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RENAL II EXAM 1 > Adrenergic Blockers - SRS > Flashcards

Adrenergic Blockers - SRS Flashcards

1
Q

What are some non-selective alpha adrenoceptor blocking agents?

(2)

A

Phenoxybenzamine

Phentolamine

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2
Q

What are the alpha-one selective adrenergic blocking agents?

(2 bolded, 4 total)

A

Prazosin

Terazosin

Tamsulosin (a1A)

Doxazosin

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3
Q

What are the non-selective beta blocking agents?

A

Propranolol (Prototype)

Nadolol

Timolol

*Pindolol

*Carteolol

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4
Q

What are the cardioselective beta blocking agents?

(4 all bolded)

A

Atenolol

*Acebutolol

Metoprolol

Betaxolol

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5
Q

What is a short acting beta blocking agent? When is it useful?

A

Esmolol - useful in surgery

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6
Q

What are two drugs that target both alpha and beta blockers?

(2 both bold)

A

Labetalol

Carvedilol

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7
Q

Describe the binding activity of phenoxybenzamine!

A

Irreversible to a1 & a2

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8
Q

Desccribe the binding of phentolamine

A

prototype reversible Alpha 1 and 2 blocker

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9
Q

Characterize the targeting of prazosin?

A

selective alpha 1 blocker

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10
Q

Characterize tamsulosins targeting!

A

selective alpha1A blocker

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11
Q

What type of pharmacodynamics does phenoxybenzamene have?

A

noncompetitive

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12
Q

What kind of pharmacodynamics does phentolamine have?

A

Competitive, reversible

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13
Q

Alpha blockers are antagonists, describe their intrinsic activity!

A

They have no intrinsic activity (haha), but do produce pharmacological changes.

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14
Q

Phenoxybenzamine (dibenzyline) binds covalently to alpha 1 and alpha 2 receptors. How is its effect terminated?

A

By metabolism and new receptor synthesis

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15
Q

What alpha blocker might be shown here?

A

Phenoxybenzamine

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16
Q

What impact does phenoxybenzamine have on vasculature? What is a related significant side effect?

A

Dependent on the degree of sympathetic tone. i.e., blocks the effects of endogenous NE. Reduces blood pressure. Significant side effect is Orthostatic hypotension.

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17
Q

What is the effect of phenoxybenzamine on the cardiac system?

A

Reflex tachycardia from reducing BP, which enhances NE release. Because alpha-2 receptors on adrenergic nerves are also blocked, this further increases NE release at the heart, where it can act on beta-1 receptors.

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18
Q

What is the effect of phenoxy benzamine on the CNS?

A

lipophilic agent which can cross the blood brain barrier. Nausea, vomiting and weakness may be signs of non-specific effects.

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19
Q

In what cases might one prescribe phenoxybenzamine?

A
  1. Pheochromocytoma: Pre-operative management to treat vascular effects of high circulating catecholamines. Always in combination with a beta blocker.
  2. Peripheral Vascular Disease. Raynaud’s syndrome where sympathetic tone to peripheral vasculature is high. Acrocyanosis from frost bite.
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20
Q

Phentolamine and tolazoline are non-selective for alpha 1 and 2 receptors. What other receptor are they known to activate, causing adverse effects?

A

Histamine

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21
Q

Name four things phentolamine is used for clinically! (one no longer)

A
  1. Pheochromocytoma. Acute hypertensive crisis.
  2. Clonidine withdrawal
  3. Treat necrosis due to vasoconstrictors such as NE and phenylephrine.
  4. For erectile dysfunction (ED) – has been replaced by drugs with less severe side-effects.
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22
Q

What side effects would you expect from phentolamine? (4)

A

tachycardia

nausea

diarrhea

orthostatic hypotension

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23
Q

Alpha-1 selective blockers cause less reflex tachycardia than non-selectives, and you may see syncope. Agents include prazosin, terazosin, doxazosin. What are 2 uses for these drugs?

A

Hypertension

benign prostatic hypertrophy

24
Q

Discuss how tamsulosin binds alpha-1 subtypes.

What are the effects it causes via each?

A

Competitive alpha blocker; binds alpha1A with little alpha1B binding

alpha1B - Very limited vascular effects, but alpha1A highly efficacious in benign prostatic hyperplasia (BPH).

25
Q

What is the prototype nonselective beta receptor antagonist?

A

Propranolol

26
Q

What are the drugs that are “like” propranolol?

A

Timolol

Pindolol

Nadolol

27
Q

What is the prototype cardioselective B blocker?

A

Atenolol

28
Q

What are the drugs that are “like” atenolol?

A

Acebutolol

Metoprolol

29
Q

Is propranolol lipid soluble?

