Konorev Adrenergic Drugs Flashcards

1
Q

adrenergic receptors can be divided what 2 was?

A

genetic analysis/separation and pharmacologically

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2
Q

alpha 1 receptor is associated with what kind of G protein?

A

Gq

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3
Q

what kind of G protein with alpha 2?

A

Gi

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4
Q

Gq activates what?

A

IP3 and MAPK pathways

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5
Q

terminally differentiated cells that have Gq stimulation results in what?

A

hypertrophy

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6
Q

beta receptors activate what?

A

AC

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7
Q

activation of which adrenergic receptor will increase levels of cAMP in tissue?

A

Beta1

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8
Q

which adrenergic receptor is found on most vascular smooth m.?

A

alpha1

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9
Q

activation of which adrenergic receptor will decrease levels of cAMP in target tissues?

A

D2 (dopamine 2)

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10
Q

how to indirect acting drugs change neurotransmission?

A

change level of concentration of norepinephrine (or dopamine) at target receptors

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11
Q

phenylephrine is mostly selective for what receptor?

A

alpha1

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12
Q

we need to know what to know the pharmacodynamics of an adrenergic drug?

A

where receptors are located and effects of receptor activation

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13
Q

what is tachyphylaxis?

A

accute (sudden) decrease in the response to a drug after its administration

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14
Q

epinephrine has what effect on cardiac function?

A

increase force of contraction (positive ionotropic effect), HR, increase conduction velocity at AV node, Beta 1 receptors

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15
Q

epinephrines effects on vascular tone varies because?

A

there are different types of receptors found in vascular beds:
skin/mucous membranes: alpha1
skeletal m.: alpha1 and beta2
renal, cerebral: D1 and alpha1

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16
Q

epinephrine effect on respiratory system?

A

relax bronchial m. (beta 2), decrease bronchial secretion and congestion within mucosa (alpha 1)

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17
Q

what does epinephrine cause in skeletal m.?

A

causes m. tremor (beta 2) — side effect!!

increases K+ uptake (beta 2)

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18
Q

increase in K+ uptake by skeletal m. can cause what systemically?

A

hypokalemia and decrease K excretion by kidneys

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19
Q

what does epinephrine do to fat cells?

A

increase free fatty levels in blood (Beta) due to increase lipolysis

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20
Q

how does epinephrine elevate blood sugar?

A

enhances liver glycogenolysis (beta 2) and
inhibits insulin release (alpha 2 and beta 2)
– decreases skeletal m. use of glucose as well.

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21
Q

norepinephrine lacks agonist effects on what kind of receptors?

A

beta 2

22
Q

NE does what to heart?

A

cardiac stimulant but reduces HR—> bradycardia

23
Q

norepinephrine has what efffect on vessels? why?

A

potent vasoconstrictor, does not have opposing Beta 2 vasodilation to offset (unlike epinephrine)

24
Q

what is blood pressure equal to?

A

BP= COx vascular resistance

25
Q

what does norepinephrine do to BP?

A

largely increase

26
Q

dopamine1 stimulation causes what?

A

vasodilation

27
Q

where are there high density D1 receptors?

A

renal, cerebral, mesenteric and coronary vessels

28
Q

activation of D2 receptor does what?

A

suppresses NE release

29
Q

at higher does dopamine causes what on heart?

A

activates B1 in heart

30
Q

even higher doses of dopamine cause what?

A

vascular (alpha1) AR–> vasoconstriction

31
Q

which acts primarily on receptors located on membrane of autonomic effector cell?

A

norepinephrine

has to be direct acting drug

32
Q

dilation of vessels in skeletal m., constriction of cutaneous vessels, and direct positive ionotropic and chronotropic effects on the heart are all actions of…?

A

epinephrine

33
Q

phenylephrine is what kind of drug?

A

alpha 1 agonist

34
Q

what effect does phenylephrine have on vessels?

A

increase in vasoconstriction and BP elevation

35
Q

phenylephrine causes activation of what reflex?

A

baroreflex

36
Q

clonidine activates what kinds of receptors?

A

alpha 2

37
Q

what does cloidine do in lower brainstem?

A

decreases sympathetic outflow, reduces BP, bradycardia

38
Q

local application of clonidine causes?

A

vasoconstriction

39
Q

where does clonidine act?

A

alpha 2 receptors pre-synaptically, decreases NE release

– NE feedback on self (to alpha 2 receptor)

40
Q

what does clonidine do to NE levels with cardiovasular system?

A

decreases:
alpha1- arterial smooth m.– vasodilation
beta 1- heart– decreases HR and CO

41
Q

isoproterenol is what kind of agonist?

A

non-selective beta agonist

42
Q

what isoproterenol do in heart?

A

increase ionotropic and chronotropic action, increase CO

43
Q

main difference in isoproterenol and epinephrine?

A

isoproterenol does not activate alpha 1 receptors

44
Q

what is the result of alpha 1 activation with isoproterenol?

A

increase in systolic but drop in diastolic, mean arterial pressure drops too

45
Q

drop in blood pressure causes activation of what?

A

baroreflex— leads to significant tachycardia

46
Q

dobutamine activates?

A

selective beta 1 (also found to have alpha 1 receptor activity, racemic mix that activates and antagonizes alpha 1)

47
Q

the alpha 1 activity of dobutamine causes what effect compared to isoproterenol?

A

less prominent chronotropic action

48
Q

what are the names for the beta2 selective agonists?

A

terbutaline, albuterol

49
Q

what can beta 2 agonists cause?

A

bronchodilation and relaxation of uterus

50
Q

phenyephrine causes what?

A

constriction of vessels in the nasal mucosa

51
Q

Adrenergic modulate what?

A

adrenergic transmission and control the function of sympathetic nervous system