Adrenergics Flashcards

1
Q

Heart receptor?

A

B1

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2
Q

vessel receptor?

A

A1 = STRONGER = constrict

B2 = dilate (coronary/skeletal)

(a2=little effect)

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3
Q

Kidney receptor?

A

B1 = release renin

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4
Q

GI tract receptor?

A

a1 = stop secretion

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5
Q

Sex organs receptor

A

a1

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6
Q

Uterus receptors?

A
contract = a1
Relax = b2
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7
Q

Catecholamines

A

epi
NE
dopamine

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8
Q

NE released at

A

postganglionic sympathetic

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9
Q

Epi released from

A

adrenal medulla

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10
Q

Isoproterenol

ISUPREL

A

selective B ag

Stim the heart

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11
Q

Dopa

A

CNS transmitter

NE precursor

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12
Q

NE synthesis

A

Transporter sucks in Tyrosine

Tyr->Dopa->DA->NE->Epi

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13
Q

Inhibit NE release?

A
  • presynaptic a2 receptor
  • PGE2

*or degrade w/in terminals w/ MAO; reacumulate from synapse if cleaning

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14
Q

Enhance NE release?

A

angiotensin II

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15
Q

Most Cirulating Epi broken down by

A

MAO/COMT

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16
Q

Most of NE removed by

A

recycled into terminal by NET

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17
Q

receptors effects dependent on

A

g protein, kinases in target cell

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18
Q

Guanethidine

Mech

A

enters via NET, depletes NE

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19
Q

Reserpine

Mech

A

Enters terminal (lipid-solube), stops VMAT, NE can’t be recycled

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20
Q

MAOI inhibitors

Mech

A

accumulate intracellular NE, increased NE synapse levels

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21
Q

MAOI 8

Rx

A

Tranylcypromine (anti-depressant)

PARNATE

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22
Q

Amphetamine

Mech

A

Increase NET activity
more NE release

Faster kinetics than guanethidine/reserpine = gradual NE depletion

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23
Q

Large Tyramine load?

wine, cheese, beer, fava beans

A
  • MAO cleans tyramine, so MAO taken up
  • up NE = HTN
  • NO MAOIs w/ large tyramine load
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24
Q

Block NET, Up synaptic NE

Rx

A

Cocaine
Imipramine TOFRANIL
Atomoxetine ASENDIN

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25
Q

Alpha Ag

A

Phenylephrine

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26
Q

Beta Ag

A

Isoproterenol ISUPREL

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27
Q

Apha blocker

A

Phentolamine REGITINE

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28
Q

Beta blocker

A

Propanolol

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29
Q

Chronic ag treatment causes

A

desensitization

Downregulation

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30
Q

Chronic blocker treatment causes

A

supersensitization

Upregulation

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31
Q

NE likes

A

1s

A1/B1

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32
Q

Isoproteranol likes

A

Betas

used to stimulate heart

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33
Q

Epi likes

A

low dose = betas b1 b2

High dose = everything

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34
Q

Dopamine likes

A

low: DA, b1

High: everything

35
Q

Dobutamine likes

A

Low: b1 (UP contractility w/o effect HR)
HUGE AMINE SUBSTITUTION
High: may affect rate

36
Q

B1 receptors like

A

Iso>epi=NE

37
Q

B2 receptors like

A

iso> epi»NE

38
Q

A1 receptors like

A

epi>NE &raquo_space; iso

Normally will see NE

39
Q

Catecholamine structure

A

OH on 3+4

amine side chain (LARGER = Up Beta receptor affinity)

40
Q

Catecholamine Mech

How to increase CNS penetration

A

remove hydroxyl groups (3+4)

41
Q

COMT ONLY breaks down

A

catecholamines

42
Q

What blocks MAO metabolism?

A

substitute A carbon

43
Q

Contractility (SBP/CO) stimulated by

A

B1

Also up O2 use
Down efficiency

44
Q

Peripheral resistance (DBP) lowered by

A

B2

45
Q

Epi effects timeline

A
  • B1+B2 = up contractility up HR, down peripheral resistance
  • then A1 = vasoconstriction
  • up HR then reflex lowers
46
Q

Epi effects

Blood pressure

A

B2 + A1

low: decrease (b2 dilation)
High: increase (a1 constriction)

47
Q

Epi effects

Respiratory

A

B2 + A1

  • Bronchioles dilated (B2)
  • Secretions decreased (A1)
48
Q

Epi effects

Metabolism

A
  • glycogen breakdown (b2)
  • DOWN glycogen synth (a1)
  • DOWN insulin secretion (a2)
  • UP free fatty acids (b3)
  • Detruser muscle relax (b3)
49
Q

Anaphylactic shock?

