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A&P Texas Wes > Opioid Agonist > Flashcards

Opioid Agonist Flashcards

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1
Q

General structures of opioid Agonist
Pheantherenes:

A

Morphine, codiene, Thebaine-

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2
Q

Structure Benzylisoqinolone:

A

Papverine and Noscapine

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3
Q

Opioid agonist MOA

A

Same receptors are activated by endogenous enkephalins, endorphins, and dynorphins
‣ Presynaptic inhibition of ACH, dopamine, NE, and Substance P
‣ Increased K conductance → HYPERPOLARIZATION
‣Ca + channel inactivation → Decreased neurotransmission

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4
Q

Opioid Agonist Uses

A
  1. Analgesia
    2.Sedation
  2. Anti-shivering
    4.Cough suppression: Codeine, dextromethorphan
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5
Q

General CV effects

A

Bradycardia from histamine release
Hypotension
Orthostatic hypotension induced syncope

NITROUS AND BENZO= ↑ CV DEPRESSION (CO&BP)

BENEFIT: cardioprotective from MI
Direct depression of SA and AV node

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6
Q

Opioid General CNS

A

Miosis,
Sedation,
Myoclonus
delta waves on EEG

Tolerance: 2-3 weeks, down regulates receptors
Depressed respiratory center (Pons/Medulla)
Depressed medullary cough center

Caution with use in head injury!Decrease in CBF

*Skeletal muscle rigidity of thoracic & abdominal
Worsened with mechanical ventilation, treat with muscle relaxers or naloxone

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7
Q

Receptor µ1 (Mu1)

A

µ1 (Mu1): Analgesia (supraspinal, spinal )
Eupohoria, low abuse potential, miosis Bradycardia, hypothermia, urinary retention.
Mu1: “slow cold cant see cen’t bee but happy”

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8
Q

Receptor µ2 (Mu2):

A

µ2 (Mu2): Analgesia (spinal)
Depressed ventilation, physical dependence Constipation (marked)
Mu2: Can’t breathe, can’t poo - addicted too!”

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9
Q

Receptor K (Kappa):

A

K (Kappa): Analgesia (supraspinal, spinal)
dysphoria, sedation, low abuse, misosis, Diuresis

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10
Q

Receptor Delta:

A

Delta: Analgeisa (supraspinal, spinal)
Depressed ventilation, physical dependence
constipation (minimal) , urinary retention

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11
Q

Receptors Overview

A
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12
Q

Opioids Respiratory Overview..

A

‣ ↓ response of ventilation centers to CO2, and this will require higher ETCO2 for them to start breathing again. CO2 NARCOSIS is an issue - if CO2 too high like 60
‣increase in resting PaCO2 (shifts curve to the right).
‣MU2 → ventilatory depression, ↓ rate but ↑ in TV (Vm doesn’t change)
‣ overdose will induce apnea, miosis, hypoventilation, and coma
‣ reversal of ventilatory depression with physostigmine! it increases levels of ACH in CNS to antagonize the ventilatory depression but does not effect the analgesia.
‣ Pre- induction dose of opioids can induce coughing

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13
Q

Opioid GI general

A

GI:
Sphincter of Oddi Spasms (can mimic MI pain)
‣ Fentanyl 99%
‣ Meperidine 61%
‣Morphine 53%
Treatment: Nalaxone or Glucagon (2 mg IV, incremental doses), glucagon preferred b/c no opioid analgesic antagonism.
If these do not relieve pain then give nitro for MI pain.

Delayed Gastric Emptying and constipation

N/V: direct stimulation of the CTZ (chemoreceptor trigger zone)

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14
Q

Opioid Misc:

A

Rigidity: chest wall and abdominal muscles
Cutaneous: Skin flushing d/t histamine
Hormonal: decreased cortisol
PLACENTAL CROSSING–> NEONATE DEPRESSION or chronic use causes dependence

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15
Q

Opioid General GU

A

Urinary urgency/retention

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16
Q

Withdrawl:

A

Initial symptoms: yawning, diaphoresis, lacrimation, or coryza, insomnia and restlessness
72 hrs: Abdominal cramps, N/V, and diarrhea

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17
Q

Least to most potent

A

Codiene: (120mg = 10 mg morphine)
Meperidine: (pethidine) 1/10th
potency of morphine
Morphine:

Hydromorphone: (5x more potent than morphine)

Alfentanil: (1/5th less potent than fentanyl)

Fentanyl: (sublimaze)
75 to 125 x more potent than morphine

Remifentanil: 15-20 x as potent as alfentanil
equipotent to fentanyl- so the order of these two is subjectional

Sufentanil:
(5-12 x more potent than fentanyl)

