Q

What is another name for aproclonidine?

A

Lodipine

309
Q

What is another name for Brimonidine?

A

Alphagan

310
Q

What are aproclonidine and Brimonidine used for?

A

Tx of glaucoma

311
Q

What is the most important side effect of β2 selective agonists? Especially if used in combination with what?

A

tachycardia

MAO Inhibitors

312
Q

Other than D1 receptors, what receptor can Fenoldopam/Colorpam activate?

A

α2

313
Q

In what situation is the use of fenoldopam appropriate? What is the side effect?

A

Hypertensive crisis

hypotension

314
Q

What is another name for isoproterenol? Does isoproterenol have any effect on α receptors?

A

Isuprel

α = zero effect

315
Q

Tx of what potentially fatal condition is isoproterenol useful?

A

TdP

316
Q

What is another name for dobutamine?

A

dobutrex

317
Q

Does dobutamine affect TPR? Why or why not?

A

no

α1 and β2 balance

318
Q

What is the therapeutic use of dobutamine?

A

short-term tx of CHF

319
Q

What receptors does epinephrine activate at small doses?

A

β1 and β2

320
Q

What receptors does epinephrine activate at mod doses?

A

β1 and β2 and α1

321
Q

What receptors does epinephrine activate at high doses, in order? What is the systemic effect of this?

A

α1 and β1 and β2

reflex bradycardia

322
Q

What two sites in the vasculature are the primary targets of epinephrine?

A

arterioles

pre-capillary sphincters

323
Q

Where can a large dose of epinephrine cause hemorrhage?

A

cerebral hemorrhage

324
Q

When is the use of epinephrine contraindicated?

A

patients on non-selective β-blockers

325
Q

What receptor does norepinephrine have little effect on?

A

β2

326
Q

What is the main CV effect of norepinephrine?

A

increase in MAP

327
Q

Is dopamine degraded by MAO? COMT?

A

MAO = yes

COMT = yes

328
Q

Through what administration route is dopamine ineffective?

A

orally

329
Q

What is the main effect of dopamine at low dose?

A

natriuresis

330
Q

What are the two main effects of dopamine at moderate doses?

A

inotropic

increase pulse pressure

331
Q

What is the main effect of dopamine at high doses? What receptor?

A

vasoconstriction

α1

332
Q

What two drugs is the use of dopamine contraindicated in?

A

MAOI

Tricyclics

333
Q

What broad class of molecules does dopamine release from vesicles?

A

biogenic amines

334
Q

What peripheral receptors does amphetamine activate?

A

α and β

335
Q

Which smooth muscle can amphetamine activate?

A

bladder smooth muscle

336
Q

What drug is contraindicated with tyramine ingestion?

A

MAO I

337
Q

What is another name for phenoxybenzamine?

A

Dibenylzine

338
Q

What is another name for Prazosin?

A

Minipress

339
Q

Is phenoxybenzamine a reversible or irreversible?

A

irreversible

340
Q

What other three receptors can phenoxybenzamine block?

A

H1, acetylcholine and serotonin

341
Q

What is another name for tamsulosin? What receptor does it antagonize?

A

Flomax

a1a

342
Q

Why do β2 agonists cause hypokalemia?

A

β2 receptors mediate potassium uptake from muscle

343
Q

Other than magneisum, what drug can be used to treat Torsades de Pointes?

A

isoproterenol

344
Q

In what condition can dobutamine be contraindicated?

A

atrial fibrillation

345
Q

What does epinephrine do to GI smooth muscle tone?

A

relax

346
Q

Which stimulates β1 receptors more, epinephrine or norepinephrine?

A

they are equal

347
Q

What do βblockers do to lipolysis?

A

decrease

348
Q

What do β-blockers do to glucagon release?

A

decrease

349
Q

What does neuropeptide Y do to norepinephrine release?

A

inhibit

350
Q

What organelle is Acetyl-CoA Synthesized?

A

mitochondria

351
Q

What drug is used to Dx parasympathetic dysfunction?

A

Pilocarpine

352
Q

Other than the kidneys, where is a common location for D1 receptors? What is the effect of activation of these receptors?

A

heart

vasodilation

353
Q

Other than D1, what receptor can fenoldopam activate? What does this lead to?

A

α2

feedback inhibition of norepinephrine

354
Q

What three receptors does dobutamine activate?

A

β1 and β2 and α1

355
Q

What can a high dose of carbachol produce?

A

cardiac risk

356
Q

What drug can be used to treat paroxymal atrial tachycardia?

A

phenylepherine

357
Q

Would dobutamine be used during atrial fibrillation?

A

no

358
Q

Why can dopamine have a positive inotropic effect at moderate doses?

A

increase NE release from nerve terminals

359
Q

Other than α1 , what three receptors can pheoxybenzamine block?

A

H1, acetylcholine and serotonin

360
Q

What does dopamine do to diastolic blood pressure?

A

nothing

361
Q

Why are bethanechol and carbachol resistant to AchE?

A

amide instead of ester bond

362
Q

What is the Rx of choice for glaucoma?

A

Pilocarpine

363
Q

In what condition is succinylcholine contraindicated?

A

patient with burns

364
Q

What is the specific function of dobutamine?

A

acute treatment of reversible heart failure

365
Q

What is the mechanism by which epinephrine can increase coronary blood flow?

A

coronary arteries have beta-two receptors

366
Q

Why can epinephrine cause cerebral hemorrhage? When can this happen?

A

severe hypertension

beta blockade

367
Q

What does norepinephrine do to cardiac output ?

A

decrease or no effect

368
Q

What can a high dose of bethanechol do to the heart?

A

cardiac arrest

369
Q

Which muscarinic alkaloid, at high doses, can stimulate the cortical neurons?

A

pilocarpine

Pharm (12 decks)

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