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Neuro 2-Unit 3 (Final) > Wednesday, 8-24-Narcotics And Analgesics-Fitzpatrick > Flashcards

Wednesday, 8-24-Narcotics And Analgesics-Fitzpatrick Flashcards

1
Q

How does an opioid agonist affect the pain impulse pre and post synaptically?

A

When opioid agonist occupies its receptor, blunts Ca influx and blunts Glu discharge pre-synapse, and increases K efflux post-synapse

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2
Q

In terms of drugs that bind to mu opioid receptors:

___ are full agonists
___ are partial agonist/mixed
___ are antagonists

A

Fentanyl and morphine=full

Buprenorphine=partial/mixed

Naloxone and naltrexone=antagonist

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3
Q

Which full agonist is more potent: fentanyl or morphine?

A

Fentanyl –> but both are equally efficacious

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4
Q

In terms of the pain treatment ladder:

___ are used for mild pain

___ are used for moderate or persisting or uncontrolled pain

___ are used for severe or persisting or uncontrolled pain

A

NSAID and acetaminophen

Codeine, codeine-related +/- Acetaminophen, Tramadol

Morphine, fentanyl

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5
Q

What is the opioid prototype?

What is the MOA of opioids?

What is the clinical utility of opioids?

A

Morphine

Mu receptor agonists

Tissue injury=acute stimuli > or equal to nerve injury

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6
Q

What are the clinical effects of agonists acting at opioid receptors?

A
  • analgesia (supra-spinal)
  • euphoria
  • CNS and resp depression
  • drug dependence
  • miosis
  • GI, uterine motility
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7
Q

What clinical effects can a person build up tolerance for morphine?

There is no tolerance to ___ with morphine

A

Analgesia, euphoria, sedation, nausea, resp depression

Miosis and constipation

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8
Q

What are contra-indications for morphine regarding respiration?

A

Brain injury, emphysema

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9
Q

What are some clinical indications for morphine?

A

Post-operative pain –> procedures and surgery
Cancer pain –> primary and metastatic malignancy
Other pain –> sickle cell crisis, trauma, severe diarrhea, dyspnea caused by pulmonary edema from LV failure

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10
Q

Group 1 opioids are full agonists that can be given IV or PO. List the drugs:

A

Morphine
Methadone
Meperidine

Hydromorphone
Oxymorphone
Levorphanol

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11
Q

Group 2 opioids are full agonists and short acting. List the drugs:

A

Fentanyl
Sufentanil
Remifentanyl

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12
Q

Group 3 opioids are codein-related. List the drugs:

A

Hydrocodone

Oxycodone

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13
Q

Which group 1 full agonists have high (good) oral bioavailability?

A

Methadone and Leveorphanol

Oral/parenteral potency ratio

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14
Q

Describe the bioavailability of oral morphine:

A

POOR bioavailability –> 1st pass metabolism effect

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15
Q

The pharmacokinetic properties of this opioid agonist drug are useful for withdrawal/maintenance and detoxification

A

Methadone

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16
Q

Compare the half life and oral bioavailability of methadone vs morphine:

A

Methadone has higher t1/2 (27 hrs vs 2 hrs for morphine)

Methadone has better oral bioavailability (90% vs 20% for morphine)

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17
Q

Methadone can affect cardiac electrical conduction, producing __ prolongation in acute overdose or during long-term methadone tx

A

QT-interval

18
Q

This mu agonist causes mydriasis. Abuse is difficult to detect via pinpoint pupils. Accordingly, those who abuse this drug can escape detection

A

Meperidine

19
Q

__ is a toxic metabolite of meperidine which accumulates and causes seizures

A

Normeperidine

20
Q

Which of the group 2 opioid agonists has affects as a kappa, delta, and mu agonist?

