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Neurology 2 > Narcotic Analgesics - Fitzpatrick > Flashcards

Narcotic Analgesics - Fitzpatrick Flashcards

1
Q

DOR
KOR
MOR

What are they?

A

Delta, kappa, mu opiod receptor

GPCRs

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2
Q

Opioid FULL AGONISTS used for analgesia

A

Fentanyl, Heroin, Hydromorphone, Meperidine, Methadone, Morphine, Oxycodone, Oxymorphone, Tramadol

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3
Q

Opioid (Mu) receptor ANTAGONISTS

Used for what?

A

Naloxone, Naltrexone, Methylnaltrexone

Management of opiod OD/addiction/side effects

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4
Q

Opioid (Mu) PARTIAL AGONIST

A

Buprenorphine, Codeine, Hydrocodone

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5
Q

Opioid Mixed AGONIST/ANTAGONIST

A

Buprenorphine-Naloxone

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6
Q

Poorly-absorbed opioid receptor AGONISTS

Used for what?

A

Loperamide, Diphenoxylate

Diarrhea

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7
Q

Common opioids w/ anti-tussive (cough) agents

A

Codeine, Dextromethorphan, Hydrocodone

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8
Q

Mu receptor ligands

A

Endorphins

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9
Q

Kappa receptor ligands

A

Dynorphins

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10
Q

Delta receptor ligands

A

Enkephalins, Endorphins

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11
Q

Sites of opioid action

A

Peripheral 1º afferent nociceptor
Dorsal horn Pre-synaptic CALCIUM channels
2º afferent post-synaptic POTASSIUM channels

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12
Q

5 steps of pain impulse propagation at SYNAPSE

A
  1. Afferent sensory signal (painful stimuli)
  2. Ca++ influx into pre-synaptic terminal
  3. Glutamate discharge
  4. Post-synaptic NMDA receptor activation
  5. Na+ influx-induced 2º neuron action potential
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13
Q

Binding of opioids at the 3 sites of action affect which steps of the process?

Function at post-synaptic terminal?

A

ALL STEPS

K+ efflux –> hyperpolarization (prevent action potential)

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14
Q

Are opioid agonists more for tissue injury or nerve injury?

Similarly to what drugs?

A

Tissue injury

NSAIDs, Acetaminophen

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15
Q

Opioid drugs to use for MODERATE, persisting or uncontrolled pain

A

Codeine, Codeine-related, Tramadol

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16
Q

Opioid drugs to use for SEVERE, persisting or uncontrolled pain

A

Morphine, Fentanyl, etc.

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17
Q

Morphine acts at which receptor?

A

Mu

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18
Q

Mu AGONISTS act MOSTLY where?

Thus, additional effects of morphine use? (4)

A

Brain and brainstem

SUPRA-SPINAL analgesia
Euphoria
CNS and respiratory depression
Drug-dependence

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19
Q

Which clinical effects of morphine use do NOT show tolerance (decrease in effect) over time?

A

Miosis (eyes ALWAYS pin-point)

Constipation (will continue to be constipated)

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20
Q

Which clinical effects of morphine use DO show tolerance over time?

A

Analgesia, Euphoria, Sedation, Pruritis, Nausea, Respiratory Depression

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21
Q

Common side effect of morphine use

So?

A

Constipation/Biliary pressure

Sometimes will need to choose a less-potent analgesic (like post-GI surgery) to reduce the constipation

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22
Q

Can the analgesic effect of morphine be elicited without the other effects?

A

NO

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23
Q

When you say respiratory depression, what does this mean?

