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Pharmacology FINAL > Adrenoreceptor Agonists Part 2 > Flashcards

Adrenoreceptor Agonists Part 2 Flashcards

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
Q

what kind of drugs enhance GLYCOGENOLYSIS in the liver?

A

sympathomimetics (beta)

leads to increased glucose in circulation

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26
Q

true or false

beta adrenoceptor stimulation leads to both increased lipolysis AND glycogenolysis

A

true

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27
Q

enhanced activation of the beta adrenergic system will lead to…………***

A

metabolic acidosis

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28
Q

true or false

sympathomimetic drugs lead to glycogen synthesis

A

FALSE

glycogenolysis

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29
Q

effect of sympathomimetic drugs on the liver

A

glycogenolysis - glucose dumped into bloodstream and may cause METABOLIC ACIDOSIS**

30
Q

TRUE OR FALSE

sympathomimetic drugs will lead to decreased glucose levels in the blood

A

FALSE - increased bc of increased glycogenolysis

31
Q

INSULIN SECRETION is stimulated by _____ and inhibited by______

A

stimulated by beta receptors (Gs) inhibited by alpha 2 receptors (Gi)***8

32
Q

where is insulin stored and what is needed to push it out?

A

need calcium

in vesicles in the pancreas

33
Q

renin secretion is stimulated by ____ and inhibited by ______**

A

stimulated by B1 and inhibited by a2

34
Q

effect of sympathomimetics on the CNS

A

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
Q

true or false

epinephrine binds both alpha and beta receptors

A

true

36
Q

since epinephrine binds both alpha and beta receptors, explain its effects

A

a very potent vasoconstrictor and cardiac stimulant

37
Q

HOW does epinephrine cause a rise in blood pressure?
can the total diastolic pressure ever decrease?

A

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
Q

epinephrine’s activation of _____ receptors in the skeletal muscle contributes to the incresed blood flow during exercise

A

B2

39
Q

Which receptor does norepinephrine have little effect on?

A

B2

40
Q

true or false

norepinephrine increases peripheral resistance and increased both diastolic and systolic blood pressure

A

true

however, reflexes tend to overcome to positive chronotropic effects of NE (speed of heart rate) but the inotropic effects remain (increased contractility)

41
Q

what leads to parkinsons disease and what is the treatment?**

A

deficiency of dopamine in the basal ganglia

treated with the precursor of dopamine - levodopa

42
Q

what is dopamine?

A

a neurotransmitter in the CNS whose reward stimulus is associated with addiction

43
Q

dopamine receptors are targets for what kind of drugs

A

antipsychotics

44
Q

ENDOGENOUS dopamine has important effects in regulating what?

A

sodium excretion and renal function

45
Q

explain the use of phenylephrine.

include its:

-selectivity
-clinical use
-duration of action compared to the catecholamines

A

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
Q

what is midrodrine used for and what is it’s selectivity**

A

prodrug - hydrolysied to desglymidodrine

selective a1 receptor agonist (like phenylephrine)

used to treat ORTHOSTATIC HYPOTENSION

47
Q

What are alpha 2 selective agonists used for?

A

they decrease blood pressure (unless directly applied to a blood vessel)

so used for the treatment of hypertension

48
Q

effect and selectivity of isoporterenol

A

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
Q

what is oxymetazoline

A

direct acting alpha agonist

used as a decongestant bc it constricts nasal mucosa

50
Q

** beta 2 selective agonist agents are important in the treatment of…..

give a specific drug

A

ASTHMA

terbutaline

causes bronchodilaiton and vasodilation

51
Q

what is the effect of Beta1 selective agents?

A

incresaed cardiac output

52
Q

selectivity and effects of dobutamine compared to isoproterenol

A

beta selective agonist

greater inotropic than chronotropic effects compared to isoprotereno

53
Q

name 2 mixed acting sympathomimetics and what they are used as***

A

ephedrine and pseudoephedrine

decongestants

54
Q

what is the duration of action of ephedrine?
what was it originally used as?

A

high bioavailability and long duration of action - hours

activates B receptors so used earlier in asthma treatment

55
Q

ephedrine effects on CNS

A

mild stimulant

56
Q

amphetamine is a CNS _____**

A

stimulant

57
Q

the action of amphetamine is mainly through the release of ____ but also ____

A

mainly through release of norepinephrine but also dopamine

58
Q

name 2 drugs that are very similar to amphetamine

which has an even higher ratio of central to peripheral actions than amphetamine

A

methamphetamine and methylphenidate

methamphetamine has even higher rate of central to peripheral actions

59
Q

amphetamine-like indirect acting sympathomimetics can also be called……..

A

displacers

60
Q

what is tyramine***

A

a byproduct of tyrosine metabolism

produced in high conc in protein rich foods

61
Q

what is modafinil

A

a psychostimulant

62
Q

what metabolizes tyramine?

A

MAO (monoamine oxidase)

63
Q

MAO inhibitors should not be taken with ______ and why?

A

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
Q

name some drugs that are indirect acting adrenergic agonists and are catecholamine reuptake inhibitors

A

tricyclic antidepressants and other antidepressants, cocaine

atomexetine (used for ADHD - selective for NE)
reboxetine - same
sibutramine - serotonin and NE
duloxetine - same

65
Q

tricyclic antidepressants are reuptake inhibitors.

they are selective for inhibiting the reuptake of what 2 things?

A

norepinephrine
serotonin

66
Q

explain the MOA of cocaine

A

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
Q

what type of drugs are used for asthma treatment

A

b2 selective drugs

68
Q

what drug is used for mydriasis in ophthalmic examination

A

phenylephrine

69
Q

what kind of drugs relax the uterus and are used to suppress premature labor>

A

beta 2 selective

70
Q

drugs used for ADHD

A

low dose methylphenidate

alpha 2 agonists like clonidine and guanficine

atomexitine - norepinephrine reuptake inhibitor

71
Q
A

Pharmacology FINAL (11 decks)

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