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A&P Texas Wes > Opioid Agonist > Flashcards

Opioid Agonist Flashcards

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
Q

Sufentanil

A

Analogue of fentanyl (1974)
meperidine analogue

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26
Q

Codiene clinical uses

A

Cough suppressant
analgesic

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27
Q

Meperidine Clinical Uses

A

Intrathecal administration
IM for postop analgesia

Post op shivering because of K and a2 receptors
***clonidine also works for postop shivering at a2 receptors

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28
Q

Morphine Clinical Uses

A

Relieves visceral, skeletal muscles, joints and integumental dull > sharp (better for post op c-fiber pain)
intermittent pain

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29
Q

Hydromorphone clinical uses

A

same as morphine

Relieves visceral, skeletal muscles, joints and integumental dull > sharp (better for post op c-fiber pain)
intermittent pain

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30
Q

Fentanyl Use Cases

A

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

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31
Q

Remifentanil Use Cases

A

Carotid endarectomy cases per CASTILLO

Induction & maintenance

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32
Q

Sufentanil Use Cases

A

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

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33
Q

Alfentanil Use Cases

A

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

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34
Q

Codeine dose

A

Cough suppressant: 15 mg
Analgesia 60 mg
PO OR IM
NEVER IV → HISTMAINE INDUCED HYPOTENSION

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35
Q

Meperidine Post-op shivering dose

A

12.5 mg IV

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36
Q

Morphine intra-op dose

A

Intra Op: 1-10 mg IV

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37
Q

Hydromorphone intra -op dose

A

Intra Op: 1-4 mg
**Give 0.5 mg intermittently!
HAVE TO REDOSE Q 4 HOURS

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38
Q

Alfentanil Dose induction

A

Induction Laryngoscopy: 15-30 µg/kg IV
**give 90 sec prior
Induction alone: 150-300 µg/kg IV

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39
Q

Alfentanil Maintenance Dose

A

Maitenance: 25-150 µg/kg/hour w/ inhaled gas

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40
Q

Alfentanil MAC considerations

A

Alfentanil = up to 70% ↓ in MAC

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41
Q

Fentanyl Induction dose

A

1.5 - 3 𝝻g/ kg IV
**give 5 mins prior

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42
Q

Fentanyl Other doses

A

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

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43
Q

Remifentanil Induction dose

A

0.5 - 1 µg/kg over 1 min
DOSE IN IBW

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44
Q

Remifentanil maintenance dose

A

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

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45
Q

Sufentanil Induction dose

A

18.9 µg/kg IV

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46
Q

Sufentanil Analgesia dose

A

Analgesia: 0.1-0.4 µg/kg IV

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47
Q

Fentanyl MAC

A

Fentanyl 3 µg/kg IV 25-30 min before surgical incision = ↓ MAC of ISO or DES to 50%

