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Pharmacology I > Adrenergic Lecture > Flashcards

Adrenergic Lecture Flashcards

1
Q

what does the sympathetic nervous system control

A
  • organ systems
  • blood pressure
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2
Q

what is the NT for the SNS

A

NE

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3
Q

what is the mechanism of adrenergic transmission

A

NE starts as tyrosine (rate limiting step -> dopamine -> NE -> calcium triggers NE release and it binds

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4
Q

what is Ach broken down by and how long does it take

A
  • ACh- esterase
  • 150ms
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5
Q

how is NE broken down

A
  • has to be reuptaked
  • if it it reuptaken into where it came from then it is broken down by monoamine oxidase (MAO)
  • if it is reuptaken into post site it is broken down into Catechol-O- Methyltransferase (COMT)
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6
Q

what are the types of sympathetic agonists

A
  • direct
  • indirect
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7
Q

what are the 2 mechanisms of indirect sympathetic agonists

A
  • catecholamine displacement: amphetamines
  • decreased NE clearance through reuptake inhibition
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8
Q

what are the adrenergic receptors and what are the two types of adrenergic receptors

A
  • alpha 1 and alpha 2
  • beta 1 and beta 2
  • dopamine
  • sympathomimetic vs sympatholytic
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9
Q

when can adrenergic receptors be downregulated

A
  • CHF
  • acidosis
  • hypoxia
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10
Q

where are alpha 1 receptors located and what do they do

A
  • peripheral vascular beds
  • excitatory
  • sympathomimetic
  • vasoconstriction
  • blood pressure increased
  • mydriasis
  • urinary sphincter constriction
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11
Q

what do alpha 2 receptors do and where are they located

A
  • inhibitory
  • sympatholytic
  • in the vasculature
  • decreased sympathetic tone
  • decreased BP
  • sedation
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12
Q

what do beta 1 receptors do and where are they located

A
  • excitatory
  • cardiac excitation
  • increased rate, contractility, and conduction
  • sympathomimetic
  • the heart
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13
Q

what do beta 2 receptors do and where are they located

A
  • bronchodilation
  • smooth muscle relaxation
  • skeletal muscle vasodilation
  • decreased vascular resistance
  • sympatholytic
  • lungs
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14
Q

what does dopamine do

A
  • resistance vessel vasodilation in renal, splanchnic, coronary, and cerebral vessels
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15
Q

what are the primary catecholamines

A

dopamine and NE

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16
Q

what do catecholamines mainly do

A

excitatory and are endogenous

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17
Q

where does dopamine act

A

brain and kidney

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18
Q

where does NE act

A

sympathetic nerve endings

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19
Q

what receptors does NE bind in order of most to least

A

-alpha 1
- beta 1
- beta 2

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19
Q

what is epinephrine released from

A

ONLY the adrenal medulla

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19
Q

what are the direct acting sympathomimetics

A
  • NE
  • epi
  • dopamine
  • dobutamine
  • phenylephrine
  • milrinone
  • vasopressin
  • alpha 2 selective agonists
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20
Q

what does NE do

A
  • endogenous
  • primary NT at sympathetic nerve endings
  • maintenance of sympathetic tone- vasoconstriction
  • increased BP
  • no CO changes
  • minimal chronotropic changes
  • increased coronary blood flow
  • caution with prolonged infusions
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21
Q

what are the uses of NE

A
  • preferred vasoconstrictor
  • first line therapy for spetic shock and hypotensive after fluids are given
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22
Q

what are the receptors epinephrine binds when given exogenously at different dosese

A
  • at higher doses: alpha 1
  • at lower doses: Beta 1
  • at lower doses: beta 2
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23
Q

what does epinephrine do

A
  • endogenous
  • stress preparation
  • increased coronary blood flow
  • caution with prolonged infusions
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24
Q

what receptors does dopamine bind

A
  • mostly dopamine
  • alpha 1
  • beta 1
  • beta 2
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25
Q

describe dopamine

A
  • endogenous
  • NE precursor
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26
Q

what are the dose specific effects of dopamine

A
  • low dose (0.5-3mcg/kg/min)
  • intermediate (3-10mcg/kg/min) : increases BP
  • high (10-20 mcg/kg/min)
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27
Q

what are the receptors that dobutamine binds in order of greatest to least

A
  • beta 1
  • beta 2
  • alpha 1
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28
Q

