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Pharmacology > ANS > Flashcards

ANS Flashcards

1
Q

M1

  • cholinergic/adrenergic
  • location
  • mechanism
  • 2nd messenger
  • Action
A
  • cholinergic
  • nerve endings
  • Gq
  • increased IP2 and DAG
  • activate myenteric plexus
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2
Q 
M2
 cholinergic/adrenergic
- location
-mechanism
-2nd messenger
-Action
A

-cholinergic
-heart, some nerve endings
-Gi
-decreases cAMP, activates K+ channels
Slows SA node

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3
Q

M3

  • cholinergic/adrenergic
  • location
  • mechanism
  • 2nd messenger
  • Action
A
  • cholinergic
  • smooth muscle, glands, endothelium
  • Gq
  • increased IP3, DAG cascade
  • contract detrusor, increase salivation
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4
Q

Nn

  • cholinergic/adrenergic
  • location
  • mechanism
  • 2nd messenger
  • Action
A
  • cholinergic
  • ANS ganglia
  • Na-K ion channel
  • Na
  • Depolarizes postgang fiber, evokes AP
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5
Q

Nm

  • cholinergic/adrenergic
  • location
  • mechanism
  • 2nd messenger
  • Action
A
  • cholinergic
  • neuromuscular plate
  • Na-K ion channel
  • Na
  • depolarizes muscle cell and evokes AP and contraction
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6
Q

A1

  • cholinergic/adrenergic
  • location
  • G protein
  • 2nd messenger
  • Action
A
  • adrenergic
  • smooth muscle (especially vasculature) , glands
  • Gq
  • increase IPR, DAG
  • increase Ca and causes contraction of vascular SM and/or secretion from glands
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7
Q

A2

  • cholinergic/adrenergic
  • location
  • G protein
  • 2nd messenger
  • Action
A
  • adrenergic
  • nerve endings and some smooth muscle
  • Gi
  • decrease cAMP
  • decrease transmitter release in the nerve and decrease contraction in smooth muscle
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8
Q

B1

  • cholinergic/adrenergic
  • location
  • G protein
  • 2nd messenger
  • Action
A
  • adrenergic
  • cardiac muscle and JGA
  • Gs
  • increase cAmP
  • increase HR and contractility and renin release
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9
Q

B2

  • cholinergic/adrenergic
  • location
  • G protein
  • 2nd messenger
  • Action
A
  • adrenergic
  • smooth muscle, liver,heart
  • Gs
  • increase cAMP
  • relax bronchiolar smooth muscle; increase glycogenolysis; increase HR and contractility
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10
Q

B3

  • cholinergic/adrenergic
  • location
  • G protein
  • 2nd messenger
  • Action
A
  • adrenergic
  • adipose cells
  • Gs
  • Increase cAMP
  • increase lipolysis
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11
Q

Dopamine

  • cholinergic/adrenergic
  • location
  • G protein
  • 2nd messenger
  • Action
A
  • adrenergic
  • smooth mucle
  • Gs
  • increased cAMP
  • relax vasculature in renal arterioles
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12
Q

Phenylephrine Description

A

synthetic alpha receptor agonist that is most selective for a1

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13
Q

Phenylephrine Action

A

vaso and venoconstriction by stimulating contraction of vascular smooth muscle

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14
Q

Phenylephrine Indications (3)

A

Nasal decongestant
Mydriatic (pupil dilator)
increased BP in vasodilator state

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15
Q 
Other facts about phenylephrine
(3)
-potency compared to Norepi
-deactivation
-routes
A

less potent than norepi
not deactivated by COMT
can be given topically and IV

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16
Q

Clonidine short card info

Description

A

-selective A2 agonist

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17
Q

Clonidine short card Action

A

stimulate a2 in brianstem, causes down regulation of sympathetic nervous system

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18
Q 
Clonidine indications (short card)
(2)
A

treat hypertension

treat migraine

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19
Q

Clonidine other facts

  • route
  • side effects
  • overdose effect
A
  • orally or patch
  • sedation/ dry mouth
  • if given IV or OD can cause high BP
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20
Q

Phenylephrine brand name

A

Neosynephrine

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21
Q

Clonidine brand name

A

Catapres

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22
Q

Isoproterenol brand name

A

Isuprel

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23
Q

Isoproterenol description

A

B1/B2 receptor agonist

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24
Q

isoproterenol actions

A

potent b1/b1 agonist

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25
Q

isoproterenol indications

3

A

increase cardiac contractility
increase HR
increase cardiac conduction

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26
Q

isoproterenol other facts

  • route
  • why isn’t it used so much
  • what else does it cause
A
  • iv
  • no longer used in CCu b/c can cause tachyarrhythmias like V-tach
  • also causes vasodilation
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27
Q

