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Pharm Unit 1 > 4. Pharmacologic Adrenergics > Flashcards

4. Pharmacologic Adrenergics Flashcards

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
Q

What are the non-selective alpha adrenergic antagonists? What are the 2 types?

A

Phentolamine (reversible)

Phenoxybenzamine (irreversible)

26
Q

What is the selective alpha 1 agonist?

A

Phenylepherine

27
Q

What is the selective alpha 1 antagonist?

A

Prazosin

28
Q

What is the selective alpha 2 agonist?

A

Clonodine

29
Q

What is the selective alpha 2 antagonist?

A

Yohimbe

30
Q

What is the non-selective beta antagonist?

A

Propranalol

31
Q

What is the selective beta 1 agonist?

A

Metoprolol

32
Q

What is the selective beta 2 agonist?

A

Metaproterenol, albuterol, ritodrine

33
Q

What is the location & function of beta 3 receptors?

A

Stim lypolysis

Fat cells

34
Q

What are agonists for the Dopamine receptor?

A

Dopamine&raquo_space; epi

35
Q

List in order of potency the receptors for NE

A

Alpha 1 = alpha 2 = beta 1&raquo_space;beta 2

36
Q

List in order of potency the receptors for Phenylepherine

A

Only alpha 1

37
Q

Effects of NE?

A

Alphas –> increase TPR & BP
Beta 1 –> increased contract
Reflex –> decreased BP

No change in CO due to beta 1 balancing out reflex

38
Q

Effects of Phenyelepherine?

A

same as NE

39
Q

BP is the dependent on what?

A

TPR x SV x HR

40
Q

List in order of potency the receptors for low dose Epi

A

beta 1 = beta 2 > alpha 1 = alpha 2

41
Q

List in order of potency the receptors for high dose Epi

A

see NE

42
Q

Effects of high dose Epi?

A

see NE

43
Q

Effects of low dose Epi?

A

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
Q

List in order of potency the receptors for high dose Isoproterenol

A

beta 1 = beta 2

45
Q

Effects of Isoproterenol?

A

Same as low dose epi but mean arterial pressure decreases slightly cuz TPR & diastolic pressure a lower more

46
Q

Effects of Ephedrine?

A

Mainly indirect but some alpha & beta

Increase contractility
beta 2 –> bronchodilation
low/moderate doses –> increase in HR
high dose –> increased BP with bradycardia

47
Q

What sympathomemtic drug has a long duration?

A

ephedrine

48
Q

Effects of albuterol?

A

relaxes smooth muscle of airway

49
Q

Effects of Ritodrine?

A

relaxes smooth muscle fo uterus –> prevent premature birth

50
Q

Effects of Dopamine?

A

Increased blood flow
Moderate dose –> increased HR & contractility
High dose –> increased TPR

51
Q

Effects of Dobutamine?

A

Increased contractility, HR & BP

High dose –> increase TPR

52
Q

Effects of Phentolamine & Phenoxybenzamine?

A

Decreased TPR
Decreased BP in standing (no change in lying)
Reflex raise in HR & blood volume

53
Q

Side effects of Phentolamine & Phenoxybenzamine?

A

Postural hypotension

Tachycardia

54
Q

Effects of Prazosin?

A

Same as non-selective but less reflex

55
Q

Effects of propranalol?

A

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
Q

Side effects of propranalol?

A

cardiac depression, lassititude (fatigue) & depression

57
Q

Effects of metoprolol?

A

Same as propranalol, but no effect on airway

58
Q

Where are dopamine receptors located?

A

CNS & renal

59
Q

What is the partial beta agonist?

A

Pindolol

60
Q

Pindolol is a what? Uses?

A

Partial beta agonist

HTN

61
Q

What is the combined alpha beta blocker?

A

Labetalol

62
Q

Labetalol is what? Uses?

A

Alpha & beta blocker

HTN emergency

Pharm Unit 1 (7 decks)

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