EXAM #3: OPOID ANALGESICS Flashcards Preview

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Flashcards in EXAM #3: OPOID ANALGESICS Deck (41)
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1
Q

What types of disease are opioid analgesics in to delay or arrest the disease process?

A

Autoimmune disease e.g. RA

2
Q

Where do opioid analgesics exert their MOA?

A

Ascending:

1) At the damaged/inflammed peripheral nerve
2) Dorsal horn/ spinal cord
3) Thalamus

Descending pathways

3
Q

What are the effects of opoids?

A
  • Euphoria
  • Analgesia
  • Sedation
  • Anti-diarrheal
  • Cough suppression
4
Q

What is opium?

A

Exudate from poppy seeds

5
Q

What is an opiate?

A

Drug extracted from the exudate of a poppy seed

6
Q

What is an opoid?

A

Natural or synthetic drug that binds to opoid receptors w/ agonist effects

7
Q

What is a narcotic?

A

General term to categorize drugs that treat moderate to severe pain

8
Q

What are the endogenous opoids?

A

Endorphins
Enkephalins
Dynorphins

9
Q

Agonism of what subtype of opoid receptor produces the MOST analgesia?

A

Mu

Kappa and delta do produce some analgesia

10
Q

What is the difference between Mu1 and Mu2?

A
Mu1= outside the CNS 
Mu2= inside the CNS
11
Q

What is morphine metabolized to? What is unique about the metabolites?

A

Morphine undergoes glucuronidation to two products:

1) Morphine-3-glucuronide (90%)
2) Morphine-6-glucuronide (10%)

Morphine 6-glucuronide is MORE potent than morphine

12
Q

What are heroin and codeine metabolized to?

A

Morphine

13
Q

What happens upon Mu opoid receptor activation to produce analgesia?

A
  • Mu opoid receptors are GPRCs coupled to Gi subunits
  • Decreased adenylyl cyclase
  • Decreased cAMP

–>Less intracellular Ca++ and increased K+ opening i.e. INHIBITION or neurotransmission

14
Q

How do opoid analgesics inhibit the ascending pain pathways?

A

1) Inhibition of afferent pain transmission
2) Blocked peripheral effects
3) Blocked dorsal horn of the spinal cord

15
Q

How do opioid analgesics affect the descending pain pathways?

A

Block inhibitory GABAergic interneurons

This leads to ENHANCED INHIBITION of nociceptive processing*

16
Q

What is unique about the analgeisa produced by opioid analgesics?

A

Reduce BOTH the sensory and affective components of pain

17
Q

What is an important adverse effect of opoid analgesics?

A

Respiratory depression

18
Q

What should you keep in mind about opoid analgesics and head trauma?

A

1) Respiratory depression leads to increased Co2 tension
2) Increased Co2= reflexive cerebral vasodilation

This can be dangerous with head trauma

19
Q

What is the effect of opioids on histamine?

A

Opioids can induce histamine release leading to urticaria

20
Q

List the theraputic indications for opioids.

A

1) Analgesia
2) Anesthetic
3) Anti-tussive
4) Anti-diarrheal
5) Acute pulmonary edema

21
Q

What class of drugs are contraindicated with opioids?

A

MAOIs

22
Q

What specific opioid should be avoided if a patient is taking a MAOI?

A

Meperidine

23
Q

What is the adverse reaction that happens with co-administration of Meperidine and MAOIs?

A

Hyperpyrexia

24
Q

What is the prototype strong opioid agonist used for severe pain?

A

Morphine

25
Q

What is the prototype moderate agonist used for moderate pain?

A

Codeine

26
Q

What is the prototype opioid antagnoist?

A

Naloxone

27
Q

What receptors do strong opioid agonists interact with?

A

Mu

28
Q

What is the only opioid agonist used as an anti-tussive agent?

A

Codeine

29
Q

What drug is related to the opioids that is used as an OTC anti-tussive?

A

Dextromethorphan

30
Q

What is loperamide?

A

Antidiarrheal

31
Q

What is the MOA of Tramadol?

A

Mu agonist PLUS:

- 5-HT/NE uptake inhibitors

32
Q

How does the potency of Hydromorphone compare to morphine?

A

7-10x more potent (Dilaudid)

33
Q

What is the only opioid that is available in a transdermal preparation?

A

Fentanyl

34
Q

Why is Codeine used as an anti-tussive when all the other opioids have anti-tussive properties too?

A

1) Less euphoria= less abuse
2) Rarely produces dependence

Note that it can still produce significant sedation*

35
Q

How long does it take for Naloxone to take effect?

A

30 seconds

36
Q

What is the clinical use for Naltrexone?

A

Maintenance drug for addicts in treatment programs

37
Q

List the strong opioid agonists.

A
Morphine 
Hydromorphone
Oxymorphone 
Methadone 
Fentanyl 
Sufentanil 
Meperidine 
Heroin
38
Q

List the moderate opioid agonists.

A

Codeine
Hydrocodone
Oxycodone

39
Q

List the mixed opioid agonist-antagonists.

A

Bupreneorphine
Butorphanol
Nalbuphine
Pentazocine

40
Q

List the “other” opioid agonists.

A

Dextromethorphan
Diphenoxylate
Loperamide
Tramadol

41
Q

List the opioid antagonists.

A

Naloxone
Naltrexone
Nalmefene

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