Lecture 03_Fall

Question 2

Define opioid.

Answer 2

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

Question 3

Name the 2 endogenous opioids.

Answer 3

[Met]-Enkephalin and Beta-Endorphin

Question 4

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

Answer 4

Kappa

they put a “Kap” on the unwanted effects

Question 5

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

Answer 5

Mu

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

Question 6

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.

Answer 6

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

Question 7

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

Answer 7

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)

Question 8

What are the 2 most common opioid receptors?

Answer 8

Mu and Kappa

Question 9

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

Answer 9

it is unknown

Question 10

What is the mechanism of action for opioids?

Answer 10

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

Question 11

IM absorption of Morphine and Meperidine takes about ___minutes.

Answer 11

20-60

Question 12

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

Answer 12

IV

Question 13

Transmucosal absorption of Fentanyl takes about ___ minutes.

Answer 13

10

Question 14

Transdermal absorption of Fentanyl takes about ___ hours.

Answer 14

14-24 hours

Question 15

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

Answer 15

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

Question 16

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

Answer 16

10mg IV = 1mg epidural = 100mcg intrathecal

Question 17

Biotransformation of opioids occurs mostly where?

Answer 17

Liver

Question 18

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

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

Answer 18

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

Question 19

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

Answer 19

remifentanil is metabolized by plasma esterases by ester hydrolysis.

Question 20

What is the active metabolite of morphine?

Answer 20

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)

Question 21

What is the active metabolite of meperidine?

Answer 21

normeperidine

Question 22

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

Answer 22

A tolerance to all except constipation can be acquired. (A,B,C,D)

Question 23

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

Answer 23

2-3 weeks

Question 24

Define addiction.

Answer 24

physical and psychological dependence

Question 25

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

Answer 25

2 days, 25 days

Question 26

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

Answer 26

False.

Question 27

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

Answer 27

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

Question 28

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

Answer 28

72 hrs, 7-10 days

Question 29

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

Answer 29

pinpoint, dilated

Question 30

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

Answer 30

False. These are all rare.

Question 31

What receptor does Morphine act on?

Answer 31

Mu

Question 32

Does morphine cross the BBB?

Answer 32

Yes, but slowly 5 min onset, but peak in 10-40 minutes

Question 33

Is morphine protein bound?

Answer 33

yes - 35% protein-bound - binds to albumin

Question 34

What is used to reverse opioid overdose?

Answer 34

naloxone (narcan)

Question 35

Why does morphine cause hypoventilation?

Answer 35

it blunts hypercapnic response

Question 36

Why does morphine cause itching?

Answer 36

It causes a histamine release

Question 37

What is the advantage of hydromorphone over morphine?

Answer 37

it does not have active metabolites

Question 38

10mg of morphine = ___mg dilaudid IV

Answer 38

1.5

Question 39

Methadone is most commonly used for ___ and ____.

Answer 39

treatment of opioid withdrawal and chronic pain

Question 40

T or F. Heroin produces fast euphoria without nausea.

Answer 40

TRUE

Question 41

___ is the only opioid with some local anesthetic properties.

Answer 41

Meperidine (Demerol)

Question 42

___ is often used in the PACU to reduce shivering.

Answer 42

Meperidine (Demerol)

Question 43

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

Answer 43

Meperidine (Demerol)

Question 44

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

Answer 44

Fentanyl

Question 45

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

Answer 45

they are very lipid-soluble and rapidly cross membranes

Question 46

T or F. Fentanyl is highly protein bound.

Answer 46

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

Question 47

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

Answer 47

Sufentanil

Question 48

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

Answer 48

Fentanyl

Question 49

The potency of ___ is between morphine and fentanyl.

Answer 49

Alfentanil

Question 50

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

Answer 50

Versed

Question 51

T or F. Ultiva is metabolized by pseudocholinesterases.

Answer 51

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

Question 52

Remifentanil can decrease MAC by up to __%.

Answer 52

90%

Question 53

Partial agonists bind to Mu-receptor with lower ____.

Answer 53

Efficacy

Question 54

Which opioid is associated with hyperalgesia?

Answer 54

Remifentanil

Question 55

___ + Acetaminophen = Roxicet, Percocet, or Percodan

Answer 55

Oxycodone or OxyContin

Question 56

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

Answer 56

codeine

Question 57

____ + Acetaminophen = Vicodin or Lorcet

Answer 57

Hydrocodone (Lortab)

Question 58

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

Answer 58

Acetaminophen

Question 59

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

Answer 59

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

Question 60

10mg Morphine = ____ Fentanyl

Answer 60

100mcg

Question 61

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

Answer 61

Kappa agonist (analgesia and sedation)Mu antagonist (analgesia, respiratory depression, pruritis, and constipation)

Question 62

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

Answer 62

Mu agonist (analgesia, respiratory depression, pruritis, and constipation)Kappa antagonist (analgesia and sedation)

Question 63

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

Answer 63

Nalbuphine (Nubain)

Question 64

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

Answer 64

Buprenorphine (Buprenex)

Question 65

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

Answer 65

Buprenorphine (Buprenex)

Question 66

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

Answer 66

TRUE

Question 67

Suboxone = ____ + ____

Answer 67

Buprenorphine + Naloxone

Question 68

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

Answer 68

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%

Question 69

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

Answer 69

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

Question 70

___ is an opioid antagonist

Answer 70

Naloxone (Narcan)

Question 71

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

Answer 71

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

Question 72

Which opioid receptor is responsible for constipation and urinary retention?

Answer 72

Delta