Adrenergics Flashcards

1
Q

gestational HTN

A

methyldopa

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2
Q

nasal decongestant

A

1) phenylphrine (also can be used orally for shock)

2) pseudoephedrine

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3
Q

acute asthma

A

albuterol

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4
Q

COPD

A

Salmeterol

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5
Q

heart block

A

isoproterenol

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6
Q

cardiac stress test

A

dobutamine

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7
Q

this is an adrenergic pro-drug

A

methyldopa

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8
Q

alpha 2 agonist

A

1) methyldopa (pro-drug, oral only, mostly gestational HTN)
2) clonidine (oral, longer lasting effect)

both work by stimulating alpha-2 in the CNS, thereby inhibiting sympathetic outflow
(in the peripheral nerves, it is used as an auto-receptor to prevent NE release)

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9
Q

acute shock

A

Norepinephrine

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10
Q

loss of sympathetic tone (e.g. spinal cord injury)

A

Norepinephrine

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11
Q

hypersensitivity reactions

A

Epinephrine

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12
Q

bradyarrythmias

A

1) Epinephrine

2) dobutamine?

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13
Q

Case: 24 y/o female presents to clinic with headaches and blurry vision after being at a Wisconsin cheese and beer festival for the past weekend. Vitals show BP 190/120. No previous history of HTN and is otherwise been healthy (no hospitalizations, no surgeries, normal BMI, athletically active, etc.). Currently is taking Phenelzine for her depression. What could be the cause of her headaches?

Follow-up: what drug could you give to help?

A

Normally, the tyramine in the beer and cheese would be broken down in the liver. However, the patient is taking a MAOI (phenylzine) which is blocking the breakdown, and causing excess tyramine to release catecholamines in the periphery (does not penetrate CNS). This causes vasoconstriction (alpha-1) and increases in systolic BP by increases in HR, CO, and contractile force (Beta-1). This overall increase in PVR and subsequent increase in BP, is causing the patient’s headaches.

Follow-up: Labetalol
(IV admin is useful in hypertensive crises; 3rd generation beta blocker, helps because it has Alpha-1 antagonist as well as Beta-1 and Beta-2 antagonist)

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14
Q

NORepinephrine

A

AGONIST
A1 + A2 + B1
(mainly a1 effects)

effects:
1) peripheral vasocon.–> incr. PV –> increase BP
(increase dia., sys., mean BP)
2) reflex bradycardia

IV only
short healf-life

USE: Acute shock + reduce symp. tone (spinal cord injury)

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15
Q

EpinePHRINE

A

AGONIST
A1 + A2 + B1 + B2

Effects:
potent vasopressor, but can dilate skeletal muscle beds at low doses (due to b2)

Low dose
... incr. HR, CO, force, systolic BP (b1 agonist)
...decr. diastolic BP (b2 agonist) 
...hyperglyemic effects 
...bronchodilation    (powerful) 

High dose/ bolus
…… incr. HR, CO, force, systolic BP (b1 agonist)
….increase dia., mean BP (a1 effect too strong)
…hyperglyemic effects
…bronchodilation (powerful)

Uses:

1) Hypersensitivity reaction
2) increase local anesthetic effects
3) restore rhythm in cardiac arrest (bradyarrhythmias)

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16
Q

isoPROtereNOL

A

B1 + B2 agonist

Effects:
...incr. HR, CO, force
...dec. PVR (B2 skeletal muscle), diastolic BP
...bronchodialation 
....(REFLEX) tachycardia 

USE:

  • Stimulate bradycardic heart during cardiac arrest
  • heart block
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17
Q

DOPamine

A

AGONIST
D1 + B1 + A1

Low Dose: “Renal Dose” = D1
…renal vasodilation
…incr renal blood flow

Intermediate dose: “cardiac dose” = B1
…incr. HR, CO, Force

High Dose: “pressor dose” = A1
…incr. PVR, BP

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18
Q

List the…
direct acting catecholamines
with varied actions

A

Norepinephrine
Epinephrine
Dopamine

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19
Q

List the…
…direct acting catecholamines
with non-selective beta agonist action

A

Isoproterenol

Dobutamine

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20
Q

List the…
…direct acting catecholamines
with Selective beta agonist action

A

Albuterol
Salmeterol

Note: Both drugs are Beta-2 selective agonists

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21
Q

List the…
…direct acting catecholamines
with Selective alpha-1 agonist action

A

Phenylephrine

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22
Q

List the…
…direct acting catecholamines
with Selective alpha-2 agonist action

A

Clonidine

Methyldopa

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23
Q

List the…

…indirect acting catecholamines

A

Amphetamine
Pseudoephedrine
Tyramine

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24
Q

DOBUTamine

A

AGONIST
B1, some other Beta

IV

Racemic mixture of A1 antagonist (+dobutamine) and agonist (-) with both isoforms with B activity

Effects
….incr. HR, CO, force

USE:
cardiac stress test

25
Q

ALBUTerol

A

AGONIST
B2

Fast acting, short half life
inhale

Effects:
…bronchodilation

USE:
Rescue inhaler for ASTHMA

26
Q

SALMETerol

A

AGONIST
B2

slow onset, long acting
inhale

Effects:
…bronchodilation

USE:
COPD

27
Q

PHENYLephrine

A

AGONIST
A1

oral, IV, spray

EFFECTS:
…incr. systolic & diastolic BP
…decr. blood flow locally (spray)
…reflex bradycardia

USE:
Nasal decongestant
Shock

28
Q

CLONidine

A

AGONIST
A2

oral
CNS Alpha-2 agonist

EFFECTS:
…DECREASES SYMPATHETIC OUTFLOW
…decr. HR, CO, Force
…decr. PVR

USE:
longer lasting HTN control

29
Q

methylDOPA

A

AGONIST
A2

oral
pro-drug
CNS Alpha-2 agonist, oral

EFFECTS:
…DECREASES SYMPATHETIC OUTFLOW
…decr. HR, CO, Force
…decr. PVR

USE:
gestational HTN

30
Q

AmPHETAmine

A

AGONIST
Releases norepinephrine and other biogenic amines (dopamine)
from granules

USE:
– Narcolepsy
– Attention deficit/hyperactivity disorder

31
Q

PSEUDOephedrine

A

AGONIST
Direct α1 agonist with some β2 agonist activity

USE
Nasal decongestant

32
Q

TYRAmine

A

AGONIST
release catecholamines in the periphery (does not penetrate CNS).

