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Pharmacology II > L4 Adrenergic Blockers (Exam #1) > Flashcards

L4 Adrenergic Blockers (Exam #1) Flashcards

1
Q

What is the one irreversible A Blocker agent, and what does being “irreversible” mean?

A

Phenoxybenzamine

- As dose increases, curve shifts right but will never meet a maximum/100% effect (less of an effect)

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2
Q

What are the four primary CV effects caused by A Blockers?

A
  • Decrease vasoconstriction (decrease BP)
  • Reflex tachycardia (increase HR to compensate for decrease BP)
  • Orthostatic hypotension (decrease BP)
  • Epi reversal (decrease BP but expose B receptors so HR increases)
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3
Q

What are four other effects caused by A Blockers (non CV)?

A
  • Miosis
  • Nasal stuffiness
  • Increased urination
  • Ejaculation inhibition
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4
Q

What is the primary role of A Blockers? What is the primary role of B Blockers?

A
  • A Blockers: decrease BP

- B Blockers: decrease HR

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5
Q

Of the two A Blockers, which is competitive and which is irreversible?

A
  • Competitive (reversible): Phentolamine

- Irreversible: Phenoxybenzamine

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6
Q

What is the primary use of Phentolamine?

A

Decrease BP in HTN crisis (RARELY used)

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7
Q

What are the four primary AEs associated with Phentolamine?

A
  • Hypotension
  • Tachycardia
  • Arrhythmias
  • MI
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8
Q

What is Phenoxybenzamine the DOC for?

A

Prevent severe HTN in patients with pheochromocytoma

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9
Q

What are the three primary AEs associated with Phenoxybenzamine?

A
  • Hypotension
  • Tachycardia
  • Ejaculation inhibition
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10
Q

What type of receptors do Phentolamine and Phenoxybenzamine act on?

A

BLOCK A (A1 = A2)

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11
Q

What are the two primary uses of Prazosin (Minipress)? In what population is it ideal for?

A

Perfect for men with HTN AND BPH

  • HTN
  • BPH
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12
Q

What are the two primary AEs associated with Prazosin (Minipress)?

A
  • Orthostatic hypotension (1st dose phenomenon)

- Reflex tachycardia

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13
Q

What two drugs are contraindicated in combination with Prazosin (Minipress)?

A
  • ED

- Nitrates

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14
Q

What drug is associated with 1st dose phenomenon, and what does this mean?

A

Prazosin (Minipress)

- Sudden/severe orthostatic hypotension the first time the drug is used, or when resuming the drug after many months off

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15
Q

What is the primary use of Tamsulosin (Flomax), and how does this relate to the receptor it is more selective for?

A

BPH

- A1A (prostate) more than A1B (blood vessels)

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16
Q

What are the three primary AEs associated with Tamsulosin (Flomax)?

A
  • ED
  • HA
  • Dizziness
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17
Q

What type of receptors do Prazosin (Minipress) and Tamsulosin (Flomax) act on?

A

BLOCK A1

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18
Q

What are the five primary CV effects caused by B Blockers?

A
  • Decrease HR
  • Decrease contractility
  • Decrease renin
  • Decrease O2 demand of heart
  • Decrease BP (IF CHRONIC USE)
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19
Q

What are four other effects caused by B Blockers (non CV)?

A
  • Bronchoconstriction
  • Decrease IOP
  • Inhibit glycogenolysis
  • Inhibit insulin secretion
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20
Q

On what system should B Blockers never be used, and why?

A

EYES

- Local anesthetic and abrasions

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21
Q

What type of receptors do Propranolol and Timolol (Timoptic) act on?

A

BLOCK B (B1 = B2)

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22
Q

In what two conditions does Propranolol reduce mortality?

A
  • Post-MI

- End-stage HF

23
Q

What are the eight primary uses of Propranolol?

A
  • Post- MI (reduce mortality)
  • End-stage HF (reduce mortality)
  • Increase exercise intolerance
  • Treat arrhythmias
  • Hyperthyroidism
  • Migraine prevention
  • Catecholamine-induced tremor/”stage fright”
  • Reduce BP with chronic use
24
Q

What are two important PKs associated with Propranolol?

A
  • Metabolized by CYP450s

- Do NOT stop abruptly

25
Q

Which medication inhibits Propranolol, and which three medications induce Propranolol? What is the ultimate effect of each?