A

Epi

  • Open airways (b2)
  • Down histamines/leukotrienes (b2)
  • Up BP (a1)
50
Q

Epi uses

A
  • anaphylactic shock
  • Asthma (B2)
  • topical hemostasis (a1)
  • cardiac arrest (b1)
51
Q

Epi S.E.

A

Arrythmia
CVA
emotional

52
Q

NE

Effects

A
  • Heart (b1)
  • BP UP sys/dia/mean (a1)
  • CO same or down (a1)
  • DOWN Glyc synthase (a1)
53
Q

Shock?
Neurogenic w/ spinal anesthesia

old-school Rx

A

NE (levophed)

54
Q

Isoproterenol effects

A
  • Heart (B1)
  • DOWN BP (B2)
  • Relax bronchi (B2)
55
Q

Stimulate Heart in Heart block/pacemaker insertion?

A

Isoproterenol

56
Q

Isoproterenol

S.E.

A
  • Fatal Arrythmia
  • Tachycardia
  • Palpitations
  • Anginal pain
57
Q

Overactive bladder?

A

Mirabegron (b3) MIRBETRYQ

58
Q

DA effects

A

DOSE-DEPENDENT

  • heart rate (b1)
  • BP = Low dose: DOWN (DA, B2) ;; High dose: UP (a1)
59
Q

Shock? (cardiogenic)

A

DA

60
Q

DA

S.E.

A
  • Tachycardia
  • anginal pain
  • arrythmia
  • N/V (DA @ CTZ)

NO CNS EFFECTS

61
Q

Dobutamine

Effects

A
  • heart (B1) CONTRACTILITY ONLY

* BP= high dose: UP (a1)

62
Q

Heart failure w/ open heart surgery/MI?

A

Dobutamine

63
Q

Dobutamine

S.E.

A

*arrythmia

NO CNS EFFECTS

64
Q

A1 ag uses

A
  • decongest mucous membranes
  • Up BP
  • Dilate Pupil
  • Eye drops
65
Q
  • decongest mucous membranes
  • Up BP
  • Dilate Pupil
  • Eye drops
A

A1 ag

66
Q

A1 ag

S.E.

A

UP BP

67
Q

Non-catecholamine A1 ag

Rx

A
  • phenylephrine (replacing psuedoephedrine) - cold
  • Phenylpropanolamine PPA (CVA risk-gone)
  • Ephedrine (CNS, nasal decongest)
68
Q

Non-catecholamine A1 ag broken down by

A

NOT COMT

Substituted A carb = NO MAO

= Longer t 1/2

69
Q

B2 ags

Uses

A
  • Bronchial asthma
  • Anaphylactic shock (stops mast cells releasing)
  • Relaxation of uterus/delay labor = many S.E.
70
Q
  • Bronchial asthma
  • Anaphylactic shock (stops mast cells releasing)
  • Relaxation of uterus/delay labor = many S.E.
A

B2 ags

Uses

71
Q

B2 ags

effects

A

Skeletal, heart (high dose

72
Q

Delay premature labor?

A
Ritodrine YUTOPAR (b2 selective)
Terbutaline BRETHINE
73
Q

COPD?

A

Formeterol (B2 ag) PERFOROMIST

74
Q

Asthma?

A
  • Albuterol/levalbuteraol

* Terbutaline

75
Q

Nasal decongestant, release NE, CNS stimulant, pressor?

b2 ag

A

Epehdrine

76
Q

Narcolepsy

A

*Amphetamine/ methamphetamine

CNS stim = Release NE

77
Q

Weight reduction

A

Amphetamine

CNS stim

78
Q

ADHD

A
  • Methylphenidate (Concerta)
  • Atomoxetine (Strattera) = NE reputake inhbitor NOT SCHEDULED

*Lisdexamfetamine dimesylate VYVANSE (amphet prodrug)

79
Q

CNS side effects

A

Abuse

Cardio/CNS stimulation

80
Q

Xanthines

A

ADENOSINE RECEPTORS

Resemble adrenergic stimulation but NOT binding adrenergic receptors (NO BETAS)

81
Q

Xanthine effects

A
  • CNS - all cortex
  • Cardio- HR + contractility up
  • Respiratory = relax bronchi
82
Q

Xanthines

Rx

A

Caffeine = CNS

Theophylline = Heart, Bronchi

83
Q

Theophylline

uses

A

Aminophylline = asthma

+B2 ag = chronic asthma