Beta Blockers

Front 1

What are the five mechanisms of action of beta-blockers?

Back 1

1. Competitive inhibition of cardiac Beta1 receptors.
2. Competitive blockade of Beta1 receptors that mediate renin release.
3. Competitive blockade of pulmonary Beta 2 receptors.
4. Blockade of presynaptic Beta2 receptors.
5. CNS effects

Front 2

What is a drawback of the competitive inhibition of cardiac Beta1 receptors when taking Beta-Blockers?

Back 2

Anytime there is a decrease Cardiac Output, acute reflexes will increase TPR to get BP back up. Because increases in CO are being blocked, this has a big effect on exercise tolerance. The ability to perform exercise will depend on dose and which Beta-Blocker being taken.

Front 3

What is the result of competitive blockade of Beta1 receptors that mediate renin release when taking Beta-Blockers?

Back 3

Decrease in Angiotensin II

Front 4

What is the danger in the competitive blockade of pulmonary Beta2 receptors when taking Beta-Blockers?

Back 4

This will decrease bronchial smooth muscle relaxation which could cause bronchospasm in asthma.

Front 5

What will the blockade of presynaptic Beta2 receptors do when taking Beta-Blockers?

Back 5

Decrease NE release

Front 6

What are two CNS effects from taking Beta-Blockers?

Back 6

1. Decrease SNS activity
2. Altered baro-reflex response

Front 7

What can decreasing the SNS activity due to taking Beta-Blockers cause?

Back 7

Some BB, especially those highly lipid soluble, can produce depression. BB have actions on migraine headaches. BB can be used prophylactically for migraines, but will actually worsen headache if taken after migraine has started.

Front 8

Scenario: 55yo female with CAD taking metoprolol. What would your recommendation be given the following data:
Resting BP - 102/80
Resting HR - 60
After Activity BP - 130/85
After Activity HR - 85

Back 8

Should increase dose of metoprolol because of HR change. One of the things to be concerned about in CAD is angina (pain associated with elevated workload on the heart). Angina is usually associated with elevation in HR. Would want to increase dose, so the HR would go up less and less likely to have pain.

Front 9

Name five ways you can differentiate Beta-Blockers.

Back 9

1. Selectivity
2. Metabolism
3. Intrinsic Sympathomimetic activity
4. Membrane stabilizing activity
5. Direct vasodilation

Front 10

How can BB differ in selectivity?

Back 10

BB can be selective or nonselective.

Front 11

How can BB differ in their metabolism?

Back 11

Some BB have hepatic metabolism with good GI absoprtion, first pass metabolism, and a decreased half-life.
Some BB have renal metabolism and are water soluble and have poor absorption.
Would have to consider patient's liver and kidney status to determine which one to use.

Front 12

How do BB differ in their intrinsic sympathomimetic activity?

Back 12

BB have inherent agonist activity even though they're antagonists. So would have to consider what kind of agonist activity would be preferred for which disease state. BB differ in amount of agonist activity they have and in which receptors they activate.

Front 13

For which three disease states would you consider a BB intrinsic sympathomimetic activity?

Back 13

1. Asthma
2. Heart Failure
3. Symptomatic bradycardia

Front 14

How do BB differ in their membrane stabilizing activity?

Back 14

Some BB have local anesthetic activity and enhanced anti-arrythmic activity. Can make a difference as to which agent you choose depending on whether local anesthetic activity would be useful. Have to give medication at higher dose range to see this effect.

Front 15

What six features will third generation BB incorporate to impact direct vasodilation?

Back 15

1. NO production
2. Alpha1 antagonist
3. Beta2 Agonist
4. Calcium entry blockade
5. Potassium channel opening
6. Antioxidant activity

Front 16

What does the lipid solubility of a Beta-Blocker determine?

Back 16

It determines how well the BB can get into the CNS. (Depression concerns)

Front 17

Name the six Non-selective Beta-Blockers.

Back 17

1. Nadolol
2. Penbutolol
3. Pindolol
4. Propranolol
5. Sotolol
6. Timolol

Front 18

What is the membrane stabilizing qualities, lipid solubility, and ISA of Nadolol?

Back 18

No membrane stabilizing
Low lipid Solubility
No ISA

Front 19

What is the membrane stabilizing qualities, lipid solubility, and ISA of Penbutolol?

