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Therapeutics > lecture 4 > Flashcards

lecture 4 Flashcards

1
Q

Norepinephrine and epinephrine structure difference

A

Epinephrine has extra CH3 group

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2
Q

Monoamine structure

A

contains 1 amino group connected to aromatic ring by two carbon chain

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3
Q

Catecholamine structure

A

Aromatic ring with two OH groups

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4
Q

rate limiting step in cathecholamine biosynthesis

A

Tyrosine hydroxylase

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5
Q

Biosynthesis of catecholamine steps

A
  1. Tyrosine will have OH added by tyrosine hydroxylase to form L-DOPA
  2. L-DOPA loses COOH by decarboxylase to form dopamine
  3. Dopamine hydroxylase adds OH to form norepinephrine
  4. Adrenal medulla adds CH3 to form epinephrine
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6
Q

Inhibitory for rate limiting step for cathecholamines

A

Metyrosine

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7
Q

Inhibitor of decarboxylase step in catecholamine synthesis

A

Carbidopa

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8
Q

Dopamine is transported into vesicle by________

A

VMAT

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9
Q

NE binds_____ on post synaptic and _____ on pre synaptic

A

Adrenergic receptor
regulatory receptor

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10
Q

NE is re-uptaken by

A

Norepinephrine transporter

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11
Q

NE is metabolized by_______

A

MAO and COMT

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12
Q

Where is COMT found?

A

highest activity in liver.

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13
Q

Where is MAO found in highest concentrations?

A

nerve terminal, liver

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14
Q

Stereochemistry required for norepinephrine with adrenergic receptors interaction

A

Only R isomer in B carbon can have a strong affinity to receptor.

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15
Q

A1 receptor action on blood vessels

A

Vasoconstriction (innervated)

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16
Q

A1 receptor action on pupils

A

Dilation

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17
Q

A1 receptor action on vas deferens

A

Ejaculation

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18
Q

A1 receptor action on GI tract

A

GI inhibition

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19
Q

A2 receptor effect on blood vessels

A

Vasoconstriction (uninnervated)

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20
Q

main use of a2 receptor

A

pre-junctional inhibition of NE release

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21
Q

A2 receptor use in CNS

A

reduce SNS in[ut

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22
Q

B1 receptor use in cardiac system

A

cardiac stimulation

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23
Q

B1 receptor use in kidney

A

Secretion of renin

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24
Q

B2 receptor use in general

A

RELAXATION

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25
Q

B2 effect on lungs

A

Bronchodilation

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26
Q

B2 effect on vasculature

A

Vasodilation

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27
Q

B2 effect on bladder

A

Relaxation

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28
Q

Which neurotransmitter acts on a1, a2, and B1 but not B2

A

Norepinephrine. Epinephrine works on all.

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29
Q

Why does epinephrine bind B2 but not norepinephrine

A

methyl added to epi makes it easier to bind.

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30
Q

Is epinephrine more selective to B or A

A

Beta

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31
Q

2 direct acting adrenergic recetpro agonists

A

Norepinephrine and epinephrine

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32
Q

Norepinephrine is a potent agonist for which receptors

A

A and B1

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33
Q

Why is Norepinephrine only IV and not oral

A

It is broken down by MAO and COMT. (First pass effect will be metabolized by liver.)

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34
Q

What receptors are targeted at lower concentrations of epinephrine

A

B1 and B2

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35
Q

Clinical use of epinephrine

A

Treats acute anaphylaxis or cardiac arrest

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36
Q

Why is epinephrine also not orally available

A

First pass effect

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37
Q

Norepinephrine effect on A1

A

Vasoconstriction

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38
Q

Norepinephrine effect on B1

A

increases cardiac force and conduction.

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39
Q

epinephrine effect on B2

A

Vasodilation and bronchodilation

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40
Q

Dopamine effect on renal system

A

Vasodilation

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41
Q

Dopamine effect on a1

A

Vasoconstriction

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42
Q

Clinical use of dopamine

A

Shock, acute heart failure (IV)

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43
Q

what is dobutamine

A

Dopamine derivative

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44
Q

Why does dobutamine need to be a racemic mixture

A

Leads to selective inotropic effect on heart rather than a chronotropic effect

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45
Q

Why does dobutamine have an inotropic effect rather than chronotropic

A

+ enantiomer is a potent B1 receptor agonist
- enantiomer is a potent A1 receptor agonist

46
Q

a1 signaling pathway and mechanism

A

Gq- Mobilizes intracellular Ca2+ to activate PKC

47
Q

a1 agonist clinical use

A

Nasal decongestion
Vascular failure and tachycardia

48
Q

a1 antagonist clinical use

A

HTN
BPH
pheocromocytoma

49
Q

structural difference between epinephrine and phenylephrine

A

Phenylephrine lacks 1 OH group

50
Q

Effect of lack of OH group in phenylephrine compared to epinephrine

A

Gives phenylephrine a1 selectivity

51
Q

clinical use of phenylephrine

A

nasal decongestant
mydriasis
vasoconstriction in anesthesia

52
Q

is phenylephrine a substrate for MAO and COMT?

A

MAO yes, not COMT

53
Q

What effect does imidazoline being charged have on its PH

A

Makes it more basic.

54
Q

What pathway does A2 have and state its mechanism

A

Gi pathway. Inhibits adenylyl cyclase and inhibits neuronal Ca2+

55
Q

Where in the synaptic system is a2 found? What is its function there?

