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Pharmacology Exam 2 > Opioids > Flashcards

Opioids Flashcards

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
Q

Which receptor subtype causes bradycardia?

A

mu

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26
Q

Which receptor subtype has no CNS effects?

A

delta

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27
Q

Which receptor subtype does not cause miosis?

A

delta

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28
Q

Which receptor subtype causes N/V, increased biliary pressure, and decreased peristalsis?

A

mu

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29
Q

Which receptor subtype does not cause pruritis?

A

kappa

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30
Q

Which receptor subtype has an anti-shivering effect?

A

kappa

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31
Q

What are the gender differences in women noticed with administration of morphine?

A

-greater analgesic potency
-slower onset of action
-longer duration of action
-lower postoperative opioid consumption

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32
Q

Which drugs are naturally occurring phenanthrene derivatives?

A

morphine
codeine
thebaine

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33
Q

Which drugs are semisynthetic morphine derivatives?

A

hydromorphone
heroin
naloxone
naltrexone

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34
Q

Which drugs are semisynthetic thebaine derivatives?

A

oxycodone

35
Q

Which drugs are synthetic piperidines?

A

meperidine

36
Q

Which drugs are synthetic phenylpiperidines?

A

fentanyl
sufentanil
remifentanil
alfentanil

37
Q

Which drugs are synthetic diphenylpropylamines?

A

Methadone

38
Q

What is the order of relative potency of opioids with equianalgesic IV dose?

A

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
Q

What is the term for when a person taking a drug will go through withdrawal upon discontinuation of that drug?

A

dependence

40
Q

What is the term for when a patient requires higher doses of a drug to achieve a given effect?

A

tolerance

41
Q

What is the term for when tolerance to one drug produces tolerance to another drug that has similar functions or effects?

A

cross-tolerance

42
Q

What is the term for when a person cannot stop using a drug despite the negative consequences from using that drug?

A

addiction

43
Q

What are the signs and symptoms of opioid withdrawal?

A

early: diaphoresis, insomnia, restlessness
late: abdominal cramping, N/V

44
Q

Which of these has the longest duration of withdrawal?
-methadone
-morphine
-fentanyl

A

methadone (6-7 weeks)

morphine (7-10 days)
fentanyl (4-5 days)

45
Q

Which opioids have active metabolites?

A

morphine (M6G)
meperidine (normeperidine)

46
Q

Which opioids should be avoided in dialysis patients?

A

morphine and meperidine due to their active metabolites being excreted in the urine

47
Q

What are the side effects of Normeperidine?

A

reduced seizure threshold and increased CNS excitability

48
Q

What is Remifentanil dosage based on?

A

lean body weight
*metabolized in the plasma

49
Q

Which opioid should be avoided in patients taking MAO inhibitors?

A

Meperidine
*risk of serotonin syndrome

50
Q

What are the s/sx of serotonin syndrome?

A

hyperthermia
mental status changes
hyperreflexia
seizures
death

51
Q

What are examples of MAO inhibitors?

A

phenelzine, isocarboxazid, and tranylcypromine

52
Q

What are the anticholinergic effects of Meperidine?

A

tachycardia, mydriasis, dry mouth

53
Q

Which opioids have an antishivering effect?

A

Meperidine & Butorphanol
*kappa stimulation

54
Q

Which opioids cause histamine release?

A

Meperidine
Morphine
Codeine

55
Q

How is Alfentanil cleared?

A

Liver P450 enyzmes (3A4)
*low hepatic extraction ratio

56
Q

What is the most common use for Alfentanil?

A

blunting the hemodynamic response to short, intense periods of stimulation
*tracheal intubation

57
Q

What does the administration of Alfentanil and Erythromycin cause?

A

prolonged respiratory depression
*erythromycin inhibits metabolism of Alfentanil

58
Q

What receptor does Remifentanil target?

A

mu

59
Q

What is the maintenance infusion dose of Remifentanil?

A

0.1-1 mcg/kg/min

60
Q

How does the context-sensitive half-time change for Remifentanil?

A

no change, stays around 4 minutes regardless of infusion duration

61
Q

What is a major side effect of Remifentanil and how can it be prevented?

A

-acute opioid-induced hyperalgesia
-ketamine or magnesium sulfate

62
Q

Which opioid should not be administered in the epidural or intrathecal space?

A

Remifentanil
*solution contains glycine which is an inhibitory neurotransmitter

63
Q

What is methadone useful for treating?

A

-chronic treatment of opioid abuse
-chronic pain syndromes
-cancer pain

64
Q

What is the mechanism of action of methadone?

A

-mu receptor agonist
-NMDA receptor antagonist
-inhibits reuptake of monoamines in the synaptic cleft

65
Q

What is the duration of action of Methadone?

A

3-6 hours

66
Q

How is Methadone cleared?

A

liver P450 enzymes

67
Q

What is a critical side effect of Methadone?

A

QT prolongation

68
Q

What is the dose for Oliceridine?

A

load: 1-2 mg IV
repeat: 1-3 mg IV
cumulative: <27 mg

69
Q

What are considerations to take into account for Oliceridine?

A

-QT prolongation
-risk of hypotension with GA
-risk of seizures with hx
-risk of serotonin syndrome

70
Q

Which medications are more likely to result in skeletal muscle rigidity?

A

Sufentanil
Fentanyl
Remifentanil
Alfentanil

71
Q

What is the best treatment for skeletal muscle rigidity?

A

paralysis and intubation

72
Q

Which opioid is difficult to reverse by Naloxone?

A

Buprenorphine
*high affinity for mu receptor

73
Q

Which opioid is good for patients with a history of heart disease?

A

Nalbuphine

74
Q

Which opioid has the side effect of reflexive coughing?

A

Fentanyl

75
Q

Which opioid is used to treat itching caused by other opioids?

A

Nalbuphine & Naloxone (neuraxial opioids)

76
Q

What is Naltrexone commonly used for?

A

ETOH withdrawal
recovering opioid abusers

77
Q

How long does it take to develop physical dependence of opioids?

A

about 25 days

78
Q

What is the dose of Naloxone?

A

1-4 mcg/kg

79
Q

What is the duration of action of Naloxone?

A

30-45 minutes

80
Q

What are critical side effects of Naloxone administration?

A

SNS activation: neurogenic pulmonary edema, tachycardia, cardiac dysrhythmias, sudden death

81
Q

What is the duration of action of Nalmefene?

A

10 hours

82
Q

What is the duration of action of Naltrexone?

A

24 hours

83
Q

What is a benefit to using Sufentanil?

A

longer period of analgesia with less respiratory depression

84
Q

What is a major side effect of Sufentanil?

A

significant bradycardia which leads to a decreased CO and BP

Pharmacology Exam 2 (5 decks)

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