Back 19

No membrane stabilizing
High lipid solubility
Minimal ISA

Front 20

What is the membrane stabilizing qualities, lipid solubility, and ISA of Pindolol?

Back 20

Minimal membrane stabilizing
Low lipid solubility
High ISA

Front 21

What is the membrane stabilizing qualities, lipid solubility, and ISA of Propranolol?

Back 21

Moderate membrane stabilizing
High lipid solubility
No ISA

Front 22

What is the membrane stabilizing qualities, lipid solubility, and ISA of Sotolol?

Back 22

No membrane stabilizing
Low lipid solubility
No ISA

Front 23

What is the membrane stabilizing qualities, lipid solubility, and ISA of Timolol?

Back 23

No membrane stabilizing
Moderate lipid solubility
No ISA

Front 24

Name the five Selective Beta1 Blockers.

Back 24

1. Acebutolol
2. Atenolol
3. Bisoprolol
4. Esmolol
5. Metoprolol

Front 25

What is the membrane stabilizing qualities, lipid solubility, and ISA of Acebutolol?

Back 25

Minimal membrane stabilizing
Low lipid solubility
Moderate ISA

Front 26

What is the membrane stabilizing qualities, lipid solubility, and ISA of Atenolol?

Back 26

No membrane stabilizing
Low lipid solubility
No ISA

Front 27

What is the membrane stabilizing qualities, lipid solubility, and ISA of Bisoprolol?

Back 27

No membrane stabilizing
Low lipid solubility
No ISA

Front 28

What is the membrane stabilizing qualities, lipid solubility, and ISA of Esmolol?

Back 28

No membrane stabilizing
Low lipid solubility
No ISA

Front 29

What is the membrane stabilizing qualities, lipid solubility, and ISA of Metoprolol?

Back 29

Minimal membrane stabilizing (at high doses)
Moderate lipid solubility
No ISA

Front 30

What are the five third generation Beta-Blockers with other actions?

Back 30

1. Cartelol
2. Carvedilol
3. Labetalol
4. Betaxolol
5. Nebivolol

Front 31

What is the membrane stabilizing qualities, lipid solubility, ISA, and other actions of Cartelol?

Back 31

No membrane stabilizing
Low lipid solubility
Moderate ISA
Actions: NO and Beta2 Agonist

Front 32

What is the membrane stabilizing qualities, lipid solubility, ISA, and other actions of Carvedilol?

Back 32

Moderate membrane stabilizing
Moderate lipid solubility
No ISA
Actions: Alpha1 Blockade, antioxidant, and antiproliferative

Front 33

What is the membrane stabilizing qualities, lipid solubility, ISA, and other actions of Labetalol?

Back 33

Some membrane stabilizing
Low lipid solubility
High ISA
Actions: Alpha1 Blockade and Beta2 agonist

Front 34

What is the membrane stabilizing qualities, lipid solubility, ISA, and other actions of Betaxolol?

Back 34

Some membrane stabilizing
Moderate lipid solubility
No ISA
Actions: Vasodilation and Calcium Entry Blocker

Front 35

What is the membrane stabilizing qualities, lipid solubility, ISA, and other actions of Nebivolol?

Back 35

No membrane stabilizing
Moderate lipid solubility
No ISA
Actions: Most Beta1 Selective, Increase NO, and antioxidant

Front 36

Name six third generation Beta-Blockers still in clinical trials.

Back 36

1. Bucindolol - non-selective; B2 agonist; A1 antagonist
2. Celiprolol - selective; B2 agonist; A2 antagonist; increase NO
3. Bopindolol - Increase NO; B2 agonist
4. Nipradilol - Increase NO; A1 antagonist (approved in Japan for CHF and glaucoma)
5. Bevantolol - A1 antagonist; Ca entry blocker
6. Tilisolol - non-selective; K+ channel opening

Front 37

True/False: Beta Blockers were developed specifically for hypertension.

Back 37

False.

It was initially thought that you wouldn't want to use BB for high blood pressure.

Front 38

What does the American Hypertensive Association (AHA) recommend for hypertension?

Back 38

AHA believes the most important thing is to get the blood pressure down, and that it doesn't matter which one you start with. If medication isn't showing results, AHA believes you should switch the medication and not worry about adjusting dose.

Front 39

In which three conditions does the AHA recommend BB as the first line treatment?

Back 39

1. Angina
2. MI
3. Atrial Fibrillation

Front 40

What medications does the AHA recommend as first line treatments for hypertension?