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18
Q

MOA for Meperidine (pethidine)

A

Agonist at 𝝻 and K receptors
Also agonist at alpha 2 receptors

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19
Q

MOA for Remifentanil

A

Selective µ opioid agonist

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20
Q

Structure of Meperidine

A

Structural similar to
lidocaine: tertiary amine, ester group and lipophilic phenyl group
Atropine (causes similar effect of spasms of muscle)

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21
Q

Structure of Hydromorphone

A

Morphine derivative

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22
Q

Structure of Alfentanil

A

Meperidine analoge

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23
Q

Structure of Fentanyl

A

meperidine analogue

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24
Q

Structure of Remifentanil

A

Ester structure
Meperidine analogue

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25
Sufentanil
Analogue of fentanyl (1974) meperidine analogue
26
Codiene clinical uses
Cough suppressant analgesic
27
Meperidine Clinical Uses
Intrathecal administration IM for postop analgesia Post op shivering because of K and a2 receptors ***clonidine also works for postop shivering at a2 receptors
28
Morphine Clinical Uses
Relieves visceral, skeletal muscles, joints and integumental dull > sharp (better for post op c-fiber pain) intermittent pain
29
Hydromorphone clinical uses
same as morphine Relieves visceral, skeletal muscles, joints and integumental dull > sharp (better for post op c-fiber pain) intermittent pain
30
Fentanyl Use Cases
Cardiopulmonary bypass (***drug may adhere to circuit lessening amount of fentanyl in blood) induction and analgesia adjunct for Direct laryngoscopy during intubation Sudden changes in surgical stimulation level
31
Remifentanil Use Cases
Carotid endarectomy cases per CASTILLO Induction & maintenance
32
Sufentanil Use Cases
Analgesia and induction Analgesia: 0.1 to 0.4 µg/kg IV Induction: 18.9 µg/kg IV Intraop: 0.3 to 1 µg/kg IV Infusion: 0.5 to 1 µg/kg/hr IV
33
Alfentanil Use Cases
Induction laryngoscopy: 15 to 30 µg/kg IV (90 seconds prior) Induction alone: 150 to 300 µg/kg IV Maintenance: 25 to 150 µg/kg/hour IV with inhaled anesthetics Parkinson’s disease = acute dystonia
34
Codeine dose
Cough suppressant: 15 mg Analgesia 60 mg PO OR IM NEVER IV → HISTMAINE INDUCED HYPOTENSION
35
Meperidine Post-op shivering dose
12.5 mg IV
36
Morphine intra-op dose
Intra Op: 1-10 mg IV
37
Hydromorphone intra -op dose
Intra Op: 1-4 mg **Give 0.5 mg intermittently! HAVE TO REDOSE Q 4 HOURS
38
Alfentanil Dose induction
Induction Laryngoscopy: 15-30 µg/kg IV **give 90 sec prior Induction alone: 150-300 µg/kg IV
39
Alfentanil Maintenance Dose
Maitenance: 25-150 µg/kg/hour w/ inhaled gas
40
Alfentanil MAC considerations
Alfentanil = up to 70% ↓ in MAC
41
Fentanyl Induction dose
1.5 - 3 𝝻g/ kg IV **give 5 mins prior
42
Fentanyl Other doses
Analgesia: 1-2 𝝻g/kg IV Adjunct with inhaled gases: 2-20 µg/kg IV Surgical Anesthesia:(solo): 50-150 µg/kg Transdermal: 75-100 µg (18 hr steady state delivery Transmucosal (oral): 5-20 µg/kg Peds 2-8 yo: 15-20 µg/kg PO 45 min prior ***1 mg PO Fentanyl=5 mg PO morphine
43
Remifentanil Induction dose
0.5 - 1 µg/kg over 1 min **DOSE IN IBW**
44
Remifentanil maintenance dose
Maitenance: 0.25-1 µg/kg n IV OR 0.25 to 1 µg/kg IV or 0.005 to 2 µg/kg/min IV *** before stopping give longer acting opioid Not recommended for spinal or epidural use
45
Sufentanil Induction dose
18.9 µg/kg IV
46
Sufentanil Analgesia dose
Analgesia: 0.1-0.4 µg/kg IV
47
Fentanyl MAC
Fentanyl 3 µg/kg IV 25-30 min before surgical incision = ↓ MAC of ISO or DES to 50%
48
Sufentanil and MAC
Sufentanil decreases MAC with Enflurane by 70 to 90% 50 to 91% decrease
49
Alfentanyl and MAC
Alfentanyl = up to 70% decrease in MAC
50
Remifentanyl and MAC
50 to 91% decrease
51
