Sweatman Alpha Blockers Flashcards

1
Q

Alpha Blocking Agents

3-Major

A

Doxazosin (cardura)
Terazosin (hytrin)
Parzosin (minipress)

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2
Q

Alpha Blocking agents (2-Minor)

A

Phenoxybenzamine (dibenzyline)

Phentolamine (regitine)

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3
Q

Agent in the major Alpha Blocker Class that due to PK’s is less amenable for therpy

A

phentolamine a1=a2 and phenoxybenzamine

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4
Q

intended effect of alpha antagonists

A

vasodilation

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5
Q

Why are phenoxybenzamine and phentolamine limited in clinical use

A

they inhibit alpha 1 and alpha 2 and can actually cause cardiac stimulation and unintended vasoconstriction

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6
Q

alpha 2 receptors are located…

A

presynaptically

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7
Q

alpha 1 receptors are located

A

postsynaptically

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8
Q

alpha 2 receptors function as

A

autoreceptors

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9
Q

alpha 1 receptors function in

A

down stream signalling

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10
Q

norepinephrine is tropic for

A

alpha-1, 2 receptors

Beta-1

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11
Q

epinephrine is tropic for

A

alpha 1 and 2 and beta 1 and 2 receptors

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12
Q

beta receptors cause

A

vasodilation

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13
Q

alpha receptors result in

A

vasoconstriction

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14
Q

SA node is accelerated by what type of receptors

A

B1 and 2

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15
Q

ectopic pacemakers are accelerated by what type of receptors

A

B1 and 2

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16
Q

contractility is increased by via which S receptors

A

B1 and 2 receptor

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17
Q

BV’s in skin are contractes by Sympa. acting on

A

alpha receptors

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18
Q

BV’s in skeletal muscle is relaxed by what type of receptors

A

beta 2

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19
Q

BV’s in skeletal muscle are contractes by acting on which type of receptor

A

alpha

20
Q

ALpha 1 receptors work via

A

activation of the receptor increasing DAG and IP3 leadings to increased intracellular calcium–>propagation of signal

21
Q

isoprotorenol tropic for

A

beta-1and 2

22
Q

alpha receptors mainly block the BP increases caused by

A

norepinephrine acting on alpha receptors

prevents vasoconstriction

23
Q

Beta blockers lower blood pressure by

A

blocking the effects of EPINEPHRINE onto alpha receptors
*in the presence of a normally functioning beta relaxation-> low blood pressure in the absence of the normal alpha vasoconstriction

24
Q

Pre-treatment with a beta blocker in the presence of epinephrine

A

rise in BP

25
Q

pretreatment with alpha blocker in presence of isoproterenol

A

no affect–> it acts on Beta receptors–> will vasodilate and reduce BP

26
Q

A1»>A2

A

terazosin, doxazosin, prazosin

*inhibits downstream signaling

27
Q

A1>A2

A

phenoxybenzamine

28
Q

a1=a2

A

phentolamine

29
Q

Alpha 1a utility

A

bladder neck and prostate –>reduce BPH and increase urine flow rate

30
Q

Alpha 1a drug useful in BPH

A

alfuzosin

31
Q

principle issue with alpha blockers

A

too rapid of a reduction in BP leading to orthostatic hypotension

32
Q

most prominent OH causing alpha blocker

A

prazosin

33
Q

second most common adverse effect os alpha 1 drugs

A

cross-talk inhibition of alpha 2 pre-synaptic receptors

–>receptor specificity is never 100%

34
Q

Adverse effects of alpha 2 blockade by alpha 1 tropic agents

A

with high doses–>autoreceptors are effected
inhibition of the feedback regulation–>leads to increased released of norepinephrine–>overstimulation of CV system in the form of tachycardia

35
Q

alpha blockers with longerhalf life

A

*regimens=once/daily
doxazosin–>22hrs
terazosin–>12 hrs

36
Q

alpha blocker that covalently binds and it non-competitive

A

phenoxybenzamine

37
Q

side effects of phenoxybenzamine

A

–>nasal congestion
–>tachycardia
*alpha one and 2 antagonist
so antiagonizes circulating E and NE on VSM while increasing release of NE–>increases CO and tempering BP lowering action

38
Q

other side effects of phenoxybenzamine

A

drowsiness, fatigue, weakness, mailaise, confusion, headache, xerostome, and ejaculatory dysfunction

39
Q

short onset–>long duration

A

phenoxybenzamine

40
Q

short acting competitive antagonist

A

phentolamine

41
Q

indications for phenoxybenzamine

A

pheochomrocytoma

42
Q

indications for phentolamine

A

pheochromocytoma and hypertensive emergency

43
Q

small doses of phentolamine…

A

positive inotropic effect –>increasing BP

44
Q

larger doses of phentolamine…

A

peripheral Vasodilation—> decreased BP

45
Q

prominent feature of phentolamine

A

POSTURAL HYPOTENSION and reflex tachycardia–>precipitating cardiac arrythmias