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NGR6462 Pharm & Chem Anesthesia I > Opioid Agonist & Antagonist > Flashcards

Opioid Agonist & Antagonist Flashcards

1
Q

A synthetic analog of codeine

A

Tramadol (Ultram)

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2
Q

This prodrug is helpful with pain management in patients unable to take NSAIDs

A

Tramadol (Ultram)

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3
Q

Tramadol MOA

A

Weak mu agonist from inhibition of NE and serotonin and presynaptic stimulation of 5-HTP release.

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4
Q

How does Naloxone effect Tramadol SE?

A

analgesia partially intact
respiratory depression reversed

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5
Q

Toxicity seen in Tramadol overdose is related to what?

A

amine uptake inhibition

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6
Q

Tramadol is a racemic mixture, what are the effects of the + and - enantiomers?

A

+ binds to mu and decreases serotonin while the - inhibits NE uptake and stimulates alpha 2 receptors

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7
Q

Tramadol(Ultram) half-life:

A

5-6h

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8
Q

Significant CNS SE of Tramadol

A

Seizures

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9
Q

Tramadol toxicity symptoms include:

A

hypotension, bradycardia, seizures, coma, rhabdomyolysis

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10
Q

Disadvantages of Tramadol:

A

Interaction with Warfarin, occurrence of serotonin syndrome, and increased risk of seizures in epileptic/high-risk patients.

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11
Q

Tramadol (Ultram) causes what significant GI side effects?

A

High incidence of N/V

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12
Q

Why is PO use of meperidine limited?

A

Significant first-pass effect

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13
Q

Meperidine interacts with which class of drugs, and how do the SE present?

A

MAOIs; respiratory depression, excitation, and delirium

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14
Q

How does Meperidine toxicity present, and what is the cause?

A

Active metabolite Normeperidine leads to CNS excitation and seizures.

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15
Q

Use of Meperidine (Demerol) in anesthesia:

A

postop shivering

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16
Q

The potency of meperidine to morphine:

A

Meperidine has 1/10 the potency of morphine.

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17
Q

What SE occur if Meperidine is given in high enough doses?

A

negative inotropic and histamine release

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18
Q

What are these symptoms reflective of? Autonomic instability with hypertension, tachycardia, diaphoresis, hyperthermia, behavioral changes including confusion and agitation, and neuromuscular changes manifesting as hyperreflexia

A

Serotonin Syndrome

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19
Q

Severe Serotonin Syndrome symptoms include:

A

Coma, seizures, coagulopathy, and metabolic acidosis

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20
Q

Which medications place patients at increased risk of Serotonin Syndrome?

A

Those on medication including MAOIs, Fluoxetine, and other antidepressants.

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21
Q

Meperidine receptor activity:

A

Mu & Kappa agonist

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22
Q

Fentanyl receptor activity:

A

Mu antagonist

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23
Q

Fentanyl v. morphine potency:

A

Fentanyl 100x more potent than morphine.

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24
Q

After high doses of fentanyl, dopaminergic stimulation in the corpus striatum may lead to what SE?

A

Muscle rigidity

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25
Q

This accounts for the rapid onset and duration of fentanyl:

A

high lipid solubility

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26
Q

Fentanyl peak effect:

A

3-5m

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27
Q

Fentanyl Vd

A

4L/kg

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28
Q

What happens when fentanyl doses exceed 20mcg/kg?

A

Redistribution is insufficient to drop plasma levels as fentanyl sequesters itself in the lungs.

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29
Q

Fentanyl induction dose:

A

1-2mcg/kg

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30
Q

Fentanyl metabolism:

A

Lungs (75%) & Liver (phase 1)

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31
Q

Which opioid requires reduced doses of benzos, propofol, or IA with induction:

A

Fentanyl (Sublimaze)

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32
Q

Pros of sole fentanyl use in anesthesia

A

lacks cardiac depressant and histamine effects, and also suppresses stress

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33
Q

Cons to sole fentanyl use in anesthesia:

A

fails to blunt SNS, awareness, ventilatory depression

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34
Q

Compare the potency of sufentanil to both fentanyl and morphine:

A

Sufentanil is 1000x more potent than morphine and 100x more potent than fentanyl.

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35
Q

Sufentanil has greater affinity for opioid receptors and a shorter EHL than fentanyl, why?

