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Pharmacology Exam 2 > Opioids > Flashcards

Opioids Flashcards

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1
Q

Which part of the pain pathway involves chemicals activating peripheral nerves and immune cells into an action potential?

A

Transduction

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2
Q

Which part of the pain pathway involves an electrical signal relayed through neurons in the afferent pathway along the spinothalamic tract?

A

Trasmission

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3
Q

Which part of the pain pathway involves the up and down regulation of pain signals?

A

Modulation

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4
Q

Which part of the pain pathway involves the processing of afferent pain signals in the cerebral cortex and limbic system?

A

Perception

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5
Q

What kind of pain is transmitted by A delta fibers?

A

fast, sharp pain that is well localized

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6
Q

What kind of pain is transmitted by C fibers?

A

slow, dull pain that is poorly localized

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7
Q

What are the two excitatory neurotransmitters that are important in the dorsal horn?

A

Glutamate & Substance P

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8
Q

How does inflammation contribute to pain?

A

-reduced threshold to pain stimulus
-increased response to pain stimulus

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9
Q

What drugs target transduction?

A

NSAIDs
Local anesthetics
Steroids
Antihistamines
Opioids

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10
Q

Where are the first, second, and third-order neurons located?

A

1st: periphery to dorsal horn
2nd: dorsal horn to thalamus
3rd: thalamus to cerebral cortex

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11
Q

What drugs target transmission?

A

local anesthetics

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12
Q

Where is the most important site of modulation?

A

substantia gelatinosa in the dorsal horn

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13
Q

Where does the descending inhibitory pathway begin?

A

the periaqueductal gray and the rostroventral medulla

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14
Q

How is pain inhibited?

A

-spinal neurons release GABA and glycine
-descending pathway releases NE, serotonin, and endorphins

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15
Q

How is pain augmented?

A

-central sensitization
-wind-up

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16
Q

What drugs target modulation?

A

neuraxial opioids
NMDA antagonists
alpha-2 agonists
AchE inhibitors
SSRIs
SNRIs

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17
Q

What drugs target perception?

A

general anesthetics
opioids
alpha-2 agonists

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18
Q

What is the mechanism of action of an opioid receptor?

A

-opioid binds to receptor
-G protein is activated
-adenylate cyclase is inhibited
-less cAMP is produced
-Ca+ conductance is decreased
-K+ conductance is increased

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19
Q

What is the precursor of Endorphins?

A

pre-proopiomelanocortin

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20
Q

What is the precursor of Enkephalins?

A

pre-enkephalin

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21
Q

What is the precursor of Dynorphins?

A

pre-dynorphin

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22
Q

What is the endogenous ligand for the mu receptor?

A

Endorphin

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23
Q

What is the endogenous ligand for the delta receptor?

A

Enkephalin

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24
Q

What is the endogenous ligand for the kappa receptor?

