Beta Blockers

Question 1

How to MOAs work? Are they older or newer?

Answer 1

block Epi and NE effects on beta adrenergic receptors.

older & cheap

Question 2

Blocking B1 has what effects on the heart?

Answer 2

Negative chronotropy–decreased HR

Negative inotropy –decreased BP

Question 3

Blocking B2 has what effects on the lungs and PV?

Answer 3

Bronchoconstriction (mild)

Vasoconstriction (mild)

Question 4

What is MSA? What effects does it have?

Answer 4

Membrane stabilizing activity–inhibits myocardial fast Na channels –> numbing effects

Question 5

What is ISA? Is it safer?

Answer 5

Intrinsic sympathomimetic activity–beta blockers with some beta agonism (door bell). May increase BP at times, so probably not safer.

Question 6

What % of BB end in -olol? and which receptors do they block?

Answer 6

99% B1-B2

Question 7

“-alol” and “-ilol” block which receptors? Are they more or less potent?

Answer 7

A1, B1, B2. More potent because they have vasodilating effects from A1 blockade.

Question 8

Give an example of a BB with ISA. What are they used for?

Answer 8

Pindolol. Patients who tend to bottom out may benefit from these.

Question 9

Give an example of a BB with MSA. What are they used for?

Answer 9

Acebutolol and propranolol. Eye drops for glaucoma.

Question 10

Give an example of a lipophilic BB. What are they used for?

Answer 10

Carvedilol, nebivolol, penbutolol. Used for seizures, delerium.

Question 11

Give an example of a BB with A1 antagonism. What are they used for?

Answer 11

Carvedilol, labetalol. Useful in treating cocaine overdose because they block B1, which drops BP and HR, and A1, which vasodilates and helps to decrease BP too.

Question 12

Give an example of a BB with NO release. What are they used for? Are they more or less potent?

Answer 12

Nebivolol. Used post MI. More potent because they have NO vasodilatory effects as well.

Question 13

General rule: as you increase the dose, the selectivity of a drug ___________.

Answer 13

Decreases.

Question 14

Give an example of a B1 Selective BB.

Answer 14

Acebutolol, atenolol, betoxolol. bisoprolol, metoprolol, nebivolol

Question 15

Why withdraw BB therapy slowly?

Answer 15

Once on BB therapy, the heart up regulates adrenergic receptors. If you stop the treatment all of the sudden, the this excess of receptors will cause the heart to be overly sensitive to E and NE. This is an emergent situation!

Question 16

Why are you cautious with BB in patients with pulmonary disease? What therapy is best in these patients?

Answer 16

Because BB block B2. B2 normally bronchodilate. So BB will cause bronchoconstriction. Selective B1 BB are best.

Question 17

Why should patients with severe allergies carry 2 Epi pens if they are on BB? Which therapy is best for these patients?

Answer 17

Because blocking the receptors decreases their sensitivity to an Epi pen if they need it. So, having double the dose is important. Selective B1 are best.

Question 18

What is the connection between BB and hypoglycemia?

Answer 18

BB mask the side effects of hypoglycemia–tremor, high HR, HA, sweating.

Question 19

What is the caution with BB and lipids? Which BB are involved the most?

Answer 19

BB may worsen the lipid panel. Nonselective BB are mostly involved.

Question 20

Why should you be cautious with BB and heart failure?

Answer 20

Decreasing inotropy will exacerbate an already struggling heart.

Question 21

What are 3 other side effects of BB that you should keep in mind?

Answer 21

depression, fatigue, sexual dysfunction

Question 22

Explain the CHF debate with BB. Which drugs are approved for CHF?

Answer 22

Although BB can decrease HR and increase fill time, they also decrease inotropy, which exacerbate HF. Bisoprolol, Carvedilol, Metoprolol.

Question 23

Which BB are approved for migraines PPX?

Answer 23

Atenolol, Bisoprolol, Metroprolol, Nadolol, Nebivolol, Propranolol, Timolol

Question 24

The C in Carvedilol stands for what?

Answer 24

CHF–studies found that it decreases mortality in CHF

Question 25

Does carvedilol have alpha blockade? How is it available?

Answer 25

Yes. PO BID only

Question 26

What does the E in esmolol stand for? What does this mean for this drug? What is it the drug of choice for?

Answer 26

ESTERASE. It is metabolized via plasma esterase, which mean it has a short half life–9 minutes. Aortic dissection.

Question 27

How do Carvedilol and Labetalol compare? What does this mean for the indications of L?

Answer 27

L > C for A1 blockade. L 7-3:1 and C 10:1.

L is used for urgent and emergent HTN.

Question 28

What is the different between urgent and emergent HTN?

Answer 28

Urgent = high HTN. Emergent = high HTN + signs of organ damage (brain, eye, kidney).

Question 29

Which BB are used for anxiety?

Answer 29

Metroprolol, Propanolol, Timolol

Question 30

Which BB are used for portal HTN?

Answer 30

Carvedilol, Nadolol, Propanolol

Question 31

Which BB has the most indications?

Answer 31

Propanolol–angina, AF, tremor, HTN, migraine PPX, Pheo, AMI, aggression, anxiety, thyroid storm, portal HTN, others…

Question 32

How is propanolol eliminated?

Answer 32

hepatic eliminated

Question 33

Which BB is used to treat open-angle glaucoma?

Answer 33

Timolol (Timoptic). Has MSA.

Question 34

A1 receptors on postynaptic neurons mediate ____________.

Answer 34

vasoconstriction.

Question 35

A2 receptors on presynaptic neurons ________ release of NTs

Answer 35

inhibit

Question 36

A1 blockers have what downside? Name some A1 blockers.

Answer 36

Postural hypotension.

Doxazosin, Prazosin, Terazosin

Question 37

A1-a blockers have what indication?

Answer 37

Bladder specific. They help men with BPH to pee more easily.

Question 38

How does blocking A1-a receptors help men pee?

Answer 38

Sympathetic innervation inhibits bladder contraction and keeps your bladder relaxed. So, inhibiting sympathetic innervation will help to contract the bladder and help you pee.

Question 39

Name an Alpha 1 agonist. What is it used for?

Answer 39

Pseudophed. Decrease nasal congestion.