describe dobutamine

A
  • synthetic
  • augments myocardial contractility
  • dose dependent increase in stroke volume and cardiac output
  • alpha agonist and antagonist
  • beta mediated vasodilation (low dose)
  • high dose increases myocardial O2 consumption
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29
Q

what are the uses for dobutamine

A
  • low dose: decreases BP
  • mid range: increases ionotropy
  • high doses: increases O2 consumption, vasoconstriction
  • cardiogenic shock- usually combined with NE
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30
Q

what receptor does phenylephrine bind to

A

alpha 1

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31
Q

describe phenylephrine and what it does

A
  • synthetic
  • all alpha no beta
  • not a catechol derivative, not metabolized by COMT
  • metabolized by MAO
  • can lead to baroreceptor mediated decrease in HR
  • push dose pressor
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32
Q

what is phenylephrine used for

A
  • transient hypotension
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33
Q

what receptor effect does milrinone have order of greatest to least

A
  • B1
  • B2
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34
Q

what does milrinone do

A
  • phosphodiesterase-3 inhibitor
  • inhibits breakdown of cAMP- positive inotropy
  • potent vasodilator
  • increased diastolic relaxation- reduced preload and afterload
    -good in the setting of receptor downregulation
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35
Q

what is milrinone used for

A

in patient with heart failure without hypotension

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36
Q

what receptor does vasopressin mimic and what is another name for it

A
  • alpha 1
  • ADH
37
Q

what are the direct acting sympathomimetics that dont directly bind the receptor they just mimic their effects

A

milrinone and vasopressin

38
Q

where is vasopressin stored and when is it released

A

stored in posterior pituitary and released when plasma osmolarity increases or BP drops

39
Q

what does vasopressin do

A
  • V1 and V2 receptor agonist
  • neutral to negative impact on CO
  • dose dependent SVR and vagal tone increase
  • not affected by pH
40
Q

what is vasopressin used for

A

septic shock with acidosis
- 3rd or 4th line of treatment for BP control

41
Q

what are the alpha 2 selective agonists

A
  • clonidine
  • dexomedetomidine
  • guanfacine
  • methyldopa
42
Q

what do alpha 2 selective agonists do

A
  • drop BP by reducing sympathetic tone
  • effective antihypertensive
  • sedation
43
Q

what does clonidine used for

A
  • 2nd line anti-hypertensive
  • used in pain
  • used in opioid and nicotine withdrawals
44
Q

what is dexmedetomidine used for

A

same as clonidine but doesnt have BP effects

45
Q

what is guanfacine used for

A

ADHD

46
Q

what is methyldopa used for

A

drug of choice with HTN during pregnancy

47
Q

what is the downside of long term use of alpha 2 selective agonists in dentistry

A

can lead to oral candidiasis and increased risk of dental caries due to decreased salivary gland activity

48
Q

what are the 2 mechanisms of indirect acting sympathomimetics

A
  • displacers
  • reuptake inhibition
48
Q

what are the indirect acting sympathomimetics

A
  • amphetamine like agents: amphetamine, methylphenidate (ritalin), modafinil(provigil)
  • catecholamine reuptake inhibitors: straterra, cocaine
49
Q

describe amphetamines

A
  • rapid CNS uptake
  • stimulant
  • effects mediated by NE and DA
50
Q

describe methylphenidate( ritalin), what is it used for and what is the caution

A
  • amphetamine variant
  • similar effect and abuse potential
  • use: ADD spectrum
  • caution: UDS
51
Q

describe modafinil (provigil), its mechanism, what it does and its use

A
  • psychostimulant
  • NE, DA reuptake inhibition
  • NE, DA, 5-HT3, glutamate increase, GABA decrease
  • use: narcolepsy
52
Q

describe straterra and its use

A
  • selective NE reuptake inhibition
  • no CV effects- clonidine like effect
  • Use; ADD
53
Q

describe cocaine and what it is used for

A
  • local anesthetic, peripheral sympathomimetic
  • reuptake inhibition especially dopamine
  • use: epistaxis
54
Q

what can excessive cocaine use cause

A

excited delirium which manifests as aggression followed by respiratory or cardiac arrest