Dobutamine trade name

A

Dobutrex

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28
Q

Dobutamine description

A

synthetic B1 receptor agonist

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29
Q

dobutamine action

A

potent b1 agonist in heart (increases contractility more than HR) and blood vessels (dilates renal and mesenteric vessels)

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30
Q 
dobutamine indications
(2)
A
  • increase cardiac contractility more than HR

- Use for in CCU for patients in cardiogenic shock where you do not want tachycardia (i.e. most MI)

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31
Q

dobuatmine other facts

  • route
  • side effects (3)
A

-IV

tachy, hypertension, ectopy

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32
Q

albuterol trade name

A

ventolin

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33
Q

albuterol description

A

synthetic b2 selective receptor agonist

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34
Q

albuterol actions

A

b2 agonist: receptors on smooth muscle cells in airways and uterus and relaxes above tissues

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35
Q

albuterol indications (2)

A

prompt acting rescue inhaler for asthma, COPD

and inhibits premature labor

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36
Q

albuterol other facts

  • most often given as..
  • other route
  • what’s the deal w/ IV
  • side effects (3)
A
  • metered dose inhaler
  • nebulizer
  • rarely given as iv infusion
  • anxiety, tachy, tremor
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37
Q

Mirabegron trade name

A

Myrbetriq

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38
Q

Mirabegron Description

A

selective B3 agonist

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39
Q

Mirabgeron action

A

stimulates b3 receptors in smooth muscle of bladder, reduces detrusor muscle tone

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40
Q

Mirabegron indications

A
  • treatment of patients w/ overactive bladder with features of urinary urgency/frequency
  • inreases bladder capacity
  • does not produce bothersome anticholinergic symptoms like tolteridine
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41
Q

other facts about mirabegron

2

A

approved in June 2012

administered orally as extended release tablets

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42
Q

Methoxamine description

A

alpha 1 and 2 agonist

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43
Q

Epinephrine tradename/ and one other name

A

EpiPen

Adrenaline

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44
Q

Epinephrine Drug class

  • pharmacologic
  • therapeutic
A
  • pharm: direct acting adrenergic agonist

- Therapeutic: vasopressor, cardiac stimulant, bronchodilator, adjunct to local anesthetics, treatment for anaphylaxis

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45
Q

Epinephrine Pharmacodynamics

A

major action is to stimulate a1 adrenoreceptors to cause vasoconstriction and venoconstriction; stimulate b1 receptors for tachycardia and increased contractility ; b2 for bronchodilation–these actions are helpful in severe allergic runs by stabilizing mast cells (b1/b2)

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46
Q

Epi Pharmacokinetics

  • route(4)
  • metabolism
A

can be given IV (immediate), IM variable , SC (5-15 min), via inhalation (1-5 min onset) , opthalmic topical
- metabolized by COMT and then renally excreted

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47
Q

Epi Toxicity (5)

A 
excessive vasoconstriction
HTN
hemorrhagic stroke
angina
arrhythmias
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48
Q

Epi Interactions

A

risk of excessive hypertension in patents taking propranolol

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49
Q

Epi special considerations (2)

A

utility w/ local anesthetics

drug of choice in severe anaphylactic runs (along w/ others)

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50
Q

Epi indications and dose/route

3

A

for anaphylaxis: 0.1-0.5 mg SC or IM
for cardiac arrest: 1-5 mg IV push
for infusion 1-4 mcg/min

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51
Q

Epi : things to monitor (5)

A 
BP
HR
rhythm
infusion site
evidence of extravasation
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52
Q

Norepinephrine trade name/ one other name

A

Levophed

noradrenaline

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53
Q

norepi drug class

  • pharm
  • therapeutic
A

pharm- direct acting adrenergic agonist

therapeutic- vasopressor, vasoconstrictor

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54
Q

Norepi pharmacodynamic

A

major action is to stimulate a1 adrenorecpetors to increase vasoconstriction and venoconstriction. This increases CO, SVR, and MAP, but decrease blood flow to vulnerable tissues like skin, muscle, and kidney
also stimulates b1 in heart, increasing HR and contractility. Main effects are vasoconstriction and cardiac stimulation

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55
Q

Norepi Toxicity

2

A

excessive vasoconstriction in mesenteric vessels, peripheral arterioles causing ischemia, infraction, gangrene, reflex brady

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56
Q

Norepi interactions

A

use cautiously in peeps takin MAO inhibitors like phenlzine;
risk of excessive hypertension in peeps taking propranolol