A

Twice as lipophilic as fentanyl

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36
Q

Sufentanil induction & infusion doses:

A

IVP: 0.1-0.2mcg/kg
Infusion: 0.1-0.2mcg/kg/hr

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37
Q

Alfentanil potency v fentanyl; alfentanil v. morphine:

A

Alfentanil is 1/3 potency of fentanyl, alfentanil is 20x more potent than morphine

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38
Q

Compare lipid solubility of alfentanil and fentanyl:

A

Alfentanil is less lipid soluble than fentanyl

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39
Q

Why did alfentanil lose popularity?

A

Unpredictable responses to medication administration, and the development of remifentanil.

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40
Q

What drug has been shown to prolong the metabolism of alfentanil (Alfenta) leading to prolonged respiratory depression and sedation?

A

Erythromycin

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41
Q

Drug 100x more potent than morphine, and equipotent to fentanyl:

A

Remifentanil

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42
Q

Metabolism of Remifentanil:

A

Non-specific plasma and tissue esterases

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43
Q

How does the Vd of remifentanil compare to the other opioids?

A

smallest Vd

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44
Q

Remifentanil CSHT:

A

<5 minutes

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45
Q

Remifentanil has the potential to cause glycine neurotoxicity, how does this impact administration?

A

No epidural/intrathecal administration

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46
Q

What plan should be in place for patients on remifentanil in the OR once they head to the PACU.

A

The administration of a longer-acting opioid.

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47
Q

This drug is an NMDA antagonist used in heroin addiction, it is a racemic mixture with a long half-life and has the potential to prolong QT intervals:

A

Methadone (methadose, dolophine)

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48
Q

Opioid usually combined with Tylenol:

A

Hydrocodone

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49
Q

This oral opioid is 10x more potent than morphine, has rapid onset, but poses high risk of N/V:

A

Oxymorphone (Opana)

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50
Q

This prodrug is metabolized into morphine. It is used as a cough suppressant, and has minimal sedation, but can lead to N/V, constipation, and dizziness:

A

Codeine

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51
Q

Patients lacking CYP2D6 or taking Quinidine will have difficulty metabolizing this drug into it’s active form:

A

Codeine

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52
Q

Rapid metabolizers of codeine experience:

A

Toxicity

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53
Q

Pure opioid competitive antagonist:

A

Naloxone (narcan)

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54
Q

Naloxone dose:

A

0.4-0.8mg IV
onset 1-2m
duration 1-4h

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55
Q

Naloxone SE:

A

Pain
Pulmonary edema
sudden death

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56
Q

This peripheral opioid mu antagonist maintains analgesia while also treating delayed gastric emptying and N//V.

A

Methylnaltrexone (Relistor)

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57
Q

Mu selective oral peripheral antagonist that depends on gut flora for metabolism, is approved for ileus and constipation treatment, but could lead to unwanted CV effects:

A

Alvimopan (Entereg)

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58
Q

Peripherally acting mu-opioid antagonist with high abuse potential, used for constipation:

A

Naloxegol (Movantik)

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59
Q

This oral opioid antagonist with high oral efficacy, used in the treatment of opioid dependence and ETOH withdrawal; however, active metabolite can lead to prolonged elimination:

A

Naltrexone (Vivitrol)

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60
Q

All opioid agonist-antagonists have a ceiling on their clinical effects, what does this mean?

A

Increased doses will not increase respiratory depression or analgesic effects further.

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61
Q

What effects seen with opioid agonist-antagonist differ from pure agonists?

A

Dysphoria, competitive antagonism at mu receptors, and agonize kappa receptors.

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62
Q

This agonist-antagonist reverses narcotic-induced postop ventilatory depression, maintains analgesia, and relieves itching.

A

Nalbuphine-Nubain

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63
Q

NSAIDs act as:

A

analgesic, antipyretic, and anti-inflammatory

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64
Q

Acetaminophen acts as:

A

analgesic, antipyretic
minimal anti-inflammatory

65
Q

NSAIDs: Inhibition of ______ leads to platelet aggregation.

A

COX-1

66
Q

NSAID use is avoided in what patients:

A

GI ulcers/bleeds, H. Pylori, caution in colorectal surgery

67
Q

act additively with antiplatelet agents resulting in increased bleeding risk:

A

NSAIDs (non-specific)

68
Q

What unwanted side-effect results from giving NSAIDs along with phenytoin, valproic acid, or digoxin?

A

increased plasma concentrations and toxicity: dig, valproic acid, phenytoin

69
Q

Which drug, when given with aspirin, decrease plasma salicylate concentrations?

A

corticosteroids

70
Q

This drug causes irreversible inhibition of COX enzymes

A

Aspirin

71
Q

What drug levels are associated with mild, moderate, and severe ASA toxicity?

