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Pharm II Exam I > Adrenergic Stimulants > Flashcards

Adrenergic Stimulants Flashcards

1
Q

Formation of adrenergic molecules

A

tyrosine –> L-Dopa –> Dopamine (ends here orrr) –> NE –> E

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2
Q

Where is NE converted to E

A

adrenal medulla

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3
Q

Rate limiting step and what is it blocked by

A

Tyrosin –> L-dopa;

blocked by metyrosine

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4
Q

Increase release of NE at presynaptic terminal

A

Tyramine and amphetamine (only have effect if noradrenergic innervation is intact)

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5
Q

What blocks reuptake of NE

A

antidepressant and cocaine

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6
Q

metabolize NE

A

monoamine oxidase (MAO) and catechol-O-methyl transferase (COMT)

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7
Q

MAO

A

on outer surface of mitochondria, breaks down NE in presynatptic terminal

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8
Q

COMT

A

found throughout body, especially in liver, breaks down circulating NE and EPI

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9
Q

How to measure NE and EPI concentrations

A

measure VMA (mandelic acid) and HVA (homovanillic acid) in 24 hour urine sample

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10
Q

Alpha receptor order

A

EPI > NE&raquo_space; Isoproterenol

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11
Q

beta-1 order

A

Iso > EPI = NE

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12
Q

Beta-2 order

A

Iso > EPI&raquo_space; NE

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13
Q

Beta-3 Order

A

Iso = NE > EPI

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14
Q

alpha 1 agonist

A

phenylephrine

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15
Q

alpha 2 agonist

A

clonidine

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16
Q

Clonidine actions

A

aggregation of platelets
some smooth muscle contraction
decrease insulin secretion

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17
Q

NE has little effect on what receptors

A

B2

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18
Q

What has a greater effect on beta3 receptors, NE or EPI?

A

NE

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19
Q

Beta1 agonst

A

Dobutamine

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20
Q

Dobutamine effects

A

increase contraction and HR
increase AV conduction
Increase renin secretion

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21
Q

Beta 2 receptor agonist

A

ALbuterol

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22
Q

Albuterol effects

A

Relax respiratory, uterine, GI smooth muscle
Relax blood vessels to skeletal muscle
promote potassium uptake in skeletal muscle
increase glycogenolysis

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23
Q

Beta-3 receptor effects

A

increase lipolysis

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24
Q

DA receptor location

A

brain, renal and splanchnic vasculature

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25
Q

D1

A

stimulate adenylyl cyclase and causes dilation of renal blood vessels (increasing RBF)

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26
Q

D2

A

inhibits adenylyl cyclase, open potassium channels, and decrease Ca influx, which generally inhibits release of transmitters from nerve terminals

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27
Q

Atherosclerosis and alpha 1 receptors

A

baroreceptor response may be impaired, so alpha agonist effect on BP will be magnified

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28
Q

Norepinephrine effects what receptors

A

alpha stimulation causes vasocontriction, increases BP

B1 stimulation increases HR, overcome by baroreceptor reflex

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29
Q

Norepinephrine facts

A

must be injected
increase PR, increased BP, PP unchanged
Dec. blood flow to kidney, spleen, liver
HR increases, reversed by baroreceptor reflex
CO unchanged or decreased
Atropine prior to NE will block vagal reflex, HR will increase
Short action, vasoconstriction at infusion site, used to reverse hypotension; necrosis if poor blood flow

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30
Q

NE clinical use

A

RARE; hypotensive crisis!

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31
Q

Epinephrine receptors

A

alpha: vasocontriction, initially increases diastolic pressure
Beta1- increases HR, contraciton (increased PP)
beta 2- dilate blood vessels to skeletal muscle, decrease diastolic
PP increases MAP doesn’t change much
CO and O2 consumption increase
Beta-2 more sensitive to EPI than alpha!!!

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32
Q

Dose dependence of epinephrine

A

low dose: B2 (vasodilation of skeletal muscle- dec. diastolic)
High dose: alpha receptors (vasoconstriciton, BP increases - inc. diastolic)

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33
Q

Other effects of epinephrine

A 
increased glycogenolysis (blood sugar increases)
increased lipolysis
dec. insulin secretion (a2)
renin increases
bronchodilation
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34
Q

Difference between NE and EPI receptor stimulation

A

NE does not stimulate B2 (bronchodilation, dilation to skeletal mm. vessels)

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35
Q

alpha block + epi

A

take away vasoconstriction, now only have vasodilation – no BP increase anymore, diastolic decreases

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36
Q

Beta block + epi

A

no increased contractility or HR increase; no more vasodilation to even out BP, so you see a LARGE increase in BP; aortic flow decreases (w/ higher diastolic)

37
Q

Used of epinephrine

A

anaphylactic shock (restore BP, decrease bronchospasm, decrease congestion and angioedema, reverse CV collapse)
Emergency tx for cardiac arrest and complete heart block
vasoconstrictor used to decrease diffusion of injected drugs such as local anesthetics
glaucoma- dec. production, increase removal
bronchodilation (emergency tx of asthma-rarely)

38
Q

SE of EPI

A

tremor, throbbing h/a, increased BP, tachycardia; angina in patients with CAD (increased O2 consumption and increased cardiac work);

most potent vasopressor available: low dose- vasodilation, high dose - alpha, vasoconstriction

Injection at high dose could cause extreme inc. in BP and cerebral hemorrhage or ventricular arrhythmias

39
Q

Contraindicationss of EPI

A

beta-blockers (severe HTN!)

