adrenergic antagonists Flashcards

1
Q

how does prazosin work?

A

blocks a1 receptor on arterioles and veins, inhibiting NE

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2
Q

how is prazosin given?

A

oral or transdermal

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3
Q

where is prazosin metabolized?

A

liver

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4
Q

prazosin toxicity/interactions

A

hypotension - especially when combined with diuretics

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5
Q

name three adrenergic antagonists selective for a1

A
  • prazosin
  • tamsulosin
  • doxazosin
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6
Q

name an adrenergic antagonist selective for a2

A

yohimbine

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7
Q

name two adrenergic antagonists selective for b1

A
  • atenolol

- metoprolol

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8
Q

name an adrenergic antagonist selective for b2

A

butoxamine

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9
Q

name two adrenergic antagonists selective for a1 and a2

A
  • phentolamine

- phenoxybenzamine

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10
Q

name two adrenergic antagonists selective for b1 and b2

A
  • propranolol

- nadolol

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11
Q

name an adrenergic antagonist that can inhibit alpha and beta

A

labetalol

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12
Q

how does tamulosin work?

A

selectively blocks a1, but preferentially in prostate, relaxation of smooth muscle and improvement of urine flow, reducing obstructive effects of benign prostatic hyperplasia

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13
Q

how is tamulosin metabolized?

A

CYP 450 enzymes

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14
Q

tamulosin half life

A

6 hours, full life up to 15 hours due to slow absorption

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15
Q

tamulosin interactions

A
  • additive with diuretics
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16
Q

special considerations with tamulosin

A
  • rule out prostate cancer first
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17
Q

why prescribe tamulosin?

A

symptoms of BPH

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18
Q

how does phentolamine work?

A

blocks a1 and a2, decreases preload and after load

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19
Q

how take phentolamine?

A

IV only

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20
Q

phentolamine toxicity?

A
  • hypotension

- syncope

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21
Q

phentolamine interactions

A
  • antihypertensives, particularly diuretics
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22
Q

phentolamine indications

A
  • Dx of pheo
  • prevention of dermal sloughing after extravasation of NE infusion
  • treat hypertension due to sympathomimetic amines
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23
Q

how does atenolol work?

A

binds directly to b1 receptors, lowers blood pressure

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24
Q

how take atenolol?

A

oral or IV

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25
Q

atenolol toxicity?

A
  • hypotension
  • bradycardia
  • can worsen severe CHF or asthma
26
Q

atenolol interactions

A
  • additive with most antihypertensives

- additive AV block with CEB’s

27
Q

special considerations for atenolol

A
  • useful with hypertensive patient with exertional angina, MI, a-fib,
28
Q

indications for atenolol

A

hypertension

29
Q

how does propranolol work?

A

binds directly to b1 and b2, lowers blood pressure

30
Q

half lives and metabolism of beta blockers

A

metoprolol - liver metabolism, shorter half life

atenolol and propranolol - renal excretion, longer half life

31
Q

how take propranolol?

A

IV or oral

32
Q

propranolol interactions

A
  • additive with antihypertensives
33
Q

propranolol indications

A

hypertension

34
Q

how does labetolol work?

A

blocks NE from getting to alpha and beta receptors, lowers BP

35
Q

labetolol metabolism

A

by liver IID6

36
Q

how take labetolol?

A

IV bolus followed by continuous infusion

there are also oral tablets

37
Q

labetolol indications

A

hypertension

38
Q

phentolamine half life

A

19 minutes, very short

39
Q

phentolamine metabolism

A

hepatic

40
Q

phenoxybenzamine pharmacodynamics

A

irreversibly binds to a1 and a2 receptors

41
Q

phenoxybenzamine indications

A
  • hypertension

- hypoplastic left heart syndrome

42
Q

phenoxybenzamine half life

A

24 hours

43
Q

phenoxybenzamine routes

A

oral

44
Q

labetolol half life

A

6-8 hours oral

5.5 hours IV

45
Q

labetolol excretion/metabolism

A
  • hepatic pass metabolism

- excreted in urine, not removed by hemodialysis

46
Q

labetolol F

A

25%, which is why you need bolus dose

47
Q

sotalol class

A
  • b-blocker

- potassium channel blocker

48
Q

sotalol indications

A
  • hypertension

- cardiac arrhythmias

49
Q

sotalol half life

A

12 hours

50
Q

sotalol 95%

A

high

51
Q

sotalol metabolism/excretion

A

not metabolized

renal excretion

52
Q

metoprolol class

A

b-blocker

53
Q

metoprolol F

A

12%

54
Q

metoprolol half life

A

3-7 hours

55
Q

metoprolol indications

A
  • hypertension
  • angina
  • acute MI
  • v-tach
  • sv-tach
  • CHF
56
Q

metoprolol metabolism/excretion

A
  • hepatic CYP

- renal excretion

57
Q

metropolol is most equivalent to:

A

atenolol

58
Q

carvedilol is most equivalent to:

A

labetalol

59
Q

carvedilol pharmacodynamics

A

non-selective b-blocker and a1 blocker, blocks NE from binding, lowers HR and contractility

60
Q

carvedilol indications

A
  • mild to severe CHF
61
Q

prazosin F and protein binding

A

F 60%, protein binding 97%

62
Q

prazosin half life

A

2-3 hours