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Pharm 512 Drugs > Opioid, Opioid agonist/antagonist, antagonist Factoids > Flashcards

Opioid, Opioid agonist/antagonist, antagonist Factoids Flashcards

1
Q

What is the potency ratio of Sufentanil?

A

500-1000

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2
Q

How do opioids provide analgesia through the CNS?

A

Inhibiting the ascending transmission of nociceptive transmission from the spinal cord AND activate pain control pathways from the midbrain

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3
Q

What is the prototype opioid drug?

A

Morphine

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4
Q

What is the potency ratio of Alfentanil?

A

10-20

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5
Q

What opioid receptor has the largest concentration?

A

The Mu receptor has the largest concentration in the cerebral cortex, limbic system, caudate putamen, thalamus, periaqueductal grey matter and pre/post synaptic neurons in the spinal cord.

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6
Q

Where is the highest concentration of Mu receptors?

A

Periaqueductal Grey Matter

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7
Q

What is the potency ratio of Butorphanol (Stadol)?

A

5

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8
Q

What cardiovascular effects do opioids have?

A

Bradycardia with little effect on blood pressure and dose dependent peripheral vasodilation.

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9
Q

What is the most stimulating part of surgery?

A

Intubation, which means you need more drugs up front.

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10
Q

What is the active metabolite of morphine and in what instance should Morphine use be avoided?

A

Morphine-6-Glucuronide (M6G) is the active metabolite that prolongs Morphines effects. It should be avoided in renal patients due to decreased elimination.

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11
Q

What is the potency ratio of Codeine?

A

0.4

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12
Q

What is an undesirable quality of Morphine?

A

Histamine release, it should be avoided in asthmatics and hemodynamically unstable patients.

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13
Q

What is the metabolite of Meperidine (Demerol) and what’s its disadvantage?

A

Normeperidine - lowers seizure threshold

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14
Q

What drug potentiates muscle rigidity in Remifentanyl use?

A

Nitrous Oxide, most significantly seen with chest wall compliance and truncal rigidity.

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15
Q

What is the major benefit to Dilaudid?

A

There is no known active metabolite, good for use in renal patients.

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16
Q

What opioid receptor reduces shivering, and causes dysphoria, sedation mitosis and analgesia?

A

Kappa Receptors

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17
Q

What is the potency ratio of Fentanyl and Remifentanyl?

A

100

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18
Q

What is unique about Fentanyl’s metabolism?

A

Fentanyl undergoes significant 1st pass effect in the lungs, however clearance is dependent on hepatic blood flow.

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19
Q

Why isn’t Alfentanil widely used?

A

There is great patient to patient variability, not very predictable.

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20
Q

What is the potency ratio of Buprenorphine?

A

30

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21
Q

How is Remifentanyl metabolized?

A

Metabolized by non-specific blood esterases (be aware when giving to patient with cholinesterase deficiency)

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22
Q

What can occur in a chronic drug user when given pain medication?

A

Down regulation of one receptor causes use of another receptor that isn’t as effective. May have to give more medication to alleviate pain.

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23
Q

What opioid agonist-antagonist has the same potency as Morphine?

A

Nubaine

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24
Q

How do opioids effect the eyes?

A

Parasympathetic stimulation of the oculomotor nerve causes vasoconstriction this is known as Miosis (small pupils)

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25
Q

What is the most potent phenylpiperidine?

A

Sufentanil

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26
Q

Meperidine (Demerol) use is contraindicated with which drug class?

A

MAOI, significant reaction and possible seretonergic crisis

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27
Q

What is the potency ratio of Meperidine (Demerol)?

A

0.1

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28
Q

Why aren’t opioids considered anesthetics?

A

Opioids do not provide amnesia and the patient will have recall if not given another medication

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29
Q

Where are Kappa receptors located in the CNS?

A

Nucleus raphe mangnus (midbrain)
Hypothalamus
Spinal Cord

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30
Q

Which opioid receptor provides analgesia, mild constipation, urinary retention, and dependence?

A

Delta Receptors

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31
Q

if a patient is not intubated, how can opioids effect ICP?

A

Opioids can increase ICP by hypoventilation which causes vasodilation and increased cerebral blood flow

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32
Q

What are the effects of stimulating the Mu opioid receptor?

A

Analgesia, euphoria, sedation, dependence, respiratory depression, miosis, marked constipation, urinary rentention, bradycardia, pruritus, muscle rigidity and biliary spasm

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33
Q

Where are Delta opioid receptors located in the CNS?

A 
Olfactory centers
Cerebral cortex
Nucleus accembens
Caudate putmen
Spinal Cord
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34
Q

True or false, respiratory depression is a very sensitive indicator of opioid effects?

A

False, respiratory depression is NOT a very sensitive indicator of opioid effects. (the respiratory drive is separate from analgesia)

35
Q

How do opioids effect the respiratory system?

A

Opioids produce dose dependent depression of ventilatory response of CO2 by directly affecting the ventilatory centers in the medulla.

36
Q

What cardiovascular mechanisms are not effected by opioid agents?

A

Opioids have no effects on myocardial contractility, baroreceptor reflexes and autonomic responsiveness.

37
Q

What causes generalized hypertonus that is associated with high dose opioids?

A

Mu receptors and dopamine and GABA pathways

38
Q

What drugs can relieve the muscle rigidity associated with opioids?

A

Relieved by muscle relaxants and antagonists (succinylcholine)

39
Q

What is the least lipophilic opioid agent?

A

Morphine

40
Q

Why is Codeine thought to be a weak opioid?

