Opiods Flashcards

1
Q

how is alfentanil supplied

A

500 mcg/mL

2mL vial

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2
Q

what are the principal uses of alfentanil

A

anesthetic induction
maintenance
monitored anesthesia care MAC

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3
Q

what is the MOA of alfentanil

A

Mu-1(supraspinal)
Mu-2(spinal)
receptor agonism

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4
Q

endogenous opioid ligand ekephalin’s receptor

A

delta

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5
Q

endogenous opioid ligand endorphin’s receptor

A

mu

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6
Q

endogenous opioid ligand dynorphin’s receptor

A

kappa

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7
Q

how do opiods work?

A

Mu-1(supraspinal)
Mu-2(spinal)
receptor agonism

inhibition of ascending transmission of nociceptive information from the spinal cord dorsal horn

activation of pain control circuits that descend from the midbrain, via rostram ventromedial medulla
to the spinal cord dorsal horn

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8
Q

mu-1 location

A

supraspinal

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9
Q

mu-2 location

A

spinal

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10
Q

mu-1 effects

A
euphoria
miosis
bradycardia
hypothermia
urinary retention
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11
Q

mu-2 effects

A

respiratory depression
constipation
physical dependence

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12
Q

potency order of opioids greatest to least

A
Sufentanil
Remifentanil-Fentanil
Alentanil
hydromorphone
Morphine
Meperidine

“Susan/Robert Formed A Happy Monique
MARS least to greatest without fent and hydro”

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13
Q

Vd of alfentanil

A

0.4-1 L/kg in adults

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14
Q

1/2 life of alfentanil

A

90-111 minutes

context sensitive 1/2 life

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15
Q

metabolism of alfentanil

A

hepatic metabolism via CYP-450
Ndealklation
glucuronide formation

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16
Q

peak of alfentanil

A

1-3 min

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17
Q

onset of alfentanil

A

60 seconds

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18
Q

duration of alfentanil

A

20 min

dose dependent

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19
Q

contraindicaions/adverse rxn alfentanil

A

hypersensitivity
N/V
chest wall rigidity

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20
Q

physiologic effects of alfentanil

A

CNS depressoin

respiratory depression

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21
Q

protein binding % of alfentanil

A

92%

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22
Q

how does acidosis/alkalosis affect protein binding?

A

protein binding increases with alkalosis

decreases with acidosis

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23
Q

Varies purpose:

Incremental injection: alfentanil

A

5-15 mcg/kg q 5-20 minutes

Max 75 assisted vent required

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24
Q

Continuous Infusion alfentanil

A

50-75 mcg/kg induction/ maintenance 1-1.5 mcg/kg/min procedure dependent

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25
Q

Induction of Anesthesia: alfentanil

A

130-245 – maintenance 0.5-1.5 mcg/kg/min *reduce concentration of inhaled agents by 30-50 for first hour

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26
Q

MAC dose alfentanil

A

3-5 mcg/kg q 5-20 min OR 0.25-1 mcg/kg/min initial dose 3-8 TOTAL dose 3-40

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27
Q

how is sufentanil supplied

A

50 mcg/mL
100 mcg/2mL
250 mcg/5mL

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28
Q

MOA of sufentanil

A

Mu-1 and Mu-2 receptor agonism

Binds to opiod receptors throughouts CNS.

Opening K channels- inhibiting Ca++ channels
Increase pain threshold

Alters pain perception

Inhibit ascending pain pathways

Inhibition of catecholamine release- controls sympathetics response to surgical stress (up to 30 mg/kg)

