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Cardio > Exam 1 - Drugs Acting on Adrenoreceptors (Alpha and Beta) > Flashcards

Exam 1 - Drugs Acting on Adrenoreceptors (Alpha and Beta) Flashcards

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1
Q

What drugs are NONSELECTIVE ß blockers? What does this mean?

A

Means they stimulate ß1 and ß2

Nadolol (corgard)
Timolol (blocadren)
Sotalol (betapace)
Propranolol (inderal)
Pindolol (visken)
Penbutolol (levatol)

(Next Track: Sabrina’s Please Please Please)

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2
Q

What drugs are selective ß1 blockers? What does this mean?

A

Means they only stimulate ß1 receptors (not ß2)

Nebivolol (bystolic)
Atenolol (tenormin)
Metoprolol tartrate (lopressor)
Esmolol (brevibloc)
Acebutolol (sectral)
Bisoprolol (zebeta)
Betaxolol (kerlone)
Metoprolol succinate (toprol xl)

(NAME A Bad Bitch? Me)

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3
Q

What is the MOA of ß blockers?

A

Bind to ß adrenoreceptors to block the binding of NE or epi

Inhibits normal sympathetic effects through these receptors

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4
Q

What are the effects of nonselective ß blockers or ß1 blockers on CO, HR, SVR, and BP?

A

CO: decreases
HR: decreases
SVR: no effect
BP: decreases

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5
Q

which ß blockers have intrinsic sympathomimetic activity?

A

Acebutolol (sectral)
Carteolol (cartrol)
Pindolol (visken)

(CAP)

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6
Q

Which ß blocker is cardioselective and also vasodilatory?

A

nebivolol (bystolic)

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7
Q

abrupt discontinuation of a ß blocker may cause ___

A

rebound HTN

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8
Q

Cardioselective ß blockers inhibit ___ at low to moderate doses. They can block ___ at higher doses

A

ß1 receptors

Can block ß2

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9
Q

What can be exacerbated when selectivity in ß blockers is lost, or when taking nonselective ß blockers? Why?

A

Asthma and COPD

Blocking ß2 receptors causes bronchoconstriction

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10
Q

Cardioselective ß blockers have additional benefits in pts with ___ or ___

A

Atrial tachyarrhythmia
Preoperative HTN

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11
Q

Nonselective ß blockers have additional benefits in patients with:

A

Essential tremor
Migraine headache
Portal HTN
Thyrotoxicosis

(TEMP)

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12
Q

There are no clear advantages to __

A

ß blockers w/ intrinsic sympathomimetic activity

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13
Q

What is a contraindication for ß blockers w/ intrinsic sympathomimetic activity?

A

patients who have had a MI

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14
Q

The additional vasodilation from ß blockers that are cardioselective and vasodilator does NOT result in more ___

A

orthostatic hypotension

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15
Q

What drugs are alpha 1 selective blockers?

A

Prazosin (minipress)
Terazosin (hytrin)
Doxazosin (cardura)

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16
Q

What drugs are nonselective alpha blockers?

A

Phentolamine (regitine)
Phenoxybenzamine

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17
Q

What is the MOA of alpha blockers?

A

Competitively block alpha 1 receptors

Causes vasodilation

Lowers peripheral vascular resistance

Lowers BP

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18
Q

Alpha blockers do NOT affect ___, ___, or ___

A

CO
Renal blood flow
Glomerular filtration rate (GFR)

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19
Q

alpha blockers block the effect of ___ on blood vessels by binding to alpha adrenoreceptors on the __

A

Sympathetic nerves
Vascular smooth muscle

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20
Q

most alpha blockers are competitive agonists to the binding of ___ that is released by ___ synapsing on ___

A

NE
Sympathetic nerves
Smooth muscle

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21
Q

Alpha blockers are also known as ___. Why?

A

Sympatholytic because they antagonize sympathetic activity

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22
Q

Some alpha blockers are noncompetitive. What does this do?

A

Greatly prolongs their action

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23
Q

How do alpha 1 antagonists cause vasodilation?