Back 40

1. ACEI
2. ARB
3. Thiazide-like Diuretics
4. Calcium Channel Blocker
(Usually two drugs to achieve)

Front 41

What does the European Society of hypertension (ESH) recommend for hypertension?

Back 41

ESH believes that BB are still the first line treatment and definitely important to select with co-morbidities.

Front 42

What does the British Hypertension Association (BHA) recommend for hypertension?

Back 42

BHA states there are too many side effects with BB, and they shouldn't be used at all. 4th line treatment.

Front 43

What type of patients do BB work best in?

Back 43

BB work best in young people with resting tachycardia, increased catecholamines, and increased renin.

Front 44

What is a common complaint of BB?

Back 44

A common complaint of BB is fatigue and limited exercise tolerance.

Front 45

Which type of hypertension do BB work best in?

Back 45

BB work best in high renin hypertension though they're still useful in low renin.

Front 46

What do BB do in people with normal blood pressure?

Back 46

BB don't do much in people with normal BP.

Front 47

What are the five mechanisms of action of BB?

Back 47

1. Decrease CO (Beta1)
2. Decrease Ang II (Beta1)
3. Decrease NE release (Beta2)
4. Decrease SNS centrally
5. Alter baro-reflex

Front 48

How is the baro-reflex altered in a person with hypertension?

Back 48

The baro-reflex in a person with hypertension has a higher set point than people with normal blood pressure. BB will return the sensitivity of the baro-reflex.

Front 49

How are ISA and CO and TPR related?

Back 49

The BB that have ISA activity have less effect on CO and more effect on TPR. The BB without ISA mainly have CO effect.

Front 50

What are additional uses for BB aside from hypertension?

Back 50

1. Glaucoma
2. Migraine Prophylaxis
3. Hyperthyroidism
4. Angina Pectoris
5. Acute MI
6. Supraventricular arrythmias
7. Acute panic attacks
8. Benign Essential Tremor
9. CHF

Front 51

How do BB improve glaucoma?

Back 51

BB decrease the production of aqueous humor in the ciliary body by blocking Beta2 receptors.

Front 52

True/False: There are no systemic effects when using a BB eyedrop for Glaucoma.

Back 52

False.

Front 53

What are the three BB used most often for Glaucoma?

Back 53

1. Timolol
2. Betaxolol
3. Cartelol

Front 54

What are the two BB used most often for migraine prophylaxis?

Back 54

1. Propranolol
2. Timolol

Front 55

What is important to tell migraine sufferers about BB?

Back 55

BB are just to be used prophylactically. If take BB after the onset of migraine, it will actually make the headache worse.

Front 56

What effect do BB have on hyperthyroidism?

Back 56

BB don't deal with the elevated thyroid levels but deal with the symptoms of the increased sympathetic activity. BB can decrease tachycardia, tremor, and anxiety.

Front 57

What do you have to watch for when administering BB for hyperthyroidism?

Back 57

When giving BB to patients with thyrotoxicosis, they may have a decreased stroke volume due to their increase in HR, so after the blockade you may see an increase in SV and BP.

Front 58

True/False: BB can decrease the peripheral conversion of T4 to T3.

Back 58

True.

Front 59

What is angina?

Back 59

Angina is the chest pain associated with the myocardial oxygen demand exceeding the supply of oxygen to the heart muscle usually due to the blockage of coronary blood vessels and increased NE/EPI. Angina results when increased HR or increases myocardial contractility beyond a certain threshold.

Front 60

How do BB help with angina?

Back 60

BB increase the time to get to the heart rate associated with the angina. BB will prolong exercise time by prolonging the time to get to the symptoms.

Front 61

How do BB help in people who have had acute myocardial infarction?

Back 61

BB lower the activity of the heart muscle itself, so they decrease oxygen demand. BB prevent the damaged heart from working as hard as it normally would and allows it time to heal. BB decrease contractility, HR, and oxygen demand preventing against recurrent MI. BB also protect ischemic myocardium from NE/EPI.

Front 62

How do BB help with supraventricular arrhythmias?

Back 62

BB have the ability to slow down conduction through cardiac tissue and through the AV node. If conduction through the AV node is slowed, the rapid impulses will arrive at AV node during refractory period. If impulse gets there during refractory period, it doesn't go through.

Front 63

How do BB help with acute panic attacks?

