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Pharm > Chapter 9: Adrenegic Agonist > Flashcards

Chapter 9: Adrenegic Agonist Flashcards

Test 2

1
Q

What NS does Adrenergic Agonist mimic?

A

SNS

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2
Q

SNS is largely mediated by which natural ligand?

A

NE

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3
Q

What is the main neurotransmitter in adrenergic agonists?

A

catecholamines

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4
Q

What are catecholamines derived from?

A

tyrosine

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5
Q

What type of adrenergic agonists do we have?

A

direct
indirect

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6
Q

What is a amine group?

A

NH(2)

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7
Q

What is a Catechol group?

A

Benzine ring with a -OH at carbon 3 and 4 (2x -OH)

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8
Q

What is a catecholamine?

A

A catechol group and a amine group combined

main adrenergic receptor neurotransmitter

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9
Q

T/F: Substitution in the catecholamine reduces potency

A

T

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10
Q

Can you take catecolamines orally? Why?

A

No

Instantly metabolized inactivated in the gut

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11
Q

What enzyme inactivates catecholaimes in the gut?

A

“COMT”

Catechol-O-methyltransferase

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12
Q

Is phenylephrine a catecholamine?

A

No. It does not have a catechol group

Lacks -OH at carbon 4

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13
Q

How do you count carbons?

A

Start at 3oclock —- Counter clockwise

Ex) 3oclock is carbon 1

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14
Q

Describe Non-catecholamines that lack a hydroxyl group

A

Longer half lives
Increased lipid solubility
increased oral bioavailability
Not inactivated by COMT

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15
Q

What is an hydroxyl group?

A

-OH

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16
Q

With catecholamines, what happens when you have a substitution at the Alpha carbon?

A

Prolonged action
Blocked oxidation by monoamine oxidase (MAO)

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17
Q

What is the Alpha Carbon?

A

The second carbon from the benzine ring in catecholamines

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18
Q

What is the beta carbon?

A

the 1st carbon from the benzine ring in catecholamines

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19
Q

Adrenergic receptors are all _______ receptors

A

GPCRs

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20
Q

T/F: No drug is specific for receptor subtype (only A2, only B1)

A

T

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21
Q

Epinephrine has the strongest affect on which receptor?

A

Alpha

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22
Q

Isoproterenol has the strongest affect on which receptor?

A

Beta

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23
Q

Beta-1 think

A

heart

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24
Q

Beta-2 think

A

lungs

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25
Q

T/F: B-1 has an equal affinity for epi and NE

A

T

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26
Q

B-2 has a greater affinty for _______

A

epi

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27
Q

Describe Clonidine

A

A2 agonist

G(i)

decrease bp

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28
Q

how many subtypes does Dopamine-R have?
Where are they found

A

5

Brain
Renal Vascular beds

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29
Q

NET =

A

NETransporter

Transport NE into Presynapse

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30
Q

DAT =

A

Dopamine Transporter

Transport Dopamine into presynapse

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31
Q

ST =

A

Serotonin Transporter

Transport Serotonin into presynapse

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32
Q

What does cocaine do NET at the synapse?

A

Blocks NET on the presynapse

Blocks NE reuptake
Prolonged NE at the synapse

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33
Q

What does amphetamines do at the synapse?

A

reverses NE through the NET
Increases/prolonged NE at synapse

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34
Q

Where is Beta-3 receptors?

A

Fat cells

35
Q

Where are Alpha 2 receptors?

A

CNS

36
Q

Many Adrenergic agonists are what type of drugs? What do they do?

A

Pressors

Increase BP

37
Q

T/F: there are both Alpha and Beta receptors in the peripheries

A

T

38
Q

Stimulation of B receptors does:

A

Increase CO

Decrease peripheral resistance

39
Q

What is CO?

A

Cardiac Output

CO= SV x HR

40
Q

What is normal CO?

A

5250 ml/min

41
Q

What type of drug is phenylephrine?

A

Alpha agonist

42
Q

T/F: There are more Beta receptors on skeletal muscles than smooth muscle

A

T

This allows them to dilate during fight or flight response

43
Q

How do catecholamines affect the eye?

A

Alpha - dilates
Beta - no effect
Beta blockers - decrease production of aqueous humor

44
Q

What catecholamines is useful in glaucoma?

A

Beta bloclers eye drops
decrease production of aqueous humor at the ciliary epithelium

45
Q

How do catecholamines affect the lung?

A

Beta-2: Dilates
Ex) Albuterol

46
Q

How do catecholamines affect the GI?

A

Alpha and Beta both relax

47
Q

Can catecholamines cross the BBB? Why?

A

Most cant

2 positively charged -OH on the catechol

48
Q

Why do non-catecholamines have an effect on the CNS?

