Adrenergic Agonists B&B Flashcards

1
Q

which 2 adrenergic agonists activate all receptor types?

A

epinephrine and dopamine - activate alpha1, alpha2, beta1, beta2

[note dopamine also activates D1 receptors in kidneys to increase renal blood flow]

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2
Q

which 2 adrenergic agonists activate just the beta receptor types (beta1 and beta2)? what is the key difference between them?

A

isoproterenol: beta1=beta2, so increases HR while lowering BP

dobutamine: beta1>beta2, but still increases HR while lowering BP

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3
Q

which 2 adrenergic agonists activate just the alpha receptors mostly (alpha1, alpha2)?

A

norepinephrine - but also binds beta1, beta2 (just not as much)

phenylephrine

therefore, it makes sense these are used as vasoconstrictors!

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4
Q

group the following adrenergic agonists into 3 groups and explain why:
a. epinephrine
b. norepinephrine
c. isoproterenol
d. dopamine
e. dobutamine
f. phenylephrine

A

activate all receptors (alpha1/2, beta1/2): epinephrine + dopamine

activate just beta receptors (beta1/2): isoproterenol (beta1=beta2) + dobutamine (beta1>beta2) —> raise HR, lower BP

activate just alpha receptors (alpha1/2): norepinephrine (also binds beta1/2 some) + phenylephrine —> vasoconstriction

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5
Q

which 2 adrenergic agonists would be best for raising HR and lowering BP?

A

isoproterenol and dobutamine: preferentially bind beta receptors (beta1, beta2)

[recall beta1 —> increase HR, beta2 —> vasodilation]

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6
Q

which 2 adrenergic agonists would be best for vasoconstriction in shock patients?

A

norepinephrine and phenylephrine: preferentially bind alpha receptors (alpha1, alpha2)

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7
Q

which receptors does epinephrine vs norepinephrine bind?

A

epinephrine: binds all adrenergic receptors well (alpha1/2, beta1/2)

norepinephrine: preferentially activates alpha receptors (alpha1/2) - great for vasoconstriction in shock patients

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8
Q

which receptors does dopamine vs dobutamine bind?

A

dopamine: binds ALL adrenergic receptors (alpha1/2, beta1/2)

dobutamine: preferentially binds beta receptors (beta1/2) —> raises HR while lowering BP

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9
Q

what is the effect of low vs medium vs high dose dopamine?

A

low dose = dopamine agonist —> binds D1 receptors in kidney to cause vasodilation

medium dose = beta1 agonist —> increased HR and contractility

high dose = alpha agonist —> vasoconstriction

DOES NOT CROSS BBB (NO CNS EFFECTS)

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10
Q

how big of a dose should you give of dopamine to achieve the following effects?
a. vasoconstriction
b. vasodilation in kidneys
c. increased HR and contractility

A

low dose = dopamine agonist —> binds D1 receptors in kidney to cause vasodilation

medium dose = beta1 agonist —> increased HR and contractility

high dose = alpha agonist —> vasoconstriction

DOES NOT CROSS BBB (NO CNS EFFECTS)

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11
Q

what is the effect of low vs high dose epinephrine?

A

epinephrine: binds all adrenergic receptors well (alpha1/2, beta1/2)

low dose: beta1 = beta2 —> increased HR and contractility + vasodilation (lower BP)

high dose: alpha agonist —> vasoconstriction

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12
Q

if you want to use epinephrine to treat a patient with anaphylaxis, what kind of dose should you give them?

A

epinephrine: binds all adrenergic receptors well (alpha1/2, beta1/2)

low dose: beta1 = beta2 —> increased HR and contractility + vasodilation (lower BP)

high dose: alpha agonist —> vasoconstriction - treats shock

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13
Q

to which adrenergic receptors do the following agonists bind? state the clinical use
a. pseudoephedrine
b. albuterol
c. salmeterol
d. terbutaline
e. ritodrine

A

a. pseudoephedrine: alpha1/2 —> nasal decongestant (constrict nasal vessels)

b. albuterol: beta2>1 —> tx asthma (bronchodilation)
c. salmeterol: beta2>1 —> tx COPD (bronchodilation)

d. terbutaline: beta2>1 —> decrease contractions (OB)
e. ritodrine: beta2 —> decrease contractions (OB)

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14
Q

what type of drug is pseudoephedrine, and what is its clinical use?

A

pseudoephedrine: alpha1/2 direct agonist

used as nasal decongestant via vasoconstriction in nose

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15
Q

direct agonist of alpha1&2 used as nasal decongestant

A

pseudoephedrine: alpha1/2 direct agonist

used as nasal decongestant via vasoconstriction in nose

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16
Q

to which adrenergic receptors do albuterol and salmeterol bind, and what are their respective clinical uses?

A

direct agonists of beta receptors (beta2>beta1) —> bronchodilation

albuterol - treats asthma
salmeterol - treats COPD

17
Q

to which adrenergic receptors do terbutaline and ritodrine bind, and what is their clinical use? what is the difference between the two drugs?

A

terbutaline: direct agonist of beta2>beta1 receptors

ritodrine: direct agonist of beta2 receptors

both used in OB to decrease contractions

18
Q

which of the following direct adrenergic agonists does NOT bind beta receptors?
a. albuterol
b. pseudoephedrine
c. terbutaline
d. salmeterol
e. ritodrine

A

a. pseudoephedrine: alpha1/2 —> nasal decongestant (constrict nasal vessels)

b. albuterol: beta2>1 —> tx asthma (bronchodilation)
c. salmeterol: beta2>1 —> tx COPD (bronchodilation)

d. terbutaline: beta2>1 —> decrease contractions (OB)
e. ritodrine: beta2 —> decrease contractions (OB)

19
Q

what types of drugs are clonidine and methyldopa, and what is their clinical use?

