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Pharm Fall 2024 > Chapter 9: Adrenegic Agonist > Flashcards

Chapter 9: Adrenegic Agonist Flashcards

Test 2 (84 cards)

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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
T/F: B-1 has an equal affinity for epi and NE
T
26
B-2 has a greater affinty for _______
epi
27
Describe Clonidine
A2 agonist G(i) decrease bp
28
how many subtypes does Dopamine-R have? Where are they found
5 Brain Renal Vascular beds
29
NET =
NETransporter Transport NE into Presynapse
30
DAT =
Dopamine Transporter Transport Dopamine into presynapse
31
ST =
Serotonin Transporter Transport Serotonin into presynapse
32
What does cocaine do NET at the synapse?
Blocks NET on the presynapse Blocks NE reuptake Prolonged NE at the synapse
33
What does amphetamines do at the synapse?
reverses NE through the NET Increases/prolonged NE at synapse
34
Where is Beta-3 receptors?
Fat cells
35
Where are Alpha 2 receptors?
CNS
36
Many Adrenergic agonists are what type of drugs? What do they do?
Pressors Increase BP
37
T/F: there are both Alpha and Beta receptors in the peripheries
T
38
Stimulation of B receptors does:
Increase CO Decrease peripheral resistance
39
What is CO?
Cardiac Output CO= SV x HR
40
What is normal CO?
5250 ml/min
41
What type of drug is phenylephrine?
Alpha agonist
42
T/F: There are more Beta receptors on skeletal muscles than smooth muscle
T This allows them to dilate during fight or flight response
43
How do catecholamines affect the eye?
Alpha - dilates Beta - no effect Beta blockers - decrease production of aqueous humor
44
What catecholamines is useful in glaucoma?
Beta bloclers eye drops decrease production of aqueous humor at the ciliary epithelium
45
How do catecholamines affect the lung?
Beta-2: Dilates Ex) Albuterol
46
How do catecholamines affect the GI?
Alpha and Beta both relax
47
Can catecholamines cross the BBB? Why?
Most cant 2 positively charged -OH on the catechol
48
Why do non-catecholamines have an effect on the CNS?
They cross the BBB better because they have 1 less -OH group on the benzine ring making it less charged Ex) Cocaine, Amphetamine
49
Drugs: Norepinephrine
Catecholamine A1/B1 agonist Increase SBP/DBP **vagus reflex overcomes chronotropic effects**
50
Drugs: Epinephrine
Catecholamine A1/B1/B2 agonist increase in BP, HR, Contractility , dilation of bronchioles
51
Drugs: Isoproterenol
Beta agonist Little to no Alpha effects Increased CO Fall in MAP slight decrease/increase in SBP
52
What does does low dose dopamine do?
DA-1 - induces diuresis
53
What does high doses of dopamine do?
Activates Alpha receptors mimic epinephrine vasoconstrictor increases HR
54
What does medium doses of dopamine do?
Activate Beta-1 receptors increase CO
55
Drugs: Dobutamine
Catecholamine B1 selective agonist Tx: Cardiac shock, Acute heart failure
56
Drugs: Phenylephrine
Non-Catecholamine Pure Alpha agonist Tx: Congestion; low BP
57
What is Tetralogy of Fallot?
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
What is Tx for Tetralogy of Fallot?
Phenylephrine Squatting can temporarily fix if turning blue.
59
Drugs: Midodrine
Sympathomimetic Alpha-1 selective agonist Tx: Orthostatic hypotension (postural) **causes HTN in supine pt**
60
Drugs: Ephedrine
**NOT AVAILABLE IN US** Sympathomimetic Direct -- mimics epi (crosses BBB) Indirect -- releases stored catecholamines Tx: Derivative Pseudoephedrine: nasal decongestant
61
What compound can you make meth from?
Ephedrine and pseudoephedrine
62
what fraction of people who try cocaine will get addicted vs meth?
2/5 for cocaine 4/5 for meth
63
Drugs: Methamphetamine
Sympathomimetic crosses BBB prone to addiction Higher effects in CNS
64
Drugs: Amphetamine
Sympathomimetic Crosses BBB - higher effects in CNS Mood elevator supresses appetite
65
Drugs: Cocaine
Indirect sympathomimetic Crosses BBB -- enters CNS Inhibits NE and Dopamine reuptake by blocking DAT and NET
66
Cocaine has similar effects to _________
Amphetamine
67
T/F: Cocaine can cause fatal arrythmias
T
68
What is Tyramine?
Byproduct of tyrosine Indirect sympathomimetic **High concentration in fermented foods** Releases stored catecholamines **Metabolized by MAOI**
69
What will happen if you taking MAOI and eat fermented foods?
fermented foods are high in tyramine which releases catecholamines when metabolized by MAOIs This will cause your BP to increase significantly
70
What are some examples of fermented foods?
Cheese Wine Yeast Sausage Smoked/Pickled Fish
71
Tx: Hypotensive Emergency
NE Phenylephrine
72
Tx: Cardiogenic shock
Dobutamine vasodilators
73
Tx: Septic shock
Volume NE
74
Describe the use of Epi in local anesthesia
Alpha 2 receptors in the periperhies cause vasoconstriction which can help achieve hemostasis during Sx. usually mixed with lidocaine for numbing
75
Tx: Heart block
Atropine, dopamine, isoproterenol
76
Tx: Cardiac arrest
Epi... Honestly everything.
77
What is the most effective way to treat a heart block?
Pacemaker
78
Tx: Asthma
B-2 selective agonists Metaproterenol Terbutaline
79
Tx: Asthma attack
B-2 selective agonists Albuterol - rescue inhaler
80
Tx: Anaphylaxis
A1/B1/B2 agonist IM Epi
81
Describe the overall effect of A2 agonists
Overall it lowers BP **decreases BP in CNS but Increases BP in peripheries**
82
Name 2 Alpha-2 agonist
Clonidine Precedex (Dexmedetomidine)
83
How do Alpha-2 agonist work?
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
Symptoms of Sympathomimetic toxicity include:
Pressors: HTN, cerebral hemorrhage, pulmonary edema, Angina, Cardiac tamponade, MI CNS (Cocaine/Amphetamines): Arrhythmias, MI, Seizures, cerebral hemorrhage

Pharm Fall 2024 (30 decks)

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