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
2
Q
Morphine and codeine are in what class of opioids?
A
Opium alkaloids - phenanthrenes
3
Q
Fentanyl is in what class of opioids?
A
Synthetic phenylpiperidines
Same with sufentanil, alfentanil, remifentanil, meperidine
4
Q
What class is hydromorphone in?
A
Semisynthetic opioids (simple substitution to the morphine molecule) Along with oxycodone, buprenorphine
5
Q
Opioid receptors are primarily responsive to ___ _________ ligands
A
3 endogenous
6
Q
Delta receptor endogenous ligand
A
Enkephalin
7
Q
Mu receptor endogenous ligand
A
Beta Endorphin
8
Q
Kappa receptor endogenous ligand
A
Dynorphan
9
Q
Opioids activate what system?
A
Pain modulating (anti-nociceptive) systems
10
Q
The ________ form gains access to the CNS most easily
A
Non-ionized
11
Q
The _______ form binds to the receptor
A
Ionized
12
Q
_________ correlates with potency
A
Receptor affinity
13
Q
MOA opioids:
Opioid receptors are present on they peripheral ends of __________ neurons
A
Primary sensory
14
Q
Opioid receptors when activated result in ________ neurotransmission and/or __________ inhibit the release of ________ neurotransmitters
A
Decreased
Release
Excitatory
15
Q
What would the ideal opioid agonist have?
A
High specificity/hi potency (affinity)
No specificity for receptors producing adverse effects
16
Q
Opioid receptors inhibit ________ which decreases ________
A
Adenyl Cyclase
CAMP
Results in hyperpolarization of cell
17
Q
Mu1 receptor effects
A
Analgesia (Supra and spinal) Euphoria Low abuse potential Miosis Bradycardia
18
Q
Mu2 Receptor effects
A
Analgesia (spinal)
Depression of ventilation
Physical dependence
Constipation
19
Q
Kappa receptor effects
A
Analgesia (supraspinal and spinal) Dysphoria** Sedation Low abuse potential Miosis
20
Q
Delta receptor effects
A
Analgesia (supraspinal and spinal)
Depression of ventilation
Physical dependence**
21
Q
Opioids effect the CO2 response curve by ?
A
Response curve shifts to the right
22
Q
Morphine produces
A
Analgesia, euphoria, sedation, decreased ability to concentrate, nausea, dry mouth, pruritis
23
Q
Morphine is effective against which pain?
A
Visceral, skeletal, joint pain
24
Q
Morphine CV side effects
A
Decreased SNS tone
Decreased HR
Histamine release
25
Morphine respiratory effects
Depression of ventilatory centers in medulla
Decreased responsiveness to CO2
Decreased RR, increased VT
26
Morphine CNS effects
Decreased CBF, CMRO2, ICP
| Skeletal muscle rigidity
27
Morphine side effects - etc
Spasm of biliary smooth muscle - may mimic pain of angina pectoris
Tx = naloxone, glucagon, nitroglycerin
28
Morphine side effects - GI
Spasm of GI smooth muscle
| N/V - d/t direct stimulation of the CTZ in the Post-Rema, floor of the 4th ventricle
29
Morphine withdrawal - occurs in _______ hours
Peaks in ________
Remission in _________
Occurs within 15-20h
Peaks 2-3D
Remission 10-14d
30
Symptoms of morphine withdrawal
Yawning, lacrimation, diaphoresis, abd cramps, N/V, diarrhea
31
Clinical uses for Meperidine
Post op analgesia, L&D analgesia, PCA for postop, treatment of shivering
32
Meperidine unique side effects
Increased HR, decreased myocardial contractility with large doses
33
Meperidine should not be given with
MAOIs
34
Meperidine interactions - Type I response
Excitatory
35
Meperidine interactions - type II response
Depressive - hypotension/vent depression/coma
36
Meperidine use with caution in ppl taking ______
TCAs
37
Fentanyl has a _____ time to onset than morphine
More rapid (2min)
38
Fentanyl has a _______ duration of action than morphine
Shorter
39
Fentanyl - ____% of single dose undergoes __________ uptake
76%
First pass pulmonary uptake
*pulmonary tissue serves as a depot for release back into circulation
40
Time to peak effect of fentanyl in adults
5-7 minutes
41
Fentanyl - time to peak effect in peds
5 minutes
42
Advantage of fentanyl
Cardiac stable
| Does not produce direct myocardial effects, no histamine release
43
Pre induction dose of fentanyl
1-5 mcg/kg
44
Fentanyl dose - analgesia for sedation
1-2 mcg/kg IV
45
What is more profound in fentanyl than in morphine?
Bradycardia
46
Why is there persistent ventilatory depression when fentanyl is given?
Saturation of inactive sites - context sensitive half time
47
Alfentanyl is used for
Transient, acute pain d/t rapid onset/short duration
48
Alfentanil dose blunt catecholamine and BP response
30mcg/kg IV
49
Alfentanil dose for unconsciousness
150-300mcg/kg IV
50
Balanced anesthesia - alfentanil dose
25-150 mcg/kg/hr infusion + IA
51
Remifentanil acts as a ______ opioid agonist
Mu
52
Remifentanil is unique d/t structure with _______
Ester linkage
53
Remifentanil is susceptible to what?
