Adrenoreceptor ANTAGONISTS part 1

Question 1

adrenoceptor blockers can be divided into…..

Answer 1

alpha blockers and beta blockers

Question 2

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

Answer 2

labetalol and carvedilol

Question 3

name a beta 2 selective beta blocker

Answer 3

butoxamine

Question 4

name 2 beta 1 selective beta blockers

Answer 4

atenolol
metoprolol

Question 5

name 3 NONSELECTIVE beta blockers

Answer 5

propanolol
pindolol
labetolol (both alpha and beta effects)

Question 6

true or false

labetolol and metoprolol have both alpha and beta blocking effects

Answer 6

FALSE

labetolol and carvedilol

Question 7

name an alpha 2 selective blocker

Answer 7

yohimbine

Question 8

prazosin is a __ selective blocker

Answer 8

a1

Question 9

name 2 nonselective alpha blockers

Answer 9

phentolamine (reversible)

phenoxybenzamine (irreversible)

Question 10

name 2 beta receptor partial agonists

Answer 10

labetelol and pindolol

Question 11

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

explain the selectivity in more detail

Answer 11

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

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

Question 12

name an alpha blocker that is irreversible and noncompetitive

Answer 12

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)

Question 13

state the effect of alpha blockers in the cardiovascular system

Answer 13

they cause decrease in heart rate due to vasodilation

Question 14

name 2 effects of alpha blockers aside from the cardiovascular effects

Answer 14

nasal stuffiness (congestion)
miosis (eye constriction)

Question 15

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

Answer 15

pheochromocytoma

Question 16

when does phenoxybenzamine have less of an effect?

Answer 16

when the pt is supine (laying down)

Question 17

true or false

cardiac output may be increased in the administration of phenozybenzamine

Answer 17

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

Question 18

name some adverse effects of phenoxybenzamine

Answer 18

orthostatic hypotension
tachycardia
fatigue

Question 19

what is phentolamine

Answer 19

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

Question 20

what does reduced peripheral resistance mean

Answer 20

blood vessels have dilated, which increases blood flow

Question 21

explain the action of phentolamine and the use

Answer 21

reduces peripheral resistance by blocking a1 and possibly a2

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

Question 22

name some side effects of phentolamine

Answer 22

severe tachycardia
arrhythmias
myocardial ischemica

Question 23

what are prazosin and terazosin?

Answer 23

HIGHLY SELECTIVE alpha 1 blockers used to treat hypertension

Question 24

besides hypertension, what else is terazosin used for

Answer 24

selective alpha 1 blocker

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

Question 25

which has a higher bioavailability - prazosin or terazosin?

Answer 25

terazosin

Question 26

true or false prazosin is a nonselective alpha antagonist

Answer 26

FALSE selective for alpha 1

Question 27

name some clinical uses of alpha blockers

Answer 27

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)

Question 28

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

Answer 28

ALPHA 1 BLOCKERS terazosin alfuzosin doxazosin tamsulosin silodosin

Question 29

where is b1 receptor found

Answer 29

the heart

Question 30

where is b2 receptor found

Answer 30

in vasculature, bronchi

Question 31

beta antagonists are used for what conditions?

Answer 31

hypertension arrhythmia angina infarction

Question 32

do beta receptor antagonists reduce or increase renin release?

Answer 32

REDUCE renin causes retention of fluid and increased blood pressure. produces angiotensin which is potent pressor agent beta blockers want to reduce BP

Question 33

the antihypertensive action of beta antagonists depends on what 3 things

Answer 33

reduced cardiac output decreased sympathetic activity reduction of renin release

Question 34

explain the mechanism of action of beta blockers

Answer 34

they competetively reduce receptor occupancy by the catecholamines and other beta agonists BIND TO SAME SITE ON RECEPTOR - COMPETITIVE

Question 35

TRUE OR FALSE most beta blocking agents are partial agonists

Answer 35

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

Question 36

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

Answer 36

labetolol and pindolol labetolol is nonselective for neither alpha nor beta pindolol is nonselective - binds both b1 and b2 SOME ARE ALSO INVERSE AGONISTs

Question 37

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

Answer 37

betaxolol and metoprolol reduce the activity of the beta receptors below the baseline in some tissues THEREFORE the person may get hypotension

Question 38

selectivity of betaxolol and metoprolol

Answer 38

both are inverse agonists both are selective for B1

Question 39

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

Answer 39

CYP2D6

Question 40

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

Answer 40

metoprolol and propanolol

Question 41

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

Answer 41

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

Question 42

besides hypotension, name 3 other uses for beta blockers

Answer 42

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

Question 43

TRUE OR FALSE beta blockers have negative inotropic and chronotropic effects

Answer 43

true

Question 44

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

Answer 44

fall

Question 45

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

Answer 45

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

Question 46

what do beta blocking agents do to the eye?

Answer 46

REDUCE intraocular pressure, especially in glaucoma**** by decreased aqueous humor production

Question 47

name a specific beta blocker that can be used for glaucoma

Answer 47

timolol eye drops

Question 48

true or false beta blockers enhance the sympathetic nervous system in the stimulation of lipolysis

Answer 48

FALSE -- inhibit lipolysis by the sympathetic nervous system

Question 49

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

Answer 49

ends with LOL

Question 50

explain how nebivolol is different from the other beta antagonists

Answer 50

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

Question 51

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

Answer 51

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

Question 52

name 4 beta blocking agents used for glaucoma

Answer 52

timolol nadolol levobunolol betaxolol

Question 53

Explain how beta blockers can be used in hyperthyroidism

Answer 53

in hyperthyroidism, there is excessive catecholamine action, ESPECIALLY in the heart beta antagonists can be used to combat this - -namely propanolol

Question 54

__________ reduces the frequency and intensity of migraines

Answer 54

PROPANOLOL ****

Question 55

Explain the discontinuation problems with beta blockers

Answer 55

requires dose tapering due to upregulation of beta receptors

Question 56

what are some cardiovascular issues in patients taking beta blockers

Answer 56

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

Question 57

name 4 drugs that are selective for b1 blocking

Answer 57

metoprolol atenolol nebivolol betaxolol

Question 58

state the characteristics of metoprolol, atenolol, nebivolol, betaxolol

Answer 58

lower heart rate and blood pressure reduce renin may be safer is asthma bc selective for B1

Question 59

true or false there is no clinical indication for butoxamine

Answer 59

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

Question 60

name 3 drugs that block b1 AND b2

Answer 60

propanolol nadolol timolol

Question 61

true or false labetolol and pindolol have intrinsic sympathomimetic effect

Answer 61

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

Question 62

tyrosine hydroxylase inhibitor

Answer 62

metyrosine helps to lower blood pressure and can be used to treat pheochromocytoma blocks synthesis of dopamine, NE, E