A

Sufentanil

21
Q

Compare the potency of Group 2 opioid agonists vs morphine and methadone (group 1 opioid agonists)

A

100x more potent than morphine and methadone

22
Q

___ is gaining popularity for providing analgesia for childbirth if regional anesthesia is either contraindicated or not desired. It is metabolized by plasma and tissue esterases. Although it transfers across the placenta, its rapid metabolism in the fetus lowers the risk for neonatal depression. Its rapid onset of action, within 1 minute following IV injection, is another advantage

A

Remifentanil

23
Q

___ is a strong mu agonist (meperidine analog), used in anesthesia, has a rapid onset and distribution (lipophilic), short DOA (procedures), transmucosal (lollipop), and can be given via transdermal patch delivery. There is high abuse potential via heating patches

A

Fentanyl

24
Q

__ is a group 3 mu partial agonist for moderate pain and cough. It has less potential for drug dependence and respiratory depression

A

Codeine

25
Q

Compare the oral bioavailability of codeine compared to morphine:

A

Reliable oral absorption–> 50% versus 20% for morphine

26
Q

Is the anti-tussive effect for cough relief with codeine mu dependent?

A

No, it is u-independent

27
Q

This a safer antitussive agent that relieves cough independently of opioid receptor. It is not an analgesic and not addictive

A

Dextromethophan

28
Q

Formulation of hydrocodone and oxycodone with acetaminophen complicates __ management

A

Overdose

29
Q

What phase 1 enzyme is responsible for converting codeine to the active metabolite morphine?

A

CYP2D6

30
Q

These opioids have a special use for anti-diarrhea with limited abuse potential:

A

Loperamide and diphenoxylate

These interact with mu opioid receptor in the gut, have low solubility, and poor penetration of BBB

31
Q

__ is a moderate mu agonist, its active metabolite is N-desmethyl, has reliable oral absorption/bioavailability (70% vs 20% for morphine), analgesia for moderate pain, inhibits catecholamine reuptake (associated with seizures) and should be cautious with patients on tricyclic or SSRIs

A

Tramadol

32
Q

__ is a mixed kappa agonist plus mu partial agonist/ delta antagonist. Used for supra-spinal analgesia, can precipitate withdrawal (in abusers), and side effects include tachycardia, hallucinations

A

Pentazocine

33
Q

___ is a mu partial agonist plus kappa and delta antagonist used for analgesia. It can precipitate withdrawal in abusers. It is also used in office-based detox/maintenance in combo with naloxone

A

Buprenorphine

34
Q

__ is an illegal substance that penetrates the BBB rapidly –> exaggerated euphoria –> addiction liability

A

Heroin (Di-acetylmorphine)

35
Q

Maintenance with this drug in addition programs has the highest compliance (50-80%):

A

Methadone

36
Q

What are signs/symptoms of opioid analgesic overdose?

A

RR

37
Q

These mu receptor antagonists occupy, but do not activate mu receptors. They competitively inhibt (displace) heroin, morphine, fentanyl from mu receptors.

A

Naloxone (IV) and Naltrexone (PO)

38
Q

What is the antidote for opioid overdose?

A

Naloxone (IV) and Naltrexone (PO)

In emergency setting, use Naloxone since it is parenteral. Naltrexone can be given after pt is revived in the ED setting since it is PO

39
Q

This mu receptor antagonist can reverse coma and respiratory depression ~1 minute after IV bolus. It has a short DOA of about 1-2 hrs and can lead to apparent “relapse” of overdose symptoms

A

Naloxone

40
Q

This mu receptor antagonist has a long DOA (48 hrs for single dose orally) in overdose

A

Naltrexone

41
Q

What strategies might work for opioid-induced side effects such as constipation?

A

Methylnaltrexone: a quaternary derivative of naltrexone with restricted ability to cross the BBB. Functions as a peripheral acting opioid antagonist, including actions on the GI tract to inhibit opioid-induced decrease GI motility and delay in GI transit time, thereby decreasing opioid-induced constipation. Does not affect opioid analgesic effects or induce opioid withdrawal symptoms

42
Q

Describe the pre- and post-synaptic pain impulse:

A

Afferent sensory signal –> opioid receptor unoccupied and an increasing influx of Ca in the pre-synaptic nerve increases glutamate discharge from pre-synaptic –> increase in NMDA-receptor Na influx on Post-synaptic side –> pain impulse

Neuro 2-Unit 3 (Final) (15 decks)

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