A

mild: 300-600mg/L
moderate: 600-800mg/L
severe: >800mg/L

72
Q

ASA toxicity symptoms:

A

nausea, vomiting, abd pain, tinnitus, hearing impairment, CNS depression

73
Q

ASA toxicity symptoms with higher doses:

A

metabolic acidosis, renal failure, agitation, confusion, hyperventilation with respiratory alkalosis

74
Q

Acidemia has what effect on ASA absorption?

A

more readily crosses the BBB

75
Q

ASA toxicity treatment

A

Hydration, activated charcoal (in 1hr), alkalinization of urine.
Severe cases require HD.

76
Q

NSAID: potent analgesic, moderate anti-inflammatory

A

Ketorolac (Toradol)

77
Q

Ketorolac dose:

A

30-60mg IV

78
Q

Ketorolac is contraindicated in what patients?

A

renal impairment, ASTHMA, bleeding disorders, ASA sensitivity, nasal polyps, lactating mothers

79
Q

Dexamethasone (Decadron) has what SE that is useful in anesthesia

A

antiemetic

80
Q

NSAID contraindicated in perioperative CABG patients:

A

Ibuprofen (Caldolor)

81
Q

What effect do NSAIDs have on the CV system?

A

It may increase the risk of serious cardiovascular (CV) thrombotic events, myocardial infarction, and stroke, which can be fatal. The risk may increase with the duration of use.

82
Q

Caldolor (Ibuprofen) is contraindicated in:

A

asthma, pregnancy, periop during a CABG.

83
Q

Common SE with Gabapentin:

A

dizziness, somnolence

84
Q

Which drug binds to auxiliary subunits 1 and 2 Ca2+ channels , reduce calcium currents. It Halts new synapses decreases sympathetic tone.

A

Gabapentin

85
Q

Approved for postherpetic neuralgia and partial seizures

A

Gabapentin

86
Q

common adverse reactions in patients treated with______were nausea, vomiting, headache, and insomnia in adult patients and nausea, vomiting, constipation, pruritus, agitation, and atelectasis in pediatric patients

A

Ofirmev

87
Q

Ofirmev is approved for patients. of what age?

A

2 and older

88
Q

Max single dose v. max daily for Ofirmev:

A

Single max: 1000mg
Daily max: 4000mg

89
Q

Magnesium MOA

A

regulation of calcium influx into cells and antagonism of NMDA receptors in the CNS, this blocks painful stimuli allowing narcotics to work better.

90
Q

Ketamine MOA

A

NMDA non-compitative antagonism

91
Q

Why would one give glucagon during a Lap choly procedure?

A

Opens biliary duct

92
Q

Respiratory depression is expected during a spinal except under what circumstances?

A

The patient is sitting when the spinal was given (lowest risk).

93
Q

receptor responsible for neuraxial effects of opioids

A

Mu 2

94
Q

Why is Toradol (Ketorolac) not given to asthma patients?

A

Bronchospasm

95
Q

Nubain classification

A

Agonist antagonist

96
Q

What is the result of the active metabolite morphine-6-glucuronide?

A

analgesia and respiratory depression via mu 2 receptor

97
Q

Increased lipid solubility translates to:

A

rapid drug onset

98
Q

decreased RR is due to what receptor?

A

mu 2

99
Q

Pure opioid antagonist

A

Narcan (Naloxone)

100
Q

Difficulty with ventilation after giving sufentanil is due to what?

A

chest wall rigidity

101
Q

side effects of neuraxial epidurals:

A

respiratory depression, itching, N/V, urine retention, sedation, CNS excitation, herpes virus reactivation

102
Q

How is remifentanil metabolized?

A

nonspecific esterases

103
Q

Where is substance P found?

A

Substantial gelatin

104
Q

Why would a shivering patient not receive demerol?

A

They are on MAOI/psych meds

105
Q

why is fentanyl eliminated more quickly than morphine?

A

more lipid soluble, and a larger Vd

106
Q

Morphine onset

A

15-30m

107
Q

Morphine half time

A

1.7-3.3h

108
Q

Effect of morphine on the immune system?

A

histamine release

109
Q

Meperidine effects what receptors?

A

Mu and kappa

110
Q

Meperidine effect on pupils:

A

mydriasis

111
Q

Why would we use nubain?

A

relieve itching while maintaining analgesia.

112
Q

Toradol is contraindicated in:

A

asthma

113
Q

Which opioid requires a drip to maintain therapeutic range?

