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CV exam 2 > Pharmacology LECT Overview of CV Receptors and Drug Classes (Martin) > Flashcards

Pharmacology LECT Overview of CV Receptors and Drug Classes (Martin) Flashcards

1
Q

norepinephrine

A

(alpha1 = alpha2, b1»b2)

sympathomimetic (agonist)

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2
Q

epinephrine

A

a1 = a2, b1 = b2

non selective sympathomimetic (agonist)

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3
Q

isoproterenol

A

b1 = b2&raquo_space;»alpha

sympathomemetic agonist (mostly beta)

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4
Q

what does sympathomimetics agonists mean?

A

mimics sympathetic nervous system activity

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5
Q

phenylephrine

A

alpha selective agonist

alpha1> alpha 2&raquo_space;»> Beta

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6
Q

albuterol

A

B2 selective agonist

B2»B1&raquo_space;»>alpha

used in asthma–> bronchiodilation

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7
Q

dobutamine

A

B1 selectve agonist

B1>B2&raquo_space; alpha

B1 is on heart

positive inotropic & some increase in rate
Cardiac output increases
little vascular effect

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8
Q

Dopamine

A

Dopamine agonist

D1=D2&raquo_space; B» alpha

renal

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9
Q

Propranolol

A

Nonselectivce Beta adrenergic antagonist

B1 = B2&raquo_space;> alpha

used to treat high blood pressure

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10
Q

Atenolol and Metoprolol

A

B1&raquo_space; B2

B1-selectice adrenergic antagonist

used to treat high blood pressure

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11
Q

what is affinity of a drug

A

how tightly these drugs bind to the receptor

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12
Q

what is the potency of the drug

A

how much drug it takes to activate the receptor

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13
Q

Phentolamine

A

non selective alpha-adrenergic antagonist

a1 = a2

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14
Q

Prazosin

A

alpha 1 SELECTIVE alpha adrenergic ANTAGonist

a1&raquo_space;»a2

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15
Q

Carvedilol

A

mixed antagonist (both alpha and beta blocking activity)

b1 = b2 ≥ a1 >a2

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16
Q

3 Muscarinic cholinergic agonists

A

Acetylcholine (muscarinic and nicotinic agonist)
Bethanechol
Methacholine

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17
Q

Bethanechol

A

muscarinic cholinergic agonist

M1-5&raquo_space;»NM (nicotinic muscle) ,NN (nicotinic neuronal)

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18
Q

Atropine

A

Muscarinic receptor antagonist

(M1 = M2 = M3&raquo_space;»>NM,NN)
(blocks M1-M5!!)

Oral, Parenteral, Opthalmic

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19
Q

what are 3 muscarinic receptor antagonists

A

atropine
ipratropium bromide (inhale)
Tiotropium (inhale only)

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20
Q

what does dopamine cause in the kidney

A

vasodilation (renal vascular smooth muscle)

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21
Q

what effect does blocking NET pump have?

A

blocks the ability of the reuptake of NE

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22
Q

where is M1 receptors found

A

in nerves

IP3 and DAG

increase Ca

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23
Q

muscarinic are what type of receptors?

A

metabotropic

excitatory and inhibitory

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24
Q

what type of receptors are nicotinic receptors?

A

ionotropic

excitatory

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25
Q

where are M2 receptors

A

cardiovascular/heart

these cause Inhibition of cAMP production and activation of K+ channels

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26
Q

where are M3’s found

A

glandular

IP3, DAG cascade leading to increased Ca

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27
Q

where are M4 and M5 found?

A

CNS

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28
Q

where are nicotinic muscular receptors ? what are they blocked by?

A

skeletal muscle

blocked by curare

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29
Q

where are nicotinic neuronal?

what are they blocked by

A

nerves

blocked by hexamethonium

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30
Q

alpha 1 on vascular smooth muscle do what when this receptor is activated?

A

Vasoconstriction

main regulator of blood pressure

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31
Q

is there parasympathetic innervation to blood vessels?

A

NO

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32
Q

are there muscarinic cholinergic receptors on blood vessels?

A

yes

but there is no nerve or signal there to release Ach so they aren’t ever activated.

if you gave a bolus injection into the blood vessel of ACh you would get vasoconstriction, but it would last only about 2 seconds b/c there ACHesterase that would chew it up and destroy it

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33
Q

what do B2 receptors do for vasculature when they are activated?