Onset of Remifentanyl, surentanil , and fentanyl
30-60 sec
52
Onset of Alfentanil
1.4 min
53
Onset of Hydromorphone and Meperidine
5-15 min
54
Onset of morphine
10-20 min
55
Morphine Peak
IM: 45-90 IV: 15-30 minutes
56
Duration of Hydromorphone and Meperidine
2-4 hrs
57
Duration of morphine
4-5 hours
58
Duration of Fentanyl
1-1.5hr
59
Duration of Remifentanyl
6-8 min
60
PK / % nonionized (pH 7.4) - Meperidine
8.5/7%
61
PK / % nonionized (pH 7.4) - Morphine
7.9/ 23%
62
PK / % nonionized (pH 7.4) - hydromorphone
Less hydrophilic than morphine
63
PK / % nonionized (pH 7.4) - Alfentanil
6.5/ 89%
64
PK / % nonionized (pH 7.4) - Fentanyl
8.4/8.5% VERY lipid soluble
65
PK / % nonionized (pH 7.4) - Remi
7.3/ 58%
66
PK / % nonionized (pH 7.4) - Sufent
8.0/20% Very lipid soluble
67
Meperidine Vd/ part Co
305 Vd / 32 part co
68
Morphine Vd
224 Vd/ 1 part co accumulates rapidly in kidneys, liver and skeletal muscles
69
Alfentinil Vd
27 L
70
Fentanyl Vd
335 L LARGE Vd - largest it seems IV (<5 mins 80% is gone) ->highly vascular tissues -> inactive tissue sites
71
Remifent Vd
30 L
72
sufent Vd
123 L Larger Vd than alfentanil
73
Protein Binding Meperidine
60%
74
Protein Binding Morphine
35%
75
Protein Binding Alfentanil
92 % Binds to α1- acid glycoprotein
76
Protien Binding Fentanyl
84%
77
Protein binding Remifent
66-93%
78
Protien Binding Sufent
92.5% to α1- acid glycoprotein
79
Metabolism Liver/hepatic
codiene, sufentanil, meperidine 90%
80
Metabolism Morphine
Glucoronic acid conjugation metabolites: Morphine -3 glucorinide (75-95%) INACTIVE Morphine -6-glucoride: ACTIVE Causes the late ventilatory depression
81
Metabolism of Alfentanil & Fentanyl
CYP3A4
82
Metabolism of Remifentanil
Hydrolysis by plasma and tissue esterases allows for brief action, rapid onset and offset, lack of accumulation and rapid recovery when discontinued. SIMILAR TO PROPOFOL AND KETAMINE
83
Meperidine Metabolite
Normeperidine
84
Does Hydromorphone have an active metabolite
Yes
85
Metabolite of Alfentanil
Noralfentanil
86
Metabolite of Fentanyl
Norfentanyl
87
Effect site equilibration time (blood/brain)- alfentanil
1.4 minutes
88
Effect site equilibration time (blood/brain)- fentanyl
6.8 min
89
Effect site equilibration time (blood/brain)- Remifent
1.1 min
90
Effect site equilibration time (blood/brain)- sufentanil
6.2 min
91
1/2 time for codeine
3-3.5 hrs
92
1/2 time for meperidine
3-5 hrs **35 hrs with Renal failure
93
1/2 time for morphine
1.5-3.5 hrs
94
1/2 time for alfentanil
**cirrhosis prolongs E 1/2 time
95
1/2 time for Remifent
6.3 minutes (99.8%)
96
clearance for meperidine
1.02 L/min Renal (acidic urine can speed up elimination)
97
clearance for morphine
1.05 L/min
98
clearance for fentanyl
Kidneys
99
clearance for Remifent
kidneys (unaffected by renal or liver dx) 3L/min **8x faster than alfentanil
100
clearance for sufentanil
renal and fecal ***Caution with chronic renal failure
101
First pass meperidine
Hepatic 80%
102
First pass morphine
25% for PO, NONE in lungs
103
first pass for fentanyl
75% in lungs
104
first pass for sufentanil
60% LUNG
105
Context sensitive half time alfentanil
60 min
106
Context sensitive half time fentanyl
260 min Greater than sufentanil (d/t inactive tissue accumulation, will return to plasma and replace what has been metabolized)
107
Context sensitive half time remifentanil
4 min
108
Context sensitive half time sufent
30 min "Shorter" - per castillo
109
CNS effects codeine
MINIMAL SEDATION DIZZINESS
110
CNS effects meperidine
Sedation, Euphoria SEROTONIN SYNDROME -- careful with TCA's and MAOI's
111
CNS effects Morphine
Analgesia, euphoria, sedation and diminished ability to concentrate
112
CNS effects Fentanyl
‣Seizure like activity on SSEP and EEG with doses > 30 µg/kg IV ‣ ↑ ICP (6-9 mmHg)
113
CNS effects Remifent
‣Seizure-like activity
114
CV effects meperidine
Tachycardia, (-) inotropic
115
CV effects morphine
Histamine release = ↓ BP
116
CV effects hydromorphone
