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Pharmacology FINAL > Adrenoreceptor ANTAGONISTS part 1 > Flashcards

Adrenoreceptor ANTAGONISTS part 1 Flashcards

1
Q

adrenoceptor blockers can be divided into…..

A

alpha blockers and beta blockers

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2
Q

name 2 drugs that have both alpha and beta blocking effects**

A

labetalol and carvedilol

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3
Q

name a beta 2 selective beta blocker

A

butoxamine

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4
Q

name 2 beta 1 selective beta blockers

A

atenolol
metoprolol

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5
Q

name 3 NONSELECTIVE beta blockers

A

propanolol
pindolol
labetolol (both alpha and beta effects)

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6
Q

true or false

labetolol and metoprolol have both alpha and beta blocking effects

A

FALSE

labetolol and carvedilol

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7
Q

name an alpha 2 selective blocker

A

yohimbine

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8
Q

prazosin is a __ selective blocker

A

a1

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9
Q

name 2 nonselective alpha blockers

A

phentolamine (reversible)

phenoxybenzamine (irreversible)

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10
Q

name 2 beta receptor partial agonists

A

labetelol and pindolol

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11
Q

as mentioned, labetolol and carvediolol have both alpha and beta blocking effects

explain the selectivity in more detail

A

b1=b2 > or equal to alpha 1> alpha 2

most selective for betas, then alpha 1, then alpha 2

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12
Q

name an alpha blocker that is irreversible and noncompetitive

A

phenoxybenamine

non selective alpha blocker that binds COVALENTLY to alpha receptors

stops catecholamine induced vasoconstriction due to tumor on adrenal gland that is releasing too much NE (phenochromocytoma)

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13
Q

state the effect of alpha blockers in the cardiovascular system

A

they cause decrease in heart rate due to vasodilation

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14
Q

name 2 effects of alpha blockers aside from the cardiovascular effects

A

nasal stuffiness (congestion)
miosis (eye constriction)

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15
Q

the major use of phenoxybenzamine is in treatment of _________**

A

pheochromocytoma

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16
Q

when does phenoxybenzamine have less of an effect?

A

when the pt is supine (laying down)

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17
Q

true or false

cardiac output may be increased in the administration of phenozybenzamine

A

true bc of reflex effects and some blocking of the a2 receptors

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18
Q

name some adverse effects of phenoxybenzamine

A

orthostatic hypotension
tachycardia
fatigue

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19
Q

what is phentolamine

A

a competitive (reversible) antagonist at BOTH ALPHA 1 AND 2 RECEPTORS****

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20
Q

what does reduced peripheral resistance mean

A

blood vessels have dilated, which increases blood flow

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21
Q

explain the action of phentolamine and the use

A

reduces peripheral resistance by blocking a1 and possibly a2

also used to treat pheochromocytoma
also used to reverse local anesthesia in soft tissue sites

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22
Q

name some side effects of phentolamine

A

severe tachycardia
arrhythmias
myocardial ischemica

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23
Q

what are prazosin and terazosin?

A

HIGHLY SELECTIVE alpha 1 blockers used to treat hypertension

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24
Q

besides hypertension, what else is terazosin used for

A

selective alpha 1 blocker

used for men with urinary retention issues due to benign prostatic hyperplasi

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25
Q

which has a higher bioavailability - prazosin or terazosin?

A

terazosin

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26
Q

true or false

prazosin is a nonselective alpha antagonist

A

FALSE

selective for alpha 1

27
Q

name some clinical uses of alpha blockers

A

pheochromocytoma (too much NE and E)*****

urinary obstruction due to BPH – go to bathroom too much bc not getting it all out every time -***

male sexual dysfunction

chronic hypertension

hypertensive emergency when alpha agonist levels too high

peripheral vascular occlusive disease (Raynaud”s)

28
Q

name drugs that can be used to treat BPH (benign prostatic hyperplasia)

A

ALPHA 1 BLOCKERS

terazosin
alfuzosin
doxazosin
tamsulosin
silodosin

29
Q

where is b1 receptor found

A

the heart

30
Q

where is b2 receptor found

A

in vasculature, bronchi

31
Q

beta antagonists are used for what conditions?

A

hypertension
arrhythmia
angina
infarction

32
Q

do beta receptor antagonists reduce or increase renin release?

