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CRRAB Week 3 - WLB > Adrenergic Agonists - Trachte > Flashcards

Adrenergic Agonists - Trachte Flashcards

1
Q

What are the steps in norepinephrine synthesis?

A
  • Tyrosine →
    • cytosol
  • DOPA →
    • cytosol
  • Dopamine →
    • leaves cytosol
  • Norepinephrine →
    • vesicular
  • Epinephrine
    • in adrenal medulla
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2
Q

What enzyme is the rate limiting step in the synthesis of adrenergic amines?

A
  • Tyrosine hydroxylase
    • cystolic
    • converts Tyrosine → DOPA
    • blocked by Metyrosine
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3
Q

Where are adrenergic amines stored?

A

in granules with ATP-protein complex

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4
Q

What are the steps in the normal release of Adrenergic amines?

A
  • Stimulation of nicotinic receptors on post-synaptic surface of the post-ganglionic nerve
  • Depolarization (Na influx) and Ca influx
  • Release of dopamine beta-hydroxylase, norepinephrine and ATP
  • Norepinephrine inhibits its own release (alpha-2 receptors)
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5
Q

What neurotransmitter does the sympathetic preganglionic nerve release?

A

ACh

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6
Q

What kind of receptor on the sympathetic postganglionic cell body receives the neurotransmitter from the preganglionic?

A

Nicotinic Receptor

(via Na+ channel)

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7
Q

Once activated, what does a sympathetic postganglionic neuron release at its nerve terminal?

A

Norepinephrine

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8
Q

What receptor does NE interact with on the heart? Lungs?

A
  • Heart = Beta-1
    • only have one heart
  • Lungs = Beta-2, Alpha-1
    • have 2 lungs, thus Beta-2
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9
Q

If ACh is released on the adrenal gland, what receptor does it act on?

A

Nicotinic

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10
Q

What does the adrenal gland release in response to activation after receiving ACh?

A

NE & Epi

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11
Q

What happens in response to NE acting on Beta-1 receptors?

A

Increase HR, increase SV

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12
Q

What happens in response to NE acting on alpha-1 receptors?

A

Vasoconstriction, increased resistance

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13
Q

How is NE eliminated?

A

Axoplasmic pump transports NE back into synaptic terminal

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14
Q

What drugs act on the axoplasmic pump that brings NE back into the synaptic terminal?

A
  • Cocaine
    • stops reuptake of NE
    • potentiate sympathetic responses
  • Amphetamine
    • reverse pump → spit out more NE
    • increases BP
  • Tricyclic antidepressents
    • inhibits axoplasmic pump
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15
Q

What is the MOA of Reserpine (one of the first bp meds)?

A
  • Inhibits the granular pump accumulating catecholamines in vesicles
    • results in depletion of catecholamines (NE)
    • also deplete serotonin, dopamine, and NE in brain = nasty side effects
      • not used anymore
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16
Q

What two enzymes degrade adrenergic amines?

A
  • COMT (catechole-O-methyl transferase)
    • cytoplasm
  • MAO (monoamine oxidase)
    • mitochondria
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17
Q

What MAO inhibitor can potentiate the action of catecholamines and consequently lead to hypertensive crisis?

A

Pargyline

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18
Q

What compound found in cheese, wine, and beer releases catecholamines and is normally degraded by MAO?

A

Tyramine

(why patients on MAO inhibitors need to avoid these foods → can become hypertensive crisis → give alpha-1 blocker to treat)

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19
Q

What happens with activation of Beta-1 receptors?

A
  • G-protein coupled receptor
    • 7 transmembrane protein
  • Adrenergic cardiac effects
    • increase HR
    • increase SV
    • increase BP
20
Q

What activates Beta-1 receptors?

A

isoproterenol > epinephrine = norepinephrine

21
Q

What activates Beta-2 receptors?

A

isoproterenol > epinephrine >> norepinephrine

22
Q

What happens with activation of Beta-2 receptors?

