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Pharmacology > Lecture # 03_Fall > Flashcards

Lecture # 03_Fall Flashcards

1
Q

Define opioid.

A

any natural, synthetic, or endogenous substance with morphine-like properties

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2
Q

Name the 2 endogenous opioids.

A

[Met]-Enkephalin and Beta-Endorphin

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3
Q

What are the 2 most common opioid receptors?

A

Mu and Kappa

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4
Q

Opioids that act on the ___ receptors cause analgesia and sedation.

A

Kappa

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5
Q

Opioids that act on the ___ receptors case analgesia, respiratory depression, pruritis, and constipation.

A

Mu

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6
Q

T or F. Morphine provides analgesia without loss of touch or proprioception, but use is limited due to significant respiratory depression and loss of consciousness.

A

False. Morphine does not cause loss of consciousness. All other statements are true.

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7
Q

Where what is the function of nociceptive neurons and where can their receptors be found?

A

These neurons transmit pain. Receptors can be found throughout the CNS and in peripheral nerves.

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8
Q

What is the mechanism of action for opioids?

A

They inhibit release of and response to excitatory neurotransmitters in nociceptive neurons

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9
Q

Which opioid receptor is responsible for causing nausea, vomiting, and pupillary constriction?

A

it is unknown

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10
Q

What is the most rapid and complete route of absorption for opioids?

A

IV

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11
Q

IM absorption of Morphine and Meperidine takes about ___minutes.

A

20-60

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12
Q

Transmucosal absorption of Fentanyl takes about ___ minutes.

A

10

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13
Q

Transdermal absorption of Fentanyl takes about ___ hours.

A

14-24 hours

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14
Q

Benefits of neuraxial absorption of opioids includes ___, ___, and ___.

A

no sympathectomy, no motor blockade, no loss of proprioception.

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15
Q

10 mg of morphine IV = ___ epidural = ___ intrathecal (spinal).

A

10mg IV = 1mg epidural = 100mcg intrathecal

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16
Q

Biotransformation of opioids occurs mostly where?

A

Liver

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17
Q

Which opioid does not undergo metabolism in the liver? Where is it metabolized?

A

remifentanil is metabolized by plasma esterases by ester hydrolysis.

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18
Q

Which of the following need to be used more carefully with ESRD patients? Why?

A. Fentanyl
B. Morphine
C. Sufentanil
D. Remifentanil
E. Demerol
A

B (morphine) and E (Demerol / Meperidine) because they have active metabolites and are renally cleared.

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19
Q

What is the active metabolite of meperidine?

A

normeperidine

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20
Q

What is the active metabolite of morphine?

A

Morphine-6-glucuronide (M6G)

Morphine-3-glucuronide is a metabolite of morphine but it is not active as an opioid agonist - it does have some action as a convulsant, which does not appear to be mediated through opioid receptors; it is mediated by GABA/glycinergic system. As a polar compound, it has a limited ability to cross the blood–brain barrier, but renal failure may lead to its accumulation and result in seizures. (from Wikipedia)

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21
Q

How long does it take to develop a tolerance to opioids?

A

2-3 weeks

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22
Q

A tolerance to which of the following side effects of opioids can be acquired? Indicate all that apply.

A. analgesia
B. euphoria
C. sedation
D. ventilatory depression
E. Constipation
A

A tolerance to all except constipation can be acquired.

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23
Q

Define addiction.

A

physical and psychological dependence

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24
Q

Although some degree occurs within ___ days, addiction to opioids usually takes about __ days to develop.

A

2 days, 25 days

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25
Q

T or F. Addiction to opioids is usually life threatening.

A

False.

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26
Q

Symptoms of opioid withdrawal mimic severe flu-like illness. List the 11 symptoms seen with opioid withdrawal.

A

rhinorrhea, sneezing, yawning, lacrimation, abdominal cramping, leg cramping, piloerection, nausea, vomiting, diarrhea, and dilated pupils.

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27
Q

Peak symptoms of opioid withdrawal occur within ___ hrs and last up to ___ days.

A

72 hrs, 7-10 days

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28
Q

A patient that is over-narcotized will have ___ pupils whereas a person who is going through opioid withdrawals will have ___ pupils.

A

pinpoint, dilated

29
Q

T or F. Seizures, altered mental status, and hallucinations are commonly experienced by a person going through opioid withdrawals.

A

False. These are all rare.

30
Q

What receptor does Morphine act on?

A

Mu

31
Q

What is used to reverse opioid overdose?

A

naloxone (narcan)

32
Q

Does morphine cross the BBB?

A

Yes, but slowly

33
Q

Is morphine protein bound?