40
Q

Where is ephedra found

A

herbal supplements and weigh loss preparations

41
Q

What is ephedra

A

stimulates alpha and Beta, and increases NE release

effects similar to EPI

CNS stimulant, Inc. HR and BP; bronchodilation; taken off market due to death from HTN

42
Q

phenylpropanolamine

A

similar to ephedra; in OTC decongestants and weight loss; taken off market due to hemorrhagic stroke in women

43
Q

Catecholamines

A

NE
EPI
Isoproterenol

44
Q

Alpha Agonists

A

Phenylephrine (a1)
pseduoephedrine
oxymetazoline
midodrine

45
Q

Phenylephrine

A

vasoconstriction inc. PR, BP increases - reflex slows HR

46
Q

Use of phenylephrine

A

Hypotensive emergency
decongestant (rebound effect)
mydriasis (eye exam)

47
Q

Phenylephrine receptor

A

selective for alpha-1

48
Q

Side effect of phenylephrine

A

rebound congestion
HTN (caution w/ hypertensive patients)
mydriasis

49
Q

Pseudoephedrine (Sudafed)

A 
alpha agonist similar to phenylephrine
OTC decongestant
caution in HTN patients
precursor for methampheatamine 
more effective orally than phenylephrine
50
Q

Precursor for meth

A

pseudoephedrine

51
Q

Use of pseudoephedrine

A

OTC decongestant

52
Q

Oxymetazoline (Afrin)

A

direct alpha agonist
vasoconstriction, used on nasal mucosa and in eye
nasal decongestatant (rebound effect)
also works on ALPHA-2 (hypotension if a large quantity)

53
Q

oxymetazoline

A

topically as nasal spray (rebound effect) - hypotension in HIGH doses (alpha-2)

54
Q

Decrease redness in eye via vasoconstriction

A

tetrahydrozoline, naphazoline

55
Q

Contraindications for tetrahydrozline, naphazoline

A

narrow angle glaucoma and HTN

56
Q

Used to treat symptomatic orthostatic hypotension

A

midodrine

57
Q

Alpha 2 agonists

A 
CLONIDINE
methyldopa
apraclonidine
dexmedetomidine
tizanidine
58
Q

Clonidine

A

selectve a2 agonist in brain (CNS!)
decreases release of NE and overall symapthetic output
oral or transdermal patch

59
Q

Effect of clonidine

A

decrease BP

60
Q

Clonidine use

A

hypertension
reduce cravity/withdrawal symptoms for opiods and alcoholics
decrease hot flashes in menopause
pre-anesthetic med to cause sedation and dry secretions

61
Q

SE of clonidine

A

dry mouth, sedation, sexual dysfunction

avoid getting patch too hot - massive release of clonidine leading to hypotension

HTN may occur if patch is withdrawn abruptly

62
Q

Methyldopa (also: guanabenz, guanfacine)

A

alpha 2 agonist similar to clonidine

63
Q

Apraclonidine (& brimonidine)

A

alpha 2 agonist; used in EYE to decrease intraocular pressure by reducing formation of aqueous humor thru a2 receptor mediated vasoconstriction

64
Q

Dexmedetomidine

A

selective a2-adrenoceptor agonist w/ centrally mediated sympatholytic, sedative and analgesic effects

65
Q

Tizanidine

A

a2 agonist w/ less effect on BP than clonidine; REDUCED MUSCLE SPASTICITY

66
Q

Isoproterenol

A

B1 and B2; vasodilation causes decreased BP with reflex increased HR;

67
Q

Use of isoproterenol

A

used to be used for asthma

68
Q

SE of isoproterenol

A

tachycardia, palpitations, arrhythmias

69
Q

Dobutamine

A

B1 selective; increased CO and contractility

70
Q

Use of dobutamine

A

cardiac stress test

increase CO in cardiogenic shock and CHF

71
Q

SE of dobutamine

A

increased HR and HTN, especially if already HTN

72
Q

Terbutaline, albuterol

A

B2 selective; bronchodilation; used to treat asthma

73
Q

Mirabegron

A

B3 selective; used for OAB

SE: HTN, sinus tachy, h/a, dizziness

74
Q

Dopamine

A

D1 selective; high dose effects almost all receptors (b1, a1)

SE: increased HR, vasoconstriction, n/v; high dose: similar to EPI

75
Q

Use for dopamine

A

cardiac shock

76
Q

Fenoldopam

A

more D1 selective; dilates renal vascular beds

77
Q

Fenoldopam use

A

decrease BP in severe HTN

78
Q

Amphetamine

A

increases release of NE and DA; CNS stimulant (euphoria, alertness, decreased need to sleep and eat)

79
Q

SE of amphetamine

A

psychosis, tachycardia, HTN, tremors

80
Q

Toxicity of amphetamine

A

cerebral hemorrhage, convulsions, coma

81
Q

Metahmphetamine

A

more central effects, less peripheral; drug of abuse

82
Q

Methylphenidate (ritalin)

A

used to treat ADHD (decreases hyperactivity)

83
Q

Cocaine MOA

A

prevents reuptake of NE and DA in nerve terminals

84
Q

Cocains effects

A

similar to amphetamine, but shorter acting and more intense; smoked (crack) to intensify effect; highly addicting;

85
Q

SE of cocaine

A

HTN and stroke in healthy individuals; tachycardia and arrhythmias and MI; psycosis in long term use

86
Q

Clinical use of cocaine

A

vasoconstrictor: nasopharyngeal surgery to decrease blood flow and produce local anesthesia

87
Q

Tyramine

A

increases release of NE and DA; forms false neurotransmitter (octopamine); tachyphylaxis develops

88
Q

Contraindication for tyramine

A

MAOI inhibitos (MAOI hydrolyzes tyramine) – can lead to hypertensive crisis

Pharm II Exam I (3 decks)

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