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Pharm Fall 2019 > Ex1 Opioids Slides > Flashcards

Ex1 Opioids Slides Flashcards

1
Q 
Rate the following from highest to lowest potency:
Meperidine
Alfentanil
Remifentanil
Sufentanil
Fentanyl
Morphine
A

Sufentanil > (Fentanyl/remifentanil) > alfentanil > morphine > meperidine

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2
Q

Morphine and codeine are in what class of opioids?

A

Opium alkaloids - phenanthrenes

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3
Q

Fentanyl is in what class of opioids?

A

Synthetic phenylpiperidines

Same with sufentanil, alfentanil, remifentanil, meperidine

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4
Q

What class is hydromorphone in?

A 
Semisynthetic opioids (simple substitution to the morphine molecule)
Along with oxycodone, buprenorphine
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5
Q

Opioid receptors are primarily responsive to ___ _________ ligands

A

3 endogenous

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6
Q

Delta receptor endogenous ligand

A

Enkephalin

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7
Q

Mu receptor endogenous ligand

A

Beta Endorphin

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8
Q

Kappa receptor endogenous ligand

A

Dynorphan

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9
Q

Opioids activate what system?

A

Pain modulating (anti-nociceptive) systems

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10
Q

The ________ form gains access to the CNS most easily

A

Non-ionized

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11
Q

The _______ form binds to the receptor

A

Ionized

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12
Q

_________ correlates with potency

A

Receptor affinity

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13
Q

MOA opioids:

Opioid receptors are present on they peripheral ends of __________ neurons

A

Primary sensory

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14
Q

Opioid receptors when activated result in ________ neurotransmission and/or __________ inhibit the release of ________ neurotransmitters

A

Decreased
Release
Excitatory

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15
Q

What would the ideal opioid agonist have?

A

High specificity/hi potency (affinity)

No specificity for receptors producing adverse effects

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16
Q

Opioid receptors inhibit ________ which decreases ________

A

Adenyl Cyclase
CAMP
Results in hyperpolarization of cell

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17
Q

Mu1 receptor effects

A 
Analgesia (Supra and spinal)
Euphoria
Low abuse potential
Miosis
Bradycardia
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18
Q

Mu2 Receptor effects

A

Analgesia (spinal)
Depression of ventilation
Physical dependence
Constipation

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19
Q

Kappa receptor effects

A 
Analgesia (supraspinal and spinal)
Dysphoria**
Sedation
Low abuse potential
Miosis
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20
Q

Delta receptor effects

A

Analgesia (supraspinal and spinal)
Depression of ventilation
Physical dependence**

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21
Q

Opioids effect the CO2 response curve by ?

A

Response curve shifts to the right

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22
Q

Morphine produces

A

Analgesia, euphoria, sedation, decreased ability to concentrate, nausea, dry mouth, pruritis

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23
Q

Morphine is effective against which pain?

A

Visceral, skeletal, joint pain

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24
Q

Morphine CV side effects

A

Decreased SNS tone
Decreased HR
Histamine release

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25
Q

Morphine respiratory effects

A

Depression of ventilatory centers in medulla
Decreased responsiveness to CO2
Decreased RR, increased VT

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26
Q

Morphine CNS effects

A

Decreased CBF, CMRO2, ICP

Skeletal muscle rigidity

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27
Q

Morphine side effects - etc

A

Spasm of biliary smooth muscle - may mimic pain of angina pectoris
Tx = naloxone, glucagon, nitroglycerin

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28
Q

Morphine side effects - GI

A

Spasm of GI smooth muscle

N/V - d/t direct stimulation of the CTZ in the Post-Rema, floor of the 4th ventricle

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29
Q

Morphine withdrawal - occurs in _______ hours
Peaks in ________
Remission in _________