A

They cross the BBB better because they have 1 less -OH group on the benzine ring making it less charged

Ex) Cocaine, Amphetamine

49
Q

Drugs: Norepinephrine

A

Catecholamine
A1/B1 agonist

Increase SBP/DBP
vagus reflex overcomes chronotropic effects

50
Q

Drugs: Epinephrine

A

Catecholamine
A1/B1/B2 agonist

increase in BP, HR, Contractility , dilation of bronchioles

51
Q

Drugs: Isoproterenol

A

Beta agonist
Little to no Alpha effects

Increased CO
Fall in MAP slight decrease/increase in SBP

52
Q

What does does low dose dopamine do?

A

DA-1 - induces diuresis

53
Q

What does high doses of dopamine do?

A

Activates Alpha receptors
mimic epinephrine
vasoconstrictor
increases HR

54
Q

What does medium doses of dopamine do?

A

Activate Beta-1 receptors
increase CO

55
Q

Drugs: Dobutamine

A

Catecholamine
B1 selective agonist

Tx: Cardiac shock, Acute heart failure

56
Q

Drugs: Phenylephrine

A

Non-Catecholamine
Pure Alpha agonist

Tx: Congestion; low BP

57
Q

What is Tetralogy of Fallot?

A
  1. Overriding aorta
  2. Pulmonic stenosis
  3. Ventricular Septal Defect
  4. Right Ventricular Hypertrophy

All 4 of these causes mixing of oxygenated and deoxygenated blood in the heart.

58
Q

What is Tx for Tetralogy of Fallot?

A

Phenylephrine

Squatting can temporarily fix if turning blue.

59
Q

Drugs: Midodrine

A

Sympathomimetic
Alpha-1 selective agonist

Tx: Orthostatic hypotension (postural)

causes HTN in supine pt

60
Q

Drugs: Ephedrine

A

NOT AVAILABLE IN US

Sympathomimetic
Direct – mimics epi (crosses BBB)
Indirect – releases stored catecholamines

Tx: Derivative Pseudoephedrine: nasal decongestant

61
Q

What compound can you make meth from?

A

Ephedrine and pseudoephedrine

62
Q

what fraction of people who try cocaine will get addicted vs meth?

A

2/5 for cocaine

4/5 for meth

63
Q

Drugs: Methamphetamine

A

Sympathomimetic
crosses BBB
prone to addiction
Higher effects in CNS

64
Q

Drugs: Amphetamine

A

Sympathomimetic
Crosses BBB - higher effects in CNS
Mood elevator
supresses appetite

65
Q

Drugs: Cocaine

A

Indirect sympathomimetic

Crosses BBB – enters CNS

Inhibits NE and Dopamine reuptake by blocking DAT and NET

66
Q

Cocaine has similar effects to _________

A

Amphetamine

67
Q

T/F: Cocaine can cause fatal arrythmias

A

T

68
Q

What is Tyramine?

A

Byproduct of tyrosine
Indirect sympathomimetic

High concentration in fermented foods

Releases stored catecholamines

Metabolized by MAOI

69
Q

What will happen if you taking MAOI and eat fermented foods?

A

fermented foods are high in tyramine which releases catecholamines when metabolized by MAOIs

This will cause your BP to increase significantly

70
Q

What are some examples of fermented foods?

A

Cheese
Wine
Yeast
Sausage
Smoked/Pickled Fish

71
Q

Tx: Hypotensive Emergency

A

NE
Phenylephrine

72
Q

Tx: Cardiogenic shock

A

Dobutamine
vasodilators

73
Q

Tx: Septic shock

A

Volume
NE

74
Q

Describe the use of Epi in local anesthesia

A

Alpha 2 receptors in the periperhies cause vasoconstriction which can help achieve hemostasis during Sx. usually mixed with lidocaine for numbing

75
Q

Tx: Heart block

A

Atropine, dopamine, isoproterenol

76
Q

Tx: Cardiac arrest

A

Epi…

Honestly everything.

77
Q

What is the most effective way to treat a heart block?

A

Pacemaker

78
Q

Tx: Asthma

A

B-2 selective agonists

Metaproterenol
Terbutaline

79
Q

Tx: Asthma attack

A

B-2 selective agonists

Albuterol - rescue inhaler

80
Q

Tx: Anaphylaxis

A

A1/B1/B2 agonist

IM Epi

81
Q

Describe the overall effect of A2 agonists

A

Overall it lowers BP

decreases BP in CNS but Increases BP in peripheries

82
Q

Name 2 Alpha-2 agonist

A

Clonidine
Precedex (Dexmedetomidine)

83
Q

How do Alpha-2 agonist work?

A
  1. the drug binds to the receptor which is on the rostral ventral lateral medulla (RVLM)
  2. This increases firing of the vagus nerve
  3. this also decreases firing of the sympathetic nerves
  4. This leads to: Decreases HR/SV/VR/Overall BP
84
Q

Symptoms of Sympathomimetic toxicity include:

A

Pressors: HTN, cerebral hemorrhage, pulmonary edema, Angina, Cardiac tamponade, MI

CNS (Cocaine/Amphetamines): Arrhythmias, MI, Seizures, cerebral hemorrhage

Pharm (30 decks)

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