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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
Which medication inhibits Propranolol, and which three medications induce Propranolol? What is the ultimate effect of each?
Inhibit: Cimetidine - Increases toxicity (drug remains in system for longer) Induce: Barbiturates, Phenytoin, Rifampin - Less effective (drug cleared before it can work)
26
What are the five primary AEs associated with Propranolol?
- Bronchoconstriction in asthmatics - Exacerbate HF if late stages - Bradycardia - Sedation/fatigue - Difficult recovery from hypoglycemia
27
What are the six primary CIs associated with Propranolol?
- Acute HF - Asthma - AV block - Bradycardia - Cariogenic shock - Pheochromocytoma
28
In what two populations should Propranolol use be cautioned?
- DM | - COPD
29
What is the primary use of Timolol (Timoptic)?
Glaucoma (topical)
30
What is the primary CI associated with Timolol (Timoptic)?
Asthmatics (some systemic absorption)
31
Which medication is similar to Timolol (Timoptic) but often preferred, and why?
Betaxolol (Betoptic) is also used to treat glaucoma (topical) - Better than Timolol because more specific
32
What is the primary use of Betaxolol (Betoptic)?
Glaucoma | - Preferred because more specific than Timolol (Timoptic)
33
What are the four primary uses of Metoprolol?
HEART - HTN - Post-MI - Angina - HF
34
What medication is similar to Propranolol but sometimes preferred, and why (3)?
Metoprolol - Safer in DM - Safer in asthmatics - Better exercise tolerance
35
What are the three primary AEs associated with Metoprolol?
- Dizziness - Bradycardia - Hypotension
36
What is the primary action of Nebivolol, and how does this effect its use?
Causes NO release from endothelial cells = direct vasodilator
37
For which population is Nebivolol the best option, and why?
Asthmatics (acts as a direct vasodilator) | - Most specific B1 Blocker so fewest side effects
38
Which medication is the most specific B1 Blocker?
Nebivolol
39
What are two important PKs associated with Esmolol (Brevibloc)?
- IV only | - Short half-life
40
What are the four primary uses associated with Esmolol (Brevibloc)?
- Ill patient with HF - Ill patient with bradycardia - Ill patient with hypotension - Arrhythmia (emergency)
41
Why is Esmolol (Brevibloc) preferred for ill patients?
It has a short half life and you don't want a medication with lasting B Blocker effects
42
What is the primary use of Labetalol, and in what population is it often specifically used?
Decrease BP in HTN emergency | - Especially in pregnant women
43
What is the primary AE associated with Labetalol, specifically?
Hepatotoxicity
44
What are the two primary uses of Carvedilol (Coreg), and with what population/condition is it specifically used?
Post-MI for... - HTN - HF
45
What is the primary AE associated with both Labetalol and Carvedilol (Coreg)?
Bronchoconstriction
46
What is the primary CI associated with both Labetalol and Carvedilol (Coreg)?
Asthmatics
47
What type of receptors do Labetalol and Carvedilol (Coreg) act on?
BLOCK combined A1 and B1
48
What naming system is specific to B Blockers?
"-olol"
49
What naming system is specific to combined A1 and B1 Blockers?
Other "-lol" aka "-alol" and "-ilol"
50
What is the first line treatment option for Glaucoma, and what is its action?
Prostaglandin analogues | - Increase fluid outflow
51
What is the second line treatment for Glaucoma, and what is its action? What are the two medications we discussed specifically?
B Blockers - Decrease fluid production Betaxolol (Betoptic) and Timolol (Timoptic)
52
What is the third line treatment for Glaucoma, and what is its action?
A2 Agonists | - Increase fluid outflow AND decrease fluid production
53
What are the top three Glaucoma treatment options in order?
1. Prostaglandin analogues 2. B Blockers (Betaxolol (Betoptic) and Timolol (Timoptic)) 3. A2 Agonists

Pharmacology II (20 decks)

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