A

Occurs within 15-20h
Peaks 2-3D
Remission 10-14d

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30
Q

Symptoms of morphine withdrawal

A

Yawning, lacrimation, diaphoresis, abd cramps, N/V, diarrhea

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31
Q

Clinical uses for Meperidine

A

Post op analgesia, L&D analgesia, PCA for postop, treatment of shivering

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32
Q

Meperidine unique side effects

A

Increased HR, decreased myocardial contractility with large doses

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33
Q

Meperidine should not be given with

A

MAOIs

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34
Q

Meperidine interactions - Type I response

A

Excitatory

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35
Q

Meperidine interactions - type II response

A

Depressive - hypotension/vent depression/coma

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36
Q

Meperidine use with caution in ppl taking ______

A

TCAs

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37
Q

Fentanyl has a _____ time to onset than morphine

A

More rapid (2min)

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38
Q

Fentanyl has a _______ duration of action than morphine

A

Shorter

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39
Q

Fentanyl - ____% of single dose undergoes __________ uptake

A

76%
First pass pulmonary uptake
*pulmonary tissue serves as a depot for release back into circulation

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40
Q

Time to peak effect of fentanyl in adults

A

5-7 minutes

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41
Q

Fentanyl - time to peak effect in peds

A

5 minutes

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42
Q

Advantage of fentanyl

A

Cardiac stable

Does not produce direct myocardial effects, no histamine release

43
Q

Pre induction dose of fentanyl

A

1-5 mcg/kg

44
Q

Fentanyl dose - analgesia for sedation

A

1-2 mcg/kg IV

45
Q

What is more profound in fentanyl than in morphine?

A

Bradycardia

46
Q

Why is there persistent ventilatory depression when fentanyl is given?

A

Saturation of inactive sites - context sensitive half time

47
Q

Alfentanyl is used for

A

Transient, acute pain d/t rapid onset/short duration

48
Q

Alfentanil dose blunt catecholamine and BP response

A

30mcg/kg IV

49
Q

Alfentanil dose for unconsciousness

A

150-300mcg/kg IV

50
Q

Balanced anesthesia - alfentanil dose

A

25-150 mcg/kg/hr infusion + IA

51
Q

Remifentanil acts as a ______ opioid agonist

52
Q

Remifentanil is unique d/t structure with _______

A

Ester linkage

53
Q

Remifentanil is susceptible to what?

A

Hydrolysis by non-specific plasma and tissue esterases to inactive metabolites

54
Q

Remifentanil onset

A

Rapid - 1.1 minute

55
Q

Remifentanil is not effected by ________

A

Pseudocholinesterase deficiencies

56
Q

Remifentanil pre-induction dose

A

1mcg/kg IV over 60-90s

** safer to infuse!

57
Q

Remifentanil infusion during anesthesia - dose

A

.05-2.0 mcg/kg/min infusion

58
Q

Remifentanil dosage when used in combo with Benzo

A

0.05-0.1 mcg/kg/min

Monitor for synergistic depression of ventilation

59
Q

Remifentanil side effects

A

N/V, Dec RR, Dec CBF/CMRO2, Dec HR/SBP
No change in ICP
HYPERALGESIA

60
Q

SUFENTANIL is _____ than fentanyl

A

10x more potent

1000x more potent than morphine

61
Q

Sufentanil effect-site equilibriation time

A

6.2 minutes

62
Q

Sufentanil - what terminates effect?

A

RRTIS

Repeated dosing results in metabolism dependent termination of effects

63
Q

Sufentanil metabolism

A

60% first pass pulmonary uptake

64
Q

Sufentanil has a ____ effect site equilibrium, ______ duration, and _______ extubation than morphine and fentanyl

A

Rapid
Shorter
Faster

65
Q

Hydromorphone is ______ potent than morphine

66
Q

1.5mg hydromorphone is equivalent to _____ mg morphine

67
Q

Hydromorphone has _______ solubility between morphine and fentanyl

A

Intermediate

68
Q

Opioid receptors are present in the ________ horn of the spinal cord

69
Q

Analgesia from neuraxial opioids is due to

A

Direct activation of the Mu receptors

Systemic absorption

70
Q

Site of action for neuraxial opioids - where effects are primarily mediated

A

Substantia gelatinosa/rexed Lamina II, III

71
Q

Epidural space contains

A

Fat, veins, spinal nerve roots

72
Q

Epidural space is located

A

Between LF and Dura

73
Q

Epidural space capacity

A

Large volume

20mL+

74
Q

Subarachnoid space contains

A

Spinal cord, CSF, spinal nerve roots

75
Q

Subarachnoid space capacity

A

Small

> 1mL will increase ICP

76
Q

Neuraxial opioids: penetration of the dura is influenced by _______

A

Lipid solubility

77
Q

Peak CSF [C] ~ ______ with fentanyl, sulfentanil

A

20 minutes

78
Q

Peak CSF [C] ~ _______ with morphine

79
Q

Why does fentanyl and sufentanil penetrate the dura faster than than morphine?