NO HISTAMINE RELEASE
117
CV effects Fentanyl
‣ Depressed Carotid sinus barreceptor reflex = Bradycardia, ↓BP, ↓CO **NO** histamine release
118
CV effects Remifent
‣↓ B/P and HR
119
CV effects Sufentanil
‣Bradycardia causes ↓CO
120
Pulmonary
Meperidine: Depression of ventilation Remifent: ‣ Synergistic depression of ventilation with propofol
121
GI
They pretty much all cause NV except fro hydromorphone, fent, alfent, and sufent... Remifent: does cause N/V
122
Other side Effects codeine:
PHYSICAL DEPENDENCE
123
Other Side effects meperidine:
TOXICITY: Delirium (confusion and hallucinations, myoclonus and seizures) CROSSES PLACENTAL BARRIER!
124
Other side effects morphine:
feeling of body warmth, heaviness of extremities, dryness of the mouth, and pruritus.
125
Side effects of fentanyl
SYNERGISM w/ Benzos and propofol
126
side effects with Remifent
Hyperalgesia d/t previous acute exposure to large opioid doses and tolerance.
127
Side effects with Sufent
CHEST WALL AND ABDOMINAL MUSCLE RIGIDITY.
128
Clinical considerations with morphine
Caution with use in renal and elderly patients. Metabolites stick around longer in renal Serum plasma concentrations increase with age. Women > men: analgesic potency and slower speed of offset
129
Consideration for Alfentanil
USE IN PARKINSON'S = ACUTE DYSTONIA
130
Other
Analogues: Fentanyl, Sufentanil, Alfentanil and Remifentanil Withdrawal onset 2-6 hrs (faster than morphine)
131
Chart
132
What blocks pain at the Brain? Perception
opioid, a2 agonists, general anesthetics
133
What blocks at the spinal cord? Modulation of afferent signals in the dorsal horn of spinal cord and production of reflex reaction
Local anesthetics, opioids, Ketamine, a2 agonists
134
What blocks pain transmission of action potential via A(delta) and C fibers
Local anesthetics
135
What blocks pain at Peripheral nociceptors (Transduction of mechanical, chemical and thermal stimuli into an action potential)
Local anesthetics, NSAIDs
136
Unmyelinated C- fiber:
burning pain from heat and pressure from sustained pressure.
137
Myelinated A-fiber:
Type I fibers ( Aβ & Aδ fibers): heat, mechanical, chemical Type II fibers (Aδ fibers): heat
138
Sensitization
Sensitization- hurts more over time.. Lowers threshold
139
Secondary Hyperalgesia:
uninjured skin surrounding the injury (only from mechanical stimuli). Sensitization of central neuronal circuits
140
Primary Hyperalgesia: at the original site of injury from heat and mechanical injury.
Decreased pain threshold Increased response to suprathreshold stimuli Spontaneous pain Expansion of receptive field
141
Laminae III & IV:
NKI receptor with substance P
142
Lamina II
(substantia gelatinosa [opioids]): afferent C Fibers
143
Periaqueductal gray -rostral ventromedial medulla (PAG-RVM) system
Depress or facilitate the integration of pain info in the spinal dorsal horn.
144
Excitatory impulses
Glutamate Calcitonin Neuropeptide Y Aspartate Substance P
145
Inhibitory impulses
GABA glycine enkephalins norepinephrine dopamine
146
Spinothalamic
Pain, temperature, and itch (Laminae I, VII, & VIII: All afferent fibers)
147
Spinobulbar -cerebellum
Behavior toward pain (Laminae I, V, & VII)
148
Spinohypothalamic
Autonomic, neuroendocrine, and emotional aspects of pain (Laminae I, V, VII, & X)
149
Where is S1 and S2
Forebrain Most of modulation of pain happens at forebrain or somatosensory cortex
150
Hyperpolarize A-delta and C fibers
Decrease release of substance P Opening of K+ channels/inhibition of Ca++ channels
151
Neuropathic pain
Persists after the tissue has healed -> allodynia and hyperalgesia Increased risk: Cancer patients d/t chemo and radiation therapy Treatment: symptomatic (opioids gabapentin, amitryptiline, cannabis)
152
PAG-RVM system:
µ, κ, δ opioid receptors hyperalgesia & Allodynia
153
When do neonates have pain perception
23 weeks of gestation

A&P Texas Wes (8 decks)

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