sympathomimetic Flashcards

1
Q

What are the 3 natural human direct acting sympathomimetic neurotransmitters and hormones?

A

Epinephrine, norepinephrine, and dopamine

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2
Q

Name five synthetic direct receptor sympathomimetic agonists

A
phenylephrine
clonidine
isoproterenol
dobutamine
albuterol
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3
Q

Name four indirect acting sympathomimetic drugs

A

ephedrine
amphetamine
tyramine
cocaine

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4
Q

Name the four steps from tyrosine to epinephrine and what happens in each step

A

tyrosine —> dopa (tyrosine hydroxylase adds OH)
dopa —> dopamine (L-dopa decarboxylation)
dopamine —> norepinephrine (OH on the beta carbon)
norepinephrine —> epinephrine (methylation of the N)

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5
Q

What two enzymes break down NE?

A

COMT and MAO (both but in either order)

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6
Q

What are the two direct alpha agonists?

A

phenylephrine

clonidine

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7
Q

What are the three mixed alpha/beta agonists?

A

epinephrine
norepinephrine
dopamine

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8
Q

What are the four beta agonists?

A

isoproterenol
dobutamine
albuterol
mirabegron

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9
Q

phenylephrine pharmacodynamics?

A

synthetic alpha receptor agonist, much greater effect on a1 than a2 receptors

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10
Q

What are the actions of phenylephrine?

A

vasoconstriction

venoconstriction

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11
Q

Why might we prescribe phenylephrine?

A

nasal congestion
pupil dilation
to increase BP in vasodilator state during anesthesia

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12
Q

How can phenylephrine be given?

A

topical (nasal spray) or intravenous

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13
Q

is phenylephrine more or less potent than NE?

A

less

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14
Q

clonidine pharmacodynamics?

A

synthetic alpha receptor agonist selective for a2

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15
Q

what are the actions of clonidine

A

down regulation of SANS via a2 receptors in brainstem

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16
Q

Why would we prescribe clonidine?

A

treatment of hypertension and or prevent migraines

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17
Q

How is clonidine given?

A

oral or patch

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18
Q

Are there any dangers to clonidine?

A

intravenous or OD can cause low blood pressure

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19
Q

How does dobutamine work?

A

synthetic b1 receptor agonist, very little alpha stimulation at high doses

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20
Q

What are the actions of dobutamine?

A

increase heart contractility via b1 receptors (more than it increases HR)
dilation of renal and mesenteric vessels

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21
Q

Why would we prescribe dobutamine?

A
  • increase contractility more than heart rate (those in cardiogenic shock where you don’t want to produce tachycardia)
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22
Q

How is dobutamine given?

A

intravenously

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23
Q

Side effects of dobutamine?

A

unwanted tachycardia
hypertension
ectopy

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24
Q

How does albuterol work?

A

synthetic b2 receptor agonist, with a little bit of b1

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25
Q

What are the actions of albuterol?

A

acts to relax smooth muscle to dilate bronchioles or prevent uterine contractions via b2 receptors

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26
Q

Why would we prescribe albuterol?

A
  • rescue inhaler for asthma, dilator for COPD

- inhibit premature labor

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27
Q

How is albuterol given?

A
  • MDI

- nebulizer

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28
Q

side effects of albuterol

A

anxiety
tachycardia
tremor

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29
Q

How does isoproterenol work?

A

b1 and b2 agonist

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30
Q

isoproterenol actions

A
  • increase contractility
  • increase HR
  • increase cardiac conduction
31
Q

how is isoproterenol given?

A

intravenous

32
Q

other effects to remember with isoproterenol

A

will also cause vasodilation and tachyarrhythmias

33
Q

How does mirabegron work?

A

synthetic b3 agonist, small effect on b1 and b2

34
Q

mirabegron actions

A

b3 receptors on smooth muscle of bladder, reduces detrusor muscle tone

35
Q

Why would we prescribe mirabegron?

A
  • overactive bladder with urgency
  • to increase bladder capacity
  • does not produce bothersome anticholinergic symptoms like tolteridine
36
Q

how is mirabegron given?

A

orally extended release tablets

37
Q

How does epinephrine work?

A

a1 - peripheral vasoconstriction and venoconstriction (increase preload and SVR)
b1 - tachycardia and increased contractility
b2 - bronchodilation

38
Q

how can epinephrine be given?

A

IV, IM, inhalation

39
Q

why would we give epinephrine?

A

anaphylaxis or cardiac arrest

40
Q

what is the important negative drug interaction with epinephrine?

A

hypertension when combined with propranolol

41
Q

what are the possible consequences of toxicity with epinephrine?

A
  • vasoconstriction
  • HTN
  • hemorrhagic stroke
  • angina
  • arrhythmias
42
Q

how does norepinephrine work?

A

a1 - vaso and venoconstriction

b1 - HR and contractility increase

43
Q

how is norepinephrine given?

A

IV only

44
Q

what are consequences of norepinephrine toxicity?

A
  • constriction of mesenteric vessels and peripheral arterioles causing ischemia, infarction, gangrene, reflex bradycardia
45
Q

when should we be cautious about prescribing NE?

A
  • someone taking a MAO inhibitor such as phenelzine

- risk of hypertension when combined with propranolol

46
Q

why would we prescribe NE?

A

acute hypotension and shock

47
Q

how does ephedrine work?

A

indirect - releases NE from adrenergic nerve endings

some direct agonism at receptors

48
Q

why would we prescribe ephedrine?

A
  • mild to moderate hypotension during surgery
  • nasal congestion
  • bronchodilation?
49
Q

side effects of ephedrine?

A
  • hypertension
  • insomnia
  • CNS stimulation…..
50
Q

how does pseudo ephedrine work?

A

indirect - releases NE from adrenergic nerve endings

some direct a and b agonism

51
Q

why would we prescribe pseudoephedrine?

A
  • nasal and sinus decongestant

- bronchodilation but less than ephedrine

52
Q

how does tyramine work?

A
  • acts indirectly to release NE from adrenergic nerve endings
53
Q

What are indications for tyramine? (not FDA approved)

A
  • obesity
  • narcolepsy
  • ADHD
54
Q

Risks with tyramine?

A
  • should not be combined with phenelzine (MAO inhibitor)
55
Q

how does cocaine work?

A

indirect - blocks reuptake of NE, epinephrine, and DA at the synapse and can also stimulate NE release

56
Q

why would we prescribe cocaine?

A

nose bleeds

anesthesia for corneal surgery

57
Q

how do amphetamines work?

A

indirect - release NE from adrenergic nerve endings

58
Q

indications for amphetamine

A

obesity, narcolepsy, ADHD

59
Q

phenylephrine F

A

38%

60
Q

how is phenylephrine metabolized?

A

liver

61
Q

phenylephrine half life

A

2-3 hours, short

62
Q

isoproterenol half life

A

2 minutes, extremely short

63
Q

clonidine F

A

60-95%, high

64
Q

clonidine metabolism

A

liver to inactive metabolites

65
Q

clonidine half life

A

8 hours

66
Q

dobutamine half life

A

2 minutes, extremely short

67
Q

albuterol metabolism and excretion

A
  • metab - hepatic

- excretion - renal

68
Q

albuterol half life

A

1.6 hours, short

69
Q

ephedrine F

A

85%

70
Q

ephedrine half life

A

3-6 hours

71
Q

ephedrine metabolism and excretion

A
  • minimal hepatic metabolism

- 22-99% renal excretion

72
Q

cocaine half life

A

1 hour

73
Q

amphetamine half life

A

9-14 hours

74
Q

amphetamine F

A

75-100%