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Spring '20/ L. Pharm Exam 3 - sympatholytics/mimetics, LAs, antiarrhythmics, vaso > Sympatholytics- Alpha Drugs > Flashcards

Sympatholytics- Alpha Drugs Flashcards

1
Q

Name three drugs that are competitive alpha adrenergic antagonists

A

phentolamine, prazosin, & yohimbine

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2
Q

what is different about the receptor binding of phenoxbenzamine

A

binds covalently to produce an IRREVERSIBLE and insurmountable type of alpha blockade

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3
Q

how does the binding of phenoxybenzamine get reversed

A

effects cannot be reversed by sympathomimetics- effects are terminated by METABOLISM

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4
Q

what does phenoxybenzamine treat

A

high BP

heavy sweating due to tumor of the adrenal glands (pheochromocytoma)

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5
Q

which two drugs are nonselective alpha antagonist

A

phentolamine & phenoxybenzamine

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6
Q

phentolamine BP effects

A

peripheral vasodilation, decrease BP

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7
Q

phentolamine manifest its effects___ and last ____

A

2 min

10-15 min

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8
Q

what are the heart rate effects of phentolamine

A

cardiac dysrhythmias

angina

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9
Q

why are there associated cardiac effects with phentolamine

A

alpha receptor blockade permits enhanced neural release of NE increase HR and CO

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10
Q

where does phentolamine have direct action

A

vascular smooth muscle

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11
Q

PNS is predominant after phentolamine what does this cause (3)

A

hyperperistalsis
abdominal pain
diarrhea

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12
Q

where is phentolamine metabolized

what percent is unchanged by the kideny

A

liver

10% unchanged by the kidney

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13
Q

what two condition does phentolamine treat

A

HTN emergencies from pheochromocytoma

autonomic nervous system hyperreflexia

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14
Q

phentolamine push dose

A

30-70mcg/kg (1-5mg)

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15
Q

phentolamine continuous infusion

A

0.1-2mg/min

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16
Q

phentolamine as a local infiltration dose of extravasation of a sympathomimetic medication

A

5-15mg in 10cc ns

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17
Q

phenoxybenzamine what is the GI absorption

A

incomplete

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18
Q

phenoxybenzamine onset of blockade

A

slow up to 60 min to peak after IV administration. This accounts for the modification of the drug molecule to become pharmacologically active

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19
Q

phenoxybenzamine elimination half time

A

24 hour

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20
Q

can phenoxybenzamine accumulate

A

yes with repeated doses

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21
Q

phenoxbenzamine receptor binding

A

alpha 1 more than 2

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22
Q

phenoxybenzamine what are the systemic bp changes in a normovolemic patient

A

little changes

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23
Q

for phenoxybenzamine what is prominent in the presence of preexisting hypertension or hypovolemia

A

orthostatic hypotension

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24
Q

what are the changes to cerebral and coronary vascular resistance with phenoxybenzamine

A

no changes

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25
Q

what is the result of phenoxybenzamine for maternal patients

A

If given during maternal treatment can cause neonatal hypotension and respiratory distress in first 72 hours of life

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26
Q

phenoxybenzamine
BP effect
CO effect
renal blood flow effect

A

decreasing BP
increased CO
renal blood flow is not greatly altered unless preexisting renal vasoconstriction is present

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27
Q

phenoxybenzamine blood loss or vasodilation effects?

A

exaggerated BP decreases in response to blood loss of vasodilating drugs such as volatile anesthetics.

