Exam 4: Adrenergic Antagonists

Question 1

What is chemical class and USAN stem of a1 antagonist?

Answer 1

Quinazolines and azosin

Question 2

What are examples of selective a1 antagonist?

Answer 2

1. Prozaosin
2. Terazosin
3. Doxazosin
4. Tamsulosin
5. Alfuzosin
6. Silodosin

Question 3

How does a2 antagonist differ from a1?

Answer 3

Can cause mimetic action due to a2 being and autoreceptor

Question 4

What is yohimbine’s characteristics?

Answer 4

1. Not clinically significant
2. Induces hypertension
3. Increases heart heat
4. Male impotence and orthostatic hypotension

Question 5

What are the therapeutic effects of b1 antagonists?

Answer 5

Reduce contractile force and heart rate lowering BP

Question 6

What are the categories of b antagonists?

Answer 6

Aryloxypropanolamines
Arylethanolamines

Question 7

What is the USAN for beta blockers?

Answer 7

Aryloxypropanolamines: olol
Arylethanolamines: alol

Question 8

What is the Aryloxypropanolamines B1 antagonist SAR?

Answer 8

1. Catechol ring can be replaced by wide variety of aromatic rings
2. OH group essential
3. Most marketed as (+) but b-blockade due to (S) (-)-configuration
4. Bulky N-substituents confer b-receptor selectivity

Question 9

What is used to treat glaucoma?

Answer 9

B-blockers such as
Timolol (Timoptic), Betaxolol (Betoptic), Levobunolol (Betagan), Metipranolol (Optipranolol), Carteolol (Ocupress)

Question 10

How should beta blockers be used to treat antihypertensives?

Answer 10

b1-selectivity important for ‘clean’ hypertension treatment

Question 11

Why is selectivity important?

Answer 11

Increased side effects by increasing the site of action

Question 12

What are the common ADRs of non-selective B-blockers?

Answer 12

1. Temporary fatigue
2. Bronchoconstriction
3. Sexual dysfunction
4. Arrhythmias

Question 13

What are the B1-selective antagonists?

Answer 13

BEAM-N
1. Acetbutolol
2. Atenolol
3. Betaxolol
4. Bisoprolol
5. Esmolol
6. Metoprolol
7. Nebivolol

Question 14

What are the B1-non selective antagonists?

Answer 14

Metopranolol

Question 15

What is the receptor specificity of propranolol?

Answer 15

B1 and 2

Question 16

What is the therapeutic use for propranolol?

Answer 16

1. Hypertension
2. Migraine
3. Hyperthyroidism
4. Angina pectoris
5. Myocardial infarction

Question 17

What is the receptor specificity of Nadolol?

Answer 17

B1 and 2

Question 18

What is the therapeutic use for Nadolol?

Answer 18

Hypertension

Question 19

What is the receptor specificity of timolol?

Answer 19

B1 and 2

Question 20

What is the therapeutic use for timolol?

Answer 20

Glaucoma and hypertension

Question 21

What is the receptor specificity of acebutolol, atenolol, esmolol, and metoprolol?

Answer 21

B1

Question 22

What is the therapeutic use for acebutolol, atenolol, esmolol, and metoprolol?

Answer 22

Hypertension

Question 23

What is the receptor specificity of nebivolol?

Answer 23

B1 and Nitric oxide increase

Question 24

What is nebivolol’s therapeutic use?

Answer 24

Hypertension

Question 25

What is pindolol’s receptor specificity?

Answer 25

B1 and 2

Question 26

What is the therapeutic use for pindolol?

Answer 26

Hypertension

Question 27

What is the receptor specificity of carvedilol and labetalol?

Answer 27

a1, b1, and 2

Question 28

What is the therapeutic use for carvedilol and labetalol?

Answer 28

Hypertension and congestive heart failure