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Pharmacology FINAL > Adrenoreceptor Agonists Part 2 > Flashcards

Adrenoreceptor Agonists Part 2 Flashcards

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1
Q

alpha 1 receptor activation causes vaso____ and a ____ in blood pressure

A

vasoconstriction and rise in blood pressure

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2
Q

in general, a2 receptor activation does what do blood pressure?
when can the opposite happen?

A

decrease in blood pressure

when a2 agonists are given IV or very high oral doses they may cause vasoconstriction – not normally

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3
Q

a2 agonists can be used as ________ in the treatment of hypertension

A

sympatholytics

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4
Q

effect of BETA receptor activation on the heart

A

increases cardiac output, incrased contractility, increased heart rate

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5
Q

beta receptor activation causes vaso______

A

dilatio

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6
Q

what is isoproterenol and what is it used for

A

NONSELECTIVE BETA AGONIST
binds b1,b2,b3

goal is to slightly increase systolic blood pressure and to lower diastolic, so that the overall BP is decreased

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7
Q

beta receptor activation results in positive ____, ___, and ____ effect

A

chronotropic, dromotropic, and inotropic

increased heart rate, electrical conduction, and increased contractility

beta blockers are able to reduce these influences

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8
Q

what does inotropic mean

A

NOT related to ion increase

relates to contractility force

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9
Q

what does lusitropy mean

A

relaxation of the heart

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10
Q

what effect does dopamine have on the heart***

A

activates beta 1 receptors, resulting in an increased heart rate

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11
Q

what happens when dopamine is administered IV

A

vasodilation of renal/splanchic/coronary/cerebral vessels

at HIGH doses of infucion, may cause vasoconstriction and MIMICS THE ACTIONS OF EPINEPHRINE

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12
Q

Name 2 drugs that can be used to treat glaucoma

A

cholinergic agonist

beta antagonist

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13
Q

______ are important in the treatment of asthma

A

beta 2 agonists

bronchial smooth muscle dilates

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14
Q

effect of phenylephrine on the eye

A

the eye contains alpha receptors - specifically the radial pupillary dilator muscles

phenylephrine will activate these alpha receptors and cause mydriasis (dilation)

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15
Q

true or false

beta agonists can be used to treat glaucoma

A

FALSE - beta antagonists

by decreasing the production of aqueous humor in the eye

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16
Q

what do alpha2 agonists do to the eye

A

increase the outflow of aqueous humor and thus reduce intraocular pressure

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17
Q

what is urinary continence

A

ability to control bladder function without any leaks

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18
Q

what drug can be used to promote urinary continence**?

A

the bladder base/urethral sphincter/prostate contain alpha 1 receptors

therefore, an alpha 1 agonist will mediate contraction and promote urinary continence

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19
Q

what drug can play a role in normal ejaculation?

A

alpha receptor activation in the ductus deferens/seminal vesicles/prostate

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20
Q

name a sympathomimetic drug that produces symptoms of dry mouth

A

clonidine

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21
Q

what are apocrine sweat glands?

A

NONthermoregulatory sweat glands that respond to stress and adrenoceptor stimulation

under control of SYMPATHETIC nervous system

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22
Q

true or false

beta adrenoceptor activation in fat cells leads to INCREASED lipolysis

A

true

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23
Q

what receptors INHIBIT lipolysis and how?

A

alpha 2 receptors****

inhibit lipolysis by decreasing intracellular cAMP levels (works through Gi!)

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24
Q

when beta adrenoceptors in fat cells are activated, what happens?