A

Disruption of CO2 sensitivity

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24
Q

Contraindications to morphine use based on respiratory depression effects

A

Brain injury, emphysema

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25
Q

Clinical indications for morphine use

A

Post-op pain
Cancer pain
Other pain (sickle cell, trauma)
SEVERE DIARRHEA (w/ risk for electrolyte imbalances)

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26
Q

Mu FULL AGONISTS given parenterally or orally

A

Morphine, Methadone, Meperidine
Hydromorphone, Oxymorphone, LEvorphanol

“Three M’s go in or around the HOLe (Mouth)”

27
Q

Mu FULL AGONISTS that are short-acting

A

Fentanyl, Sufentanil, Remifentanyl

“Three Fentanyl’s die Fast”

28
Q

Mu Receptor agonists - codeine-related drugs

A

Codeine, Hydrocodone, Oxycodone

29
Q

A patient needs an oral Mu FULL AGONIST drug. What are her options?

Why?

A

Methadone, Levorphanol

Good bioavailability

30
Q

A patient needs a Mu FULL AGONIST drug, but is “NPO” in the hospital. What can be given parenterally?

A

Morphine, Hydromorphone, Oxymorphone, Meperedine

31
Q

Contrast the potencies of the 6 different Mu FULL AGONISTS

A

Morphine = Methadone
Meperedine is WEAK (6x weaker than morphine)
HOLe (all 3) are STRONG (5x stronger than morphine)

32
Q

Oral, STRONGER (lower dose) Mu full agonist

A

Levorphanol

33
Q

Oral version of morphine

A

Methadone

34
Q

Stronger parenteral morphine-like drugs

A

Hydromorphone, Oxymorphone

35
Q

WEAKER (higher dose) version of morphine

A

Meperidine

36
Q

Why is morphine poor when taken orally?

What does this?

A

First-pass effect

CYP3A4 in the liver

37
Q

Why can people react differently to morphine?

A

Different ACTIVE metabolites, some of which are even MORE active than morphine (hydromorphone)

38
Q

Inactive metabolite of morphine

Via what?

A

Normorphine

CYP3A4

39
Q

Why might methadone be chosen over morphine?

A

Much longer 1/2 life = only give ONCE per day

40
Q

Other clinical uses of methadone?

Why?

A

Withdrawal/detoxification, maintenance

Stays in body longer, allows for slow decrease rather than constantly falling towards zero after morphine dose

41
Q

A patient is on long-term methadone treatment for detoxification from heroin. What is a potential side effect developed over time?

Why?

A

Long QT syndrome (on EKG)

Acts directly on inward rectifying K+ (IRK) channels, thus could cause delayed ability of heart cells to re-polarize

42
Q

A patient is as a common opiate narcotic abuser with a recent history of seizures. He admits to using it at work and has never been caught.

What is he using?
Why has he never been caught?
Why is he having seizures?

A

Meperidine

Only opiate to cause pupillary DILATION (can’t detect using the standard pin-point pupil test)

Normeperidine = TOXIC METABOLITE that accumulates and causes SEIZURES

43
Q

A patient is having a bad opioid withdrawal episode and needs an IMMEDIATE IV drug dose to calm the symptoms before he can be slowly withdrawn from the drugs.

What are your best options?
Why?

A

Fentanyl, Sufentanil, Remifentanyl

Act VERY FAST, then have SHORT DURATION
- Good for stabilizing the patient

44
Q

COMPARE and CONTRAST the 3 short-acting IV Mu receptor agonists

A

ALL 3 = Short duration (

45
Q

A pregnant woman needs immediate analgesia during childbirth, but she cannot have typical regional anesthesia. What are her options?
Which is the best option?
- Why?

A

Fentanyl, Sufentanil, Remifentanil

Remifentanil (VERY rapid onset, metabolized by plasma/tissue esterases - so baby does not need hepatic enzymes to break it down)

46
Q

A patient needs an immediate analgesic for whatever reason. However, the pain needs to be kept off for a while after the near-immediate effect. What is a good combo to give?

A

Fentanyl + Morphine

47
Q

Benefit of a transdermal skin patch for Fentanyl delivery

A

Slows onset, prolongs delivery

48
Q

Danger of Fentanyl skin patches

A

Can be heated –> ABUSE POTENTIAL

49
Q

Benefits to Codeine use for pain relief (3)

A
  1. Partial Mu Agonist, so less abuse or resp. depression
  2. Better oral bioavailability than morphine (50% > 20%)
  3. Anti-tussive (cough) effect
50
Q

A patient has a bad acute cough and needs a medication. However, they have a history of drug abuse. What is the best medication?

