Beta Blockers and Vasodilators

Question 1

Two water soluble BB’s? What is unique about their pharmacokinetics?

Answer 1

• Atenolol, nadolol
• long half-lives
• metabolized by the kidney

Question 2

How is esmolol metabolized?

Answer 2

plasma esterases (10 min half life)

Question 3

Where are B2 receptors found?

Answer 3

vascular and bronchial smooth muscle

Question 4

Which generation of BB’s is non-selective and vasodilatory?

Answer 4

3rd

Question 5

Two ways 3rd gen BB’s assert vasodilation and associated drugs?

Answer 5

• direct via NO (carvedilol, nebivolol)

- indirect via alpha blockade (carvedilol, labetalol)

Question 6

7 functions of carvedilol?

Answer 6

• non-selective BB
• alpha blocker
• calcium blocker
• NO
• anti-oxidant
• anti-proliferative
• blocks expression of genes involved in myocardial damage

Question 7

Four classes of oral meds proven in RCT’s to reduce CV M&M?

Answer 7

• BB’s
• ACEI’s
• statins
• anti-platelets

Question 8

3 typical functions of the B1 blockade?

Answer 8

• neg inotropism
• neg chronotropsim
• blocked renin secretion (regulated by B1R)

Question 9

Two typical AE’s specific to non-selective BB’s?

Answer 9

• bronchoconstriction

- exacerbation of PVD

Question 10

Three typical AE’s associated with all BB’s?

Answer 10

• sedation, fatigue, mental impairment
• hypotension and bradycardia
• inc tri’s and dec HDL

Question 11

What 5 conditions can BB’s be used to treat?

Answer 11

• HF
• post-MI
• SVT
• ischemic HD
• HTN

Question 12

Why should BB’s be used with cautious in diabetic patients?

Answer 12

• catecholamines utilize B2R to promote glycogenolysis and mobilize Glc
• block of this receptor may induce or exacerbate hypoglycemia (and mask tacky associated with hypoglycemia)

Question 13

6 contraindications for BB Tx?

Answer 13

• severe brady
• high grade AVB
• cardiogenic shock (LVF)
• severe bronchospasm
• severe depression
• symptomatic PVD

Question 14

In HF, what state should you make sure the patient is in before Rx’ing BB’s?

Answer 14

hemodynamically stable

Question 15

What molecule does eNOS used to make NO?

Answer 15

L-arginine –> citrulline + NO

Question 16

How are lipid soluble BB’s metabolized?

Answer 16

• hepatic – first-pass effect and variable bioavailability
• shorter 1/2 life but distributed in the fat
• cross BBB – CNS effects

Question 17

Which BB has intrinsic sympathomimetic activity?

Answer 17

Pindolol (used in anxiety)

Question 18

What two BB’s possess alpha blocking activity?

Answer 18

• carvedilol

- labetalol

Question 19

Which BB is good to used in bad ED cases and why?

Answer 19

Nebivolol because it potentiates NO (inc L-arginine)

Question 20

Name two classic, non-selective 1st gen BB’s:

Answer 20

• nadolol

- propranolol

Question 21

Name three B1 selective, 2nd gen BB’s:

Answer 21

• atenolol
• esmolol
• metoprolol

Question 22

Name two non-selective BB’s with additional actions (3rd gen):

Answer 22

• carvedilol

- labetalol

Question 23

Name one B1 selective BB with additional actions (3rd gen):

Answer 23

• nebivolol (NO potentiation)

Question 24

B1 selective BB’s? = MANE

Answer 24

metoprolol, atenolol, nebivolol, esmolol

Question 25

Which two lipid-soluble BB's are metabolize by CYP2D6?

Answer 25

metoprolol and carvedilol

Question 26

Which non-selective BB has an extremely long half life?

Answer 26

nadolol (water soluble) - 24 hours

Question 27

What two drug classes are recommended for all patients with prior MI?

Answer 27

BB's and ACEI's

Question 28

What are two calcium channel blockers than act on the vasculature only?

Answer 28

amiodipine and nifedipine

Question 29

What are two venous selective vasodilators?

Answer 29

isosorbide dinitrate, nitroglycerin = organic nitrates

Question 30

What group of vasodilators block hypertrophic growth responses?

Answer 30

RAAS interfering drugs - aliskerin, lisinopril, losartan

Question 31

What are two indications for CCB tx? Additional indication with non-dihydropyridine CCB's?

Answer 31

- ischemic HD, HTN | - SVT (nodal)

Question 32

What are two organic nitrates that are metabolized to NO?

Answer 32

nitroglycerin and isosorbide dinitrate

Question 33

Primary indication for use of organic nitrates?

Answer 33

ischemic HD (some use in HF)

Question 34

Why does nitroglycerin have such a short half-life? Indication?

Answer 34

- hepatic metabolism (can be lengthened by creams, patches to avoid first-pass effect) - rapid relief of angina pectoris

Question 35

NG vs. isosorbide dinitrate?

Answer 35

ID has a longer plasma half life and can additionally be used to Tx HF

Question 36

Which vasodilator contains CN?

Answer 36

sodium nitroprusside

Question 37

Two main indications for balanced vasodilator (short half-life) drug sodium nitroprusside?

Answer 37

- rapid reduction of BP in HTN crisis | - rapid decrease in preload and after load due to venous and arterial effects --> effective in Tx decompensated CHF

Question 38

Mechanism of action and target vessels of Minoxidil?

Answer 38

- arterial vasodilator | - stimulates an outward K+ channel resulting in hyper polarization of vascular smooth muscle cell

Question 39

What is Minoxidil reserved for? Novel indication?

Answer 39

- Tx of moderate to severe HTN | - hair growth = Rogaine

Question 40

What are two balanced vasodilators?

Answer 40

Terazosin (alpha antagonist) and sodium nitroprusside (organic nitrate)

Question 41

What vessels are relaxed by hydralazine? Two uses of the drug?

Answer 41

- arteries - second line anti-HTN - HF in combination with isosorbide dinitrate (dec in pre-load AND after-load with combination - very strong response in African Americans)

Question 42

What enzyme is inhibited by milrinone?

Answer 42

PDE3 in heart and BV's

Question 43

Outcome of inhibition of cardiac PDE vs. vascular smooth muscle PDE?

Answer 43

- increased force of contraction and cardiac output = positive isotropism (inc calcium etc) - vasodilation