A

direct alpha2 agonists used to treat hypertension

20
Q

what kind of drug is apraclonidine, and what is its clinical use?

A

direct alpha2 agonist (with weak alpha1 activity) used in glaucoma to lower intraocular pressure

21
Q

clonidine vs apraclonidine

A

clonidine: direct alpha2 agonist used to treat hypertension

apraclonidine: direct alpha2 agonist (with weak alpha1 activity) used in glaucoma to lower intraocular pressure

22
Q

which of the following is used to treat HTN?
a. pseudoephedrine
b. albuterol
c. salmeterol
d. clonidine
e. terbutaline
f. ritodrine
g. apraclonidine

A

d. clonidine: direct alpha2 agonist used to treat hypertension

23
Q

which of the following is used to treat COPD?
a. pseudoephedrine
b. albuterol
c. salmeterol
d. clonidine
e. terbutaline
f. ritodrine
g. apraclonidine

A

c. salmeterol: beta2>1 —> tx COPD (bronchodilation)

24
Q

how do indirect adrenergic agonists work?

A

do not bind alpha or beta receptor to activate directly (that would be a direct agonist duh!)

instead, they increase the activity of norepinephrine either by promoting its release or blocking its reuptake

25
Q

how do the following drugs act as indirect adrenergic agonists, and what are their respective clinical uses?
a. amphetamine
b. ephedrine
c. cocaine

A

a. amphetamine: blocks NE reuptake + promotes NE release —> stimulate to treat narcolepsy, obesity, ADHD

b. ephedrine: promotes NE release —> nasal decongestant, urinary incontinence

c. cocaine: blocks NE reuptake —> vasoconstriction, local anesthetic

26
Q

which of the following drugs is used as a local anesthetic?
a. amphetamine
b. ephedrine
c. cocaine

A

a. amphetamine: blocks NE reuptake + promotes NE release —> stimulate to treat narcolepsy, obesity, ADHD

b. ephedrine: promotes NE release —> nasal decongestant, urinary incontinence

c. cocaine: blocks NE reuptake —> vasoconstriction, local anesthetic… however, note this is because of separate action of blocking Na channels in nerves!!!

27
Q

ephedrine vs pseudoephedrine

A

pseudoephedrine: alpha1/2 direct agonist

ephedrine: indirect adrenergic agonist via promoting NE release

both used as nasal decongestant via vasoconstriction in nose

28
Q

indirect adrenergic agonist used as nasal decongestant

A

ephedrine: promotes NE release

treats nasal congestion + urinary incontinence

[recall pseudoephedrine is a direct alpha1/2 agonist that treats nasal congestion]

29
Q

what kind of neurotransmitters does cocaine act on? how does it exert this effect?

A

enhances monoamine [read: single NH2 group] neurotransmitter activity via blocking presynaptic reuptake pumps - dopamine, NE, serotonin

—> generalized sympathetic activation

cocaine intoxication induces massive alpha and beta stimulation —> HTN, tachycardia, coronary spasm (chest pain + increased O2 demand)

30
Q

how does cocaine function as a local anesthetic?

A

aside from its action as indirect adrenergic agonist enhancing monoamine NT activity (dopamine, NE, 5-HT)…

… cocaine also blocks Na+ channels in nerves, allowing it to function as a local anesthetic

31
Q

what is the treatment for cocaine intoxication, and how does it work? what drug should be AVOIDED?

A

cocaine: indirect adrenergic agonist via blocking monoamine NT reuptake - NE, dopamine, 5-HT

cocaine intoxication = massive alpha and beta receptor stimulation —> HTN, tachycardia, coronary spasm

tx: benzodiazepines - sedatives via GABA activation

AVOID beta blockers - this would cause unopposed alpha activation and SEVERE HTN

32
Q

A college student presents to the ED with chest pain due to coronary spasms and HTN. It is discovered they are experiencing cocaine intoxication. Your fellow medical student on ED round is about to administer a beta blocker. You jump in just in time to stop them. Why? What will you do instead?

A

cocaine: indirect adrenergic agonist via blocking monoamine NT reuptake - NE, dopamine, 5-HT

cocaine intoxication = massive alpha and beta receptor stimulation —> HTN, tachycardia, coronary spasm

tx: benzodiazepines - sedatives via GABA activation

AVOID beta blockers - this would cause unopposed alpha activation and SEVERE HTN

33
Q

what drug should you give?

5yo M presents with hives and wheezing following bee sting

A

anaphylaxis —> give epinephrine

alpha1/2 AND beta1/2 direct agonist = vasoconstrictor + bronchodilator

34
Q

what drug should you give?

75yo M presents with pneumonia and hypotension

A

septic shock —> give norepinephrine OR phenylephrine

direct alpha1/2 agonists = vasoconstrictors

35
Q

what direct adrenergic agonist should you give?

66yo M presents with massive myocardial infraction and hypotension

A

cardiogenic shock —> give dobutamine

direct beta1 agonist = increase cardiac contractility and HR

36
Q

what adrenergic agonist should you give?

Pt is 10yo M with PMH of asthma presenting with wheezing and dyspnea

A

asthma flare —> give albuterol

direct beta2 agonist = bronchodilator

37
Q

what direct adrenergic agonist should you give?

22yo M presents with runny nose

A

rhinitis —> give pseudophedrine OR phenylephrine

direct alpha1 agonists = vasoconstrictors