Unit 4: Adrenergic Agonists Flashcards

1
Q

Stimulation of the adrenal glands causes secretion of…

A

epinephrine and norepinephrine

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2
Q

The drugs that cause effects similar to epinephrine or norepinephrine are called _____ or ____

A

adrenomimetics

sympathomimetics

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3
Q

The adrenoreceptors are …

A

alpha
beta
dopamine

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4
Q

define SELECTIVITY

A

drug binds preferentially to one subset of adrenoreceptors

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5
Q

define SPECIFICITY

A

near absolute selectivity; also, some drugs interact with more classes of receptors at higher doses/concentration

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6
Q

list 3 terms that describe the desensitization that happens when a cell or tissue is exposed to an agonist over time, and that cell/tissue becomes less responsive to further stimulation from the agent

A

tolerance
refractoriness
tachyphylaxis

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7
Q

major action that occurs with stimulation of alpha 1 receptors

A

smooth muscle contraction

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8
Q

alpha 1 receptors are located…

A
eye
hair shaft
prostate
heart
vascular smooth muscle
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9
Q

stimulation of ALPHA 1 RECEPTORS causes _____ in the EYE

A

contraction of muscle –> dilates pupil

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10
Q

stimulation of ALPHA 1 RECEPTORS causes ____ in the HAIR

A

erection

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11
Q

stimulation of ALPHA 1 RECEPTORS causes ____ in the PROSTATE

A

contraction

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12
Q

stimulation of ALPHA 1 RECEPTORS causes ____ in the HEART

A

increase in contractile force

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13
Q

stimulation of ALPHA 1 RECEPTORS causes ____ in the VASCULAR SMOOTH MUSCLE

A

contraction –> arterial and venous vasoconstriction

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14
Q

What does PHENYLEPHRINE do?

A

pure alpha agonist –> increases peripheral arterial resistance and venous capacitance –> dose-dependent increase in BP –> baroreceptor-mediated increase in vagal tone –> decrease in heart rate

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15
Q

locations of alpha 2 receptors

A
postsynaptic CNS neurons
platelets
adrenergic and cholinergic nerve terminals
some vascular smooth muscle
fat cells
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16
Q

stimulation of ALPHA 2 RECEPTORS causes ____ in the PLATELETS

A

aggregation

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17
Q

stimulation of ALPHA 2 RECEPTORS causes ____ in the ADRENERGIC and CHOLINERGIC NERVE TERMINALS

A

inhibition of transmitter release

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18
Q

stimulation of ALPHA 2 RECEPTORS causes ____ in the VASCULAR SMOOTH MUSCLE

A

contraction

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19
Q

stimulation of ALPHA 2 RECEPTORS causes ____ in the FAT CELLS

A

inhibits lipolysis

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20
Q

SYSTEMIC administration of alpha 2 agonists do what

A

inhibit sympathetic tone and decrease BP

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21
Q

What is clonidine and what is it used for?

A

alpha 2 agonist, used to treat HTN

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22
Q

Where are the beta 1 receptors located?

A

heart

juxtaglomerular cells

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23
Q

Where are the beta 2 receptors located?

A

smooth muscle of respiratory system, uterus, vascular system
skeletal muscle
human liver

24
Q

Where are the beta 3 receptors located?

A

bladder

fat cells

25
Q

What does stimulation of Beta 1 receptors cause?

A

heart –> increased rate and contractile force

juxtaglomerular cells –> increased renin release

26
Q

What does stimulation of Beta 2 receptors cause?

A

smooth muscle of respiratory system, uterus, vascular system –> muscle relaxation
skeletal muscle –> promotes uptake of potassium
human liver –> activates glycogenolysis

27
Q

What does stimulation of Beta 3 receptors cause?

A

bladder –> relaxes detrusor muscle

fat cells –> activates lipolysis

28
Q

What does ISOPROTERENOL do?

A

nonselective beta agonist that activates both beta 1 and beta 2
increases cardiac output due to increased contractility and direct SA node activation which increases heart rate

29
Q

Where are the dobutamine receptors located?

A

D1: smooth muscle
D2: nerve endings

30
Q

What does stimulation of Dopamine 1 receptors cause?

A

smooth muscle: dilates renal blood vessels

31
Q

What does stimulation of Dopamine 2 receptors cause?

A

nerve endings: modulates neurotransmitter release

32
Q

What does DOPAMINE do and what is it used for?

A

D1 receptor activation –> causes vasodilation; improves perfusion

33
Q

What does DOPAMINE do in low vs high doses?

A

LOW: decreased peripheral resistance
HIGH: vasoconstriction due to activation of vascular alpha receptors

34
Q

How do we deal with the vasoconstriction of DOPAMINE in high doses?

A

add DOBUTAMINE

35
Q

What does DOBUTAMINE do?

A

beta 1 agonist

increase heart rate, contractility, and cardiac output to maintain renal perfusion

36
Q

What effect does a beta 2 agonist have on the lungs?

A

bronchodilation to treat asthma

37
Q

What effect does an alpha 2 agonist have on the eyes?

A

constricts “constrictor muscle” to improve flow of aqueous humor and decrease intraocular pressure for treatment of glaucoma

38
Q

What effect does an alpha 1 agonist have on the genitourinary system?

A

contracts bladder base, urethral sphincter, and prostate to treat urinary incontinence

39
Q

What effect does a beta agonist have on glucose, insulin, and metabolism?

A

increased lipolysis –> increased free fatty acids in the blood
increased insulin secretion from the pancreas

40
Q

What effect does an alpha 2 agonist have on the pancreas?

A

decreased insulin secretion

41
Q

What effect does alpha 1 agonism have on smooth muscle?

A

contraction of blood vessels, eye, bladder, prostate, uterus

42
Q

What effect does alpha 1 agonism have on the liver?

A

glycogenolysis

43
Q

What effect does alpha 1 agonism have on the salivary glands?

A

profuse secretion

44
Q

What effect does a beta 1 agonist have?

A

increased heart rate and force as well as increased automaticity

45
Q

What effect does a beta 2 agonist have?

A

smooth muscle relaxation

46
Q

What effect does a beta 3 agonist have?

A

increased lipolysis

47
Q

What do the indirect sympathomimetics do?

A

act by releasing previously-selected norephinephrine

48
Q

What are some of the uses of indirect sympathomimetics?

A

ephedra: weight loss
phenylpropanolamine: appetite suppressant
AMPHETAMINES: CNS stimulants used to treat ADHD and narcolepsy

49
Q

What is the risk of a sympathomimetic?

A

widespread and nonspecific effects which can impact the cardiovascular system

50
Q

Most important effects to remember for sympathomimetics

A

alpha 1: most vascular smooth muscle; agonists CONTRACT
beta 1: heart; agonists INCREASE RATE
beta 2: respiratory and uterine smooth muscle; agonists RELAX

51
Q

Which drugs activate both alpha and beta receptors?

A

EPINEPHRINE and NOREPINEPHRINE

52
Q

Why is epinephrine and not norepinephrine used for the treatment of bronchospasm?

A

because epinephrine has a low affinity for beta 2, so is not as good at relaxing bronchial smooth muscle

53
Q

What does EPINEPHRINE do?

A

primarily affects heart via beta 1 receptors; causes increase in heart rate, stroke volume, and cardiac output

54
Q

What does NOREPINEPHRINE do?

A

vasoconstriction –> increases blood pressure –> reflex increase in parasympathetic output to heart, which slows the heart rate (happens DESPITE agonism of beta 1)

55
Q

Effect of EPINEPHRINE on blood pressure

A

DOSE DEPENDENT