A

REDUCE

renin causes retention of fluid and increased blood pressure. produces angiotensin which is potent pressor agent

beta blockers want to reduce BP

33
Q

the antihypertensive action of beta antagonists depends on what 3 things

A

reduced cardiac output
decreased sympathetic activity
reduction of renin release

34
Q

explain the mechanism of action of beta blockers

A

they competetively reduce receptor occupancy by the catecholamines and other beta agonists

BIND TO SAME SITE ON RECEPTOR - COMPETITIVE

35
Q

TRUE OR FALSE

most beta blocking agents are partial agonists

A

FALSE - most are pure antagonists that cause NO effect of the beta receptor when it’s bound

however, SOME are partial agonists like labetolol and pindolol

36
Q

name 2 beta blockers that are partial agonists and state their selectivity

A

labetolol and pindolol

labetolol is nonselective for neither alpha nor beta

pindolol is nonselective - binds both b1 and b2

SOME ARE ALSO INVERSE AGONISTs

37
Q

NAME 2 BETA BLOCKERS THAT ARE INVERSE AGONISTS AND WHAT THIS MEANS

A

betaxolol and metoprolol

reduce the activity of the beta receptors below the baseline in some tissues

THEREFORE the person may get hypotension

38
Q

selectivity of betaxolol and metoprolol

A

both are inverse agonists

both are selective for B1

39
Q

name the enzyme that is a major determinant of individual differences in metoprolol plasma clearance**

A

CYP2D6

40
Q

__ and ___ are extensively metabolized in the liver, with little unchanged drug appearing in the urine

A

metoprolol and propanolol

41
Q

true or false

beta blockers are given chronically to lower blood pressure in patients with hypertension

these drugs usually cause hypotension in healthy individuals with normal blood pressure

A

FALSE

all is true except that they cause hypotension in healthy patients with normal blood pressure

42
Q

besides hypotension, name 3 other uses for beta blockers

A

angina
chronic heart failure
following a myocardial infarction
arrhythmias
ischemic heart disease
obstructive cardiomyopathy (can increase stroke volume)

GLAUCOMA

43
Q

TRUE OR FALSE

beta blockers have negative inotropic and chronotropic effects

A

true

44
Q

CHRONIC administration of beta blockers leads to a ___ in peropheral resistance in patients with hypertension

A

fall

45
Q

blocking the beta 2 receptors causes what?
what can you conclude from this?

A

may lead to airway resistance in bronchial smooth muscle, particularly in asthma patients

therefore, beta 1 selective antagonists like metoprolol and atenolol have an advantage over nonselective beta antagonists

46
Q

what do beta blocking agents do to the eye?

A

REDUCE intraocular pressure, especially in glaucoma**

by decreased aqueous humor production

47
Q

name a specific beta blocker that can be used for glaucoma

A

timolol eye drops

48
Q

true or false

beta blockers enhance the sympathetic nervous system in the stimulation of lipolysis

A

FALSE – inhibit lipolysis by the sympathetic nervous system

49
Q

drugs with beta adrenoceptor antagonist action generally have what kind of name?

A

ends with LOL

50
Q

explain how nebivolol is different from the other beta antagonists

A

it is the MOST SELECTIVE B1 antagonist AND elicits vasodilation due to its action on endothelial nitric oxide production

51
Q

true or false

metoprolol, atenolol, and other Beta 1 selective antagonists should not be used in patients with asthma

A

not necessarily

they can be used - definitely preferred over non selective beta antagonists, but they should be used in asthma patients with caution

benefits outweigh the risks in patients who’ve had a mycoardial infarction

52
Q

name 4 beta blocking agents used for glaucoma

A

timolol
nadolol
levobunolol
betaxolol

53
Q

Explain how beta blockers can be used in hyperthyroidism

A

in hyperthyroidism, there is excessive catecholamine action, ESPECIALLY in the heart

beta antagonists can be used to combat this - -namely propanolol

54
Q

__________ reduces the frequency and intensity of migraines

A

PROPANOLOL **

55
Q

Explain the discontinuation problems with beta blockers

A

requires dose tapering due to upregulation of beta receptors

56
Q

what are some cardiovascular issues in patients taking beta blockers

A

reduce in heart rate and contractility and should be used cautiously in myocardial infarction patients

57
Q

name 4 drugs that are selective for b1 blocking

A

metoprolol
atenolol
nebivolol
betaxolol

58
Q

state the characteristics of metoprolol, atenolol, nebivolol, betaxolol

A

lower heart rate and blood pressure

reduce renin

may be safer is asthma bc selective for B1

59
Q

true or false

there is no clinical indication for butoxamine

A

true

it is a selective B2 blocker
increases peripheral resistance and provokes asthma

60
Q

name 3 drugs that block b1 AND b2

A

propanolol
nadolol
timolol

61
Q

true or false

labetolol and pindolol have intrinsic sympathomimetic effect

A

TRUE

this basically just means they are partial agonists

they lower BP like other b blockers, but only slightly lower heart rate bc of partial agonist/intrinsic sympathomimetic effect

62
Q

tyrosine hydroxylase inhibitor

A

metyrosine

helps to lower blood pressure and can be used to treat pheochromocytoma

blocks synthesis of dopamine, NE, E

63
Q
A

Pharmacology FINAL (11 decks)

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