Adrenergic Antagonists- T2 Flashcards

1
Q

alpha adrenergic receptor antagonists may be classified as

A

reversible competitive antagonists and irreversible competitive alpha-adrenergic antagonists

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2
Q

phentolamine is a

A

non-selective (both alpha 1 and 2) reversible competitive alpha-adrenergic receptor antagonists.

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3
Q

prazosin, doxazosin, and terazosin are

A

alpha1 selective reversible competitive alpha-adrenergic receptor antagonists

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4
Q

tamsulosin and silodosin (rapaflo) are

A

alpha1A/D selective reversible competitive alpha-adrenergic receptor antagonists

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5
Q

phenoxybenzamine is

A

a irreversible competitive non selective alpha adrenergic antagonist

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6
Q

4 piperazinyl quinazolines

A

prazosin, terazosin, doxazosin, alfuzosin

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7
Q

3 indoles

A

yohimbine, indoramin, silodosin

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8
Q

alpha1 and 2 adrenoceptors are responsible for the

A

maintenance of TPR and maintain pressure.

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9
Q

in many patients with essential HTN, TPR may be abnormally elevated due to

A

increased alpha-adrenergic receptor stimulation.

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10
Q

the 6 alpha-adrenergic receptor subtypes

A

1a, 1b, 1d, 2a, 2b, 2c

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11
Q

agents that antagonize both alpha1 and 2 tend to be

A

less efficacious in lowering BP than alpha1 selective

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12
Q

blockade of alpha2 adrenoceptors will cause

A

enhanced release of NE at the sympathetic neurons leading to excess adrenoceptor stimulation.

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13
Q

alpha2 blockage causes veno___ which leads to__

A

venodilation leading to a reduction in preload and then reduces SV.

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14
Q

why would we want to give a selective alpha antagonist opposed to non selective

A

giving a selective reduces the peripheral resistance, if it doesn’t have selectivity, we won’t have effects that come from antagonizing a specific alpha receptor.

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15
Q

prazosin and htn tx

A

a alpha1 selective antagonist that is prone to hepatic metabolism, has the shortest half life and primarily eliminated in the bile. if the patient has renal impairment you would want to use this.

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16
Q

doxazosin and terazosin in htn tx.

A

alpha1 selective antagonists have more renal eliminated of the parent compound and longer half life of elimination, would want to use these if the pt had liver failure.

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17
Q

antagonism of alpha1 adrenoceptors result in

A

dilation of arteries, arterioles, and veins.

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18
Q

arteriolar dilation results in

A

decreased after load (decreased TPR)

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19
Q

afterload is

A

the pressure that the heart has to work against.

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20
Q

venous dilation causes

A

decreased preload

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21
Q

decreased preload decreases

A

myocardial stretch and thus the CO.

22
Q

efferent arteriolar dilation causes

A

decrease GFR which causes decrease Na in DCT and causes increased renin release.

23
Q

what agents have equivalent BP lowering capacity to alpha1 selective antagonists

A

Ca channel blockers and thiazides

24
Q

adverse effects of alpha1 selective adrenergic receptor antagonists

A

hypotension (first dose or orthostatic), dizziness, HA, congestion, impaired ejaculation and miosis

25
Q

the lest well tolerated alpha1 selective antagonist

A

prazosin

26
Q

alpha1 selective antagonists contraindicated in pts with

A

right heart failure or cardiac valvular stenosis.

27
Q

how do alpha blockers make right heart failure worse

A

right HF is the right ventricle not ejecting the right amount of blood, too little filling, not enough stretch. alpha blockers decrease the preload, which makes RHF worse.

28
Q

alternative use for alpha1 selective antagonists other than HTN

A

benign prostatic hyperplasia

29
Q

tamsulosin is selective for what receptor

A

alpha1a

30
Q

___ receptors predominate in the vasculature

A

alpha1b

31
Q

why would you give terazosin for HTN and BPH?

A

because it isn’t subtype selective like flomax is.

32
Q

what is phenoxybenamines MOA and what is its therapeutic use

A

alkylates alpha 1 &2 adrenoceptors to cause decrease in receptors available for activation by catecholamines. used for pheochromocytoma where excess catecholamine production results in dangerously high BP

33
Q

yohimbine is a selective

A

alpha2 receptor blocker that produces increase BP via CNS effects.

34
Q

4 non selective b-receptor antagonists

A

propranolol, nadolol, timolol, pindolol

35
Q

4 b1 receptor selective antagonists

A

metoprolol, atenolol, esmolol, acebutolol

36
Q

2 beta and alpha1 selective antagonists

A

labetalol and carvedilol

37
Q

what drug is a beta blocker with additional effects

A

bystolic, dilates blood vessels by NO release.

38
Q

5 general things that distinguish members of the beta adrenergic receptor antagonist class

A

b1 vs non selectivity, partial agonism, alpha adrenoceptor blocking, lipid solubility, and inverse agonists.

39
Q

b1 vs non-selectivity

A

propranolol has equivalent affinities for the 2 receptors while metoprolol, esmolol and atenolol show greater b1 receptor affinity

40
Q

partial agonism with beta adrenergic antagonists

A

propranolol is an antagonist with no ability to active b-receptors; while pindolol and acebutolol behave more as a partial agonist

41
Q

alpha-adrenoceptor blocking activity in regards to beta-adrenergic antagonist

A

most agents in this class are relatively b-selective however labetalol and carvedilol have significant alpha1 blocking activity.

42
Q

lipid solubility

A

more lipophilic agents have greater CNS effects. this is why propranolol can be used for stage fright.

43
Q

generally b-blockade causes

A

greater decreases in HR and contractility during sympathetic NS activity.

44
Q

major effect of b-blockade

A

decrease cardiac rate and contractility to decrease Co and thereby MBP

45
Q

initially ___ may rise due to beta2-blockade and/or reflex baroreceptor mechanism to maintain BP

A

TPR

46
Q

partial agonists or alpha blocking activity may produce less increase in

A

TPR

47
Q

b-antagonists also ___ renin release..

A

decrease. causing less circulating angiotensin II.

48
Q

how do mixed antagonists decrease BP

A

by slpha1 blockage in the vasculature as well as beta-blockade in the heart.

49
Q

partial b-receptor agonists produce smaller decreases in __ and may be preferred in pts with

A

CO. preferred in pts with bradycardia or decreased cardiac reserve.

50
Q

pharmacological adverse effects of b-adrenergic antagonists

A

HF, bradycardia, angina after withdrawal, bronchoconstriction in asthmatics, fatigue, insomnia, depression.