A

Inhibit: Cimetidine
- Increases toxicity (drug remains in system for longer)

Induce: Barbiturates, Phenytoin, Rifampin
- Less effective (drug cleared before it can work)

26
Q

What are the five primary AEs associated with Propranolol?

A
  • Bronchoconstriction in asthmatics
  • Exacerbate HF if late stages
  • Bradycardia
  • Sedation/fatigue
  • Difficult recovery from hypoglycemia
27
Q

What are the six primary CIs associated with Propranolol?

A
  • Acute HF
  • Asthma
  • AV block
  • Bradycardia
  • Cariogenic shock
  • Pheochromocytoma
28
Q

In what two populations should Propranolol use be cautioned?

A
  • DM

- COPD

29
Q

What is the primary use of Timolol (Timoptic)?

A

Glaucoma (topical)

30
Q

What is the primary CI associated with Timolol (Timoptic)?

A

Asthmatics (some systemic absorption)

31
Q

Which medication is similar to Timolol (Timoptic) but often preferred, and why?

A

Betaxolol (Betoptic) is also used to treat glaucoma (topical)
- Better than Timolol because more specific

32
Q

What is the primary use of Betaxolol (Betoptic)?

A

Glaucoma

- Preferred because more specific than Timolol (Timoptic)

33
Q

What are the four primary uses of Metoprolol?

A

HEART

  • HTN
  • Post-MI
  • Angina
  • HF
34
Q

What medication is similar to Propranolol but sometimes preferred, and why (3)?

A

Metoprolol

  • Safer in DM
  • Safer in asthmatics
  • Better exercise tolerance
35
Q

What are the three primary AEs associated with Metoprolol?

A
  • Dizziness
  • Bradycardia
  • Hypotension
36
Q

What is the primary action of Nebivolol, and how does this effect its use?

A

Causes NO release from endothelial cells = direct vasodilator

37
Q

For which population is Nebivolol the best option, and why?

A

Asthmatics (acts as a direct vasodilator)

- Most specific B1 Blocker so fewest side effects

38
Q

Which medication is the most specific B1 Blocker?

A

Nebivolol

39
Q

What are two important PKs associated with Esmolol (Brevibloc)?

A
  • IV only

- Short half-life

40
Q

What are the four primary uses associated with Esmolol (Brevibloc)?

A
  • Ill patient with HF
  • Ill patient with bradycardia
  • Ill patient with hypotension
  • Arrhythmia (emergency)
41
Q

Why is Esmolol (Brevibloc) preferred for ill patients?

A

It has a short half life and you don’t want a medication with lasting B Blocker effects

42
Q

What is the primary use of Labetalol, and in what population is it often specifically used?

A

Decrease BP in HTN emergency

- Especially in pregnant women

43
Q

What is the primary AE associated with Labetalol, specifically?

A

Hepatotoxicity

44
Q

What are the two primary uses of Carvedilol (Coreg), and with what population/condition is it specifically used?

A

Post-MI for…

  • HTN
  • HF
45
Q

What is the primary AE associated with both Labetalol and Carvedilol (Coreg)?

A

Bronchoconstriction

46
Q

What is the primary CI associated with both Labetalol and Carvedilol (Coreg)?

A

Asthmatics

47
Q

What type of receptors do Labetalol and Carvedilol (Coreg) act on?

A

BLOCK combined A1 and B1

48
Q

What naming system is specific to B Blockers?

A

“-olol”

49
Q

What naming system is specific to combined A1 and B1 Blockers?

A

Other “-lol” aka “-alol” and “-ilol”

50
Q

What is the first line treatment option for Glaucoma, and what is its action?

A

Prostaglandin analogues

- Increase fluid outflow

51
Q

What is the second line treatment for Glaucoma, and what is its action? What are the two medications we discussed specifically?

A

B Blockers
- Decrease fluid production

Betaxolol (Betoptic) and Timolol (Timoptic)

52
Q

What is the third line treatment for Glaucoma, and what is its action?

A

A2 Agonists

- Increase fluid outflow AND decrease fluid production

53
Q

What are the top three Glaucoma treatment options in order?

A
  1. Prostaglandin analogues
  2. B Blockers (Betaxolol (Betoptic) and Timolol (Timoptic))
  3. A2 Agonists

Pharmacology II (20 decks)

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