A

10% is converted to morphine

41
Q

What opioid is structurally similar to atropine?

A

Meperidine (Demerol) has antispasmodic properties

42
Q

What opioid can be given post operatively to reduce shivering?

A

Meperidine (Demerol), works at the Kappa receptors

43
Q

What opioid is the most lipid soluble?

A

Sufentanil

44
Q

Why shouldn’t we bolus Remifentanil?

A

Increased risk for muscle rigidity, limits bolus dosing

45
Q

What opioid can not be used in an epidural?

A

Remifentanil, it causes glycine neurotoxicity

46
Q

Define Agonist

A

Drugs that occupy a receptor and activate them

47
Q

Define Antagonist

A

Drugs that occupy receptors but do not activate them, antagonists block receptor activation by agonists.

48
Q

How do antagonists, agonists and partial agonists effect their receptor sites?

A

Agonists exhibit unlimited effect
partial agonists reach maximum effect after specific dose
True antagonists never exhibit the clinical effect

49
Q

What types of drugs have a ceiling effect?

A

Partial agonists

50
Q

What does a steep dose response curve indicate?

A

The drug is more responsive with higher doses, small changes in dose produce large effects

51
Q

Which drug’s antagonistic affects relates to its ability to displace opioid agonists from their receptors?

A

Buprenorphine

52
Q

Which receptor site does Buprenorphine compete for?

A

Mu

53
Q

Which antagonist-agonist opioid is an agonist at the Kappa receptor and a weak antagonist at the Mu receptor?

A

Butorphanol

54
Q

Why aren’t we as worried about respiratory depression in opioid agonist-antagoinist agents?

A

Respiratory depression exhibits a ceiling effect in opioid agonist-antagoinist agents

55
Q

What factors should be considered if you are using an agonist-antagonist as a primary analgesic?

A

Consider the options for rescue or further treatment of pain

56
Q

What is a non-selective antagonist at all opioid receptors?

A

Naloxone, treats opioid induced respiratory depression, pruritus and suspected drug overdose

57
Q

How should Naloxone be administered?

A

Naloxone should be given in small incremental doses because it can cause flash pulmonary edema.

58
Q

Which opioid antagonist has an active metabolite?

A

Naltrexone

59
Q

Which agonist antagonist opioid agent causes an increase in cardiovascular effects and why?

A

Butorphanol causes an increase in circulating catecholamines

60
Q

Which partial opioid agonist is very slow to dissociate from the opioid receptor?

A

Buprenorphine, there is not a rescue drug for this, should be used with caution

61
Q

Where is nociception suppressed in neuraxial opioids?

A

Lamina II and V cells of the dorsal horn of the spinal cord and Kappa receptors in the substantia gelatinosa

62
Q

What two side effects are seen more in neuraxial opioids than if the opioid was given IV?

A

Greater incidence of pruritus and urinary retention

63
Q

What is the difference between spinal anesthesia and an epidural?

A

Spinal anesthesia is injected into the CSF on the spinal cord where an epidural is placed in the potential space

64
Q

What three factors determine opioid uptake from neuraxial anesthesia?

A

Epidural fat
CSF
Systemic circulation of blood

65
Q

Why is it beneficial to add epinephrine to a neuraxial opioid?

A

Epi constricts the vessels decreasing blood flow and keeping the medication in the the affected area longer

66
Q

What two opioid agents are associated with early respiratory depression in neuraxial anesthesia?

A

Fentanyl and Sufentanil ( <2 hrs) central circulation

67
Q

What opioid agent is associate with delayed respiratory depression in neuraxial anesthesia?

A

Morphine ( >2hrs) ventral medulla

68
Q

What determines how fast or slow an opioid will take effect in neuraxial anesthesia?

A

Dependent on the lipid solubility of the drug

69
Q

What is the major cause of respiratory depression in neuraxial anesthesia?

A

Additional medication given because time was not allowed for epidural/spinal to work

70
Q

What is the intrathecal or subarachnoid single dose of Fentanyl?

A

5-25 mcg

71
Q

What is the intrathecal or subarachnoid single dose of Morphine?

A

0.1-0.3 mg

72
Q

What is the epidural single dose of Fentanyl?

A

50-100mcg

73
Q

What is the epidural single dose of Morphine?

A

1-5mg

74
Q

What is the epidural continuous infusion of Fentanyl?

A

25-100mcg/hr

75
Q

What is the epidural continuous infusion of Morphine?

A

0.1-1mg/hr

76
Q

What is the onset and duration of Alfentanil in comparison to fentanyl?

A

Alfentanil has a more rapid onset and a shorter duration of action than fentanyl.

77
Q

What type of surgery would warrant the use of Nalbuphene (Nubain) for post-operative pain management?

A

Brain surgery! Because it reverses sedative qualities.

78
Q

Why is continuous monitoring important after a dose of Narcan is given?

A

Because of its short half-life in comparison to opioids, respiratory depression may return once Narcan wears off.

79
Q

Which opioid agonist-antagonist is useful in the cardiovascular population?

A

Nalbuphine (Nubian)

80
Q

What adverse effects does Naloxone have on the body?

A

Nausea and Vomiting
Increased SNS activity
Pulmonary edema
Sudden death

81
Q

What drug is often given to drug addicts to prevent the euphoric effects of the drug they abuse?

A

Naltrexone

82
Q

Why is the SNS unable to be activated during neuraxial opioid administration?

A

SNS is inhibited due to blockage of the sympathetic chain ganglia

83
Q

Where can neuraxial opioids be given?

A

Can be given via epidural and intrathecal routes

Pharm 512 Drugs (16 decks)

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