EFFECTS:
…vasoconstriction (alpha-1)
…. increases in BP
…. increases in HR, CO, and contractile force

NOTE: NOT A DRUG.

Can lead to hypertensive crises when dietary tyramine (found in fermented foods; cheese, beer, wine, sausages) is combined with an MAOI.

33
Q

treat: HTN (adrenergic antagonist)

A
Guanethidine or Guanadrel 
Reserpine 
phenOXYbenzene (many side effects)
phenTOLamine (many side effects)
praZOsin
...all the beta blockers
34
Q

VMAT blocker

A

Reserpine

35
Q

treat: release local action of epinephrine

A

phenOXYbenzene (many side effects)

phenTOLamine (many side effects)

36
Q

treat: Excess Catecholamines

A

phenOXYbenzene (many side effects)

phenTOLamine (many side effects)

37
Q

treat: HTN (adrenergic agonists)

A

CLONidine

methylDOPA

38
Q

treat: BPH

A

taMULOsin

39
Q

treat: myocardial infarction

A

any of the beta blockers
1st Gen:
…proPRANolol
…TIMolol

2nd Gen:
…metoPROolol
…aTENolol

3rd gen:
…laBETAlol
…carVIDilol

40
Q

treat: Angina (2nd gen)

A

2nd Gen:
…metoPROolol
…aTENolol

41
Q

treat: Angina (2nd gen; only 1x day dosing)

A

aTENolol

42
Q

treat: wide angle glaucoma

A

TIMolol

43
Q

treat: Angina (2nd gen; no CNS effects)

A

aTENolol

44
Q

treat: HTN emergencies

A

laBETAlol

45
Q

treat: HTN (adrenergic antagonists)

A
...guanETHIDINE
...guanADREL
...phenOXYbenzene (many side effects)
...phenTOLamine (many side effects)
...praZOsin
...proPRANolol
...TIMolol
...metoPROolol
...aTENolol
...laBETAlol
...carVIDilol

NOT Tamulosin, this is only A1a-antgonist for BPH

46
Q

guaneTHIDINE

A

Mechanism:
…Depletes NE from granules
(depletes vesicles thus, reduce sympathetic outflow at periphery).

Effect: decreases sympathetic responses
(pvr, HR, CO, ETC.)

Does NOT enter CNS

use: essential HTN

47
Q

guanDREL

A

same as GUANETHIDINE
(depletes vesicles thus, reduce sympathetic outflow at periphery).

Does NOT enter CNS

use: essential HTN

48
Q

reSERpine

A

blocks VMAT (i.e. dopamine uptake into NE granules/vesicles), less dopamine and NE to be releases

DOES enter CNS (thus, LOTS of side effects)

use: HTN

49
Q

phenOXYBENZENE

A

non-selective alpha antagonist
(A1 + A2 antagonist)

oral
IRREVERSIBLE

A2 antagonist means lots of side effects

use:
…pheochromocytoma <===MAIN USE
…release local effect of epinephrine
…HTN

50
Q

phenTOLamine

A

non-selective alpha antagonist
(A1 + A2 antagonist)

oral
COMPETITIVE

A2 antagonist means lots of side effects

use:
…release local effect of epinephrine
…HTN

51
Q

praZOsin

A

selective alpha antagonist
(A1 antagonist)

oral, competitive

decreases PVR,BP, LDL
increases HDL
(improves lipid profile)

uses:
…short term CHF
…HTN

52
Q

tamuLOsin

A

selective alpha antagonist
(A1a - antagonist) …only the prostate vessels

oral, competitive

decreases PVR to prostate (vasodilation to prostate; improve blood flow)

uses:
…BPH only

53
Q

proPRANolol

A

non-selective beta antagonist
B1 + B2 antagonist

1st gen

USES of all beta blockers....
...HTN
...Angina
...excess catecholamines
...MI 
...essential tremor
...migraine prophylaxis 
(these will be represented as "same" in further discussion of beta blockers)
54
Q

TIMolol

A

non-selective beta antagonist
B1 + B2 antagonist

1st gen

USES of all beta blockers….
…“same”
+
…“wide angle glaucoma”

55
Q

metoPROlol

A

selective beta antagonist
B1 antagonist

2nd gen

USES of all beta blockers….
…“same”
+
…“heart failure”

56
Q

aTENolol

A

selective beta antagonist
B1 antagonist

2nd gen
Does NOT enter CNS
Longer half-life = 1x day dosing

USES of all beta blockers….
…“same”

57
Q

LABETAlol

A

non-selective beta antagonist with extra properties
A1 + B1 + B2 antagonist

3rd gen

USES of all beta blockers….
…“same”
+
…“HTN”

especially. ..two formulations:
1) oral –> HTN
2) IV –> Hypertensive Crises

58
Q

carveDilol

A

non-selective beta antagonist with extra properties
A1 + B1 + B2 antagonist + L-TYPE Ca2+ blocker

3rd gen

USES of all beta blockers….
…“same”
(especially MI and Heart Failure)