A

It is found pre synaptically and functions as an autoreceptor to inhibit sympathetic output

56
Q

How does a2 inhibit sympathetic output

A

Acts as an autoreceptor. It is a feedback inhibitor.

57
Q

a2 agonist clinical use

A

HTN
pain
glaucoma

58
Q

a2 agonist drugs structures?

A

clonidine, apraclonidine, methyldopa, guanabenz, guanafacine, brimonidine

59
Q

use of the 2 Cls in clonidine

A

Since Cls are electron withdrawing, this lessens the PKA. This increases CNS access.

60
Q

activation a2 receptors in CNS ________ SNS activity

A

Decrease

61
Q

side effects of a2 agonist

A

hypotension, sedation, dry mouth

62
Q

effects of a2 on CNS

A

a2 limits sympathetic output. This decreases HR and renin release.

63
Q

example of a2 agonists with open ring imidazoline

A

guanabenz, guanafacine

64
Q

a2 agonist with shortest half life

A

Guanabenz

65
Q

why is methyldopa a prodrug and not a drug

A

Methyldopa has CNS access. It is transformed to methylnorepinephrine on action site.

66
Q

the pro drug methyl dopa is transformed to

A

methylnorepinephrine

67
Q

difference in water solubility between methyldopate and methyldopa

A

Methyldopate has good water solubility
methyldopa does not.

68
Q

why is methyldopa oral

A

non-water soluble

69
Q

why is methyldopate parenteral?

A

is highly soluble

70
Q

Brimonidine clinical use

A

Glaucoma

71
Q

how does brimonidine treat glaucoma

A

inhibits aqueous humor production

72
Q

What drug has para NH2 on clonidine

A

Apraclonidine

73
Q

Effect of para NH2 on apraclonidine

A

increases PKA

74
Q

B1 found in

A

heart and kidney

75
Q

B1 effect on heart

A

increase force, HR and conduction

76
Q

B1 effect on kidney

A

Increase renin release

77
Q

B1 agonist use

A

shock, congestive HF

78
Q

B1 antagonist use

A

hypertension
angina
arrythmia
congestive HF

79
Q

B2 generally used for

A

Relaxation

80
Q

B2 agonist clinical use

A

Asthma, premature labour

81
Q

B2 antagonist use

A

Glaucoma

82
Q

B3 found in

A

urinary bladder

83
Q

B3 agonist use

A

Overactive bladder

84
Q

B1 selective 2 drugs

A

Dobutamine, Dopamine

85
Q

B2 selective 2 drugs

A

Albuterol, Salmeterol

86
Q

Non-selective B agonist drug name

A

Isoprotorenol

87
Q

Why is isoproterenol more selective for B than A

A

It has a bulky substitute (just like epinephrine)

88
Q

Clinical use of isoproterenol

A

Bronchodilation and increase cardiac output

89
Q

Is isoproterenol sensitive to MAO?

A

No. (can be used oral)

90
Q

reflex tachycardia definition

A

When BP decreases, heart rate is automatically increased

91
Q

reflex bradycardia definition

A

increased BP leads to increase in HR

92
Q

why are metaproterenol and terbutaline B2 selective

A

Position of OH in catechol ring is different

93
Q

Are metaproterenol and terbutaline metabolized by MAO and COMT

A

No

94
Q

why is albuterol B2 selective

A

hydroxy methyl instead of hydroxy

95
Q

Side effects of B2 agonist drugs

A

Minor cardiac output in high doses

96
Q

indirect acting sympathomimetics example

A

Ampthetamines, cocaine

97
Q

How does amphetamine indirectly affect NE concentration

A

Amphetamines reverse norepinephrine transporters. This is why they act so long.

98
Q

How does cocaine affect the Norepinephrine

A

Cocaine completely blocks the norepinephrine transporters from reuptaking the neurotransmitter from the cleft.

99
Q

Why doesn’t amphetamine bind to adrenergic receptor

A

lacks catechol. (Also the reason it is not metabolized by COMT)

100
Q

Is amphetamine susceptible to MAO? why or why not

A

No. Methyl group on amphetamine interferes.

101
Q

how do we treat amphetamine/methamphetamine overdose

A

Acidify urine to increase excretion

102
Q

why does ephedrine have a direct A and B agonist activity on adrenergic receptors

A

Has R configuration

103
Q

Why does ephedrine have A and B agonist activity, but not pseudoephedrine.

A

R-config at B-OH in ephedrine. S config in pseudoephedrine reduces agonist activity

104
Q

Biggest caution when taking ephedrine and pseudoephedrine

A

DO not use if taking MAO-inhibitors

105
Q

Why avoid MAOI when taking ephedrine and pseudoephedrine

A

NE will not be degraded, giving a strong sympathetic response.

106
Q

Action of cocaine

A

Blocks NET, decreases reuptake, enhances NE signaling by keeping more neurotransmitters in cleft

107
Q

Side effects of cocaine

A

Increase BP and HR

108
Q

methylphenidate action

A

blocks NE and dopamine reuptake.

109
Q

Use of methylphenidate

A

ADHD, narcolepsy

110
Q

Atomoxetine action

A

inhibits NET

111
Q

Issues for atomoxetine

A

Blackbox indication for suicidal ideation

Therapeutics (46 decks)

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