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29
Q

trade name of sufentanil

A

sufenta

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30
Q

protein binding % of sufentanil

A

91-93%

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31
Q

1/2 life elimination of sufentanil

A

2-4 hr

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32
Q

1/2 Context Sensative of sufentanil

A

25 min 3 hour infusion

40 min 6 hour infusion

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33
Q

metabolism of sufentanil

A

CYP3A4
liver
small intestine

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34
Q

excretion of sufentanil

A

urine

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35
Q

first pass uptake of sufentanil- pulmonary %

A

60

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36
Q

peak of sufentanil

A

5 min

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37
Q

onset of sufentanil

A

10 seconds

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38
Q

duration of sufentanil

A

30-60 minutes

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39
Q

contraindications of sufenanil

A

chest wall rigidity

hypersensitivity

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40
Q

Premed: sufenta

A

2-5 mcg

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41
Q

Induction: w/60-70% N2O sufenta

A

1.5-2.5 mcg/kg/hr

42
Q

High Dose Opiod: sufenta

A

1-30 mcg/kg induction & 1-2 mcg/kg/hr

43
Q

Balanced Anes: sufenta

A

0.1-0.3 mcg/kg bolus w/0.005-0.015 mcg/kg/min infusion

44
Q

TIVA: sufenta

A

0.25-2 mcg/kg, 2.5-10 mcg bolus, 0.5-1.5 mcg/kg/hr

45
Q

Analgesia: sufenta

A

0.1-0.3 mcg/kg or 0.0015-0.01 mcg/kg/min infusion

46
Q

MAC: sufenta

A

2.5-10 mcgbolus

47
Q

trade name of remifentanil

A

Ultiva

48
Q

MOA of remifentanil

A

binds to mu-opiod receptors within CNS
increases pain threshold
alters pain reception
inhibits asscending pain pathways