55
Q

what should you avoid with cocaine use

A

concurrent beta blockade

56
Q

describe beta-2 agonism

A
  • key to management of acute asthma
  • common allergy in dentistry is actually asthma 7.9% of the time
  • triggered by allergens, stress, food and drugs
57
Q

what drugs are used for short term control of asthma

A
  • short acting beta agonists (SABA)
  • albuterol
  • levalbuterol
  • terbutaline
58
Q

what is used for long term control of asthma

A
  • long acting beta agonists (LABA)
  • formoterol
  • salmeterol
59
Q

how long go LABA drugs work

A

12-18 hours

60
Q

LABA drugs must be used with:

A

steroids

61
Q

what is advair made of

A

salmeterol + fluticasone

62
Q

what is symbicort made of

A

formoterol + budesonide

63
Q

what is dulera made of

A

formoterol + mometasone

64
Q

what is the protocol for patient management with asthma in the dental settign

A
  • minimize likelihood of exacerbation
  • talk to your patient to learn their management strategies
  • instruct patient to bring albuterol inhaler to all appointments
  • decrease stressors
  • drug considerations
65
Q

what are the drug considerations in patients with asthma

A
  • no ASA or NSAIDs
  • avoid histaminic drugs
  • avoid antihistamines
  • avoid cholinergics
66
Q

what do you do in an emergency with an asthma patients

A
  • supplemental O2 immediately
  • consider epi: 0.3mg IM or use epipen
67
Q

what are the two types of alpha receptor antagonists

A
  • reversible and irreversible
68
Q

describe reversible alpha receptor antagonists

A
  • concentration dependent
  • duration dependent on half life
69
Q

describe irreversible alpha receptor antagonists

A
  • body has to regenerate new receptors
  • drug effect can persist even after drug is cleared
  • longer recovery process
70
Q

what are the pharmacologic effects of alpha antagonists

A

-cardiovascular: alpha 1 blockade blocks vasoconstriction, orthostatic hypotension
- miosis, nasal stuffiness
- decreased resistance to urinary flow

71
Q

what are the alpha receptor antagonist drugs

A
  • phentolamine
  • prazosin, terazosin, doxazosin
  • tamsulosin
72
Q

what does phentolamine do

A
  • blocks alpha 1 and alpha 2
  • decreased PVR and cardiac stimulation
  • can lead to CV adverse reactions
73
Q

what are the uses of phentolamine

A
  • pheochromocytoma
  • mainly used for extravasation reactions
74
Q

what do prazosin, terazosin and doxazosin do and what are they used for

A
  • selective alpha 1
  • arterial and venous vascular smooth muscle relaxation and prostate relaxation
  • 50% bioavailability- first pass effect
  • use: BPH
75
Q

what drugs cause orthostatic hypotension

A
  • prazosin
  • terazosin
  • doxazosin
76
Q

what does tamsulosin do

A
  • competitive alpha 1 blocker
  • high bioavailability
  • more specific to prostate
  • less orthostatic hypotension
77
Q

what is tamsulosin used for

A

best drug for BPH

78
Q

what do beta receptor antagonists do

A
  • antagonize effects of catecholamines and beta agonists
  • differ in affinity for beta 1 and beta 2
  • beta 1 specificity decreases as dose increases
  • end in -lol
79
Q

what receptors do beta blockers ending in -olol act on

A

beta receptors only

80
Q

what receptors do beta blockers ending in -ilol act on

A

mostly beta and some alpha receptors

81
Q

what receptors do beta blockers ending in -alol act on

A

mostly beta and some alpha receptors

82
Q

what affinities do labetalol and carvedilol have

A

B1 = B2 > alpha 1 > alpha 2

83
Q

what affinities do metoprolol, betaxolol, acebutolol, esmolol, atenolol, nebivolol have

A

B1&raquo_space;» B2

84
Q

what affinities do propanolol, carteolol, penbutol, pindolol and timolol have

A

B1 = B2

85
Q

what are the beta specific beta antagonists - “be a man”

A
  • Betaxolol
  • Esmolol
  • Acebutol
  • Metoprolol
  • Atenolol
  • Nebivolol
86
Q

describe esmolol

A
  • beta 1 selective
  • short half life
  • quick onset
  • requires central line for administration
  • great for tight BP control
  • used for aortic dissection
87
Q

describe labetalol

A
  • beta and alpha blockade
  • 3:1 ratio orally
  • 7:1 ratio Iv
  • dose dependent duration of action- up to 20 hours
88
Q

what beta blocker drugs are safer for asthmatic patients

A

beta 1 specific

89
Q

caution with non specific beta blockers and:

A

epi

90
Q
A

Pharmacology I (12 decks)

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