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Pharmacology Exam 3 > Sympathomimetics > Flashcards

Sympathomimetics Flashcards

1
Q

Sympathomimetic drugs work at what receptors?

A

Adrenergic and Cholinergic

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2
Q

What type of receptors are Adrenergic receptors?

A

G protein coupled

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3
Q

What are 3 main classes of adrenergic receptors?

A

alpha-1, alpha-2, beta-1, beta-2, dopamine

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4
Q

What does stimulation of alpha 1 receptor with NE or epi do?

A

fight/flight; mydriasis, increase BP, increase HR, urinary retention, gluconeogenesis (make sugar)

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5
Q

What does beta-1 receptor activation with epi do?

A

increase conduction through SA node so increase HR, increase CO, increase BP, increase renin release.

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6
Q

What does stimulation of beta-2 receptor do?

A

bronchodilate, pancreas increase production to combat sugar.

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7
Q

What do agonists at the alpha-1 receptor sites do to calcium?

A

increase levels of calcium

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8
Q

What do alpha-2 agonists do to cAMP

A

decrease cAMP levels when stimulated by INHIBITING adenylate cyclase

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9
Q

What g-protein is at alpha-1 receptors?

A

Gq

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10
Q

What g-protein is at alpha-2 receptors?

A

Gi

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11
Q

What g-protein is at beta 1-2 receptors?

A

Gs

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12
Q

Which g-protein is inhibitory?

A

Gi, inhibits adenylate cyclase, Gi and Gs are stimulatory

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13
Q

What’s the effector at alpha-1 receptors?

A

phospholipase C

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14
Q

What’s the 2nd messengers at alpha-1 receptors?

A

IP3, Ca+, DAG

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15
Q

What is the effector at alpha-2 receptors?

A

adenylate cyclase

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16
Q

What are the 2nd messengers at alpha-2 receptors?

A

ATP, cAMP (inhibited)

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17
Q

What is the effector at beta 1-2 receptors?

A

Adenylate cyclase

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18
Q

What are the 2nd messengers at beta 1-2 receptors?

A

ATP, cAMP.

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19
Q

Which beta receptor has a higher affinity for epi than norepi?

A

beta-2, beta-1 has equal affinity for epi and norepi

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20
Q

What happens with action at dopamine-1 receptors?

A

STIMULATE adenyl cyclase due to INCREASED cAMP, causes relaxation.

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21
Q

What happens with action at dopamine-2 receptors?

A

INHIBIT adenyl cyclase, opens K channels, DECREASE calcium influx; primarily in brain

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22
Q

What neurons synthesize dopamine?

A

CNS neurons

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23
Q

What neurons synthesize epinephrine?

A

2nd order neurons of the SNS in adrenal medulla

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24
Q

What neurons synthesize Norepi?

A

2nd order neurons of the SNS in adrenal medulla and CNS neurons

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25
Q

How are sympathomimetics grouped?

A

by mode of action and spectrum of receptors they affect; direct mode, indirect mode

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26
Q

What’s the ratio of epi:norepi in the blood from adrenals?

A

80%epi:20% norepi

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27
Q

What are some alpha agonists?

A

phenylephrine/methoaxamine, clonidine

28
Q

What are the mixed alpha/beta agonists?

A

norepi, epi

29
Q

What are the beta agonists?

A

dobutamine, isoproterenol, terbutaline/albuterol

30
Q

What are the dopamine agonists?

A

dopamine

31
Q

What receptors does phenyl have more affinity for?

A

A1>A2»B

32
Q

What receptors does clonidine have more affinity for?

A

A2>A1»B

33
Q

What receptors does Norepi have more affinity for?

A

A1=A2; B1>B2

34
Q

What receptors does Epi have more affinity for?

A

A1=A2; B1=B2

35
Q

What receptors does dobutamine have more affinity for?

A

B1>B2»A

36
Q

What receptors does isoproterenol have more affinity for?

