Section 2c Adrenergic Antagonists

Question 1

2 reversible alpha antagonists

Answer 1

phentolamine and prazosin

Question 2

an irreversible alpha antagonist

Answer 2

phenoxybenzamine

Question 3

2 drugs that are non-selective alpha antagonists

Answer 3

phentolamine and phenoxybenzamine

Question 4

8 drugs that are a1-selective antagonists

Answer 4

prazosin, terazosin, doxazosin, tamsulosin <– more important
less important = alfuzosin, indoramin, urapidil, and bunazosin

Question 5

2 drugs that are a2-selective antagonists

Answer 5

yohimbine and mirtazapine

Question 6

Will a healthy person given an alpha-adrenoceptor antagonist show effects?

Answer 6

not much, if at all

Question 7

What is Pheochromocytoma

Answer 7

tumor of the adrenal medulla releasing catecholamines

Question 8

If a person has Pheochromocytoma what would you recommend about phenoxybenzamine and phentolamine?

Answer 8

phenoxybenzamine = pre-operative period
phentolamine = short-term control of HTN

Question 9

What do you use to fix a-agonist problems?

Answer 9

Phentolamine

Question 10

What are the Adverse effects of non-selective alpha antagonists?

Answer 10

nasal stuffiness, orthostatic hypotension, tachycardia

Question 11

What would you recommend first-dose users to do with selective a1-atagonistic drugs?

Answer 11

The smaller dose should be taken just before bedtime to avoid postural hypotension and syncope

Question 12

What could selective a1-antagonists be used for? and which one has a longer half-life?

Answer 12

1. HTN, BPH, Raynaud’s syndrome, PTSD

2. doxazosin (22hrs)

Question 13

What does Tamsulosin do?

Answer 13

a1A - antagonist: selective for prostate smooth muscle

Question 14

What are 2 B+a-antagonistic drugs?

Answer 14

Labetalol (has 4 stereoisomers) and Carvedilol

Question 15

What is Yohimbine used for?

Answer 15

orthostatic hypotension and ED

Question 16

What is Mirtazapine used for?

Adverse effects?

Answer 16

1. MDD (it can work in the CNS)

2. Adverse effects: arrhythmias (QT prolongation), drowsiness, suicide

Question 17

3 drugs that are non-selective B - antagonists

Answer 17

propranolol (competitive), nadolol (longest 1/2 life - 12-24hrs), timolol

Question 18

5 drugs that are B1 - selective antagonists

Answer 18

atenolol, esmolol (short 1/2 life use only IV), metoprolol, acebutolol, bisoprolol

Question 19

Butoxamine is only used in research… what is its MOA?

Answer 19

B2 - selective antagonist

Question 20

What are Beta partial agonists? (ISA - intrinsic sympathomimetic activity)

Answer 20

pindolol and acebutolol

Question 21

What Beta antagonists are used as a local anesthetic? (membrane-stabilizing activity)

Answer 21

acebutolol, pindolol, and propranolol

Question 22

What is the MOA for Nebivolol?

Answer 22

B blocker + NO production (vasodilator)

Question 23

Propranolol is used to treat HTN, what 2 things could it also do that could be contradictory to health?

Answer 23

B2 effects: broncho-constriction & reflex peripheral vaso-constriction

Question 24

What B-blockers are used for Glaucoma? (4)

Answer 24

timolol - topical

betaxolol, carteolol, levobunolol - oral?

Question 25

What is Propranolol also used for besides BP? (3)

Answer 25

migraines, tremors, anxiety (stage fright)

Question 26

What are other uses of Beta - antagonists in general? (4)

Answer 26

Ischemic heart disease (angina pectoris), cardiac arrhythmias, hyperthyroidism (thyrotoxicosis - tachycardia control), and prophylaxis of variceal (esophageal) hemorrahage [Nadolol]

Question 27

What Beta - antagonists are select agents for HF?

Answer 27

metoprolol, bisoprolol (B1), and carvedilol (B, a1)

Question 28

What drug do all Beta blockers interact with?

Answer 28

verapamil = hypotension, bradycardia, HF

Question 29

What are possible outcomes of abrupt discontinuation of a B blocker?

Answer 29

high risk of cardiac ischemia and/or arrhythmias