A

cause relaxation of smooth muscle so vasodilation!

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34
Q

arteriole diameter is controlled by tonic release of what?

A

norepinephrine

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35
Q

what would happen if there was inhibition of medullary vasoconstrictor center?

A

decrease in sympathetic output and decrease in peripheral vascular resistance

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36
Q

what are the effects of alpha 1 receptor activation in the eye?

spleen?
uterus?
pilomotor muscle?
heart?

liver?

A

a1mydriasis (dilates pupil)
contraction of iris radial muscle

a1 contraction of spleen
a1 contraction of uterus
a1 contraction of pilomotor muscle (erects hair)
a1 increases force of contraction in heart
less important than b1 effect

liver–> glycogenolysis

37
Q

what are the effects of alpha 1 receptor activation in the intestinal smooth muscle

A

hyperpolarization and relaxation

38
Q

what happens when someone becomes hypoglycemic?

A

Sympathetics fire (alpha 1’s) and release norepinephrine onto the liver causing glycogenolysis breaking down stored energy into glucose

39
Q

what is the role of alpha 2 receptors mainly?

A

regulation of neurotransmitter release

these are presynaptic!!!

Autoreceptors” – NE activation of presynaptic a2 receptors decreases NE release from nerve ending.

these can also cause vasoconstriction but only is certain vascular beds and are of minor physiological significance

40
Q

what does stimulation of B1 receptors do?

A

B1 receptors are most prominent and important in the heart

stimulation causes increase in heart rate
(chronotropic effect)

increased force of contraction
inotropic effect

41
Q 
what does activation of B2 receptors in the lungs do?
vasculature?
uterus?
bladder?
intestinal smooth muscle?
A

relaxation of bronchioles b2***

relaxation of vascular smooth muscle*** b2 (vasodilation, certain vascular beds only)

relaxation of uterus b2

relaxation of detrusor (bladder) b2

relaxation of intestinal smooth muscle b2

42
Q

what would be beneficial for an asthmatic patient?

A

a beta-2 agonist

this is because in asthma the airways are constricted due to inflammation, so it is necessary to open up the airways! bronchiodilation

43
Q

what does beta-2 receptor activation do in skeletal muscle?

A

stimulates potassium uptake

44
Q 
what are the metabolic and hormonal effects of beta receptor activation?
liver
fat cells
insulin
renin
A

glycogenolysis b2 (liver) (release of glucose from the liver)

lipolysis b3 (fat cells)
stimulation of insulin release b2
stimulation of renin release b1

45
Q

when sympathetics fire, but is the effect on the kidney? what receptor?

A

D1

firing of sympathetics causes dilation
increases blood flow to the kidneys ***

so in the scenario of shock, you need good kidney flow!!! to maintain electrolytes in balance

46
Q

how is selectivity different than specificity?

A

lets say something is B2 selective agonist

the selectivity means it is dose dependent and has higher potency/higher affinity at B2 than B1 but this does not mean we won’t have any B1 effects!! because it is not SPECIFIC but rather SELECTIVE

47
Q

what is chronotropic effect?

A

something to do with heart rate

48
Q

what is inotropic effect

A

having to do with contraction of heart

49
Q

what is epinephrines effect on the heart? (rate, contraction, conduction velocity)

A

positive chronotropic effect

positive inotropic effect

increased conduction velocity in atria, A-V nodes & purkinje fibers
**
the work of the heart is increased substantially
increased oxygen consumption
**

50
Q

what is the effect of epinephrine during a heart attack? and how is this counteracted?

A

epinephrine would make things worse during a heart attack because it increases the oxygen consumption b/c the work of the heart is increased (increased contraction force, rate, and conduction velocity)

SO use a beta-blocker to slow the heart, decrease O2 consumption and work of heart

51
Q

what is the effect of epinephrine on the blood vessels?

A

a1 vasoconstriction

b2 vasodilation

***Epinephrine is more potent at B2 than alpha 1
so at the lowest levels of Epi B2 will be on first and then as Epi rises, alpha 1 will be turned on

52
Q

what predominates (alpha 1 or beta 2) at high doses of epinephrine?