A

increased lipolysis

release of free fatty acids and glycerol into the blood

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25
what kind of drugs enhance GLYCOGENOLYSIS in the liver?
sympathomimetics (beta) leads to increased glucose in circulation
26
true or false beta adrenoceptor stimulation leads to both increased lipolysis AND glycogenolysis
true
27
enhanced activation of the beta adrenergic system will lead to............*******
metabolic acidosis
28
true or false sympathomimetic drugs lead to glycogen synthesis
FALSE glycogenolysis
29
effect of sympathomimetic drugs on the liver
glycogenolysis - glucose dumped into bloodstream and may cause METABOLIC ACIDOSIS****
30
TRUE OR FALSE sympathomimetic drugs will lead to decreased glucose levels in the blood
FALSE - increased bc of increased glycogenolysis
31
INSULIN SECRETION is stimulated by _____ and inhibited by______
stimulated by beta receptors (Gs) inhibited by alpha 2 receptors (Gi)*******8
32
where is insulin stored and what is needed to push it out?
in vesicles in the pancreas need calcium =
33
renin secretion is stimulated by ____ and inhibited by ______****
stimulated by B1 and inhibited by a2
34
effect of sympathomimetics on the CNS
catecholamines almost completely excluded from the CNS bc of the BBB only at very high rates of infusion are CNS effects observed - like adrenaline rush and impending doom feeling NONCATECHOLAMINES, however, that are INDIRECT adrenergic agonists like amphetamine, READILY ENTER THE CNS FROM CIRCULATION and provide mild altering effects and improved attention
35
true or false epinephrine binds both alpha and beta receptors
true
36
since epinephrine binds both alpha and beta receptors, explain its effects
a very potent vasoconstrictor and cardiac stimulant
37
HOW does epinephrine cause a rise in blood pressure? can the total diastolic pressure ever decrease?
has positive inotropic and chronotropic effects on the heart (B1) and causes vasoconstriction (alpha receptor) HOWEVER, also activates B2 bc it's not selective. this causes vasodilation and thus the total diastolic pressure may actually decrease
38
epinephrine's activation of _____ receptors in the skeletal muscle contributes to the incresed blood flow during exercise
B2
39
Which receptor does norepinephrine have little effect on?
B2
40
true or false norepinephrine increases peripheral resistance and increased both diastolic and systolic blood pressure
true however, reflexes tend to overcome to positive chronotropic effects of NE (speed of heart rate) but the inotropic effects remain (increased contractility)
41
what leads to parkinsons disease and what is the treatment?****
deficiency of dopamine in the basal ganglia treated with the precursor of dopamine - levodopa
42
what is dopamine?
a neurotransmitter in the CNS whose reward stimulus is associated with addiction
43
dopamine receptors are targets for what kind of drugs
antipsychotics
44
ENDOGENOUS dopamine has important effects in regulating what?
sodium excretion and renal function
45
explain the use of phenylephrine. include its: -selectivity -clinical use -duration of action compared to the catecholamines
selective alpha 1 agonist used as a nasal decongestant - causes vasoconstriction it has a longer duration of action than the catecholamines because it is NOT inactivated by COMT (catechol-O-methyltrasnferase)
46
what is midrodrine used for and what is it's selectivity****
prodrug - hydrolysied to desglymidodrine selective a1 receptor agonist (like phenylephrine) used to treat ORTHOSTATIC HYPOTENSION
47
What are alpha 2 selective agonists used for?
they decrease blood pressure (unless directly applied to a blood vessel) so used for the treatment of hypertension
48
effect and selectivity of isoporterenol
potent beta receptor agonist (binds all) - has little effect on a receptors positive chronotropic and inotropic actions potent vasodilator and decreases BP, INCREASES cardiac output
49
what is oxymetazoline
direct acting alpha agonist used as a decongestant bc it constricts nasal mucosa
50
**** beta 2 selective agonist agents are important in the treatment of..... give a specific drug
ASTHMA terbutaline causes bronchodilaiton and vasodilation
51
what is the effect of Beta1 selective agents?
incresaed cardiac output
52
selectivity and effects of dobutamine compared to isoproterenol
beta selective agonist greater inotropic than chronotropic effects compared to isoprotereno
53
name 2 mixed acting sympathomimetics and what they are used as***
ephedrine and pseudoephedrine decongestants
54
what is the duration of action of ephedrine? what was it originally used as?
high bioavailability and long duration of action - hours activates B receptors so used earlier in asthma treatment
55
ephedrine effects on CNS
mild stimulant
56
amphetamine is a CNS _____****
stimulant
57
the action of amphetamine is mainly through the release of ____ but also ____
mainly through release of norepinephrine but also dopamine
58
name 2 drugs that are very similar to amphetamine which has an even higher ratio of central to peripheral actions than amphetamine
methamphetamine and methylphenidate methamphetamine has even higher rate of central to peripheral actions
59
amphetamine-like indirect acting sympathomimetics can also be called........
displacers
60
what is tyramine*******
a byproduct of tyrosine metabolism produced in high conc in protein rich foods
61
what is modafinil
a psychostimulant
62
what metabolizes tyramine?
MAO (monoamine oxidase)
63
MAO inhibitors should not be taken with ______ and why?
should not be taken with high tyramine diet tyramine is a regulator of blood pressure. if a MAO inhibitor is taken, there will be too much tyramine in the body bc it can't be metabolized by MAO ----- increased BP
64
name some drugs that are indirect acting adrenergic agonists and are catecholamine reuptake inhibitors
tricyclic antidepressants and other antidepressants, cocaine atomexetine (used for ADHD - selective for NE) reboxetine - same sibutramine - serotonin and NE duloxetine - same
65
tricyclic antidepressants are reuptake inhibitors. they are selective for inhibiting the reuptake of what 2 things?
norepinephrine serotonin
66
explain the MOA of cocaine
inhibits dopamine reuptake into neurons in the CNS readily enters the CNS and produces amphetamine-like effect that is shorter but more intense than amphetamine
67
what type of drugs are used for asthma treatment
b2 selective drugs
68
what drug is used for mydriasis in ophthalmic examination
phenylephrine
69
what kind of drugs relax the uterus and are used to suppress premature labor>
beta 2 selective
70
drugs used for ADHD
low dose methylphenidate alpha 2 agonists like clonidine and guanficine atomexitine - norepinephrine reuptake inhibitor
71

Pharmacology FINAL (11 decks)

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