A

yes - binds to albumin

34
Q

Why does morphine cause hypoventilation?

A

it blunts hypercapnic response

35
Q

Why does morphine cause itching?

A

It causes a histamine release

36
Q

What is the advantage of hydromorphone over morphine?

A

it does not have active metabolites

37
Q

10mg of morphine = ___mg dilaudid IV

A

1.5

38
Q

Methadone is most commonly used for ___ and ____.

A

treatment of opioid withdrawal and chronic pain

39
Q

T or F. Heroin produces fast euphoria without nausea.

A

True

40
Q

___ is the only opioid with some local anesthetic properties.

A

Meperidine (Demerol)

41
Q

___ is often used in the PACU to reduce shivering.

A

Meperidine (Demerol)

42
Q

____ can cause CNS excitation, tremors, myoclonus, and seizures

A

Meperidine (Demerol)

43
Q

___ is a synthetic Mu receptor agonists that is about 100x more potent than morphine.

A

Fentanyl

44
Q

Why do Fentanyl, Sufentanil, and Alfentanil have rapid onset and redistribution to inactive sites?

A

they are very lipid-soluble and rapidly cross membranes

45
Q

T or F. Fentanyl is highly protein bound.

A

True. It is pH dependent though…acidosis leads to unbinding and more free drug

46
Q

___ is about 1000x more potent than morphine and 10x more potent than Fentanyl.

A

Sufentanil

47
Q

Chest wall rigidity is most commonly associated with high doses of ____.

A

Fentanyl

48
Q

The potency of ___ is between morphine and fentanyl.

A

Alfentanil

49
Q

Respiratory depression seen with Fentanyl is exacerbated when given with ____.

A

Versed

50
Q

T or F. Ultiva is metabolized by pseudocholinesterases.

A

False. Remifentanil (Ultiva) = ester hydrolysis by blood and tissue esterases.

51
Q

Remifentanil can decrease MAC by up to __%.

A

90%

52
Q

Partial agonists bind to Mu-receptor with lower ____.

A

Efficacy

53
Q

Which opioid is associated with hyperalgesia?

A

Remifentanil

54
Q

___ has good bioavailability, is a strong cough suppressant, and gets converted in to morphine in the body.

A

codeine

55
Q

___ + Acetaminophen = Roxicet, Percocet, or Percodan

A

Oxycodone and OxyContin

56
Q

____ + Acetaminophen = Vicodin or Lorcet

A

Hydrocodone (Lortab)

57
Q

Codeine + _____ = Tylenol #2, #3, #4

A

Acetaminophen

58
Q

100mg meperidine ~ ___mg Morphine ~ 1mg____ ~ ____mcg Fentanyl ~10mcg ____

A

100mg meperidine ~10mg Morphine ~ 1mg Hydromorphone ~ 100mcg Fentanyl ~10mcg Sufentanil

59
Q

10mg Morphine = ____ Fentanyl

A

100mcg

60
Q

Nalbuphine (Nubain) is a strong __ receptor agonist and ___ receptor antagonist.

A

Kappa agonist (analgesia and sedation)

Mu antagonist (analgesia, respiratory depression, pruritis, and constipation)

61
Q

Buprenorphine (Buprenex) is a partial ___ receptor agonist and ___receptor antagonist.

A

Mu agonist (analgesia, respiratory depression, pruritis, and constipation)

Kappa antagonist (analgesia and sedation)

62
Q

____ could reverse morphine-induced respiratory depression without compromise of analgesia

A

Nalbuphine (Nubain)

63
Q

____ has 50x greater affinity for the Mu receptor than morphine

A

Buprenorphine (Buprenex)

64
Q

_____ is used in management of chronic pain as well as opioid dependence . It binds more strongly to receptors than other opioids do.

A

Buprenorphine (Buprenex)

65
Q

T or F. Buprenorphine (Buprenex) has a prolonged duration of action due to slow dissociation from receptors and is resistant to antagonsim with narcan.

A

True

66
Q

Suboxone = ____ + ____

A

Buprenorphine + Naloxone

67
Q

___ is an opioid antagonist

A

Naloxone (Narcan)

68
Q

What does “context” refer to in “context-sensitive half time?” What is “context-sensitive half time?”

A

Context is the duration of the infusion prior o stopping it. Context-sensitive half time is the amount of time required for drug concentration in the central compartment to decrease by 50%

69
Q

Ccontext-sensitive half time increases as a function of the duration of infusion before it was stopped due to ____

A

movement of drug stored in the peripheral compartments back into the central compartment

Pharmacology (22 decks)

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