A

vasoconstriction dominates

53
Q

what is the distribution of alpha 1 and beta receptors in skeletal muscle?

A

both b2 and alpha 1

so it is DOSE DEPENDENT

first start to exercise–> have vasodilation (b2)

if you go into shock or really high stress now there is alot of epi –> vasoconstriction a1

54
Q

what is distribution of alpha and beta receptors in coronaries?

A

vasodilation due to both B2 and metabolic (NO and adenosine)

55
Q

what is distribution of alpha and beta receptors in the kidney, skin, mucosa?

mesenteric beds?

cerebral?

pulmonary?

A

primarily alpha 1 vasoconstriction

mesenteric–> both b2 and a1, density varies

cerebral–> unchanged

pulmonary –> vasoconstriction alpha 1

56
Q

what is a vasopressor?

A

elevated blood pressure

so epi would be a vasopressor, used for vasoconstriction

57
Q

what is asthma treatment in kids?

A

racemic epinephrine solution in a nebulizer for kids

opens up airways b/c of B2 activation

58
Q

why is epinephrine not used in adults?

A

because it is too short acting

instead use Albuterol which activates B2 receptors selectively

59
Q 
what is epinephrines effects at smooth muscle?
lungs
GI
bladder x2
Spleen
Eye
Uterus
A

Bronchial smooth muscle relaxation b2
Opens the bronchial airways

GI-relaxation; slight decrease in muscle tone

Bladder
relax detrusor b2
contract sphincter a1

Spleen contraction

Eye - mydriasis, lowers IOP

Uterus - relax (b2) during last month of pregnancy

60
Q

at which receptors is norepinephrine an agonist? at which receptors does it have very low potency ?

A 
Agonist at a1, a2, a1 receptors
very weak (low potency) at b2 receptors**
61
Q

what is the effect of norepinephrine on the heart?

A

direct: positive inotropic and chronotropic (B1)
indirect: reflex bradycardia (blocked by atropine) muscarinic cholinergic blocker

net effect: increase force; decreased rate
slow, forceful heartbeat***

62
Q

what is norepinephrines effect on blood vessels

A

alpha 1 mediated vasoconstriction which causes an increase in BP

63
Q

what is norepinephrines use in anesthesia?

A

used as a pressor in spinal anesthesia when all autonomic control has been turned off so anesthesiologist can titrate BP and HR with NE

64
Q

where is isoproternol an agonist

what are the effects of Iso on heart

on blood vessels?

A

B receptors

NO alpha effects

Heart b1 increased heart rate and force

Blood vessels:
B2 vasodilation in skeletal muscle & mesentery
decreased diastolic BP
increased systolic BP
no change or decreased mean BP
65
Q

What are dopamines receptors

A

D1
Beta 1
alpha 1

66
Q

what are the pharmacological effects of dopamine
on blood vessels (high and low doses)
heart

A

blood vessels–> low does vasodilates renal and mesenteric (D1 receptors) increases blood flow to the kidney ***

at mildly high doses heart–> mild increase in rate and force because it is a partial agonist of B1

at even higher doses doses blood vessels–> causes vasoconstriction and increased BP (alpha 1)

this is because dopamine is related in structure to epi and NE

67
Q

what happens in cardiogenic shock and what can be done about it?

A

weak heart and not efficient in pumping and not providing enough blood flow and oxygenation

and this includes blood flow to the kidneys and electrolytes get screwed up!

So give patients a low drip rate of dopamine to increase blood flow to kidney

increase the drip a little bit more … now kicking in B1 for better CO, more forceful contraction and rate

even higher drip rate would kick in alpha receptors, which is NOT good b/c there is already very intense vasoconstriction in the periphery

***so must titrate just right

68
Q

what is the clinical use of dobutamine

what are the adverse effects>

A

MI, CHF, cardiogenic shock

Adverse effects: may increase size of infarct
potential arrhythmias

69
Q

what is the use of alpha 1 adrenergic agonists

A

pressor agents to increase BP

70
Q

what is phenylephrine

A

vasoconstricts the nasal mucosa

DECONGESTANT

doing alpha 1 mediated vasoconstriction because it is a alpha1 adrenergic agonist

Vasoconstriction nasal mucosa/ decongestant
(pressor agent) increase peripheral resistance; increase BP
increased blood pressure causes reflex bradycardia (blocked by atropine-muscarinic blocker)

