Adrenergic Antagonist: Adrenergic receptor blockers Flashcards Preview

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Flashcards in Adrenergic Antagonist: Adrenergic receptor blockers Deck (35)
1

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

Adrenergic antagonists

2

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

catecholamines

3

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

agonists
NE

4

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

F; they generally don't do this

5

Phenoxybenzamine and phentolamine are:

α adrenergic antagonists (generally 1 and 2)

6

phenoxybenzamine is an________ antagonist

irreversible

7

Phenoxybenzamine works via what type of bonding?

covalent

8

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

need to resynthesize receptors

9

This drg produces vasodilation proportional to the degree of sympathetic tone

phenoxybenzamine

10

Phentolamine is a:

competitive reversible antagonist

11

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

phentolamine

12

Why can phentolamine ve overcome by increaseing levels of agonists

because it's competitive reversible

13

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

hypertension

14

pheochromocytoma is treated with:

(phenoxybenzamine, phentolamine)

15

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

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

16

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

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

17

Selective orally active competitive blocker of α1 receptors

Prazosin

18

What does Prazosin work?

Selective orally active competitive blocker of α1 receptors

19

How does Prazosin improve your lipid profile?

Produces favorable lipid profile - ↓ LDL, ↑ HDL

20

Produces favorable lipid profile - ↓ LDL, ↑ HDL

Prazosin

21

What effect does Prazosin have on arterioles and veins?

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

22

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

pre-synaptic α2 receptors

23

Major clinical uses of Prazosin
- preload and afterload________ agent

reducing

24

– relaxes α1 mediated contraction of
prostate and bladder neck that contributes to resistance to urine flow

Prazosin

25

Treatment option for Benign Prostatic Hyperplasia (BPH)

Prazosin

26

How does Prazosin help with hypertension/hypotension?

Hypertension

27

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

Nope: Short-term treatment of congestive heart failure

28

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

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

29

Prazosin can occastionally causes persistant:

orthostatic hypotension (occasionally)

30

Prazosin causes edema: T/F

True

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

α1 receptor antagonist with some selectivity for α1A versus α1B subtypes

32

Tamsulosin has some selectivity for _____ versus ____ subtypes

α1A
α1B

33

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

prostate

34

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

Tamsulosin

35

T/F
Tamulosin is approved for treatment of hypertension

False