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A

by blocking NE from binding to smooth muscle receptors

24
Q

When should the first dose of an alpha blockers be given?

25
why should patients rise from sitting or laying down slowly?
to minimize orthostatic hypotension risk
26
Who may see additional benefits with alpha blockers?
men w/ BPH
27
What effect would blocking alpha/alpha 1 receptors have on CO, HR, SVR, and BP?
CO: none HR: none SVR: decrease BP: decrease
28
What drugs are alpha and beta blockers
Labetalol (trandate) Carvedilol (coreg)
29
what is labetalol?
combined alpha and ß blocker
30
labetalol is a ____ at ß receptors and a ___ of postsynaptic alpha-1 receptors
Nonselective antagonist Competitive antagonist
31
Is labetalol more potent at alpha-1 receptors or ß receptors?
ß receptors
32
labetalol is ___ after oral admin
readily absorbed (almost 100%)
33
what is the MOA of alpha + ß blockers?
Blocks alpha 1 and ß receptors Slows sinus HR Decreases peripheral vascular resistance Decreases CO Decreases arterial BP (Brains Suck, Date Dumb Dudes)
34
What issue can occur when taking labetalol?
It can produce dose-related falls in BP These can happen without reflex tachycardia or a significant reduction in HR This happens through a mix of its alpha and ß blocking effects
35
What is carvedilol?
Nonselective ß blocker + alpha 1 blocker
36
Carvedilol is a racemic mixture. Where is the ß blocking activity and where is the alpha blocking?
Nonselective ß blocking is in the S(-) enantiomer Alpha blocking is in both R(+) and S(-) enantiomers at = potency
37
what does the ß blocking ability of carvedilol do?
decreases HR, myocardial contractility, and myocardial oxygen demand
38
what does the alpha 1 blocking of carvedilol do?
decreases SVR
39
what is the absorption of carvedilol?
rapid and extensive following oral admin
40
what can abrupt discontinuation of alpha+ß blockers cause?
rebound HTN
41
In alpha+ß blockers, what does the additional alpha blockage produce?
vasodilation and orthostatic hypotension
42
What are the effects of alpha+ß blockers on CO, HR, SVR, and BP?
All will decrease
43
What are the other names of alpha 2 agonists?
Antiadrenergics Central sympatholytics
44
what drugs are alpha 2 agonists?
Clonidine (catapres) Methyldopa (aldomet) Guanabenz (wytensin) Guanfacine (tenex)
45
where do alpha 2 agonists act?
presynaptic nerve endings
46
What does the activation of sympathetic adrenergic nerves to the heart INCREASE?
HR (positive chronotropy) Contractility (positive inotropy) Velocity of electrical impulse conduction (positive dromotropy)
47
What is the MOA of alpha 2 agonists?
1: Activate alpha 2 receptors to block sympathetic activity Reduce sympathetic outflow to heart Decrease HR and contractility Decrease CO 2: Reduced sympathetic outflow to vasculature Decrease sympathetic vascular tone Vasodilation Reduced SVR Decrease arterial pressure
48
what is the MOA of clonidine?
alpha 2 agonist Lowers sympathetic outflow to heart and vasculature Lowers CO and peripheral resistance Lowers BP
49
PK of clonidine
Oral Excreted by kidney Available as a patch
50
what is the MOA of methyldopa?
Alpha 2 agonist Converted to methylnorepinephrine centrally Lowers adrenergic outflow from CNS
51
What mediates the antihypertensive action of guanbenz? What does this do?
Stimulation of central alpha receptors Decreases sympathetic outflow from brain
52
What % of oral guanbenz is absorbed and metabolized?
75%
53
what may abrupt discontinuation of alpha 2 blockers cause?
rebound HTN
54
When is an alpha 2 blocker most effective? Why?
When used w/ a thiazide to diminish fluid retention
55
how often is the clonidine patch replaced?
once weekly
56
What effects do alpha 2 agonists have on CO, HR, SVR, and BP?
all will decrease

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