Hydrolysis by non-specific plasma and tissue esterases to inactive metabolites
54
Remifentanil onset
Rapid - 1.1 minute
55
Remifentanil is not effected by ________
Pseudocholinesterase deficiencies
56
Remifentanil pre-induction dose
1mcg/kg IV over 60-90s
| ** safer to infuse!
57
Remifentanil infusion during anesthesia - dose
.05-2.0 mcg/kg/min infusion
58
Remifentanil dosage when used in combo with Benzo
0.05-0.1 mcg/kg/min
| Monitor for synergistic depression of ventilation
59
Remifentanil side effects
N/V, Dec RR, Dec CBF/CMRO2, Dec HR/SBP
No change in ICP
HYPERALGESIA
60
SUFENTANIL is _____ than fentanyl
10x more potent
| 1000x more potent than morphine
61
Sufentanil effect-site equilibriation time
6.2 minutes
62
Sufentanil - what terminates effect?
RRTIS
| Repeated dosing results in metabolism dependent termination of effects
63
Sufentanil metabolism
60% first pass pulmonary uptake
64
Sufentanil has a ____ effect site equilibrium, ______ duration, and _______ extubation than morphine and fentanyl
Rapid
Shorter
Faster
65
Hydromorphone is ______ potent than morphine
More
66
1.5mg hydromorphone is equivalent to _____ mg morphine
10
67
Hydromorphone has _______ solubility between morphine and fentanyl
Intermediate
68
Opioid receptors are present in the ________ horn of the spinal cord
Dorsal
69
Analgesia from neuraxial opioids is due to
Direct activation of the Mu receptors
| Systemic absorption
70
Site of action for neuraxial opioids - where effects are primarily mediated
Substantia gelatinosa/rexed Lamina II, III
71
Epidural space contains
Fat, veins, spinal nerve roots
72
Epidural space is located
Between LF and Dura
73
Epidural space capacity
Large volume
| 20mL+
74
Subarachnoid space contains
Spinal cord, CSF, spinal nerve roots
75
Subarachnoid space capacity
Small
| > 1mL will increase ICP
76
Neuraxial opioids: penetration of the dura is influenced by _______
Lipid solubility
77
Peak CSF [C] ~ ______ with fentanyl, sulfentanil
20 minutes
78
Peak CSF [C] ~ _______ with morphine
1-4hours
79
Why does fentanyl and sufentanil penetrate the dura faster than than morphine?
1000x more lipid soluble
80
Addition of epinephrine in a neuraxial opioid _______ systemic absorption and ______ postop analgesia by _______ the epidural vessels
Decreases
Enhances
Constricting
81
Why would epinephrine be added to a neuraxial opioid?
Epi constricts the vessels to prolong duration of action
Analgesia is enhanced
Absorption into plasma is decreased
82
Lipophilic opioids in the SA spaced result in a:
_______ onset
________ DOA
________ diffuse out of CSF
Rapid onset
Short DOA
Rapidly diffuse out
83
Lipophilic opioids in the SA space result in ________ depression of ventilation
Early
84
Hydrophilic opioids in the SA space result in:
________ onset
_______ DOA
_______ diffuse out of CSF
Slow onset
Long DOA
Slowly diffuse out
85
Hydrophilic opioids in the SA space result in ________ depression of ventilation
Late (due to rostral spread)
86
Neuraxial opioids - classic side effects
Pruritis - most common
Urinary retention
Ventilatory depression
Sedation
87
```
Hydrophilic opioids in the epidural space result in:
________ onset
_______ DOA
_______ systemic uptake
_______ depression of ventilation
```
Slow onset
Long DOA
Greater systemic uptake
Early and late
88
```
Lipophilic opioids in the epidural space result in:
________ onset
_______ DOA
_______ diffuse out of epidural space
_________ depression of ventilation
```
Rapid onset
Short DOA
Rapidly diffuse out of epidural space
Early depression of ventilation
89
Opioid antagonists are used for
Restore ventilation in patients after opioid overdose
90
Opioid antagonists may reduce
N/V, pruritis, urinary retention, rigidity, biliary spasm
91
Naloxone is a __________
Pure Mu receptor antagonist
92
Naloxone dosage
1-4 mcg/kg
93
DOA Naloxone
30-45 minutes
94
E1/2t Naloxone
1-1.5hours
95
Titration of naloxone
0.04mg/minute
96
Side effects of naloxone
N/V
CV stimulation :: tachycardia, HTN, pulmonary edema, dysrythmias
Pain
97
Methylnaltrexone is a ________
Quaternary ammonium opioid receptor antagonist
98
Characteristics of methylnaltrexone
Constipation relief, delayed gastric emptying reversed, reverses opioid effects at peripheral receptors, does NOT cross BBB, + charge
99
Methylnaltrexone dosage
0.3 mg/kg IV
100
Opioid agonist antagonists bind to _____ receptors
Mu - produce limited/no response
| May bind to Kappa/Delta receptors: agonist effects
101
Effect of Opioid agonist-antagonists
Produce analgesia with less ventilatory depression than opioid agonists
Less potential for abuse than opioid agonists
102
Butorphanol acts on which receptors?
Kappa agonist
Mu antagonist
Mu partial agonist
103
Butorphanol is _____ potent than morphine
5-8x MORE
104
Butorphanol side effects
Sweating, drowsiness, nausea, CNS stimulation
| Withdrawal after cessation of chronic admin
