Adrenergic Antagonist: Adrenergic receptor blockers

Question 1

agents that produce their major actions inhibiting α and β receptors.

Answer 1

Adrenergic antagonists

Question 2

Adrenergic antagonists block the effects of both exogenously administered as well as endogenously released__________

Answer 2

catecholamines

Question 3

Adrenergic antagonists bind receptors and compete with ________
May affect release of____ from sympathetic fibers

Answer 3

agonists

NE

Question 4

T/F

Adrenergic antagonists often abolish the responses mediated through other types of receptors

Answer 4

F; they generally don’t do this

Question 5

Phenoxybenzamine and phentolamine are:

Answer 5

α adrenergic antagonists (generally 1 and 2)

Question 6

phenoxybenzamine is an________ antagonist

Answer 6

irreversible

Question 7

Phenoxybenzamine works via what type of bonding?

Answer 7

covalent

Question 8

phenoxybenzamine is orally active; long duration of action; blockade persists for days; thus we need to do what to overcome it’s action

Answer 8

need to resynthesize receptors

Question 9

This drg produces vasodilation proportional to the degree of sympathetic tone

Answer 9

phenoxybenzamine

Question 10

Phentolamine is a:

Answer 10

competitive reversible antagonist

Question 11

This adrenergic antgonist is orally active; shorter duration of action, and it’s block can be overcome by increasing levels of agonists

Answer 11

phentolamine

Question 12

Why can phentolamine ve overcome by increaseing levels of agonists

Answer 12

because it’s competitive reversible

Question 13

Phentolamine is uses to tx: _______– in combination with other agents

Answer 13

hypertension

Question 14

pheochromocytoma is treated with:

Answer 14

(phenoxybenzamine, phentolamine)

Question 15

why would you use phetolamine or phenoxybenamine if you had someone anesthitizes

Answer 15

to reverse or shorten the duration of soft-tissue anesthesia produced by
combined local anesthetic and sympathomimetic

Question 16

Side effects of phenoxybenzamine and phentolamine (severely limit usefulness) and include:

Answer 16

tachycardia and salt/water retention (edema) - orthostatic hypotension

Question 17

Selective orally active competitive blocker of α1 receptors

Answer 17

Prazosin

Question 18

What does Prazosin work?

Answer 18

Selective orally active competitive blocker of α1 receptors

Question 19

How does Prazosin improve your lipid profile?

Answer 19

Produces favorable lipid profile - ↓ LDL, ↑ HDL

Question 20

Produces favorable lipid profile - ↓ LDL, ↑ HDL

Answer 20

Prazosin

Question 21

What effect does Prazosin have on arterioles and veins?

Answer 21

Decreases vascular tone in resistance (arterioles) and capacitance (veins) beds

Question 22

Because Prazosin has little blockade of __________ reflex tachycardia is less
problematic - minimal increase in cardiac output

Answer 22

pre-synaptic α2 receptors

Question 23

Major clinical uses of Prazosin

- preload and afterload________ agent

Answer 23

reducing

Question 24

– relaxes α1 mediated contraction of

prostate and bladder neck that contributes to resistance to urine flow

Answer 24

Prazosin

Question 25

Treatment option for Benign Prostatic Hyperplasia (BPH)

Answer 25

Prazosin

Question 26

How does Prazosin help with hypertension/hypotension?

Answer 26

Hypertension

Question 27

Would you use Prazosin for long term tx option of congestive heart failure?

Answer 27

Nope: Short-term treatment of congestive heart failure

Question 28

Major side effects of Prazosin known as ‘first dose effect’ is what?

Answer 28

hypotension and syncope 30-90 min after the first dose – administer the first dose at bedtime

Question 29

Prazosin can occastionally causes persistant:

Answer 29

orthostatic hypotension (occasionally)

Question 30

Prazosin causes edema: T/F

Answer 30

True

Question 31

Tamsulosin is an orally active:

• Favors blockade of α1A receptors in prostate (versus subtypes in blood vessels) - Effective for treatment of BPH with little effect on blood pressure (less propensity
  for orthostatic hypotension) - not approved for treatment of hypertension - Silodosin (Rapaflo®) – also exhibits selectivity for α1A over α1B receptors and used
  for BPH

Answer 31

α1 receptor antagonist with some selectivity for α1A versus α1B subtypes

Question 32

Tamsulosin has some selectivity for _____ versus ____ subtypes

Answer 32

α1A

α1B

Question 33

Tamsulosin gavors blockade of α1A receptors in_______ (versus subtypes in blood vessels)

Answer 33

prostate

Question 34

Effective for treatment of BPH with little effect on blood pressure (less propensity
for orthostatic hypotension)

Answer 34

Tamsulosin

Question 35

T/F

Tamulosin is approved for treatment of hypertension

Answer 35

False