Why?

A

Dextromethorphan

NOT analgesic (opioid-receptor independent), so not addictive

51
Q

You suspect an opioid overdose, specfically of the codeine group (codeine, hydrocodone, oxycodone). What must be taken into consideration when treating the OD?

A

Some forms of codeine-type drugs come along with ACETAMINOPHEN, so must be careful of drug-drug interactions

52
Q

Contrast the 3 codeine-related drugs

A

Codeine - Partial Mu agonist, less potent, better orally
Hydrocodone - Partial agonist, more potent than codeine
Oxycodone - FULL agonist, more potent than codeine

53
Q

Why is it bad to give codeine to an opioid addict?

A

Metabolized to MORPHINE via CYP2D6, as well as to other active metabolites

54
Q

A patient is trying to take codeine for a cough, but the effects wear off much quicker than they should. Additionally, she constantly feels “high” shortly after taking it. However, her friend also takes it, but does not seem to feel these narcotic effects at all.

Why?

A

Patient = ULTRAFAST metabolizer –> morphine
- Extra CYP2D6 allele(s)

Friend = SLOW metabolizer (gene deletion for CYP2D6)

55
Q

A patient needs an analgesic for a post-op period. However, they have a history of drug abuse. What are the best options?

Why?

A

Hydromorphone, Oxymorphone, Fentanyl

Have NO active or toxic metabolites

56
Q

A patient is a chronic heroin abuser. Why is the drug so potent?

Why do the effects of heroin last so long?

A

2 ACETYL groups on morphine –> rapidly penetrates BBB to cause EXAGGERATED euphoria

Metabolized into morphine

57
Q

A patient has chronic bad diarrhea. The normal autonomic drugs do not seem to work. You think of opioid options.

What are your best options?
Why are these good for the gut?
Why are they OTC?

A

Loperamide, Diphenoxylate

Interact w/ Mu receptors in the gut

Poor solubility in blood, poor penetration of BBB
- Limited risk of abuse, dependence, or toxicity

58
Q

What is Tramadol?
What is it like?
What is unique about it?

Cautions? (2)

A

Moderate/Partial Mu agonist (like codeine)
Good oral availability (like codeine)
Active metabolite (like codeine)
INHIBITS CATECHOLAMINE RE-UPTAKE

  1. Careful when using w/ patients on anti-depression meds
  2. Metabolite build-up –> SEIZURES
59
Q

Buprenorphine action

Used for what?

A

Mu PARTIAL agonist + Kappa/Delta ANTAGONIST

OUTPATIENT withdrawal maintenance in abusers

60
Q

Death by morphine (Mu agonist) overdose?

A

Respiratory depression

61
Q

3 cardinal signs of opioid use/overdose

A
  1. Slow respiratory rate (
62
Q

2 Mu receptor ANTAGONISTS

Function?
- Used when?

Contrast them

A

Naloxone, Naltrexone

Competitive antagonists of Mu receptor
- ANTIDOTE FOR OPIOID OVERDOSE

Naloxone = IV, use FIRST (immediate effect)
Naltrexone = oral, use AFTER NALOXONE (48 hr duration)
63
Q

Why do opioid agonists cause nausea and vomiting?

A

Increased GI smooth muscle tone, but INHIBITED coordination of peristalsis

64
Q

A patient is taking morphine for post-op analgesia (pain relief), but is having severe trouble with constipation. The patient wants to continue with the analgesia, but not the constipation. What is a good cure?

A

Methylnaltrexone

Quaternary (charged), so cannot cross BBB. Acts as PERIPHERAL opioid antagonist, so does NOT affect the analgesic (CNS) effects of morphine.

Neurology 2 (22 decks)

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