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Pharmacology I > Lecture 03_Fall > Flashcards

Lecture 03_Fall Flashcards

2
Q

Define opioid.

A

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

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3
Q

Name the 2 endogenous opioids.

A

[Met]-Enkephalin and Beta-Endorphin

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4
Q

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

A

Kappa

they put a “Kap” on the unwanted effects

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5
Q

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

A

Mu

Mu rhymes with “BOO” - Mu has unwanted side effects…BOO!

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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.

Proprioception = “one’s own”, “individual” and perception, is the sense of the relative position of neighbouring parts of the body and strength of effort being employed in movement

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7
Q

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.

Nociception = “the neural processes of encoding and processing noxious stimuli.” It is the afferent activity produced in the peripheral and central nervous systems by stimuli that have the potential to damage tissue. This activity is initiated by nociceptors, (also called pain receptors), that can detect mechanical, thermal or chemical changes above a set threshold. Once stimulated, a nociceptor transmits a signal along the spinal cord, to the brain. Nociception triggers a variety of autonomic responses and may also result in a subjective experience of pain in sentient beings. Nociceptive neurons generate trains of action potentials in response to painful stimuli, and the frequency of firing signals the intensity of the pain. (from Wikipedia)

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8
Q

What are the 2 most common opioid receptors?

A

Mu and Kappa

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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 mechanism of action for opioids?

A

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

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11
Q

IM absorption of Morphine and Meperidine takes about ___minutes.

A

20-60

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12
Q

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

A

IV

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13
Q

Transmucosal absorption of Fentanyl takes about ___ minutes.

A

10

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14
Q

Transdermal absorption of Fentanyl takes about ___ hours.

A

14-24 hours

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15
Q

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

A

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

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16
Q

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

A

10mg IV = 1mg epidural = 100mcg intrathecal

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17
Q

Biotransformation of opioids occurs mostly where?

A

Liver

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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

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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20
Q

What is the active metabolite of morphine?

A

Morphine-6-glucuronide (M6G)

*Ask Dr. Altose about this b/c in my lecture he told us only MPG was active but in your notes he has them both listed as active metabolites…Wikipedia says this:

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

What is the active metabolite of meperidine?

A

normeperidine

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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. (A,B,C,D)

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23
Q

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

A

2-3 weeks

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24
Q

Define addiction.

A

physical and psychological dependence

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25
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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26
Q

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

A

False.

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27
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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28
Q

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

A

72 hrs, 7-10 days

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29
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

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30
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.

31
Q

What receptor does Morphine act on?

A

Mu

32
Q

Does morphine cross the BBB?

A

Yes, but slowly

5 min onset, but peak in 10-40 minutes

33
Q

Is morphine protein bound?

A

yes - 35% protein-bound - binds to albumin

34
Q

What is used to reverse opioid overdose?

A

naloxone (narcan)

35
Q

Why does morphine cause hypoventilation?

A

it blunts hypercapnic response

36
Q

Why does morphine cause itching?

A

It causes a histamine release

37
Q

What is the advantage of hydromorphone over morphine?

A

it does not have active metabolites

38
Q

10mg of morphine = ___mg dilaudid IV

A

1.5

39
Q

Methadone is most commonly used for ___ and ____.

A

treatment of opioid withdrawal and chronic pain

40
Q

T or F. Heroin produces fast euphoria without nausea.

A

TRUE

41
Q

___ is the only opioid with some local anesthetic properties.

A

Meperidine (Demerol)

42
Q

___ is often used in the PACU to reduce shivering.

A

Meperidine (Demerol)

43
Q

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

A

Meperidine (Demerol)

44
Q

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

A

Fentanyl

45
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

46
Q

T or F. Fentanyl is highly protein bound.

A

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

47
Q

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

A

Sufentanil

48
Q

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

A

Fentanyl

49
Q

The potency of ___ is between morphine and fentanyl.

A

Alfentanil

50
Q

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

A

Versed

51
Q

T or F. Ultiva is metabolized by pseudocholinesterases.

A

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

52
Q

Remifentanil can decrease MAC by up to __%.

A

90%

53
Q

Partial agonists bind to Mu-receptor with lower ____.

A

Efficacy

54
Q

Which opioid is associated with hyperalgesia?

A

Remifentanil

55
Q

___ + Acetaminophen = Roxicet, Percocet, or Percodan

A

Oxycodone or OxyContin

56
Q

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

A

codeine

57
Q

____ + Acetaminophen = Vicodin or Lorcet

A

Hydrocodone (Lortab)

58
Q

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

A

Acetaminophen

59
Q

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

A

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

60
Q

10mg Morphine = ____ Fentanyl

A

100mcg

61
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)

62
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)

63
Q

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

A

Nalbuphine (Nubain)

64
Q

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

A

Buprenorphine (Buprenex)

65
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)

66
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

67
Q

Suboxone = ____ + ____

A

Buprenorphine + Naloxone

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 to 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

Context-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

70
Q

___ is an opioid antagonist

A

Naloxone (Narcan)

71
Q

You are waking up a patient that has been fully reversed after confirming 4/4 TOF and sustained tetanus for 5sec, has almost no more gas on board (0.1 MAC), and EtCO2 is 57. They are taking adequate tidal volumes but their respiratory rate is

A

The may be over narcotized, and if they are it is not safe to extuabte them. You should look at their pupils. If they are over-narcotized they will be “pin-point” - you will know it when you see it - they get very small - in this case you should give them narcan. Titrate 20-40 mcg (0.02-0.04mg) every 1-2 minutes

72
Q

Which opioid receptor is responsible for constipation and urinary retention?

A

Delta

Pharmacology I (3 decks)

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