Adrenergic Drugs Flashcards

1
Q

Is epinephrine an agonist or antagonist and what receptor types does it effect?

A

agonist; a1, a2, B1, B2 (nonselective)

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2
Q

Is norepinephrine an agonist or antagonist and what receptor types does it effect?

A

agonist; a1, a2, B1 (nonselective)

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3
Q

Is amphetamine indirect or direct acting and what is its mechanism of action?

A

indirect; increases release of NE

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4
Q

Is Isoproterenol an agonist or antagonist and what receptor types does it effect?

A

non selective B agonist; B1 and B2

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5
Q

Is Dobutamine an agonist or antagonist and what receptor types does it effect?

A

Agonist; B1

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6
Q

Is Albuterol an agonist or antagonist and what receptor types does it effect?

A

Agonist; B2

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7
Q

Is Terbutaline an agonist or antagonist and what receptor types does it effect?

A

Agonist; B2

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8
Q

Is Phenylephrine an agonist or antagonist and what receptor types does it effect?

A

Agonist; a1

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9
Q

Is Colnidine an agonist or antagonist and what receptor types does it effect?

A

Agonist; a2

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10
Q

Is a-methyldopa an agonist or antagonist and what receptor types does it effect?

A

Agonist; a2

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11
Q

What class of drugs is Fenoldopam in and what is its mechanism?

A

selective dopamine agonist; vasodilation

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12
Q

Is dopamine and indirect acting, or direct acting drug?

A

both

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13
Q

Is dopamine an agonist or antagonist and what receptor types does it effect?

A

agonist; D1, a1, B1

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14
Q

What is NE used to treat?

A

hypotension

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15
Q

What is Epi used to treat?

A

Anaphylactic shock (a1 and B2), combined with local anesthetic to control hemorrhage and contain the anasthetic (a1), glaucoma

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16
Q

What is amphetamine used for?

A

ADHD, narcolepsy and recreational drug

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17
Q

What is Isoproterenol used to treat?

A

Bronchodilator/asthma, shock (increases CO), heart block (increases HR)

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18
Q

What is Dobutamine used to treat?

A

cardiac decompensation (increases contractility), shock (increases HR), and heart block

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19
Q

What is Albuterol used to treat?

A

Prevent or reverse exercise-induced bronchospasm, mild asthma, COPD

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20
Q

What is Terbutaline used to treat?

A

Prevent or reverse exercise-induced bronchospasm, mild asthma, COPD

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21
Q

What are some side effects of Albuterol and Terbutamine?

A

masking of progressively severe inflammation, tachycardia, muscle tremors

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22
Q

What is phenyephrine used to treat and how does it work?

A

Nasal congestion and postural hypotension by vasoconstriction (a1)

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23
Q

Whats is Clonidine used to treat and how does it work?

A

Hypertension, shock, withdrawal from drug dependence by decreasing sympathetic outflow from CNS (a2 agonist)

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24
Q

What is a-methyldopa used to treat and how does it work?

A

Hypertension, shock, withdrawal from drug dependence by decreasing synthesis of NE

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25
Q

What is Fenoldopam used for?

A

to increase blood flow at renal, mesenteric, and cerebral arteries (only 10 min t1/2 though)

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26
Q

What is dopamine used to treat?

A

shock, renal failure (d1vasodilation) in renal and mesenteric arteries), and hypotension (a1 vasoconstriction)

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27
Q

What can happen at high doses of dopamine? low doses?

A

high doses- a1 direct activity and NE release indirect activity causing vasoconstriction
low doses- direct action on D1 receptors causing vasodilation

28
Q

What are some side effects of NE?

A

hypertension, arrhythmia and headache

29
Q

What are some side effects of Epi?

A

palpitations, arrythmia,headache and tremor

30
Q

What are some side effects of Amphetamines?

A

hypertension, insomnia, anxiety and arrythmias

31
Q

What are some side effects of Isoproterenol?

A

palpitations, tachyarrythmia and headche

32
Q

What are some side effects of Dobutamine?

A

tachyarrythmia, and hypertension

33
Q

What are some side effects of Phenylephrine?

A

hypertension and reflex bradycardia

34
Q

Which of the following is a pro-drug and can cross the BBB? Phenylephrine, Clonidine or a-Methyldopa

A

a-methyldopa

35
Q

Is phentolamine an agonist or antagonist and what receptor types does it effect?

A

antagonist; a1 and a2

36
Q

Is phenoxybenzamine an agonist or antagonist and what receptor types does it effect?

A

antagonist; a1 and a2 (non competitive blockers)

37
Q

Is prazosin an agonist or antagonist and what receptor types does it effect?

