Exam 2

Question 1

Dichloroisoproterenol

Answer 1

Non-Selective B Antagonist.

Question 2

Pronethalol

Answer 2

Non-Selective B Antagonist.

Discontinued - Tumors in mice; did not make it through clinical trials.

Question 3

Propranolol* (Inderal)

Answer 3

Non-Selective B Antagonsists.

Crosses BBB - Performance anxiety.

Question 4

Pindolol

Answer 4

Non-Selective B Antagonist.

Partial Agonist.

Question 5

Timolol (Timoptic)

Answer 5

Non-Selective B Antagonist.
Glaucoma.
Be careful in asthmatics, systemically absorbed.

Question 6

Sotalol

Answer 6

Non-Selective B Antagonist.

Doesn’t cross BBB: Cardiovascular uses only.

Question 7

Labetalol

Answer 7

Non-Selective B Antagonist *With* A1 Antagonist Activity.
R,R - B1 antagonist, B2 partial agonist.
R,S - Inactive.
S,R - A1 antagonist.
S,S - A1 antagonist (5 times less)
Very effective HTN treatment.

Question 8

Carvedilol

Answer 8

Non-Selective B Antagonist With A1 Antagonist Activity.
S - B antagonism and A1 antagonism
R - only A1 antagonism
B antagonism > A1 antagonism.
Good HTN treatment.
Additional antioxidant/antiproliferative effects on smooth muscle - prevents atherosclerotic complications.

Question 9

Metoprolol

Answer 9

Selective B1 Antagonist.
Inverse Agonist.
Metabolism by CYP2D6 - genetic polymorphisms:
EM t1/2 = 3-4hrs.
PM t1/2 = 7-9hrs.

Question 10

Atenolol

Answer 10

Selective B1 Antagonist.
Inverse Agonist.
No CYP2D6 metabolism.

Question 11

Esmolol

Answer 11

Selective B1 Antagonist.
Only for short-term use - IV.
Terminal ester in para-position - Carboxylate product.

Question 12

Acebutolol*

Answer 12

Selective B1 Antagonist.
Weak Partial agonist = Partial Antagonist.
Two step modification: Amidase, N-Acetylation - yields Diacetalol; B1-selective antagonist as well.
Acebutolol t1/2 = 3hr.
Diacetalol t1/2 = 8-12hr.

Question 13

Nevbivolol

Answer 13

Selective B1 Antagonist With Vasodilating Properties.
Stimulates endothelial cell NO production.
d-Nevbivolol = SRRR; B1-antagonism.
l-Nevbivolol - RSSS; NO

Question 14

Phentolamine

Answer 14

Non-Selective A Antagonist.
Pheochromocytoma.
Competitive.

Question 15

Phenoxybenzamine*

Answer 15

Non-Selective A Antagonist.
Pheochromocytoma.
Irreversible - Aziridium Ion covalently binds A-receptor sulfur or nitrogen residues.
Problem - also acylates Serotonin and Histamine receptors.

Question 16

Prazosin

Answer 16

Selective A1 Antagonist.
Crosses BBB - PTSD.
Three parts: Quinazoline, Peperazine, Furan.
t1/2 = 2-4hrs.
Bioavailability = 50%
HTN

Question 17

Terazosin

Answer 17

Selective A1 Antagonist.
Three parts: Quinazoline, Piperazine, Tetrahydrofuran.
t1/2 = 12hrs.
Bioavailability = 90%
HTN, BPH

Question 18

Alfuzosin

Answer 18

Selective A1 Antagonist.
Three parts: Quinazoline, No piperazine, Tetrahydrofuran.
t1/2 = 10hrs.
Bioavailability = 50%
BPH

Question 19

Tamsulosin (Flomax)

Answer 19

Selective A1 Antagonist.
A1a-Selective
BPH

Question 20

Silodosin (Rapaflo)

Answer 20

Selective A1 Antagonist.
A1a-Selective
Benign Prostatic-HTN.
t1/2 = 13hrs.
Glucuronide-Product: may be contributing to the overall antagonist properties
- t1/2 = 24hrs.