71
Q

what is the main use of B2 selective agonists

A

used to treat asthma

72
Q

what is albuterol

what are its side effects

A

relatively selective b2 (10x) agonist

bronchodilation
used for treated bronchospasm in asthma

aerosol delivery - restricts to lungs, decreases systemic absorption and side effects

Oral - sometimes used, more side effects when oral

Side effects:
muscle tremors, tachycardia (B1 and reflex), anxiety, restlessness, headache, hypoglycemia, hypokalemia

73
Q

what is the difference in effects of propranolol in a person that is resting or someone who is exercising.

A

in a person who is resting there is not going to be much sympathetic tone (because rest and digest is going to be predominating)

SOOOO…. there is going to be a much greater effect in someone who is exercising or under alot of stress

74
Q

what are the pharmacological effects of propanolol?

A

decrease heart rate and cardiac output b/c blocking beta 1

decrease exercise tolerance

decrease rate of depolarization of ectopic pacemakers
Clinical –> cardiac arrhythmias, MI

Decrease work of the heart and decrease O2 demand*** MOST IMPORTANT

decrease AV nodal conduction (can produce AV block)

decrease infarct size & re-infarction- prevent sudden death

75
Q

what is an absolute contraindication to using nonselective beta blocker *** know

A

COPD and asthma patient

b/c these people already have constricted airways and are using B2 to keep them vasodilated

so you can’t block their B2 stimulation b/c it would make their breathing worse

ALSO DIABETICS b/c it masks the signs of hypoglycemia (which are usually sympathetic output like tachycardia, bp changes)

76
Q

what are B1 selective blockers used for? clinically

A

more potent at B1 than B2

at higher doses block B2 as well

lessen the risk of bronchospasm and are preferred in people with diabetes because it they usually do not prolong hypoglycemia

still contraindicated in asthmatic

77
Q

what are two examples of B1 selective blockers

A

Atenolol

Metoprolol

78
Q

what is Carvedilol (Coreg)

A

Nonselective B blocker and alpha blocker

Very lipid soluble

Decreases mortality by 65 percent in CHF clinical trials

slows the heart!! so it has to work less hard and uses less O2 and ATP most likely

79
Q

what is the parasympathetic effect (using muscarinic Ach receptors) on extravascular smooth muscle …

Bronchials
GI
Urinary bladder
Eye muscle

A

Bronchial smooth muscle contraction

GI–> increased tone and motility

Urinary bladder: contraction of detrusor, contraction (opening) of trigone and sphincter

Eye muscle: miosis via iris sphincter accommodation via ciliary muscle contraction

80
Q

what is the sympathetic effect on the eye

A

mydriasis (contraction of the radial muscle, iris)
dilates the pupils (alpha 1)

relaxes the ciliary muscle (B2)

81
Q

what is the parasympathetic effect on the eye

A

contraction (miosis) of the sphincter muscle of the iris (M3)
contraction of the ciliary muscle (M3)

82
Q

atropine is what… what does it do for the heart and vasculature

A

an antagonist of muscarinic receptors
so it reverses bradycardia by stopping the parasympathetic input to the heart (M2)

vasculature–> no direct effect b/c there is no parsympathetic innervation to vasculature

83
Q

Ipratropium

A

Muscarinic antagonist

used to treat asthma COPD (drug of choice) b/c it blocks the constriction that parasympathetic muscarinic receptors cause

84
Q

Tiotropium

A 
muscarinic antagonist  (inhalation) 
used to treat COPD and asthma

longer acting than Ipratropium

85
Q

what is combivent

A

albuterol + ipratropium bromide

86
Q

b2

A

vasodilation

causes subsequent drop in blood pressure which means decreased rate of baroreceptor firing, leading to decrease parasympathetic output and increased sympathetic output –> Increase HR

87
Q

alpha 1

A

vasoconstriction

causes increase in blood pressure and baroreceptor firing leading to increase in parasympathetic output and decreased sympathetic output meaning DECREASE HR

88
Q

muscarinic

A

decrease in heart rate b/c muscarinics usually cause vasoconstriction

89
Q

b1

A

stimulation of heart rate and force (increase)

CV exam 2 (4 decks)

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