A

antagonist; a1

38
Q

Is terazosin an agonist or antagonist and what receptor types does it effect?

A

antagonist; a1

39
Q

What are phentolamine and phenoxybenzamine used to treat?

A

Pheochromocytoma, Raynaud’s, frostbite (cause vasodilation)

40
Q

What are Prazosin and Terazosin used to treat?

A

primary hypertension and benign prostatic hypertrophy (causes vasodilation)

41
Q

What are some side effects of phentolamine and phenoxybenzamine?

A

Postural hypotension and inhibition of ejaculation

42
Q

What are some side effects of Prazosin and Terazosin?

A

Postural hypotension (usually only with 1st dose b/c it is selective)

43
Q

Name the 1st generation B antagonist drugs and whether they are nonselective or selective.

A

propanolol and timolol; non selective B1 and B2

44
Q

Name the 2nd generation B antagonist drugs and whether they are selective or non selective.

A

metoprolol, bisoprolol and atenolol; B1 selective

45
Q

Name the 3rd generation B antagonist drugs and whether they are selective or non selective.

A

carvedilol and labetalol; non selective B1 and B2

betaxolol; selective B1

46
Q

What are some of the side effects of the non selective, 1st generation B antagonist drugs, Propanolol and timolol?

A

Bradycardia, bronchoconstriction and sexual dysfunction

47
Q

What are the non selective, 1st generation B antagonist drugs, Propanolol and timolol used to treat?

A

Angina, hypertension, and Arrythmias

48
Q

Which B antagonist is the one that all other are compared to?

A

Propanolol

49
Q

What are the selective, 2nd generation B antagonist drugs, metoprolol, bisoprolol and atenolol, used to treat?

A

hypertension, angina, arrythmias and CHF

50
Q

What are some side effects of the selective, 2nd generation B antagonist drugs, metoprolol, bisoprolol and atenolol?

A

Bradycardia and sexual dysfunction

51
Q

What are the nonselective/selective 3rd generation B antagonist drugs, carvediol (NS), labetalol (NS), and betaxolol (S) used to treat?

A

CHF and hypertension

52
Q

What are some side effects of the non selective 3rd generation B antagonist drugs, carvediol and labetalol?

A

Bradycardia and fatigue

53
Q

What are some side effects of the selective 3rd generation B antagonist drug, betaxolol?

A

bradycardia

54
Q

What is the mechanism of action of cocaine?

A

prevents NE reuptake (main process for terminating NE signal)

55
Q

What is the mechanism of action of tyramine?

A

Increases cytoplasmic NE release via an exchange transporter-tyramine goes in, NE goes out

56
Q

What is the mechnism of action of Guanethidine and what is it used to treat?

A

False NT-vesicles fill with guanethidine instead of NE; used to treat hypertension
doesn’t cross BBB*

57
Q

What is the mechanism of action of reserpine and what is it used to treat?

A

It binds to the uptake transporter and inhibits it causing the vesicles that normally contain NT to be empty; used to be used an antihypertensive but not used in US anymore

58
Q

What is the mechanism of action of a-me-tyrosine and what is it used to treat?

A

inhibits tyrosine hydroxylase causing a decrease in NE synthesis; used to treat pheochromocytoma

59
Q

What is Ephedrine used to treat?

A

nasal congestion, is also an anorexic

60
Q

Which of the following drugs has depression and suicide as a possible side effect? Guanethidine, reserpine or a-me-tyrosine

A

Reserpine

61
Q

Name the 3 mechanisms for removal of NE from the synaptic cleft.

A

Uptake1-into neuron, Uptake2-into extraneuronal cells, and diffusion into bloodstream

62
Q

What is the difference in release between norepinephrine and epinephrine?

A

norepi- released locally into synapse (neurotransmitter)

epi- released into blood stream from adrenal medulla (neurohormone)

63
Q

What are the 2 main enzymes that metabolize adrenergic drugs?

A

monoamine oxidase and catechol-O-methyltransferase

64
Q

What medications/therapies should be considered to treat shock?

A
volume
NE
Isoproterenol
Dopamine-vasodilation to save kidneys
a-blockers-vasodilation
65
Q

What are the 3 main cautions to think about when treating with a-agonists?

A

localized ischemia at infusion site, avoid extravasation and gradually decrease infusion

66
Q

Why are beta blockers better at treating hypertension than alpha blockers?

A

not sure but most likely possibilities include: blocks renin release from JGA, and blocking of presynaptic receptors that enhance NE release

67
Q

Why are Beta blockers the first line therapy in CHF?

A

slows the system down to save the heart muscle from going downhill faster