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Autonomics > Adrenergic Antagonists > Flashcards

Adrenergic Antagonists Flashcards

1
Q

Metoprolol, Atenolol, and Esmolol, are what drug class?

A

B1-selective antagonists

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2
Q

what is unique about the function of Acebutolol?

A

it is actually a weak partial agonist. it blocks the effects of a full agonist which will overall limit the effects of NE

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3
Q

uses of B1-selective antagonists?

A

post MI, ischemic heart disease, angina, hypertension, slow heart, decrease cardiac output

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4
Q

B1-selective antagonists are classified as?

A

cardio protectants

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5
Q

B1-selective antagonists are used to reduce _____ ______ arrhythmias

A

ventricular tachycardic

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6
Q

why should insulin-dependent diabetics not use beta1 blockers?

A

if diabetics blood glucose becomes too low they will not feel the common side effect of heart palpitations from low blood sugar because the beta blocker masks this effect of hypoglycemia.

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7
Q

what are the three notable side effects of beta1 selective antagonists?

A

bradycardic arrhythmias
fatigue and exercise intolerance
withdrawal syndrome and rebound tachycardia with disrupt continuation

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8
Q

why should a patient not exercise after immediately going off of a b1 blocker?

A

b1 blockers increase beta receptors on heart, meaning it can be more easily stimulated when the beta receptors are not being blocked and will over stimulate the heart

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9
Q

what do the two isomers of Nebivolol do?

A

one is a B1-selective blocker

other promotes endothelial NO-dependent vasorelaxation

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10
Q

what are the summative effects from the two isomers of Nebivolol?

A

reduce heart rate by relaxing vascular smooth muscle and reduce blood pressure without triggering the baroreflex

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11
Q 
what drug class is Propranolol?
what is it used for?
what does it penetrate?
A

non-selective B antagonist
used for performance anxiety; helps with shakiness
penetrates the BBB

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12
Q

what drug class is Sotalol?
what is it used for?
it has little to no ___ penetration

A

non-selective B antagonist
arrhythmias
CNS

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13
Q 
what drug class is Pindolol?
what is it used for?
A

weak partial B agonist

high BP

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14
Q 
what drug class is Timolol?
what is it used for?
A

non-selective B antagonist

topical glaucoma treatment

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15
Q

T/F non-selective B blockers cross the BBB

A

true

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16
Q

non-selective B blockers are used for:

A 
performance anxiety (if CNS-penetrating)
familial palsy and other tremors
symptoms of hyperthyroidism
prophylactic migraine therapy
ventricular tachycardia arrhythmias
glaucoma
hypertension (not first line of therapy)
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17
Q

people with what conditions should not use non-selective B blockers?

A

insulin-dependent diabetes

asthma and COPD

18
Q

non-selective B blockers may cause depressive episodes if?

A

the individual is prone to depression

19
Q

what are the side effects of non-selective B blockers?

A

malaise (if person is prone to depression)
fatigue and exercise intolerance
hyperkalemia (from blocking K+ entering neurons)
histamine release
bradycardic arrhythmias
withdrawal syndrome and rebound tachycardia upon abrupt discontinuation

20
Q

what is the main function of a1-selective antagonists?

what else do they do?

A

treat hypertension

block vasoconstriction, reduce prostate swelling

21
Q

Prazosin, Terazosin, Alfuzosin, Tamsulosin, and Silodosin are what drug class?

A

a1-selective antagonists

22
Q

which a1-selective antagonists is used off label for PTSD?

A

Prazosin

23
Q

what resulting effect occurs from taking Terazosin, Alfuzosin, Tamsulosin, and Silodosin?

A

increased urinary output

24
Q

70% of prostate receptors are?

A

a1A receptors

25
Q

T/F a1-selective antagonists are more selective for a1B receptors

A

false, more selective for a1A

26
Q

given that a1-selective antagonists increase urinary output, what are they an effective treatment for?

A

Benign prostatic hyperplasia

27
Q

what is the mechanism of action of a1-selective antagonists that makes them a treatment for Benign prostatic hyperplasia?

A

they block the a1 receptors causing relaxation of sphincter and prostate muscle

28
Q

what are the 3 main treatments of a1-selective antagonists?

A

hypertension, congestive heart failure, and frostbite and raynaud’s syndrome

29
Q

why would a1-selective antagonists not be an appropriate choice of treatment for hypertension or congestive heart failure in patients who are prone to tachycardia?

A

a1-selective antagonists decrease peripheral resistance.
for hypertension: decreasing BP will inc HR which is a contraindication.
for congestive heart failure: same thing HR will inc

30
Q

what is Raynaud’s syndrome?

A

when there’s not enough blood flow to the periphery

31
Q

what are side effects from a1-selective antagonists?

A

tachycardia
syncope (fainting due to drop in BP) and orthostatic hypotension
nasal congestion
inhibition of male ejaculation

32
Q

why counsel patients to take a1-selective antagonists at night?

A

so they aren’t getting up quickly to avoid orthostatic hypotension causing them to faint

33
Q

why is fainting in the shower a concern for people taking a1-selective antagonists?

A

the heat from the shower causes additional vasodilation on top of the vasodilation caused by the drug

34
Q

why would an older man need to stop taking his medication for BPH before his eye surgery? (surgery requires complete dilation of pupil)

A

BPH is treated with a1-selective antagonists, and a1 receptors in the eye cause dilation of the pupil. the a1-selective antagonists will prevent the eye from being able to dilate

35
Q

Labetolol is given in a mixture of four stereoisomers each with unique properties.
what selectivity will each isomer have regarding receptors? (antagonist/agonist)
identify what these antagonists/agonists effects will be
identify what the overall effect from this drug will be

A

RR: B1 antagonist and B2 partial agonist
SR, SS: a1 antagonist
RS: no activity
B1 antagonist: blocks increasing HR
B2 partial agonist: blocks vasoconstriction
a1 antagonist: causes vasodilation in skeletal muscle
overall effect: very effective antihypertensive

36
Q

Carvedilol is a mix of two enantiomers, what are they and what selectivity do they have regarding receptors?
what is the drugs effect?

A

S: B antagonist and a1 antagonist
R: a1 antagonist
good antihypertensive

37
Q

how does Carvedilol protect against atherosclerotic complications of hypertension?

A

has antioxidant and antiproliferative effects on vascular smooth muscle

38
Q

what effects would you expect to see from non-selective alpha1/2 antagonists?

A

decrease in BP and large inc in HR

39
Q

what classification is phentolamine?

what is it used for?

A

competitive alpha antagonist

quick reversal of numbness following dental procedures

40
Q

what classification is phenoxybenzamine?
what is it used for?
it must be in combination with?

A

irreversible alpha antagonist
used to manage pheochromocytoma
in combo with propranolol

41
Q

what are the side effects of non-selective alpha1/2 antagonists?

A

since they block a2 receptors they block the inhibition of the baroreflex causing a greater baroreflex response (hence the large inc in HR)
since they block a2 receptors they block inhibition of NE release onto the heart leading to greater NE release

42
Q

what is pheochromocytoma?

A

a small vascular tumor of the adrenal medulla, causing irregular secretion of epinephrine and norepinephrine, leading to attacks of raised blood pressure, palpitations, and headache

Autonomics (14 decks)

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