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28
Q

phenoxybenzamine chronic therapy effects

A

sedation

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29
Q

phenoxybenzamine sinus effect

A

Nasal stuffiness is d/t unopposed vasodilation in mucous membranes in the presence of alpha adrenergic block

30
Q

phenoxybenzamine alpha receptor stimulation prevents epi from doing what

A

prevents the inhibitory action of epi on the secretion of insulin

31
Q

phenoxybenzamine po dose

A

0.5-1mg/kg PO

32
Q

when do we give phenoxybenzamine

A

preop to control BP in patients with pheochromocytoma

33
Q

phenoxbenzamine HCT effects

A

expansion of intravascular fluid volume by relieving intense peripheral vasoconstriction thus will see a fall in HCT

34
Q

does phenoxbenzamine help with PVD

A

no because PVD is skeletal muscle blood flow and not cutaneous blood flow

35
Q

other than administration for pheochromocytoma what else can we give phenoxybenzamine for?

A

raynauds disease- due to the cutaneous vasoconstriction

36
Q

once volume has been restored on a patient and we still see tissue ischemia from vasoconstriction what medication relieves the vasconstriciton

A

phenoxybenzamine

37
Q

yohimibine receptor

A

alpha 2 receptor antagonist

38
Q

yohimibine
past uses
current uses

A

past impotence

current orthostatic hypotension

39
Q

doxazosin receptor

A

alpha 1 antagonist

40
Q

doxazosin uses

A

HTN

benign prostatic hypertrophy

41
Q

prazosin receptor

A

alpha 1 antagonist

42
Q

prazosin uses

A

pheochromocytoma

43
Q

terazosin receptor

A

alpha 1 antagonist

44
Q

terazosin uses

A

BPH

45
Q

tamsulosin receptor

A

alpha 1 antagonist

46
Q

tamsulosin uses

A

BPH

47
Q

tamsulosin which medication decreases the clearance of it

A

cimetidine

48
Q

tolazoline receptor

A

non selective alpha antagonists

49
Q

tolazoline uses

A

pul HTN in new borns replaced by nitric oxide

50
Q

alpha 2 agonist pharmacology effects (3)

A

sedation, hypotension, bradycardia

51
Q

alpha 2 receptors are found where

A

CNS- Brainstem and locus ceruleus

52
Q

where are alpha 2 receptors pre or post synpatic

A

presynaptic

53
Q

which mechanism do alpha 2 receptors use

A

negative feed back mechanism

54
Q

as a result of alpha 2 negative feed back what is not being released from the presynaptic nerve terminal

A

NE

55
Q

inhibition of alpha 2 receptors has what effect on glucose and insulin

A

inhibition of insulin release and induction of glucagon from pancreas

56
Q

is binding of alpha 2 agonist reversible

A

yes

57
Q

withdrawal from alpha 2 agonist can result in what

A

increase HR and HTN

58
Q

clonidine cardiac effects?

A

dose dependent decreases in HR and BP

59
Q

clonidine what two things does it treat

A

resistant HTN and tremors from central stimulant medication

60
Q

what forms do we give clonidine

A

IV, PO, transdermal

61
Q

clonidine terminal half life

A

12-16 hours

62
Q

clonidine partial agonists on which receptors

A

400:1 alpha 2 over alpha 1

63
Q

clonidine metabolized where and excreted where

A

liver and excreted in the bile and feces

64
Q

Dexmedetomidine: receptor

A

Selective alpha 2 agonist with 1,600:1 preference of alpha 2

65
Q

dex IV dose

A

0.1-1.5mcg/kg/min

66
Q

dex terminal elimination half life

A

2 hours

67
Q

when is dex used most often

A

icu or OR as a sedative and analgesic d/t its central sympatholytic effects

68
Q

dex is under goes what in the liver and excreted mostly in the

A

biotransformation in liver and excreted in the urine

69
Q

dex withdrawal

A

tachycardia HTN Anxiety

70
Q

Dexmedetomidine

A

Large IV boluses (0.25 to 1 mcg/kg over 3-5 min) result in a paradoxical hypertension with a decrease in HR and resembles phenylephrine and is the resultant effect of crossover alpha 1 stimulation.

Spring '20/ L. Pharm Exam 3 - sympatholytics/mimetics, LAs, antiarrhythmics, vaso (17 decks)

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