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CVT Apex > ANS Pharm: Adrenergic Antagonists > Flashcards

ANS Pharm: Adrenergic Antagonists Flashcards

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1
Q

Common side effect of prazosin

A

ortho hypoTN

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2
Q

Why shouldn’t hypovolemic patients get A1 antagonists?

A

reduction in arterial BP
&
reflex tachycardia

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3
Q

Drugs that affect the ANS may mimic or block these 2 NTs

A

ACh & NE

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4
Q
A
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5
Q
A
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6
Q
A

propranolol

(nonselective, so less popular now)

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7
Q

Why is labetalol special in its action?

A

has both selective A1 antag + B1 & B2 antag

vasodilates without reflex tachycardia

alpha : beta blockade is 1:7.

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8
Q

Alpha antagonits are good for HTN, __, ___, & ___

A

heart failure
BPH
pheochromocytoma

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9
Q

Why do we need to carefully titrate alpha & beta antagonists?

A

susceptible to variable response based on receptor up/down regulation (both), receptor densities in diff tissues (alpha), & genetics (beta)

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10
Q

the nonselective & selective Alpha antag.

A
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11
Q

Which is competitive? non-competitive?

A

phentolamine = competitive

phenoxybenzamine = non-competitive (IRREVERSIBLE)

phenoxybenzamine = prototype nonselective

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12
Q

The only way to stop phenoxybenzamine’s effects

non-competitive (IRREVERSIBLE) non-selective apha antagonist

A

synthesize new receptors

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13
Q

you gave phenoxybenzamine but now have hypoTN. Which pressors will NOT work?

A
  • norepi & neo d/t the irreversible block
  • epi may worsen HypoTN d/t unopposed B2 stimulation (“epi-reversal”)

“epi-reversal”: epi’s A-mediated pressor turns into B-mediated depressor

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14
Q

Expected effects from phenoxybenzamine

use low dose initiation

A
  • blocks A-activity of epi & NE (↓SVR)
  • reflex tachycardia (baroreceptors & increased free NE)
  • ortho hypoTN; fall risk
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15
Q

best treatment for phenoxybenzamine hypoTN

A

vaspressin and fluids

NO!: epi, norepi, neo

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16
Q

how to reverse phentolamine

A

A-agonist

(neo, NE)

phenoxybenzamine cannot be reversed; only by making new receptors

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17
Q
A
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18
Q

phentolamine has an affinity for ___ receptors, which….

A

5HT

  • stomach acid secretion
  • mast cell degranulation

Mast cell degranulation: release inflammatory substances (histamine, TNF-α, tryptase)

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19
Q

Prazosin selectivity

A

A1:A2

1000:1

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20
Q

Prazosin
expected effects

A

↓PVR in arterioles and veins
↑venous capacitance, ↓preload

little change in HR
ortho hypoTN

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21
Q
A

prazosin

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22
Q

which selective A-antagonist is mainly used for BPH?

A

terazosin

less potent, longer doA

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23
Q

Why do we care if a patient is on a -“zosin”?

selective A-antag

Study These Flashcards
A

may worsen ANE induced hypoTN

24
Q

Yohimbe effects

not used as HTN Rx anymore, but still present illegally in supplements

Study These Flashcards
A

selective A2 antag

  • ↑PNS/cholinergic activity
  • ↓SNS/adrenergic activity
  • may lessen effects of anti-HTN drugs
25
26
What happens if you sudddently stop taking your Beta blocker?
risk rebound HTN and tachycardia
27
bradyarrhythmias from beta blockers may impair the response to...
* hypovolemia * progressive heart block * heart failure * bronchoconstriction
28
## Footnote propranolol & acebutalol
29
# Beta blockers intrinsic sympathomimetic activity (ISA)
partial beta stimulation (agonist) + blocking endog. catechols. from binding to Beta receptors (less potency than catecholamine & other BBs) ## Footnote labetalol!!
30
* bronchconstriction * hypoglycemia * periph. vasoconstriction
31
Dont give this BB to Raynaud's & periph. vascular Dz
propranolol ## Footnote blocks B2 = periph. vasoconstriction
32
Propranolol moA ## Footnote the prototype nonselective BB
* competitive * B1 & B2 antag. * blocks epi, NE,DA, dobutmaine, isoproterenol
33
The nonselective BBs
* Propranolol * Nadolol * Pindolol * Labetalol * Sotalol * Carvedilol * Timolol
34
BB w/ very long HL
Nadolol
35
Blocking Beta receptors will decrease conduction through the ___ node
AV
36
* metoprolol * acebutalol * esmolol * bisprolol
37
which selective BB has weak B agonist effects (ISA)?
acebutalol less bradycardia and BP effects
38
T/F: Giving higher doses of selective BB's will decrease the selective action.
True! higher dose = less selectivity
39
metoprolol
40
metoprolol moA
* competitive cardioselective (B1) * blocks epi and NE * can be used in HR
41
metoprolol max dose
15 mg give as 2.5 -5 mg
42
these two selective BBs block epi and NE
metoprolol & esmolol
43
Why is esmolol first line for rapid periop control for HR & BP
* fast onset * brief doA (<15 mins) * can titrate as it causes DD ↓HR
44
esmolol
45
esmolol dose
* 10-80 mg bolus * 50-300 mcg/kg/min drip
46
Does esmolol have ISA or MSA?
not at clinical doses
47
esmolol metab
nonspecific esterases from RBCs
48
atenolol
49
which BB decreases conductivity & intotropy from NE release?
atenolol
50
Labetalol receptor activity
unique! (ISA) A1 & Beta antag. B : A block 7 : 1
51
Labetalol primary indication
acute HTN
52
Labetalol's mixed activity (A1 & Beta antag) produces ____ without ....
vasodilation baroreceptor HR increase
53
Labetalol HL
6H
54
Labetalol dose
2.5 mg increments highly variable responses! may acutely exaggerate existing bradycardia
55
# Labetalol & Carvedilol Both are nonselective BB's, how does their action compare?
both A1, B1, B2 antagonism carvedilol has more modest HR reduction; caution w/ labetalol
56
this BB has antioxidant & anti-inflammatory properties
carvedilol
57
atenolol

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