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Q3 Pharm Cholinergics > Adrenergic Blockers > Flashcards

Adrenergic Blockers Flashcards

1
Q

Adrenergic β- Blockers have what result on ⍺ responses?

A

⍺ processes become dominant

reverse true for ⍺-Blockers?

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2
Q

Normal result of ⍺1 stim?

A 
Excitatory:
mydriasis (C radial mm)
C bv to skeletal mm, skin
C hold urine
ejaculation
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3
Q

Normal result of ⍺2 stim?

A

Inhibitory:
↓ NE release
↓ insulin secretion
R GI

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4
Q

⍺1-Blockade causes?

A 
(Decreased vasoconstriction)
↓ peripheral resistance -> ↓ BP
↓ venous return (ortho/standing hypoTN)
Miosis
Nasal congestion
↑ urine flow (tx BPH)
↓ ejaculation
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5
Q

⍺2-Blockade causes?

A

↑ NE release

↑ insulin release

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6
Q

Normal results of β1 stim?

A

Inhibitory:
↑ renin
↑ HR, cond, contr

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7
Q

Normal results of β2 stim?

A 
Inhibitory:
R bronchioles
R bv in skeletal mm
R coronary/cerebral arteries (↑ HR, cond, contr)
R GI/U
↑ glycogenolysis/genesis
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8
Q

Normal results of β3 stim?

A

Inhibitory:

↑ lipolysis

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9
Q

β1-Blockade causes?

A

↓ renin

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10
Q

β2-Blockade causes?

A

Bronchoconstriction
↓ rate/force contraction = ↓ CO, ↓ O2 demand
↓ IO pressure
↓ glycogenolysis

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11
Q

β3-Blockade causes?

A

↓ lipolysis

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12
Q

Competitive ⍺ agonsists shift dose-response curve?

A

Right (need more NE to cause effect)

Max effect is same

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13
Q

Competitive ⍺ agonsists duration dependent on? (2)

A

dissociation from receptor

1/2 life

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14
Q

Irreversible ⍺ agonsists shift does-response curve?

A

Right

Max response diminished

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15
Q

Irreversible ⍺ agonsists duration dependent on?

A

exceed 1/2 life (stays bound)

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16
Q

Reflex tachycardia results from ⍺-Blockade why? (2)

A

1) ↓ BP -> stim baro -> stim sypathetics (↓ vagal input)

2) ⍺2 block -> ↑ NE release -> ↑ β heart stim

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17
Q

Ortho HTN results from ⍺-Blockade why?

A

⍺1 block = ↓ vasoconstriction of veins

↓ contraction -> ↓ filling pressure -> ↓ BP

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18
Q

EpiNE reversal of ⍺-Blockade?

A

blocked ⍺ exposes β:
Epi dilates bv to skeletal mm ->
↓ BP -> reflex ↑ HR

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19
Q

Phentolamine (Regitine) affects what receptors?

A

⍺1 and ⍺2

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20
Q

Phentolamine effects on ⍺1?

A

(⍺-block)

↓ peripheral resistance -> ↓ BP

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21
Q

Phentolamine effects on ⍺2?

A

(⍺-block)

↑ NE = ↑ baro -> cardiac stim (β)

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22
Q

Phentolamine side-effects?

A

HypoTN
Tachycardia
Arryth
myocard ischemia

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23
Q

Phentolamine used to tx?

A

HTN from pheonchromocytoma or MAO inhibitors

necrosis post ⍺-agonist infusion

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24
Q

Phentolamine contraindicated for?

A 
CAD
peptic ulcers (stims histamine = acid prdxn)
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25
Q

Phenoxybenzamine affects what receptors?

A

IRREVERSIBLE ⍺-block

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26
Q

Phenoxybenzamine effects on ⍺ receptors?

A

(lasts several days)

↓ BP -> reflex tachycardia

⍺1 block = ↓ vasoconstriction -> ortho hypoTN
⍺2 block = inhibit NE reuptake

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27
Q

Phenoxybenzamine side-effects?

A

tachycardia
ortho hypoTN
nasal congestion
↓ ejaculation

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28
Q

Phenoxybenzamine used to tx?