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48
Q

Sufentanil and MAC

A

Sufentanil decreases MAC with Enflurane by 70 to 90%

50 to 91% decrease

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49
Q

Alfentanyl and MAC

A

Alfentanyl = up to 70% decrease in MAC

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50
Q

Remifentanyl and MAC

A

50 to 91% decrease

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51
Q

Onset of Remifentanyl, surentanil , and fentanyl

A

30-60 sec

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52
Q

Onset of Alfentanil

A

1.4 min

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53
Q

Onset of Hydromorphone and Meperidine

A

5-15 min

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54
Q

Onset of morphine

A

10-20 min

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55
Q

Morphine Peak

A

IM: 45-90
IV: 15-30 minutes

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56
Q

Duration of Hydromorphone and Meperidine

A

2-4 hrs

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57
Q

Duration of morphine

A

4-5 hours

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58
Q

Duration of Fentanyl

A

1-1.5hr

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59
Q

Duration of Remifentanyl

A

6-8 min

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60
Q

PK / % nonionized (pH 7.4) - Meperidine

A

8.5/7%

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61
Q

PK / % nonionized (pH 7.4) - Morphine

A

7.9/ 23%

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62
Q

PK / % nonionized (pH 7.4) -
hydromorphone

A

Less hydrophilic than morphine

63
Q

PK / % nonionized (pH 7.4) -
Alfentanil

A

6.5/ 89%

64
Q

PK / % nonionized (pH 7.4) - Fentanyl

A

8.4/8.5%
VERY lipid soluble

65
Q

PK / % nonionized (pH 7.4) - Remi

A

7.3/ 58%

66
Q

PK / % nonionized (pH 7.4) - Sufent

A

8.0/20%
Very lipid soluble

67
Q

Meperidine Vd/ part Co

A

305 Vd / 32 part co

68
Q

Morphine Vd

A

224 Vd/ 1 part co
accumulates rapidly in kidneys, liver and skeletal muscles

69
Q

Alfentinil Vd

A

27 L

70
Q

Fentanyl Vd

A

335 L
LARGE Vd - largest it seems
IV (<5 mins 80% is gone)
->highly vascular tissues
-> inactive tissue sites

71
Q

Remifent Vd

A

30 L

72
Q

sufent Vd

A

123 L
Larger Vd than alfentanil

73
Q

Protein Binding Meperidine

A

60%

74
Q

Protein Binding Morphine

A

35%

75
Q

Protein Binding Alfentanil

A

92 % Binds to α1- acid glycoprotein

76
Q

Protien Binding Fentanyl

A

84%

77
Q

Protein binding Remifent

A

66-93%

78
Q

Protien Binding Sufent

A

92.5% to α1- acid glycoprotein

79
Q

Metabolism Liver/hepatic

A

codiene, sufentanil, meperidine 90%

80
Q

Metabolism Morphine

A

Glucoronic acid conjugation

metabolites:
Morphine -3 glucorinide (75-95%) INACTIVE
Morphine -6-glucoride: ACTIVE
Causes the late ventilatory depression

81
Q

Metabolism of Alfentanil & Fentanyl

A

CYP3A4

82
Q

Metabolism of Remifentanil

A

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
Q

Meperidine Metabolite

A

Normeperidine

84
Q

Does Hydromorphone have an active metabolite

A

Yes

85
Q

Metabolite of Alfentanil

A

Noralfentanil

86
Q

Metabolite of Fentanyl

A

Norfentanyl

87
Q

Effect site equilibration time (blood/brain)- alfentanil

A

1.4 minutes

88
Q

Effect site equilibration time (blood/brain)- fentanyl

A

6.8 min

89
Q

Effect site equilibration time (blood/brain)- Remifent

A

1.1 min

90
Q

Effect site equilibration time (blood/brain)- sufentanil

A

6.2 min

91
Q

1/2 time for codeine

A

3-3.5 hrs

92
Q

1/2 time for meperidine

A

3-5 hrs
**35 hrs with Renal failure

93
Q

1/2 time for morphine

A

1.5-3.5 hrs

94
Q

1/2 time for alfentanil

A

**cirrhosis prolongs E 1/2 time

95
Q

1/2 time for Remifent

A

6.3 minutes (99.8%)

96
Q

clearance for meperidine

A

1.02 L/min
Renal (acidic urine can speed up elimination)

97
Q

clearance for morphine

A

1.05 L/min

98
Q

clearance for fentanyl

A

Kidneys

99
Q

clearance for Remifent

A

kidneys (unaffected by renal or liver dx)
3L/min
**8x faster than alfentanil

100
Q

clearance for sufentanil

A

renal and fecal
***Caution with chronic renal failure

101
Q

First pass meperidine

A

Hepatic 80%

102
Q

First pass morphine

A

25% for PO,
NONE in lungs

103
Q

first pass for fentanyl

A

75% in lungs

104
Q

first pass for sufentanil

A

60% LUNG

105
Q

Context sensitive half time alfentanil

A

60 min

106
Q

Context sensitive half time fentanyl

A

260 min
Greater than sufentanil (d/t inactive tissue accumulation, will return to plasma and replace what has been metabolized)

107
Q

Context sensitive half time remifentanil

A

4 min

108
Q

Context sensitive half time sufent

A

30 min
“Shorter” - per castillo

109
Q

CNS effects codeine

A

MINIMAL SEDATION
DIZZINESS

110
Q

CNS effects meperidine

A

Sedation, Euphoria
SEROTONIN SYNDROME – careful with TCA’s and MAOI’s

111
Q

CNS effects Morphine

A

Analgesia, euphoria, sedation and diminished ability to concentrate

112
Q

CNS effects Fentanyl

A

‣Seizure like activity on SSEP and EEG with doses > 30 µg/kg IV
‣ ↑ ICP (6-9 mmHg)

113
Q

CNS effects Remifent

A

‣Seizure-like activity

114
Q

CV effects meperidine

A

Tachycardia, (-) inotropic

115
Q

CV effects morphine

A

Histamine release = ↓ BP

116
Q

CV effects hydromorphone

A

NO HISTAMINE RELEASE

117
Q

CV effects Fentanyl

A

‣ Depressed Carotid sinus barreceptor reflex = Bradycardia, ↓BP, ↓CO
NO histamine release