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57
Q

Norepi special considerations

3

A

correct volume depletion before giving NE
select infusion site carefully-extravasation is a major problem; monitor patent and BP continuously in ICu; use cautiously in ped and geriatric patients

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58
Q

Norepi Indications and dose/route

A

for adults with acute hypotension and shock related to low SVR
infuse 2-12 mcg/min

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59
Q

norepi things to monitor (4)

A

BP
HR
infusion site
extravasation

60
Q

Dopamine trade name

A

intropin

61
Q

dopamine descrption

A

agonist at DA, B1, and a1 receptors

62
Q

dopamine actions

A

relative potency depends on dose being delivered; DA agonist at low dose, B1 agonist at medium dose; a1 agonist at high dose

63
Q

Dopamine indications (2)

A

shock of various etiologies in ICu
can produce increased contractility (B1)
vasoconstriction (a1) and improve mesenteric and renal perfusion (DA)

64
Q

Dopamine Other facts

-route

A

given IV , preferably for a short period of time

65
Q

Norepi pharmacokinetics

A 
F~ 100%
Given IV only
metabolized by comt and mao in liver
metabolites excreted in urine
half life is 1-2 minutes
can cross placenta, but not BBB
66
Q

Ephedrine description

A

Alkaloid obtained from plants

67
Q

Ephedrine action

A

acts inertly to release NE from adrenergic nerve endings, also some direct agonism at receptors

68
Q

Ephedrine Indications (2)

A

Mild to moderate hypotension during surgery (very fast acting)
Nasal decongestion

69
Q

other facts about ephedrine

  • duration of action
  • potent stimulant of what
  • side effects (2)
  • FDA status
A
  • somewhat prolonged action
  • potent CNS stimulant
  • side effects = hypertension and insomnia
  • OtC banned by FDA
70
Q

Pseudoephedrine description

A

synthetic derivative of ephedrine

71
Q

actions of pseudoephedrine

A

acts indirectly to release NE from adrenergic nerve endings, and some direct agonism at alpha and beta adrenergic receptors

72
Q

pseudoephedrine indications

A
  • nasal and sinus decongestant

- less ability to dilate bronchioles than ephedrine

73
Q

other fact about pseudo ephedrine

  • when approved
  • what year were bulk sales reported
  • what year increased security
  • what year labeled as risk of injury/death or no cold products for kids
A
  • 1959
  • 1996
  • 2005
  • 2008
74
Q

Amphetamine description

A

synthetic compound similar to ephedrine

75
Q

amphetamine actions

A

acts indirectly to release NE from adrenergic nerve endings

76
Q

amphetamine indications

A
  • none are FDA approved
  • obesity
  • narcolepsy
  • ADHD
77
Q

amphetamine other facts

  • approval
  • risk of dependence
  • side effects
A
  • 1939
  • high risk of dependence
  • insomnia, restlessness, tremor
78
Q

Tyramine description

A

naturally occurring byproduct of tyrosine metabolism; present in fermented food

79
Q

tyramine actions

A

indirectly releases NE from adrenergic nerve endigns

80
Q

tyramine indications

A

none are FDA approved

  • obesity
  • narcolepsy
  • ADHD
81
Q

tyramine other facts

  • metabolized by what enzyme
  • what kind of patients should be watched out for
  • what is a common interations
A
  • MAO
  • patients on MAOIs
  • food/drug
  • MAOI+ food= hypertensive crisis
82
Q

Cocaine description

A

purifed alkaloid extract from coca plant

83
Q

cocaine actions

A

indirectly blocks reuptake of NE, Epi, and DA, and can stimulate release of Ne, Epi, and DA
can also sat as local anesthetic and CNS stimulant

84
Q

indications (2)

A
  • nose bleeds (anesthesia plus vasoconstriction)

- anesthesia for corneal surgery

85
Q

other facts about cocaine

  • effects compared to amphetamine
  • routes
  • side effects (5)
A

more intense, longer lasting
smoked, snorted, injected
HTN, tachy, arrhythmias, seizures, MI

86
Q

Prazosin Trade name

A

Minipress

87
Q

Prazosin Drug class

  • pharmacologic
  • therapeutic
A
  • selective alpha 1 adrenoreceptor blocker

- antihypertensive, treatment of BPH

88
Q

Prazosin pharmacodynamics

A

blocks alpha 1 receptors on arterioles and veins, thereby inhibiting NE-mediated faso and venoconstriction

89
Q

Prazosin pharmacokinetics

  • route
  • bioavailability
  • onset
  • duration
  • where is it metabolized
A

available po or transdermal

variable oral bioavailability (~60%) , onset 2h, duration 12-24h; extensively metabolized in liver

90
Q

Prazosin Toxicity

A

excessive hypotension with syncope, especially orthostatic, especially in patients on diuretics

91
Q

Prazosin Interactions

A

additive effects w/ most other antihypertensives, especially diuretics

92
Q

Prazosin special considerations

2

A

start gradually, and at bedtime, to avoid first time passing out; male patients w/ BPH?