A

1000x more lipid soluble

80
Q

Addition of epinephrine in a neuraxial opioid _______ systemic absorption and ______ postop analgesia by _______ the epidural vessels

A

Decreases
Enhances
Constricting

81
Q

Why would epinephrine be added to a neuraxial opioid?

A

Epi constricts the vessels to prolong duration of action
Analgesia is enhanced
Absorption into plasma is decreased

82
Q

Lipophilic opioids in the SA spaced result in a:
_______ onset
________ DOA
________ diffuse out of CSF

A

Rapid onset
Short DOA
Rapidly diffuse out

83
Q

Lipophilic opioids in the SA space result in ________ depression of ventilation

84
Q

Hydrophilic opioids in the SA space result in:
________ onset
_______ DOA
_______ diffuse out of CSF

A

Slow onset
Long DOA
Slowly diffuse out

85
Q

Hydrophilic opioids in the SA space result in ________ depression of ventilation

A

Late (due to rostral spread)

86
Q

Neuraxial opioids - classic side effects

A

Pruritis - most common
Urinary retention
Ventilatory depression
Sedation

87
Q 
Hydrophilic opioids in the epidural space result in:
\_\_\_\_\_\_\_\_ onset
\_\_\_\_\_\_\_ DOA
\_\_\_\_\_\_\_ systemic uptake 
\_\_\_\_\_\_\_ depression of ventilation
A

Slow onset
Long DOA
Greater systemic uptake
Early and late

88
Q 
Lipophilic opioids in the epidural space result in:
\_\_\_\_\_\_\_\_ onset
\_\_\_\_\_\_\_ DOA
\_\_\_\_\_\_\_ diffuse out of epidural space
\_\_\_\_\_\_\_\_\_ depression of ventilation
A

Rapid onset
Short DOA
Rapidly diffuse out of epidural space
Early depression of ventilation

89
Q

Opioid antagonists are used for

A

Restore ventilation in patients after opioid overdose

90
Q

Opioid antagonists may reduce

A

N/V, pruritis, urinary retention, rigidity, biliary spasm

91
Q

Naloxone is a __________

A

Pure Mu receptor antagonist

92
Q

Naloxone dosage

A

1-4 mcg/kg

93
Q

DOA Naloxone

A

30-45 minutes

94
Q

E1/2t Naloxone

A

1-1.5hours

95
Q

Titration of naloxone

A

0.04mg/minute

96
Q

Side effects of naloxone

A

N/V
CV stimulation :: tachycardia, HTN, pulmonary edema, dysrythmias
Pain

97
Q

Methylnaltrexone is a ________

A

Quaternary ammonium opioid receptor antagonist

98
Q

Characteristics of methylnaltrexone

A

Constipation relief, delayed gastric emptying reversed, reverses opioid effects at peripheral receptors, does NOT cross BBB, + charge

99
Q

Methylnaltrexone dosage

A

0.3 mg/kg IV

100
Q

Opioid agonist antagonists bind to _____ receptors

A

Mu - produce limited/no response

May bind to Kappa/Delta receptors: agonist effects

101
Q

Effect of Opioid agonist-antagonists

A

Produce analgesia with less ventilatory depression than opioid agonists
Less potential for abuse than opioid agonists

102
Q

Butorphanol acts on which receptors?

A

Kappa agonist
Mu antagonist
Mu partial agonist

103
Q

Butorphanol is _____ potent than morphine

104
Q

Butorphanol side effects

A

Sweating, drowsiness, nausea, CNS stimulation

Withdrawal after cessation of chronic admin

Pharm Fall 2019 (33 decks)

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