A

pheochromocytoma (high symp tone),

irreversible binding prevents HTN

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29
Q

Phenoxybenzamine contraindicated?

A

hypovolemic,
alcohol use,
vasodilators
= severe hyopTN

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30
Q

Pheochromocytoma is?

A

adrenal neoplasm:

releases NE/Epi

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31
Q

Pheochromocytoma signs/sxs?

tx?

A

sudden-onset severe HTN, tachycardia, arrhy

Phenoxybenzamine
surgery

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32
Q

Prazosin affects what receptors?

A

⍺1 antagonist

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33
Q

Prazosin effects on ⍺1?

A

relax artery/vein smooth mm ->
↓ peripherial resistance,
↓ venous return/preload

no effect on ⍺2 means:
No ↑ CO
No tachycardia reflex
No NE increase

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34
Q

Prazosin administered?

1/2 life?

A

orally

3 hrs (doubles if CHF)

35
Q

Prazosin side-effects?

A

1st dose phenom:
ortho hypoTN/syncope 90 mins post dose

nasal congestion
ortho hypoTN, esp w/ viagra

36
Q

Prazosin used to tx?

37
Q

Other drugs similar to Prazosin?

A

Terazosin, Doxazosin

longer 1/2 lives = once daily dose

38
Q

Tamsulosin (Flomax) affects what receptors?

A

(Antagonist)
⍺1A (prostate)
⍺1B (bv)

has very little effect on BP

39
Q

Tamsulosin used to tx?

A

BPH (relaxes urinary sphincter)

low BP effects makes good alternate is “zosins” cause ortho hypoTN

40
Q

Yohimbin affects what receptors?

Causes?

A

⍺2 antagonist

↑ NE release (CNS/periphery) ->
↑ symp tone -> ↑ BP and HR

41
Q

Yohimbin used for?

A

“natural” viagra

42
Q

Yohimbin contraindications?

A

interferes w/ Clonidine

pts w/ HTN

43
Q

Short term β-Block vs long term β-block effect on BP?

A

short = ↑ BP

long = ↓ BP

44
Q

Effect of exercise/stress on HR when taking β-Block?

A

HR can’t ↑ as much

45
Q

β-block effect on EpiNE?

A

↑ pressor effect (vasoconstriction/↑ BP) due to block of 2 dilators

**don’t give for pheochromocytoma w/o ⍺-block too

46
Q

Danger of β-block effect on glycogenolysis?

A

↓ glycogenolysis masks and impairs tx of hypoglycemia

47
Q

Propranolol (Inderal) affects what receptors?

A

β1 and β2

competitive antagonist

48
Q

Propranolol effects on β1 and β2?

A 
competitive antagonist:
↓ HR, force, conduction
↓ renin
↓ glycogenolysis
↓ lipolysis
local anesthetic
49
Q

Propranolol administered?

Metabolized by?

Soluble to CNS?

A

oral but variable 1st pass metabolism (wide dosage)

liver

yes

50
Q

Propranolol used to tx?

A 
↓ mortality from MI
Angina (↓ O2 demands)
Obstructive cardiomyopathy (antiarrhythmic)
Early CHF
Migraine
stage fright
51
Q

Propranolol side-effects?

A 
Bronchoconstriction (ø asthma or COPD)
Bradycardia
Abrupt disuse -> arrhythmia (up-regulated β rec)
Worsen Late CHF
sedation, depression (CNS)
52
Q

Propranolol drug interactions?

A

drug that inhibit P450 = ↑ hypoTN
(Cimetidine, chlorpromazine)

drug that speed metabolism = ↓ effectiveness
(smoking, barbituates, rifampin)

Ca2+ channel blockers = additive effect

53
Q

Timolol affects what receptors?

A

all β

antagonist

54
Q

Timolol primary use?

A

treat glaucoma

55
Q

Timolol caution?

A

absorbed systemically so ø asthmatics

56
Q

Nadolol affects what receptors?

A

all β

antagonist

57
Q

Nadolol benefits over other non-specific β-blokers?

A

no CNS penetration
no local anesthesia
less variability of absorption
long-acting

58
Q

Sotalol affects what receptors?

A

all β

antagonist

59
Q

Sotalol benefits over other non-specific β-blokers?