93
Q

Prazosin indications and dose/route

A

as mono therapy begin with 1 mg tid, advance to 20mg per day divided tie

94
Q

Prazosin monitor

A

BP, weight, edema

95
Q

Tamsulosin tradename

A

Flomax

96
Q

Tamsulosin cost

A

5-70 $ per month

97
Q

Tamsulosin drug class

  • phram
  • therapeutic
A

selective a1blocker

treatment of obstructive symptoms of BPH

98
Q

Tamsulosin pharmacodynamics

A

selectively blocks a1 receptors, but preferentially in the prostate, leading to relaxation of smooth muscles in the bladder neck and prostate, improving urine flow, and reducing obstructive symptoms of BPH venoconstricton

99
Q

Tamsulosin Pharmacokinetics

  • how much is absorbed
  • what % metabolized by CYP 450 enzymes
  • half life
  • duration of action
A

completely absorbed after oral ingestion; >90% metabolized by CYP 450 enzymes
half life about 6 hrs, but duration of action up to 15 hours due to slow absorption

100
Q

Tamsulosin Toxicity (3)

A

excessive hypotension with syncope, especially orthostatic, especially in patients on diuretics,allergic rxns, decreased libido

101
Q

Tamsulosin Interactions

A

additive effects w/ most antihypertensives, especially diuretics

102
Q

Tamsulosin special considerations (3)

A
  • rule out carcinoma of prostate before beginning treatment
  • do not crush or chew tablets, as that wills speed up absorption;
  • can ask be used to treat spasm of ureter in patients with kidney stones
103
Q

Tamsulosin Indications and dose/route

A

for symptoms of BPH, 0.4 mg po qd or bid; similar doses for renal colic

104
Q

Tamsulosin monitor

A

BP

105
Q

Prazosin cost

A

4-20 $ per month

106
Q

Phentolamine trade name

A

Regitine

107
Q

Phentolsamine Drug class

  • pharm
  • therapeutic
A
  • non-selective competitive alpha adrenergic receptor blocker
  • antihypertensive drug for patents w/ pheochromocytoma
108
Q

phentolamine pharmacodynamics

A

blocks a1/a2 adrenergic receptors and presynaptic and post synaptic alpha receptors , decreasing preload and after load

109
Q 
phentolamine/regitine
pharmacokinetics 
- route 
-F
- plasma half-life
A

only comes in IV formulations, so F=100%; plasma half-life about 20 min after IV dose

110
Q

phentolamine/regitine toxicity (3)

A
  • excessive hypotension w/ syncope especially orthostatic, especially in patients on diuretics;
  • allergic rxns;
  • decrease libido
111
Q

phentolamine interactions

A

additive effects w/ most other antihypertensives, especially diuretics

112
Q

phentolamine special considerations

3

A
  • rule out carcinoma of prostate before beginning treatment
  • do not crush or chew tablets, as that wills speed up absorption;
  • can ask be used to treat spasm of ureter in patients with kidney stones
113
Q

phentolamine indications and dose/route

-indications (4

A
  • Aid Dx of pheo
  • treatment of intraop HTN during pheo removal surgery
  • prevention of dermal slugging after extravasation of NE infusion
  • hypertensive crisis from sympathomimetic amines
  • Dose 5 mg IV, then titrate
114
Q

phentolamine/regitine monitor

A

BP

115
Q

Atenolol brand name

A

Tenormin

116
Q

Atenolol similar drugs (2)

A

metroprolol

Toprol XL

117
Q

atenolol class price range

A

4/52 to $100 for Toprol XL

118
Q

Atenolol/Tenormin

  • pharm
  • therapeutic (4)
A
  • specific b1 blocker

- antihypertensive, anti arrhythmic, primary and secondary prevention of MI, anti anginal

119
Q

Atenolol/Tenormin pharmacodynamics

A

binds directly to B1 receptors w/ preference for beta-1 –leads to lower bP via several potential mechanisms; recent evidence suggests less effective in preventing strokes than other drugs