A

remifentanil

114
Q

Effects of opioids on GI

A

spasm of biliary smooth muscle, decreased LES, increased pyloric tone and sphincter of oddi tone

115
Q

Effects of opioids on respiratory:

A

Increased RR, decreased TV, chest wall rigidity

116
Q

Where do opioid agonists work? (locations, not receptor)

A

pre & post synaptic, spinal cord, peripherals

117
Q

presynaptic release of _____ stops substance P.

A

glutamate

118
Q

A decrease in what cation results in diminished action potential and signaling. (decreased pain)

A

Calcium

119
Q

This opioid agonist may cause an increase in HR and negative inotropy due to histamine release:

A

Meperidine (Demerol)

120
Q

Methadone receptors

A

mu, delta agonist, NMDA antagonist

121
Q

Can lead to QT prolongation and torsades:

A

Methadone

122
Q

Least lipophilic opioid agonist, causes extreme itching, and can lead to urine retention

A

Morphine

123
Q

Remifentanil CSHL and wake up time?

A

cshl is <5 min, wake up in 20m

124
Q

Naloxone (Narcan) SE:

A

Increased RR, NV, sphincter spasm, decreased sedation, itching, pulm. edema, pain, sudden death

125
Q

How long should one wait between doses of Naloxone?

A

3-5m

126
Q

Agonist-antagonist MOA

A

Compete with opioids for mu receptors

127
Q

Butorphanol (stadol) receptors

A

Kappa agonist, mu antagonist

128
Q

Buprenorphine (Subutex) receptor

A

weak mu agonist, weak kappa antagonist

129
Q

Buprenorphine (Subutex) should be stopped 2-4 wks before surgery; why?

A

not fully reversible with Narcan

130
Q

How long are platelets inhibited after the use of NSAIDs?

A

7 days

131
Q

This drug’s antipyretic effect may mask post-op fever:

A

Ofirmev (acetaminophen)

132
Q

How often is Ofirmev given to maintain SS?

A

Q6H

133
Q

Avoid use of this NSAID with epileptic/ those at risk for seizures:

A

Tramadol (Ultram)

134
Q

Alkaloid extract most widely used to relieve pain:

A

Morphine

135
Q

Opioids bind to ________ that are associated with mu receptors.

A

G-proteins

136
Q

Endogenous opioids are released by ______.

A

interneurons

137
Q

What two mechanisms occuring at the mu opioid receptor result in the decreased transmission of pain?

A

Inhibition of presynaptic glutamate release
Increased potassium conductase across the post-synaptic membrane.

138
Q

How does dosing for chronic and acute alcohol use differ?

A

acute intox= decreased dose
chronic intox= increased dose
(phase 1 enzyme induction-Py1)

139
Q

Drug withdrawal symptoms:

A

diaphoresis, lacrimation, coryza, insomnia, restlessness

140
Q

Severe withdrawal symptoms peaking in 72 hours & diminish progressively over 7-10 days:

A

abd cramps, N/V, diarrhea

141
Q

Opioids metabolized by phase I:

A

Fentanyl, alfentanil, sufentanil, methadone

142
Q

Opioids metabolized by phase 2:

A

Hydromorphone, Meperidine, Morphine

143
Q

Receptor related to euphoria

A

mu1

144
Q

receptor related to drug dependence and depressed RR

A

Mu2

145
Q

receptor related to constipation:

A

mu2

146
Q

receptor related to hallucinations

A

Kappa

147
Q

endogenous ligand for delta receptors:

A

enkephalins

148
Q

This drug is used to suppress cough. Does not produce analgesia or depress ventilation:

A

Codeine

149
Q

These drugs are associated with reflex coughing:

A

fentanyl, sufentanil, alfentanil

150
Q

How is the CO2/hypoxia response curve affected by opioids?

A

decreased response, shifts right

151
Q

What CV SE can express in patients with increased SNS activity?

A

hypotension (worse)

152
Q

These two drugs have the most histamine release:

A

morphine and meperidine

153
Q

Codeine 60mg is equivalent to what dose of ASA?

A

650mg

154
Q

Codeine 120mg IM is equivalent to how much morphine?

A

10mg

155
Q

Heroine (diacetylmorphine) v. morphine potency:

A

Heroine is 2.5x more potent than morphine

156
Q

This drug is five times more potent than morphine leading to increased sedative effects.

A

Hydromorphone (Dilaudid)

157
Q

Can cause serotonin syndrome

A

Tramadol, meperidine

158
Q

Alfentanil pKa

A

6.5

159
Q

Narcan preperation

A

0.4mg/cc, dilute with 10cc to make 0.04mg/cc

NGR6462 Pharm & Chem Anesthesia I (4 decks)

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