A
  • found in lungs
    • taken by asthmatics
  • relaxation of smooth muscle & metabolic (glyogenolytic) effects
  • primary site in CV system is blood vessels
    • G-protein coupled receptor, increase cAMP
23
Q

What happens with activation of alpha-1 receptors?

A
  • mediates smooth muscle contraction
  • primary CV system location is on blood vessels
  • activates phospholipase C
    • to increase intracellular calcium via inositol trisphosphate
24
Q

What activates alpha-1 receptors?

A

epinephrine > norepinephrine >> isoproterenol

25
Q

What activates Alpha-2 receptors?

A

epinephrine > norepinephrine >> isoproterenol

26
Q

What happens with activation of Alpha-2 receptors?

A
  • inhibition of neural norepinephrine release
  • prejunctional nerve terminal, platelets, gut, medulla oblongata
    • inhibit sympathetic activity
  • acts to decrease cAMP or activate Na/H antiporter
27
Q

What is the only Alpha-1 agonist that is used clinically?

A

Phenlyephrine

  • used to reverse hypotension and paroxysmal atrial tachycardia
  • vasoconstriction –> increases resistance
  • doesn’t work if gave alpha-1 antagonist prior because all receptors are blocked

(also dilates pupils)

28
Q

What does Albuterol do to blood pressure?

A
  • lower pressure
  • Beta-2 agonist
    • action would be blocked if propanolol given prior (beta-2 antagonist)
29
Q

What does Isoproterenol do to blood pressure?

A
  • increase HR, SV → increase BP
    • tachycardia (Beta-1)
    • cardiac stimulant
  • lower resistance → decrease BP
    • vasodilate (Beta-2)
  • OVERALL = decrease BP!!!
    • radius4
  • will have no effect if enough Beta-blocker is given
    • all beta receptors blocked
30
Q

What does epinephrine do to blood pressure?

A
  • Can do anything!
  • Normal response = raise bp
    • Increase HR, SV, resistance
  • If alpha-blocker given (Terazosin), take away vascular effect
    • no vasoconstrictor
    • acts on Beta-2 → vasodilate
      • decrease bp
31
Q

What is the MOA of Imipramine?

A

potentiate sympathetics by blocking norepinephrine accumulation (block axoplasmic transporter)

(MOA similar to cocaine)

32
Q

What is the MOA of Tyramine, Amphetamine, and Ephedrine?

A

reverse axoplasmic transporter → increase NE

(mimic sympathetic stimulation)

33
Q

What is the MOA of Guanethidine and Guanadrel?

A
  • induce release of NE from vesicle, probably via displacement
  • depletes NE stores
  • reduces responses to sympathetic stimulation
34
Q

What receptors does Epinephrine activate?

A
  • Alpha-1
  • Alpha-2
  • Beta-1
  • Beta-2
35
Q

What receptors does Norepinephrine activate?

A
  • Alpha-1
  • Alpha-2
  • Beta-1
36
Q

What receptors does Isoproterenol activate?

A

Beta-1 & Beta-2

37
Q

What receptor(s) does Phenlyephrine activate?

A

Alpha-1

38
Q

What receptor(s) does Clonidine activate?

A

alpha-2

39
Q

What receptor(s) does alpha methyl Dopa activate?

A

alpha-2

40
Q

What receptor(s) does Guanabenz activate?

A

alpha-2

41
Q

What receptor(s) does Dobutamine activate?

A

Beta-1

42
Q

What receptor(s) does Albuterol activate?

A

Beta-2

43
Q

What receptor(s) does Metaproterenol activate?

A

Beta-2

44
Q

What receptor(s) does Ritodrine activate?

A

Beta-2

45
Q

What receptor(s) does Terbutaline activate?

A

beta-2

46
Q

What receptor(s) does Salmeterol activate?

A

beta-2

47
Q

What does Acetylcholine do to blood pressure and what blocks its effects?

A
  • Reduce HR
  • Vasodilation
  • Decreased BP
  • Blocked by anticholinergic meds (atropine)

CRRAB Week 3 - WLB (5 decks)

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