Beta Blockers and Vasodilators Flashcards

1
Q

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

A
  • Atenolol, nadolol
  • long half-lives
  • metabolized by the kidney
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2
Q

How is esmolol metabolized?

A

plasma esterases (10 min half life)

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3
Q

Where are B2 receptors found?

A

vascular and bronchial smooth muscle

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4
Q

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

A

3rd

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5
Q

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

A
  • direct via NO (carvedilol, nebivolol)

- indirect via alpha blockade (carvedilol, labetalol)

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6
Q

7 functions of carvedilol?

A
  • non-selective BB
  • alpha blocker
  • calcium blocker
  • NO
  • anti-oxidant
  • anti-proliferative
  • blocks expression of genes involved in myocardial damage
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7
Q

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

A
  • BB’s
  • ACEI’s
  • statins
  • anti-platelets
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8
Q

3 typical functions of the B1 blockade?

A
  • neg inotropism
  • neg chronotropsim
  • blocked renin secretion (regulated by B1R)
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9
Q

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

A
  • bronchoconstriction

- exacerbation of PVD

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10
Q

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

A
  • sedation, fatigue, mental impairment
  • hypotension and bradycardia
  • inc tri’s and dec HDL
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11
Q

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

A
  • HF
  • post-MI
  • SVT
  • ischemic HD
  • HTN
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12
Q

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

A
  • catecholamines utilize B2R to promote glycogenolysis and mobilize Glc
  • block of this receptor may induce or exacerbate hypoglycemia (and mask tacky associated with hypoglycemia)
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13
Q

6 contraindications for BB Tx?

A
  • severe brady
  • high grade AVB
  • cardiogenic shock (LVF)
  • severe bronchospasm
  • severe depression
  • symptomatic PVD
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14
Q

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

A

hemodynamically stable

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15
Q

What molecule does eNOS used to make NO?

A

L-arginine –> citrulline + NO

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16
Q

How are lipid soluble BB’s metabolized?

A
  • hepatic – first-pass effect and variable bioavailability
  • shorter 1/2 life but distributed in the fat
  • cross BBB – CNS effects
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17
Q

Which BB has intrinsic sympathomimetic activity?

A

Pindolol (used in anxiety)

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18
Q

What two BB’s possess alpha blocking activity?

A
  • carvedilol

- labetalol

19
Q

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

A

Nebivolol because it potentiates NO (inc L-arginine)

20
Q

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

A
  • nadolol

- propranolol

21
Q

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

A
  • atenolol
  • esmolol
  • metoprolol
22
Q

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

A
  • carvedilol

- labetalol

23
Q

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

A
  • nebivolol (NO potentiation)
24
Q

B1 selective BB’s? = MANE

A

metoprolol, atenolol, nebivolol, esmolol

25
Q

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

A

metoprolol and carvedilol

26
Q

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

A

nadolol (water soluble) - 24 hours

27
Q

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

A

BB’s and ACEI’s

28
Q

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

A

amiodipine and nifedipine

29
Q

What are two venous selective vasodilators?

A

isosorbide dinitrate, nitroglycerin = organic nitrates

30
Q

What group of vasodilators block hypertrophic growth responses?

A

RAAS interfering drugs - aliskerin, lisinopril, losartan

31
Q

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

A
  • ischemic HD, HTN

- SVT (nodal)

32
Q

What are two organic nitrates that are metabolized to NO?

A

nitroglycerin and isosorbide dinitrate

33
Q

Primary indication for use of organic nitrates?

A

ischemic HD (some use in HF)

34
Q

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

A
  • hepatic metabolism (can be lengthened by creams, patches to avoid first-pass effect)
  • rapid relief of angina pectoris
35
Q

NG vs. isosorbide dinitrate?

A

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

36
Q

Which vasodilator contains CN?

A

sodium nitroprusside

37
Q

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

A
  • 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

38
Q

Mechanism of action and target vessels of Minoxidil?

A
  • arterial vasodilator

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

39
Q

What is Minoxidil reserved for? Novel indication?

A
  • Tx of moderate to severe HTN

- hair growth = Rogaine

40
Q

What are two balanced vasodilators?

A

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

41
Q

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

A
  • 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)
42
Q

What enzyme is inhibited by milrinone?

A

PDE3 in heart and BV’s

43
Q

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

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