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Pharm Unit 1 > 4. Pharmacologic Adrenergics > Flashcards

4. Pharmacologic Adrenergics Flashcards

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1
Q

What are the steps of NE synthesis?

A

Phenyalanine –> tyrosine –> uptake by nerve–> DOPA –> Dopamine –> taken up into storage granules by active transport –> NE –> release

In renal medulla NE converted to Epi

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2
Q

Enzyme that converts phyalanine into tyrosine?

A

Phenylalanine hydroxylase

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3
Q

Enzyme that converts Tyrosine to Dopa? What drug inhibits this enzyme?

A

Tyrosine hydroxylase

Metyrosine

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4
Q

What is the rate limiting step of NE synth?

A

Tyrosine to Dopa

Tyrosine hydroxylase

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5
Q

Enzyme that converts Dopa to Dopamine? What drug inhibits this enzyme?

A

Aromatic acid decarboxylase

Alpha methyl dopa

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6
Q

Enzyme that converts Dopamine to NE? What drug inhibits this enzyme?

A

Dopamine beta hydroxylase

Reserpine

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7
Q

Enzyme that converts NE to Epi?

A

Phenylethanolamine N methyl transferase

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8
Q

What is the most important way for NE to be removed from the cleft?

A

Reuptake into presynaptic side (active transport)

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9
Q

How is NE removed from the cleft?

A

Reuptake into presynaptic side (active transport)
Diffusion into circulation
Uptake by postsynaptic side (active transport)
Metab by COMT & MAO

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10
Q

What enzymes metabolize NE?

A 
Monoamine oxidase (MAO)
Catecholomethyltransferase (COMT)
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11
Q

What does MAO do? Where is it located?

A

Metab catecholamines by deaminating

Pre-synaptic & postsynaptic

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12
Q

What does COMT do? Where is it located?

A

Metab catecholamines by causing O-methylation

Postsynaptic

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13
Q

Main mechanism of Ach removal from cleft? Main mechanism of NE removal from cleft?

A

Breakdown

Reuptake

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14
Q

What are Sympathomimetic drugs? What are the 2 main types?

A

Mimic symp stimulation
Direct (interact with receptor)
Indirect (affect release or reuptake of endogenous)
Combo

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15
Q

What are the direct Sympathomimetic drugs?

A

NE
Epi
Isopterenol (Iso)

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16
Q

What are the indirect Sympathomimetic drugs?

A

Amphetamine
Tyramine
Cocaine
Imipramine

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17
Q

Which drug(s) increase NE release?

A

Amphetamine

Tyramine

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18
Q

Which drug(s) decrease NE reuptake?

A

Cocaine

Imipramine

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19
Q

How would you test if a drug had direct or indirect Sympathomimetic effects?

A

Give reserpine to deplete endogenous NE, then give drug. If it works it is direct

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20
Q

Which Sympathomimetic drugs work via a combo of direct & indirect action?

A

Dopamine

Ephedrine

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21
Q

What are Sympatholytic drugs?

A

Inhibit NE synth pathway

No longer used very often

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22
Q

What are the Sympatholytic drugs?

A

Reserpine, Metyrosine, Alpha methyl dopa & Guanathidine

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23
Q

What drug inhibits NE release into the cleft?

A

Guanathidine

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24
Q

List the non-selective adrenergic receptor agonists in order of potency for alpha & beta:

A 
Alpha = Epi > NE >> Isopterenol
Beta = Iso > Epi > NE
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25
What are the non-selective alpha adrenergic antagonists? What are the 2 types?
Phentolamine (reversible) | Phenoxybenzamine (irreversible)
26
What is the selective alpha 1 agonist?
Phenylepherine
27
What is the selective alpha 1 antagonist?
Prazosin
28
What is the selective alpha 2 agonist?
Clonodine
29
What is the selective alpha 2 antagonist?
Yohimbe
30
What is the non-selective beta antagonist?
Propranalol
31
What is the selective beta 1 agonist?
Metoprolol
32
What is the selective beta 2 agonist?
Metaproterenol, albuterol, ritodrine
33
What is the location & function of beta 3 receptors?
Stim lypolysis | Fat cells
34
What are agonists for the Dopamine receptor?
Dopamine >> epi
35
List in order of potency the receptors for NE
Alpha 1 = alpha 2 = beta 1 >>beta 2
36
List in order of potency the receptors for Phenylepherine
Only alpha 1
37
Effects of NE?
Alphas --> increase TPR & BP Beta 1 --> increased contract Reflex --> decreased BP No change in CO due to beta 1 balancing out reflex
38
Effects of Phenyelepherine?
same as NE
39
BP is the dependent on what?
TPR x SV x HR
40
List in order of potency the receptors for low dose Epi
beta 1 = beta 2 > alpha 1 = alpha 2
41
List in order of potency the receptors for high dose Epi
see NE
42
Effects of high dose Epi?
see NE
43
Effects of low dose Epi?
Beta 1 --> increased HR Beta 2 --> decrease in TPR & decreased diastolic pressure Alphas --> decreased renal & skin perfusion Mean arterial pressure only increases slightly (systolic increases but diastolic decreases)
44
List in order of potency the receptors for high dose Isoproterenol
beta 1 = beta 2
45
Effects of Isoproterenol?
Same as low dose epi but mean arterial pressure decreases slightly cuz TPR & diastolic pressure a lower more
46
Effects of Ephedrine?
Mainly indirect but some alpha & beta Increase contractility beta 2 --> bronchodilation low/moderate doses --> increase in HR high dose --> increased BP with bradycardia
47
What sympathomemtic drug has a long duration?
ephedrine
48
Effects of albuterol?
relaxes smooth muscle of airway
49
Effects of Ritodrine?
relaxes smooth muscle fo uterus --> prevent premature birth
50
Effects of Dopamine?
Increased blood flow Moderate dose --> increased HR & contractility High dose --> increased TPR
51
Effects of Dobutamine?
Increased contractility, HR & BP | High dose --> increase TPR
52
Effects of Phentolamine & Phenoxybenzamine?
Decreased TPR Decreased BP in standing (no change in lying) Reflex raise in HR & blood volume
53
Side effects of Phentolamine & Phenoxybenzamine?
Postural hypotension | Tachycardia
54
Effects of Prazosin?
Same as non-selective but less reflex
55
Effects of propranalol?
beta 1 --> decreased HR, AV conduction, contractility & CO = decreased BP Beta 1 --> decrease renin --> decrease ang II beta 2 --> Acute increase in TPR & increase in airway resistance
56
Side effects of propranalol?
cardiac depression, lassititude (fatigue) & depression
57
Effects of metoprolol?
Same as propranalol, but no effect on airway
58
Where are dopamine receptors located?
CNS & renal
59
What is the partial beta agonist?
Pindolol
60
Pindolol is a what? Uses?
Partial beta agonist HTN
61
What is the combined alpha beta blocker?
Labetalol
62
Labetalol is what? Uses?
Alpha & beta blocker HTN emergency

Pharm Unit 1 (7 decks)

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