A

B1=B2»A

37
Q

What receptors does terbutaline/albuterol have more affinity for?

A

B2>B1»A

38
Q

What receptors do dopamine agonists have more affinity for?

A

D1=D2»B»A

39
Q

What is the parent drug that sympathomimetic drugs are derived from?

A

Phenylethylamine

40
Q

What substitutions yield catecholamines?

A

subs by OH groups at the 3 and 4 positions on the benzene ring

41
Q

What metabolic effects do sympathomimetics have?

A

enhance glycogenolysis in liver leading to increased glucose in circulation, high catecholamine presence in system can cause metabolic acidosis

42
Q

What do alpha and beta receptors do to the blood vessels?

A

Alpha increase arterial resistance, beta promote smooth muscle relaxation

43
Q

What effect do pure alpha agonists have on BP?

A

increase in peripheral arterial resistance and decreased venous capacitance so increase BP and slow HR due to baroreceptor mediated increase in vagal tone

44
Q

What effect do pure beta agonists have on BP?

A

increased cardiac output, decreased peripheral vascular resistance by dilating vascular beds so increased or decreased BP with decreased DBP

45
Q

What effect do mixed alpha/beta agonists have on BP?

A

skeletal muscle bed relaxation so decreased DBP but alpha constriction of arterial beds

46
Q

Which receptor directly affects the heart?

A

beta-1, increased chronotropy and increased conduction velocity through AV node, increased contractility

47
Q

What affects on the respiratory system do beta-2 have?

A

bronchodilation

48
Q

What do alpha agonists do to the eye?

A

mydriasis (dilation) of pupil

49
Q

What do alpha and betas do to the GI tract?

A

relaxation

50
Q

What receptors are at bladder base and urethral sphincter?

A

alpha–promote urinary continence

51
Q

Where is epi synthesized, stored, and released?

A

adrenal medulla

52
Q

What are the clinical uses of epinephrine?

A

anaphylaxis, glaucoma, asthma, vasoconstrictor for LA, CPR, hemo instability, promote inotropy during weaning from bypass

53
Q

Discuss synthesis of epi.

A

Tyrosine +tyrosine hydroxylase >dihydroxyphenylalanine (DOPA) + DOPA decarboxylase >dopamine +dopamine beta-hydroxylase >Norepi +phenylethanolamine N-methyltransferase >Epi

54
Q

What is the limiting factor in the synthesis of epi?

A

tyrosine hydroxylase.

55
Q

What reduces tyrosine hydroxylase?

A

too much NE

56
Q

How much of the release of NE undergoes reuptake?

A

80%, to the presynaptic nerve

57
Q

How else is norepi removed from the site of action?

A

reuptake by extraneuronal tissues containing MAO and COMT; diffusion away from synaptic cleft–metabolized by the kidney and liver by COMT and MAO

58
Q

What does COMT metabolize epi to?

A

metanephrine

59
Q

What does MAO metabolize epi to?

A

dihydroxymandelic acid

60
Q

What does COMT metabolize dihydroxymandelic acid to?

A

Vanillylmandelic acid (VMA)

61
Q

What does MAO metabolize NE to?

A

dihydroxymandelic acid

62
Q

What does COMT metabolize NE to?

A

normetanephrine

63
Q

What does MAO metabolize metanephrine and normetanephrine to?

A

Vanillylmandelic acid (VMA)

64
Q

What do you do if your patient gets nauseous when you lay them down after a spinal.

A

treat BP…likely due to hypotension

65
Q

What drug do you use if infant BP drops?

A

Ephedrine…stroke volume is fixed in peds so the only way to fix is by fixing heart rate

66
Q

What 2 IV push meds do you have ready for a trauma coming into your room?

A

epi and vasopressin IV push. double dilute epi to get 10mcg/mL, draw vaso in 19cc saline to get 1u/mL

Pharmacology Exam 3 (5 decks)

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