Adrenergics Flashcards

(58 cards)

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
ALBUTerol
AGONIST B2 Fast acting, short half life inhale Effects: ...bronchodilation USE: Rescue inhaler for ASTHMA
26
SALMETerol
AGONIST B2 slow onset, long acting inhale Effects: ...bronchodilation USE: COPD
27
PHENYLephrine
AGONIST A1 oral, IV, spray EFFECTS: ...incr. systolic & diastolic BP ...decr. blood flow locally (spray) ...reflex bradycardia USE: Nasal decongestant Shock
28
CLONidine
AGONIST A2 oral CNS Alpha-2 agonist EFFECTS: ...DECREASES SYMPATHETIC OUTFLOW ...decr. HR, CO, Force ...decr. PVR USE: longer lasting HTN control
29
methylDOPA
AGONIST A2 oral pro-drug CNS Alpha-2 agonist, oral EFFECTS: ...DECREASES SYMPATHETIC OUTFLOW ...decr. HR, CO, Force ...decr. PVR USE: gestational HTN
30
AmPHETAmine
AGONIST Releases norepinephrine and other biogenic amines (dopamine) from granules USE: – Narcolepsy – Attention deficit/hyperactivity disorder
31
PSEUDOephedrine
AGONIST Direct α1 agonist with some β2 agonist activity USE Nasal decongestant
32
TYRAmine
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
treat: HTN (adrenergic antagonist)
``` Guanethidine or Guanadrel Reserpine phenOXYbenzene (many side effects) phenTOLamine (many side effects) praZOsin ...all the beta blockers ```
34
VMAT blocker
Reserpine
35
treat: release local action of epinephrine
phenOXYbenzene (many side effects) | phenTOLamine (many side effects)
36
treat: Excess Catecholamines
phenOXYbenzene (many side effects) | phenTOLamine (many side effects)
37
treat: HTN (adrenergic agonists)
CLONidine | methylDOPA
38
treat: BPH
taMULOsin
39
treat: myocardial infarction
any of the beta blockers 1st Gen: ...proPRANolol ...TIMolol 2nd Gen: ...metoPROolol ...aTENolol 3rd gen: ...laBETAlol ...carVIDilol
40
treat: Angina (2nd gen)
2nd Gen: ...metoPROolol ...aTENolol
41
treat: Angina (2nd gen; only 1x day dosing)
aTENolol
42
treat: wide angle glaucoma
TIMolol
43
treat: Angina (2nd gen; no CNS effects)
aTENolol
44
treat: HTN emergencies
laBETAlol
45
treat: HTN (adrenergic antagonists)
``` ...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
guaneTHIDINE
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
guanDREL
same as GUANETHIDINE (depletes vesicles thus, reduce sympathetic outflow at periphery). Does NOT enter CNS use: essential HTN
48
reSERpine
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
phenOXYBENZENE
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
phenTOLamine
non-selective alpha antagonist (A1 + A2 antagonist) oral COMPETITIVE A2 antagonist means lots of side effects use: ...release local effect of epinephrine ...HTN
51
praZOsin
selective alpha antagonist (A1 antagonist) oral, competitive decreases PVR,BP, LDL increases HDL (improves lipid profile) uses: ...short term CHF ...HTN
52
tamuLOsin
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
proPRANolol
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
TIMolol
non-selective beta antagonist B1 + B2 antagonist 1st gen USES of all beta blockers.... ..."same" + ..."wide angle glaucoma"
55
metoPROlol
selective beta antagonist B1 antagonist 2nd gen USES of all beta blockers.... ..."same" + ..."heart failure"
56
aTENolol
selective beta antagonist B1 antagonist 2nd gen Does NOT enter CNS Longer half-life = 1x day dosing USES of all beta blockers.... ..."same"
57
LABETAlol
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
carveDilol
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)