49
Q

how is remifentanil supplied

A

1 mg
2 mg
5 mg
when reconstituted is 1mg/mL

50
Q

% protein bound of remifentanil

A

70%

51
Q

High Dose Opioid: remifentanl

A

1-3 mcg/kg/min infusion w/propofol 3 mg/kg/hr

52
Q

Induction w/hypnotic: remifentanil

A

0.5-1 mcg/kg bolus 0.1-1 mcg/kg/min

53
Q

Balanced: anesthesia remifentanil

A

0.1-1 mcg/kg/min

54
Q

TIVA: remifentanil

A

1-2 mcg/kg, 0.1-1 mcg/kg bolus

55
Q

Analgesia: remifentanil

A

0.05-0.25 mcg/kg/min

56
Q

MAC remifentanil

A

12.5-25 mcgbolus or 0.01-0.2 mcg/kg/min infusion

57
Q

1/2 life context sensitive remifentanil

A

0-5 minutes

no matter how long the infusion

58
Q

half life elimination remifentanil

A

dose dependent
terminal 10-20
effective 3-20

59
Q

metabolism remifentanil

A

rapid via blood and tissue esterases

60
Q

excretion remifentanil

A

urine

61
Q

peak remifentanil

A

1-3 min

62
Q

onset remifentanil

A

60 seconds

63
Q

duration remifentanil

A

10 min

64
Q

contrainications/AE remifentanil

A

Hypersensitivity
chest wall rigidity
N/V

65
Q

trade name fentanyl

A

duragesic

sublimaze

66
Q

how is fentanyl supplied

A

100 mcg/2mL
250 mcg/5mL
500 mcg/10 mL
1000mcg/20mL

67
Q

MOA of fentanyl

A

Binds to stereospecific receptors at many sites within the CNS

Relief of pain
Pre-operative medication
Adjunt to general or regional anesthesia

68
Q

% first pass uptake by the lungs of fentanyl

A

75%

69
Q

elimination half life fentanyl

A

2-4 hours

70
Q

Context sensitive half time fentaynl

A

75 minutes

71
Q

peak fentanyl

A

5 min

72
Q

onset fentanyl

A

10 sec

73
Q

duration fentanyl- post bolus

A

30-60 min for full recovery

74
Q

contraindications/AE fentanyl

A

hypersensitivity

chest wall rigidity

75
Q

Premed: fentanyl

A

25-50 mcg

76
Q

High Dose Opiod Anes: fentanyl

A

25-50 mcg/kg induction dose with 0.5mcg/kg/min infusion

77
Q

Induction w/hypnotic fentanyl

A

1/5-5 mcg/kg

78
Q

Induction w/60-70% N2O: fentanyl

A

8-20 mcg/kg

79
Q

TIVA: fentanyl

A

5-20 mcg/kg, 25-100 mcg bolus 2-10 mcg/kg/hr

80
Q

Balanced:fentanyl

A

25-100 mcg bolus or 0.5-5 mcg/kg

81
Q

Analgesia fentanyl

A

1-3 mcg/kg bolus or 0.01-0.05 mcg/kg/min

82
Q

MAC: fentanyl

A

12.5-50 mcg bolus

83
Q

IV infusion rate fentanyl

A

10mcg/mL concentration

84
Q

trade name of naloxone

A

narcan

evzio

85
Q

how is naloxone supplied

A

0.4 mg/mL

86
Q

MOA naloxone

A

Non-specific opiod receptor competitive antagonist (mu, delta, kappa)
Pure opioid antagonist
Compete and displaces opioids at receptor sites
Greatest affinity for mu-receptor

87
Q

use of naloxone

A

Reverses opioid effects: RD, overdose, dependence, prurities, relax sphincter of Oddi spasm, urinary retention

88
Q

onset naloxone

A

2 minutes

89
Q

duration of action naloxone

A

15-45 minutes OFTEN SHORTER THAN THE HALF LIFE OF THE OPIOID- REDOSE POTENTIAL HIGH

90
Q

half life naloxone

A

0.5-1.5 hours

91
Q

excretion of naloxone

A

Urine as metabolites- adjust dose for renal pt

92
Q

metabolism naloxone

A

Primarily hepatic via glucuronidation
(inactive metabolites)

no dose adjustment with liver dz

93
Q

A/E of naloxone

A

MANY
CV- HTN, V-tach/fib, hypotension, flushing, fever
CNS- agitation/coma/pain/seizure/restless/hallucination
GI- N/V/Diarrhea crams
NMS- aches, paresthesias, piloerection, tremorn weakness
PULM- Dysp, hypoxia, pulm edema,
MISC- diaphoresis, sweating, hot flash, shiver, yawn, injection site rsn

  • withdrawal symptoms induction of sympathetic excess- catecholamines

abrubt reversal may cause acute N/V/sweat/tachy is given post op – seizures, htn, pulmonary edema and arrhythmias- caution

94
Q

concerns with naloxone

A

Renarcotization

No need with remifentanyl gtts- just turn it off

Buprenorphine- need much larger dose 2-4 mg/hr because high affinity for opioid receptor

May have methyl or propylparabens in formulation

95
Q

dilution how to &

dose for naloxone

A

0.4mg/10mL = 40 mcg/mL or 0.04 mg/mL = most common dose

96
Q

IV push: naloxone

A

1st dose= naloxone 0.04-0.4mg

repeat for effect

97
Q

Infusion for pruritis naloxone

A

= 0.25 mcg/kg/hour

98
Q

IF no response at 0.8 mg consider?

A

total consider other causes of RD

99
Q

Heroin overdose naloxone

A

0.4-2 mg/dose repeat 2-3 min for effect

100
Q

order from most lipophilic to least lipophilic (hydrophilic) or opiods

A

She F’d All My Random House Mates

Sufentanil- lipophilic
Fentanyl
Altenanil
Meperidine
Remifentanil
Hydromorphone
Morphine- hydrophils
101
Q

properties of lipophilic neuroaxial opioids

A
Rapid onset
sort duration
limited rostral spread
good for PCA
less side effects
102
Q

properties of hydrophilic neuroaxial opioids

A
prolonged single dose analgesia
cephalic spread- concern for 2nd RD 6-12 hours later
slow onset
long lasting
thoracic analgesia with lumbar admin
NOT good for PCA 
side effects