Adrenergic Antagonists

Question 1

Important side effect to remember with alpha adrenergic antagonists

Answer 1

Sexual Dysfunction

Question 2

Three examples of alpha1 adrenergic antagonists

Answer 2

Prazosin
Terazosin
Doxazosin

Question 3

Clinical use of alpha1 adrenergic antagonists

Answer 3

Hypertension, Benign Prostatic Hypertrophy

Question 4

Side effects of alpha1 adrenergic antagonists

Answer 4

Orthostatic Hypertension
Inhibition of Ejaculation
Nasal stuffiness
Tachycardia

Question 5

Important thing to remember about phenoxybenzamine

Answer 5

Nonselective (Dirty Drug)

Irreversible antagonist resulting from covalent modification of receptor

Question 6

Chemical details about phentolamine

Answer 6

Non-selective alpha receptor agonist

Competitive

Question 7

Effects of phentolamine use

Answer 7

Potent vasodilator, but gives pronounced tachycardia

blocks presynaptic alpha2 and 5HT

Question 8

Important difference between Prazosin, Terazosin, and Doxazosin

Answer 8

Halflife.
P3
T12
D20

Question 9

Effects of Prazosin, Terazosin, and Doxazosin?

Answer 9

Vasodilators

Relaxation of smooth muscle in enlarged prostate and bladder base

Question 10

What is the first dose effect?

Answer 10

In drugs like Prazosin, Terazosin, and Doxazosin, first dose may lead to orthostatic hypotension

Question 11

What is Yohimbine?

Answer 11

Indole alkaloid

Blocks alpha2 receptors, increasing sympathetic discharge

Question 12

beta blockers were one of the first major _______ drugs

Answer 12

Rationally Designed

Question 13

Who is the original G of beta blockers

Answer 13

Propranolol

Question 14

Important chemical attributes of beta blockers

Answer 14

Non-selective
Lipophillic - CNS access
Local anesthetic properties
Blockade is activity-dependent

Question 15

Pharmacological effects of Propranolol

Answer 15

Lowers CO and heart rate
Reduced Renin Release
Increased VLDL, HDL (inhibited lipolysis)
Inhib. compensatory glycogenolysis and GLU release
Increases bronchial airway resistance

Question 16

Main way beta blockers inhibit HTN?

Answer 16

Reduced Renin Release

Question 17

Therapeutic uses for beta-blockers?

Answer 17

HTN, angina, arrythmia,
migraine, stage fright,
thyrotoxicosis, glaucoma,
CHFII-III

Question 18

What should you know about Nadolol

Answer 18

Less lipophilic than propranolol
Long Half life (20h)
Used for HTN, angina, migraine

Question 19

What should you know about Timolol

Answer 19

Thiadiazole nucleus with morpholine ring

HTN, angina, migraine, GLAUCOMA

Question 20

How do beta blockers affect pupil size?

Answer 20

They don’t

They’ll decrease pressure without effects like cholinergic

Question 21

What is unique about Pindolol?

Answer 21

Possesses Intrinsic sympathomimetic Activity (Partial Agonist)
Less likely to cause bradycardia and lipid abnormalities
HTN, Angina, Migraine

Question 22

Other than Pindolol, whats the other important partial agonist? Why care?

Answer 22

Carteolol
Less likely to cause bradycardia and lipid abnormalities
Used for HTN and glaucoma

Question 23

Three selective beta1 adrenergic receptor antagonists

Answer 23

Metoprolol, Bisoprolol, Atenolol, Esmolol

Question 24

Metoprolol and Bisoprolol – what does it do?

Answer 24

Cardioselective, doesn’t trigger the bronchoconstriction

Question 25

Metoprolol and Bisoprolol half life

Answer 25

3-4 hours

Question 26

Metoprolol and Bisoprolol uses?

Answer 26

HTN, angina, anti-arrhythmic, CHF

Question 27

What's the deal with atenolol?

Answer 27

Cardioselective, low lipophilicity, 6-9 hour halflife | Treats HTN and angina

Question 28

What characteristic of Esmolol different from the other beta1 adrenergic receptor antagonists?

Answer 28

Very short half life (ex. 9 minutes) caused by rapid hydrolysis by esterases found in RBCs

Question 29

What is Esmolol used to treat?

Answer 29

Supraventricular tachycardia Atrial fibrillation/Fluter Perioperative HTN

Question 30

Who did he say was a 3rd gen beta blocker

Answer 30

Nebivolol (Bystolic)

Question 31

Important details for nebivolol

Answer 31

Beta1 selective, but also causes vasodilation by NO production Used to treat HTN

Question 32

Two examples of mixed adrenergic receptor antagonists

Answer 32

Labetalol | Carvedilol

Question 33

Chemical mechanism of Labetalol

Answer 33

Non-selective beta receptor antagonist + alpha1 receptor antagonist

Question 34

What is Labetalol used for?

Answer 34

beta-blocking activity prevents reflex tachycardia normally associated with alpha 1 receptor antagonists HTN, Hypertensive Crisis

Question 35

Chemical data for Carvedilol?

Answer 35

Non-selective beta antagonist, alpha1 receptor antagonist

Question 36

How does Carvedilol work?

Answer 36

Beta blocking activity prevents reflex tachycardia normally associated with alpha1 receptor antagonists

Question 37

Uses for Carvedilol?

Answer 37

HTN, CHF

Question 38

Side effects associated with beta-blockers

Answer 38

Bradycardia, AV block, sedation, mask symptoms of hypoglycemia, withdrawl

Question 39

Contraindications for beta blockers?

Answer 39

Asthma, COPD, CHF-Type 4

Question 40

Example given for a catecholamine depleter

Answer 40

Reserpine

Question 41

Molecular activity of Reserpine

Answer 41

Block vesicular monoamine transporters | Depletes the vesicular pool of NE

Question 42

Reserpine is used to treat...

Answer 42

HTN

Question 43

Important side effect of Reserpine

Answer 43

Depression