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CRRAB 1 > Week 3: Adrenergic agonists (sympathetic nerves) > Flashcards

Week 3: Adrenergic agonists (sympathetic nerves) Flashcards

1
Q

What are the steps of synthesis of norepinephrine?

A

Tyrosin –> DOPA –> Dopamine –> Norepinephrine (which can be converted into epinephrine)

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2
Q

What two routes of adrenergic amine uptake accounts for the concentration gradient inside vesicles?

A

Axoplasmic (50x) and granular uptake (200x)

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3
Q

How are adrenergic amines released normally?

A

stimulation of nicotinic receptors on post-synaptic surface of post-ganglionic nerve

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4
Q

How are adrenergic amines released via indirectly-acting sympathomimetics (amphetamine, tyramine, ephedrine)?

A

Can induce the release of norepi without the dopamine beta hydroxylase, basically reverse the pump on the cell membrane

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5
Q

What is the effect of cocaine and imipramine on adrenergic amines?

A

inhibit the axoplasmic pump to potentiate sympathetic responses (inhibits reuptake)

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6
Q

What is the effect of reserpine on adrenergic amines?

A

Inhibts granular pump accumulating catecholamines in vesicles which results in depletion

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7
Q

What is the effect of guanethidine on adrenergic amines?

A

induce release of vesicles of norepi slowly, depleting the stores; reduces response to sympathetic stimulation

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8
Q

What are the effects of MAOIs? (i.e. pargyline)

A

Inhibit the breakdown of catecholamines, increasing their effects

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9
Q

What is the breakdown product of epinephrine/norepinephrine?

A

Vanillylmandelic acid (VMA)

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10
Q

What amines interact with alpha 1 receptors from most to least?

A

epinephrine >= norepinephrine&raquo_space; isoproterenol

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11
Q

What amines interact with alpha 2 receptors from most to least?

A

epinephrine >= norepinephrine&raquo_space; isoproterenol

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12
Q

What is the effect of alpha1 agonist?

A

mediates smooth muscle contraction via GCPR (Gq)

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13
Q

What is the effect of an alpha 2 agonist?

A

inhibits neural norepi release by binding to G-alpha-i proteins

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14
Q

What toxin binds to Gi proteins and irreversibly inhibits them?

A

Pertussis toxin

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15
Q

What amines interact with beta 1 receptors from most to least?

A

isoproterenol > epinephrine = norepinephrine

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16
Q

What amines interact with beta 2 receptors from most to least?

A

isoproterenol > epinephrine&raquo_space; norepinephrine

17
Q

What is the effect of beta 1 agonists?

A

adrenergic cardiac effects, renin release

18
Q

What is the effect of beta 2 agonists?

A

relaxation of smooth muscle and metabolic (glycogenolytic) effects - Mostly in lungs and somewhat in blood vessels

19
Q

What toxin binds to beta 2 receptors?

A

Cholera

20
Q

What drug is a beta 1 agonist?

A

Dobutamine

21
Q

What is the effect of dobutamine?

A

Beta1 agonist, positive inotrope

22
Q

What are the effects of dopamine?

A

positive inotrope, vasodilation in renal and mesenteric vasculature at low dose, vasoconstrictor (alpha 1) at high dose

23
Q

What drug is an alpha 1 agonist?

A

Phenylephrine

24
Q

What are the effects of phenylephrine?

A

Used to reverse hypotension or to treat paroxysmal atrial tachycardia, topical vasoconstrictor and mydriatic. Decreases tachycardia due to reflex bradycardia

25
Q

What drugs are beta 2 selective agonists?

A

metaproterenol, terbutaline, albuterol, ritodrine, salmeterol

26
Q

What are the effects of beta 2 agonists?

A

bronchodilation, delay labor. Major side effects: tachycardia and palpatations

27
Q

What is the effects of isoproteronol?

A

Beta2: vasodilation, Beta1: tachycardia

28
Q

What does isoproteronol do to blood pressure? Explain.

A

Decreases it. It does affect CO, but because radius is raised to the 4th power in the TPR equation, it will affect that significantly more.

29
Q

What are the cardiovascular actions of norepinephrine? What receptors do they interact with to do this?

A

Vasoconstriction (alpha1), increased heart rate and force (beta 1), reflex reduction in heart rate (vagus nerve)

30
Q

What are cardiovascular actions of epinephrine? And what are the receptors that mediate this?

A

Vasoconstriction (alpha 1), vasodilation (beta 2), heart rate and force increase but reflexes to the elevation in blood pressure can suppress heart rate (vagal stimulation)

31
Q

What is the effect of amphetamine?

A

releases norepinephrine, increasing BP

32
Q

What is the effect of ephedrine?

A

Releases norepinephrine (which interacts with alpha 1 and beta 1 receptors to vasoconstrict, but also interacts with Beta 2 receptors to vasodilate)

33
Q

What is the effect of pseudoephedrine?

A

Releases norepinephrine (raises BP via alpha 1 and beta 1, lowers via beta 2)

34
Q

What is the MOA of pargyline?

A

MAOI- potentiates sympathetic responses

35
Q

What are the effects of guanethidine and guanadrel?

A

releases NE from vesicles, depleting it.

CRRAB 1 (5 decks)

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