118
Q

CV effects Remifent

A

‣↓ B/P and HR

119
Q

CV effects Sufentanil

A

‣Bradycardia causes ↓CO

120
Q

Pulmonary

A

Meperidine: Depression of ventilation
Remifent: ‣ Synergistic depression of ventilation with propofol

121
Q

GI

A

They pretty much all cause NV except fro hydromorphone, fent, alfent, and sufent…

Remifent: does cause N/V

122
Q

Other side Effects codeine:

A

PHYSICAL DEPENDENCE

123
Q

Other Side effects meperidine:

A

TOXICITY: Delirium (confusion and hallucinations, myoclonus and seizures)
CROSSES PLACENTAL BARRIER!

124
Q

Other side effects morphine:

A

feeling of body warmth,
heaviness of extremities,
dryness of the mouth,
and pruritus.

125
Q

Side effects of fentanyl

A

SYNERGISM w/ Benzos and propofol

126
Q

side effects with Remifent

A

Hyperalgesia d/t previous acute exposure to large opioid doses and tolerance.

127
Q

Side effects with Sufent

A

CHEST WALL AND ABDOMINAL MUSCLE RIGIDITY.

128
Q

Clinical considerations with morphine

A

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
Q

Consideration for Alfentanil

A

USE IN PARKINSON’S = ACUTE DYSTONIA

130
Q

Other

A

Analogues: Fentanyl, Sufentanil, Alfentanil and Remifentanil

Withdrawal onset 2-6 hrs (faster than morphine)

131
Q

Chart

A
132
Q

What blocks pain at the Brain? Perception

A

opioid, a2 agonists, general anesthetics

133
Q

What blocks at the spinal cord? Modulation of afferent signals in the dorsal horn of spinal cord and production of reflex reaction

A

Local anesthetics, opioids, Ketamine, a2 agonists

134
Q

What blocks pain transmission of action potential via A(delta) and C fibers

A

Local anesthetics

135
Q

What blocks pain at Peripheral nociceptors (Transduction of mechanical, chemical and thermal stimuli into an action potential)

A

Local anesthetics, NSAIDs

136
Q

Unmyelinated C- fiber:

A

burning pain from heat and pressure from sustained pressure.

137
Q

Myelinated A-fiber:

A

Type I fibers ( Aβ & Aδ fibers): heat, mechanical, chemical

Type II fibers (Aδ fibers): heat

138
Q

Sensitization

A

Sensitization- hurts more over time.. Lowers threshold

139
Q

Secondary Hyperalgesia:

A

uninjured skin surrounding the injury (only from mechanical stimuli).
Sensitization of central neuronal circuits

140
Q

Primary Hyperalgesia: at the original site of injury from heat and mechanical injury.

A

Decreased pain threshold
Increased response to suprathreshold stimuli
Spontaneous pain
Expansion of receptive field

141
Q

Laminae III & IV:

A

NKI receptor with substance P

142
Q

Lamina II

A

(substantia gelatinosa [opioids]): afferent C Fibers

143
Q

Periaqueductal gray -rostral ventromedial medulla (PAG-RVM) system

A

Depress or facilitate the integration of pain info in the spinal dorsal horn.

144
Q

Excitatory impulses

A

Glutamate
Calcitonin
Neuropeptide Y
Aspartate
Substance P

145
Q

Inhibitory impulses

A

GABA
glycine
enkephalins
norepinephrine
dopamine

146
Q

Spinothalamic

A

Pain, temperature, and itch (Laminae I, VII, & VIII: All afferent fibers)

147
Q

Spinobulbar -cerebellum

A

Behavior toward pain (Laminae I, V, & VII)

148
Q

Spinohypothalamic

A

Autonomic, neuroendocrine, and emotional aspects of pain (Laminae I, V, VII, & X)

149
Q

Where is S1 and S2

A

Forebrain

Most of modulation of pain happens at forebrain or somatosensory cortex

150
Q

Hyperpolarize A-delta and C fibers

A

Decrease release of substance P
Opening of K+ channels/inhibition of Ca++ channels

151
Q

Neuropathic pain

A

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
Q

PAG-RVM system:

A

µ, κ, δ opioid receptors
hyperalgesia & Allodynia

153
Q

When do neonates have pain perception

A

23 weeks of gestation

A&P Texas Wes (8 decks)

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