A

Highly lipid solubility - will see some drowsiness

30
Q

What effect does propranolol have on the heart?

A

Decreases HR, cardiac output, and pacemaker activity

31
Q

What does propranolol do to the blood vessels?

A

Slow developing decrease in peripheral resistance. Possibly due to: central reduction in sympathetic tone and reduction in renin release (beta-1 effect)

32
Q

What does propranolol do in the lungs? Any problems here?

A

Bronchial Smooth Muscle

  • Block sympathomimetic bronchodilation
  • precaution or contraindication in asthma & COPD
33
Q

What are the metabolic effects of propranolol? Anything to keep in mind here?

A
  • Blocks beta receptor effects on lipolysis and glycogenolysis.
  • May mask signs of hypoglycemia, e.g., tachycardia, BP changes. May potentiate insulin-induced hypoglycemia.
34
Q

Propranolol has a quinidine-like effect, what is it?

A

“Membrane stabilizing activity”, decreased cardiac excitability

35
Q

Propranolol is well absorbed on oral admin. to what degree is it impacted by first pass metabolism?

A

75% may be inactivated. (highly variable), must titrate the dose upward for each individual.

36
Q

Name 9 clinical applications of B blockers!

A
  1. Angina pectoris
  2. HTN
  3. Migraine headache
  4. Arrhytmias
  5. pheochromocytoma
  6. thyrotoxicosis
  7. adjuctive treatment for anxiety (panic) attacks
  8. MI and post MI phrophylaxis
  9. CHF
37
Q

Why do B blockers help with angina pectoris?

A

decrease cardiac work and O2 consumption

38
Q

What do B blockers do to help with HTN?

A

Decrease CO

Slow decrease in peripheral resistance due to blockade of renin release.

39
Q

What are some arrythmias that B blockers are used for?

A

Sinus tachycardia and supraventricular ectopic beat.

40
Q

Why are beta blockers used in thyrotoxicosis?

A

Hyperthyroid patients have increased B receptor sensitivity

41
Q

How do beta blockers help with MI and post-MI prophylaxis?

A

protects against arrhythmias & limits infarct size
5-12 days after MI, reduces O2 demand & spread of infarct zone

42
Q

Beta blockers have been shown to have dramatic results in CHF patients, with mortality reductions of 65%, 34% and 33% for carvedilol, metoprolol and bisoprolol, respectively. Prevent heart failure in 50% and decrease risk of stroke by 38%. What do they do to make this possible?

A

Beta blockers increase LVEF,

cause beneficial remodeling of heart

43
Q

What are side effects associated with propranolol?

(7 common, plus 3 severe)

A

Common:

  1. dizziness
  2. fatigue
  3. diarrhea
  4. constipation
  5. nausea
  6. depression
  7. bizarre dreams

Severe

  1. purpura
  2. rash
  3. fever
44
Q

Propranolol interferes with SGOT and BUN tests, and chronic use for HTN can lead to what?

A

Increased ­VLDL & HDL

45
Q

Why must you use caution in providing B blockers to diabetics?

A

Ininhibits compensatory response to hypoglycemia (glycogenolysis with glucose release) masks signs of hypoglycemia (tachycardia) that are important “clues” to diabetic patient

46
Q

Why are B blockers contraindicated in patients with most asthmatics and COPD

A

Blocks B2 bronchodilation

47
Q

What can happen if a patient abruptly discontinues B blockers? Explain why this happens.

A

rebound hypertension, anginal attack & possibly MI if drug suddenly withdrawn after chronic therapy.

Because Beta receptor synthesis is increased by beta blocker use. Example of receptor up-regulation.

48
Q

What are some noteable contraindications for B blockers?

A

Acute treatment of decompensated heart failure

2nd and 3rd degree heart block

cardiogenic shock

49
Q

As you’ve seen mentioned a couple times, B blockers can be used for glaucoma, which one would be best? How does it do this?

A

Timolol

reduces aqueous humor production

50
Q

What is metoprolol selective for?

A

B1 receptors. At high dose can block B2 though

51
Q

What are two common uses for metoprolol?

A

HTN and CHF

52
Q

Are B1 selective blockers contraindicated in asthmatics?

A

Yes, d/t potential at higher doses to block B2

53
Q

Esmolol is selective for what?

A

B1

54
Q

Under what circumstances is Esmolol useful?

A
  • Used as IV infusion for peri-operative tachycardia and hypertension, arrhythmias
  • Used in electroconvulsive therapy
55
Q

What receptors does labetolol target?

A

Selective a 1 blocker
Nonselective b1 & b2 blocker

56
Q

Carvedilol is a blocker of?

A

Nonselective b-blocker and a-blocker

57
Q

Is carvedilol lipid soluble?

A

Yes

RENAL II EXAM 1 (8 decks)

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