120
Q

Atenolol/ Tenormin pharmacokinetics

  • route
  • F
  • onset
  • duration
  • how many times/ day
  • how excreted
  • metroprolol metabolism
A
  • po/iv
  • variable
  • onset 1-2 hrs
  • durations 12-24h
  • can be given once per day
  • renally excreted (so has longer half life)
  • metoprolol has hepatic metabolism so has shorter half life
121
Q

Atenolol/ Tenormin Toxicity

5

A
  • excessive hypotension
  • bradycardia
  • heart block
  • can worsen severe cHF (but indicated for mild/moderate/stable CHF)
  • worsen bronchospasm in severe asthmatics
122
Q

Atenolol/Tenormin Interactions

A
  • additive effects w/ most other anti-hypertensives

- additive AV block with CEBs (calcium entry blockers)

123
Q

Atenolol/Tenormin Special Considerations

A

may be especially useful in HTN patients w/ exertional angina, MI, A fib
watch out for abrupt withdrawal
metoprolol has more data for use in patents s/p MI

124
Q

Atenolol/Tenormin Inidcations and dose/route

A

for HTN patients

25-100 mg per day in one or two doses

125
Q

Atenolol/Tenormin monitor (3)

A

BP HR exercise

126
Q

Propranolol trade name

A

Inderal

127
Q

Propranolol/Inderal drug class

  • pharm
  • therapeutic (4)
A

-non specific B blocker
-antihypertensive, antiarrhythmic, primary and secondary prevention of MI
; anti-anginal

128
Q

Propranolol/Inderal cost

A

4$ up to $180

129
Q

Propronalol/Inderal pharmacodynamics

A

binds to B1/B2 receptors leading to lower BP via several potential mechanisms; recent evidence suggests less effective in preventing strokes than other drugs

130
Q

Propranolol/Inderal Pharmacokinetcs

  • route
  • F
  • onset
  • duration
  • how often given / day
  • how cleared/metabolized
A 
availabel po or iv
variable F
onset 1-2 hrs
duration: 12-24h
can be given once per day
cleared by hepatic metabolism
131
Q

Propranolol/Inderal Toxicity

-4

A

excessive hypotension; brady; heart block can worse severe CHF (but indicated for mild/moderate/stable CHF; worsen bronchospasm in severe asthmatics

132
Q

Propranolol/Inderal Interactions

A
  • additive effects w/ most other anti-hypertensives

- additive AV block with CEBs (calcium entry blockers)

133
Q

Propranolol/Inderal Special considerations

A

may be especially useful in HTN patients w/ exertional angina, MI, A fib
watch out for abrupt withdrawal
metoprolol has more data for use in patents s/p MI

134
Q

Propranolol/Inderal indications and dose/route

A

for HTN patients

25-100 mg per day in one or two doses

135
Q

Propranolol/Inderal

Monitoring

A

BP, HR, exercise tolerance

136
Q

Labetalol brand name

A

Trandate

137
Q

Labetalol/Trandate similar drugs

A

carvedilol/Coreg (brand name)

138
Q

Labetalol class cost

A

$4 (carvedilol) to $24 per month

139
Q

Labetalol/Trandate drug class

  • pharm
  • therapeutic
A

mixed a/b blocker

therapeutic- antihypertensive, treatment of stable CHF (corey)

140
Q

Labetalol/Trandate Pharmacodynamics

A

reduce BP by blocking b/a receptors and thereby lowering BP by several different mechanisms; patents differ in degree of beta and alpha blockade

141
Q

Labetalol/Trandate Pharmacokinetics

  • absorption
  • F
  • onset
  • metabolism: where/which enzyme
A

-excellent absorption but high first pass effect leading to F~25%
onset 1-2 hours after po
2-5 minutes when given IV
- extensively metabolized by liver 2D6

142
Q

Labetalol/Trandate Toxicity

  • avoid in ( 5)
  • cautious use (3)
A 
avoid in patients with brady, heart block, cHF, asthma, shock
-use cautiously in patients with cardiomyopathy, pheochromocytoma, or pregnancy class D
143
Q

Labetalol/Trandate Interactions

A

additive effect with most antihypertensives

144
Q

Labetalol/Trandate Special considerations

  • liver fxn
  • most troubling side effect
  • most often used in which situation
A
  • use reduced doses w/ reduced liver fxn
  • dizziness is most troubling side effect
  • most often used for HTN crisis
145
Q

Labetalol/Trandate Indications and dose/route

  • most common
  • chronic treatment
A

most commonly given IV with small initial boluses of 20 mg, followed by continuous infusion at 2 mg/min
not usually given po for chronic treatment
80 mg thrice daily, or 240 mg SR (sustained release) once daily

146
Q

Labetalol/Trandate Monitor (2)

A

BP, HR

Pharmacology (9 decks)

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