Back 63

BB sometimes used in performance anxiety. BB do not help the cause of the anxiety ut do help the sympathetic symptoms.

Front 64

How do BB help benign essential tumor?

Back 64

Benign essential tremors are due to overactivation of Beta2 receptors. BB help block this effect.

Front 65

What were two contraindications of BB when they were first developed?

Back 65

1. Hypertension
2. CHF

Front 66

How do BB help with CHF?

Back 66

The three year mortality rate for CHF is 40-50%. In a normal person, BB will decrease CO, increase TPR, and increase HR. In HF with impaired ventricular function, BB increase CO, decrease TPR, and decrease HR.

Front 67

What is the caution with giving BB for CHF?

Back 67

Patient has to be started on a very low dose and increased slowly due to the symptoms initially worsening when first starting BB.

Front 68

What are the top four BB used in CHF?

Back 68

1. Carvedilol
2. Metoprolol
3. Bisoprolol
4. Nebivolol

Front 69

What are seven possible adverse effects from BB?

Back 69

1. Bronchoconstriction
2. Cardio-depressive Actions
3. Disturbed Glucose Metabolism
4. Impaired Peripheral Circulation
5. Sudden Withdrawal Syndrome
6. CNS Effects
7. Elevated Triglycerides

Front 70

What types of patients would be contraindicated for BB because of possible bronchoconstriction?

Back 70

Asthma patients could have exacerbation if put on BB, and rescue inhalers wouldn't work. Also a third of COPD patients have bronchospasm, so BB would be contraindicated for them. The bronchoconstriction is less likely with Beta1 selective agents, but not completely unlikely.

Front 71

Why do BB have possible Cardio-Depressive Actions?

Back 71

The decreased force of contraction and decreased heart rate due to BB can lead to fatigue and CHF. If the heart rate is slowed down too much (<60 beats/min), patient can develop ectopic pacemakers and may not be able to pump enough blood to meet needs of body. BB can also create heart block.

Front 72

How do BB disturb glucose metabolism in Type I diabetics?

Back 72

In Type I diabetics, BB decrease glucose metabolism. EPI will try and make glucose, but won't have enough insulin to use it. If patient is on BB, have to titrate insulin doses very carefully because BB inhibit glycogenolysis, prolong hypoglycemia, and can mask the symptoms of hypoglycemia.

Front 73

How do BB disturb glucose metabolism in Type II diabetics?

Back 73

In Typer II diabetics, BB decrease insulin which can increase the amount of glucose in the blood. This makes the glucose levels difficult to control. BB mask any symptoms of glucose disturbance.

Front 74

Are there any BB that are good for diabetics?

Back 74

If BB has to be used in a diabetic, Beta1 selective BB should be chosen. Some evidence that 3rd generation agents increase insulin sensitivity in Type II diabetics

Front 75

How do BB contribute to Impaired Peripheral Circulation?

Back 75

There are Beta2 receptors in blood vessels that normally relax the BV. BB can cause cold extremities (Raynaud's Phenomenon) and skeletal muscle fatigue. Peripheral artery disease can result. Intermittent claudication and vasospasms in the arteries.

Front 76

What are some CNS effects of BB?

Back 76

Depression, nightmares, vivid dreams, hallucinations, and fatigue are some CNS effects that can result from BB.

Front 77

What kind of BB cause this effect?

Back 77

Highly lipid soluble agents

Front 78

True/False: A patient can abruptly stop their BB.

Back 78

FALSE!

A patient should never be withdrawn suddenly because this can result in rebound angina, MI, increase in BP, and even death. The BB cause upregulation of receptors, so patients have to be slowly withdrawn.

Front 79

Which element(s) of a patient's lipid profile can be affected by BB?

Back 79

Nonselective BB can decrease HDL but increase LDL and TG. 3rd generation BB improve lipid profile slightly.

Front 80

Which drugs do BB have interactions with?

Back 80

Calcium Channel Blockers (Verapamil and Diltiazem) and Clonidine

Front 81

What interaction do BB have with Calcium Channel Blockers?

Back 81

Synergistic effects to decrease blood pressure, decrease heart rate, and decrease contractility. If used in combination, need lower doses of each.

Front 82

What interaction do BB have with Clonidine?

Back 82

Clonidine is a Alpha2 agonist. Clonidine combined with BB results in a big decrease in BP. Abrupt Clonidine withdrawal will cause enormous spike in BP.