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

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
pretreatment with alpha blocker in presence of isoproterenol
no affect--> it acts on Beta receptors--> will vasodilate and reduce BP
26
A1>>>A2
terazosin, doxazosin, prazosin | *inhibits downstream signaling
27
A1>A2
phenoxybenzamine
28
a1=a2
phentolamine
29
Alpha 1a utility
bladder neck and prostate -->reduce BPH and increase urine flow rate
30
Alpha 1a drug useful in BPH
alfuzosin
31
principle issue with alpha blockers
too rapid of a reduction in BP leading to orthostatic hypotension
32
most prominent OH causing alpha blocker
prazosin
33
second most common adverse effect os alpha 1 drugs
cross-talk inhibition of alpha 2 pre-synaptic receptors | -->receptor specificity is never 100%
34
Adverse effects of alpha 2 blockade by alpha 1 tropic agents
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
alpha blockers with longerhalf life
*regimens=once/daily doxazosin-->22hrs terazosin-->12 hrs
36
alpha blocker that covalently binds and it non-competitive
phenoxybenzamine
37
side effects of phenoxybenzamine
-->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
other side effects of phenoxybenzamine
drowsiness, fatigue, weakness, mailaise, confusion, headache, xerostome, and ejaculatory dysfunction
39
short onset-->long duration
phenoxybenzamine
40
short acting competitive antagonist
phentolamine
41
indications for phenoxybenzamine
pheochomrocytoma
42
indications for phentolamine
pheochromocytoma and hypertensive emergency
43
small doses of phentolamine...
positive inotropic effect -->increasing BP
44
larger doses of phentolamine...
peripheral Vasodilation---> decreased BP
45
prominent feature of phentolamine
POSTURAL HYPOTENSION and reflex tachycardia-->precipitating cardiac arrythmias