A

Dynorphin

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25
Which receptor subtype causes bradycardia?
mu
26
Which receptor subtype has no CNS effects?
delta
27
Which receptor subtype does not cause miosis?
delta
28
Which receptor subtype causes N/V, increased biliary pressure, and decreased peristalsis?
mu
29
Which receptor subtype does not cause pruritis?
kappa
30
Which receptor subtype has an anti-shivering effect?
kappa
31
What are the gender differences in women noticed with administration of morphine?
-greater analgesic potency -slower onset of action -longer duration of action -lower postoperative opioid consumption
32
Which drugs are naturally occurring phenanthrene derivatives?
morphine codeine thebaine
33
Which drugs are semisynthetic morphine derivatives?
hydromorphone heroin naloxone naltrexone
34
Which drugs are semisynthetic thebaine derivatives?
oxycodone
35
Which drugs are synthetic piperidines?
meperidine
36
Which drugs are synthetic phenylpiperidines?
fentanyl sufentanil remifentanil alfentanil
37
Which drugs are synthetic diphenylpropylamines?
Methadone
38
What is the order of relative potency of opioids with equianalgesic IV dose?
Meperidine (0.1-100 mg) Morphine (1-10 mg) Hydromorphone (7-1.4 mg) Alfentanil (10-1000 mcg) Remifentanil (100-100 mcg) Fentanyl (100-100 mcg) Sufentanil (1000-10 mcg)
39
What is the term for when a person taking a drug will go through withdrawal upon discontinuation of that drug?
dependence
40
What is the term for when a patient requires higher doses of a drug to achieve a given effect?
tolerance
41
What is the term for when tolerance to one drug produces tolerance to another drug that has similar functions or effects?
cross-tolerance
42
What is the term for when a person cannot stop using a drug despite the negative consequences from using that drug?
addiction
43
What are the signs and symptoms of opioid withdrawal?
early: diaphoresis, insomnia, restlessness late: abdominal cramping, N/V
44
Which of these has the longest duration of withdrawal? -methadone -morphine -fentanyl
methadone (6-7 weeks) morphine (7-10 days) fentanyl (4-5 days)
45
Which opioids have active metabolites?
morphine (M6G) meperidine (normeperidine)
46
Which opioids should be avoided in dialysis patients?
morphine and meperidine due to their active metabolites being excreted in the urine
47
What are the side effects of Normeperidine?
reduced seizure threshold and increased CNS excitability
48
What is Remifentanil dosage based on?
lean body weight *metabolized in the plasma
49
Which opioid should be avoided in patients taking MAO inhibitors?
Meperidine *risk of serotonin syndrome
50
What are the s/sx of serotonin syndrome?
hyperthermia mental status changes hyperreflexia seizures death
51
What are examples of MAO inhibitors?
phenelzine, isocarboxazid, and tranylcypromine
52
What are the anticholinergic effects of Meperidine?
tachycardia, mydriasis, dry mouth
53
Which opioids have an antishivering effect?
Meperidine & Butorphanol *kappa stimulation
54
Which opioids cause histamine release?
Meperidine Morphine Codeine
55
How is Alfentanil cleared?
Liver P450 enyzmes (3A4) *low hepatic extraction ratio
56
What is the most common use for Alfentanil?
blunting the hemodynamic response to short, intense periods of stimulation *tracheal intubation
57
What does the administration of Alfentanil and Erythromycin cause?
prolonged respiratory depression *erythromycin inhibits metabolism of Alfentanil
58
What receptor does Remifentanil target?
mu
59
What is the maintenance infusion dose of Remifentanil?
0.1-1 mcg/kg/min
60
How does the context-sensitive half-time change for Remifentanil?
no change, stays around 4 minutes regardless of infusion duration
61
What is a major side effect of Remifentanil and how can it be prevented?
-acute opioid-induced hyperalgesia -ketamine or magnesium sulfate
62
Which opioid should not be administered in the epidural or intrathecal space?
Remifentanil *solution contains glycine which is an inhibitory neurotransmitter
63
What is methadone useful for treating?
-chronic treatment of opioid abuse -chronic pain syndromes -cancer pain
64
What is the mechanism of action of methadone?
-mu receptor agonist -NMDA receptor antagonist -inhibits reuptake of monoamines in the synaptic cleft
65
What is the duration of action of Methadone?
3-6 hours
66
How is Methadone cleared?
liver P450 enzymes
67
What is a critical side effect of Methadone?
QT prolongation
68
What is the dose for Oliceridine?
load: 1-2 mg IV repeat: 1-3 mg IV cumulative: <27 mg
69
What are considerations to take into account for Oliceridine?
-QT prolongation -risk of hypotension with GA -risk of seizures with hx -risk of serotonin syndrome
70
Which medications are more likely to result in skeletal muscle rigidity?
Sufentanil Fentanyl Remifentanil Alfentanil
71
What is the best treatment for skeletal muscle rigidity?
paralysis and intubation
72
Which opioid is difficult to reverse by Naloxone?
Buprenorphine *high affinity for mu receptor
73
Which opioid is good for patients with a history of heart disease?
Nalbuphine
74
Which opioid has the side effect of reflexive coughing?
Fentanyl
75
Which opioid is used to treat itching caused by other opioids?
Nalbuphine & Naloxone (neuraxial opioids)
76
What is Naltrexone commonly used for?
ETOH withdrawal recovering opioid abusers
77
How long does it take to develop physical dependence of opioids?
about 25 days
78
What is the dose of Naloxone?
1-4 mcg/kg
79
What is the duration of action of Naloxone?
30-45 minutes
80
What are critical side effects of Naloxone administration?
SNS activation: neurogenic pulmonary edema, tachycardia, cardiac dysrhythmias, sudden death
81
What is the duration of action of Nalmefene?
10 hours
82
What is the duration of action of Naltrexone?
24 hours
83
What is a benefit to using Sufentanil?
longer period of analgesia with less respiratory depression
84
What is a major side effect of Sufentanil?
significant bradycardia which leads to a decreased CO and BP

Pharmacology Exam 2 (5 decks)

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