A

blocks K+ channels
no local anesthetic
antiarrythmic

60
Q

Effects of β1-selective Antagonists w/o Intrinsic Sympathetic Activity?

A

Mostly heart:

↓ HR, force

61
Q

Benefits of β1-selective Antagonists w/o Intrinsic Sympathetic Activity?

A

ø block of bv dilation in skeletal mm = better exercise tolerance

less inhibition of glycogenolysis = ↓ hypoglycemia risk (safer for DM)

62
Q

β1-selective Antagonists w/o Intrinsic Sympathetic Activity use to tx?

A

HTN
Migraine prophylaxis
Post MI&raquo_space; life
Glaucoma (Betaxolol only)

63
Q

β1-selective Antagonists w/o Intrinsic Sympathetic Activity side-effects?

A

bradycardia
hypoTN
(P) develop DM II
C/I asthmatics, COPD

64
Q

β1-selective Antagonists w/o Intrinsic Sympathetic Activity drugs? (3)

A 
Metroprolol (Lopressor)
Atenolol (Tenormin)
Bisoprolol (Zebeta)
Betaxolol (Betoptic)
Nebivolol (Bystolic)
Esmolol (Brevibloc)
65
Q

Benefits of Nebivolol over other β1-selective Antagonists w/o Intrinsic Sympathetic Activity drugs?

A

↑ NO release from endo cells = vasodilator,
MOST selective for β1,
↓ arterial BP w/o depressing LV fxn,
Better ↓ of central aortic pressure,
Signification ↓ cholesterol, trigly, glucose
Fewer s/e

66
Q

Benefits of Esmolol over other β1-selective Antagonists w/o Intrinsic Sympathetic Activity drugs?

A

Very short duration (1/2 life 8 min)
IV
Use for urgent need for rapid effects

67
Q

Intrinsic Sympathetic Activity (ISA) means what?

A

PARTIAL AGONIST activity:
stim receptors when symp activity low,
reduce effects when NE/Epi is high

68
Q

β-NON-selective Antagonists with Intrinsic Sympathetic Activity (ISA) drugs?

A

Pindolol (Visken)
Carteolol (Cartrol)
Penbutolol (Levatol)

69
Q

β1-selective Antagonist w/ ISA drug?

A

Acebutolol (Sectral)

70
Q

β-Antagonists ISA drugs used to tx?

A

HTN
Angina
Glaucoma (Carteolol)

71
Q

β-Antagonists ISA drug benefits?

A

less - effects on plasma lipids?

(P) less bronchocon, bradycard

72
Q

Labetalol affects what receptors?

A

⍺1, β1, β2

blocker

73
Q

Labetalol effects on ⍺1?

β1?

A

↓ peripheral vascular resistance

prevents reflex ↑ HR (tachycardia)

74
Q

Labetalol use to tx?

A

HTN

HTN emergencies

75
Q

Carvedilol affects what receptors?

A

⍺1, β

blocker

76
Q

Carvedilol effects on ⍺1?

β?

A

↓ peripheral vascular resistance

prevents reflex ↑ HR (tachycardia)

77
Q

Carvedilol used to tx?

A

HTN
CHF
post MI

78
Q

Guanethidine (Ismelin) affects neurotransmitters how?

Method of action?

A

inhibits release of NE from terminal

replaces NE stores in vesicles

79
Q

Guanethidine effects inhibited by what type of drugs?

A

uptake inhibitors:

TSA, cocaine

80
Q

Guanethidine s/e?

A

complete loss of sympathetic activity:
severe hypoTN
↓ blood to brain/heart

81
Q

Reserpine affects neurotran how?

Results in?

A

interefers w/ uptake and storage

depletion of NE, DA, serotonin in periphery/brain

82
Q

Reserpine s/e?

A

sedation, depression, parkinson’s sxs

83
Q

Metyrosine (Demser) affects neurotrans how?

Results in?

A

blocks synthesis of DA (blocks tyrosine hydroxylase enz)

↓ NE, Epi

84
Q

Metyrosine used for?

A

pre-surg and inoperable pheochromocytoma

Q3 Pharm Cholinergics (7 decks)

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